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

[Image: see text] 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...

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Autores principales: Yan, Tianping, Shu, Baoyu, Deng, Xuezhen, Qian, Kun, Pan, Rongbin, Qiu, ShouLiang, Yang, Jie, Fu, Qingxia, Ma, Yuexing
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2023
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10286293/
https://www.ncbi.nlm.nih.gov/pubmed/37360497
http://dx.doi.org/10.1021/acsomega.3c00580
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author Yan, Tianping
Shu, Baoyu
Deng, Xuezhen
Qian, Kun
Pan, Rongbin
Qiu, ShouLiang
Yang, Jie
Fu, Qingxia
Ma, Yuexing
author_facet Yan, Tianping
Shu, Baoyu
Deng, Xuezhen
Qian, Kun
Pan, Rongbin
Qiu, ShouLiang
Yang, Jie
Fu, Qingxia
Ma, Yuexing
author_sort Yan, Tianping
collection PubMed
description [Image: see text] 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.
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spelling pubmed-102862932023-06-23 Antibacterial and Anticancer Activity, Acute Toxicity, and Solubility of Co-crystals of 5-Fluorouracil and Trimethoprim Yan, Tianping Shu, Baoyu Deng, Xuezhen Qian, Kun Pan, Rongbin Qiu, ShouLiang Yang, Jie Fu, Qingxia Ma, Yuexing ACS Omega [Image: see text] 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. American Chemical Society 2023-06-06 /pmc/articles/PMC10286293/ /pubmed/37360497 http://dx.doi.org/10.1021/acsomega.3c00580 Text en © 2023 The Authors. Published by American Chemical Society https://creativecommons.org/licenses/by-nc-nd/4.0/Permits non-commercial access and re-use, provided that author attribution and integrity are maintained; but does not permit creation of adaptations or other derivative works (https://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Yan, Tianping
Shu, Baoyu
Deng, Xuezhen
Qian, Kun
Pan, Rongbin
Qiu, ShouLiang
Yang, Jie
Fu, Qingxia
Ma, Yuexing
Antibacterial and Anticancer Activity, Acute Toxicity, and Solubility of Co-crystals of 5-Fluorouracil and Trimethoprim
title Antibacterial and Anticancer Activity, Acute Toxicity, and Solubility of Co-crystals of 5-Fluorouracil and Trimethoprim
title_full Antibacterial and Anticancer Activity, Acute Toxicity, and Solubility of Co-crystals of 5-Fluorouracil and Trimethoprim
title_fullStr Antibacterial and Anticancer Activity, Acute Toxicity, and Solubility of Co-crystals of 5-Fluorouracil and Trimethoprim
title_full_unstemmed Antibacterial and Anticancer Activity, Acute Toxicity, and Solubility of Co-crystals of 5-Fluorouracil and Trimethoprim
title_short Antibacterial and Anticancer Activity, Acute Toxicity, and Solubility of Co-crystals of 5-Fluorouracil and Trimethoprim
title_sort antibacterial and anticancer activity, acute toxicity, and solubility of co-crystals of 5-fluorouracil and trimethoprim
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10286293/
https://www.ncbi.nlm.nih.gov/pubmed/37360497
http://dx.doi.org/10.1021/acsomega.3c00580
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