%0 Journal Article
%@ 1741-427X
%A  Áy Eva
%A  Hunyadi Attila
%A  Mezei Mária
%A  Minárovits János
%A  Hohmann Judit
%A Természetes Vegyületek Interdiszciplináris Központ SZTE / KE TVIK [2016-],
%A Farmakognóziai Intézet SZTE / GYTK FI [2000-],
%D 2019
%F publicatio:14980
%J EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE
%P Paper 1064793-6 p
%T Flavonol 7-O-Glucoside Herbacitrin Inhibits HIV-1 Replication through Simultaneous Integrase and Reverse Transcriptase Inhibition
%U http://publicatio.bibl.u-szeged.hu/14980/
%V 2019
%X 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 μM 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 μM, while it was a more potent integrase inhibitor already active at 2.15 μM. 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.
%Z FELTÖLTŐ: Kiss Tivadar kiss.tivadar@pharmacognosy.hu