秋水仙碱及其 C-10 含硫衍生物的细胞毒性、镇痛和抗炎活性。

Cytotoxic, analgesic and anti-inflammatory activity of colchicine and its C-10 sulfur containing derivatives.

机构信息

Department of Bioactive Products, Faculty of Chemistry, Adam Mickiewicz University, Uniwersytetu Poznańskiego 8, 61-614, Poznan, Poland.

Department of Toxicology, Poznań University of Medical Sciences, Dojazd 30, 60-631, Poznan, Poland.

出版信息

Sci Rep. 2021 Apr 27;11(1):9034. doi: 10.1038/s41598-021-88260-1.

10-Alkylthiocolchicines have been obtained and characterized by spectroscopic methods and their biological activities as: cytotoxic, anti-inflammatory and analgesic activities have been tested. Cytotoxic activity against SKOV-3 ovarian cell line for 10-alkylthiocolchicine analogues was reported and tested compounds showed to be more active than commonly used doxorubicin. Some of tested C-10 alkylthiolated colchicines have been found to exhibit cytotoxicity at levels comparable to that of the natural product-colchicine. 10-Methylthiocolchicine has IC = 8 nM and 10-ethylthiocolchicine has IC = 47 nM in comparison to colchicine IC = 37 nM. Moreover for 10-alkylthioderivatives apoptosis test, cyclin B1 and cell cycle tests were performed. 10-n-Butylthiocolchicine was tested for anti-inflammatory and analgesic activities it showed to produce analgesic rather than anti-inflammatory effect.

10-烷基硫代秋水仙碱已通过光谱方法获得和表征，并对其生物活性进行了测试，包括细胞毒性、抗炎和镇痛活性。报道了对 SKOV-3 卵巢癌细胞系的 10-烷基硫代秋水仙碱类似物的细胞毒性活性，测试化合物比常用的多柔比星更具活性。一些测试的 C-10 烷基硫代秋水仙碱已被发现具有与天然产物秋水仙碱相当的细胞毒性。与秋水仙碱的 IC=37 nM 相比，10-甲基硫代秋水仙碱的 IC=8 nM，10-乙基硫代秋水仙碱的 IC=47 nM。此外，还对 10-烷基硫代秋水仙碱进行了细胞凋亡试验、细胞周期 B1 和细胞周期试验。测试了 10-正丁基硫代秋水仙碱的抗炎和镇痛活性，结果表明它具有镇痛作用而不是抗炎作用。