Synthesis of asiatic acid derivatives and determination of their anti-tumor activities
10.11665/j.issn.1000-5048.2024051002
- VernacularTitle:积雪草酸衍生物的合成及抗肿瘤活性测定
- Author:
Guo CHEN
1
;
Liming LIU
;
Tongtong GU
;
Yanqiu MENG
Author Information
1. 沈阳化工大学制药工程教研室, 沈阳 110142
- Publication Type:Journal Article 期刊文章
- Keywords:
asiatic acid derivatives;
structural modification;
anti-tumor activity;
synthesis
- From:
Journal of China Pharmaceutical University
2025;56(4):453-459
- CountryChina
- Language:Chinese
-
Abstract:
Twelve derivatives of asiatic acid were synthesized through acylation, alkylation, oxidative dehydrogenation and other reactions using asiatic acid from usoxane-type pentacyclic triterpenoids as the parent compound. Their structures were confirmed by 1H NMR and 13C NMR, and determined to be novel compounds never reported in literature. Through the MTT method, high-expression human cancer cells (A549 and SGC-7901) were selected for a preliminary in vitro anti-tumor activity study on these compounds. Among them, the IC50 of compound I1 were 11.39 and 9.08 μmol/L respectively, and those of compound I2 were 12.64 and 9.15 μmol/L respectively, which were close to those of sorafenib, a common drug for clinical use. The experimental results show that the synthesized asiatic acid derivatives have certain anti-proliferative effects on the two types of human cancer cells, A549 and SGC-7901, significantly higher than those of asiatic acid. Compounds I1 and I2 show quite strong anti-proliferative effects on human cancer cells A549 and SGC-7901.
