甘草次酸衍生物的设计、制备及细胞毒性研究。
Design, Preparation and Studies Regarding Cytotoxic Properties of Glycyrrhetinic Acid Derivatives.
机构信息
Marine College, Shandong University.
Molecular Design and Synthesis, Department of Chemistry, KU Leuven.
出版信息
Biol Pharm Bull. 2020;43(1):102-109. doi: 10.1248/bpb.b19-00615.
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). The results indicated that these target compounds have a wide molar activity range and some of them show better activity than the commercial drugs gefitinib and doxorubicin. Compound 6g induces apoptosis of 7, 10 and 44% of MDA-MB-231 cells at 5, 10, and 20 µM, respectively.
甘草次酸（GA）是一种具有一定抗肿瘤活性的天然产物。为了增强其细胞毒性，设计并合成了总共 18 种 GA 的衍生物。采用 MTT 法（3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四氮唑溴盐）评估它们对 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。结果表明，这些靶化合物具有广泛的摩尔活性范围，其中一些化合物的活性优于商业药物吉非替尼和阿霉素。化合物 6g 在 5、10 和 20μM 时分别诱导 MDA-MB-231 细胞凋亡 7%、10%和 44%。
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