囊性纤维化跨膜传导调节因子抑制药在分泌性腹泻中的应用研究进展

Application Progress in CFTR Inhibitors in the Treatment of Secretory Diarrhea

分泌性腹泻威胁着全球健康,是儿童发病和死亡的主要原因之一。肠上皮细胞腔内Cl-通道激活导致肠道液体过度分泌是肠毒素引起腹泻的主要原因。在霍乱及其他细菌肠毒素引发的腹泻中,囊性纤维化跨膜传导调节因子(cystic fibrosis transmembrane conductance regulator,CFTR)是主要的c AMP-调节Cl-通道,其主要功能是促进上皮细胞液体分泌。利用肠上皮细胞CFTR抑制药抗分泌性腹泻是一种新途径。已有的CFTR抑制药有噻唑啉酮类、甘氨酸酰肼类和喹喔啉二酮等。同时,从天然植物中提取分离的一些成分也具有CFTR抑制作用,但研究还不够深入。因此,对CFTR抑制药的研究进展进行了综述。

Secretory diarrhea provides a major health challenge worldwide, which is one of the most important reasons for children morbidity and death. The activation of Cl- channels in intestinal epithelial cells resulting in the excessive fluid secretion in the intestine is the main reason of diarrhea caused by enterotoxins. In diarrhea caused by cholera and the other bacterial enterotoxins, cystic fibrosis transmembrane conductance regulator （ CFTR） is the main cAMP-control Cl- channel to promote the fluid secretion in epithelial cells. Therefore, CFTR inhibitors are the new choices for secretory diarrhea. CFTR inhibitors include thiazolidinone, glycine hydrazide and quinoxalinedione chemical classes, and some components from natural plants also exhibit CFTR inhibition activity, however, further studies should be done.