In vitro antileishmanial, antiplasmodial and cytotoxic activities of a new ventiloquinone and five known triterpenes from Parinari excelsa.

CONTEXT: Parinari excelsa Sabine (Chrysobalanaceae) is an indigenous tree from West and Eastern Africa. This tree is used in Ivory Coast as an antimalaria remedy. OBJECTIVE: The in vitro antiplasmodial and antileishmanial activities of the stem bark, the leaf and the major compounds from the stem bark were investigated. MATERIALS AND METHODS: The leaves and stem bark from P. excelsa were separately collected, air-dried and powdered. Two extracts (methylene chloride and methanol) were realized for both powders. Every extract was tested for its antiplasmodial and antileishmanial activities. Only the stem bark crude extracts were fractionated by column chromatography and their major components were analyzed by NMR, HRESIMS and IR methods. The compounds were tested for their antiplasmodial and antileishmanial activities. RESULTS: The comparison of the IC(50) values of the crude extracts were in this order: 3.41 (IC(50) of PeBMc) <4.10 (IC(50) of PeBMc) <4.42 (IC(50) of PeLMe) against P. falciparum and 5.19 (IC(50) of PeBMc) <12.32 (IC(50) of PeBMe) <19.33 (IC(50) of PeLMc) <32.37 (IC(50) of PeLMe) against L. donovani. The stem bark crude extracts were the most active against both parasites. Their fractionation leaded to a new ventiloquinone, five triterpenes and one chlorogenic acid. All these compounds were isolated for the first time from P. excelsa. High activities were observed with (3ß)-3-hydroxyolean-12-en-28-oic acid (IC(50) = 8.2 µM) and 3ß-hydroxyolean-5,12-dien-28-oic acid (IC(50) = 7.7 µM) against L. donovani. With the antiplasmodial activity, the best activity was observed with 16ß-hydroxylupane-1,20(29)-dien-3-one (IC(50) = 28.3 µM). DISCUSSION AND CONCLUSION: These findings demonstrated that the constituents of P. excelsa stem bark have in vitro antiplasmodial and antileishmanial activities.

[Evaluation of the anti-inflammatory activity and phytochemical screening of Annona senegalensis leaves]. / Évaluation de l'activité anti-inflammatoire et screening phytochimique des feuilles de Annona senegalensis.

OBJECTIVE: This study aims to highlight the anti-inflammatory activity of ethanol extract of Annona senegalensis and do its phytochemical screening. METHODS: Rats were divided into three groups. The first group received only saline injection and instillation by intraperitoneal injection on days D0 and D7. This phase was the sensitization of that group. Then, on days D21, D22 and D23, the rats of the same group (Group 1) were injected with saline under anesthesia. The second group (Group 2) was composed of rats had not undergone treatment with the extract of Annona senegalensis. The rats in this batch have been sensitized by intraperitoneal injection (50 µL) of a solution of albumin (50 mg/rat) dissolved in aluminum hydroxide on days 0 and 7. Then during the challenge phase, saline containing 0.9% sodium chloride were injected intraperitoneally on days D21, D22 and D23. The sacrifice took place at D24 or 24 hours after the last challenge to ovalbumin. Similarly, rats of the third group (Group 3) have been sensitized by ovalbumin combined with aluminum hydroxide on days D0 and day D7. Then during the stage of provocation, rats in this batch received at days D21, D22 and D23, conjugated injection of albumin and ethanol extract of Annona senegalensis (injection of 0.4 mL of 7.10(-2) mg/kg body weight). The aqueous extract of Annona senegalensis has been previously prepared in saline. Twenty four hours after the last injection corresponding to D23, the rats were sacrificed under anesthesia. Secondary metabolites have been characterized by physico-chemical properties. RESULTS: Rats in the control (Group 1) gave an average of 24 ± 0.02 mast cells, 7 ± 0.1 macrophages, 9 ± 0.05 eosinophils. In the control group was not revealed the presence of neutrophils. Following the steps of provocation and awareness albumin (Group 2), we observed a significant increase in the number of inflammatory cells compared to control group (p < 0.001). Indeed, mast cells and macrophages have suffered increased respectively to 164 ± 0.01 and 253 ± 0.04. While eosinophils have increased from 9 ± 0.05 to 81 ± 0.01. There were 31 ± 0.02 neutrophils in Group 2. Group 3 treated with Annona senegalensis (7.10(-2) mg/kg) induced a significant decrease in the number of inflammatory cells compared to control group (p < 0.001). Indeed, mast cells decreased from 164 ± 0.01 to 89 ± 0.03. Similarly, the number of macrophages decreased from 253 ± 0.04 to 175 ± 0.06 and neutrophils decreased from 31 ± 0.02 to 10 ± 0.05. Finally, the eosinophils have suffered a decrease (from 81 ± 0.01 to 61 ± 0.08). However, after treatment with the extract, the values of different cell types have always been significantly higher (p < 0.001) compared to those in the control group (except neutrophils). This result indicates that the extract of Annona senegalensis did not completely inhibit the inflammatory effect induced by albumin. The major classes of secondary metabolites, terpenoids, coumarins, flavonoids and tannins were detected in the leaves of the plant. However, they are low in alkaloids and substances quinone. CONCLUSION: The extract induced a significant decrease in the number of inflammatory cells. This effect is likely due to higher concentrations of tannins and phenolic compounds in the extract of plant. Thus this study provides a scientific validation of the use of this plant against asthma and cough in the Ivorian pharmacopoeia. However, its mechanism of action remains to be elucidated.

Laxative activities of Mareya micrantha (Benth.) Müll. Arg. (Euphorbiaceae) leaf aqueous extract in rats.

BACKGROUND: Mareya micrantha (Benth.) Müll. Arg. (Euphorbiaceae) is a shrub that is commonly used in Côte d'Ivoire (West Africa) for the treatment of constipation and as an ocytocic drug. The present study was carried out to investigate the laxative activity of Mareya micrantha in albino's Wistar rats. METHODS: Rats were divided in 5 groups of 5 animals each, first group as control, second group served as standard (sodium picosulfate) while group 3, 4 and 5 were treated with leaf aqueous extract of Mareya micrantha at doses of 100, 200 and 400 mg/kg body weight (b.w.), per os respectively. The laxative activity was determined based on the weight of the faeces matter. The effects of the leaves aqueous extract of Mareya micrantha and castor oil were also evaluated on intestinal transit, intestinal fluid accumulation and ions secretion. RESULTS: Phytochemicals screening of the extract revealed the presence of flavonoids, alkaloids, tannins, polyphenols, sterols and polyterpenes. The aqueous extract of Mareya micrantha applied orally (100, 200 and 400 mg/kg; p.o.), produced significant laxative activity and reduced loperamide induced constipation in dose dependant manner. The effect of the extract at 200 and 400 mg/kg (p.o.) was similar to that of reference drug sodium picosulfate (5 mg/kg, p.o). The same doses of the extract (200 and 400 mg/kg, p.o.) produced a significant increase (p < 0.01) of intestinal transit in comparison with castor oil (2 mL) (p < 0.01). Moreover, the extract induced a significant enteropooling and excretion of Cl-, Na+, K+ and Ca2+ in the intestinal fluid (p < 0.01). CONCLUSIONS: The results showed that the aqueous extract of Mareya micrantha has a significant laxative activity and supports its traditional use in herbal medicine.