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在小鼠神经肌肉标本中,用野生嘉赐树(大风子科)水提取物对蛇毒磷脂酶A2毒素进行中和作用。

Neutralization of snake venom phospholipase A2 toxins by aqueous extract of Casearia sylvestris (Flacourtiaceae) in mouse neuromuscular preparation.

作者信息

Cavalcante Walter L G, Campos Tayná O, Dal Pai-Silva Maeli, Pereira Paulo S, Oliveira Clayton Z, Soares Andreimar M, Gallacci Márcia

机构信息

Departamento de Farmacologia, Instituto de Biociências, Universidade Estadual Paulista, UNESP, Botucatu, SP, Brazil.

出版信息

J Ethnopharmacol. 2007 Jul 25;112(3):490-7. doi: 10.1016/j.jep.2007.04.002. Epub 2007 Apr 24.

Abstract

Aqueous extract of Casearia sylvestris (Flacourtiaceae) has been shown to inhibit enzymatic and biological properties of some Bothrops and Crotalus venoms and their purified phospholipase A(2) (PLA(2)) toxins. In this work we evaluated the influence of C. sylvestris aqueous extract upon neuromuscular blocking and muscle damaging activities of some PLA(2)s (crotoxin from C. durissus terrificus, bothropstoxin-I from B. jararacussu, piratoxin-I from B. pirajai and myotoxin-II from B. moojeni) in mouse phrenic-diaphragm preparations. Crotoxin (0.5 microM) and all other PLA(2) toxins (1.0 microM) induced irreversible and time-dependent blockade of twitches. Except for crotoxin, all PLA(2) toxins induced significant muscle damage indices, assessed by microscopic analysis. Preincubation of bothropstoxin-I, piratoxin-I or myotoxin-II with C. sylvestris extract (1:5 (w/w), 30 min, 37 degrees C) significantly prevented the neuromuscular blockade of preparations exposed to the mixtures for 90 min; the extent of protection ranged from 93% to 97%. The vegetal extract also neutralized the muscle damage (protection of 80-95%). Higher concentration of the C. sylvestris extract (1:10, w/w) was necessary to neutralize by 90% the neuromuscular blockade induced by crotoxin. These findings expanded the spectrum of C. sylvestris antivenom activities, evidencing that it may be a good source of potentially useful PLA(2) inhibitors.

摘要

已证明野鸦椿(大风子科)水提取物可抑制某些矛头蝮属和响尾蛇属蛇毒及其纯化的磷脂酶A2(PLA2)毒素的酶活性和生物学特性。在本研究中,我们评估了野鸦椿水提取物对小鼠膈-膈肌制备物中某些PLA2(巴西矛头蝮的响尾蛇毒素、巴西矛头蝮的矛头蝮毒素-I、皮氏矛头蝮的皮氏蝰毒素-I和莫氏矛头蝮的肌毒素-II)的神经肌肉阻断和肌肉损伤活性的影响。响尾蛇毒素(0.5微摩尔)和所有其他PLA2毒素(1.0微摩尔)诱导不可逆且时间依赖性的抽搐阻断。除响尾蛇毒素外,所有PLA2毒素通过显微镜分析评估均诱导了显著的肌肉损伤指数。将矛头蝮毒素-I、皮氏蝰毒素-I或肌毒素-II与野鸦椿提取物(1:5(w/w),30分钟,37℃)预孵育,可显著预防暴露于混合物90分钟的制备物的神经肌肉阻断;保护程度为93%至97%。植物提取物还中和了肌肉损伤(保护率为80-95%)。需要更高浓度的野鸦椿提取物(1:10,w/w)才能将响尾蛇毒素诱导的神经肌肉阻断中和90%。这些发现扩展了野鸦椿抗蛇毒活性的范围,表明它可能是潜在有用PLA2抑制剂的良好来源。

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