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Planta Med 2014; 80(08/09): 682-687
DOI: 10.1055/s-0034-1368583
Biological and Pharmacological Activity
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Genistein as Antiviral Drug against HIV Ion Channel

Daniel Sauter
1   Shanghai Research Center for Acupuncture & Meridians, Shanghai, China
2   Institute for Biophysics, JW-Goethe-University, Frankfurt a. M., Germany
4   Present address: University of Copenhagen, Copenhagen, Denmark
,
Silvia Schwarz
1   Shanghai Research Center for Acupuncture & Meridians, Shanghai, China
,
Kai Wang
3   Key Laboratory of Molecular Virology & Immunology, Institut Pasteur of Shanghai, Chinese Academy of Sciences, Shanghai, China
,
Ronghua Zhang
3   Key Laboratory of Molecular Virology & Immunology, Institut Pasteur of Shanghai, Chinese Academy of Sciences, Shanghai, China
,
Bing Sun
3   Key Laboratory of Molecular Virology & Immunology, Institut Pasteur of Shanghai, Chinese Academy of Sciences, Shanghai, China
,
Wolfgang Schwarz
1   Shanghai Research Center for Acupuncture & Meridians, Shanghai, China
2   Institute for Biophysics, JW-Goethe-University, Frankfurt a. M., Germany
› Author Affiliations
Further Information

Publication History

received 09 March 2014
revised 14 May 2014

accepted 17 May 2014

Publication Date:
25 June 2014 (online)

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Abstract

Various drugs found in Chinese herbs are well known for their antiviral potency. We have tested several flavonoids with respect to their potency to block the viral protein U of the human immunodeficiency type 1 virus, which is believed to form a cation-permeable ion channel in the infected cell. We used Xenopus oocytes with heterologously expressed viral protein U as model system to test the efficacy of the drugs in voltage-clamp experiments. This method had been demonstrated in the past as a useful tool to screen drugs for their potency in inhibition of ion channel activity. The viral protein U-mediated current could be inhibited by Ba2+ with a K1/2 value of 1.6 mM. Therefore, we determined viral protein U-mediated current as current component blocked by 10 mM Ba2+. We screened several flavonoids with respect to their effects on this current. The flavonols quercetin and kaempferol, and the flavanols (−)epigallochatechin and (−)epichatechin were ineffective. The flavanone naringenin showed at 20 µM slight (about 10 %) inhibition. The most potent drug was the isoflavon genistein which exhibited at 20 µM significant inhibition of about 40 % with a K1/2 value of 81 ± 4 µM. We suggest that viral ion channels, in general, may be a good target for development of antiviral agents, and that, in particular, isoflavons may be candidates for development of drugs targeting viral protein U.

Key words

flavonoids - genistein - HIV-1 - ion channel - virus release
 

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