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de Sousa ACC, Combrinck JM, Maepa K, et al. THC shows activity against cultured Plasmodium falciparum. Bioorg Med Chem Lett. 2021;54:128442doi: 10.1016/j.bmcl.2021.128442.
de Sousa, A. C. C., Combrinck, J. M., Maepa, K., & Egan, T. J. (2021). THC shows activity against cultured Plasmodium falciparum. Bioorganic & medicinal chemistry letters, 54128442. https://doi.org/10.1016/j.bmcl.2021.128442
de Sousa, Ana Carolina C, et al. "THC shows activity against cultured Plasmodium falciparum." Bioorganic & medicinal chemistry letters vol. 54 (2021): 128442. doi: https://doi.org/10.1016/j.bmcl.2021.128442
de Sousa ACC, Combrinck JM, Maepa K, Egan TJ. THC shows activity against cultured Plasmodium falciparum. Bioorg Med Chem Lett. 2021 Dec 15;54:128442. doi: 10.1016/j.bmcl.2021.128442. Epub 2021 Nov 08. PMID: 34763083.
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Bioorg Med Chem Lett. 2021 Dec 15;54:128442. doi: 10.1016/j.bmcl.2021.128442. Epub 2021 Nov 08.

THC shows activity against cultured Plasmodium falciparum.

Bioorganic & medicinal chemistry letters

Ana Carolina C de Sousa, Jill M Combrinck, Keletso Maepa, Timothy J Egan

Affiliations

  1. University of Cape Town, Department of Chemistry, Rondebosch 7701, South Africa. Electronic address: [email protected].
  2. University of Cape Town, Division of Pharmacology, Department of Medicine, Observatory 7925, South Africa.
  3. University of Cape Town, Department of Chemistry, Rondebosch 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa. Electronic address: [email protected].

PMID: 34763083 DOI: 10.1016/j.bmcl.2021.128442

Abstract

The FDA approved drug Dronabinol was identified in a previous study applying virtual screening using the haemozoin crystal as a target against malaria parasites. The active ingredient of dronabinol is synthetic tetrahydrocannabinol (THC), which is one of the major cannabinoids from Cannabis sativa. Traditional use of cannabis for malaria fever was reported in the world's oldest pharmacopoeia, dating to around 5000 years ago. In this research we report that THC inhibits β-haematin (synthetic haemozoin) and malaria parasite growth. Due the psychoactivity of THC, CBD, the other major naturally occurring cannabinoid that lacks the off-target psychoactive effects of THC, was also tested and inhibited β-haematin but showed only a mild antimalarial activity. To evaluate whether THC inhibit haemozoin formation, we performed a cellular haem fractionation assay that indicated that is not the likely mechanism of action. For the first time, the cannabinoid chemical structure is raised as a new chemical class to be further studied for malaria treatment, aiming to overcome the undesirable psychoactive effects of THC and optimize the antimalarial effects.

Copyright © 2021 Elsevier Ltd. All rights reserved.

Keywords: Cannabinoids; Cannabis; Dronabinol; Haemozoin; Malaria; β-haematin

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