TY  - JOUR
N1  - FELTÖLT?: Kiss Tivadar kiss.tivadar@pharmacognosy.hu
UR  - http://publicatio.bibl.u-szeged.hu/14980/
EP  - 6 p
SP  - Paper 1064793
ID  - publicatio14980
AV  - public
TI  - Flavonol 7-O-Glucoside Herbacitrin Inhibits HIV-1 Replication through Simultaneous Integrase and Reverse Transcriptase Inhibition
Y1  - 2019///
A1  -  Áy Eva
A1  -  Hunyadi Attila
A1  -  Mezei Mária
A1  -  Minárovits János
A1  -  Hohmann Judit
VL  - 2019
SN  - 1741-427X
JF  - EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE
N2  - 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 (CC50=27.8 and 63.64 ?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 ?M, while it was a more potent integrase inhibitor already active at 2.15 ?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.
ER  -