Cheng Ling, Pricolo Victor, Biancani Piero, Behar Jose
Department of Medicine, Rhode Island Hospital and Warren Alpert Medical School, Brown University, Providence, RI 02903, USA.
Am J Physiol Gastrointest Liver Physiol. 2008 Sep;295(3):G493-502. doi: 10.1152/ajpgi.90214.2008.
Colon muscle strips and cells from female patients with slow-transit constipation (STC) exhibit impaired motility, signal transduction abnormalities characterized by downregulation of Gq/11 and upregulation of Gs proteins, decreased cyclooxygenase (COX)-1 and thromboxane (Tx)B2 levels, increased COX-2 and PGE2 levels, and overexpression of progesterone receptors (PGR). Progesterone (P4) treatment of normal cells reproduced these motility and signal transduction abnormalities. The purpose of the study was to examine whether overexpression of PGR-B reproduces these abnormalities by rendering the cells more sensitive to physiological concentrations of P4. Cultured human colon muscle was transfected with a plasmid DNA expressing PGR-B. The mRNAs of PGR, COX-1, COX-2, and Gq/11 were determined by quantitative real-time PCR. Their protein expression was determined by Western blot, and prostaglandins were measured by radioimmunoassay. Cultured muscle cells maintained their phenotypic features determined with myosin light chain (MLC) and h-caldesmon antibodies. Control and transfected muscle cells responded to 10(-6) M P4. In contrast, muscle cells transfected with PGR-B responded to lower P4 concentration (10(-7) M). This P4 concentration reduced MLC phosphorylation induced by CCK-8 (10(-8) M), downregulated Gq/11, and decreased COX-1 and TxB2 levels. It upregulated Gs proteins. It also increased COX-2 and PGE2 levels. We conclude that overexpression of PGR-B renders the cells more sensitive to physiological concentrations of P4. These results are consistent with the hypothesis that overexpression of PGR-B contributes to the motility and signal transduction abnormalities observed in female patients with STC and normal serum levels of P4.
慢传输型便秘(STC)女性患者的结肠肌条和细胞表现出运动功能受损、信号转导异常,其特征为Gq/11下调和Gs蛋白上调、环氧化酶(COX)-1和血栓素(Tx)B2水平降低、COX-2和前列腺素E2(PGE2)水平升高以及孕激素受体(PGR)过表达。用孕激素(P4)处理正常细胞可重现这些运动和信号转导异常。本研究的目的是检验PGR-B的过表达是否通过使细胞对生理浓度的P4更敏感来重现这些异常。用表达PGR-B的质粒DNA转染培养的人结肠肌。通过定量实时PCR测定PGR、COX-1、COX-2和Gq/11的mRNA。通过蛋白质印迹法测定它们的蛋白表达,并用放射免疫分析法测量前列腺素。培养的肌细胞保持了用肌球蛋白轻链(MLC)和h-钙调蛋白抗体确定的表型特征。对照和转染的肌细胞对10⁻⁶ M P4有反应。相比之下,用PGR-B转染的肌细胞对较低的P4浓度(10⁻⁷ M)有反应。该P4浓度降低了由胆囊收缩素-8(CCK-8,10⁻⁸ M)诱导的MLC磷酸化,下调了Gq/11,并降低了COX-1和TxB2水平。它上调了Gs蛋白。它还增加了COX-2和PGE2水平。我们得出结论,PGR-B的过表达使细胞对生理浓度的P4更敏感。这些结果与以下假设一致,即PGR-B的过表达导致在血清P4水平正常的STC女性患者中观察到的运动和信号转导异常。