Bioassay-guided isolation and identification of gametocytocidal compounds from Artemisia afra (Asteraceae)
- PMID: 30849984
- PMCID: PMC6408838
- DOI: 10.1186/s12936-019-2694-1
Bioassay-guided isolation and identification of gametocytocidal compounds from Artemisia afra (Asteraceae)
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 < 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.
Keywords: Artemisia afra; Gametocytes; Malaria; Natural products; Plasmodium falciparum; Sesquiterpene lactone; Transmission-blocking.
Figures




Similar articles
-
In vitro inhibition of Plasmodium falciparum early and late stage gametocyte viability by extracts from eight traditionally used South African plant species.J Ethnopharmacol. 2016 Jun 5;185:235-42. doi: 10.1016/j.jep.2016.03.036. Epub 2016 Mar 16. J Ethnopharmacol. 2016. PMID: 26994818
-
In vitro dual activity of Aloe marlothii roots and its chemical constituents against Plasmodium falciparum asexual and sexual stage parasites.J Ethnopharmacol. 2022 Oct 28;297:115551. doi: 10.1016/j.jep.2022.115551. Epub 2022 Jul 16. J Ethnopharmacol. 2022. PMID: 35850311
-
In vitro antiplasmodial evaluation of medicinal plants from Zimbabwe.Phytother Res. 2003 Feb;17(2):123-8. doi: 10.1002/ptr.1066. Phytother Res. 2003. PMID: 12601673
-
Artemisia afra, a controversial herbal remedy or a treasure trove of new drugs?J Ethnopharmacol. 2019 Nov 15;244:112127. doi: 10.1016/j.jep.2019.112127. Epub 2019 Jul 31. J Ethnopharmacol. 2019. PMID: 31376515 Review.
-
Future antimalarials from Artemisia? A rationale for natural product mining against drug-refractory Plasmodium stages.Nat Prod Rep. 2023 Jun 21;40(6):1130-1144. doi: 10.1039/d3np00001j. Nat Prod Rep. 2023. PMID: 37021639 Review.
Cited by
-
Ethnomedicinal herbs in African traditional medicine with potential activity for the prevention, treatment, and management of coronavirus disease 2019.Futur J Pharm Sci. 2021;7(1):72. doi: 10.1186/s43094-021-00223-5. Epub 2021 Mar 20. Futur J Pharm Sci. 2021. PMID: 33778086 Free PMC article. Review.
-
Immune System and Epidemics: The Role of African Indigenous Bioactive Substances.Nutrients. 2023 Jan 5;15(2):273. doi: 10.3390/nu15020273. Nutrients. 2023. PMID: 36678143 Free PMC article. Review.
-
Ethyl gallate isolated from phenol-enriched fraction of Caesalpinia mimosoides Lam. Promotes cutaneous wound healing: a scientific validation through bioassay-guided fractionation.Front Pharmacol. 2023 Jun 16;14:1214220. doi: 10.3389/fphar.2023.1214220. eCollection 2023. Front Pharmacol. 2023. PMID: 37397484 Free PMC article.
-
Molecular Diversity and Biochemical Content in Two Invasive Alien Species: Looking for Chemical Similarities and Bioactivities.Mar Drugs. 2022 Dec 22;21(1):5. doi: 10.3390/md21010005. Mar Drugs. 2022. PMID: 36662178 Free PMC article.
-
Contemporary exploitation of natural products for arthropod-borne pathogen transmission-blocking interventions.Parasit Vectors. 2022 Aug 24;15(1):298. doi: 10.1186/s13071-022-05367-8. Parasit Vectors. 2022. PMID: 36002857 Free PMC article. Review.
References
-
- WHO . Guidelines for the treatment of malaria. Geneva: World Health Organization; 2015. - PubMed
MeSH terms
Substances
Grants and funding
LinkOut - more resources
Full Text Sources