作者: Francisco J Luna-Vázquez , César Ibarra-Alvarado , María del Rayo Camacho-Corona , Alejandra Rojas-Molina , J Isela Rojas-Molina
DOI: 10.3390/MOLECULES23061474
关键词: Mechanism of action 、 Potency 、 Cyclic guanosine monophosphate 、 EC50 、 Nitric oxide 、 Potassium channel 、 Chemistry 、 Corosolic acid 、 Traditional medicine 、 Vasodilation
摘要: Arterial hypertension is one of the main risk factors in development cardiovascular diseases. Therefore, it important to look for new drugs treat hypertension. In this study, we carried out screening 19 compounds (triterpenes, diterpenes, sesquiterpenes, lignans, and flavonoids) isolated from 10 plants used Mexican traditional medicine determine whether they elicited vascular smooth muscle relaxation and, therefore, could represent novel anti-hypertension drug candidates. The vasorelaxant activity these was evaluated on rat aorta assay results obtained evaluation showed that three 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 (EC50, 108.9 6.7 Emax, 96.4 4.2%); 5,8,4′-trihydroxy-3,7-dimethoxyflavone 122.3 7.6 99.5 5.4%). Subsequently, involvement NO/cyclic guanosine monophosphate (cGMP) H₂S/ATP-sensitive potassium channel (KATP) pathways vasodilator assessed. derived analysis activation both contributes acid. On other hand, 5,8,4′-trihydroxy-3,7-dimethoxyflavone, partly involves stimulation NO/cGMP pathway. However, also an endothelium-independent effect, whose mechanism action remains be clarified. This study indicates acid, as lead synthesis derivatives with higher potency developed prevention treatment