Neutralization of Apis mellifera bee venom activities by suramin

In this work we evaluated the ability of suramin, a polysulfonated naphthylurea derivative, to antagonize the cytotoxic and enzymatic effects of the crude venom of Apis mellifera. Suramin was efficient to decrease the lethality in a dose-dependent way. The hemo-concentration caused by lethal dose injection of bee venom was abolished by suramin (30 mu g/g). The edematogenic activity of the venom (0.3 mu g/g) was antagonized by suramin (10 mu g/g) in all treatment protocols. The changes in the vascular permeability caused by A. mellifera (1 mu g/g) venom were inhibited by suramin (30 mu g/g) in the pre- and post-treatment as well as when the venom was preincubated with suramin. In addition, suramin also inhibited cultured endothelial cell lesion, as well as in vitro myotoxicity, evaluated in mouse extensor digitorum longus muscle, which was inhibited by suramin (10 and 25 mu M), decreasing the rate of CM release, showing that suramin protected the sarcolemma against damage induced by components of bee venom (2.5 mu g/mL). Moreover, suramin inhibited the in vivo myotoxicity induced by i.m. injection of A. mellifera venom in mice (0.5 mu g/g). The analysis of the area under the plasma CK vs. time curve showed that preincubation, pre- and posttreatment with suramin (30 mu g/g) inhibited bee venom myotoxic activity in mice by about 89%, 45% and 40%, respectively. Suramin markedly inhibited the PLA(2) activity in a concentration-dependent way (1-30 mu M). Being suramin a polyanion molecule, the effects observed may be due to the interaction of its charges with the polycation components present in A. mellifera bee venom. (C) 2013 Elsevier Ltd. All rights reserved.