Design, Preparation and Studies Regarding Cytotoxic Properties of Benzyl Oleanates

被引：0

作者：

Zheng, Qing-Xuan ^{[1
]}

Wang, Rui ^{[2
]}

Li, Hui-Jing ^{[3
]}

Dehaen, Wim ^{[2
]}

Huai, Qi-Yong ^{[1
]}

机构：

[1] Shandong Univ, Marine Coll, Weihai 264209, Peoples R China

[2] Katholieke Univ Leuven, Dept Chem, Sustainable Chem Met & Mol, Celestijnenlaan 200F, B-3001 Leuven, Belgium

[3] Harbin Inst Technol Weihai, Sch Marine Sci & Technol, Weihai 264209, Peoples R China

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2023年 / 57卷 / 08期

基金：

中国国家自然科学基金;

关键词：

oleanolic acid; cytotoxicity; apoptosis; OLEANOLIC ACID; DERIVATIVES;

D O I：

10.1007/s11094-024-03023-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Oleanolic acid (OA) is a natural product with certain antitumor activity. In order to enhance its cytotoxicity, a total of five derivatives of OA were designed and synthesized. Their cytotoxicity against MDA-MB-231cells (human breast cancer cells), A549 cells (human nonsmall cell lung cancer cells) and BEAS-2B cells (human cervical cancer cells) were evaluated by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method. The results indicated that these target compounds have a wide molar activity range and some of them showed better activity than the commercial drug, doxorubicin. Compound 2a induces apoptosis of 14, 27, and 56% of MDA-MB-231 cells at 2, 4, and 8 mM respectively, and shows a linear correlation of concentration.

引用

页码：1174 / 1178

页数：5

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