Antibacterial and Anticancer Activity, Acute Toxicity, and Solubility of Co-crystals of 5-Fluorouracil and Trimethoprim

被引：6
|
作者：
Yan, Tianping [1 ]
Shu, Baoyu [1 ]
Deng, Xuezhen [1 ]
Qian, Kun [1 ]
Pan, Rongbin [2 ]
Qiu, ShouLiang [1 ]
Yang, Jie [1 ]
Fu, Qingxia [1 ]
Ma, Yuexing [3 ]
机构：
[1] Jiangxi Univ Chinese Med, Coll Pharm, Nanchang 330006, Peoples R China
[2] Jiangxi Univ Chinese Med, Integrated Chinese & Western Med Oncol Res Ctr, Nanchang 330006, Peoples R China
[3] Jiangxi Univ Tradit Chinese Med, Sci & Technol Coll, Nanchang 330004, Peoples R China
来源：
ACS OMEGA | 2023年 / 8卷 / 24期
基金：
中国国家自然科学基金;
关键词：
PHARMACEUTICAL COCRYSTALS;
D O I：
10.1021/acsomega.3c00580
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
5-Fluorouracil ismainly used for the treatment of tumorsand hasrelatively high toxicity. Trimethoprim is a common broad-spectrumantibiotic agent with extremely poor water solubility. We hoped tosolve these problems by synthesizing co-crystals (compound 1) of 5-fluorouracil and trimethoprim. Solubility tests showed thatthe solubility of compound 1 was improved compared tothat of trimethoprim. In vitro anticancer activity tests of compound 1 showed higher activity against human breast cancer cellsthan 5-fluorouracil. Acute toxicity showed that its toxicity was muchlower than that of 5-fluorouracil. In the test of anti-Shigella dysenteriae activity, compound 1 showed much stronger antibacterial activity than trimethoprim.
引用
收藏
页码：21522 / 21530
页数：9
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