Page 57 - 《中国药科大学学报》2025年第4期

学报
Journal of China Pharmaceutical University 2025, 56(4): 453 − 459 453

·论 文·

积雪草酸衍生物的合成及抗肿瘤活性测定

陈 果，刘黎明，谷彤彤，孟艳秋 *

（沈阳化工大学制药工程教研室, 沈阳 110142）

摘 要 以乌苏烷型五环三萜类化合物积雪草酸为母体，通过酰化、烷基化、氧化脱氢等反应合成了 12 个积雪草酸衍生物，
1
13
其结构通过 H NMR 和 C NMR 确证，确定均为未经文献报道的新型化合物。通过 MTT 法，选用人癌细胞 (A549 和 SGC-7 901)
对这些化合物进行初步的体外抗肿瘤活性研究。其中化合物 I 1 的 IC 5 分别为 11.39 和 9.08 μmol/L，化合物 I 2 的 IC 5 分别
0
0
为 12.64 和 9.15 μmol/L，与临床常用药物索拉非尼接近。实验结果表明，合成的积雪草酸衍生物对两种人癌细胞 (A549 和
SGC-7 901) 具有一定的抗增殖作用且明显高于积雪草酸，其中化合物 I 1 和 II 2 对 A549 和 SGC-7 901 人癌细胞显示的抗增殖
作用较强。
关键词 积雪草酸衍生物；结构修饰；抗肿瘤活性；合成
中图分类号 R914; R965 文献标志码 A 文章编号 1000−5048(2025)04−0453−07
doi：10.11665/j.issn.1000−5048.2024051002

引用本文 陈果，刘黎明，谷彤彤，等. 积雪草酸衍生物的合成及抗肿瘤活性测定 [J]. 中国药科大学学报，2025，56（4）：453 − 459.

Cite this article as: CHEN Guo, LIU Liming, GU Tongtong, et al. Synthesis of asiatic acid derivatives and determination of their anti-tumor
activities[J]. J China Pharm Univ, 2025, 56(4): 453 − 459.

Synthesis of asiatic acid derivatives and determination of their anti-tumor
activities
CHEN Guo, LIU Liming, GU Tongtong, MENG Yanqiu *
Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China

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
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1
compound. Their structures were confirmed by H NMR and C 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
IC of compound I were 11.39 and 9.08 μmol/L respectively, and those of compound I were 12.64 and 9.15
1
50
2
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 I and I 2
1
show quite strong anti-proliferative effects on human cancer cells A549 and SGC-7901.
Key words asiatic acid derivatives; structural modification; anti-tumor activity; synthesis
This study was supported by the National Natural Science Foundation of China (No.82473787); Liaoning Provincial Key Research
and Development project (2019JH2/10300034); and Shenyang Major Scientific and Technological Achievement Transformation
Project (20-203-5-45)

收稿日期 2024-05-10 * 通信作者 Tel：15940588671 E-mail：myq6581@163.com
基金项目 国家自然科学基金项目（No.82473787）；辽宁省重点研发计划项目 (2019JH2/10300034)；沈阳市重大科技成果转化项目
(20-203-5-45)