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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Antitrypanosomal Activity & Docking Studies of Isolated Constituents from the Lichen Cetraria islandica: Possibly Multifunctional Scaffolds

Author(s): John Ogbaji Igoli, Alexander Irvine Gray, Carol Jean Clements, Poorna Kantheti and Rajeev Kumar Singla

Volume 14, Issue 8, 2014

Page: [1014 - 1021] Pages: 8

DOI: 10.2174/1568026614666140324122323

Price: $65

Abstract

Chemical investigation of the lichen Cetraria islandica has led to the isolation of four compounds identified as protolichesterinic acid, lichesterinic acid, protocetraric acid and fumarprotocetraric acid. Their structures were characterized using their physical and spectroscopic data. Using an Alamarblue 96 well microplate assay, these compounds were tested to evaluate their trypanocidal activity against Trypanosoma brucei brucei. Protolichesterinic acid (MIC = 6.30 µM) and lichesterinic acid (MIC = 12.5 µM) showed very significant activity against the test organism. Docking studies (GRIP technique) of these molecules revealed their strong affinity towards possible targets of Trypanosoma brucei such as riboflavin kinase, sterol-14α-demethylase (CYP51), rohedsain and glutathione synthetase. Hydrophobicity played a significant role in their antitrypanosomal activity.

Keywords: Antitrypanosomal activity, Cetraria islandica, grip docking, iceland moss, phytoconstituents.

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