Scholarlink

<p>Flavonoids have diverse pharmacological effects, such as the relaxant action on the vascular smooth muscle. In the present research, we determined the functional mode of action of the 2-phenyl-1-benzopyran-4-one or flavone, to be used as a prototype to obtain new drugs for treating arterial hypertension. For this, an ex vivo model of isolated rat aortic rings, an in silico approach, an <i>in vivo</i> assay on spontaneously hypertensive rats, and an acute oral toxicity test were used. The results showed a significant vasorelaxant action of 2-phenyl-1-benzopyran-4-one in rings with (E +) and without (E-) endothelium in a concentration-dependent manner, being more potent in the presence of endothelium (<i>p</i> &lt; 0.05). The observed functional mode of action indicated that relaxant action is related to nitric oxide (NO) production and calcium channel blockade, which was corroborated by docking studies. Finally, intragastric administration of 2-phenyl-1-benzopyran-4-one (50&#xa0;mg/kg) significantly decreased systolic and diastolic blood pressure and showed no <i>in vivo</i> acute toxicity. These results demonstrate that flavone generates significant antihypertensive activity by vasorelaxation.</p> Graphical Abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Preclinical Exploration of 2-Phenyl-1-benzopyran-4-one as a Potential Antihypertensive Agent

  • 期刊论文

  • 发表日期：

    2025年3月25日

查看全文
  • Luis Arias-Durán,
  • Samuel Estrada-Soto,
  • Emmanuel Gaona-Tovar,
  • César Millán-Pacheco,
  • Rafael Villalobos-Molina,
  • Erandi Ortiz-Barragán,
  • Jacqueline R. Del Villar Licona,
  • Julio C. Almanza-Pérez

摘要

Flavonoids have diverse pharmacological effects, such as the relaxant action on the vascular smooth muscle. In the present research, we determined the functional mode of action of the 2-phenyl-1-benzopyran-4-one or flavone, to be used as a prototype to obtain new drugs for treating arterial hypertension. For this, an ex vivo model of isolated rat aortic rings, an in silico approach, an in vivo assay on spontaneously hypertensive rats, and an acute oral toxicity test were used. The results showed a significant vasorelaxant action of 2-phenyl-1-benzopyran-4-one in rings with (E +) and without (E-) endothelium in a concentration-dependent manner, being more potent in the presence of endothelium (p < 0.05). The observed functional mode of action indicated that relaxant action is related to nitric oxide (NO) production and calcium channel blockade, which was corroborated by docking studies. Finally, intragastric administration of 2-phenyl-1-benzopyran-4-one (50 mg/kg) significantly decreased systolic and diastolic blood pressure and showed no in vivo acute toxicity. These results demonstrate that flavone generates significant antihypertensive activity by vasorelaxation.

Graphical Abstract