Publication in refereed journal
香港中文大学研究人员 ( 现职)
| 郑彦铭教授 (内科及药物治疗学系) |
| 郑彦铭教授 (内科及药物治疗学系) |
| 徐宗宪博士 (肿瘤学系) |
| 郭汉龙博士 (生物医学学院) |
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Web of Sciencehttp://aims.cuhk.edu.hk/converis/portal/Publication/18WOS source URL
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摘要Cantharidin isolated from Mylabris caraganae and other insects has been used as an anti-cancer drug in China for many years. However, its toxicity on the renal system and suppression effect on bone marrow limits its usage clinically. Based on the core structure of cantharidin, we have chemically synthesized two cantharidin analogues (compounds 2 and 3). The cytotoxic activity of these analogues was demonstrated on the Hep3B hepatocellular carcinoma, MDA-MB231 breast cancer, A549 non-small cell lung carcinoma and KG1a acute myelogenous leukaemia (AML) cell lines by monitoring the intracellular adenosine triphosphate level. Morphological changes in these cancer cell lines, including cell shrinkage and loss of adherent potential, were readily observed. By making use of the KG I a AML cells as a test model, we further found that mitochondrial membrane potential depolarization and reduction of intracellular bcl-2 anti-apoptotic protein level were involved. These resulted in the activation of caspase 3 protease activity and oligonucleosomal length DNA fragment formation as detected by both time resolved fluorescence technology-based caspase activity assay and TdT-mediated dUTP nick end-labelling assay.
着者Kok SHL, Chui CH, Lam WS, Chen J, Tang JCO, Lau FY, Cheng GYM, Wong RSM, Chan ASC
期刊名称International Journal of Molecular Medicine
出版年份2006
月份1
日期1
卷号17
期次1
出版社PROFESSOR D A SPANDIDOS
页次151 - 157
国际标準期刊号1107-3756
电子国际标準期刊号1791-244X
语言英式英语
关键词apoptosis; cantharidin; carcinoma
Web of Science 学科类别Medicine, Research & Experimental; MEDICINE, RESEARCH & EXPERIMENTAL; Research & Experimental Medicine
