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THC shows activity against cultured Plasmodium falciparum.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2021 Dec 15; Vol. 54, pp. 128442. Date of Electronic Publication: 2021 Nov 08. - Publication Year :
- 2021
-
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.<br /> (Copyright © 2021 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antimalarials chemistry
Cannabis chemistry
Dose-Response Relationship, Drug
Dronabinol chemistry
HL-60 Cells
Hemeproteins antagonists & inhibitors
Humans
Molecular Structure
Parasitic Sensitivity Tests
Structure-Activity Relationship
Antimalarials pharmacology
Dronabinol pharmacology
Malaria drug therapy
Plasmodium falciparum drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 54
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 34763083
- Full Text :
- https://doi.org/10.1016/j.bmcl.2021.128442