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Vasodilatory actions of xanthones isolated from a Tibetan herb, Halenia elliptica.

机译:从藏药哈伦氏菌中提取的黄酮的血管舒张作用。

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In this study, six major xanthones, isolated and identified from Halenia elliptica were investigated for their vasodilatory actions in isolated rat coronary artery. The xanthones, including 1-hydroxy-2,3,5-trimethoxy-xanthone (HM-1), 1-hydroxy-2,3,4,7-tetramethoxy-xanthone (HM-2), 1-hydroxy-2,3,4,5-tetramethoxy-xanthone (HM-3), 1,7-dihydroxy-2,3,4,5-tetramethoxy-xanthone (HM-4), 1,5-dihydroxy-2,3-dimethoxy-xanthone (HM-5) and 1,7-dihydroxy-2,3-dimethoxy-xanthone (HM-7) caused vasodilation in the coronary artery pre-contracted with 1 microM 5-hydroxytryptamine (5-HT), with EC(50) values ranging from 1.4+/-0.1 microM (HM-1) to 6.6+/-1.4 microM (HM-2). The EC(50) values of the other xanthones were between those of HM-1 and HM-2. Removal of endothelium of the coronary artery led to decreases in the vasorelaxant effects of HM-1, HM-7 but not HM-2, HM-3, HM-4 and HM-5. Our results showed that xanthones isolated from Halenia elliptica are vasoactive substances which exhibit either endothelium-dependent or endothelium-independent mechanisms in rat coronary artery. The potency and mechanism(s) of the vasorelaxant effects of these xanthones may be relevant to the structure-activity differences in the level and the position of the substituent groups with the primary xanthone structure.
机译:在这项研究中,调查了从椭圆形哈雷氏菌中分离并鉴定出的六种主要的氧杂蒽酮在离体大鼠冠状动脉中的血管舒张作用。氧杂蒽,包括1-羟基-2,3,5-三甲氧基-蒽酮(HM-1),1-羟基-2,3,4,7-四甲氧基-蒽酮(HM-2),1-羟基-2, 3,4,5-四甲氧基-an吨酮(HM-3),1,7-二羟基-2,3,4,5-四甲氧基-an吨酮(HM-4),1,5-二羟基-2,3-二甲氧基-黄酮(HM-5)和1,7-二羟基-2,3-二甲氧基-蒽酮(HM-7)导致与1 microM 5-羟色胺(5-HT)以及EC(50)预收缩的冠状动脉血管舒张)值范围从1.4 +/- 0.1 microM(HM-1)到6.6 +/- 1.4 microM(HM-2)。其他x吨的EC(50)值介于HM-1和HM-2之间。冠状动脉内皮的去除导致HM-1,HM-7的血管舒张作用降低,但HM-2,HM-3,HM-4和HM-5却没有降低。我们的结果表明,从椭圆形哈雷氏菌中分离出的氧杂蒽酮是血管活性物质,在大鼠冠状动脉中表现出内皮依赖性或内皮依赖性机制。这些氧杂蒽酮的血管舒张作用的效力和机理可能与具有初级x吨酮结构的取代基的水平和位置的结构活性差异有关。

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