Vasorelaxan Effect and Potent Antioxidant Activity of Natural Flavones Isolated from Lourteigia stoechadifolia and Ageratina stevioides, Two Venezuelan Plants

Morán-Pinzón, Juan; Mondolis, Eily; Abad, Antonio; Amaro-Luis, Juan M.; Sevilla, María A.; Montero, María; López-Pérez, Jose Luis; León, Estela Guerreo De

doi:10.9734/ejmp/2017/31985

Cited by 2 publications

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“…Considering the slight rightward shift of the CRCs in the absence of endothelium ( p = 0.009) and in the presence of L-NAME ( p = 0.99), it is evident that this compound mainly produces its vasodilator effect through an endothelium-independent mechanism. Our results are in accordance with previous studies which proved that methoxy-flavones, structurally related to compound 18 , elicit vasodilation [ 65 , 66 ], at least partly, through an endothelium-dependent mechanism that involves activation of the NO/cGMP pathway [ 65 ]. However, our findings differ from those of other researchers who found that certain methoxy-flavones produce an endothelium-dependent vasodilatory effect via activation of the potassium channels [ 67 , 68 ].…”

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confidence: 93%

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

et al. 2018

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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.

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