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
相关论文
共 50 条
  • [21] Structural, spectral, theoretical and anticancer studies on new co-crystal of the drug 5-fluorouracil
    Kumar, S. Suresh
    Athimoolam, S.
    Sridhar, B.
    JOURNAL OF MOLECULAR STRUCTURE, 2018, 1173 : 951 - 958
  • [22] REDUCTION OF 5-FLUOROURACIL TOXICITY IN MAN WITH RETENTION OF ANTICANCER EFFECTS BY PROLONGED INTRAVENOUS ADMINISTRATION IN 5-PERCENT DEXTROSE
    LEMON, HM
    CANCER CHEMOTHERAPY REPORTS, 1960, (08): : 97 - 101
  • [23] Relationship between 5-fluorouracil disposition, toxicity and dihydropyrimidine dehydrogenase activity in cancer patients
    Di Paolo, A
    Danesi, R
    Falcone, A
    Cionini, L
    Vannozzi, F
    Masi, G
    Allegrini, G
    Mini, E
    Bocci, G
    Conte, PF
    Del Tacca, M
    ANNALS OF ONCOLOGY, 2001, 12 (09) : 1301 - 1306
  • [24] THE INFLUENCE OF AMINAZINE AND PHENAZEPAM ON TOXICITY AND ANTI-TUMOR ACTIVITY OF FTORAFUR AND 5-FLUOROURACIL
    SUSLOV, NI
    MIKHAILOVA, LM
    EKSPERIMENTALNAYA ONKOLOGIYA, 1983, 5 (02): : 70 - 73
  • [25] Folylpolyglutamate synthase and γ-glutamyl hydrolase regulate leucovorin-enhanced 5-fluorouracil anticancer activity
    Sakamoto, Etsuko
    Tsukioka, Sayaka
    Oie, Shinji
    Kobunai, Takashi
    Tsujimoto, Hiroaki
    Sakamoto, Kazuki
    Okayama, Yoshihiro
    Sugimoto, Yoshikazu
    Oka, Toshinori
    Fukushima, Masakazu
    Oka, Tatsuzo
    BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2008, 365 (04) : 801 - 807
  • [26] Chitosan mediated 5-Fluorouracil functionalized silica nanoparticle from rice husk for anticancer activity
    Dhinasekaran, Durgalakshmi
    Raj, Rishvanth
    Rajendran, Ajay Rakkesh
    Purushothaman, Bargavi
    Subramanian, Balakumar
    Prakasarao, Aruna
    Singaravelu, Ganesan
    INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES, 2020, 156 : 969 - 980
  • [27] The Potential Anticancer Activity of 5-Fluorouracil Loaded in Cellulose Fibers Isolated from Rice Straw
    Yusefi, Mostafa
    Shameli, Kamyar
    Jahangirian, Hossein
    Teow, Sin-Yeang
    Umakoshi, Hiroshi
    Saleh, Bahram
    Rafiee-moghaddam, Roshanak
    Webster, Thomas J.
    INTERNATIONAL JOURNAL OF NANOMEDICINE, 2020, 15 : 5417 - 5432
  • [28] Synergistic Role of Thymoquinone on Anticancer Activity of 5-Fluorouracil in Triple Negative Breast Cancer Cells
    Zheng, Meiling
    Mei, Zhiqiang
    Junaid, Md
    Tania, Mousumi
    Fu, Junjiang
    Chen, Han-Chun
    Khan, Md Asaduzzaman
    ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY, 2022, 22 (06) : 1111 - 1118
  • [29] Vitamin D analogs enhance the anticancer activity of 5-fluorouracil in an in vivomouse colon cancer model
    Magdalena Milczarek
    Mateusz Psurski
    Andrzej Kutner
    Joanna Wietrzyk
    BMC Cancer, 13
  • [30] Prolonged exposure of colon cancer cells to 5-fluorouracil nanoparticles improves its anticancer activity
    Tawfik, Essam
    Ahamed, Maqusood
    Almalik, Abdulaziz
    Alfaqeeh, Mohammad
    Alshamsan, Aws
    SAUDI PHARMACEUTICAL JOURNAL, 2017, 25 (02) : 206 - 213
12345