Gambogic acid and epigambogic acid, C-2 epimers with novel anticancer effects from Garcinia hanburyi

Quanbin Han, Ling Yang, Yong Liu, Yulin Wang, Chunfeng Qiao, Jingzheng Song, Lijia Xu, Dajian Yang, Shilin Chen, Hongxi Xu*

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

58 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)281-284
Number of pages4
JournalPlanta Medica
Issue number3
Publication statusPublished - Jan 2006

Scopus Subject Areas

  • Analytical Chemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine
  • Organic Chemistry


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