Snake venom PLA2s inhibitors isolated from Brazilian plants: synthetic and natural molecules.

Snake venom PLA2s inhibitors isolated from Brazilian plants: synthetic and natural molecules.
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DOI:
10.1155/2013/153045
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发表时间:
2013
影响因子:
--
通讯作者:
Marchi-Salvador DP
Marchi-Salvador DP
中科院分区:
生物学3区
文献类型:
--
作者:
Carvalho BM;Santos JD;Xavier BM;Almeida JR;Resende LM;Martins W;Marcussi S;Marangoni S;Stábeli RG;Calderon LA;Soares AM;Da Silva SL;Marchi-Salvador DP

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蛇类毒液蛰入是巴西和其他南美国家的一个重要健康问题。在民间医学中,特别是在发展中国家,在缺乏及时获得血清治疗的社区,几种植物物种被用于治疗蛇咬伤。然而,鉴定和表征能够抑制蛇毒活性的几种新植物或其分离的化合物的作用是极其重要的,此类研究是必要的。蛇毒含有多种有机和无机化合物;磷脂酶A2(PLA 2)是蛇毒的主要毒性成分之一。PLA 2具有广泛的药理学活性,如神经毒性、肌肉毒性、心脏毒性、抗凝、出血和水肿诱导作用。PLA 2抑制具有药理学和治疗学意义,因为这些酶参与几种炎性疾病。本文综述了几项研究的结果,植物提取物及其分离的有效成分,当用于对粗蛇毒或其有毒馏分。分离的抑制剂,如类固醇、萜类化合物和酚类化合物,能够抑制来自不同蛇毒的PLA 2。PLA 2特异性抑制剂的设计可能有助于开发新的药物,更特异的抗蛇毒血清,甚至作为治疗蛇咬伤的替代方法。
Ophidian envenomation is an important health problem in Brazil and other South American countries. In folk medicine, especially in developing countries, several vegetal species are employed for the treatment of snakebites in communities that lack prompt access to serum therapy. However, the identification and characterization of the effects of several new plants or their isolated compounds, which are able to inhibit the activities of snake venom, are extremely important and such studies are imperative. Snake venom contains several organic and inorganic compounds; phospholipases A2 (PLA2s) are one of the principal toxic components of venom. PLA2s display a wide variety of pharmacological activities, such as neurotoxicity, myotoxicity, cardiotoxicity, anticoagulant, hemorrhagic, and edema-inducing effects. PLA2 inhibition is of pharmacological and therapeutic interests as these enzymes are involved in several inflammatory diseases. This review describes the results of several studies of plant extracts and their isolated active principles, when used against crude snake venoms or their toxic fractions. Isolated inhibitors, such as steroids, terpenoids, and phenolic compounds, are able to inhibit PLA2s from different snake venoms. The design of specific inhibitors of PLA2s might help in the development of new pharmaceutical drugs, more specific antivenom, or even as alternative approaches for treating snakebites.
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