Planta Med 2013; 79 - PN15
DOI: 10.1055/s-0033-1348696

Antileishmanial Agents Isolated from the Stems of Pentalinon andrieuxii

L Pan 1, C Terrazas 2, CM Lezama-Davila 2, S Varikuti 2, SR Kotha 3, AB Shelton 3, AP Isaac-Marquez 4, JR Fuchs 1, NL Parinandi 3, AR Satoskar 2, AD Kinghorn 1
  • 1College of Pharmacy, Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy
  • 2Department of Pathology, College of Medicine
  • 3Dorothy M. Davis Heart and Lung Research Institute, The Ohio State University, Columbus, Ohio 43210, USA
  • 4Centro de Investigacion en Enfermedades Tropicales, Universidad Autonoma de Campeche, 24030, Campeche, Mexico

Bioassay-guided fractionation was conducted on hexane- and chloroform-soluble extracts of the stems of Pentalinon andrieuxii, using a Leishmania (L.) mexicana strain of parasites. This led to the isolation of three new compounds and 17 known compounds. All isolates were evaluated in vitro for their ability to inhibit the growth of promastigotes of L. mexicana. Four C21 sterol derivatives were found to exhibit potent leishmanicidal activity in this assay. Furthermore, the effects of NF-κB activation and cytokine production, as well as the lipid altering properties of these compounds were investigated in macrophage model systems derived from the RAW264.7 cell line.