磷酸二酯酶的抑制对雌激素抑制血管平滑肌细胞中胶原蛋白合成的能力具有累加效应。

Inhibition of phosphodiesterase has an additive effect on estrogen's ability to inhibit collagen synthesis in vascular smooth muscle cells.

作者信息

Dimopoulos George J, Langner Ronald O

机构信息

Department of Pharmaceutical Sciences, School of Pharmacy, University of Connecticut, Storrs, CT, United States.

出版信息

Vascul Pharmacol. 2009 Jan-Feb;50(1-2):78-82. doi: 10.1016/j.vph.2008.10.003. Epub 2008 Oct 31.

DOI:10.1016/j.vph.2008.10.003

PMID:19007913

Abstract

Several studies have shown that estrogen has the ability to decrease collagen synthetic rates in vascular smooth muscle cells (VSMCs) by increasing cellular cyclic AMP (cAMP) levels. Phosphodiesterase inhibitors have also been shown to inhibit collagen synthesis in VSMCs presumably by preventing the degradation of cAMP. Since estrogens and phosphodiesterase inhibitors are used clinically, it is important to determine the potential for phosphodiesterase inhibitors to potentiate estrogen's ability to inhibit collagen synthesis in VSMCs. The results of the present study demonstrate that the phosphodiesterase inhibitors cilostamide and Ro-20-1724 had an additive effect on estrogen's ability to inhibit collagen synthesis in VSMC. Also, the data suggests that phosphodiesterase inhibitors mediated this additive effect by increasing cellular levels of cAMP.

摘要

多项研究表明，雌激素能够通过提高细胞内环磷酸腺苷（cAMP）水平来降低血管平滑肌细胞（VSMC）中的胶原蛋白合成速率。磷酸二酯酶抑制剂也已被证明可抑制VSMC中的胶原蛋白合成，推测其作用机制是阻止cAMP的降解。由于雌激素和磷酸二酯酶抑制剂都在临床中使用，因此确定磷酸二酯酶抑制剂增强雌激素抑制VSMC中胶原蛋白合成能力的可能性很重要。本研究结果表明，磷酸二酯酶抑制剂西洛酰胺和Ro-20-1724对雌激素抑制VSMC中胶原蛋白合成的能力具有相加作用。此外，数据表明磷酸二酯酶抑制剂通过提高细胞内cAMP水平介导了这种相加作用。