Synthesis, characterization and antitumor activity of 5-fluorouracil-nicotinamide cocrystal.
- Author:
Wu MIN
1
;
Xingang LIU
1
;
Yu XUE
1
;
Qi CHEN
1
;
Hu XIURONG
2
;
Jun ZHOU
1
;
Guping TANG
3
Author Information
1. Department of Chemistry, Zhejiang University, Hangzhou 310027, China.
2. Department of Chemistry, Zhejiang University, Hangzhou 310027, China. huxiurong@zju.edu.cn.
3. Department of Chemistry, Zhejiang University, Hangzhou 310027, China. tangguping@zju.edu.cn.
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
pharmacology;
Cell Line, Tumor;
Cell Movement;
drug effects;
Cell Survival;
drug effects;
Crystallization;
Fluorouracil;
chemistry;
Humans;
Liver Neoplasms;
Niacinamide;
chemistry;
Solubility
- From:
Journal of Zhejiang University. Medical sciences
2017;46(2):127-133
- CountryChina
- Language:Chinese
-
Abstract:
To synthesize 5-fluorouracil-nicotinamide (5-FU-NCT) cocrystal and to investigate its physicochemical and biological properties. The cocrystal of 5-Fu-NCT was prepared through the cooling technology. PXRD, NMR, FTIR and DSC were used to characterize the structure of 5-FU-NCT cocrystal. Solubility was measured by HPLC method. Drug resistant human liver cancer BEL-7402/5-FU cells were treated with 5-FU-NCT cocrystal, the inhibition effect was tested by MTT and HE staining, and cancer cell migration was determined by scratch test. According to PXRD, NMR, FTIR and DSC results, the cocrystal of 5-Fu-NCT had been synthesized successfully. The characteristic diffraction peaks (2θ/°) of the cocrystal were 16.4, 20.4, 22.3, 27.9 and 30.1. The solubility of 5-FU-NCT was 13.5 g/L as measured by HPLC. The antitumor activity tests showed that 5-FU-NCT cocrystal enhanced anticancer effect of 5-FU, and the IC50 of 5-FU and 5-FU-NCT was 129.6 μg/mL and 42.6 μg/mL, respectively. 5-Fu-NCT cocrystal have been synthesized successfully through the cooling technology and it shows an enhanced anticancer effect in comparison to 5-FU on BEL-7402/5-FU cells.
