Abstract
BackgroundConsidering the need for new anti-malarial drugs, further investigations on Keetia leucantha (Rubiaceae), an in vitro antiplasmodial plant traditionally used to treat malaria, were carried out. This paper aimed to assess the in vivo anti-malarial efficacy of K. leucantha triterpenic esters previously identified as the most in vitro active components against Plasmodium falciparum and their potential toxicity as well as those of anti-malarial extracts.ResultsThese eight triterpenic esters and the major antiplasmodial triterpenic acids, ursolic and oleanolic acids, were quantified in the twigs dichloromethane extract by validated HPLC–UV methods. They account for about 19% of this extract (16.9% for acids and 1.8% for esters). These compounds were also identified in trace in the twigs decoction by HPLC-HRMS. Results also showed that extracts and esters did not produce any haemolysis, and were devoid of any acute toxicity at a total cumulative dose of 800 and 150 mg/kg respectively. Moreover, esters given intraperitoneally at 50 mg/kg/day to Plasmodium berghei-infected mice showed a very significant (p < 0.01) parasitaemia inhibition (27.8 ± 5.4%) on day 4 post-infection compared to vehicle-treated mice.ConclusionsThese results bring out new information on the safety of K. leucantha use and on the identification of anti-malarial compounds from its dichloromethane extract. Its activity can be explained by the presence of triterpenic acids and esters which in vivo activity and safety were demonstrated for the first time.
Highlights
Considering the need for new anti-malarial drugs, further investigations on Keetia leucantha (Rubi‐ aceae), an in vitro antiplasmodial plant traditionally used to treat malaria, were carried out
Nature and mostly plants are a resourceful supplier of potential active metabolites [4] with the successful 2016 Nobel prize example of the sesquiterpenic artemisinin isolated from Artemisia annua (Asteraceae) used for thousands years as Chinese herbal remedy [5] or quinine, the first anti-malarial medicine
Bioguided fractionations of dichloromethane extract led to the isolation and identification of in vitro antiplasmodial triterpenic acids: ursolic and oleanolic acids (IC50 = 32.4 and 59.4 μM, respectively on 3D7 and SI < 3 compared to WI38 mammalian cell line) and eight more selective triterpenic esters (Fig. 1; IC50 of the mixture = 1.66 μg/ml, about 2.6 μM on 3D7, SI = 34.6 compared to WI38) [11]
Summary
Considering the need for new anti-malarial drugs, further investigations on Keetia leucantha (Rubi‐ aceae), an in vitro antiplasmodial plant traditionally used to treat malaria, were carried out. Nature and mostly plants are a resourceful supplier of potential active metabolites [4] with the successful 2016 Nobel prize example of the sesquiterpenic artemisinin isolated from Artemisia annua (Asteraceae) used for thousands years as Chinese herbal remedy [5] or quinine, the first anti-malarial medicine. In this context, further investigations were carried out on Keetia leucantha (Rubiaceae), a West African tree mainly used traditionally as a whole plant decoction in Benin to treat malaria.
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