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)
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
b Research Unit Analytical BioGeoChemistry, Helmholtz Zentrum München - German Research Center for Environmental Health, Neuherberg, Germany
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.
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.