Coralyne chloride 是一种具有强抗癌活性的原小檗碱化合物。Coralyne chloride 可以作为一种有效的拓扑异构酶 I (topoisomerase I) 毒性分子，诱导拓扑异构酶 I 介导 DNA 裂解。Coralyne chloride 可用于制备 Coralyne 衍生物，并可以用作 DNA 结合荧光探针制备。
Coralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomerase I poison and induces Top I mediated DNA cleavage[2]. Coralyne chloride can be used for preparing coralyne derivatives as DNA binding fluorescent probes[3].
Coralyne (6.25-100 μM; 24-72 hours) has cytotoxicity effect on breast cancer cell lines. It against MCF-7, MDA-MB-231 and MCF-10A cells with IC50s of 76.4 uM, 76.4 uM, and 99 uM,respectively at 24 hours. And it against MCF-7, MDA-MB-231 and MCF-10A cells with IC50s of 21.9 uM, 19.1 uM, and 91 μM, respectively at 72 hours[1].Coralyne (25 μM; 48 hours) significantly downregulates cancer cell attachment of MCF-7 and MDA-MB-231 compared to the untreated controls. The percent of reduction in adhesion of MCF-7 is 55%, whereas 53% in reduction in the adhesion of MDA-MB-23 and 62% in reduction of MCF-10A,respectively[1].
参考文献:
[1]. Seema Kumari, et al. Synergistic effects of coralyne and paclitaxel on cell migration and proliferation of breast cancer cells lines. Biomed Pharmacother. 2017 Jul;91:436-445.
[2]. D Makhey, et al. Coralyne and related compounds as mammalian topoisomerase I and topoisomerase II poisons. Bioorg Med Chem. 1996 Jun;4(6):781-91.
[3]. P M Pithan, et al. 8-Styryl-substituted coralyne derivatives as DNA binding fluorescent probes.RSC Adv. 2017 Feb 8;7(18):10660-10667.
动态评分
0.0