Possible regulation of P-glycoprotein function by adrenergic agonists in a vascular-luminal perfused preparation of small intestine.
Possible regulation of P-glycoprotein function by adrenergic agonists in a vascular-luminal perfused preparation of small intestine.
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小肠血管腔灌注制剂中肾上腺素能激动剂对 P-糖蛋白功能的可能调节。
DOI：
10.1016/j.xphs.2021.09.014
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发表时间：
2022
影响因子：
3.8
通讯作者：
Kazutaka Higaki
中科院分区：
文献类型：
--
作者：
Hironori Mukai;Masashi Takanashi;Ken-ichi Ogawara;Masato Maruyama;Kazutaka Higaki
虽然小肠的功能主要受肠神经系统（enteric nervous system，ENS）和中枢神经系统（central nervous system，CNS）的调节，但小肠药物吸收的神经调节机制尚不清楚。为了获得一些信息，肾上腺素能激动剂对P-糖蛋白（P-gp）功能的影响，利用血管腔灌注大鼠小肠。肾上腺素显著减少罗丹明-123（R-123）向肠腔的分泌，而二丁酰cAMP（DBcAMP）显著增强R-123的分泌。奎尼丁的抑制研究清楚地表明，肾上腺素对R-123的分泌清除率降低或DBcAMP对R-123的分泌清除率升高分别归因于P-gp活性的降低或升高。P-gp在整个粘膜匀浆中的表达水平没有改变，在所有的任何化学物质检查，但那些刷状缘膜（BBM）的肠上皮细胞显着降低或增加肾上腺素或DBcAMP，分别。此外，肾上腺素能激动剂和DBcAMP引起的P-gp活性变化与BBM中P-gp表达水平的变化显着相关，表明P-gp从胞浆池向BBM的运输受到肾上腺素能激动剂和DBcAMP的调节。
Although the functions of small intestine are largely regulated by enteric nervous system (ENS), an independent intrinsic innervation, as well as central nervous system (CNS), the neural regulation of drug absorption from the small intestine still remains to be clarified. To obtain some information on it, the effect of adrenergic agonists on P-glycoprotein (P-gp) function was investigated by utilizing a vascular-luminal perfused rat small intestine. Adrenaline significantly decreased the secretion of rhodamine-123 (R-123) into the intestinal lumen, but dibutyryl cAMP (DBcAMP) significantly enhanced R-123 secretion. The inhibition study with quinidine clearly indicated that the decrease in secretory clearance of R-123 by adrenaline or the increase by DBcAMP would be attributed to the decrease or increase in P-gp activity, respectively. Expression levels of P-gp in whole mucosal homogenates were not changed at all by any chemicals examined, but those on brush border membrane (BBM) of intestinal epithelial cells were significantly decreased or increased by adrenaline or DBcAMP, respectively. Furthermore, changes in P-gp activity caused by adrenergic agonists and DBcAMP were significantly correlated with changes in expression level of P-gp in BBM, suggesting that the trafficking of P-gp from cytosolic pool to BBM would be regulated by adrenergic agonists and DBcAMP.
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影响因子：
29.4
作者：
Helen J. Cooke
通讯作者：
Helen J. Cooke
环核苷酸依赖性蛋白激酶抑制剂可防止上皮紧密连接的破坏
影响因子：
2.3
作者：
Cécile Klingler;U. Kniesel;S. Bamforth;H. Wolburg;B. Engelhardt;W. Risau
通讯作者：
W. Risau
细胞内介质和细胞骨架对肠道细胞旁通透性的调节。
影响因子：
2.1
作者：
M. Pérez;A. Barber;F. Ponz
通讯作者：
F. Ponz
肝 cAMP 的激素调节可预防雌二醇 17β-d-葡萄糖醛酸苷诱导的大鼠灌注肝脏胆汁淤积
影响因子：
3.1
作者：
A. Zucchetti;I. Barosso;Andrea C. Boaglio;M. Luquita;M. Roma;F. Crocenzi;E. J. Sánchez Pozzi
通讯作者：
E. J. Sánchez Pozzi
肠道“小脑”在水和电解质稳态中的作用1
DOI：
--
发表时间：
1989
期刊：
The FASEB Journal
影响因子：
--
作者：
H. Cooke
通讯作者：
H. Cooke