The anti-ZIKA virus activity of tenofovir disoproxil fumarate in vitro
10.16438/j.0513-4870.2018-1135
- VernacularTitle:富马酸替诺福韦二吡呋酯体外抗寨卡病毒活性研究
- Author:
Xiu-xiu CHEN
1
,
2
,
3
;
Rong-hua LUO
4
;
Chang-bo ZHENG
5
;
Zhai-wen YAO
1
,
2
,
3
;
Qiu-ju TANG
5
;
Si-dong XIONG
6
;
Yong-tang ZHENG
3
,
4
Author Information
1. College of Pharmacy, Soochow University, Suzhou 215021, China
2. Key Laboratory of Bioactive Peptides of Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China
3. KIZ-SU Joint Laboratory of Animal Model and Drug Development, College of Pharmaceutical Sciences, Soochow University, Suzhou 215021, China
4. Key Laboratory of Bioactive Peptides of Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China
5. School of Pharmaceutical Science and Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming 650500, China
6. KIZ-SU Joint Laboratory of Animal Model and Drug Development, College of Pharmaceutical Sciences, Soochow University, Suzhou 215021, China
- Publication Type:Research Article
- Keywords:
tenofovir disoproxil fumarate;
nucleoside analogue;
Zika virus;
antiviral activity;
therapy
- From:
Acta Pharmaceutica Sinica
2019;54(9):1582-1587
- CountryChina
- Language:Chinese
-
Abstract:
Tenofovir disoproxil fumarate (TDF) is a nucleoside analogue that has been widely used for clinical treatment of human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infection. The aim of this study was to investigate whether TDF has anti-Zika virus (ZIKV) activity in vitro. The inhibitory effect of TDF on ZIKV was detected by plaque reduction assay. Then, the anti-ZIKV activity of TDF at RNA level and protein level was verified by real time quantitative PCR and Western blot. Finally, MTT assay was used to determine the cytotoxicity of TDF. Our results showed that TDF not only reduced the formation of plaque after ZIKV infection, but also inhibited the replication of ZIKV RNA or expression of ZIKV NS2B protein. The 50% effective concentration (EC50) of TDF in inhibition of ZIKV replication were 14.96-27.47 μmol·L-1, while that of ribavirin was 56.01 ± 12.16 μmol·L-1, which served as the positive control. The cytotoxicity of TDF and ribavirin in Vero cells were very low, with their 50% cytotoxic concentration (CC50) values being greater than 500 μmol·L-1. The therapeutic index of TDF calculated by CC50/EC50 was greater than 18.20, which was significantly higher than that of ribavirin. The results suggest that TDF has good anti-ZIKV activity in vitro and is expected to become a candidate drug for anti-ZIKV therapy.
