Design, Preparation and Studies Regarding Cytotoxic Properties of Glycyrrhetinic Acid Derivatives

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...

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Bibliographic Details
Published in:Biological & pharmaceutical bulletin 2020/01/01, Vol.43(1), pp.102-109
Main Authors: Zheng, Qing-Xuan, Wang, Rui, Xu, Yan, He, Chang-Xin, Zhao, Cai-Yun, Wang, Zhi-Fang, Zhang, Rui, Dehaen, Wim, Li, Hui-Jing, Huai, Qi-Yong
Format: Article
Language:English
Subjects:
Antitumor activity
Apoptosis
Breast cancer
Cervical cancer
Cervix
Cytotoxicity
Doxorubicin
Gefitinib
glycyrrhetinic acid
MDA-MB-231
Natural products
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Summary: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.
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.b19-00615