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Lipid emulsion inhibits vasodilation induced by a toxic dose of bupivacaine by suppressing bupivacaine-induced PKC and CPI-17 dephosphorylation but has no effect on vasodilation induced by a toxic dose of mepivacaine
The Korean Journal of Pain ; : 229-238, 2016.
Article en En | WPRIM | ID: wpr-130327
Biblioteca responsable: WPRO
ABSTRACT
BACKGROUND: The goal of this in vitro study was to investigate the effect of lipid emulsion on vasodilation caused by toxic doses of bupivacaine and mepivacaine during contraction induced by a protein kinase C (PKC) activator, phorbol 12,13-dibutyrate (PDBu), in an isolated endothelium-denuded rat aorta. METHODS: The effects of lipid emulsion on the dose-response curves induced by bupivacaine or mepivacaine in an isolated aorta precontracted with PDBu were assessed. In addition, the effects of bupivacaine on the increased intracellular calcium concentration ([Ca²⁺]ᵢ) and contraction induced by PDBu were investigated using fura-2 loaded aortic strips. Further, the effects of bupivacaine, the PKC inhibitor GF109203X and lipid emulsion, alone or in combination, on PDBu-induced PKC and phosphorylation-dependent inhibitory protein of myosin phosphatase (CPI-17) phosphorylation in rat aortic vascular smooth muscle cells (VSMCs) was examined by western blotting. RESULTS: Lipid emulsion attenuated the vasodilation induced by bupivacaine, whereas it had no effect on that induced by mepivacaine. Lipid emulsion had no effect on PDBu-induced contraction. The magnitude of bupivacaine-induced vasodilation was higher than that of the bupivacaine-induced decrease in [Ca²⁺]ᵢ. PDBu promoted PKC and CPI-17 phosphorylation in aortic VSMCs. Bupivacaine and GF109203X attenuated PDBu-induced PKC and CPI-17 phosphorylation, whereas lipid emulsion attenuated bupivacaine-mediated inhibition of PDBu-induced PKC and CPI-17 phosphorylation. CONCLUSIONS: These results suggest that lipid emulsion attenuates the vasodilation induced by a toxic dose of bupivacaine via inhibition of bupivacaine-induced PKC and CPI-17 dephosphorylation. This lipid emulsion-mediated inhibition of vasodilation may be partly associated with the lipid solubility of local anesthetics.
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Texto completo: 1 Base de datos: WPRIM Asunto principal: Aorta / Fosforilación / Solubilidad / Vasodilatación / Técnicas In Vitro / Proteína Quinasa C / Bupivacaína / Forbol 12,13-Dibutirato / Western Blotting / Calcio Límite: Animals Idioma: En Revista: The Korean Journal of Pain Año: 2016 Tipo del documento: Article
Texto completo: 1 Base de datos: WPRIM Asunto principal: Aorta / Fosforilación / Solubilidad / Vasodilatación / Técnicas In Vitro / Proteína Quinasa C / Bupivacaína / Forbol 12,13-Dibutirato / Western Blotting / Calcio Límite: Animals Idioma: En Revista: The Korean Journal of Pain Año: 2016 Tipo del documento: Article