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Molecules 2018, 23(6), 1474; https://doi.org/10.3390/molecules23061474

Vasodilator Activity of Compounds Isolated from Plants Used in Mexican Traditional Medicine

1
Laboratorio de Investigación Química y Farmacológica de Productos Naturales, Facultad de Química, Universidad Autónoma de Querétaro, C.P. 76010 Querétaro, Mexico
2
Universidad Autónoma de Nuevo León, Facultad de Ciencias Químicas, Ciudad Universitaria, San Nicolás de los Garza, CP 66451 Nuevo León, Mexico
*
Authors to whom correspondence should be addressed.
Received: 6 April 2018 / Revised: 11 June 2018 / Accepted: 12 June 2018 / Published: 18 June 2018
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Abstract

Arterial hypertension is one of the main risk factors in the development of cardiovascular diseases. Therefore, it is important to look for new drugs to treat hypertension. In this study, we carried out the screening of 19 compounds (triterpenes, diterpenes, sesquiterpenes, lignans, and flavonoids) isolated from 10 plants used in Mexican traditional medicine to determine whether they elicited vascular smooth muscle relaxation and, therefore, could represent novel anti-hypertension drug candidates. The vasorelaxant activity of these compounds was evaluated on the isolated rat aorta assay and the results obtained from this evaluation showed that three compounds induced a significant vasodilatory effect: meso-dihydroguaiaretic acid [half maximal effective concentration (EC50), 49.9 ± 11.2 µM; maximum effect (Emax), 99.8 ± 2.7%]; corosolic acid (EC50, 108.9 ± 6.7 µM; Emax, 96.4 ± 4.2%); and 5,8,4′-trihydroxy-3,7-dimethoxyflavone (EC50, 122.3 ± 7.6 µM; Emax, 99.5 ± 5.4%). Subsequently, involvement of the NO/cyclic guanosine monophosphate (cGMP) and H2S/ATP-sensitive potassium channel (KATP) pathways on the vasodilator activity of these compounds was assessed. The results derived from this analysis showed that the activation of both pathways contributes to the vasorelaxant effect of corosolic acid. On the other hand, the vasodilator effect of meso-dihydroguaiaretic acid and 5,8,4′-trihydroxy-3,7-dimethoxyflavone, partly involves stimulation of the NO/cGMP pathway. However, these compounds also showed an important endothelium-independent vasorelaxant effect, whose mechanism of action remains to be clarified. This study indicates that meso-dihydroguaiaretic acid, corosolic acid, and 5,8,4′-trihydroxy-3,7-dimethoxyflavone could be used as lead compounds for the synthesis of new derivatives with a higher potency to be developed as drugs for the prevention and treatment of cardiovascular diseases. View Full-Text
Keywords: corosolic acid; 5,8,4′-trihydroxy-3,7-dimethoxyflavone; meso-dihydroguaiaretic acid hydrogen sulfide; nitric oxide; vasorelaxation corosolic acid; 5,8,4′-trihydroxy-3,7-dimethoxyflavone; meso-dihydroguaiaretic acid hydrogen sulfide; nitric oxide; vasorelaxation
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Luna-Vázquez, F.J.; Ibarra-Alvarado, C.; Camacho-Corona, M.R.; Rojas-Molina, A.; Rojas-Molina, J.I.; García, A.; Bah, M. Vasodilator Activity of Compounds Isolated from Plants Used in Mexican Traditional Medicine. Molecules 2018, 23, 1474.

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