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白皮杉醇多酚混合物对血管的影响:α-肾上腺素受体亚型的作用。

Vascular effects of a polyphenolic fraction from L.: role of α-adrenergic receptors Sub-types.

机构信息

Laboratory of Pharmacology and Pharmaceutical Care, Faculty of Pharmacy University of Coimbra, Coimbra, Portugal.

Coimbra Institute for Clinical and Biomedical Research (iCBR), Faculty of Medicine, University of Coimbra, Coimbra, Portugal.

出版信息

Nat Prod Res. 2020 Dec;34(23):3369-3372. doi: 10.1080/14786419.2018.1564291. Epub 2019 Jan 30.

Abstract

L. is a plant of the family, from which several compounds have been previously identified. Recently, we showed that an L. extract inhibits the vasopressor effect of noradrenaline. In this work we aimed to explore the mechanisms involved in this effect. The results confirmed that the flavonoid fraction present in the extract inhibits noradrenaline-induced contractions and that this effect is concentration-dependent. Also, a parallel shift to the right in the noradrenaline concentration-response curve was observed, suggesting a decrease in efficacy and also in potency. Together these results support the assumption that the extract could exert a non-competitive antagonism on the α-adrenergic receptors. However, experiments in the presence of competitive antagonists for α-adrenergic receptor sub-types (i.e. prazosin, yohimbine and phentolamine) showed that the effect may not be directly mediated by α-adrenergic receptors. Thus, the interaction of this extract with the adrenergic system remains to be confirmed.

摘要

L. 是科的一种植物,先前已经从该科中鉴定出几种化合物。最近,我们发现 L. 提取物可抑制去甲肾上腺素的升压作用。在这项工作中,我们旨在探讨涉及这种作用的机制。结果证实,提取物中存在的类黄酮部分可抑制去甲肾上腺素引起的收缩,并且这种作用呈浓度依赖性。此外,还观察到去甲肾上腺素浓度-反应曲线的平行右移,表明效力和效价均降低。这些结果共同支持提取物可能对α-肾上腺素能受体发挥非竞争性拮抗作用的假设。然而,在存在α-肾上腺素能受体亚型的竞争性拮抗剂(即哌唑嗪、育亨宾和酚妥拉明)的情况下进行的实验表明,这种作用可能不是直接由α-肾上腺素能受体介导的。因此,这种提取物与肾上腺素能系统的相互作用仍有待证实。

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