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亚马逊植物Humirianthera ampla 提取物及其成分的抗蛇毒活性。

Antiophidic activity of the extract of the Amazon plant Humirianthera ampla and constituents.

机构信息

Instituto de Ciências Biomédicas, Centro de Ciências da Saúde, Universidade Federal do Rio de Janeiro, Avenida Brigadeiro Trompowski, Rio de Janeiro, RJ 21941-590, Brazil.

出版信息

J Ethnopharmacol. 2013 Jan 9;145(1):50-8. doi: 10.1016/j.jep.2012.10.033. Epub 2012 Nov 1.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Although serotherapy against snakebite has been discovered more than one hundred years ago, antivenom is not available all over Brazil. The use of plants from folk medicine is common mainly in the Brazilian Amazon area. One of these plants is named Humirianthera ampla (HA).

MATERIALS AND METHODS

We have investigated HA extract and constituents' antiophidic activity in different experimental protocols against some Bothrops snake venoms (Bothrops jararacussu, Bothrops atrox and Bothrops jararaca). The protocols investigated include phospholipase, proteolytic, pro-coagulant, hemorrhagic, edematogenic and myotoxic activities induced by these venoms in Swiss mice.

RESULTS

All the venoms caused an increase in the rate of creatine kinase (CK) release from isolated muscles, indicating damage to the sarcolemma. The crude extract of HA decreased the myotoxic activity in a concentration-dependent fashion. The presence of HA 300 μg/mL decreased up to 96% of Bothrops jararacussu and 94% of Bothrops atrox myotoxicity after 90 min of exposure. In vivo myotoxicity of Bothrops atrox venom was decreased in 75% when the venom was preincubated with HA 500 mg/kg. Similar results were observed with lupeol against Bothrops jararacussu and Bothrops atrox venoms. The hemorrhagic activity was evaluated by intradermal injection of Bothrops atrox venom. Preincubation and oral pre- and posttreatment with HA decreased hemorrhage by 100%, 45% and 45%, respectively. Bothrops atrox venom also induced formation of edema, which was significantly inhibited by pre- and posttreatment with HA. All the venoms showed extensive pro-coagulating properties, and these activities were inhibited by up to 90% with HA, which presented concentration-dependent inhibition. Finally, proteolytic and phospholipase activities of the venoms were all inhibited by increasing concentrations of HA, lupeol and sitosterol. The inhibition of these activities might help explain the actions against in vivo myotoxicity and the in vivo effects observed, i.e., edema, myotoxicity, pro-coagulation and hemorrhage.

CONCLUSIONS

Altogether, our results give support for the popular use of HA extracts in cases of accidents with snakes, suggesting that it can be used as an adjunct in the management of venomous snakebites.

摘要

民族药理学相关性

尽管抗蛇毒血清已经被发现超过一百年了,但在巴西并不是所有地方都能获得抗蛇毒血清。使用民间医学中的植物是很常见的,特别是在巴西亚马逊地区。其中一种植物被称为 Humirianthera ampla(HA)。

材料和方法

我们已经研究了 HA 提取物及其成分对几种矛头蝮蛇毒液(巴西矛头蝮,矛头蝮和矛头蝮)的抗蛇毒活性。研究的方案包括磷脂酶、蛋白水解酶、促凝、出血、水肿和肌毒性活性,这些毒液会在瑞士小鼠中引起这些活性。

结果

所有毒液都导致从分离的肌肉中肌酸激酶(CK)释放率增加,表明肌膜受损。HA 的粗提物以浓度依赖的方式降低肌毒性活性。HA 300μg/mL 的存在使巴西矛头蝮和矛头蝮的肌毒性分别降低了 96%和 94%,暴露 90 分钟后。当毒液与 500mg/kg 的 HA 预孵育时,矛头蝮毒液的体内肌毒性降低了 75%。用羽扇豆醇处理巴西矛头蝮和矛头蝮毒液也观察到了类似的结果。通过皮内注射巴西矛头蝮毒液评估出血活性。HA 的预孵育和口服预治疗和后治疗分别使出血减少了 100%、45%和 45%。矛头蝮毒液还引起水肿形成,HA 的预治疗和后治疗显著抑制了水肿形成。所有毒液都显示出广泛的促凝特性,HA 可将这些活性抑制高达 90%,呈浓度依赖性抑制。最后,HA、羽扇豆醇和谷甾醇的浓度增加抑制了毒液的蛋白水解酶和磷脂酶活性。这些活性的抑制可能有助于解释体内肌毒性和体内观察到的水肿、肌毒性、促凝血和出血的作用。

结论

总的来说,我们的结果为 HA 提取物在蛇咬伤事故中的广泛使用提供了支持,表明它可作为毒蛇咬伤管理的辅助手段。

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