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

  • Evid Based Complement Alternat Med. 2019 Feb 3:2019:1064793. doi: 10.1155/2019/1064793.
Éva Áy  1 ,  Attila Hunyadi  2  3 ,  Mária Mezei  1 ,  János Minárovits  4 ,  Judit Hohmann  2  3
Affiliations
  • 1. National Public Health Institute, Department of Retroviruses, National Reference Laboratory of HIV, 1097 Budapest, Hungary.
  • 2. Institute of Pharmacognosy, Interdisciplinary Excellence Centre, University of Szeged, 6720 Szeged, Hungary.
  • 3. Interdisciplinary Centre of Natural Products, University of Szeged, 6720 Szeged, Hungary.
  • 4. Department of Oral Biology and Experimental Dental Research, Faculty of Dentistry, University of Szeged, 6720 Szeged, Hungary.
PMID: 30853999 DOI: 10.1155/2019/1064793
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.

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