Next Article in Journal
Phytochemical Modulation of MiRNAs in Colorectal Cancer
Next Article in Special Issue
In Vitro Evaluation of the Phytopharmacological Potential of Sargassum incisifolium for the Treatment of Inflammatory Bowel Diseases
Previous Article in Journal
Music Therapy as Treatment of Negative Symptoms for Adult Patients Diagnosed with Schizophrenia—Study Protocol for a Randomized, Controlled and Blinded Study
Previous Article in Special Issue
Antioxidant, Cytotoxic, and Antimicrobial Activities of Glycyrrhiza glabra L., Paeonia lactiflora Pall., and Eriobotrya japonica (Thunb.) Lindl. Extracts
Article Menu
Issue 2 (June) cover image

Export Article

Open AccessArticle

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

Faculty of Pharmacy, Rhodes University, Grahamstown 6139, South Africa
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
Biomedical Biotechnology Research Unit (BioBRU), Department of Biochemistry and Microbiology, Rhodes University, Grahamstown 6139, South Africa
School of Pharmacy, University of the Western Cape, Bellville 7535, South Africa
Author to whom correspondence should be addressed.
Medicines 2019, 6(2), 47;
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)
PDF [1136 KB, uploaded 5 May 2019]


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

Graphical abstract

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).

Supplementary material

Printed Edition Available!
A printed edition of this Special Issue is available here.

Share & Cite This Article

MDPI and ACS Style

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.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Medicines EISSN 2305-6320 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top