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pubmed-article:16534739pubmed:abstractTextGambogic acid, usually isolated as an inseparable stereomeric mixture of C-2 epimers, was newly separated into two epimers (1 and 2) from the gamboges of Garcinia hanburyi. The stereochemistry at C-2 was clearly defined by extensive spectroscopic analysis and direct comparison of NMR and HPLC data with those of the known R-epimer. Both epimers were examined for their cytotoxicities against human leukemia K562 (K562/S) and doxorubicin-resistant K562 (K562/R) cell lines. Different from doxorubicin (IC (50) = 10.78 microM for K562/R and 0.66 microM for K562/S), epimers 1 and 2 exhibited similar activities against both cell lines (IC(50) = 1.32 and 0.89 microM for 1, IC(50) = 1.11 and 0.86 microM for 2). These results suggested that both epimers were not multidrug resistance (MDR) substrates. Furthermore, epimers 1 and 2 were tested for their inhibitory effects against six human cytochrome P-450 enzymes. Epimers 1 and 2 showed little inhibitory effects toward five of the enzymes except CYP2C9. Interestingly, when tested against CYP2C9, S-epimer 2 had an inhibitory effect 20-fold stronger than that of R-epimer 1.lld:pubmed
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pubmed-article:16534739pubmed:authorpubmed-author:LiuYongYlld:pubmed
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pubmed-article:16534739pubmed:authorpubmed-author:YangDajianDlld:pubmed
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pubmed-article:16534739pubmed:authorpubmed-author:SongJingzheng...lld:pubmed
pubmed-article:16534739pubmed:authorpubmed-author:XuLijiaLlld:pubmed
pubmed-article:16534739pubmed:authorpubmed-author:ChenShilinSlld:pubmed
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pubmed-article:16534739pubmed:pagination281-4lld:pubmed
pubmed-article:16534739pubmed:dateRevised2006-11-15lld:pubmed
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pubmed-article:16534739pubmed:articleTitleGambogic acid and epigambogic acid, C-2 epimers with novel anticancer effects from Garcinia hanburyi.lld:pubmed
pubmed-article:16534739pubmed:affiliationChinese Medicine Laboratory, Hong Kong Jockey Club Institute of Chinese Medicine, Shatin, NT, PR China.lld:pubmed
pubmed-article:16534739pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:16534739pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed
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