Planta Med 2006; 72(3): 281-284
DOI: 10.1055/s-2005-916193
Letter
© Georg Thieme Verlag KG Stuttgart · New York

Gambogic Acid and Epigambogic Acid, C-2 Epimers with Novel Anticancer Effects from Garcinia hanburyi

Quanbin Han1 , Ling Yang2 , Yong Liu2 , Yulin Wang2 , Chunfeng Qiao1 , Jingzheng Song1 , Lijia Xu3 , Dajian Yang3 , Shilin Chen3 , Hongxi Xu1
  • 1Chinese Medicine Laboratory, Hong Kong Jockey Club Institute of Chinese Medicine, Shatin, N.T., Hong Kong, P. R. China
  • 2Laboratory of Pharmaceutical Resources Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian, P. R. China
  • 3Department of Applied Biology & Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong
Further Information

Publication History

Received: July 13, 2005

Accepted: August 18, 2005

Publication Date:
05 December 2005 (online)

Abstract

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 μM for K562/R and 0.66 μM for K562/S), epimers 1 and 2 exhibited similar activities against both cell lines (IC50 = 1.32 and 0.89 μM for 1, IC50 = 1.11 and 0.86 μM 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.

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Dr. Hongxi Xu

Hong Kong Jockey Club Institute of Chinese Medicine

Shatin

N.T.

Hong Kong

People’s Republic of China

Fax: +852-2603-6263

Email: xuhongxi@hkjcicm.org