Publication in refereed journal
香港中文大学研究人员 ( 现职)
| 郑彦铭教授赖宝山教授 (内科及药物治疗学系) |
| (外科学系) |
| 徐宗宪博士 (肿瘤学系) |
| 郭汉龙博士 (生物医学学院) |
| 梁惠棠教授 (肿瘤学系) |
| 郑彦铭教授 (内科及药物治疗学系) |
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Web of Sciencehttp://aims.cuhk.edu.hk/converis/portal/Publication/19WOS source URL
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摘要Cantharidin isolated from Mylabris caraganae and other insects is used traditionally as an anti-cancer drug. However, its toxicity on the renal system and suppression effect on bone marrow limits its clinical usage. Recently, we have synthesized two cantharidin analogues, CAN 029 (compound 2) and CAN 030 (compound 3). Although both showed an apoptotic induction ability on cancer cells, they were still relatively toxic towards non-malignant haematological disordered bone marrow. Based on the principle structure of cantharidin, we have further chemically synthesized another analogue, CAN 032. The cytotoxic activity of this analogue was screened on both Hep3B hepatocellular carcinoma and SK-Hep-1 liver adenocarcinoma cell lines by [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)2-(4-sulfophenyl)-2H-tetrazolium] (MTS) assay. Morphological changes of hepatoma cell lines were recorded under an inverted microscope. The possible tolerance of these analogues was further investigated using non-malignant haematological bone marrow primary culture. CAN 032 showed a significant cytotoxic response on both hepatoma cell lines in which the potencies were comparable to that of cantharidin. Further screening on the bone marrow tolerance revealed that compound CAN 032 showed a relatively less toxic effect. Phase contrast microscopy demonstrated that cell shrinkage, rounding, loss of adherent property and loss of colony-formation ability were induced. The dose-dependence of the response of CAN 032 on Hep3B was further assayed by DNA fragmentation gel electrophoresis. The G, peak of Hep3B cells was reduced. Chemically synthesized CAN 032 may provide an improved therapeutic advantage over traditional cantharidin.
着者Kok SHL, Chui CH, Lam WS, Chen J, Lau FY, Cheng GYM, Wong RSM, Lai PPS, Leung TWT, Tang JCO, Chan ASC
期刊名称International Journal of Molecular Medicine
出版年份2006
月份5
日期1
卷号17
期次5
出版社PROFESSOR D A SPANDIDOS
页次945 - 949
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; hepatoma
Web of Science 学科类别Medicine, Research & Experimental; MEDICINE, RESEARCH & EXPERIMENTAL; Research & Experimental Medicine
