The anti-HIV-1 activities of benzophenones non-nucleoside reverse transcriptase inhibitors in vitro
10.16438/j.0513-4870.2016-0598
- VernacularTitle:二甲苯酮类非核苷类逆转录酶抑制剂的体外抗HIV-1活性
- Author:
Ping WANG
1
;
Gao-hong ZHANG
1
;
Si-ying XIANG
1
;
Liu-meng YANG
1
;
Cheng-run TANG
1
;
Xiao-dong MA
2
;
Yong-tang ZHENG
3
Author Information
1. Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Science and Yunnan Province, Kun-ming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China
2. College of Pharmacy, Dalian Medical University, Dalian 116044, China
3. School of Pharmaceutical Science and Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming 650500, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
non-nucleoside reverse transcriptase inhibitor;
HIV-1;
laboratory-adapted strain;
drug-resistant strain;
primary isolated strain;
anti-HIV-1 activity
- From:
Acta Pharmaceutica Sinica
2016;51(11):1704-
- CountryChina
- Language:Chinese
-
Abstract:
To evaluate the anti-HIV-1 activities of 5 benzophenones non-nucleoside reverse transcriptase inhibitors (NNRTIs) such as DY1203, DY1204, DY1119, DY1208 and DY1209 in vitro, the cytotoxicity of 5 compounds were tested on C8166, MT-4, H9 and PBMC with the MTT assay. The anti-HIV-1 activities of compounds were evaluated on laboratory-adapted strain, drug-resistant strains and primary isolated strains by p24 antigen expression ELISA. The inhibition of HIV-1 recombinant reverse transcriptase activity was assessed by ELISA assay. Among 5 compounds, DY1203 and DY1204 showed low cytotoxicities with CC50 greater than 200 μg·mL-1. DY1119, DY1208 and DY1209 showed strong anti-HIV-1 activities against HIV-1IIIB, HIV-174V, HIV-1RF/V82F/184V, HIV-1NL4-3 gp41(36G) N42S, HIV-1KM018, HIV-1TC-1 and HIV-1Wan. However, NNRTIs drug-resistant strain HIV-1A17 showed different resistance to these compounds. The 5 compounds proved active against HIV-1 recombinant reverse transcriptase. DY1208 is expected to become a new lead compound for its high therapeutic index. The results can provide new information for HIV-1 drug research and promote the development of new HIV-1 drugs.
