The root extract of the medicinal plant Pelargonium sidoides is a potent HIV-1 attachment inhibitor.
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 EPs®7630, 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.
Institute of Virology, Helmholtz Zentrum München - German Research Center for Environmental Health, Neuherberg, Germany.
Markus
M
Helfer
Institute of Virology, Helmholtz Zentrum München - German Research Center for Environmental Health, Neuherberg, Germany.
Herwig
H
Koppensteiner
Institute of Virology, Helmholtz Zentrum München - German Research Center for Environmental Health, Neuherberg, Germany.
Martha
M
Schneider
Institute of Virology, Helmholtz Zentrum München - German Research Center for Environmental Health, Neuherberg, Germany.
Stephanie
S
Rebensburg
Research Unit Analytical BioGeoChemistry, Helmholtz Zentrum München - German Research Center for Environmental Health, Neuherberg, Germany.
Sara
S
Forcisi
Research Unit Analytical BioGeoChemistry, Helmholtz Zentrum München - German Research Center for Environmental Health, Neuherberg, Germany.
Constanze
C
Müller
Research Unit Analytical BioGeoChemistry, Helmholtz Zentrum München - German Research Center for Environmental Health, Neuherberg, Germany.
Philippe
P
Schmitt-Kopplin
Institute of Virology, Helmholtz Zentrum München - German Research Center for Environmental Health, Neuherberg, Germany.
Michael
M
Schindler
Institute of Virology, Helmholtz Zentrum München - German Research Center for Environmental Health, Neuherberg, Germany.
Ruth
R
Brack-Werner
D019380:Anti-HIV Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D057809:HEK293 Cells; D015658:HIV Infections / Q000188:drug therapy; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D031316:Pelargonium / Q000737:chemistry*; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry*; D010946:Plants, Medicinal / Q000737:chemistry; D059808:Polyphenols / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D053585:Virus Attachment / Q000187:drug effects*
D019380:Anti-HIV Agents; D010936:Plant Extracts; D059808:Polyphenols