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Mechanistic insight into a novel synthetic cantharidin analogue in a leukaemia model (2006)_香港中文大学

香港中文大学 辅仁网/2017-06-27

Mechanistic insight into a novel synthetic cantharidin analogue in a leukaemia model
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/11WOS source URL

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摘要Cantharidin isolated from Mylabris caraganae and other insects is used traditionally as an anti-cancer drug especially on hepatoma and leukaemia. Previously, we demonstrated that the novel synthetic cantharidin analogue CAN 032 possessed apoptotic activity on two human hepatoma cell lines Hep3B hepatocellular carcinoma and SK-Hep-1 liver adenocarcinoma. However, its underlying mechanistic action on cancer cells remained unclear. Herein, we furthered our work by making use of KG1a acute myelogenous leukaemia (AML) and K562 chronic myelogenous leukaemia (CML) as experimental models. As anticipated, both leukaemia cell lines were;sensitive to the cytotoxic action of CAN 032. The activity of CAN 032 was both dose- and time-course-dependent. CAN 032 readily inhibited the colony formation potential of both leukaemia cell lines. KG1a AML treated with CAN032 decreased G1 phase cell population, mitochondrial membrane potential collapse, caspase 3 activation and hence DNA fragmentation. Pre-incubation of leukaemia cells with the general caspase inhibitor Z-VAD-FMK could partially reversed the apoptotic action of CAN 032. This result suggested that the caspase-dependent pathway is necessary for the apoptotic action of CAN 032. CAN 032 provides a new direction for novel drug discovery in experimental cancer therapy.

着者Kok SHL, Chui CH, Lam WS, Chen J, Lau FY, Wong RSM, Cheng GYM, Tang WK, Cheng CH, Tang JCO, Chan ASC
期刊名称International Journal of Molecular Medicine
出版年份2006
月份8
日期1
卷号18
期次2
出版社PROFESSOR D A SPANDIDOS
页次375 - 379
国际标準期刊号http://aims.cuhk.edu.hk/converis/portal/Publication/1107-3756
电子国际标準期刊号1791-244X
语言英式英语

关键词cantharidin; caspase; leukaemia
Web of Science 学科类别Medicine, Research & Experimental; MEDICINE, RESEARCH & EXPERIMENTAL; Research & Experimental Medicine

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