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.
Current Topics in Medicinal Chemistry
Title:Antitrypanosomal Activity & Docking Studies of Isolated Constituents from the Lichen Cetraria islandica: Possibly Multifunctional Scaffolds
Volume: 14 Issue: 8
Author(s): John Ogbaji Igoli, Alexander Irvine Gray, Carol Jean Clements, Poorna Kantheti and Rajeev Kumar Singla
Affiliation:
Keywords: Antitrypanosomal activity, Cetraria islandica, grip docking, iceland moss, phytoconstituents.
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.
Export Options
About this article
Cite this article as:
Igoli Ogbaji John, Gray Irvine Alexander, Clements Jean Carol, Kantheti Poorna and Singla Kumar Rajeev, Antitrypanosomal Activity & Docking Studies of Isolated Constituents from the Lichen Cetraria islandica: Possibly Multifunctional Scaffolds, Current Topics in Medicinal Chemistry 2014; 14 (8) . https://dx.doi.org/10.2174/1568026614666140324122323
DOI https://dx.doi.org/10.2174/1568026614666140324122323 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements