Research - HIV
Betulinic Acid and Its Derivatives: A Review on their Biological Properties
Perumal Yogeeswari* and Dharmarajan Sriram
Pharmacy Department, Birla Institute of Technology & Science, Pilani-333031, INDIA
Abstract:
Betulinic acid is a naturally occurring pentacyclic triterpenoid and has been shown to exhibit a variety of biological activities including inhibition of human immunodeficiency virus (HIV), antibacterial,antimalarial, anti inflammatory, anthelmintic and antioxidant properties. This article reports a survey of the literature dealing with betulinic acid related biological properties that has appeared from the 1990’s to the beginning of 2003. A broad range of medical and pharmaceutical disciplines are covered, including a brief introduction about discovery, phytochemical aspects, organic synthesis, anti-HIV and cytotoxic mechanisms ofaction. Various structural modifications carried out and their biological and pharmacokinetic profiles are also incorporated.
Source : Current Medicinal Chemistry
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The Root Extract of the Medicinal Plant Pelargonium sidoides Is a Potent HIV-1 Attachment Inhibitor
- Markus Helfer,
- Herwig Koppensteiner,
- Martha Schneider,
- Stephanie Rebensburg,
- Sara Forcisi,
- Constanze Müller,
- Philippe Schmitt-Kopplin,
- Michael Schindler,
- Ruth Brack-Werner
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 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.
Source : PLOS ONE
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