Document Type
Article
Original Publication Date
2009
Journal/Book/Conference Title
Malaria Journal
Volume
8
Issue
139
DOI of Original Publication
10.1186/1475-2875-8-139
Date of Submission
August 2014
Abstract
Background
Malaria is the third most prevalent cause of infectious disease in the world. Resistance of the parasite to classical drugs makes the discovery of new and effective drugs more urgent. The oxidized derivative of hydroxy-cis terpenone (OHCT) is a synthetic molecule that is not toxic to cultured human liver cells at concentrations as high as 60 μM and inhibits activity of cytochrome P450s that metabolize many drugs.
Methods
OHCT activity against chloroquine-sensitive and -resistant strains of Plasmodium falciparum, and aP. falciparum clone that is partially resistant to artemisinin was assayed in vitro.
Results
OHCT at nanomolar concentrations was effective against all intraerythrocytic stages of P. falciparum and exhibited activity in vitro against both chloroquine-sensitive and -resistant strains of P. falciparum as well as a P. falciparum clone that is partially resistant to artemisinin. Moreover, OHCT exhibited potent activity against gametocytes, the form that is transmitted by mosquitoes and essential for the spread of malaria.
Conclusion
OHCT displays strong growth inhibitory activity against all stages of P. falciparum and no evidence of toxicity to human cells in culture. It is easily synthesized and has the potential for inhibiting metabolism of drugs used in combination therapies.
Rights
© 2009 Mayer et al; licensee BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Is Part Of
VCU Biology Publications
Comments
Originally published at http://dx.doi.org/10.1186/1475-2875-8-139