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
收藏
页码：1174 / 1178
页数：5
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