Apoptosis-inducing effects of two anthraquinones from Hedyotis diffusa WILLD.
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.
College of Life Sciences, Zhejiang University, Zijinggang Campus, Hangzhou, China. zju.life@yahoo.com.cn
Ying
Y
Shi
Chen-Hui
CH
Wang
Xing-Guo
XG
Gong
D017304:Annexin A5; D000880:Anthraquinones / Q000494:pharmacology*; D000972:Antineoplastic Agents, Phytogenic; D017209:Apoptosis / Q000187:drug effects*; D006690:Bisbenzimidazole; D053148:Caspase 3 / Q000378:metabolism; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004396:Coloring Agents; D016650:Fluorescein-5-isothiocyanate / Q000031:analogs & derivatives; D005456:Fluorescent Dyes; D032064:Hedyotis / Q000737:chemistry*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008564:Membrane Potentials / Q000187:drug effects; D051336:Mitochondrial Membranes / Q000187:drug effects; D000091402:Prohibitins; D020112:Rhodamine 123; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet; D013778:Tetrazolium Salts; D013844:Thiazoles; D019061:src-Family Kinases / Q000037:antagonists & inhibitors
D017304:Annexin A5; D000880:Anthraquinones; D000972:Antineoplastic Agents, Phytogenic; D004396:Coloring Agents; C492760:FITC-annexin A5; D005456:Fluorescent Dyes; C000717331:PHB2 protein, human; D000091402:Prohibitins; D013778:Tetrazolium Salts; D013844:Thiazoles; D020112:Rhodamine 123; D019061:src-Family Kinases; D053148:Caspase 3; C022616:thiazolyl blue; D016650:Fluorescein-5-isothiocyanate; D006690:Bisbenzimidazole