1: Hamada M, Iikubo K, Ishikawa Y, Ikeda A, Umezawa K, Nishiyama S. Biological activities of alpha-mangostin derivatives against acidic sphingomyelinase.Bioorg Med Chem Lett. 2003 Oct 6;13(19):3151-3.
PMID: 12951083 [PubMed - in process]Biological activities of alpha-mangostin derivatives against acidic sphingomyelinase.
Hamada M, Iikubo K, Ishikawa Y, Ikeda A, Umezawa K, Nishiyama S.
Department of Chemistry, Faculty of Science and Technology, Keio University,
Hiyoshi 3-14-1, Kohoku-ku, Yokohama 223-8522, Japan.
Deprenyl and benzofenone-type congeners of alpha-mangostin 1 have been synthesized to understand their role for the inhibitory activity against sphingomyelinase(SMase). While removal of the prenyl group of the right side (11 and 12) caused loss of the selectivity between ASMase (acidic sphingomyelinase) and NSMase (neutral sphingomyelinase), the prenyl group of the left side appeared to increase the inhibitory activities (16 and 17).
PMID: 12951083 [PubMed - in process]
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2: Matsumoto K, Akao Y, Kobayashi E, Ohguchi K, Ito T, Tanaka T, Iinuma M, Nozawa Y.
Induction of apoptosis by xanthones from mangosteen in human leukemia cell lines.
j Nat Prod. 2003 Aug;66(8):1124-7.
PMID: 12932141 [PubMed - in process]
Induction of apoptosis by xanthones from mangosteen in human leukemia cell lines.
Matsumoto K, Akao Y, Kobayashi E, Ohguchi K, Ito T, Tanaka T, Iinuma M, Nozawa Y.
Gifu International Institute of Biotechnology, 1-1 Naka-Fudogaoka, Kakamigahara,
Gifu 504-0838, Japan.
We examined the effects of six xanthones from the pericarps of mangosteen, Garcinia mangostana, on the cell growth inhibition of human leukemia cell line HL60.All xanthones displayed growth inhibitory effects. Among them, alpha-mangostin showed complete inhibition at 10 microM through the induction of apoptosis.
PMID: 12932141 [PubMed - in process]
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3: Nakatani K, Nakahata N, Arakawa T,
Yasuda H, Ohizumi Y.
Inhibition of cyclooxygenase and prostaglandin E2 synthesis by gamma-mangostin,a xanthone derivative in mangosteen, in C6 rat glioma cells.
Biochem Pharmacol. 2002 Jan 1;63(1):73-9.
PMID: 11754876 [PubMed - indexed for MEDLINE]
Inhibition of cyclooxygenase and prostaglandin E2 synthesis by gamma-mangostin, a xanthone derivative in mangosteen, in C6 rat glioma cells.
Nakatani K, Nakahata N, Arakawa T, Yasuda H, Ohizumi Y.
Department of Pharmaceutical Molecular Biology, Graduate School of Pharmaceutical Sciences, Tohoku University, Aoba, Aramaki, Aoba-ku, 980-8578, Sendai, Japan.
The fruit hull of mangosteen, Garcinia mangostana L., has been used for many years as a medicine for treatment of skin infection, wounds, and diarrhea in Southeast Asia. In the present study, we examined the effect of gamma-mangostin, a tetraoxygenated diprenylated xanthone contained in mangosteen, on arachidonic acid (AA) cascade in C6 rat glioma cells. gamma-Mangostin had a potent inhibitory activity of prostaglandin E2 ( PGE2) release induced by A23187, a Ca2+ ionophore. The inhibition was concentration-dependent, with the IC50 value of about 5 microM. gamma-Mangostin had no inhibitory effect on A23187-induced phosphorylation of p42/p44 extracellular signal regulated kinase/mitogen-activated protein kinase or on the liberation of [14C]-AA from the cells labeled with [14C]-AA. However, gamma-mangostin concentration-dependently inhibited the conversion of AA to PGE2 in microsomal preparations, showing its possible inhibition of cyclooxygenase (COX). In enzyme assay in vitro, gamma-mangostin inhibited the activities of both constitutive COX (COX-1) and inducible COX (COX-2) in a concentration-dependent manner, with the IC50 values of about 0.8 and 2 microM, respectively. Lineweaver-Burk plot analysis indicated that gamma-mangostin competitively inhibited the activities of both COX-1 and -2. This study is a first demonstration that gamma-mangostin, a xanthone derivative, directly inhibits COX activity.
PMID: 11754876 [PubMed - indexed for MEDLINE]
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4: Mahabusarakam W, Proudfoot J, Taylor W,
Croft K.
Inhibition of lipoprotein oxidation by prenylated xanthones derived from mangostin. Free Radic Res. 2000 Nov;33(5):643-59.
PMID: 11200095 [PubMed - indexed for MEDLINE]
Inhibition of lipoprotein oxidation by prenylated xanthones derived from mangostin.
Mahabusarakam W, Proudfoot J, Taylor W,
Croft K.
Chemistry Department, Prince of Songkla University, Hat Yai, Thailand.
Oxidative damage is thought to play a critical role in cardiovascular and other chronic diseases. This has led to considerable interest in the antioxidant activity of dietary compounds. Flavonoids have received the most attention and much is known about the structural requirements for antioxidant activity. However, little is known about the antioxidant activity of other plant derived phenolic compounds such as the xanthones. We have previously shown that the prenylated xanthone, mangostin, can inhibit the oxidation of low density lipoprotein. In order to examine the effects of structure modification on antioxidant activity of this class of compound we have prepared a number of derivatives of mangostin and tested antioxidant activity in an isolated LDL and plasma assay. The results of this study show that structural modification of mangostin can have a profound effect on antioxidant activity. Derivatisation of the C-3 and C-6 hydroxyl groups with either methyl, acetate, propane diol or nitrile substantially reduces antioxidant activity. In contrast, derivatisation of C-3 and C-6 with aminoethyl derivatives enhanced antioxidant activity, which may be related to changes in solubility. Cyclisation of the prenyl chains had little influence on antioxidant activity.
PMID: 11200095 [PubMed - indexed for MEDLINE]
5: Okudaira C, Ikeda Y, Kondo S, Furuya S, Hirabayashi Y, Koyano T, Saito Y, Umezawa K.Inhibition of acidic sphingomyelinase by xanthone compounds isolated from Garcinia speciosa.
J Enzyme Inhib. 2000;15(2):129-38.
PMID: 10938539 [PubMed - indexed for MEDLINE]Inhibition of acidic sphingomyelinase by xanthone compounds isolated from Garcinia speciosa.
Okudaira C, Ikeda Y, Kondo S, Furuya S, Hirabayashi Y, Koyano T, Saito Y, Umezawa K.
Department of Applied Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama 223-0061, Japan.
Sphingomyelinase is considered to be involved in the regulation of apoptosis (cell death) and cell growth. In the course of our screening for acidic sphingomyelinase inhibitors we isolated three xanthone compounds, alpha-mangostin, cowanin, and cowanol, from the bark of Garcinia speciosa. These compounds competitively inhibited bovine brain-derived acidic sphingomyelinase with IC(50) values of 14.1, 19.2, and 10.9 microM, respectively and inhibited the acidic sphingomyelinase more effectively than the neutral sphingomyelinase of bovine brain. alpha-Mangostin inhibited the acidic sphingomyelinase in the most selective manner. alpha-Mangostin was chemically modified and its structure-activity relationships are discussed.
PMID: 10938539 [PubMed - indexed for MEDLINE]
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6: Lu ZX, Hasmeda M, Mahabusarakam W, Ternai B, Ternai PC, Polya GM.
Inhibition of eukaryote protein kinases and of a cyclic nucleotide-binding phosphatase by prenylated xanthones.
Chem Biol Interact. 1998 Jul 3;114(1-2):121-40.
PMID: 9744560 [PubMed - indexed for MEDLINE]
Inhibition of eukaryote protein kinases and of a cyclic nucleotide-binding phosphatase by prenylated xanthones.
Lu ZX, Hasmeda M, Mahabusarakam W, Ternai B, Ternai PC, Polya GM.
School of Biochemistry, La Trobe University, Bundoora, Victoria, Australia.
A series of prenylated xanthones are variously potent inhibitors of the catalytic subunit (cAK) of rat liver cyclic AMP-dependent protein kinase (PKA), rat brain Ca2+ and phospholipid-dependent protein kinase C (PKC), chicken gizzard myosin light chain kinase (MLCK), wheat embryo Ca2+-dependent protein kinase (CDPK) and potato tuber cyclic nucleotide-binding phosphatase (Pase). The prenylated xanthones examined are mostly derivatives of alpha-mangostin in which the 3-hydroxyl and 6-hydroxyl are variously substituted with groups R or R’, respectively, or derivatives of 3-isomangostin (mangostanol) in which the 9-hydroxyl is substituted with groups R’ or the prenyl side chain is modified. The most potent inhibitors of cAK have non-protonatable and relatively small R’ and R groups. Conversely, the most potent inhibitors of PKC and MLCK have bulkier and basic R’ groups. Some prenylated xanthones are also potent inhibitors of CDPK. PKC and cAK are competitively inhibited by particular prenylated xanthones whereas the compounds that are the most potent inhibitors of MLCK and CDPK are non-competitive inhibitors. Prenylated xanthones having relatively small and non-protonatable R’ and R groups inhibit a high-affinity cyclic nucleotide binding Pase in a non-competitive fashion.
(Protein kinases make up a veritable treasure trove of targets for a variety of indications, including diabetes, inflammatory disorders, and especially cancer.)
PMID: 9744560 [PubMed - indexed for MEDLINE]
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7: Hopert AC, Beyer A, Frank K, Strunck E, Wunsche W, Vollmer G.
Characterization of estrogenicity of phytoestrogens in an endometrial-derived experimental model.
Environ Health Perspect. 1998 Sep;106(9):581-6.
PMID: 9721258 [PubMed - indexed for MEDLINE]
Characterization of estrogenicity of phytoestrogens in an endometrial-derived experimental model.
Hopert AC, Beyer A, Frank K, Strunck E, Wunsche W, Vollmer G.
Institut fur Molekulare Medizin, Medizinische Universitat zu Lubeck, Lubeck, Germany.
Severe developmental and reproductive disorders in wild animals have been linked to high exposure to persistent environmental chemicals with hormonal activity. These adverse effects of environmental estrogens have raised considerable concern and have received increasing attention. Although numerous chemicals with the capacity to interfere with the estrogen receptor (ER) have been identified, information on their molecular mechanism of action and their relative potency is rather limited. For the endometrium, the lack of information is due to the lack of a suitable experimental model. We investigated the functions of phytoestrogens in an endometrial-derived model, RUCA-I rat endometrial adenocarcinoma cells. The cells were cultured on a reconstituted basement membrane to preserve their functional differentiation and estrogen responsiveness. We assessed the relative binding affinity to the estrogen receptor of the selected phytoestrogens coumestrol, genistein, daidzein, and the putative phytoestrogen mangostin compared to estradiol by a competitive Scatchard analysis. The following affinity ranking was measured: 17beta-estradiol >>> coumestrol > genistein > daidzein >>> mangostin. In addition, we investigated the capacity of these compounds to promote the increased production of complement C3, a well-known estradiol-regulated protein of the rat endometrium. All substances tested increased the production of complement C3, although different concentrations were necessary to achieve equivalent levels of induction compared to estradiol. Mechanistically we were able to demonstrate that the increase of complement C3 production was mediated by primarily increasing its steady-state mRNA level. These findings indicate that RUCA-I cells represent a sensitive model system to elucidate relative potencies and functions of environmental estrogens in an endometrium-derived model.
PMID: 9721258 [PubMed - indexed for MEDLINE]
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8: Chairungsrilerd N, Furukawa K, Tadano T,
Kisara K, Ohizumi Y.
Effect of gamma-mangostin through the inhibition of 5-hydroxy-tryptamine2A receptors in 5-fluoro-alpha-methyltryptamine-induced head-twitch responses
of mice.
Br J Pharmacol. 1998 Mar;123(5):855-62.
PMID: 9535013 [PubMed - indexed for MEDLINE]
Effect of gamma-mangostin through the inhibition of 5-hydroxy-tryptamine2A receptors in 5-fluoro-alpha-methyltryptamine-induced head-twitch responses of mice.
Chairungsrilerd N, Furukawa K, Tadano T,
Kisara K, Ohizumi Y.
Department of Molecular Biology, Faculty of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.
1. Intracerebronventricular (i.c.v.) injection of gamma-mangostin (10-40 nmol/mouse), a major compound of the fruit hull of Garcinia mangostana Lin., like ketanserin (10, 20 nmol/mouse, i.c.v.) inhibited 5-fluoro-alpha-methyltryptamine (5-FMT) (45 mg kg(-1), i.p.)-induced head-twitch response in mice in the presence or absence of citalopram (a 5-hydroxytryptamine (5-HT)-uptake inhibitor). 2. Neither the 5-FMT- nor the 8-hydroxy-2-(di-n-propylamino)tetralin 5-HT1A-agonist)-induced 5-HT syndrome (head weaving and hindlimb abduction) was affected by gamma-mangostin or ketanserin. 3. The locomotor activity stimulated by 5-FMT through the activation of alpha1-adrenoceptors did not alter in the presence of gamma-mangostin. 4. 5-HT-induced inositol phosphates accumulation in mouse brain slices was abolished by ketanserin. Gamma-mangostin caused a concentration-dependent inhibition of the inositol phosphates accumulation. 5. Gamma-mangostin caused a concentration-dependent inhibition of the binding of [3H]-spiperone, a specific 5-HT2A receptor antagonist, to mouse brain membranes. 6. Kinetic analysis of the [3H]-spiperone binding revealed that gamma-mangostin increased the Kd value without affecting the Bmax value, indicating the mode of the competitive nature of the inhibition by gamma-mangostin. 7. These results suggest that gamma-mangostin inhibits 5-FMT-induced head-twitch response in mice by blocking 5-HT2A receptors not by blocking the release of 5-HT from the central neurone.Gamma-mangostin is a promising 5-HT2A receptor antagonist in the central nervous system.
PMID: 9535013 [PubMed - indexed for MEDLINE]
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9: Vlietinck AJ, De Bruyne T, Apers S, Pieters LA.
Plant-derived leading compounds for chemotherapy of human immunodeficiency virus (HIV) infection.
Planta Med. 1998 Mar;64(2):97-109. Review.
PMID: 9525100 [PubMed - indexed for MEDLINE]
Plant-derived leading compounds for chemotherapy of human immunodeficiency virus (HIV) infection.
Vlietinck AJ, De Bruyne T, Apers S, Pieters LA.
Department of Pharmaceutical Sciences, University of Antwerp (UA), Belgium.
Many compounds of plant origin have been identified that inhibit different stages in the replication cycle of human immunodeficiency virus (HIV): 1) virus adsorption: chromone alkaloids (schumannificine), isoquinoline alkaloids (michellamines), sulphated polysaccharides and polyphenolics, flavonoids, coumarins (glycocoumarin, licopyranocoumarin) phenolics (caffeic acid derivatives, galloyl acid derivatives, catechinic acid derivatives), tannins and triterpenes (glycyrrhizin and analogues, soyasaponin and analogues); 2) virus-cell fusion: lectins (mannose- and N-acetylglucosamine-specific) and triterpenes (betulinic acid and analogues); 3) reverse transcription; alkaloids (benzophenanthridines, protoberberines, isoquinolines, quinolines), coumarins (calanolides and analogues), flavonoids, phloroglucinols, lactones (protolichesterinic acid), tannins, iridoids (fulvoplumierin) and triterpenes; 4) integration: coumarins (3-substituted-4-hydroxycoumarins), depsidones, O-caffeoyl derivatives, lignans (arctigenin and analogues) and phenolics (curcumin); 5) translation: single chain ribosome inactivating proteins (SCRIP’s); 6) proteolytic cleavage (protease inhibition): saponins (ursolic and maslinic acids), xanthones (mangostin and analogues) and coumarins; 7) glycosylation: alkaloids including indolizidines (castanospermine and analogues), piperidines (1-deoxynojirimicin and analogues) and pyrrolizidines (australine and analogues); 8) assembly/release: naphthodianthrones (hypericin and pseudohypericin), photosensitisers (terthiophenes and furoisocoumarins) and phospholipids. The target of action of several anti-HIV substances including alkaloids (O-demethyl-buchenavianine, papaverine), polysaccharides (acemannan), lignans (intheriotherins, schisantherin), phenolics (gossypol, lignins, catechol dimers such as peltatols, naphthoquinones such as conocurvone) and saponins (celasdin B, Gleditsia and Gymnocladus saponins), has not been elucidated or does not fit in the proposed scheme. Only a very few of these plant-derived anti-HIV products have been used in a limited number of patients suffering from AIDS viz. glycyrrhizin, papaverine, trichosanthin, castanospermine, N-butyl-1-deoxynojirimicin and acemannan.
Publication Types:
· Review
· Review, Academic
PMID: 9525100 [PubMed - indexed for MEDLINE]
10: Furukawa K, Chairungsrilerd N, Ohta T, Nozoe S, Ohizumi Y.
[Novel types of receptor antagonists from the medicinal plant Garcinia mangostana]
Nippon Yakurigaku Zasshi. 1997 Oct;110 Suppl 1:153P-158P. Japanese.
PMID: 9503424 [PubMed - indexed for MEDLINE]
[Novel types of receptor antagonists from the medicinal plant Garcinia mangostana]
[Article in Japanese]
Furukawa K, Chairungsrilerd N, Ohta T, Nozoe S, Ohizumi Y.
Department of Pharmaceutical Molecular Biology, Faculty of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.
A crude methanolic extract of the fruit hull of Garcinia mangostana L. inhibited the contraction of the isolated rabbit aorta induced by histamine and serotonin. The extract has been fractionated by silica gel chromatography, monitoring the pharmacological activity to give active compounds. On the basis of physicochemical data, the active substances were identified as alpha-mangostin and gamma-mangostin. To define the pharmacological properties of alpha-mangostin, the effect of alpha-mangostin on both histamine H1 and H2 receptors were examined by monitoring the mechanical responses of smooth muscles and measuring the radioligand binding to cultured vascular smooth muscle cells. The results suggest thatalpha-mangostin acts as a selective and competitive histamine H1 receptor antagonist. The pharmacological actions of gamma-mangostin on 5-HT receptors were also investigated by using contractile response of vascular smooth muscle, platelet aggregation and radioligand binding studies. The results provide the evidence that gamma-mangostin is a selective and competitive 5-HT2A receptor antagonist. It is of great interest that the structures of alpha-mangostin and gamma-mangostin free from nitrogen atom are not resemble to the common structures of histamine and serotonin receptor antagonists. alpha-Mangostin and gamma-mangostin may become novel types of lead compounds for histamine and serotonin receptor antagonists.
PMID: 9503424 [PubMed - indexed for MEDLINE]
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11: Likhitwitayawuid K, Phadungcharoen T,
Krungkrai J.
Antimalarial xanthones from Garcinia cowa.
Planta Med. 1998 Feb;64(1):70-2.
PMID: 9491769 [PubMed - indexed for MEDLINE]
Antimalarial xanthones from Garcinia cowa.
Likhitwitayawuid K, Phadungcharoen T,
Krungkrai J.
Five xanthones from the bark of Garcinia cowa, namely 7-O-methylgarcinone E (1), cowanin (2), cowanol (3), cowaxanthone (4), and beta-mangostin (5), were found to possess in vitro antimalarial activity against Plasmodium falciparum with IC50 values ranging from 1.50 to 3.00 micrograms/ml. Complete 1H- and 13C-NMR assignments of these compounds are also reported.
Publication Types:
· Letter
PMID: 9491769 [PubMed - indexed for MEDLINE]
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12: Chairungsrilerd N, Furukawa KI, Ohta T, Nozoe S, Ohizumi Y.
Gamma-mangostin, a novel type of 5-hydroxytryptamine 2A receptor antagonist.
Naunyn Schmiedebergs Arch Pharmacol. 1998 Jan;357(1):25-31.
PMID: 9459569 [PubMed - indexed for MEDLINE]
Gamma-mangostin, a novel type of 5-hydroxytryptamine 2A receptorantagonist.
Chairungsrilerd N, Furukawa KI, Ohta T, Nozoe S, Ohizumi Y.
Department of Pharmaceutical Molecular Biology, Faculty of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.
Gamma-mangostin, purified from the fruit hull of the medicinal plant Garcinia mangostana caused a parallel rightwards shift of the concentration/response curve for the contraction elicited by 5-hydroxytryptamine (5-HT) in the rabbit aorta (pA2 = 8.2) without affecting the contractile responses to KCl, phenylephrine (alpha1) or histamine (H1). The perfusion pressure response of rat coronary artery to 5-HT (5-HT2A) was reduced concentration dependently by gamma-mangostin (IC50 = 0.32 microM). 5-HT amplified, ADP-induced aggregation of rabbit platelets (5-HT2A) was inhibited by gamma-mangostin (IC50 = 0.29 microM), whereas that induced by thrombin was not affected, nor did gamma-mangostin affect 5-HT-induced contraction of the guinea-pig ileum (5-HT3)in the presence of 5-HT1, 5-HT2 and 5-HT4 receptor antagonists. Furthermore, 5-HT-induced contraction of the rat fundus (5-HT2B) and 5-HT-induced relaxation of the rabbit aorta in the presence of ketanserin (5-HT1) and carbachol-induced contraction of the guinea-pig ileum (muscarinic M3) were not affected by gamma-mangostin (5 microM). Gamma-mangostin inhibited [3H]spiperone binding to cultured rat aortic myocytes (IC50 = 3.5 nM). The Kd for [3H]spiperone binding was increased by gamma-mangostin (3 nM) from 11.7 to 27.4 nM without affecting Bmax.These results suggest that gamma-mangostin is a novel competitive antagonist, free from a nitrogen atom, for the 5-HT2A receptors in vascular smooth muscles and platelets.
PMID: 9459569 [PubMed - indexed for MEDLINE]
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13: Gopalakrishnan G, Banumathi B, Suresh G.
Evaluation of the antifungal activity of natural xanthones from Garcinia mangostana and their synthetic derivatives.
J Nat Prod. 1997 May;60(5):519-24.
PMID: 9213587 [PubMed - indexed for MEDLINE]
Evaluation of the antifungal activity of natural xanthones from Garcinia mangostana and their synthetic derivatives.
Gopalakrishnan G, Banumathi B, Suresh G.
Centre for Agrochemical Research, SPIC Science Foundations, Madras, India.
The antifungal activity of several xanthones isolated from the fruit hulls of Garcinia mangostana and some derivatives of mangostin against three phytopathogenic fungi, Fusarium oxysporum vasinfectum, Alternaria tenuis, and Dreschlera oryzae, has been evaluated. The natural xanthones showed good inhibitory activity against the three fungi. Substitution in the A and C rings has been shown to modify the bioactivities of the compounds.
PMID: 9213587 [PubMed - indexed for MEDLINE]
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14: Chairungsrilerd N, Furukawa K, Ohta T, Nozoe S, Ohizumi Y.
Pharmacological properties of alpha-mangostin, a novel histamine H1 receptor antagonist.
Eur J Pharmacol. 1996 Oct 31;314(3):351-6.
PMID: 8957258 [PubMed - indexed for MEDLINE]
Pharmacological properties of alpha-mangostin, a novel histamine H1 receptor antagonist.
Chairungsrilerd N, Furukawa K, Ohta T, Nozoe S, Ohizumi Y.
Department of Pharmaceutical Molecular Biology, Faculty of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.
In the isolated rabbit thoracic aorta and guinea-pig trachea, alpha-mangostin inhibited histamine-induced contractions in a concentration-dependent manner in the presence or absence of cimetidine, a histamine H2 receptor antagonist. But KCl-, phenylephrine- or carbachol-induced contractions were not affected by alpha-mangostin. The concentration-contractile response curve for histamine was shifted to the right in a parallel manner by alpha-mangostin. In the presence of chlorpheniramine, a histamine H1 receptor antagonist, alpha-mangostin did not affect the relaxation of the rabbit aorta induced by histamine. In the guinea-pig trachea, alpha-mangostin had no effect on the relaxation induced by dimaprit, a histamine H2 receptor agonist. alpha-Mangostin caused a concentration-dependent inhibition of the binding of [3H]mepyramine, a specific histamine H1 receptor antagonist to rat aortic smooth muscle cells. Kinetic analysis of [3H]mepyramine binding indicated the competitive inhibition by alpha-mangostin. These results suggest that alpha-mangostin is a novel competitive histamine H1 receptor antagonist in smooth muscle cells.
PMID: 8957258 [PubMed - indexed for MEDLINE]
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15: Chairungsrilerd N, Furukawa K, Ohta T, Nozoe S, Ohizumi Y.
Histaminergic and serotonergic receptor blocking substances from the medicinal plant Garcinia mangostana.
Planta Med. 1996 Oct;62(5):471-2.
PMID: 8923814 [PubMed - indexed for MEDLINE]
Histaminergic and serotonergic receptor blocking substances from the medicinal plant Garcinia mangostana.
Chairungsrilerd N, Furukawa K, Ohta T, Nozoe S, Ohizumi Y.
A crude methanolic extract of the fruit hull of Mangosteen, Garcinia mangostana L. inhibited the contractions of isolated thoracic rabbit aorta induced by histamine and serotonin. The extract of the fruit hull has been fractionated by silica gel chromatography, monitoring the pharmacological activity to give alpha- and gamma-mangostin. On the basis of pharmacological data, it is suggested that alpha-mangostin and gamma-mangostin are a histaminergic and a serotonergic receptor blocking agent, respectively.
Publication Types:
· Letter
PMID: 8923814 [PubMed - indexed for MEDLINE]
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16: Iinuma M, Tosa H, Tanaka T, Asai F, Kobayashi Y, Shimano R, Miyauchi K.
Antibacterial activity of xanthones from guttiferaeous plants against methicillin-resistant Staphylococcus aureus.
J Pharm Pharmacol. 1996 Aug;48(8):861-5.
PMID: 8887739 [PubMed - indexed for MEDLINE]
Antibacterial activity of xanthones from guttiferaeous plants against methicillin-resistant Staphylococcus aureus.
Iinuma M, Tosa H, Tanaka T, Asai F, Kobayashi Y, Shimano R, Miyauchi K.
Department of Pharmacognosy, Gifu Pharmaceutical University, Japan.
Extracts of Garcinia mangostana (Guttiferae) showing inhibitory effects against the growth of S. aureus NIHJ 209p were fractionated according to guidance obtained from bioassay and some of the components with activity against methicillin-resistant Staphylococcus aureus (MRSA) were characterized. One active isolate, alpha-mangostin, a xanthone derivative, had a minimum inhibitory concentration (MIC) of 1.57-12.5 micrograms mL-1. Other related xanthones were also examined to determine their anti-MRSA activity. Rubraxanthone, which was isolated from Garcinia dioica and has a structure similar to that of alpha-mangostin, had the highest activity against staphylococcal strains (MIC = 0.31-1.25 micrograms mL-1), an activity which was greater than that of the antibiotic vancomycin (3.13-6.25 micrograms mL-1). The inhibitory effect against strains of MRSA of two of the compounds when used in conjunction with other antibiotics was also studied. The anti-MRSA activity of alpha-mangostin was clearly increased by the presence of vancomycin; this behaviour was not observed for rubraxanthone. The strong in-vitro antibacterial activity of xanthone derivatives against both methicillin-resistant and methicillin-sensitive Staphylococcus aureus suggests the compounds might find wide pharmaceutical use.
PMID: 8887739 [PubMed - indexed for MEDLINE]
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17: Furukawa K, Shibusawa K, Chairungsrilerd N, Ohta T, Nozoe S, Ohizumi Y.
The mode of inhibitory action of alpha-mangostin, a novel inhibitor, on the sarcoplasmic reticulum Ca(2+)-pumping ATPase from rabbit skeletal muscle.
Jpn J Pharmacol. 1996 Aug;71(4):337-40.
PMID: 8886932 [PubMed - indexed for MEDLINE]
The mode of inhibitory action of alpha-mangostin, a novel inhibitor, on the sarcoplasmic reticulum Ca(2+)-pumping ATPase from rabbit skeletal muscle.
Furukawa K, Shibusawa K, Chairungsrilerd N, Ohta T, Nozoe S, Ohizumi Y.
Department of Pharmaceutical Molecular Biology, Faculty of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.
alpha-Mangostin, the principal ingredient of the fruit hull of Garcinia mangostana,caused a concentration-dependent decrease in the activities of both Ca(2+)-ATPase and Ca(2+)-transport of the sarcoplasmic reticulum from rabbit skeletal muscle with an IC50 value of 5 microM. Neither Ca2+ release nor other enzyme activities were affected by alpha-mangostin. Kinetic analysis of the inhibitory effects of alpha-mangostin on Ca(2+)-ATPase suggests that the inhibition of the ATPase is a noncompetitive-type with respect to ATP or Ca2+. alpha-Mangostin may become a useful pharmacological tool for clarifying the physiological functions of Ca(2+)-pumping ATPase and sarcoplasmic reticulum.
PMID: 8886932 [PubMed - indexed for MEDLINE]
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18: Chen SX, Wan M, Loh BN.
Active constituents against HIV-1 protease from Garcinia mangostana.
Planta Med. 1996 Aug;62(4):381-2.
PMID: 8792678 [PubMed - indexed for MEDLINE]
Active constituents against HIV-1 protease from Garcinia mangostana.
Chen SX, Wan M, Loh BN.
The ethanol extract of Garcinia mangostana L. (Guttiferae) showed potent inhibitory activity against HIV-1 protease. The activity-guided purification of the extract resulted in the isolation of two active, known compounds. The chemical structures of the isolated compounds were established by spectroscopic analyses as mangostin (IC50 = 5.12 +/- 0.41 microM) and gamma-mangostin (IC50 = 4.81 +/- 0.32 microM). The type of inhibition by both compounds is noncompetitive.
PMID: 8792678 [PubMed - indexed for MEDLINE]
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19: Williams P, Ongsakul M, Proudfoot J, Croft K, Beilin L.
Mangostin inhibits the oxidative modification of human low density lipoprotein.
Free Radic Res. 1995 Aug;23(2):175-84.
PMID: 7581813 [PubMed - indexed for MEDLINE]
Mangostin inhibits the oxidative modification of human low density lipoprotein.
Williams P, Ongsakul M, Proudfoot J, Croft K, Beilin L.
University of Western Australia, Department of Medicine, Royal Perth Hospital, Australia.
The oxidation of low density lipoprotein (LDL) may play an important role in atherosclerosis. We investigated the possible antioxidant effects of mangostin, isolated from Garcinia mangostana, on metal ion dependent (Cu2+) and independent (aqueous peroxyl radicals) oxidation of human LDL. Mangostin prolonged the lagtime to both metal ion dependent and independent oxidation of LDL in a dose dependent manner over 5 to 50 microM as monitored by the formation of conjugated dienes at 234 nm (P < p =” 0.027)” p =” 0.163).” style=”background:#FFFF66″>we conclude that mangostin is acting as a free radical scavenger to protect the LDL from oxidative damage in this in vitro system.
PMID: 7581813 [PubMed - indexed for MEDLINE]
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20: Jinsart W, Ternai B, Buddhasukh D, Polya GM.
Inhibition of wheat embryo calcium-dependent
protein kinase and other kinases by mangostin and gamma-mangostin.
Phytochemistry. 1992 Nov;31(11):3711-3.
PMID: 1368866 [PubMed - indexed for MEDLINE]
Inhibition of wheat embryo calcium-dependent protein kinase and other kinases by mangostin and gamma-mangostin.
Jinsart W, Ternai B, Buddhasukh D, Polya GM.
Department of Chemistry, La Trobe University, Bundoora, Victoria, Australia.
The hull of the fruit of the mangosteen tree (Garcinia mangostana) contains four inhibitors of plant Ca(2+)-dependent protein kinase. Two of these inhibitors have been purified and identified as the xanthones 1,3,6-trihydroxy-7-methoxy-2,8-bis(3-methyl-2-butenyl)-9H- xanthen-9-one (mangostin) and 1,3,6,7-tetrahydroxy-2,8-bis(3-methyl-2-butenyl)- 9H-xanthen-9-one (gamma-mangostin). Both xanthones also inhibit avian myosin light chain kinase and rat liver cyclic AMP-dependent protein kinase. This is the first report of inhibition of plant and animal | second messenger-regulated protein kinases by plant-derived xanthones.
PMID: 1368866 [PubMed - indexed for MEDLINE]
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21: Sundaram BM, Gopalakrishnan C, Subramanian S, Shankaranarayanan D, Kameswaran L.
Antimicrobial activities of Garcinia mangostana.
Planta Med. 1983 May;48(1):59-60. No abstract available.
PMID: 6611746 [PubMed - indexed for MEDLINE]
Antimicrobial activities of Garcinia mangostana.
Sundaram BM, Gopalakrishnan C, Subramanian S, Shankaranarayanan D, Kameswaran L.
PMID: 6611746 [PubMed - indexed for MEDLINE]
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22: Gopalakrishnan C, Shankaranarayanan D, Kameswaran L, Nazimudeen SK.
Effect of mangostin, a xanthone from Garcinia mangostana Linn. in immunopathological & inflammatory reactions.
Indian J Exp Biol. 1980 Aug;18(8):843-6. No abstract available.
PMID: 7461736 [PubMed - indexed for MEDLINE]
Effect of mangostin, a xanthone from Garcinia mangostana Linn. inimmunopathological & inflammatory reactions.
Gopalakrishnan C, Shankaranarayanan D, Kameswaran L, Nazimudeen SK.
PMID: 7461736 [PubMed - indexed for MEDLINE]
23: Shankaranarayan D, Gopalakrishnan C, Kameswaran L.
Pharmacological profile of mangostin and its derivatives.
Arch Int Pharmacodyn Ther. 1979 Jun;239(2):257-69.
PMID: 314790 [PubMed - indexed for MEDLINE]
Pharmacological profile of mangostin and its derivatives.
Shankaranarayan D, Gopalakrishnan C, Kameswaran L.
Mangostin (M), a naturally occurring xanthone in the rinds of the fruits of Garcinia mangostana Linn. (Guttiferae) and its derivatives such as 3-0-methyl mangostin (MM), 3,6-di-O-methyl mangostin (DM), 1-isomangostin (IM), mangostin triacetate (MT), mangostin 3,6-di-O-(tetra acetyl) glucoside (MTG) and mangostin-6,6-di-O-glucoside (MOG) were screened for various pharmacological effects in experimental animals… M, IM and MT produced pronounced antiinflammatory activity both by intraperitoneal and oral routes in rats as tested by carrageenininduced hind paw oedema, cotton pellet implantation and granuloma pouch techniques.Antiinflammatory activity for M, IM and MT was observed even in bilaterally adrenalectomised rats. M, IM and MT did not produce any mast cell membrane stabilising effect and the degranulation effect of polymyxin B, diazoxide and Triton X-100 on rat peritoneal mast cells in vitro was not prevented. M, IM and MT did not alter the prothrombin time of albino rats. M alone produced significant antiulcer activity in rats.
PMID: 314790 [PubMed - indexed for MEDLINE]
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*Antiproliferation, *antioxidation and induction of *apoptosis by Garcinia mangostana (mangosteen) on SKBR3 human breast cancer cell line
Primchanien Moongkarndi, , a, Nuttavut Kosema, Sineenart Kaslungkab, Omboon Luanratanac, Narongchai Pongpanc and Neelobol Neungtond
Department of Microbiology, Faculty of Pharmacy, Mahidol University, Sri Ayudthaya Road, Rajdhevee, Bangkok 10400, Thailand The Government Pharmaceutical Organization, Rama VI Road, Bangkok 10400, Thailand
Department of Pharmacognosy, Faculty of Pharmacy, Mahidol University, Sri Ayudthaya Road, Rajdhevee, Bangkok 10400, Thailand
Department of Biochemistry, Faculty of Medicine, Siriraj Hospital, Bangkok 10700, Thailand
Received 15 June 2002; revised 10 September 2003; accepted 22 September 2003. ; Available online 5 December 2003.
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Abstract
This study was designed to determine the antiproliferative, apoptotic and antioxidative properties of crude methanolic extract (CME) from the pericarp of Garcinia mangostana (family Guttiferae) using human breast cancer (SKBR3) cell line as a model system. SKBR3 cells were cultured in the presence of CME at various concentrations (0–50 g/ml) for 48 h and the percentage of cell viability was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-di phenyl tetrazolium bromide (MTT) assay. CME showed a dose-dependent inhibition of cell proliferation with ED50 of 9.25±0.64 g/ml. We found that antiproliferative effect of CME was associated with apoptosis on breast cancer cell line by determinations of morphological changes and oligonucleosomal DNA fragments. In addition, CME at various concentrations and incubation times were also found to inhibit ROS production. Theseinvestigations suggested that the methanolic extract from the pericarp of Garcinia mangostana had strong antiproliferation, potent antioxidation and induction of apoptosis.Thus, it indicates that this substance can show different activities and has potential for cancer chemoprevention which were dose dependent as well as exposure time dependent.
Antiproliferation = stops the cell from spreading
Antioxidation = stops free radical damage which can result in further mutation
Induction of apoptosis = This is a process of cell death – Apoptotic cells break into smaller pieces called apoptotic bodies that other body cells recognize and eat.
Terjemahan oleh Google
1: Hamada M, Iikubo K, Ishikawa Y, Ikeda A, Umezawa K, Nishiyama S. Aktivitas biologi dari derivatif alpha-mangostin terhadap sphingomyelinase asam.
Bioorg Med Chem Lett. 2003 Oktober 6; 13 (19) :3151-3.
PMID: 12951083 [PubMed - dalam proses]
Biologi kegiatan derivatif alpha-mangostin terhadap sphingomyelinase asam.
Hamada M, K Iikubo, Y Ishikawa, Ikeda A, Umezawa K, Nishiyama S.
Jurusan Kimia, Fakultas Sains dan Teknologi, Universitas Keio,
3-14-1 Hiyoshi, Kohoku-ku, Yokohama 223-8522, Jepang.
Deprenyl dan congener benzofenone-jenis alpha-mangostin 1 telah disintesis untuk memahami peran mereka untuk kegiatan penghambatan terhadap sphingomyelinase (SMase). Sementara penghapusan kelompok prenyl dari sisi kanan (11 dan 12) menyebabkan hilangnya selektivitas antara ASMase (sphingomyelinase asam) dan NSMase (sphingomyelinase netral), kelompok prenyl dari sisi kiri tampaknya meningkatkan aktivitas hambat (16 dan 17 ).
PMID: 12951083 [PubMed - dalam proses]
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2: Matsumoto K, Y Akao, E Kobayashi, K Ohguchi, T Ito, Tanaka T, Iinuma M, Nozawa Y.
Induksi apoptosis oleh santon dari manggis dalam baris sel leukemia manusia.
Nat j Prod. Agustus 2003; 66 (8) :1124-7.
PMID: 12932141 [PubMed - dalam proses]
Induksi apoptosis oleh santon dari manggis dalam baris sel leukemia manusia.
Matsumoto K, Y Akao, E Kobayashi, K Ohguchi, T Ito, Tanaka T, M Iinuma, Nozawa Y.
Gifu International Institute of Biotechnology, 1-1 Naka-Fudogaoka, Kakamigahara,
Gifu 504-0838, Jepang. [email protected]
Kami memeriksa efek dari enam santon dari pericarps manggis, Garcinia mangostana, pada penghambatan pertumbuhan sel sel leukemia garis santon manusia HL60.All ditampilkan pertumbuhan efek penghambatan.Di antara mereka, alpha-mangostin menunjukkan inhibisi selengkapnya di 10 microM melalui induksi apoptosis.
PMID: 12932141 [PubMed - dalam proses]
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3: Nakatani K, N Nakahata, T Arakawa,
Yasuda H Ohizumi, Y.
Penghambatan siklooksigenase dan sintesis prostaglandin E2 oleh gamma-mangostin, sebuah santon derivatif manggis, pada sel C6 tikus glioma.
Biochem Pharmacol. 2002 Januari 1, 63 (1) :73-9.
PMID: 11754876 [PubMed - diindeks untuk MEDLINE]
Penghambatan siklooksigenase dan sintesis prostaglandin E2 oleh gamma-mangostin, sebuah santon derivatif manggis, pada sel C6 tikus glioma.
Nakatani K, N Nakahata, Arakawa T, Yasuda H, Ohizumi Y.
Departemen Biologi Molekuler Farmasi, Sekolah Pascasarjana Ilmu Farmasi, Universitas Tohoku, Aoba, Aramaki, Aoba-ku,, 980-8578 Sendai, Jepang.
Lambung buah manggis, Garcinia mangostana L., telah digunakan selama bertahun-tahun sebagai obat untuk pengobatan infeksi kulit, luka, dan diare di Asia Tenggara.Dalam studi ini, kami menguji efek gamma-mangostin, sebuah santon diprenylated tetraoxygenated terkandung dalam manggis, asam arakhidonat (AA) cascade pada sel glioma tikus C6. gamma-Mangostin mempunyai aktivitas penghambatan ampuh prostaglandin E2 (PGE2) pelepasan disebabkan oleh A23187, sebuah ionofor Ca2.penghambatan itu tergantung konsentrasi, dengan nilai IC50 sekitar 5 microM. gamma-Mangostin tidak memiliki efek penghambatan terhadap A23187-fosforilasi diinduksi dari p42/p44 sinyal ekstraseluler diatur protein kinase / kinase mitogen-diaktifkan atau pada pembebasan [14C]-AA dari sel diberi label dengan [14C]-AA. Namun, gamma-mangostin konsentrasi-ketergantungan menghambat konversi AA untuk PGE2 dalam persiapan mikrosoma, yang mungkin menunjukkan penghambatan siklooksigenase (COX). Dalam assay enzim in vitro, gamma-mangostin menghambat aktivitas kedua COX konstitutif (COX-1) dan COX diinduksi (COX-2) dengan cara konsentrasi-tergantung, dengan nilai-nilai IC50 dari sekitar 0,8 dan 2 microM, masing-masing.Lineweaver-Burk plot analisis menunjukkan bahwa gamma-mangostin secara kompetitif menghambat kegiatan kedua-COX 1 dan -2. Penelitian ini merupakan demonstrasi pertama yang gamma-mangostin, derivatif santon, langsung menghambat aktivitas COX.
PMID: 11754876 [PubMed - diindeks untuk MEDLINE]
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4: Mahabusarakam W, Proudfoot J, W Taylor,
Croft K.
Penghambatan oksidasi lipoprotein oleh santon terprenilasi berasal dari mangostin.Free Radic Res.November 2000; 33 (5) :643-59.
PMID: 11200095 [PubMed - diindeks untuk MEDLINE]
Penghambatan oksidasi lipoprotein oleh santon terprenilasi berasal dari mangostin.
Mahabusarakam W, Proudfoot J, W Taylor,
Croft K.
Jurusan Kimia, Prince of Songkla University, Hat Yai, Thailand.
kerusakan oksidatif berpikir untuk memainkan peran penting dalam penyakit kronis jantung dan lainnya. Hal ini menyebabkan minat yang besar terhadap aktivitas antioksidan senyawa makanan. Flavonoid telah menerima perhatian yang besar dan banyak yang diketahui tentang persyaratan struktural untuk aktivitas antioksidan.Namun, sedikit yang diketahui tentang aktivitas antioksidan tanaman lain yang berasal senyawa fenolik seperti santon. Kami sebelumnya telah menunjukkan bahwa santon terprenilasi, mangostin, dapat menghambat oksidasi low density lipoprotein. Dalam rangka untuk mengetahui pengaruh modifikasi struktur aktivitas antioksidan senyawa kelas ini kami telah menyiapkan sejumlah turunan dari mangostin dan aktivitas antioksidan diuji dalam LDL terisolasi dan pengujian plasma. Hasil studi ini menunjukkan bahwa modifikasi struktural mangostin dapat memiliki efek yang mendalam pada aktivitas antioksidan. Derivatisation dari C-3 dan C-6 kelompok hidroksil dengan baik metil, asetat, diol propane atau nitril secara substansial mengurangi aktivitas antioksidan. Sebaliknya, derivatisation C-3 dan C-6 dengan turunan aminoethyl meningkatkan aktivitas antioksidan, yang mungkin terkait dengan perubahan kelarutan. Cyclisation rantai prenyl memiliki pengaruh yang kecil terhadap aktivitas antioksidan.
PMID: 11200095 [PubMed - diindeks untuk MEDLINE]
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5: Okudaira C, Y Ikeda, S Kondo, Furuya S, Y Hirabayashi, T Koyano, Y Saito, K. Umezawa
Penghambatan sphingomyelinase asam oleh senyawa santon diisolasi dari Garcinia speciosa.
J Inhib Enzim. 2000; 15 (2) :129-38.
PMID: 10938539 [PubMed - diindeks untuk MEDLINE]
Penghambatan sphingomyelinase asam oleh senyawa santon diisolasi dari Garcinia speciosa.
Okudaira C, Ikeda Y, S Kondo, Furuya S, Y Hirabayashi, T Koyano, Y Saito, K. Umezawa
Jurusan Kimia Terapan, Fakultas Sains dan Teknologi, Universitas Keio, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama 223-0061, Jepang.
Sphingomyelinase dianggap terlibat dalam regulasi apoptosis (kematian sel) dan pertumbuhan sel. Dalam proses skrining kami untuk inhibitor sphingomyelinase asam kita diisolasi tiga senyawa santon, alpha-mangostin, cowanin, dan cowanol, dari kulit Garcinia speciosa. Senyawa ini menghambat kompetitif sphingomyelinase asam yang diturunkan dari otak sapi dengan IC (50) nilai sebesar 14,1, 19,2, dan 10,9 microM, masing-masing dan menghambat sphingomyelinase asam lebih efektif daripada sphingomyelinase netral dari otak sapi. alpha-Mangostin menghambat sphingomyelinase asam dalam cara yang paling selektif.alpha-Mangostin dimodifikasi secara kimia dan struktur-aktivitas hubungan yang dibahas.
PMID: 10938539 [PubMed - diindeks untuk MEDLINE]
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6: Lu ZX, M Hasmeda, W Mahabusarakam, B Ternai, Ternai PC, GM Polya.
Penghambatan kinase protein eukariot dan dengan fosfatase siklik nukleotida-mengikat oleh santon terprenilasi.
Biol Chem Interact. 1998 Juli 3; 114 (1-2) :121-40.
PMID: 9744560 [PubMed - diindeks untuk MEDLINE]
Penghambatan kinase protein eukariot dan dengan fosfatase siklik nukleotida-mengikat oleh santon terprenilasi.
Lu ZX, M Hasmeda, W Mahabusarakam, B Ternai, Ternai PC, GM Polya.
Sekolah Biokimia, La Trobe University, Bundoora, Victoria, Australia.
Serangkaian santon terprenilasi waktu bervariasi inhibitor ampuh subunit katalitik (CAK) dari hati tikus otak siklik AMP-dependent kinase (PKA), protein tikus Ca2 dan fosfolipid-tergantung protein kinase C (PKC), rempela ayam myosin rantai ringan kinase ( MLCK), embrio gandum bergantung Ca2 protein kinase (CDPK) dan umbi kentang fosfatase mengikat nukleotida siklik (Pase). The santon terprenilasi diperiksa sebagian besar turunan dari alfa-mangostin di mana 3-hidroksil dan 6-hidroksi yang beragam disubstitusi dengan gugus R atau R ‘masing-masing, atau derivatif dari 3-isomangostin (mangostanol) di mana 9-hidroksil digantidengan kelompok R ‘atau rantai samping prenyl dimodifikasi. Inhibitor yang paling potensial CAK memiliki kelompok R ‘dan R non-protonatable dan relatif kecil. Sebaliknya, penghambat yang paling ampuh dari BIS dan MLCK telah bulkier dan kelompok dasar R ‘. Beberapa santon terprenilasi juga inhibitor ampuh CDPK.PKC dan CAK yang kompetitif dihambat oleh santon terprenilasi tertentu sedangkan senyawa yang merupakan inhibitor yang paling ampuh MLCK dan CDPK adalah inhibitor non-kompetitif. santon terprenilasi memiliki R relatif kecil dan non-protonatable ‘dan kelompok R menghambat afinitas tinggi Pase nukleotida siklik mengikat secara non-kompetitif.
(Protein kinase membentuk sebuah harta karun target untuk berbagai indikasi, termasuk diabetes, gangguan inflamasi, dan terutama kanker.)
PMID: 9744560 [PubMed - diindeks untuk MEDLINE]
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7: AC Hopert, Beyer A, K Frank, E Strunck, W Wunsche, Vollmer G.
Karakterisasi estrogenicity phytoestrogen dalam model eksperimental yang diturunkan dari endometrium.
Kesehatan lingkungan Perspect. September 1998; 106 (9) :581-6.
PMID: 9721258 [PubMed - diindeks untuk MEDLINE]
Karakterisasi estrogenicity phytoestrogen dalam model eksperimental yang diturunkan dari endometrium.
AC Hopert, Beyer A, K Frank, E Strunck, W Wunsche, Vollmer G.
Institut bulu Molekulare Medizin, Universitat zu Lubeck Medizinische, Lubeck, Jerman.
parah gangguan perkembangan dan reproduksi pada hewan liar telah dikaitkan dengan paparan tinggi untuk bahan kimia lingkungan terus menerus dengan aktivitas hormonal.Ini efek samping dari estrogen lingkungan telah mengangkat keprihatinan yang cukup dan telah menerima peningkatan perhatian. Meskipun banyak bahan kimia dengan kapasitas untuk mengganggu dengan reseptor estrogen (ER) telah diidentifikasi, informasi tentang mekanisme molekuler mereka aksi dan potensi relatif agak terbatas.Untuk endometrium, kurangnya informasi adalah karena kurangnya model yang cocok.Kami meneliti fungsi phytoestrogen dalam model endometrium yang diturunkan, RUCA-aku tikus sel adenokarsinoma endometrium. Sel dikultur pada membran basement dibentuk kembali untuk mempertahankan diferensiasi fungsional dan responsif estrogen. Kami menilai afinitas mengikat relatif terhadap reseptor estrogen dari coumestrol phytoestrogen yang dipilih, genistein, daidzein, dan phytoestrogen mangostin putatif dibandingkan dengan estradiol dengan analisis Scatchard kompetitif.Peringkat afinitas berikut diukur: 17beta-estradiol>>> coumestrol> genistein> daidzein>>> mangostin. Selain itu, kami meneliti kemampuan senyawa ini untuk mempromosikan peningkatan produksi komplemen C3, protein estradiol-diatur terkenal endometrium tikus. Semua zat diuji meningkatkan produksi komplemen C3, meskipun konsentrasi yang berbeda diperlukan untuk mencapai tingkat setara induksi dibandingkan dengan estradiol. Mechanistically kami mampu menunjukkan bahwa peningkatan produksi komplemen C3 dimediasi oleh terutama meningkatkan tingkat steady-state mRNA-nya. Temuan ini menunjukkan bahwa RUCA-aku sel merupakan suatu sistem model yang sensitif untuk mengetahui potensi relatif dan fungsi estrogen lingkungan dalam model endometrium yang diturunkan.
PMID: 9721258 [PubMed - diindeks untuk MEDLINE]
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8: N Chairungsrilerd, Furukawa K, T Tadano,
Kisara K Ohizumi, Y.
Pengaruh gamma-mangostin melalui penghambatan reseptor 5-hidroksi-tryptamine2A dalam 5-fluoro-alpha-methyltryptamine-induced kepala berkedut tanggapan
mencit.
Br J Pharmacol. 1998 Mar; 123 (5) :855-62.
PMID: 9535013 [PubMed - diindeks untuk MEDLINE]
Pengaruh gamma-mangostin melalui penghambatan reseptor 5-hidroksi-tryptamine2A dalam 5-fluoro-alpha-methyltryptamine-induced kepala berkedut respon mencit.
Chairungsrilerd N, K Furukawa, T Tadano,
Kisara K Ohizumi, Y.
Departemen Biologi Molekuler, Fakultas Ilmu Farmasi, Universitas Tohoku, Sendai, Jepang.
1. Intracerebronventricular (ICV) suntikan gamma-mangostin (10-40 nmol / mouse), suatu senyawa utama dari lambung buah Garcinia mangostana Lin., Seperti ketanserin (10, 20 nmol / mouse, ICV) menghambat 5-fluoro-alpha- methyltryptamine (5-FMT) (45 mg kg (-1), ip)-induced kepala berkedut respon pada tikus dengan adanya atau tidak adanya citalopram (a 5-hydroxytryptamine (5-HT) inhibitor-serapan). 2. Baik 5-FMT-maupun 8-hidroksi-2-(di-n-propylamino) tetralin 5-HT1A-agonist)-sindrom 5-HT diinduksi (kepala tenun dan penculikan hindlimb) telah dipengaruhi oleh gamma-mangostin atau ketanserin. 3. Aktivitas lokomotor distimulasi oleh 5-FMT melalui aktivasi alpha1-adrenoceptors tidak mengubah di hadapan gamma-mangostin.4. 5-HT-akibat akumulasi inositol fosfat dalam irisan otak tikus itu dihapus oleh ketanserin.Gamma-mangostin menyebabkan hambatan konsentrasi-tergantung dari akumulasi inositol fosfat. 5. Gamma-mangostin menyebabkan hambatan konsentrasi-tergantung dari pengikatan [3H]-spiperone, antagonis reseptor 5-HT2A, untuk selaput otak tikus. 6.Kinetik analisis [3H]-spiperone mengikat menunjukkan bahwa gamma-mangostin meningkatkan nilai Kd tanpa mempengaruhi nilai Bmax, menunjukkan modus sifat kompetitif penghambatan oleh gamma-mangostin. 7. Hasil ini menunjukkan bahwa gamma-mangostin menghambat 5-FMT-induced kepala berkedut respon pada tikus dengan memblokir reseptor 5-HT2A tidak dengan menghalangi pelepasan 5-HT dari neuron pusat. Gamma-mangostin adalah 5-HT2A menjanjikan reseptor antagonis dalam sistem saraf pusat.
PMID: 9535013 [PubMed - diindeks untuk MEDLINE]
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9: Vlietinck AJ, De Bruyne T, S Apers, Pieters LA.
Tanaman yang berasal dari senyawa terkemuka untuk kemoterapi human immunodeficiency virus (HIV).
Planta Med. 1998 Mar, 64 (2) :97-109. Review.
PMID: 9525100 [PubMed - diindeks untuk MEDLINE]
Tanaman yang berasal dari senyawa terkemuka untuk kemoterapi human immunodeficiency virus (HIV).
Vlietinck AJ, T De Bruyne, Apers S, Pieters LA.
Departemen Ilmu Farmasi, Universitas Antwerpen (UA), Belgium.vlietink @ uta.ua.ac.be
Banyak senyawa yang berasal dari tumbuhan telah diidentifikasi yang menghambat tahapan yang berbeda dalam siklus replikasi human immunodeficiency virus (HIV): 1) adsorpsi virus: alkaloid chromone (schumannificine), alkaloid isoquinoline (michellamines), polisakarida sulfat dan polyphenolic, flavonoid, kumarin (glycocoumarin, licopyranocoumarin) phenolics (turunan asam caffeic, turunan asam galloyl, turunan asam catechinic), tanin dan triterpen (glycyrrhizin dan analog, soyasaponin dan analog); 2) virus-sel fusi: lektin (mannose-dan N-asetilglukosamin-spesifik) dan triterpen (betulinic asam dan analog); 3) reverse transkripsi; alkaloid (benzophenanthridines, protoberberines, isoquinolines, quinolines), kumarin (calanolides dan analog), flavonoid, phloroglucinols, lakton (asam protolichesterinic), tanin, iridoids (fulvoplumierin) dan triterpen ; 4) integrasi: kumarin (3-tersubstitusi-4-hydroxycoumarins), depsidones, derivatif O-caffeoyl, lignan (arctigenin dan analog) dan fenolat (kurkumin); 5) terjemahan: rantai tunggal protein inactivating ribosom (Scrip’s); 6) pembelahan proteolitik (inhibisi protease): saponin (asam ursolat dan maslinic), santon (mangostin dan analog) dan kumarin; 7) glikosilasi: alkaloid termasuk indolizidines (castanospermine dan analog), piperidines (1-deoxynojirimicin dan analog) dan pyrrolizidines (australine dan analog); 8) perakitan / rilis: naphthodianthrones (hypericin dan pseudohypericin), photosensitisers (terthiophenes dan furoisocoumarins) dan fosfolipid. Sasaran tindakan zat anti-HIV, termasuk beberapa alkaloid (O-demethyl-buchenavianine, papaverin), polisakarida (acemannan), lignan (intheriotherins, schisantherin), fenolat (gosipol, lignins, dimer katekol seperti peltatols, naphthoquinones seperti conocurvone ) dan saponin (celasdin B, Gleditsia dan saponin Gymnocladus), belum dijelaskan atau tidak masuk dalam skema yang diusulkan. Hanya sangat sedikit dari produk-produk anti-HIV tanaman-berasal telah digunakan dalam jumlah terbatas yaitu pasien yang menderita AIDS. glycyrrhizin, papaverin, trichosanthin, castanospermine, N-butil-1-deoxynojirimicin dan acemannan.
Publikasi Jenis:
• Review
• Review, Akademik
PMID: 9525100 [PubMed - diindeks untuk MEDLINE]
10: Furukawa K, N Chairungsrilerd, T Ohta, S Nozoe, Ohizumi Y.
[Novel jenis antagonis reseptor dari tanaman obat Garcinia mangostana]
Nippon Yakurigaku Zasshi. Oktober 1997; 110 Suppl 1:153 P-158P. Jepang.
PMID: 9503424 [PubMed - diindeks untuk MEDLINE]
[Novel jenis antagonis reseptor dari tanaman obat Garcinia mangostana]
[Pasal dalam bahasa Jepang]
Furukawa K, N Chairungsrilerd, T Ohta, S Nozoe, Ohizumi Y.
Departemen Biologi Molekuler Farmasi, Fakultas Ilmu Farmasi, Universitas Tohoku, Sendai, Jepang.
Sebuah metanol ekstrak kasar lambung buah Garcinia mangostana L. menghambat kontraksi dari aorta kelinci terisolasi yang disebabkan oleh histamin dan serotonin.Ekstrak telah difraksinasi secara kromatografi silika gel, untuk memonitor aktivitas farmakologi untuk memberikan senyawa aktif. Atas dasar data fisikokimia, zat aktif yang diidentifikasi sebagai alpha-mangostin dan gamma-mangostin. Untuk menentukan sifat farmakologi alpha-mangostin, efek alpha-mangostin terhadap kedua reseptor histamin H1 dan H2 diperiksa dengan memantau respon mekanik otot halus dan mengukur radioligand mengikat berbudaya sel otot pembuluh darah halus. Hasil penelitian menunjukkan bahwa alpha-mangostin bertindak sebagai antagonis reseptor histamin H1 selektif dan kompetitif. Tindakan farmakologi gamma-mangostin pada reseptor 5-HT juga diteliti dengan menggunakan respon kontraktil otot polos vaskuler, agregasi platelet dan studi mengikat radioligand. Hasil penelitian ini memberikan bukti bahwa gamma-mangostin merupakan antagonis reseptor selektif dan kompetitif 5-HT2A. Ini sangat menarik bahwa struktur alpha-mangostin dan gamma-mangostin bebas dari atom nitrogen tidak mirip dengan struktur umum histamin dan serotonin reseptor antagonis. alpha-Mangostin dan gamma-mangostin bisa menjadi novel jenis senyawa timbal untuk antagonis reseptor histamin dan serotonin.
PMID: 9503424 [PubMed - diindeks untuk MEDLINE]
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11: K Likhitwitayawuid, T Phadungcharoen,
Krungkrai J.
Antimalaria santon dari Garcinia cowa.
Planta Med. Februari 1998; 64 (1) :70-2.
PMID: 9491769 [PubMed - diindeks untuk MEDLINE]
Antimalaria santon dari Garcinia cowa.
Likhitwitayawuid K, T Phadungcharoen,
Krungkrai J.
Lima santon dari kulit Garcinia cowa, yaitu E 7-O-methylgarcinone (1), cowanin (2), cowanol (3), cowaxanthone (4), dan beta-mangostin (5), ditemukan memiliki anti malaria secara in vitro aktivitas terhadap Plasmodium falciparum dengan nilai IC50 berkisar antara 1,50-3,00 mikrogram / ml. Lengkap 1H-dan 13C-NMR tugas senyawa ini juga dilaporkan.
Publikasi Jenis:
• Surat
PMID: 9491769 [PubMed - diindeks untuk MEDLINE]
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12: N Chairungsrilerd, Furukawa KI, Ohta T, S Nozoe, Ohizumi Y.
Gamma-mangostin, jenis baru dari antagonis reseptor 5-hydroxytryptamine 2A.
Schmiedebergs Naunyn Arch Pharmacol. 1998 Jan; 357 (1) :25-31.
PMID: 9459569 [PubMed - diindeks untuk MEDLINE]
Gamma-mangostin, jenis novel receptorantagonist 2A 5-hydroxytryptamine.
Chairungsrilerd N, Furukawa KI, Ohta T, S Nozoe, Ohizumi Y.
Departemen Biologi Molekuler Farmasi, Fakultas Ilmu Farmasi, Universitas Tohoku, Sendai, Jepang.
Gamma-mangostin, dimurnikan dari lambung buah Garcinia mangostana tanaman obat disebabkan pergeseran paralel ke sebelah kanan dari konsentrasi / Kurva respons untuk kontraksi ditimbulkan oleh 5-hydroxytryptamine (5-HT) dalam aorta kelinci (pA2 = 8.2) tanpa mempengaruhi yang kontraktil tanggapan terhadap KCl, fenilefrin (alpha1) atau histamin (H1). Tekanan perfusi arteri tikus Respon koroner untuk 5-HT (5-HT2A) berkurang konsentrasi ketergantungan oleh gamma-mangostin (IC50 = 0,32 microM).5-HT diperkuat, ADP-induced agregasi trombosit kelinci (5-HT2A) dihambat oleh gamma-mangostin (IC50 = 0,29 microM), sedangkan yang disebabkan oleh trombin tidak terpengaruh, juga tidak gamma-mangostin mempengaruhi 5-HT-induced kontraksi ileum guinea-babi (5-HT3) di hadapan antagonis reseptor 5-HT1, 5-HT2 dan 5-HT4.Selanjutnya, 5-HT-diinduksi kontraksi fundus tikus (5-HT2B) dan 5-HT-relaksasi diinduksi dari aorta kelinci di hadapan ketanserin (5-HT1) dan carbachol-kontraksi yang disebabkan dari ileum guinea-babi ( muscarinic M3) tidak dipengaruhi oleh gamma-mangostin (5 microM). Gamma-mangostin menghambat [3H] spiperone mengikat miosit tikus berbudaya aorta (IC50 = 3,5 nM). The Kd untuk [3H] spiperone mengikat meningkat oleh gamma-mangostin (3 nM) 11,7-27,4 nM tanpa mempengaruhi hasil Bmax.These menunjukkan bahwa gamma-mangostin merupakan antagonis kompetitif novel, bebas dari atom nitrogen, selama 5 - HT2A reseptor pada otot polos vaskular dan trombosit.
PMID: 9459569 [PubMed - diindeks untuk MEDLINE]
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13: Gopalakrishnan G, B Banumathi, Suresh G.
Evaluasi aktivitas antijamur santon alam dari Garcinia mangostana dan turunannya sintetik mereka.
J nat Prod. 1997 Mei; 60 (5) :519-24.
PMID: 9213587 [PubMed - diindeks untuk MEDLINE]
Evaluasi aktivitas antijamur santon alam dari Garcinia mangostana dan turunannya sintetik mereka.
Gopalakrishnan G, B Banumathi, Suresh G.
Pusat Penelitian agrokimia, Yayasan Ilmu orang Amerika Latin, Madras, India.
Aktivitas antijamur dari beberapa santon terisolasi dari lambung buah Garcinia mangostana dan beberapa turunan mangostin terhadap tiga jamur phytopathogenic, vasinfectum Fusarium oxysporum, tenuis Alternaria, dan oryzae Dreschlera, telah dievaluasi. The santon alam menunjukkan aktivitas hambat yang baik terhadap tiga jamur. Substitusi pada cincin A dan C telah ditunjukkan untuk memodifikasi bioactivities senyawa.
PMID: 9213587 [PubMed - diindeks untuk MEDLINE]
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14: Chairungsrilerd N, K Furukawa, T Ohta, S Nozoe, Ohizumi Y.
Farmakologi sifat alpha-mangostin, sebuah novel antagonis reseptor histamin H1.
Eur J Pharmacol. 1996 Oktober 31; 314 (3) :351-6.
PMID: 8957258 [PubMed - diindeks untuk MEDLINE]
Farmakologi sifat alpha-mangostin, sebuah novel antagonis reseptor histamin H1.
Chairungsrilerd N, K Furukawa, T Ohta, S Nozoe, Ohizumi Y.
Departemen Biologi Molekuler Farmasi, Fakultas Ilmu Farmasi, Universitas Tohoku, Sendai, Jepang.
Dalam kelinci terisolasi aorta dada dan trakea guinea-babi, alpha-mangostin menghambat histamin-induced kontraksi dengan cara konsentrasi tergantung pada ada atau tidaknya cimetidine, suatu antagonis reseptor histamin H2. Tapi KCl-, fenilefrin-atau kontraksi carbachol-induced tidak dipengaruhi oleh alpha-mangostin.Kurva respons kontraktil konsentrasi untuk histamin dialihkan ke kanan secara paralel oleh alpha-mangostin.Di hadapan chlorpheniramine, antagonis reseptor histamin H1, alpha-mangostin tidak mempengaruhi relaksasi aorta kelinci diinduksi dengan histamin.Dalam trakea babi guinea, alpha-mangostin tidak berpengaruh pada relaksasi disebabkan oleh dimaprit, suatu agonis reseptor histamin H2. alpha-Mangostin menyebabkan hambatan konsentrasi-tergantung dari pengikatan [3H] mepyramine, sebuah histamin antagonis reseptor H1 khusus untuk tikus sel-sel otot polos aorta.Analisis Kinetika [3H] mepyramine mengikat menunjukkan inhibisi kompetitif dengan alpha-mangostin. Hasil ini menunjukkan bahwa alpha-mangostin merupakan novel histamin H1 reseptor antagonis kompetitif dalam sel otot polos.
PMID: 8957258 [PubMed - diindeks untuk MEDLINE]
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15: Chairungsrilerd N, K Furukawa, T Ohta, S Nozoe, Ohizumi Y.
Histaminergic dan serotonergik memblokir reseptor zat dari Garcinia mangostana tanaman obat.
Planta Med. Oktober 1996; 62 (5) :471-2.
PMID: 8923814 [PubMed - diindeks untuk MEDLINE]
Histaminergic dan serotonergik memblokir reseptor zat dari Garcinia mangostana tanaman obat.
Chairungsrilerd N, K Furukawa, T Ohta, S Nozoe, Ohizumi Y.
Sebuah metanol ekstrak kasar lambung buah manggis, Garcinia mangostana L. menghambat kontraksi dari aorta kelinci terisolasi dada yang disebabkan oleh histamin dan serotonin. Ekstrak dari buah lambung telah difraksinasi secara kromatografi silika gel, untuk memonitor aktivitas farmakologi untuk memberikan alpha dan gamma-mangostin. Berdasarkan data farmakologi, disarankan bahwa alpha-mangostin dan gamma-mangostin adalah histaminergic dan memblokir reseptor serotonergik agen, masing-masing.
Publikasi Jenis:
• Surat
PMID: 8923814 [PubMed - diindeks untuk MEDLINE]
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16: Iinuma M, H Tosa, Tanaka T, Asai M, Kobayashi Y, R Shimano, Miyauchi K.
Aktivitas antibakteri santon dari tanaman guttiferaeous terhadap Staphylococcus aureus resisten methicillin.
J Pharm Pharmacol. Agustus 1996; 48 (8) :861-5.
PMID: 8887739 [PubMed - diindeks untuk MEDLINE]
Aktivitas antibakteri santon dari tanaman guttiferaeous terhadap Staphylococcus aureus resisten methicillin.
Iinuma M, H Tosa, Tanaka T, Asai M, Kobayashi Y, R Shimano, Miyauchi K.
Departemen pharmacognosy, Farmasi Universitas Gifu, Jepang.
Ekstrak Garcinia mangostana (Guttiferae) menunjukkan efek inhibisi terhadap pertumbuhan S. aureus NIHJ 209p difraksinasi sesuai petunjuk yang diperoleh dari bioassay dan beberapa komponen dengan aktivitas terhadap Staphylococcus aureus resisten methicillin (MRSA) yang ditandai. Salah satu isolat aktif, alpha-mangostin, derivatif santon, memiliki konsentrasi hambat minimum (MIC) dari 1,57-12,5 mikrogram mL-1.santon terkait lainnya juga diperiksa untuk menentukan kegiatan anti-MRSA mereka. Rubraxanthone, yang diisolasi dari Garcinia dioica dan memiliki struktur yang sama dengan yang alpha-mangostin, memiliki aktivitas tertinggi terhadap strain staphylococcal (MIC = 0,31-1,25 mikrogram mL-1), sebuah kegiatan yang lebih besar daripada vankomisin antibiotik (3,13-6,25 mikrogram-mL 1). Efek penghambatan terhadap strain MRSA dari dua senyawa bila digunakan bersama dengan antibiotik lainnya juga dipelajari. Kegiatan anti-MRSA alpha-mangostin jelas meningkat dengan kehadiran vankomisin; perilaku ini tidak diamati untuk rubraxanthone. Di kuat-vitro aktivitas antibakteri turunan santon terhadap kedua Staphylococcus aureus resisten methicillin dan methicillin-sensitive menunjukkan senyawa mungkin menemukan penggunaan farmasi luas.
PMID: 8887739 [PubMed - diindeks untuk MEDLINE]
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17: Furukawa K, K Shibusawa, N Chairungsrilerd, T Ohta, S Nozoe, Ohizumi Y.
Modus tindakan penghambatan alpha-mangostin, inhibitor novel, pada retikulum sarkoplasma Ca (2)-pompa ATPase dari kelinci otot rangka.
Jpn J Pharmacol. Agustus 1996; 71 (4) :337-40.
PMID: 8886932 [PubMed - diindeks untuk MEDLINE]
Modus tindakan penghambatan alpha-mangostin, inhibitor novel, pada retikulum sarkoplasma Ca (2)-pompa ATPase dari kelinci otot rangka.
Furukawa K, K Shibusawa, N Chairungsrilerd, T Ohta, S Nozoe, Ohizumi Y.
Departemen Biologi Molekuler Farmasi, Fakultas Ilmu Farmasi, Universitas Tohoku, Sendai, Jepang.
alpha-Mangostin, bahan utama dari lambung buah Garcinia mangostana, menyebabkan penurunan konsentrasi yang bergantung pada aktivitas dari kedua Ca (2)-ATPase dan Ca (2)-pengangkutan retikulum sarkoplasma dari kelinci otot kerangka dengan sebuah IC50 nilai 5 microM. Baik rilis Ca2 maupun aktivitas enzim lain dipengaruhi oleh alpha-mangostin. Analisis Kinetika efek inhibisi alpha-mangostin terhadap Ca (2)-ATPase menunjukkan bahwa penghambatan ATPase adalah jenis-nonkompetitif berkenaan dengan ATP atau Ca2. alpha-Mangostin dapat menjadi alat yang berguna untuk memperjelas farmakologi fungsi fisiologis Ca (2)-pompa ATPase dan retikulum sarkoplasma.
PMID: 8886932 [PubMed - diindeks untuk MEDLINE]
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18: Chen SX, Wan M, Loh BN.
Konstituen aktif terhadap HIV-1 protease dari Garcinia mangostana.
Planta Med. Agustus 1996; 62 (4) :381-2.
PMID: 8792678 [PubMed - diindeks untuk MEDLINE]
Konstituen aktif terhadap HIV-1 protease dari Garcinia mangostana.
Chen SX, Wan M, Loh BN.
etanol ekstrak Garcinia mangostana L. (Guttiferae) menunjukkan aktivitas inhibisi yang manjur melawan HIV-1 protease. Pemurnian aktivitas-dipandu dari ekstrak mengakibatkan isolasi dua aktif, senyawa yang diketahui. struktur kimia dari senyawa terisolasi didirikan oleh analisis spektroskopi sebagai mangostin (IC50 = 5.12 / – 0,41 microM) dan gamma-mangostin (IC50 = 4.81 / – 0,32 microM). Jenis inhibisi oleh kedua senyawa yang kompetitif.
PMID: 8792678 [PubMed - diindeks untuk MEDLINE]
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19: Williams P, M Ongsakul, Proudfoot J, K Croft, Beilin L.
Mangostin menghambat modifikasi oksidatif lipoprotein kepadatan manusia yang rendah.
Free Radic Res. Agustus 1995; 23 (2) :175-84.
PMID: 7581813 [PubMed - diindeks untuk MEDLINE]
Mangostin menghambat modifikasi oksidatif lipoprotein kepadatan manusia yang rendah.
Williams P, M Ongsakul, Proudfoot J, K Croft, Beilin L.
University of Western Australia, Departemen Kedokteran, Rumah Sakit Royal Perth, Australia.
Oksidasi low density lipoprotein (LDL) dapat memainkan peran penting dalam aterosklerosis. Kami meneliti efek antioksidan kemungkinan mangostin, terisolasi dari Garcinia mangostana, pada ion logam bergantung (Cu2) dan independen (radikal peroxyl berair) oksidasi LDL manusia. Mangostin berkepanjangan lagtime untuk kedua oksidasi ion logam dependen dan independen LDL secara dosis tergantung selama 5 sampai 50 microM sebagaimana yang diawasi oleh pembentukan Diena konjugasi pada 234 nm (P <0,001).>Tidak ada pengaruh yang signifikan mangostin pada tingkat di mana Diena terkonjugasi dibentuk dalam tahap liar oksidasi. Tingkat zat reaktif thiobarbituric (TBARS) yang dihasilkan dalam LDL diukur 4 dan 24 jam setelah oksidasi dengan 5 Cu2 microM di hadapan atau tidak adanya 50 microM atau 100 mangostin microM. Kami mengamati hambatan pembentukan TBARS dengan 100 mangostin microM pada 4 jam (P = 0,027) tetapi tidak pada 24 jam (P = 0,163). Hasil yang serupa diamati di hadapan 50 mangostin microM. Mangostin, di 100 microM, menghambat mobilitas elektroforesis relatif LDL pada kedua 4 dan 24 jam setelah oksidasi diinduksi Cu2. Mangostin (100 microM) secara signifikan menghambat konsumsi alpha-tokoferol dalam LDL selama oksidasi dimulai Cu2 selama 75 menit (P <0,001).>Dari hasil ini, kami menyimpulkan mangostin yang bertindak sebagai scavenger radikal bebas untuk melindungi LDL dari kerusakan oksidatif di dalam sistem in vitro.
PMID: 7581813 [PubMed - diindeks untuk MEDLINE]
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20: Jinsart W, B Ternai, Buddhasukh D, GM Polya.
Penghambatan kalsium gandum embrio yang tergantung
kinase dan protein kinase lain dengan mangostin dan gamma-mangostin.
Fitokimia. November 1992; 31 (11) :3711-3.
PMID: 1368866 [PubMed - diindeks untuk MEDLINE]
Penghambatan embrio gandum kalsium bergantung kinase dan protein kinase lain dengan mangostin dan gamma-mangostin.
Jinsart W, B Ternai, Buddhasukh D, GM Polya.
Departemen Kimia, La Trobe University, Bundoora, Victoria, Australia.
Lambung dari buah pohon manggis (Garcinia mangostana) mengandung empat inhibitor tanaman Ca protein kinase (2)-dependen. Dua dari inhibitor telah dimurnikan dan diidentifikasi sebagai 1,3,6-trihydroxy-7-metoksi-2 ,8-bis santon (3-metil-2-butenil)-9H-xanthen-9-satu (mangostin) dan 1,3,6,7-tetrahidroksi-2 ,8-bis (3-metil-2-butenil) – 9H-xanthen-9-satu (gamma-mangostin). Kedua santon juga menghambat cahaya myosin rantai kinase burung dan hati tikus protein kinase siklik AMP-dependent. Ini adalah laporan pertama dari penghambatan tanaman dan hewan | kedua kinase protein kurir-diatur oleh santon tanaman berasal.
PMID: 1368866 [PubMed - diindeks untuk MEDLINE]
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21: Sundaram BM, C Gopalakrishnan, Subramanian S, Shankaranarayanan D, Kameswaran L.
Antimikroba kegiatan Garcinia mangostana.
Planta Med. 1983 Mei; 48 (1) :59-60. Tidak ada abstrak tersedia.
PMID: 6611746 [PubMed - diindeks untuk MEDLINE]
Antimikroba kegiatan Garcinia mangostana.
Sundaram BM, C Gopalakrishnan, Subramanian S, Shankaranarayanan D, Kameswaran L.
PMID: 6611746 [PubMed - diindeks untuk MEDLINE]
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22: Gopalakrishnan C, Shankaranarayanan D, Kameswaran L, SK Nazimudeen.
Pengaruh mangostin, sebuah santon dari Garcinia mangostana Linn. dalam reaksi immunopathological & inflamasi.
Indian J Exp Biol. Agustus 1980; 18 (8) :843-6. Tidak ada abstrak tersedia.
PMID: 7461736 [PubMed - diindeks untuk MEDLINE]
Pengaruh mangostin, sebuah santon dari Garcinia mangostana Linn.inimmunopathological & inflamasi reaksi.
Gopalakrishnan C, Shankaranarayanan D, Kameswaran L, SK Nazimudeen.
PMID: 7461736 [PubMed - diindeks untuk MEDLINE]
23: Shankaranarayan D, Gopalakrishnan C, Kameswaran L.
Farmakologi profil mangostin dan turunannya.
Arch Int Pharmacodyn Ada. Juni 1979; 239 (2) :257-69.
PMID: 314790 [PubMed - diindeks untuk MEDLINE]
Farmakologi profil mangostin dan turunannya.
Shankaranarayan D, Gopalakrishnan C, Kameswaran L.
Mangostin (M), santon alami di rinds dari buah Garcinia mangostana Linn. (Guttiferae) dan turunannya seperti mangostin 3-0-metil (MM), 3,6-di-O-metil mangostin (DM), 1-isomangostin (IM), mangostin triasetat (MT), mangostin 3,6 - di-O-(asetil tetra) glukosida (MTG) dan mangostin-6 ,6-di-O-glukosida (Mog) diskrining terhadap berbagai efek farmakologi pada hewan percobaan … M, IM dan MT dihasilkan aktivitas antiinflamasi diucapkan baik oleh rute intraperitoneal dan oral pada tikus yang diuji oleh edema kaki carrageenininduced belakang, implantasi kapas pelet dan teknik granuloma kantong. Antiinflamasi kegiatan untuk M, IM dan MT diamati bahkan pada tikus bilateral adrenalectomised. M, IM dan MT tidak menghasilkan menstabilkan membran sel mast efek dan efek degranulation dari polimiksin, diazoxide B dan Triton X-100 pada sel mast peritoneum tikus in vitro tidak dicegah. M, IM dan MT tidak mengubah waktu protrombin tikus albino. M sendiri dihasilkan aktivitas antiulcer signifikan pada tikus.
PMID: 314790 [PubMed - diindeks untuk MEDLINE]
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* Antiproliferasi, * antioxidation dan induksi apoptosis * oleh Garcinia mangostana (manggis) on line kanker payudara SKBR3 manusia sel
Primchanien Moongkarndi,, sebuah, Kosema Nuttavut, Kaslungkab Sineenart, Omboon Luanratanac, Narongchai Neungtond Pongpanc dan Neelobol
Departemen Mikrobiologi, Fakultas Farmasi, Universitas Mahidol, Sri Ayudthaya Road, Rajdhevee, Bangkok 10400, Thailand Organisasi Farmasi Pemerintah, Rama VI Road, Bangkok 10400, Thailand
Departemen pharmacognosy, Fakultas Farmasi, Universitas Mahidol, Sri Ayudthaya Road, Rajdhevee, Bangkok 10400, Thailand
Departemen Biokimia, Fakultas Kedokteran, Rumah Sakit Siriraj, Bangkok 10700, Thailand
Diterima 15 Juni 2002; revisi 10 September 2003; diterima 22 September 2003. ; Tersedia online 5 Desember 2003.
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Abstrak
Penelitian ini dirancang untuk menentukan sifat antiproliferatif, apoptosis dan antioksidan ekstrak metanol kasar (CME) dari pericarp dari Garcinia mangostana (keluarga Guttiferae) menggunakan kanker payudara manusia (SKBR3) line sel sebagai sistem model. SKBR3 sel dikultur dalam kehadiran CME di berbagai konsentrasi (0-50 g / ml) selama 48 jam dan persentase viabilitas sel dievaluasi oleh 3 – (4,5-dimethylthiazol-2-il) -2,5 - di fenil tetrazolium bromide (MTT) assay. CME menunjukkan inhibisi dosis-tergantung dari proliferasi sel dengan ED50 sebesar 9,25 ± 0,64 g / ml. Kami menemukan bahwa efek antiproliferatif CME dikaitkan dengan apoptosis pada sel kanker payudara line oleh penentuan perubahan morfologi dan fragmen DNA oligonucleosomal. Selain itu, CME di berbagai konsentrasi dan waktu inkubasi juga ditemukan untuk menghambat produksi ROS. Theseinvestigations menyarankan bahwa ekstrak metanol dari pericarp dari mangostana Garcinia telah antiproliferasi kuat, antioxidation kuat dan induksi apoptosis.Thus, ini menunjukkan bahwa zat ini dapat menunjukkan kegiatan yang berbeda dan memiliki potensi untuk chemoprevention kanker yang tergantung dosis serta waktu paparan tergantung .
Antiproliferasi = berhenti sel dari penyebaran
Antioxidation = berhenti kerusakan radikal bebas yang dapat menyebabkan mutasi lebih lanjut
Induksi apoptosis = Ini adalah proses kematian sel – sel apoptosis istirahat menjadi potongan-potongan lebih kecil yang disebut badan apoptosis sel-sel tubuh lainnya mengakui dan makan.
