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胡椒叶甲醇提取物在大鼠膈神经-半膈肌标本中的神经肌肉阻滞活性。

Neuromuscular blocking activity of methanolic extract of Piper sarmentosum leaves in the rat phrenic nerve-hemidiaphragm preparation.

作者信息

Ridtitid W, Rattanaprom W, Thaina P, Chittrakarn S, Sunbhanich M

机构信息

Department of Pharmacology, Faculty of Science, Prince of Songkla University, Hat Yai, Thailand.

出版信息

J Ethnopharmacol. 1998 Jun;61(2):135-42. doi: 10.1016/s0378-8741(98)00025-7.

Abstract

Methanolic extract of Piper sarmentosum Roxb. (Piperaceae) leaves was studied for the neuromuscular blocking activity in rat phrenic nerve-hemidiaphragm preparations. The plant extract, at concentrations of 3.2, 4.0, 4.8 and 6.4 mg/ml, exhibited an initially transient increase in twitch tension which was followed by a marked dose-related neurally-evoked twitch depression. The neuromuscular blocking effect produced by the plant extract was compared with d-tubocurarine (dTC) and succinylcholine (SCh). The EC50 for neurally-evoked twitch depression of the extract, dTC and SCh was 4.07 mg/ml, 1.1 microM and 15 microM, respectively. The neurally-evoked twitch depression produced by the extract was partially antagonized by tetraethylammonium (TEA) but not by neostigmine (NS). These findings suggested that the plant extract possessed a marked neuromuscular blocking activity at the neuromuscular junction and a possible mechanism which was likely to inhibit neurotransmitter (acetylcholine) release at the presynaptic terminal.

摘要

对胡椒科荜茇叶的甲醇提取物在大鼠膈神经 - 半膈肌标本中的神经肌肉阻断活性进行了研究。该植物提取物在浓度为3.2、4.0、4.8和6.4mg/ml时,最初表现为抽搐张力短暂增加,随后出现明显的剂量相关的神经诱发抽搐抑制。将该植物提取物产生的神经肌肉阻断作用与筒箭毒碱(dTC)和琥珀酰胆碱(SCh)进行了比较。提取物、dTC和SCh对神经诱发抽搐抑制的半数有效浓度(EC50)分别为4.07mg/ml、1.1μM和15μM。提取物产生的神经诱发抽搐抑制作用部分被四乙铵(TEA)拮抗,但不被新斯的明(NS)拮抗。这些发现表明,该植物提取物在神经肌肉接头处具有明显的神经肌肉阻断活性,其可能的机制是抑制突触前终末神经递质(乙酰胆碱)的释放。

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