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Semi-Synthesis and Evaluation of Sargahydroquinoic Acid Derivatives as Potential Antimalarial Agents

1
Faculty of Pharmacy, Rhodes University, Grahamstown 6139, South Africa
2
Pharmacology Division, Department of Pharmacy and Pharmacology, WITS Research Institute for Malaria (WRIM), MRC Collaborating Centre for Multidisciplinary Research on Malaria, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2000, South Africa
3
Biomedical Biotechnology Research Unit (BioBRU), Department of Biochemistry and Microbiology, Rhodes University, Grahamstown 6139, South Africa
4
School of Pharmacy, University of the Western Cape, Bellville 7535, South Africa
*
Author to whom correspondence should be addressed.
Medicines 2019, 6(2), 47; https://doi.org/10.3390/medicines6020047
Received: 25 February 2019 / Revised: 27 March 2019 / Accepted: 28 March 2019 / Published: 1 April 2019
(This article belongs to the Special Issue Biological Potential and Medical Use of Secondary Metabolites)
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Abstract

Background: Malaria continues to present a major health problem, especially in developing countries. The development of new antimalarial drugs to counter drug resistance and ensure a steady supply of new treatment options is therefore an important area of research. Meroditerpenes have previously been shown to exhibit antiplasmodial activity against a chloroquinone sensitive strain of Plasmodium falciparum (D10). In this study we explored the antiplasmodial activity of several semi-synthetic analogs of sargahydroquinoic acid. Methods: Sargahydroquinoic acid was isolated from the marine brown alga, Sargassum incisifolium and converted, semi-synthetically, to several analogs. The natural products, together with their synthetic derivatives were evaluated for their activity against the FCR-3 strain of Plasmodium falciparum as well as MDA-MB-231 breast cancer cells. Results: Sarganaphthoquinoic acid and sargaquinoic acid showed the most promising antiplasmodial activity and low cytotoxicity. Conclusions: Synthetic modification of the natural product, sargahydroquinoic acid, resulted in the discovery of a highly selective antiplasmodial compound, sarganaphthoquinoic acid. View Full-Text
Keywords: sargaquinoic acid; sarganaphthoquinoic acid; antiplasmodial; malaria sargaquinoic acid; sarganaphthoquinoic acid; antiplasmodial; malaria
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Munedzimwe, T.C.; van Zyl, R.L.; Heslop, D.C.; Edkins, A.L.; Beukes, D.R. Semi-Synthesis and Evaluation of Sargahydroquinoic Acid Derivatives as Potential Antimalarial Agents. Medicines 2019, 6, 47.

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