Bastaki Salim M A, Chandranath Irwin S, Singh Jaipaul
Faculty of Medicine & Health Sciences, UAE University, P.O. Box-17666, Al Ain, United Arab Emirates.
Mol Cell Biochem. 2008 Feb;309(1-2):167-75. doi: 10.1007/s11010-007-9657-5. Epub 2007 Nov 28.
Proton pump inhibitors (PPIs) are widely used to treat hyperacid secretion and stomach ulcers. The study investigated the anti-secretory and anti-ulcer effects of esomeprazole, the S-isomer of omeprazole on dimaprit, histamine and dibutyryl adenosine 3, 5 cyclic monophosphate (dbcAMP)-evoked gastric acid secretion, acidified ethanol (AE) and indomethacin (INDO)-induced haemorrhagic lesions and on prostaglandin E2 (PGE2) level in the rat in vivo and rabbit in vitro preparations. The effect of omeprazole was also investigated for comparison. Dimaprit-induced acid secretion was significantly (P < 0.05) inhibited by both PPIs in a dose-dependent manner. In the isolated rabbit gastric glands, both PPIs elicited marked reductions in histamine- and dbcAMP-evoked acid secretion with similar potency. The lesions induced by either AE or INDO were significantly (P < 0.05) reduced in the presence of either esomeprazole or omeprazole compared to control values. Increasing doses of esomeprazole before AE treatment resulted in a marked degree of cytoprotection and an elevation in the concentration of bound PGE2 in the stomach tissue homogenate. The results show that esomeprazole and omeprazole were equally effective against gastric haemorrhagic lesions induced by either AE or INDO and in inhibiting dimaprit-, dbcAMP- and histamine-induced gastric acid secretion in the rat and rabbit stomach both in vivo and in vitro. The gastro-protective effect of esomeprazole was found to be proportional to the bound PGE2 levels in the glandular area of the stomach.
质子泵抑制剂（PPIs）被广泛用于治疗胃酸分泌过多和胃溃疡。该研究调查了奥美拉唑的S-异构体埃索美拉唑对大鼠体内和兔体外实验中，由二甲双胍、组胺和二丁酰腺苷3,5-环磷酸（dbcAMP）诱发的胃酸分泌、酸化乙醇（AE）和吲哚美辛（INDO）诱导的出血性损伤以及前列腺素E2（PGE2）水平的抗分泌和抗溃疡作用。同时也研究了奥美拉唑的作用以作比较。两种PPIs均以剂量依赖性方式显著（P<0.05）抑制二甲双胍诱导的胃酸分泌。在分离的兔胃腺中，两种PPIs均能显著降低组胺和dbcAMP诱发的胃酸分泌，且效力相似。与对照组相比，在埃索美拉唑或奥美拉唑存在的情况下，AE或INDO诱导的损伤均显著（P<0.05）减少。在AE处理前增加埃索美拉唑的剂量会导致明显的细胞保护作用，并使胃组织匀浆中结合型PGE2的浓度升高。结果表明，埃索美拉唑和奥美拉唑在体内和体外对AE或INDO诱导的大鼠和兔胃出血性损伤以及抑制二甲双胍、dbcAMP和组胺诱导的胃酸分泌方面同样有效。发现埃索美拉唑的胃保护作用与胃腺区结合型PGE2水平成正比。
