Centre of Biophysics and Biochemistry, Venezuelan Institute for Scientific Research, Caracas 1020A, Venezuela.
Faculty of Health Sciences, University of Brasilia, Darcy Ribeiro University Campus, Asa Norte, Federal District, Brasília CEP 70910-900, Brazil.
Molecules. 2023 May 23;28(11):4256. doi: 10.3390/molecules28114256.
Esquamosan, a new furofuran lignan, has been isolated by bio-guided assays from the methanolic extract of the leaves of L., and its structure was elucidated by spectroscopic methods. Esquamosan inhibited the rat aortic ring contraction evoked by phenylephrine in a concentration-dependent manner and showed an inhibitory effect on vasocontraction of the depolarized aorta with high-concentration potassium. The vasorelaxant effect by esquamosan could be attributed mainly to the inhibition of calcium influx from extracellular space through voltage-dependent calcium channels or receptor-operated Ca channels and also partly mediated through the increased release of NO from endothelial cells. The ability of esquamosan to modify the vascular reactivity of rat aortic rings incubated with high glucose (D-glucose 55 mM) was then evaluated, and this furofuran lignan reverted the endothelium-dependent impairment effect of high glucose in rat aortic rings. The antioxidant capacity of esquamosan was assessed using DPPH and FRAP assays. Esquamosan exhibited a similar antioxidant capacity compared to ascorbic acid, which was used as a positive control. In conclusion, this lignan showed a vasorelaxant effect, free radical scavenging capacity, and potential reductive power, suggesting its potential beneficial use to treat complex cardiometabolic diseases due to free radical-mediated diseases and its calcium antagonist effect.
从 的甲醇提取物中通过生物导向测定分离得到新的呋喃木脂素 esquamosan，并通过光谱方法阐明了其结构。esquamosan 以浓度依赖性方式抑制由苯肾上腺素引起的大鼠主动脉环收缩，并对高浓度钾引起的去极化主动脉的血管收缩显示出抑制作用。esquamosan 的血管舒张作用主要归因于抑制通过电压依赖性钙通道或受体操纵的 Ca 通道从细胞外空间进入细胞的钙内流，并且部分通过增加内皮细胞中 NO 的释放来介导。然后评估 esquamosan 对用高葡萄糖（D-葡萄糖 55 mM）孵育的大鼠主动脉环的血管反应性的修饰能力，并且这种呋喃木脂素恢复了高葡萄糖对大鼠主动脉环的内皮依赖性损伤作用。使用 DPPH 和 FRAP 测定法评估 esquamosan 的抗氧化能力。与用作阳性对照的抗坏血酸相比，esquamosan 表现出相似的抗氧化能力。总之，该木脂素表现出血管舒张作用、自由基清除能力和潜在的还原能力，表明其由于自由基介导的疾病及其钙拮抗剂作用而具有治疗复杂的心脏代谢疾病的潜在益处。
