Qu Jingtian, Liu Fang, Zhang Xuezhu, Wang Jialong
First Teaching Hospital of Tianjin University of Traditional Chinese Medicine, 314 Anshanxi Road, Nankai District, Tianjin 300193, China.
Guang'anmen Hospital, China Academy of Chinese Medical Sciences, 5 Beixiange, Xicheng District, Beijing 100053, China.
Evid Based Complement Alternat Med. 2020 Jan 30;2020:9257950. doi: 10.1155/2020/9257950. eCollection 2020.
Oroxylin A, a flavonoid, is naturally produced in many medicinal plants. Our previous study identified it as a phytoestrogen. Based on this, the present study investigated its vasoconstriction reducing effects and whether the action was mediated by the estrogen receptor (ER) signal pathway. Long-term in vitro treatment with oroxylin A reduced Ach-induced vasorelaxation and NE-mediated or KCl-mediated contractile responses in rat aortic rings. These effects were interfered by an ER inhibitor ICI 182,780. Rat cardiac microvascular endothelial cells (CMECs) and aortic vascular smooth muscle cells (VSMCs) were used to study the possible underlying mechanisms. Oroxylin A activated the ER signal pathway. In CMECs, it increased NO production and eNOS protein expression. In VSMCs, it promoted NO production and iNOS protein expression. These effects were also inhibited by ICI 182,780. Besides, oroxylin A stimulated ER and ER protein expression in CMECs and VSMCs. All these findings suggest that the ER signal pathway takes part in the vasoconstriction reducing effects of oroxylin A.
木犀草素A是一种黄酮类化合物,在许多药用植物中天然产生。我们之前的研究将其鉴定为一种植物雌激素。基于此,本研究调查了其降低血管收缩的作用以及该作用是否由雌激素受体(ER)信号通路介导。用木犀草素A进行长期体外处理可降低乙酰胆碱诱导的大鼠主动脉环血管舒张以及去甲肾上腺素介导或氯化钾介导的收缩反应。这些作用受到ER抑制剂ICI 182,780的干扰。使用大鼠心脏微血管内皮细胞(CMECs)和主动脉血管平滑肌细胞(VSMCs)来研究可能的潜在机制。木犀草素A激活了ER信号通路。在CMECs中,它增加了一氧化氮(NO)的产生和内皮型一氧化氮合酶(eNOS)蛋白表达。在VSMCs中,它促进了NO的产生和诱导型一氧化氮合酶(iNOS)蛋白表达。这些作用也受到ICI 182,780的抑制。此外,木犀草素A刺激了CMECs和VSMCs中的ER和ER蛋白表达。所有这些发现表明,ER信号通路参与了木犀草素A降低血管收缩的作用。