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

Autor: Phanankosi Moyo, Phaladi Kunyane, Mamoalosi A. Selepe, Jacobus N. Eloff, Jandeli Niemand, Abraham I. Louw, Vinesh J. Maharaj, Lyn-Marie Birkholtz
Jazyk: angličtina
Rok vydání: 2019
Předmět:
Zdroj: Malaria Journal, Vol 18, Iss 1, Pp 1-11 (2019)
Druh dokumentu: article
ISSN: 1475-2875
DOI: 10.1186/s12936-019-2694-1
Popis: Abstract 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 Two guaianolide sesquiterpene lactones, 1α,4α-dihydroxybishopsolicepolide and yomogiartemin, were isolated and shown to be active (IC50
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