Melo PA, Pinheiro DA, Ricardo HD, Fernandes FF, Tomaz MA, El-Kik CZ, Strauch MA, da Fonseca TF, Sifuentes DN, Calil-Elias S, Buarque CD, Brito FV, Costa PR, Da Silva AJ
Ability of a Synthetic Coumestan to Antagonize Bothrops Snake Venom Activities. [JOURNAL ARTICLE]
Toxicon 2009 Oct 30.
We investigated a synthetic coumestan named LQB93 and similar compounds abilities to antagonize activities of Bothrops jararacussu and Bothrops jararaca crude venoms in different protocols. The anti-myotoxic activity was evaluated in vitro by the rate of release of creatine kinase (CK) from isolated mouse extensor digitorum longus muscle (EDL) induced by B. jararacussu (25 mg/ml). For in vivo studies, B. jararacussu venom (1.0mg/kg) was pre-incubated with LQB93 (0.1-30 mg/kg), during 30min, for later injection in mouse tight and evaluation of the anti-myotoxic and antiedematogenic effects. LQB93 antagonized in vitro, the increase of CK release from the EDL muscle (IC50=0.0291mM). It also showed in vivo, anti-myotoxic and anti-edematogenic effects that were dosedependent with ID50 of 0.17mg/kg and 0.14mg/kg, respectively. The hemorrhage induced by B.jararaca (1.0mg/kg) venom in the mouse skin, was abolished by LQB93 (10.0mg/kg) pre-incubated with venom. Like wedelolactone, LQB93 protected rat isolated heart on a Langendorff preparation, from the cardiotoxicity of B. jararacussu venom. LQB93 inhibit the effects of Bothrops venoms like wedelolactone, a natural compound isolated from the plant Eclipta prostrata.
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