Open AccessFlavonol 7-O-Glucoside Herbacitrin Inhibits HIV-1 Replication through Simultaneous Integrase and Reverse Transcriptase Inhibition
Author(s) -
Éva Áy,
Attila Hunyadi,
Mária Mezei,
János Minárovits,
Judit Hohmann
Publication year - 2019
Publication title -
evidence-based complementary and alternative medicine
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.552
H-Index - 90
eISSN - 1741-4288
pISSN - 1741-427X
DOI - 10.1155/2019/1064793
Subject(s) - integrase , reverse transcriptase , flavonoid , chemistry , integrase inhibitor , viral replication , enzyme , virology , quercetin , biology , human immunodeficiency virus (hiv) , biochemistry , virus , antiretroviral therapy , rna , viral load , gene , antioxidant
Here we report the evaluation of the antiretroviral effect of two flavonoid 7- O -glucosides, herbacitrin ( 1 ) and gossypitrin ( 2 ), together with quercetin ( 3 ), a well-studied flavonol. Antiviral activity of the flavonoids was assessed by analyzing HIV-1 p24 core protein levels in the supernatants of HIV-1 infected MT-4 and MT-2 cell cultures. The compounds showed mild to weak cytotoxic activities on the host cells; herbacitrin was the strongest in this regard (CC 50 =27.8 and 63.64 μ M on MT-4 and MT-2 cells, respectively). In nontoxic concentrations, herbacitrin and quercetin reduced HIV-1 replication, whereas gossypitrin was ineffective. Herbacitrin was found to inhibit reverse transcriptase at 21.5 μ M, while it was a more potent integrase inhibitor already active at 2.15 μ M. Therefore, our observations suggest that herbacitrin exerts antiretroviral activity through simultaneously acting on these two targets of HIV-1 and that integrase inhibition might play a major role in this activity.