Institut für Mangostan & natürliche Antioxidantien
Wissenschaftliche Studien und internationale Forschungsergebnisse | 36-55
36: Chem Pharm Bull (Tokyo). 2006 Mar;54(3):301-5.
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Cytotoxic prenylated xanthones from the young fruit of Garcinia mangostana.
Suksamrarn S, Komutiban O, Ratananukul P, Chimnoi N, Lartpornmatulee N, Suksamrarn A.
Department of Chemistry, Faculty of Science, Srinakharinwirot University, Sukhumvit, Bangkok, Thailand. sunit@swu.ac.th
Three new prenylated xanthones, mangostenones C (1), D (2), and E (3), together with 16 known xanthones 4-19, were isolated from the young fruit (7-week maturity stage) of Garcinia mangostana. The structural elucidation of the new compounds was mainly established on the basis of 1D and 2D NMR and HR-MS spectroscopic analysis. Compound 1 showed cytotoxic properties against three human cancer cell lines, epidermoid carcinoma of the mouth (KB), breast cancer (BC-1), and small cell lung cancer (NCI-H187), with IC50 values of 2.8, 3.53, and 3.72 microg/ml, respectively. Among the isolates, alpha-mangostin (12), the major metabolite, exhibited the most potent effects against the BC-1 cells with an IC50 value of 0.92 microg/ml, an activity greater than that of the standard drug ellipticine (IC50 = 1.46 microg/ml). Compound 12 also showed the highest activity against KB cells, while gartanin (10) displayed the strongest activity against the NCI-H187 cells at the respective IC50 values of 2.08 microg/ml and 1.08 microg/ml.
Publication Types:
PMID: 16508181 [PubMed - indexed for MEDLINE]
37: Chem Pharm Bull (Tokyo). 2006 Jan;54(1):111-3.
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Prenylated xanthone derivatives with antiplasmodial activity from Allanblackia monticola STANER L.C.
Azebaze AG, Meyer M, Valentin A, Nguemfo EL, Fomum ZT, Nkengfack AE.
Department of Chemistry, Faculty of Science, University of Douala, Cameroon. azebaze@yahoo.com
Further study of the methanol extract of the stem bark of Allanblackia monticola STANER L.C. resulted in the isolation of a new prenylated xanthenedione, designated allanxanthone C, together with the five known xanthones, garciniafuran, tovophyllin A, rubraxanthone, norcowanin and mangostin and one saponin, stigmasterol-3-O-beta-D-glucopyranoside. The structure of the new compound was established by detailed spectroscopic analysis to be 1,2-dihydro-3,6,8-trihydroxy-1,1,7-tri(3-methylbut-2-enyl)xanthen-2,9-dione (3-hydroxyapetalinone C). The methanol extract and pure compounds were tested on two strains of Plasmodium falciparum, F32 (chloroquine sensitive) and FcM29 (chloroquine resistant). The IC50 values obtained ranged from 0.6 to 8.9 microg/ml. Their cytotoxicity was estimated on human melanoma cells (A375) and the cytotoxicity/antiplasmodial ratio was found to be between 15.45 and 30.46. The antimicrobial activities against a range of microorganisms of the crude extract and some of these compounds are also reported.
Publication Types:
PMID: 16394561 [PubMed - indexed for MEDLINE]
38: Neurosci Lett. 2006 Feb 20;394(3):206-10. Epub 2005 Nov 2.
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Garcinone B reduces prostaglandin E2 release and NF-kappaB-mediated transcription in C6 rat glioma cells.
Yamakuni T, Aoki K, Nakatani K, Kondo N, Oku H, Ishiguro K, Ohizumi Y.
Department of Pharmaceutical Molecular Biology, Graduate School of Pharmaceutical Sciences, Tohoku University, Aoba, Aramaki, Aoba-ku, Sendai 980-8578, Japan.
In the course of our survey of natural compounds inhibiting prostaglandin E2 release and/or lipopolysaccharide (LPS)-induced transcriptional stimulation via NF-kappaB, a central regulator of inflammatory genes, from natural resources, we found garcinone B, a xanthone from callus tissue culture of Hypericum patulum, as a compound with such pharmacological activities, that is a derivative of gamma-mangostin which potently inhibits COX-1 and COX-2 activities to reduce PGE2 release from C6 rat glioma cells, and inhibits IKK activity to prevent NF-kappaB-dependent COX-2 gene transcription. Garcinone B, to a lesser extent, reduced A23187-induced increase in prostaglandin E2 release than gamma-mangostin and its structurally related compound, patulone, in C6 cells. This compound also prevented LPS-induced stimulation of NF-kappaB-dependent transcription. These results suggest that garcinone B becomes a unique pharmacological tool to investigate intracellular signaling pathways involved in inflammation.
Publication Types:
PMID: 16260090 [PubMed - indexed for MEDLINE]
39: Phytochemistry. 2005 Jul;66(14):1718-23.
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Xanthones and benzophenones from Garcinia griffithii and Garcinia mangostana.
Nguyen LH, Venkatraman G, Sim KY, Harrison LJ.
Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543, Republic of Singapore.
A new polyisoprenylated benzophenone, guttiferone I, together with the known compounds cambogin, 1,7-dihydroxyxanthone, 1,3,6,7-tetrahydroxyxanthone and 1,3,5,6-tetrahydroxyxanthone were isolated from the stem bark of Garcinia griffithii. The acetone extract of the heartwood of Garcinia mangostana contained one new diprenylated xanthone (mangoxanthone) and a new benzophenone (3',6-dihydroxy-2,4,4'-trimethoxybenzophenone) as well as the known xanthones dulxanthone D, 1,3,7-trihydroxy-2-methoxyxanthone, 1,3,5-trihydroxy-13,13-dimethyl-2H-pyran[7,6-b]xanthen-9-one. Their structures were established on the basis of spectroscopic studies and chemical correlation.
Publication Types:
PMID: 16173114 [PubMed - indexed for MEDLINE]
40: Bioorg Med Chem. 2005 Nov 1;13(21):6064-9.
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Xanthones induce cell-cycle arrest and apoptosis in human colon cancer DLD-1 cells.
Matsumoto K, Akao Y, Ohguchi K, Ito T, Tanaka T, Iinuma M, Nozawa Y.
Gifu International Institute of Biotechnology, 1-1 Naka-Fudogaoka, Kakamigahara, Gifu 504-0838, Japan. matsumoto@bio.rd.pref.gifu.jp
We investigated the antiproliferative effects of four structurally similar prenylated xanthones, alpha-mangostin, beta-mangostin, gamma-mangostin, and methoxy-beta-mangostin, in human colon cancer DLD-1 cells. These xanthones differ in the number of hydroxyl and methoxy groups. Except for methoxy-beta-mangostin, the other three xanthones strongly inhibited cell growth at 20 microM and their antitumor efficacy was correlated with the number of hydroxyl groups. Hoechst 33342 nuclear staining and nucleosomal DNA-gel electrophoresis revealed that the antiproliferative effects of alpha- and gamma-mangostin, but not that of beta-mangostin, were associated with apoptosis. It was also shown that their antiproliferative effects were associated with cell-cycle arrest by affecting the expression of cyclins, cdc2, and p27; G1 arrest was by alpha-mangostin and beta-mangostin, and S arrest by gamma-mangostin. These findings provide a relevant basis for the development of xanthones as an agent for cancer prevention and combination therapy with anti-cancer drugs.
Publication Types:
PMID: 16112579 [PubMed - indexed for MEDLINE]
41: J Ethnopharmacol. 2005 Oct 3;101(1-3):330-3.
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Antimicrobial effects of Thai medicinal plants against acne-inducing bacteria.
Chomnawang MT, Surassmo S, Nukoolkarn VS, Gritsanapan W.
Department of Microbiology, Faculty of Pharmacy, Mahidol University, 447 Sri Ayudthaya Road, Rachathevi, Bangkok 10400, Thailand. scmtd@mahidol.ac.th
Propionibacterium acnes and Staphylococcus epidermidis have been recognized as pus-forming bacteria triggering an inflammation in acne. The present study was conducted to evaluate antimicrobial activities of Thai medicinal plants against these etiologic agents of acne vulgaris. Crude extracts were tested for antimicrobial activities by disc diffusion and broth dilution methods. The results from the disc diffusion method showed that 13 medicinal plants could inhibit the growth of Propionibacterium acnes. Among those, Senna alata, Eupatorium odoratum, Garcinia mangostana, and Barleria lupulina had strong inhibitory effects. Based on a broth dilution method, the Garcinia mangostana extract had the greatest antimicrobial effect. The MIC values were the same (0.039 mg/ml) for both bacterial species and the MBC values were 0.039 and 0.156 mg/ml against Propionibacterium acnes and Staphylococcus epidermidis, respectively. In bioautography assay, the Garcinia mangostana extract produced strong inhibition zones against Propionibacterium acnes. Antimicrobial activity from fractions of column chromatography revealed one of the active compounds in Garcinia mangostana could be mangostin, a xanthone derivative. Taken together, our data indicated that Garcinia mangostana had a strong inhibitory effect on Propionibacterium acnes and Staphylococcus epidermidis. Therefore, this plant would be an interesting topic for further study and possibly for an alternative treatment for acne.
Publication Types:
PMID: 16009519 [PubMed - indexed for MEDLINE]
42: Clin Microbiol Infect. 2005 Jun;11(6):510-2.
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Activity of medicinal plant extracts against hospital isolates of methicillin-resistant Staphylococcus aureus.
Voravuthikunchai SP, Kitpipit L.
Department of Microbiology, Faculty of Science, Prince of Songkla University, Hatyai, Songkla, Thailand. supayang.v@psu.ac.th
Aqueous and ethanolic extracts of ten traditional Thai medicinal plants were investigated for their ability to inhibit 35 hospital isolates of methicillin-resistant Staphylococcus aureus (MRSA). Nine medicinal plants displayed activity against all isolates tested. Ethanolic extracts of Garcinia mangostana, Punica granatum and Quercus infectoria were most effective, with MICs for MRSA isolates of 0.05-0.4, 0.2-0.4 and 0.2-0.4 mg/mL, respectively, and for S. aureus ATCC 25923 of 0.1, 0.2 and 0.1 mg/mL, respectively. MBCs for MRSA isolates were 0.1-0.4, 1.6-3.2 and 0.4-1.6 mg/mL, and for S. aureus ATCC 25923 were 0.4, 3.2 and 1.6 mg/mL, respectively.
PMID: 15882206 [PubMed - indexed for MEDLINE]
43: Phytomedicine. 2005 Mar;12(3):203-8.
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Antibacterial activity of alpha-mangostin against vancomycin resistant Enterococci (VRE) and synergism with antibiotics.
Sakagami Y, Iinuma M, Piyasena KG, Dharmaratne HR.
Osaka Prefectural Institute of Public Health, Osaka, Japan. sakagami@iph.pref.osaka.jp
alpha-Mangostin, isolated from the stem bark of Garcinia mangostana L., was found to be active against vancomycin resistant Enterococci (VRE) and methicillin resistant Staphylococcus aureus (MRSA), with MIC values of 6.25 and 6.25 to 12.5 microg/ml, respectively. Our studies showed synergism between alpha-mangostin and gentamicin (GM) against VRE, and alpha-mangostin and vancomycin hydrochloride (VCM) against MRSA. Further studies showed partial synergism between alpha-mangostin and commercially available antibiotics such as ampicillin and minocycline. These findings suggested that alpha-mangostin alone or in combination with GM against VRE and in combination with VCM against MRSA might be useful in controlling VRE and MRSA infections.
PMID: 15830842 [PubMed - indexed for MEDLINE]
44: Nat Prod Res. 2005 Apr;19(3):239-43.
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A geranylated biphenyl derivative from Garcinia malvgostana.
Dharmaratne HR, Piyasena KG, Tennakoon SB.
Natural Products Programme, Institute of Fundamental Studies, Kandy 20000, Sri Lanka. hrwd@ifs.ac.lk
Extracts of root bark, stem bark and the latex collected from the green fruits of Garcinia mangostana gave alpha-mangostin, beta-mangostin, gamma-mangostin, garcinone-E, methoxy-beta-mangostin and a new geranylated biphenyl derivative 3-hydroxy-4-geranyl-5-methoxybiphenyl. The latex of G. mangostana consists of more than 75% of xanthones which have strong antibacterial (anti-MRSA and -VRE), anti-inflammatory, antifungal and a number of other biological activities. Hence the presence of the above highly bioactive compounds in large quantities should be the causative factor for G. mangostana's medicinal value in indigenous medicine.
PMID: 15702637 [PubMed - indexed for MEDLINE]
45: Asian Pac J Cancer Prev. 2004 Oct-Dec;5(4):433-8.
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Inhibitory effects of crude alpha-mangostin, a xanthone derivative, on two different categories of colon preneoplastic lesions induced by 1, 2-dimethylhydrazine in the rat.
Nabandith V, Suzui M, Morioka T, Kaneshiro T, Kinjo T, Matsumoto K, Akao Y, Iinuma M, Yoshimi N.
Tumor Pathology Division, Faculty of Medicine, University of the Ryukyus, Okinawa 903-0215, Japan.
The purpose of this study was to examine whether crude alpha-mangostin (a major xanthone derivative in mangosteen pericarp (Garcinia mangostana)) has short-term chemopreventive effects on putative preneoplastic lesions involved in rat colon carcinogenesis. The crude preparation was obtained by simple recrystallization of an ethylacetate extract of mangosteen pericarps. A total of 33 five-week-old male F344 rats were randomly divided into 5 experimental groups. Rats in groups 1-3 were given a subcutaneous injection of 1,2-dimethylhydrazine (DMH)(40 mg/kg body weight) once a week for 2 weeks. Starting one week before the first injection of DMH, rats in groups 2 and 3 were fed a diet containing 0.02% and 0.05% crude alpha-mangostin, respectively, for 5 weeks. Rats in group 4 also received the diet containing 0.05% crude alpha-mangostin, while rats in group 5 served as untreated controls. The experiment was terminated 5 weeks after the start. Dietary administration of crude alpha-mangostin at both doses significantly inhibited the induction and/or development of aberrant crypt foci (ACF) (P<0.05 for 0.02% crude alpha-mangostin, P<0.01 for 0.05% crude alpha-mangostin), when compared to the DMH-treated group (group 1). Moreover, treatment of rats with 0.05% crude alpha-mangostin significantly decreased dysplastic foci (DF) (P<0.05) and beta-catenin accumulated crypts (BCAC) (P<0.05), to below the group 1 values. The proliferating cell nuclear antigen (PCNA) labeling indices of colon epithelium and focal lesions in groups 2 and 3 were also significantly lower than in group 1 and this effect occurred in a dose dependent manner of the crude alpha-mangostin. This finding that crude alpha-mangostin has potent chemopreventive effects in our short-term colon carcinogenesis bioassay system suggests that longer exposure might result in suppression of tumor development.
Publication Types:
PMID: 15546251 [PubMed - indexed for MEDLINE]
46: Bioorg Med Chem. 2004 Nov 15;12(22):5799-806.
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Preferential target is mitochondria in alpha-mangostin-induced apoptosis in human leukemia HL60 cells.
Matsumoto K, Akao Y, Yi H, Ohguchi K, Ito T, Tanaka T, Kobayashi E, Iinuma M, Nozawa Y.
Gifu International Institute of Biotechnology, 1-1 Naka-Fudogaoka, Kakamigahara, Gifu 504-0838, Japan. kmatsumo@giib.or.jp
Our previous study has shown that alpha-mangostin, a xanthone from the pericarps of mangosteen, induces caspase-3-dependent apoptosis in HL60 cells. In the current study, we investigated the mechanism of apoptosis induced by alpha-mangostin in HL60 cells. Alpha-mangostin-treated HL60 cells demonstrated caspase-9 and -3 activation but not -8, which leads us to assume that alpha-mangostin may mediate the mitochondrial pathway in the apoptosis. Parameters of mitochondrial dysfunction including swelling, loss of membrane potential (deltapsim), decrease in intracellular ATP, ROS accumulation, and cytochrome c/AIF release, were observed within 1 or 2 h after the treatment. On the other hand, alpha-mangostin-treatment did not affect expression of bcl-2 family proteins and activation of MAP kinases. These findings indicate that alpha-mangostin preferentially targets mitochondria in the early phase, resulting in indication of apoptosis in HL60 cells. Furthermore, we examined the structure-activity relationship between xanthone derivatives including alpha-mangostin and the potency of deltapsim-loss in HL60 cells. Interestingly, replacement of hydroxyl group by methoxy group remarkably decreased its potency. It was also shown that the cytotoxicity substantially correlated with deltapsim decrease. These results indicate that alpha-mangostin and its analogs would be candidates for preventive and therapeutic application for cancer treatment.
Publication Types:
PMID: 15498656 [PubMed - indexed for MEDLINE]
47: Life Sci. 2004 Nov 5;75(25):3077-85.
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Antimalarial xanthones from Calophyllum caledonicum and Garcinia vieillardii.
Hay AE, Hélesbeux JJ, Duval O, Labaïed M, Grellier P, Richomme P.
SONAS, UFR des Sciences pharmaceutiques et Ingénierie de la santé, 16, Bd Daviers, Angers, France.
The antimalarial activity of 22 xanthones against chloroquino-resistant strains of Plasmodium falciparum was evaluated. Natural caloxanthone C (1), demethylcalabaxanthone (2), calothwaitesixanthone (3), calozeyloxanthone (4), dombakinaxanthone (5), macluraxanthone (6), and 6-deoxy-gamma-mangostin (7) were isolated from Calophyllum caledonicum. 1,6-dihydroxyxanthone (8), pancixanthone A (9), isocudraniaxanthone B (10), isocudraniaxanthone A (11), 2-deprenylrheediaxanthone B (12) and 1,4,5-trihydroxyxanthone (13) were isolated from Garcinia vieillardii. Moreover, synthetic compounds (14-22) are analogues or intermediates of xanthones purified from Calophyllum caledonicum (Oger J.M., Morel C., Helesbeux J.J., Litaudon M., Seraphin D., Dartiguelongue C., Larcher G., Richomme P., Duval O. 2003. First 2-Hydroxy-3-Methylbut-3-Enyl substituted xanthones isolated from Plants: structure elucidation, synthesis and antifungal activity. Natural Product Research 17(3), 195-199; Helesbeux J.J., Duval O., Dartiguelongue C., Seraphin D., Oger J.M., Richomme P., 2004. Synthesis of 2-hydroxy-3-methylbut-3-enyl substituted coumarins and xanthones as natural products. Application of the Schenck ene reaction of singlet oxygen with ortho-prenylphenol precursors. Tetrahedron 60(10), 2293-2300). The relationship between antimalarial activity and molecular structure of xanthones has also been explored. The most potent xanthones (2), (3) and (7) (IC50 = c.a. 1.0 microg/mL) are 1,3,7 trioxygenated and prenylated on the positions 2 and 8.
Publication Types:
PMID: 15474559 [PubMed - indexed for MEDLINE]
48: Mol Pharmacol. 2004 Sep;66(3):667-74.
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gamma-Mangostin inhibits inhibitor-kappaB kinase activity and decreases lipopolysaccharide-induced cyclooxygenase-2 gene expression in C6 rat glioma cells.
Nakatani K, Yamakuni T, Kondo N, Arakawa T, Oosawa K, Shimura S, Inoue H, Ohizumi Y.
Department of Pharmaceutical Molecular Biology, Graduate School of Pharmaceutical Sciences, Tohoku University, Aoba, Aramaki, Aoba-ku, Sendai 980-8578, Japan.
We investigated the effect of gamma-mangostin purified from the fruit hull of the medicinal plant Garcinia mangostana on spontaneous prostaglandin E(2) (PGE(2)) genase release and inducible cyclooxy-2 (COX-2) gene expression in C6 rat glioma cells. An 18-h treatment with gamma-mangostin potently inhibited spontaneous PGE(2) release in a concentration-dependent manner with the IC(50) value of approximately 2 microM, without affecting the cell viability even at 30 microM. By immunoblotting and reverse-transcription polymerase chain reaction, we showed that gamma-mangostin concentration-dependently inhibited lipopolysaccharide (LPS)-induced expression of COX-2 protein and its mRNA, but not those of constitutive COX-1 cyclooxygenase. Because LPS is known to stimulate inhibitor kappaB (IkappaB) kinase (IKK)-mediated phosphorylation of IkappaB followed by its degradation, which in turn induces nuclear factor (NF)-kappaB nuclear translocation leading to transcriptional activation of COX-2 gene, the effect of gamma-mangostin on the IKK/IkappaB cascade controlling the NF-kappaB activation was examined. An in vitro IKK assay using IKK protein immunoprecipitated from C6 cell extract showed that this compound inhibited IKK activity in a concentration-dependent manner, with the IC(50) value of approximately 10 microM. Consistently gamma-mangostin was also observed to decrease the LPS-induced IkappaB degradation and phosphorylation in a concentration-dependent manner, as assayed by immunoblotting. Furthermore, luciferase reporter assays showed that gamma-mangostin reduced the LPS-inducible activation of NF-kappaB-and human COX-2 gene promoter region-dependent transcription. gamma-Mangostin also inhibited rat carrageenan-induced paw edema. These results suggest that gamma-mangostin directly inhibits IKK activity and thereby prevents COX-2 gene transcription, an NF-kappaB target gene, probably to decrease the inflammatory agent-stimulated PGE(2) production in vivo, and is a new useful lead compound for anti-inflammatory drug development.
Publication Types:
PMID: 15322259 [PubMed - indexed for MEDLINE]
49: Fitoterapia. 2004 Jun;75(3-4):375-7.
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Antiproliferative activity of Thai medicinal plant extracts on human breast adenocarcinoma cell line.
Moongkarndi P, Kosem N, Luanratana O, Jongsomboonkusol S, Pongpan N.
Department of Microbiology, Faculty of Pharmacy, Mahidol University, Rajdhevee, Sri Ayudthaya Rd, Bangkok 10400, Thailand. pypmk@mahidol.ac.th
Ethanolic extracts of selected nine Thai medicinal plants were tested for antiproliferative activity against SKBR3 human breast adenocarcinoma cell line using MTT assay. Garcinia mangostana showed the most potent activity. However, all plant extracts showed activity in potential range for further investigation on cancer cells. Copyright 2004 Elsevier B.V.
Publication Types:
PMID: 15158999 [PubMed - indexed for MEDLINE]
50: J Pharmacol Sci. 2004 May;95(1):33-40.
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Alpha-mangostin induces Ca2+-ATPase-dependent apoptosis via mitochondrial pathway in PC12 cells.
Sato A, Fujiwara H, Oku H, Ishiguro K, Ohizumi Y.
Department of Pharmaceutical Molecular Biology, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.
We investigated the cell death effects of eight xanthones on PC12 rat pheochromocytoma cells. Among these compounds, alpha-mangostin, from the fruit hull of Garcinia mangostana L., had the most potent effect with the EC(50) value of 4 microM. Alpha-mangostin-treated PC12 cells demonstrated typical apoptotic DNA fragmentation and caspase-3 cleavage (equivalent to activation). The flow cytometric analysis indicated that this compound induced apoptosis in time-and concentration-dependent manners. Alpha-mangostin showed the features of the mitochondrial apoptotic pathway such as mitochondrial membrane depolarization and cytochrome c release. Furthermore, alpha-mangostin inhibited the sarco(endo)plasmic reticulum Ca(2+)-ATPase markedly. There was a correlation between the Ca(2+)-ATPase inhibitory effects and the apoptotic effects of the xanthone derivatives. On the other hand, c-Jun NH(2)-terminal kinase (JNK/SAPK), one of the signaling molecules of endoplasmic reticulum (ER) stress, was activated with alpha-mangostin treatment. These results suggest that alpha-mangostin inhibits Ca(2+)-ATPase to cause apoptosis through the mitochondrial pathway.
Publication Types:
PMID: 15153648 [PubMed - indexed for MEDLINE]
51: J Ethnopharmacol. 2004 Jan;90(1):161-6.
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Antiproliferation, antioxidation and induction of apoptosis by Garcinia mangostana (mangosteen) on SKBR3 human breast cancer cell line.
Moongkarndi P, Kosem N, Kaslungka S, Luanratana O, Pongpan N, Neungton N.
Department of Microbiology, Faculty of Pharmacy, Mahidol University, Sri Ayudthaya Road, Rajdhevee, Bangkok 10400, Thailand. pypmk@mahidol.ac.th
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 microg/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 ED(50) of 9.25+/-0.64 microg/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. These investigations 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.
Publication Types:
PMID: 14698525 [PubMed - indexed for MEDLINE]
52: Bioorg Med Chem Lett. 2003 Oct 6;13(19):3151-3.
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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).
Publication Types:
PMID: 12951083 [PubMed - indexed for MEDLINE]
53: J Nat Prod. 2003 Aug;66(8):1124-7.
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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. kmatsumoto@giib.or.jp
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 - indexed for MEDLINE]
54: Chem Pharm Bull (Tokyo). 2003 Jul;51(7):857-9.
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Antimycobacterial activity of prenylated xanthones from the fruits of Garcinia mangostana.
Suksamrarn S, Suwannapoch N, Phakhodee W, Thanuhiranlert J, Ratananukul P, Chimnoi N, Suksamrarn A.
Department of Chemistry, Faculty of Science, Srinakharinwirot University, Bangkok, Thailand. sunit@swu.ac.th
Prenylated xanthones, isolated from the fruit hulls and the edible arils and seeds of Garcinia mangostana, were tested for their antituberculosis potential. Alpha- and beta-mangostins and garcinone B exhibited strong inhibitory effect against Mycobacterium tuberculosis with the minimum inhibitory concentration (MIC) value of 6.25 microg/ml. Tri- and tetra-oxygenated xanthones with di-C5 units or with a C5 and a modified C5 groups are essential for high activities. Substitution in the A and C rings has been shown to modify the bioactivity of the compounds.
Publication Types:
PMID: 12843596 [PubMed - indexed for MEDLINE]
55: Planta Med. 2002 Nov;68(11):975-9.
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Garcinone E, a xanthone derivative, has potent cytotoxic effect against hepatocellular carcinoma cell lines.
Ho CK, Huang YL, Chen CC.
Department of Medical Research & Education, Veterans General Hospital, Taipei, ROC.
Treatment of hepatocellular carcinomas (HCCs) with chemotherapy has generally been disappointing and it is most desirable to have more effective new drugs. We extracted and purified 6 xanthone compounds from the rinds (peel) of the fruits of Garcinia mangostana L., using partitioned chromatography and then tested the cytotoxic effects of these compounds on a panel of 14 different human cancer cell lines including 6 hepatoma cell lines, based on the MTT method. Several commonly used chemotherapeutic agents were included in the assay to determine the relative potency of the potential new drugs. Our results have shown that one of the xanthone derivatives which could be identified as garcinone E has potent cytotoxic effect on all HCC cell lines as well as on the other gastric and lung cancer cell lines included in the screen. We suggest that garcinone E may be potentially useful for the treatment of certain types of cancer.
Publication Types:
PMID: 12451486 [PubMed - indexed for MEDLINE]
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