The root extract of the medicinal plant Pelargonium sidoides is a potent HIV-1 attachment inhibitor

PLoS ONE

Volume 9, Issue 1, 29 January 2014, Article number e87487

The root extract of the medicinal plant Pelargonium sidoides is a potent HIV-1 attachment inhibitor  (Article)

Helfer, M.^a, 

Koppensteiner, H.^a, 

Schneider, M.^a, 

Rebensburg, S.^a, 

Forcisi, S.^b, 

Müller, C.^b, 

Schmitt-Kopplin, P.^b, 

Schindler, M.^a, 

Brack-Werner, R.^a 

^a  Institute of Virology, Helmholtz Zentrum München - German Research Center for Environmental Health, Neuherberg, Germany
^b  Research Unit Analytical BioGeoChemistry, Helmholtz Zentrum München - German Research Center for Environmental Health, Neuherberg, Germany

View references (48)

Abstract

Global HIV-1 treatment would benefit greatly from safe herbal medicines with scientifically validated novel anti-HIV-1 activities. The root extract from the medicinal plant Pelargonium sidoides (PS) is licensed in Germany as the herbal medicine EPsH7630, with numerous clinical trials supporting its safety in humans. Here we provide evidence from multiple cell culture experiments that PS extract displays potent anti-HIV-1 activity. We show that PS extract protects peripheral blood mononuclear cells and macrophages from infection with various X4 and R5 tropic HIV-1 strains, including clinical isolates. Functional studies revealed that the extract from PS has a novel mode-of-action. It interferes directly with viral infectivity and blocks the attachment of HIV-1 particles to target cells, protecting them from virus entry. Analysis of the chemical footprint of anti-HIV activity indicates that HIV-1 inhibition is mediated by multiple polyphenolic compounds with low cytotoxicity and can be separated from other extract components with higher cytotoxicity. Based on our data and its excellent safety profile, we propose that PS extract represents a lead candidate for the development of a scientifically validated herbal medicine for anti-HIV-1 therapy with a mode-of-action different from and complementary to current single-molecule drugs. © 2014 Helfer et al.

Indexed keywords

EMTREE drug terms: antiretrovirus agent; efavirenz; enfuvirtide; griffithsin; Human immunodeficiency virus 1 attachment inhibitor; Human immunodeficiency virus fusion inhibitor; Pelargonium sidoides extract; plerixafor; polyphenol derivative; umckaloabo; unclassified drug; zidovudine

EMTREE medical terms: antiviral activity; article; cell protection; concentration response; controlled study; cytotoxicity; drug isolation; drug potency; drug safety; drug targeting; human; human cell; Human immunodeficiency virus 1; Human immunodeficiency virus 1 infection; macrophage; peripheral blood mononuclear cell; plant root; prophylaxis; virus attachment; virus entry; virus infectivity; virus inhibition; virus particle; virus strain

MeSH: Anti-HIV Agents; Drug Evaluation, Preclinical; HEK293 Cells; HIV Infections; HIV-1; Humans; Pelargonium; Plant Extracts; Plant Roots; Plants, Medicinal; Polyphenols; Virus Attachment
Medline is the source for the MeSH terms of this document.

Chemicals and CAS Registry Numbers: efavirenz, 154598-52-4; enfuvirtide, 159519-65-0; plerixafor, 110078-46-1, 155148-31-5; zidovudine, 30516-87-1

Drug tradename: amd 3100,eps 7630,t 20, Hoffmann La Roche,umckaloabo.

Manufacturers:Drug manufacturer: Biomol GmbH;Hoffmann La Roche;Sigma Aldrich.