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

5-Fluorouracil is mainly used for the treatment of tumors and has relatively high toxicity. Trimethoprim is a common broad-spectrum antibiotic agent with extremely poor water solubility. We hoped to solve these problems by synthesizing co-crystals (compound 1) of 5-fluorouracil and trimethoprim. Solubility tests showed that the solubility of compound 1 was improved compared to that of trimethoprim. In vitro anticancer activity tests of compound 1 showed higher activity against human breast cancer cells than 5-fluorouracil. Acute toxicity showed that its toxicity was much lower than that of 5-fluorouracil. In the test of anti-Shigella dysenteriae activity, compound 1 showed much stronger antibacterial activity than trimethoprim.5-氟尿嘧啶（5-Fluorouracil）主要用于肿瘤治疗，但其毒性相对较高。甲氧苄啶（Trimethoprim）为常用广谱抗菌药物，水溶性极差。本研究旨在通过合成5-氟尿嘧啶与甲氧苄啶的共晶（化合物1）以解决上述问题。溶解度测试结果显示，化合物1的溶解度较甲氧苄啶有所提升。体外抗癌活性测试表明，化合物1对人乳腺癌细胞的活性优于5-氟尿嘧啶。急性毒性实验证实，其毒性远低于5-氟尿嘧啶。在抗痢疾志贺菌（Shigella dysenteriae）活性测试中，化合物1的抗菌活性远强于甲氧苄啶。