Abstract

This review discusses the contribution of the use of the isolated rat aorta (IRA) as a model for the evaluation of extracts and metabolites produced by plants with a vasodilator effect in animals. This model continues to be a valuable approach for the search and development of new phytochemicals consumed as medicinal plants or foods. In most cases, the sources of phytochemicals have been used in folk medicine to treat ailments that include hypertension. In this model, the endothelium is emphasized as a key component that modulates the vessel contractility, and therefore the basal tone and blood pressure. Based on the functional nature of the model, we focused on studies that determined the endothelium-dependent and -independent vasodilatory activity of phytochemicals. We describe the mechanisms that account for aorta contraction and relaxation, and subsequently show the vasoactive effect of a series of phytochemicals acting as vasodilators and its endothelium dependence. We highlight information regarding the cardiovascular benefits of phytochemicals, especially their potential antihypertensive effect. On this basis, we discuss the advantages of the IRA as a predictive model to support the research and development of new drugs that may be of help in the prevention and treatment of cardiovascular diseases, the number one cause of death worldwide.

Highlights

  • A Review of Endothelium-Dependent andMarcela Knox 1 , Raúl Vinet 1,2 , Lida Fuentes 2 , Bernardo Morales 3 and José L

  • One of the first steps in the sequence of events leading to cardiovascular disease is the reduction of endothelial cell capacity to release nitric oxide (NO), phenomena that can be experimentally evidenced by an impairment of endothelium-dependent relaxation (EDR)

  • Kim et al, [39] studied the potential relaxing effect of an extract of P. ginseng, which contained ginsenosides in isolated rat aorta (IRA); the results showed that the extract with a high content of ginsenosides induced EDR, which was corroborated by ginsenoside Rg3 and ginsenoside Rg1, two major ginsenosides of the protopanaxatriol group

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Summary

A Review of Endothelium-Dependent and

Marcela Knox 1 , Raúl Vinet 1,2 , Lida Fuentes 2 , Bernardo Morales 3 and José L. Laboratory of Pharmacology, Center of Micro Bioinnovation (CMBi), Faculty of Pharmacy, Universidad de Valparaíso, Valparaíso 2360102, Chile. Faculty of Chemistry and Biology, Universidad de Santiago de Chile, Santiago 9160020, Chile. Vice Chancellor of Investigation, Development and Innovation, Universidad de Santiago de Chile, Santiago 9160020, Chile. Simple Summary: Cardiovascular diseases are the leading cause of death worldwide, so the investigation of new therapeutic tools is a priority for their prevention and treatment. This review shows the relevant contribution of the isolated rat aorta as an in vitro experimental model to validate the therapeutic potential of phytochemicals, mainly those present in plants traditionally used in folk medicine to relieve hypertension. The results of the assays carried out in this model show that a variety of plant extracts and their isolated compounds produce vasodilation, which may explain their use, especially to treat hypertension

Introduction
Materials and Methods
Isolated Rat Aortic Preparation
The Contractility Mechanism in Vessels
The Endothelial Control of VSMCs
Phytochemical Assays of Plant Extracts and Isolated Compounds
Plant Extracts
Alkaloids
Non-Alkaloid Compounds
Findings
Conclusions
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