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百里香中黄酮类化合物的解痉活性。

Spasmolytic activity of the flavonoids from Thymus vulgaris.

作者信息

Van Den Broucke C O, Lemli J A

出版信息

Pharm Weekbl Sci. 1983 Feb 25;5(1):9-14. doi: 10.1007/BF01959645.

Abstract

Flavonoids from Thymus vulgaris L. have been studied in vitro for spasmolytic activity on the smooth muscles of the guinea-pig ileum and trachea and of the rat vas deferens. The flavones and thyme extracts inhibit responses to agonists which stimulate specific receptors (acetylcholine, histamine, L-noradrenaline) as well as to agents whose actions are not mediated via specific receptors (BaCl2). Cumulative dose-response curves point to a non-competitive antagonism. Inhibition of Ca2+ contractions on K+ depolarized smooth muscles suggest inhibition of availability of Ca2+ for muscle contraction. pD'2 values were determined to compare the potency of these components to each other and to standard drugs. Flavones induce relaxation of the carbachol contracted tracheal strip without stimulation of the beta 2-receptors, which were blocked by propranolol.

摘要

对百里香中的类黄酮进行了体外研究,以观察其对豚鼠回肠、气管以及大鼠输精管平滑肌的解痉活性。黄酮类化合物和百里香提取物可抑制对刺激特定受体的激动剂(乙酰胆碱、组胺、L-去甲肾上腺素)以及作用不通过特定受体介导的药物(氯化钡)的反应。累积剂量-反应曲线表明存在非竞争性拮抗作用。对钾离子去极化平滑肌上钙离子收缩的抑制表明其抑制了钙离子用于肌肉收缩的可用性。测定了pD'2值以比较这些成分彼此之间以及与标准药物的效力。黄酮类化合物可使卡巴胆碱收缩的气管条松弛,且不刺激被普萘洛尔阻断的β2受体。

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