Design, Preparation and Studies Regarding Cytotoxic Properties of Glycyrrhetinic Acid Derivatives
作者:Qing-Xuan Zheng、Rui Wang、Yan Xu、Chang-Xin He、Cai-Yun Zhao、Zhi-Fang Wang、Rui Zhang、Wim Dehaen、Hui-Jing Li、Qi-Yong Huai
DOI:10.1248/bpb.b19-00615
日期:2020.1.1
Glycyrrhetinic acid (GA) is a natural product with certain antitumor activity. In order to enhance the cytotoxicity, a total of eighteen derivatives of GA were designed and synthesized. Their cytotoxicity against MDA-MB-231cells (human breast cancer cells) and HeLa cells (human cervical cancer cells), were evaluated by the MTT method (3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide).
甘草次酸(GA)是一种具有一定抗肿瘤活性的天然产物。为了增强细胞毒性,设计并合成了总共18种GA衍生物。通过MTT法(3-(4,5-二甲基噻唑-2-基)-2、5-二苯基四唑鎓)评价了它们对MDA-MB-231细胞(人乳腺癌细胞)和HeLa细胞(人宫颈癌细胞)的细胞毒性。溴化物)。结果表明,这些目标化合物具有较宽的摩尔活性范围,其中一些具有比商品药物吉非替尼和阿霉素更好的活性。化合物6g分别以5、10和20 µM诱导7、10和44%的MDA-MB-231细胞凋亡。