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Bioassay-guided isolation and identification of gametocytocidal compounds from Artemisia afra (Asteraceae)

Article scientifique 2019 Anglais

Résumé

BACKGROUND: Optimal adoption of the malaria transmission-blocking strategy is currently limited by lack of safe and efficacious drugs. This has sparked the exploration of different sources of drugs in search of transmission-blocking agents. While plant species have been extensively investigated in search of malaria chemotherapeutic agents, comparatively less effort has been channelled towards exploring them in search of transmission-blocking drugs. Artemisia afra (Asteraceae), a prominent feature of South African folk medicine, is used for the treatment of a number of diseases, including malaria. In search of transmission-blocking compounds aimed against Plasmodium parasites, the current study endeavoured to isolate and identify gametocytocidal compounds from A. afra. METHODS: A bioassay-guided isolation approach was adopted wherein a combination of solvent-solvent partitioning and gravity column chromatography was used. Collected fractions were continuously screened in vitro for their ability to inhibit the viability of primarily late-stage gametocytes of Plasmodium falciparum (NF54 strain), using a parasite lactate dehydrogenase assay. Chemical structures of isolated compounds were elucidated using UPLC-MS/MS and NMR data analysis. RESULTS: < 10 μg/ml; ~ 10 μM) against both gametocytes and intra-erythrocytic asexual P. falciparum parasites. Interestingly, 1α,4α-dihydroxybishopsolicepolide was significantly more potent against late-stage gametocytes than to early-stage gametocytes and intra-erythrocytic asexual P. falciparum parasites. Additionally, both isolated compounds were not overly cytotoxic against HepG2 cells in vitro. CONCLUSION: This study provides the first instance of isolated compounds from A. afra against P. falciparum gametocytes as a starting point for further investigations on more plant species in search of transmission-blocking compounds.

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Moyo, P., Kunyane, P., Selepe, M., Eloff, J., Niemand, J., Louw, A., Maharaj, V., Birkholtz, L. (2019). Bioassay-guided isolation and identification of gametocytocidal compounds from Artemisia afra (Asteraceae). https://doi.org/10.1186/s12936-019-2694-1

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Phanankosi Moyo Phaladi Kunyane Mamoalosi A. Selepe J.N. Eloff Jandeli Niemand Abraham I. Louw Vinesh Maharaj Lyn‐Marié Birkholtz

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