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Gambogic acid and epigambogic acid, C-2 epimers with novel anticancer effects from Garcinia hanburyi
Han, QB; Yang, L; Liu, Y; Wang, YL; Qiao, CF; Song, JZ; Xu, LJ; Yang, DJ; Chen, SL; Xu, HX
Source PublicationPLANTA MEDICA
2006-02-01
DOI10.1055/s-2005-916193
Volume72Issue:3Pages:281-284
Indexed BySCI
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine
WOS SubjectPlant Sciences ; Chemistry, Medicinal ; Pharmacology & Pharmacy
WOS Research AreaPlant Sciences ; Pharmacology & Pharmacy
WOS KeywordIN-VITRO ; CELLS ; APOPTOSIS
AbstractGambogic 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.
Language英语
WOS IDWOS:000236279400019
Citation statistics
Cited Times:42[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/140376
Collection中国科学院大连化学物理研究所
Affiliation1.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
GB/T 7714
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.
APA Han, QB.,Yang, L.,Liu, Y.,Wang, YL.,Qiao, CF.,...&Xu, HX.(2006).Gambogic acid and epigambogic acid, C-2 epimers with novel anticancer effects from Garcinia hanburyi.PLANTA MEDICA,72(3),281-284.
MLA Han, QB,et al."Gambogic acid and epigambogic acid, C-2 epimers with novel anticancer effects from Garcinia hanburyi".PLANTA MEDICA 72.3(2006):281-284.
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