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三萜皂苷,从大果豆科植物中分离出的新型金属蛋白酶蛇毒抑制剂。

Triterpenoid saponins, new metalloprotease snake venom inhibitors isolated from Pentaclethra macroloba.

作者信息

da Silva Jocivânia O, Fernandes Renata S, Ticli Fábio K, Oliveira Clayton Z, Mazzi Maurício V, Franco João J, Giuliatti Silvana, Pereira Paulo S, Soares Andreimar M, Sampaio Suely V

机构信息

Departamento de Análises Clínicas, Toxicológicas e Bromatológicas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, FCFRP, Universidade de São Paulo, USP, Ribeirão Preto-SP, Brazil.

出版信息

Toxicon. 2007 Aug;50(2):283-91. doi: 10.1016/j.toxicon.2007.03.024. Epub 2007 Apr 13.

DOI:10.1016/j.toxicon.2007.03.024
PMID:17517426
Abstract

We report here the antiproteolytic and antihemorrhagic properties of triterpenoid saponin inhibitors, named macrolobin-A and B, from Pentaclethra macroloba, against Bothrops snake venoms. The inhibitors were able to neutralize the hemorrhagic, fibrin(ogen)olytic, and proteolytic activities of class P-I and P-III metalloproteases isolated from B. neuwiedi and B. jararacussu venoms. Clotting and fibrinogenolytic activities induced by snake venoms and isolated thrombin-like enzymes were partially inhibited. Furthermore, the potential use of these inhibitors to complement antivenom therapy as an alternative treatment and/or used as molecular models for development of new therapeutical agents in the treatment of snake bite envenomations needs to be evaluated in future studies.

摘要

我们在此报告了从大果豆科植物中提取的三萜皂苷抑制剂——大叶相思素-A和B,对矛头蝮蛇毒的抗蛋白水解和抗出血特性。这些抑制剂能够中和从新维德矛头蝮和巴西矛头蝮蛇毒中分离出的P-I类和P-III类金属蛋白酶的出血、纤维蛋白(原)水解和蛋白水解活性。蛇毒和分离出的类凝血酶诱导的凝血和纤维蛋白原水解活性受到部分抑制。此外,这些抑制剂作为抗蛇毒血清疗法的补充替代治疗方法的潜在用途,以及用作开发治疗蛇咬伤中毒新治疗剂的分子模型,有待在未来的研究中进行评估。

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