Cruz-Torres Karla Catalina, Estrada-Soto Samuel, Arias-Durán Luis, Navarrete-Vázquez Gabriel, Almanza-Pérez Julio César, Mora-Ramiro Beatriz, Perea-Arango Irene, Hernández-Núñez Emanuel, Villalobos-Molina Rafael, Carmona-Castro Gabriela, Medina-Díaz Irma-Martha, Ávila-Villarreal Gabriela
Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca 62209, Morelos, Mexico.
Ciencias de la Salud, Universidad Autónoma Metropolitana-Iztapalapa, Iztapalapa, Ciudad de Mexico 09340, Mexico.
Pharmaceutics. 2023 Sep 19;15(9):2346. doi: 10.3390/pharmaceutics15092346.
The aim of this work was to evaluate the vasorelaxant and antihypertensive effects of a standardized precipitate of the hydroalcoholic extract from (PP), comprising ursolic acid, oleanolic acid, acacetin, luteolin and tilianin, among others. In the ex vivo experiments, preincubation with L-NAME (nonspecific inhibitor of nitric oxide synthases) reduced the relaxation induced by PP; nevertheless, preincubation with indomethacin (nonspecific inhibitor of cyclooxygenases) did not generate any change in the vasorelaxation, and an opposed effect was observed to the contraction generated by CaCl addition. Oral administration of 100 mg/kg of PP induced a significant acute decrease in diastolic (DBP) and systolic (SBP) blood pressure in spontaneously hypertensive rats, without changes in heart rate. Additionally, PP showed a sustained antihypertensive subacute effect on both DBP and SBP for 10 days compared to the control group. On the other hand, human umbilical vein cells treated with 10 µg/mL of PP showed a significant reduction ( < 0.05) in intracellular adhesion molecule-1, compared to the control, but not on vascular cell adhesion molecule-1. In conclusion, PP induces a significant antihypertensive effect in acute- and subacute-period treatments, due to its direct vasorelaxant action on rat aortic rings through NO production and Ca channel blockade.
本研究的目的是评估一种标准化的水醇提取物沉淀物(PP)的血管舒张和降压作用,该沉淀物包含熊果酸、齐墩果酸、刺槐素、木犀草素和田基黄苷等。在体外实验中,用L-NAME(一氧化氮合酶的非特异性抑制剂)预孵育可降低PP诱导的舒张;然而,用吲哚美辛(环氧化酶的非特异性抑制剂)预孵育并未使血管舒张产生任何变化,并且观察到对添加氯化钙所产生的收缩有相反作用。口服100 mg/kg的PP可使自发性高血压大鼠的舒张压(DBP)和收缩压(SBP)显著急性降低,心率无变化。此外,与对照组相比,PP对DBP和SBP均显示出持续10天的亚急性降压作用。另一方面,用10 µg/mL的PP处理的人脐静脉细胞与对照组相比,细胞间黏附分子-1显著降低(P<0.05),但对血管细胞黏附分子-1无影响。总之,PP在急性和亚急性治疗期均诱导显著的降压作用,这是由于其通过产生一氧化氮和阻断钙通道对大鼠主动脉环具有直接的血管舒张作用。