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叶下珠甲素和乙素对肾上腺素能及胆碱能受体的作用。

Effect of cleistanthin A and B on adrenergic and cholinergic receptors.

作者信息

Parasuraman S, Raveendran R

机构信息

Department of Pharmacology, Jawaharlal Institute of Postgraduate Medical Education and Research, Pondicherry, India.

出版信息

Pharmacogn Mag. 2011 Jul;7(27):243-7. doi: 10.4103/0973-1296.84239.

DOI:10.4103/0973-1296.84239
PMID:21969796
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3173900/
Abstract

OBJECTIVE

The aim was to study the in vitro and in silico interactions of cleistanthin A and B on the adrenergic and cholinergic receptors using isolated animal tissues and bioinformatics tools.

MATERIALS AND METHODS

The alpha adrenergic receptor activities of cleistanthin A and B were studied in vitro using a guinea pig vas deferens preparation. The beta adrenergic receptor activities of cleistanthin A and B on an isolated rat heart were studied in vitro using a modified Langendorff apparatus. The effects of cleistanthin A and B on the nicotinic and muscarinic cholinergic receptors were studied in vitro using rabbit vas deferens and rabbit jejunum, respectively. All the drug responses were recorded using a data acquisition system through a variable force transducer. The receptor-ligand interactions of cleistanthin A and B with adrenergic and cholinergic receptor proteins were determined using the ArgusLab molecular modeling and drug docking program.

RESULTS

Cleistanthin A and B significantly inhibited the actions of the alpha adrenergic receptor and the nicotinic cholinergic receptor. Cleistanthin A and B shifted the dose-response curve to the right with an increased EC(50) value of phenylephrine and acetylcholine. Both cleistanthin A and B did not have any significant effect on the beta adrenergic and muscarinic cholinergic receptors.

CONCLUSION

Cleistanthin A and B block the alpha adrenergic and nicotinic cholinergic receptors, but these compounds do not interact at all with the beta adrenergic and muscarinic cholinergic receptors.

摘要

目的

旨在利用分离的动物组织和生物信息学工具研究克利斯坦辛A和B与肾上腺素能和胆碱能受体的体外及计算机模拟相互作用。

材料与方法

使用豚鼠输精管制备物体外研究克利斯坦辛A和B的α肾上腺素能受体活性。使用改良的Langendorff装置体外研究克利斯坦辛A和B对离体大鼠心脏的β肾上腺素能受体活性。分别使用兔输精管和兔空肠体外研究克利斯坦辛A和B对烟碱型和毒蕈碱型胆碱能受体的影响。所有药物反应均通过可变力换能器使用数据采集系统进行记录。使用ArgusLab分子建模和药物对接程序确定克利斯坦辛A和B与肾上腺素能和胆碱能受体蛋白的受体-配体相互作用。

结果

克利斯坦辛A和B显著抑制α肾上腺素能受体和烟碱型胆碱能受体的作用。克利斯坦辛A和B使去氧肾上腺素和乙酰胆碱的剂量-反应曲线右移，且其半数有效浓度（EC50）值增加。克利斯坦辛A和B对β肾上腺素能和毒蕈碱型胆碱能受体均无显著影响。

结论

克利斯坦辛A和B阻断α肾上腺素能和烟碱型胆碱能受体，但这些化合物与β肾上腺素能和毒蕈碱型胆碱能受体完全不相互作用。

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