Antiparasitic activities of two sesquiterpenic lactones isolated from Acanthospermum hispidum D.C.

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AuteurGANFON, MEDESSOU YOWEL HABIB
AuteurGBAGUIDI, AHOKANOU FERNAND
AuteurBERO, JOANNE
AuteurTCHINDA, ALEMBERT
AuteurGBENOU, J
AuteurMOUDACHIROU, MANSOUROU
AuteurQUETIN LECLERCQ, JOELLE
AuteurFREDERICH, MICHEL
Date d'ajout2026-06-02T16:06:57Z
Date de disponibilite2026-06-02T16:06:57Z
Date de publication2012
ResumeEthnopharmacological relevance: Aerial parts of Acanthospermum hispidum D.C. are often used by traditional healers in Benin for various diseases and especially for malaria. Aim of the study: To identify active compounds from extracts of Acanthospermum hispidum D.CV. leaves previously shown to possess antimalarial properties and analyse in vivo activity and toxicity of crude extracts. Materials and methods: Compounds were isolated from aerial part of Acanthospermum hispidum D.C. and structurally elucidated using extensive spectroscopic analysis. Antiplasmodial activity was evaluated in vitro against a chloroquine-sensitive strain of Plasmodium falciparum (3D7) using the measurement of the plasmodial lactate dehydrogenase activity and in vivo against Plasmodium berghei berghei by the 4-day suppressive test. Selectivity of extract and purified compounds on Plasmodium parasites were evaluated by using MTT test on J774 macrophage like murine cells and WI38 human normal fibroblasts and also against two other parasites: Trypanosoma brucei brucei and Leishmania mexicana mexicana. Acute and sub-acute toxicities of a crude extract were evaluated on mice. Results: Two known sesquiterpenic lactones were isolated: 1 (15-acetoxy-8-[(2-methylbutyryloxy)]- 14-oxo-4,5-cis-acanthospermolide) and 2 (9-acetoxy-15-hydroxy-8-(2-methylbutyryloxy)-14-oxo- 4,5-trans-acanthospermolide). 1 and 2 showed in vitro antiplasmodial activity against the chloroquinesensitive strain (3D7) with IC50 of 2.9 ± 0.5 and 2.23 ± 0.09 M respectively. Only 2 showed a high selectivity index (SI: 18.4) on Plasmodium compared to cytotoxicity against human fibroblasts cell line (WI38). 1 and 2 also showed interesting antiparasitic activities in vitro against Trypanosoma brucei brucei (IC50 of 2.45 ± 0.49 and 6.36 ± 1.42 M respectively) and Leishmania mexicana mexicana (IC50 of 0.94 ± 0.05 and 2.54 ± 0.19 M respectively). Furthermore, crude acidic water extract and fractions containing one of the two isolated compounds displayed a weak in vivo antimalarial activity against Plasmodium berghei berghei with a long half-life causing a delayed effect. In vivo acute (2000 mg/kg) and sub-acute (1000 mg/kg) toxicity tests on the crude acidic water extract did not show toxicity. Conclusion: Crude acidic water extract, fractions and pure isolated compounds from Acanthospermum hispidum showed promising in vitro antiplasmodial activity. Despite our study did not show in vivo acute and subacute toxicities of the crude acidic water extract, its weak in vivo antimalarial activity and the in vitro cytotoxicity of pure compounds and enriched extracts containing 1 and 2 indicate that the aerial parts of Acanthospermum hispidum should be used with caution for malaria treatments.
Autre identifiantBECDB-4411
URIhttps://dspace.uac.bj/handle/123456789/4193
Languefr
Fait partie deJournal of Ethnopharmacology
SujetAcanthospermum hispidum
SujetAcanthopermolide
SujetAntiplasmodial activity
SujetAntitrypanosomial activity
SujetAntileischmanial activity
SujetBénin
TitreAntiparasitic activities of two sesquiterpenic lactones isolated from Acanthospermum hispidum D.C.
TypeArticle

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