Institut für Mangostan & natürliche Antioxidantien
Wissenschaftliche Studien und internationale Forschungsergebnisse | 16-35
16: J Agric Food Chem. 2007 Nov 28;55(24):9805-10. Epub 2007 Oct 26.
Related Articles,
Links
Assay-guided fractionation study of alpha-amylase inhibitors from Garcinia mangostana pericarp.
Loo AE, Huang D.
Department of Chemistry, National University of Singapore, Republic of Singapore.
Alpha-amylase inhibitor (alpha-AI) activity of Garcinia mangostana, commonly known as mangosteen, pericarp extracts was studied by assay guided fractionations from lipophilic to hydrophilic using combined solvent extraction and Amberlite XAD2 adsorption chromatography. Neither the lipophilic, xanthone containing fraction, nor the highly polar fraction, which has no affinity on Amberlite XAD2, showed any alpha-AI. The fraction that shows very high inhibitory activity contains primarily polyphenols and can be adsorbed on Amberlite XAD2. The IC50 of 5.4 microg/mL of this fraction is comparable to that of acarbose, a prescribed alpha-AI used in the control of type II diabetes, at 5.2 microg/mL. Total phenolic content (TPC) of each fraction was measured and the TPC has no correlation with the alpha-AI activity. The lipophilic fraction contains mainly xanthones as revealed by HPLC-MS analysis. Colorimetric analysis coupled with UV-vis and IR spectroscopic analysis demonstrated that the fractions with high alpha-AI activity are primarily oligomeric proanthocyanidins (OPCs) with little gallate moiety. There is also evidence to show that the alpha-AI by these OPCs is not purely by nonspecific protein complexation. Both tannic acid and G. mangostana OPCs precipitate BSA equally well but G. mangostana OPCs are 56 times more effective in inhibiting alpha-amylase.
Publication Types:
PMID: 17960880 [PubMed - indexed for MEDLINE]
17: Bioorg Med Chem. 2007 Nov 15;15(22):6900-8. Epub 2007 Aug 22.
Related Articles,
Links
Discovery of platelet-type 12-human lipoxygenase selective inhibitors by high-throughput screening of structurally diverse libraries.
Deschamps JD, Gautschi JT, Whitman S, Johnson TA, Gassner NC, Crews P, Holman TR.
Department of Chemistry and Biochemistry, University of California, Santa Cruz, CA 95064, USA.
Human lipoxygenases (hLO) have been implicated in a variety of diseases and cancers and each hLO isozyme appears to have distinct roles in cellular biology. This fact emphasizes the need for discovering selective hLO inhibitors for both understanding the role of specific lipoxygenases in the cell and developing pharmaceutical therapeutics. To this end, we have modified a known lipoxygenase assay for high-throughput (HTP) screening of both the National Cancer Institute (NCI) and the UC Santa Cruz marine extract library (UCSC-MEL) in search of platelet-type 12-hLO (12-hLO) selective inhibitors. The HTP screen led to the characterization of five novel 12-hLO inhibitors from the NCI repository. One is the potent but non-selective michellamine B, a natural product, anti-viral agent. The other four compounds were selective inhibitors against 12-hLO, with three being synthetic compounds and one being alpha-mangostin, a natural product, caspase-3 pathway inhibitor. In addition, a selective inhibitor was isolated from the UCSC-MEL (neodysidenin), which has a unique chemical scaffold for a hLO inhibitor. Due to the unique structure of neodysidenin, steady-state inhibition kinetics were performed and its mode of inhibition against 12-hLO was determined to be competitive (K(i)=17microM) and selective over reticulocyte 15-hLO-1 (K(i) 15-hLO-1/12-hLO>30).
Publication Types:
PMID: 17826100 [PubMed - indexed for MEDLINE]
PMCID: PMC2203963 [Available on 11/15/08]
18: J Agric Food Chem. 2007 Sep 19;55(19):7689-94. Epub 2007 Aug 23.
Related Articles,
Links
Oligomeric proanthocyanidins from mangosteen pericarps.
Fu C, Loo AE, Chia FP, Huang D.
Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543, Republic of Singapore.
Oligomeric proanthocyanidins were extracted from mangosteen pericarps and fractionated by a Sephadex LH-20 column to give 0.66% yield (dry matter). (13)C and (1)H NMR signals showed the presence of predominantly procyanidins together with a few prodelphinidin units along with small amounts of stereoisomers of afzelechin/epiafzelechin, catechin/epicatechin, and gallocatechin/epigallocatechin. Depolymerization with benzylmercaptan resulted in epicatechin thioether as the major product, and the mean degree of polymerization was determined to be 6.6. The electron spray ionization-mass spectrometry and matrix-assisted laser desorption/ionization time-of-flight mass spectra revealed the dominant B type oligomers with mainly epicatechin units and with a small amount of A type oligomers. The isolated proanthocyanidins are potent peroxyl radical scavengers as evidenced by the high oxygen radical scavenging capacity at 1.7 x 10 (4) micromol TE/g, much higher than that of pine bark and grape seed extracts.
Publication Types:
PMID: 17715900 [PubMed - indexed for MEDLINE]
19: Fitoterapia. 2007 Sep;78(6):401-8. Epub 2007 Jun 2.
Related Articles,
Links
Effect of Garcinia mangostana on inflammation caused by Propionibacterium acnes.
Chomnawang MT, Surassmo S, Nukoolkarn VS, Gritsanapan W.
Department of Microbiology, Faculty of Pharmacy, Mahidol University, Rachathevi, Bangkok, Thailand. scmtd@mahidol.ac.th
The present study was aimed to investigate the activity of Thai medicinal plants on inflammation caused by Propionibacterium acnes in terms of free radical scavenging and cytokine reducing properties. P. acnes have been recognized as pus-forming bacteria triggering an inflammation in acne. Antioxidant activity was determined by DPPH scavenging and NBT reduction assay. The result showed that Garcinia mangostana possessed the most significant antioxidant activity and reduced reactive oxygen species production. Houttuynia cordata, Eupatorium odoratum, and Senna alata had a moderate antioxidant effect. In addition, Garcinia mangostana extracts could reduce the TNF-alpha production as determined by ELISA. Garcinia mangostana was highly effective in scavenging free radicals and was able to suppress the production of pro-inflammatory cytokines. This study has identified the promising source of anti-inflammatory agent which could be useful in treatment of acne vulgaris.
Publication Types:
PMID: 17644272 [PubMed - indexed for MEDLINE]
20: J Sep Sci. 2007 Jun;30(9):1229-34.
Related Articles,
Links
HPLC analysis of selected xanthones in mangosteen fruit.
Walker EB.
Department of Chemistry, Weber State University, Ogden, Utah 84403-2503, USA. ewalker@weber.edu
Xanthones are unique chemical compounds found in nature, composed of a tricyclic aromatic system with a variety of phenolic, methoxy, and isoprene substituents, giving rise to numerous derivatives. They dissolve to varying degrees in solvents ranging from alcohol to hexane. An optimum solvent mixture of acetone/water (80:20) selectively and effectively extracts a wide variety of xanthones. Subsequent HPLC analysis using standard C-18 RP and a 30-min gradient of 65-90% MetOH in 0.1% formic acid detects and separates numerous different xanthones with UV detection at 254 nm. The xanthones alpha-mangostin, 8-desoxygartanin, gartanin, beta-mangostin, 3-mangostin, and 9-hydroxycalabaxanthone have been extracted, identified, and quantitatively determined using this method. This analytical method is applied to the analysis of these xanthones in the rind of the mangosteen fruit, Garcinia mangostana.
PMID: 17623461 [PubMed - indexed for MEDLINE]
21: J Agric Food Chem. 2007 Jul 11;55(14):5842-9. Epub 2007 Jun 13.
Related Articles,
Links
Comparative study of health properties and nutritional value of durian, mangosteen, and snake fruit: experiments in vitro and in vivo.
Haruenkit R, Poovarodom S, Leontowicz H, Leontowicz M, Sajewicz M, Kowalska T, Delgado-Licon E, Rocha-Guzmán NE, Gallegos-Infante JA, Trakhtenberg S, Gorinstein S.
Faculty of Agricultural Industry and Department of Soil Science, King Mongkut's Institute of Technology Ladkrabang, Ladkrabang, Bangkok 10520, Thailand.
In vitro and in vivo studies of the health and nutritional properties of durian (Durio zibethinus Murr.) were compared with snake fruit (Salacca edulis Reinw.) and mangosteen (Garcinia mangostana). Dietary fibers, minerals, and trace metals were comparable. Total polyphenols (mg of GAE/100 g of FW) and flavonoids (85.1+/-6.1) were significantly higher (p<0.05) than in snake fruit (217.1+/-13.2 (mg of CE/100 g of FW)), durian (309.7+/-19.3 and 61.2+/-4.9), and mangosteen (190.3+/-12.1 and 54.1+/-3.8). Antioxidant activity (microM TE/100 g of FW) of durian measured by DPPH and ABTS assays (228.2+/-13.4 and 2016.3+/-81.1) was significantly higher (p<0.05) than in snake fruit (110.4+/-7.9 and 1507.5+/-70.1) and mangosteen (79.1+/-5.9 and 1268.6+/-62.3). HPLC/DAD analysis of durian (microg/100 g of FW) showed that quercetin (1214.23+/-116.7) was present at levels three times that of caffeic acid, and twice as high as p-coumaric and cinnamic acids. The correlation coefficients between the bioactive compounds of fruits and their antioxidant activities were high (R2=0.99). Male Wistar rats (25) were divided into five dietary groups: the control group was fed the basal diet (BD); in addition to BD, the cholesterol (Chol) group was supplemented with 1% of Chol; the diets of the Chol/Durian, Chol/Snake, and Chol/Mangosteen groups were supplemanted with 5% of these fruits, respectively. It was found that diets supplemented with durian, and to a lesser degree with snake fruit and mangosteen, significantly hindered the rise in plasma lipids and the decrease in antioxidant activity. The nutritional values were comparably high. In conclusion, it could be suggested that inclusion of studied tropical fruits, especially durian, in known disease-preventing diets could be beneficial.
Publication Types:
PMID: 17567034 [PubMed - indexed for MEDLINE]
22: Bioorg Med Chem. 2007 Aug 15;15(16):5620-8. Epub 2007 May 18.
Related Articles,
Links
Characterized mechanism of alpha-mangostin-induced cell death: caspase-independent apoptosis with release of endonuclease-G from mitochondria and increased miR-143 expression in human colorectal cancer DLD-1 cells.
Nakagawa Y, Iinuma M, Naoe T, Nozawa Y, Akao Y.
Gifu International Institute of Biotechnology, 1-1 Naka-Fudogaoka, Kakamigahara, Gifu 504-0838, Japan.
alpha-Mangostin, a xanthone from the pericarps of mangosteen (Garcinia mangostana Linn.), was evaluated for in vitro cytotoxicity against human colon cancer DLD-1 cells. The number of viable cells was consistently decreased by the treatment with alpha-mangostin at more than 20 microM. The cytotoxic effect of 20 microM alpha-mangostin was found to be mainly due to apoptosis, as indicated by morphological findings. Western blotting, the results of an apoptosis inhibition assay using caspase inhibitors, and the examination of caspase activity did not demonstrate the activation of any of the caspases tested. However, endonuclease-G released from mitochondria with the decreased mitochondrial membrane potential was shown. The levels of phospho-Erk1/2 were increased in the early phase until 1h after the start of treatment and thereafter decreased, and increased again in the late phase. On the other hand, the level of phospho-Akt was sharply reduced with the process of apoptosis after 6h of treatment. Interestingly, the level of microRNA-143, which negatively regulates Erk5 at translation, gradually increased until 24h following the start of treatment. We also examined the synergistic growth suppression in DLD-1 cells by the combined treatment of the cells with alpha-mangostin and 5-FU which is one of the most effective chemotherapeutic agents for colorectal adenocarcinoma. The co-treatment with alpha-mangostin and 5-FU, both at 2.5 microM, augmented growth inhibition compared with the treatment with 5 microM of alpha-mangostin or 5 microM 5-FU alone. These findings indicate unique mechanisms of alpha-mangostin-induced apoptosis and its action as an effective chemosensitizer.
Publication Types:
PMID: 17553685 [PubMed - indexed for MEDLINE]
23: Nat Prod Res. 2006 Dec;20(14):1332-7.
Related Articles,
Links
Antioxidant xanthones from Cratoxylum cochinchinense.
Phuwapraisirisan P, Udomchotphruet S, Surapinit S, Tip-Pyang S.
Natural Product Research Unit, Department of Chemistry, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand. preecha.p@chula.ac.th
A new xanthone named cratoxylumxanthone A (1), together with five known compounds: dulcisxanthone B (2), alpha-mangostin (3), beta-mangostin (4), 2-geranyl-1,3,7-trihydroxy-4-(3-methylbut-2-enyl)xanthone (5) and tectochrystin (6), was isolated from Cratoxylum cochinchinense stems. The structure of new compound was characterized by 1D and 2D NMR techniques. The isolated compounds showed free radical scavenging against DPPH and lipid peroxidation inhibition.
Publication Types:
PMID: 17393660 [PubMed - indexed for MEDLINE]
24: Commun Agric Appl Biol Sci. 2006;71(2 Pt B):475-81.
Related Articles,
Links
The novel botanical insecticide for the control brown planthopper (Nilaparvata lugens Stal.).
Bullangpoti V, Visetson S, Milne M, Milne J, Pornbanlualap S, Sudthongkongs C, Tayapat S.
Dept. of Zoology, Faculty of Science, Kasetsart University, Bangkok 10900 Thailand.
Brown planthopper, Nilaparvata lugens Stal., (BPH) was the most devastating insect pest on rice in many partS of Asia. The Outbreak of BPH? which is resistant to many synthetic insecticides can cause total rice crop loss. This research was done to evaluate the efficiency of mangostin from the pericarp of mangosteen fruit extract (Garcina mangostana L.) as the alternative control of BPH. The pericarp of mangosteen fruit was extracted by Soxhlet apparatus using ethanol as a solvent and purified by chromatography method then qualified structure by 2D-NMR, MS and IR. The crude extracts contained mangostin ca. 2.956% w/w. This extract was trailed by the topical sprayer method with 1st, 2nd, 3rd, 4th and 5th nymph and adult BPH shows toxicity in term of LC50 ca. 1.39, 2.26, 5.44, 4.49, 4.03 and 3.84 % w/v at 24 h exposure, respectively. The in vitro enzyme activity from BPH survived after 24 h exposure and showed to inhibit the carboxylesterase (CarE), acetylchoinesterase (AchE) and glutathione-S-transferase (GST) activities which the correction factors of CarE, AchE and GST indicated ca. 1.21-2.05 fold, 1.24-2.50 fold and 1.01-3.34 fold, respectively. Moreover, the data shows that the carboxylesterase may play an important role to detoxify this extract. The results suggested that pericarp of mangosteen fruit extract which have mangostin as active ingredient compound shows mechanism as the inhibitor of detoxification enzymes. Thus, it is likely to be uses this extract as an insecticide alternative to the control of BPH.
PMID: 17385515 [PubMed - indexed for MEDLINE]
25: J Int Acad Periodontol. 2007 Jan;9(1):19-25.
Related Articles,
Links
Effects of herbal mouthwash containing the pericarp extract of Garcinia mangostana L on halitosis, plaque and papillary bleeding index.
Rassameemasmaung S, Sirikulsathean A, Amornchat C, Hirunrat K, Rojanapanthu P, Gritsanapan W.
Department of Oral Medicine, Faculty of Dentistry, Mahidol University, Bangkok, Thailand. dtsrs@mahidol.ac.th
OBJECTIVES: To determine the effects of herbal mouthwash containing the pericarp extract of Carcinia mangostana L on volatile sulfur compound (VSC) levels, plaque index (PI) and papillary bleeding index (PBI) in gingivitis subjects and the recurrence of these parameters after periodontal treatment. METHODS: Sixty subjects who were diagnosed as having mild or moderate chronic gingivitis were randomly distributed into herbal or placebo mouthwash groups. On day 1, all parameters were recorded. Subjects rinsed with the assigned mouthwash and VSC was measured at 30 min and 3 h post-rinsing. For the following 2 weeks, subjects practiced their usual oral hygiene and rinsed with the assigned mouthwash twice daily after tooth brushing. On day 15, parameters were recorded. In the 4-week washout period that followed, subjects received scaling and polishing. After another baseline examination, they were re-randomized into the herbal or placebo group and rinsed with mouthwash for 2 weeks. All parameters were re-evaluated on day 15. RESULTS: All parameters were significantly different compared to baseline in both groups at 30 min, 3 h and day 15 (p < 0.05). When compared between groups, VSC was significantly different at day 15 (p < 0.05). After scaling, poloshing and rinsing with mouthwash for 2 weeks, PI and PBI were significantly different compared to baseline (p < 0.05) while VSC was not (p > 0.05). When compared between groups, VSC was significantly different (p < 0.05). CONCLUSION: Herbal mouthwash containing the pericarp extract of G. mangostana may be used as an adjunct in treating oral malodor.
Publication Types:
PMID: 17274236 [PubMed - indexed for MEDLINE]
26: Ann Trop Med Parasitol. 2007 Jan;101(1):23-30.
Related Articles,
Links
Antimalarial and vasorelaxant constituents of the leaves of Allanblackia monticola (Guttiferae).
Azebaze AG, Dongmo AB, Meyer M, Ouahouo BM, Valentin A, Laure Nguemfo E, Nkengfack AE, Vierling W.
Department of Chemistry, Faculty of Science, University of Douala, P.O. Box 24157, Douala, Cameroon. azebaze@yahoo.com
Phytochemical investigation of the leaves of Allanblackia monticola led to the isolation and characterisation of five prenylated xanthones [1,6-dihydroxy-3,7-dimethoxy-2-(3-methylbut-2-enyl)xanthone 1, alpha-mangostin 2, tovophyllin A 3, allanxanthone C 4 and 1,7-dihydroxy-3-methoxy-2-(3-methylbut-2-enyl)xanthone 5], two biflavonoid derivatives (amentoflavone 6 and podocarpusflavone A 7) and one pentacyclic triterpene (friedelan-3-one 8). The structures of these compounds were established on the basis of homo- and hetero-nuclear, one- and two-dimensional, nuclear magnetic resonance. Compounds 2-8 and a crude methanolic extract of A. monticola leaves were each tested for antimalarial activity in vitro, using the chloroquine-sensitive F32 and chloroquine-resistant FcM29 strains of Plasmodium falciparum; the median inhibitory concentrations (IC(50)) recorded varied from 0.7 to 83.5 mug/ml. The cytotoxicities of the compounds and crude extract, against cultures of human melanoma cells (A375), were then investigated, and cytotoxicity/antimalarial IC(50) ratios of 0.6-16.75 were recorded. In tests involving aortic rings from guinea pigs, a crude extract of the leaves of A. monticola was found to induce concentration-dependent vasorelaxation, causing up to 82% and 42% inhibition of noradrenaline- and KCl-induced contractions, respectively. The corresponding values for compounds 2 and 6 when tested against noradrenaline-induced contractions were approximately 18% and 35%, respectively.
Publication Types:
PMID: 17244407 [PubMed - indexed for MEDLINE]
27: J Pharm Biomed Anal. 2007 Mar 12;43(4):1270-6. Epub 2006 Nov 28.
Related Articles,
Links
Quantitative and qualitative determination of six xanthones in Garcinia mangostana L. by LC-PDA and LC-ESI-MS.
Ji X, Avula B, Khan IA.
National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.
A new method was developed for the simultaneous analysis of six naturally occurring xanthones (3-isomangostin, 8-desoxygartanin, gartanin, alpha-mangostin, 9-hydroxycalabaxanthone and beta-mangostin). The quantitative determination was conducted by reversed phase high performance liquid chromatography with photodiode array detector (LC-PDA). Separation was performed on a Phenomenex Luna C18(2) (150 mm x 3.00 mm, 5 microm) column. The xanthones were identified by retention time, ultraviolet (UV) spectra and quantified by LC-PDA at 320 nm. The precision of the method was confirmed by the relative standard deviation (R.S.D.), which was < or =4.6%. The recovery was in the range from 96.58% to 113.45%. A good linear relationship was established in over two orders of magnitude range. The limits of detection (LOD) for six xanthone compounds were < or =0.248 microg/mL. The identity of the peaks was further confirmed by high performance liquid chromatography with time-of-flight mass spectrometry (LC-TOF MS) system coupled with electrospray ionization (ESI) interface. The developed methods were applied to the determination of six xanthones in Garcinia mangostana products. The satisfactory results showed that the methods are effective for the analysis of real samples.
Publication Types:
PMID: 17129697 [PubMed - indexed for MEDLINE]
28: Nat Prod Res. 2006 Oct;20(12):1067-73.
Related Articles,
Links
Xanthones from Garcinia mangostana (Guttiferae).
Ee GC, Daud S, Taufiq-Yap YH, Ismail NH, Rahmani M.
Department of Chemistry, Faculty of Science, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia. gwen@fsas.upm.edu.my
Studies on the stem of Garcinia mangostana have led to the isolation of one new xanthone mangosharin (1) (2,6-dihydroxy-8-methoxy-5-(3-methylbut-2-enyl)-xanthone) and six other prenylated xanthones, alpha-mangostin (2), beta-mangostin (3), garcinone D (4), 1,6-dihydroxy-3,7-dimethoxy-2-(3-methylbut-2-enyl)-xanthone (5), mangostanol (6) and 5,9-dihydroxy-8- methoxy-2,2-dimethyl-7-(3-methylbut-2-enyl)-2H,6H-pyrano-[3,2-b]-xanthene-6-one (7). The structures of these compounds were determined by spectroscopic methods such as 1H NMR, 13C NMR, mass spectrometry (MS) and by comparison with previous studies. All the crude extracts when screened for their larvicidal activities indicated very good toxicity against the larvae of Aedes aegypti. This article reports the isolation and identification of the above compounds as well as bioassay data for the crude extracts. These bioassay data have not been reported before.
Publication Types:
PMID: 17127660 [PubMed - indexed for MEDLINE]
29: FEMS Immunol Med Microbiol. 2006 Dec;48(3):367-72. Epub 2006 Oct 18.
Related Articles,
Links
Antimicrobial activity in cultures of endophytic fungi isolated from Garcinia species.
Phongpaichit S, Rungjindamai N, Rukachaisirikul V, Sakayaroj J.
Natural Products Research Unit and Department of Microbiology, Faculty of Science, Prince of Songkla University, Hat Yai, Songkla, Thailand. souwalak.p@psu.ac.th
The aim of the present study was to screen for antimicrobial activity in endophytic fungi isolated from surface sterilized leaves and branches of five Garcinia plants, G. atroviridis, G. dulcis, G. mangostana, G. nigrolineata and G. scortechinii, found in southern Thailand. Fermentation broths from 377 isolated fungi were tested for antimicrobial activity by the agar diffusion method. Minimum inhibitory concentrations (MICs) were obtained for crude ethyl acetate extracts. Seventy isolates (18.6%) displayed antimicrobial activity against at least one pathogenic microorganism, such as Staphylococcus aureus, a clinical isolate of methicillin-resistant S. aureus, Candida albicans and Cryptococcus neoformans. The results revealed that 6-10%, 1-2% and 18% of the crude ethyl acetate extracts inhibited both strains of S. aureus (MIC 32-512 microg mL(-1)), Ca. albicans and Cr. neoformans (MIC 64-200 microg mL(-1)), and Microsporum gypseum (MIC 2-64 microg mL(-1)), respectively. Isolates D15 and M76 displayed the strongest antibacterial activity against both strains of S. aureus. Isolates M76 and N24 displayed strong antifungal activity against M. gypseum. Fungal molecular identification based on internal transcribed spacer rRNA gene sequence analysis demonstrated that isolates D15 (DQ480353), M76 (DQ480360) and N24 (DQ480361) represented Phomopsis sp., Botryosphaeria sp. and an unidentified fungal endophyte, respectively. These results indicate that some endophytic fungi from Garcinia plants are a potential source of antimicrobial agents.
Publication Types:
PMID: 17052267 [PubMed - indexed for MEDLINE]
30: Virol J. 2006 Sep 1;3:68.
Related Articles,
Links
Natural products that reduce rotavirus infectivity identified by a cell-based moderate-throughput screening assay.
Shaneyfelt ME, Burke AD, Graff JW, Jutila MA, Hardy ME.
Veterinary Molecular Biology, Montana State University, Bozeman, MT 59715, USA. mshaneyf@gonzaga.edu
BACKGROUND: There is widespread interest in the use of innate immune modulators as a defense strategy against infectious pathogens. Using rotavirus as a model system, we developed a cell-based, moderate-throughput screening (MTS) assay to identify compounds that reduce rotavirus infectivity in vitro, toward a long-term goal of discovering immunomodulatory agents that enhance innate responses to viral infection. RESULTS: A natural product library consisting of 280 compounds was screened in the assay and 15 compounds that significantly reduced infectivity without cytotoxicity were identified. Time course analysis of four compounds with previously characterized effects on inflammatory gene expression inhibited replication with pre-treatment times as minimal as 2 hours. Two of these four compounds, alpha-mangostin and 18-beta-glycyrrhetinic acid, activated NFkappaB and induced IL-8 secretion. The assay is adaptable to other virus systems, and amenable to full automation and adaptation to a high-throughput format. CONCLUSION: Identification of several compounds with known effects on inflammatory and antiviral gene expression that confer resistance to rotavirus infection in vitro suggests the assay is an appropriate platform for discovery of compounds with potential to amplify innate antiviral responses.
Publication Types:
- Research Support, N.I.H., Extramural
- Research Support, Non-U.S. Gov't
- Research Support, U.S. Gov't, Non-P.H.S.
PMID: 16948846 [PubMed - indexed for MEDLINE]
PMCID: PMC1564392
31: Planta Med. 2006 Aug;72(10):912-6. Epub 2006 Aug 10.
Related Articles,
Links
Prenylated xanthones as potential antiplasmodial substances.
Mahabusarakam W, Kuaha K, Wilairat P, Taylor WC.
Department of Chemistry, Prince of Songkla University, Hat Yai, Songkhla, Thailand. wilawan.m@psu.ac.th
Mangostin, the major xanthone of Garcinia mangostana, and a series of synthetic derivatives were investigated for their in vitro antiplasmodial activity against Plasmodium falciparum. Mangostin itself showed moderate activity, but prenylated xanthones containing alkylamino functional groups exhibited quite potent antiplasmodial activity. Some structure-activity relationships are proposed.
Publication Types:
PMID: 16902859 [PubMed - indexed for MEDLINE]
32: Med Princ Pract. 2006;15(4):281-7.
Related Articles,
Links
Antioxidative and neuroprotective activities of extracts from the fruit hull of mangosteen (Garcinia mangostana Linn.).
Weecharangsan W, Opanasopit P, Sukma M, Ngawhirunpat T, Sotanaphun U, Siripong P.
Faculty of Pharmacy, Silpakorn University, Nakhonpathom, Thailand.
OBJECTIVE: The aim of this study was to investigate the antioxidative and neuroprotective activities of various extracts from the fruit hull of mangosteen (Garcinia mangostana Linn., GM). MATERIALS AND METHODS: Four extracts: water, 50% ethanol, 95% ethanol and ethyl acetate, were used. The antioxidative activity was evaluated using 2,2-diphenyl-1-picrylhydrazyl free-radical scavenging assay at extract concentrations of 1, 10, 50 and 100 microg/ml. Based on the free radical scavenging activity of the extracts, two (water and 50% ethanol) were selected for their protective activity in NG108-15 neuroblastoma cells against H(2)O(2)-induced oxidative stress and for cell viability using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. RESULTS: All extracts exhibited antioxidative activity. The water and 50% ethanol extracts showed high free-radical scavenging activity with IC(50) values of 34.98 +/- 2.24 and 30.76 +/- 1.66 microg/ml, respectively. Both water and 50% ethanol extracts exhibited neuroprotective activity on NG108-15 cells. The highest activity was observed at the concentration of 50 microg/ml for both the water and 50% ethanol extracts. For cytotoxicity test, none of the extracts was toxic to the cells except at the high concentration of 100 microg/ml. CONCLUSIONS: These results suggest that the water and 50% ethanol extracts from the fruit hull of GM may be potent neuroprotectants.
Publication Types:
PMID: 16763395 [PubMed - indexed for MEDLINE]
33: J Am Diet Assoc. 2006 Jun;106(6):986.
Related Articles,
Links
What are the facts and myths about mangosteen?
Marcason W.
American Dietetic Association's Knowledge Center, Chicago, IL, USA. knowledge@eatright.org
PMID: 16720137 [PubMed - indexed for MEDLINE]
34: Chem Pharm Bull (Tokyo). 2006 May;54(5):745-7.
Related Articles,
Links
Cytotoxic and antimalarial prenylated xanthones from Cratoxylum cochinchinense.
Laphookhieo S, Syers JK, Kiattansakul R, Chantrapromma K.
School of Science, Mae Fah Luang University, Thasud, Muang, Chiang Rai 57100, Thailand. surat@mfu.ac.th
A new prenylated xanthone, 5-O-methylcelebixanthone (1), together with six known compounds; celebixanthone (2), 1,3,7-trihydroxy-2,4-di(3-methylbut-2-enyl)xanthone (3), cochinchinone A (4), alpha-mangostin (5), beta-mangostin (6) and cochinchinone C (7) were isolated from roots of Cratoxylum cochinchinense. Their structures were elucidated by spectroscopic methods. Compounds 2 and 4-7 showed cytotoxic activity against the human lung cancer cell line (NCI-H187) with IC(50) values ranging from 0.65 to 5.2 microg/ml. Compounds 1, 2, 6 and 7 also showed antimalarial activity against Plasmodium falciparum with IC(50) values of 3.2, 4.9, 7.2 and 2.6 microg/ml, respectively.
PMID: 16651783 [PubMed - indexed for MEDLINE]
35: J Agric Food Chem. 2006 Mar 22;54(6):2077-82.
Related Articles,
Links
Antioxidant xanthones from the pericarp of Garcinia mangostana (Mangosteen).
Jung HA, Su BN, Keller WJ, Mehta RG, Kinghorn AD.
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, USA.
As part of ongoing research on cancer chemopreventive agents from botanical dietary supplements, Garcinia mangostana L. (commonly known as mangosteen) was selected for detailed study. Repeated chromatography of a CH2Cl2-soluble extract of the pericarp led to the isolation of two new highly oxygenated prenylated xanthones, 8-hydroxycudraxanthone G (1) and mangostingone [7-methoxy-2-(3-methyl-2-butenyl)-8-(3-methyl-2-oxo-3-butenyl)-1,3,6-trihydroxyxanthone, 2], together with 12 known xanthones, cudraxanthone G (3), 8-deoxygartanin (4), garcimangosone B (5), garcinone D (6), garcinone E (7), gartanin (8), 1-isomangostin (9), alpha-mangostin (10), gamma-mangostin (11), mangostinone (12), smeathxanthone A (13), and tovophyllin A (14). The structures of compounds 1 and 2 were elucidated by spectroscopic data analysis. Except for compound 2, which was isolated as a minor component, the antioxidant activities of all isolates were determined using authentic and morpholinosydnonimine-derived peroxynitrite methods, and compounds 1, 8, 10, 11, and 13 were the most active. Alpha-mangostin (10) inhibited 7,12-dimethylbenz[alpha]anthracene-induced preneoplastic lesions in a mouse mammary organ culture assay with an IC50 of 1.0 microg/mL (2.44 microM).
Publication Types:
PMID: 16536578 [PubMed - indexed for MEDLINE]
nach oben