Bothrops jararacussu venom drastically decreases sarcoplasmic Ca(2+)-ATPase (SERCA) protein expression in vivo and inhibits its activity in vitro, in contrast to a slight increase of Na(+)/K(+)-ATPase expression in murine EDL. We investigated the effect of myotoxins bothropstoxin-I and/or -II (BthTX-I, BthTX-II and BthTX-I+II) on this model. No changes were seen in SERCA1, SERCA2 and Na(+)/K(+)-ATPase α1 protein expression as well as (2+)Ca-ATPase activity, but BthTX-II (1 μg/g) reduced Na(+)/K(+)-ATPase α2 expression by 50% one day after perimuscular injection. Interestingly, BthTX-II inhibited Ca(2+)-ATPase activity (IC50 around 6 nM). Our findings suggest that only BthTX-II affects ion transport ATPases, being a potent SERCA inhibitor and a putative target for antivenom drug development.
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http://dx.doi.org/10.1016/j.toxicon.2015.06.009 | DOI Listing |
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