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Evidence-Based Complementary and Alternative Medicine
Volume 2019, Article ID 1064793, 6 pages
https://doi.org/10.1155/2019/1064793
Research Article

Flavonol 7-O-Glucoside Herbacitrin Inhibits HIV-1 Replication through Simultaneous Integrase and Reverse Transcriptase Inhibition

1National Public Health Institute, Department of Retroviruses, National Reference Laboratory of HIV, 1097 Budapest, Hungary
2Institute of Pharmacognosy, Interdisciplinary Excellence Centre, University of Szeged, 6720 Szeged, Hungary
3Interdisciplinary Centre of Natural Products, University of Szeged, 6720 Szeged, Hungary
4Department of Oral Biology and Experimental Dental Research, Faculty of Dentistry, University of Szeged, 6720 Szeged, Hungary

Correspondence should be addressed to Attila Hunyadi; uh.degezs-u.mrahp@a.idaynuh and Judit Hohmann; uh.degezs-u.mrahp@nnamhoh

Received 1 February 2018; Revised 31 October 2018; Accepted 14 January 2019; Published 3 February 2019

Academic Editor: G. K. Jayaprakasha

Copyright © 2019 Éva Áy et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

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.