Malheiros Jéssica, Simões Daniela M, Antunes Pedro E, Figueirinha Artur, Cotrim Maria Dulce, Fonseca Diogo A
Laboratory of Pharmacology and Pharmaceutical Care, Faculty of Pharmacy, University of Coimbra, 3000-548 Coimbra, Portugal.
Coimbra Institute for Clinical and Biomedical Research (iCBR), Faculty of Medicine, University of Coimbra, 3000-548 Coimbra, Portugal.
Pharmaceuticals (Basel). 2022 May 22;15(5):638. doi: 10.3390/ph15050638.
L. has been traditionally used for the treatment of inflammatory diseases but also as a hypotensive. To our knowledge, only one study has previously suggested an improvement in vascular endothelial function in diabetic conditions, as the underlying mechanisms and responsible compounds are unknown. In this study, we aimed to assess the direct vascular effects of L. in human arteries. The infusion elicited a mild increase in basal vascular tone and a significant potentiation of the adrenergic contraction of 49.18% at 0.02 mg/mL, suggesting the presence of compounds with mild vasoconstrictor activity. In contrast, the ethyl acetate fraction inhibited adrenergic contraction by 80.65% at 2 mg/mL and elicited no effect on basal vascular tone. A potent concentration-dependent vasorelaxation was observed for both the infusion and the ethyl acetate fraction (maximal relaxation above 76% and 47%, respectively). Inhibition of nitric oxide synthase and cyclooxygenase elicited significant decreases in the vasorelaxation to the infusion, as, for the ethyl acetate fraction, only the cyclooxygenase pathway appeared to be involved. Isoquercitrin elicited a vasoactivity consistent with the ethyl acetate fraction, suggesting this is a major component responsible for the vasorelaxant properties of . Further research is warranted to fully evaluate its vasoprotective properties with therapeutic potential in several conditions, e.g., atherosclerosis.
L. 传统上一直用于治疗炎症性疾病,也用作降压药。据我们所知,此前仅有一项研究表明其在糖尿病情况下可改善血管内皮功能,但其潜在机制和起作用的化合物尚不清楚。在本研究中,我们旨在评估L. 对人体动脉的直接血管作用。输注引起基础血管张力轻度增加,在0.02 mg/mL时肾上腺素能收缩显著增强49.18%,表明存在具有轻度血管收缩活性的化合物。相比之下,乙酸乙酯部分在2 mg/mL时可抑制肾上腺素能收缩80.65%,且对基础血管张力无影响。对于输注液和乙酸乙酯部分均观察到强效的浓度依赖性血管舒张作用(最大舒张率分别高于76%和47%)。抑制一氧化氮合酶和环氧化酶可使对输注液的血管舒张作用显著降低,而对于乙酸乙酯部分,似乎仅涉及环氧化酶途径。异槲皮苷引起的血管活性与乙酸乙酯部分一致,表明这是导致L. 血管舒张特性的主要成分。有必要进行进一步研究,以全面评估其在多种病症(如动脉粥样硬化)中具有治疗潜力的血管保护特性。