Apoptosis-Inducing Effects of Two Anthraquinones from Hedyotis diffusa WILLD

• Published in: Biological & Pharmaceutical Bulletin Vol. 31; no. 6; pp. 1075 - 1078
• Main Authors: Gong, Xing-Guo, Wang, Chen-Hui, Shi, Ying
• Format: Journal Article
• Language: English
• Published: Japan The Pharmaceutical Society of Japan 01.06.2008; Pharmaceutical Society of Japan; Japan Science and Technology Agency
• Subjects: Annexin A5; anthraquinone; Anthraquinones - pharmacology; Antineoplastic Agents, Phytogenic; apoptosis; Apoptosis - drug effects; Bisbenzimidazole; c-src protein tyrosine kinase; Caspase 3 - metabolism; caspase-3; Cell Line, Tumor; Cell Proliferation - drug effects; Cell Survival - drug effects; Coloring Agents; Fluorescein-5-isothiocyanate - analogs & derivatives; Fluorescent Dyes; Hedyotis - chemistry; Hedyotis diffusa; Humans; Magnetic Resonance Spectroscopy; Mass Spectrometry; Membrane Potentials - drug effects; mitochondrial membrane potential; Mitochondrial Membranes - drug effects; Rhodamine 123; Spectrophotometry, Infrared; Spectrophotometry, Ultraviolet; src-Family Kinases - antagonists & inhibitors; Tetrazolium Salts; Thiazoles
• ISSN: 0918-6158; 1347-5215
• DOI: 10.1248/bpb.31.1075

Two anthraquinones which inhibit activity of the Src tyrosine kinase were isolated from a water extract of Hedyotis diffusa WILLD. and identified as 2-hydroxy-3-methylanthraquinone (compound 1) and 1-methoxy-2-hydroxyanthraquinone (compound 2). Both compounds showed inhibitory activity against protein tyrosine kinases v-src and pp60src and arrested the growth of SPC-1-A, Bcap37 and HepG2 cancer cells. Observation of mitochondrial membrane potential collapse and caspase-3 activation following treatment with the compounds indicates that their apoptotic induction activity may act via the mitochondrial apoptotic pathway. Compared with compound 2, compound 1 is more active as an antagonist of Src kinase, which might account for its higher potency to induce growth arrest and apoptosis. These results provide a deeper insight into the functions of these two simple anthraquinones and the anti-tumour pathway of Hedyotis diffusa WILLD.