Synthesis, characterization and antitumor activity of 5-fluorouracil-nicotinamide cocrystal
10.3785/j.issn.1008-9292.2017.04.07
- VernacularTitle:5-氟尿嘧啶—烟酰胺共晶的制备及其抗肿瘤活性研究
- Author:
Min WU
1
;
Xingang LIU
;
Yu XUE
;
Qi CHEN
;
Xiurong HU
;
Jun ZHOU
;
Guping TANG
Author Information
1. 浙江大学化学系
- Keywords:
Technology,pharmaceutical;
Lens,crystalline;
Pharmaceutical preparations/chemistry;
Niacinamide/pharmacology;
Fluorouracil/pharmacology;
Solubility;
Antineoplastic neoplastic/pharmacology
- From:
Journal of Zhejiang University. Medical sciences
2017;46(2):160-166
- CountryChina
- Language:Chinese
-
Abstract:
Objective:To synthesize 5-fluorouracil-nicotinamide (5-FU-NCT) cocrystal and to investigate its physicochemical and biological properties.Methods: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.Results: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.Conclusion:5-Fu-NCT cocrystal have been synthesized successfully through the cooling technology and it shows a more enhanced anticancer effect in comparison to 5-FU on BEL-7402/5-FU cells.
