The study of azvudine activity against dengue viruses in vitro
10.16438/j.0513-4870.2018-0245
- VernacularTitle:阿兹夫定体外抗登革病毒活性研究
- Author:
Chun-tao ZHANG
1
;
Rong-hua LUO
2
;
Huan CHEN
2
;
Guang-ming LIU
1
;
Jun-biao CHANG
3
;
Liu-meng YANG
2
;
Yong-tang ZHENG
2
Author Information
1. College of Pharmacy and Chemistry, Dali University, Dali 671000, China
2. Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China
3. Henan Normal University, Xinxiang 453007, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
azvudine;
dengue virus;
antiviral activity;
in vitro
- From:
Acta Pharmaceutica Sinica
2018;53(6):944-949
- CountryChina
- Language:Chinese
-
Abstract:
In this study, azvudine (FNC), hydrochloride salt of azvudine (FNC-HCl) and triphosphate azovudine (FNC-TP) were tested against DENV-Ⅱ recombinant virus (DENV-Ⅱ Luc+). The inhibitory activity of FNC, FNC-HCl and FNC-TP on DENVs were detected by plaque assay. The effect on the expression of DENV-Ⅱ envelope protein E was detected by Western blot; the inhibitory of DENV-Ⅱ viral RNA by compounds was detected by real-time quantitative PCR. MTT assay was used to determine the cytotoxicity of the three compounds on Vero cells. The results showed that FNC, FNC-HCl and FNC-TP inhibited the viral replication by inhibition of renilla luciferase activity of DENV-Ⅱ Luc+. The 50% effective concentration (EC50) of FNC, FNC-HCl and FNC-TP in the inhibition of DENVs replication were from 0.54-25.42 μmol·L-1, while that of ribavirin was 40.78 ±1.02 μmol·L-1 as the positive control. Western blot and real time quantitative PCR results showed that FNC, FNC-HCl and FNC-TP significantly inhibited the expression of DENV-Ⅱ E protein, and the replication of DENV-Ⅱ viral RNA. The 50% cytotoxic concentrations of FNC, FNC-HCl and FNC-TP were all greater than 3 000.00 μmol·L-1. The results suggest that in vitro anti-DENVs activities of FNC, FNC-HCl and FNC-TP are superior to ribavirin, which are expected to become new candidates of anti-DENV drugs.
