Carissa edulis Vahl (Apocynaceae) extract, a medicinal plant of Benin pharmacopoeia, induces potent endothelium-dependent relaxation of coronary artery rings involving nitric oxide.

BACKGROUND: Hypertension is a major cardiovascular risk factor that affects most countries including those of Africa. Although Carissa edulis Vahl, Diodia scandens Sw. and Cleome gynandra L. are traditionally used in Benin as antihypertensive treatments with some efficacy mentioned by the local population, their biological activity on the cardiovascular system remains poorly studied. AIM: The study investigated the vasoreactivity of the plants and assessed the underlying mechanisms using isolated arteries. STUDY DESIGN: Aqueous-ethanolic extracts of aerial parts of C. edulis, D. scandens and C. gynandra were prepared by maceration before being subjected to multi-step liquid-liquid fractionation with solvents of increasing polarity. The vasoreactivity of the extracts and fractions were assessed on isolated porcine coronary artery and rat aorta using organ chambers, the role of nitric oxide (NO) using NG-nitro-L-arginine (NO synthase inhibitor), prostanoids using indomethacin (cyclooxygenases inhibitor) and endothelium-dependent hyperpolarization using TRAM-34 plus UCL 1684 (inhibitors of calcium-dependent K+ channels), and the vascular uptake of polyphenols using Neu reagent. RESULTS: The aqueous-ethanolic crude extract of C. edulis (CECE) induced potent relaxations that were exclusively endothelium-dependent and more pronounced than those to D. scandens and C. gynandra. The n-butanolic fraction of C. edulis (CEBF) was more active than the cyclohexane, dichloromethane, and ethyl acetate fractions. The relaxation induced by CECE and CEBF were inhibited by NG-nitro-L-arginine and affected neither by TRAM-34 plus UCL 1684 nor by indomethacin. CEBF induced sustained endothelium-dependent relaxations for at least 60 min, and inhibited, in a concentration-dependent manner, contractions to KCl, CaCl2, U46619 and serotonin in rings with endothelium. Analysis of CEBF by LCHRMS indicated the presence of polyphenols, terpenes, and alkaloids. Exposure of coronary artery and aorta rings to CEBF caused the accumulation of polyphenols predominantly in the endothelium. CONCLUSION: C. edulis leaf extract induced pronounced endothelium-dependent relaxations and inhibited contractile responses by stimulating the endothelial formation of NO. LCHRMS analysis of the most active fraction, the butanolic fraction, revealed the presence of numerous compounds including polyphenols, terpenes, and alkaloids. The polyphenols of CEBF accumulated preferentially in the endothelium of the arterial wall. Thus, these observations support the folkloric use of C. edulis in hypertension.

Procyanidin-rich fractions from Parkia biglobosa (Mimosaceae) leaves cause redox-sensitive endothelium-dependent relaxation involving NO and EDHF in porcine coronary artery.

AIM OF THE STUDY: Parkia biglobosa leaves are traditionally used as an antihypertensive agent in Benin. The present study assessed the vasorelaxant activity of different Parkia biglobosa leaf extracts using isolated porcine coronary artery rings. MATERIALS AND METHODS: A hydroalcoholic leaf extract was submitted to a multi-step liquid-liquid fractionation with solvents of increasing polarity and the polyphenolic content of the different fractions was analyzed. Vascular reactivity of the different extracts was assessed using porcine coronary artery rings, in the presence or absence of specific pharmacological inhibitors. RESULTS: The hydroalcoholic, ethyl acetate and butanolic extracts contained mainly procyanidins and monomeric flavonoids. Parkia biglobosa leaf crude extract induced a redox-sensitive endothelium-dependent relaxation mediated by both nitric oxide (NO) and endothelium-derived hyperpolarizing factor (EDHF). The fractionation of the butanolic extract generated 6 fractions, two of which induced stronger vasorelaxation than the original extract and they had a higher phenolic content. CONCLUSIONS: Parkia biglobosa leaf extract is able to induce endothelium-dependent NO- and EDHF-mediated relaxation in porcine coronary artery rings. The vasorelaxant activity is dependent on their phenolic content and appears to involve mainly procyanidins.