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题名: Gambogic acid and epigambogic acid, C-2 epimers with novel anticancer effects from Garcinia hanburyi
作者: Han, QB;  Yang, L;  Liu, Y;  Wang, YL;  Qiao, CF;  Song, JZ;  Xu, LJ;  Yang, DJ;  Chen, SL;  Xu, HX
刊名: PLANTA MEDICA
发表日期: 2006-02-01
DOI: 10.1055/s-2005-916193
卷: 72, 期:3, 页:281-284
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Plant Sciences ;  Chemistry, Medicinal ;  Pharmacology & Pharmacy
研究领域[WOS]: Plant Sciences ;  Pharmacology & Pharmacy
英文摘要: Gambogic 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 (IC50 = 10.78 mu M for K562/R and 0.66 mu M for K562/S), epimers 1 and 2 exhibited similar activities against both cell lines (IC50 = 1.32 and 0.89 mu M for 1, IC50 = 1.11 and 0.86 mu M 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.
关键词[WOS]: IN-VITRO ;  CELLS ;  APOPTOSIS
语种: 英语
WOS记录号: WOS:000236279400019
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/140376
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Hong Kong Jockey Club Inst Chinese Med, Chinese Med Lab, Shatin, Hong Kong, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resources Discovery, Dalian, Peoples R China
3.Hong Kong Polytech Univ, Dept Appl Biol & Chem Technol, Kowloon, Hong Kong, Peoples R China

Recommended Citation:
Han, QB,Yang, L,Liu, Y,et al. Gambogic acid and epigambogic acid, C-2 epimers with novel anticancer effects from Garcinia hanburyi[J]. PLANTA MEDICA,2006,72(3):281-284.
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