Sakaguchi H, Anai N, Miyamoto A, Ishiguro S, Nishio A
Department of Veterinary Pharmacology, Faculty of Agriculture, Kagoshima University, Japan.
Jpn J Pharmacol. 1995 Jan;67(1):9-13. doi: 10.1254/jjp.67.9.
The mechanisms underlying the enhanced contractile response to phorbol 12,13-dibutyrate (PDBu) were examined in de-endothelialized thoracic aortas isolated from rats with dietary magnesium (Mg) deficiency. PDBu (1.0 nM)-induced contractions were significantly larger in Mg-deficient rats than in the controls. The contraction was completely inhibited by nifedipine, removal of external Ca2+ or by l-(5-isoquinolinesulfonyl)-2-methylpiperazine (H7). PDBu (1.0 nM) and phorbol 12-myristate 13-acetate (1.0 microM) significantly decreased the KD value and increased the Bmax for the binding of [3H]PN200-110 to the aortas. The degree of the decrease in the KD value was significantly greater in Mg-deficient rats than in the controls. The PDBu-induced decrease in the KD value was abolished by H7. These results suggest that activation of protein kinase C by phorbol esters may participate in the activation of L-type Ca2+ channels, which increases both the affinity of [3H]PN200-110 binding and the magnitude of the external Ca(2+)-dependent contraction. Dietary Mg-deficiency may enhance these processes.
在从饮食性镁(Mg)缺乏的大鼠分离的去内皮胸主动脉中,研究了对佛波醇12,13 - 二丁酸酯(PDBu)收缩反应增强的潜在机制。PDBu(1.0 nM)诱导的收缩在缺镁大鼠中比在对照组中显著更大。硝苯地平、去除细胞外Ca2+或1 -(5 - 异喹啉磺酰基)- 2 - 甲基哌嗪(H7)可完全抑制该收缩。PDBu(1.0 nM)和佛波醇12 - 肉豆蔻酸酯13 - 乙酸酯(1.0 microM)显著降低了[3H]PN200 - 110与主动脉结合的KD值并增加了Bmax。缺镁大鼠中KD值降低的程度比对照组显著更大。PDBu诱导的KD值降低被H7消除。这些结果表明,佛波醇酯激活蛋白激酶C可能参与L型Ca2+通道的激活,这增加了[3H]PN200 - 110结合的亲和力以及细胞外Ca(2+)依赖性收缩的幅度。饮食性镁缺乏可能会增强这些过程。