Translator Disclaimer
1 November 2015 Active Compounds Against Anopheles minimus Carboxypeptidase B for Malaria Transmission-Blocking Strategy
Author Affiliations +
Abstract

Malaria transmission-blocking compounds have been studied to block the transmission of malaria parasites, especially the drug-resistant Plasmodium. Carboxypeptidase B (CPB) in the midgut of Anopheline mosquitoes has been demonstrated to be essential for the sexual development of Plasmodium in the mosquito. Thus, the CPB is a potential target for blocking compounds. The aim of this research was to screen compounds from the National Cancer Institute (NCI) diversity dataset and U.S. Food andDrug Administration (FDA)-approved drugs that could reduce the Anopheles CPB activity. The cDNA fragment of cpb gene from An. minimus (cpbAmi) was amplified and sequenced. The three-dimensional structure of CPB was predicted from the deduced amino acid sequence. The virtual screening of the compounds from NCI diversity set IV and FDA-approved drugs was performed against CPBAmi. The inhibition activity against CPBAmi of the top-scoring molecules was characterized in vitro. Three compounds—NSC-1014, NSC-332670, and aminopterin with IC50 at 0.99 mM, 1.55mM, and 0.062 mM, respectively—were found to significantly reduce the CPBAmi activity.

© The Authors 2015. Published by Oxford University Press on behalf of Entomological Society of America. All rights reserved. For Permissions, please email: journals.permissions@oup.com
Watcharakorn Mongkol, Uraiwan Arunyawat, Wunrada Surat, and Anchanee Kubera "Active Compounds Against Anopheles minimus Carboxypeptidase B for Malaria Transmission-Blocking Strategy," Journal of Medical Entomology 52(6), 1322-1332, (1 November 2015). https://doi.org/10.1093/jme/tjv133
Received: 10 June 2015; Accepted: 13 August 2015; Published: 1 November 2015
JOURNAL ARTICLE
11 PAGES

This article is only available to subscribers.
It is not available for individual sale.
+ SAVE TO MY LIBRARY

SHARE
ARTICLE IMPACT
RIGHTS & PERMISSIONS
Get copyright permission
Back to Top