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J.Health Sci., 50(1), 1-8, 2004
Comparison of the Effects of Pantoprazole Enantiomers on Gastric Mucosal Lesions and
Gastric Epithelial Cells in Rats
Hong Cao,*, a, 1 Minwei
Wang,a Jianhui
Jia,a Qinghe
Wang,b and Maosheng
Chengb
aDepartment of Pharmacology and
bDepartment of Pharmaceutical Engineering, Shenyang Pharmaceutical University (41#), 103
Wenhua Road, Shenyang, 110016, China
(±)-Pantoprazole sodium, [(±)-PAN·Na], is a proton pump inhibitor that is administered as a racemate. The
protective effects of (-)-PAN·Na, (+)-PAN·Na and (±)-PAN·Na on various experimental ulcers in animals were
compared. (-)-PAN·Na inhibited gastric lesions induced by water-immersion stress, aspirin, ethanol, and
reserpine in a dose-dependent manner. The dose that inhibited 50% of lesion
(ID50) were 2.72 ± 1.03, 1.60 ± 0.64, 4.12 ± 2.18, and 2.77 ± 0.86 mg/kg, respectively. The
ID50 values of (+)-PAN·Na and (±)-PAN·Na were 1.7, 2.6,
1.8, 2.7 and 1.5, 1.7, 1.6, 1.9 times higher, respectively, than that of (-)-PAN·Na. Primary culture of rat gastric
epithelial cells was investigated as an in
vitro model for comparing the cell protective effects among the three
agents. Exposed to the three drugs at the concentrations of
2.5 × 10-1-2.5 × 10-5 mg/ml, cultured cells were
treated with either pH 3.5 medium or 3.5 mM indomethacin. Cytoprotection was evaluated by MTT. (-)-PAN·Na,
(+)-PAN·Na and (±)-PAN·Na provided significant cytoprotective effects when the cells were pretreated with the
drugs prior to exposure to 3.5 mM indomethacin, whereas, when they were treated concurrently, no significant
cytoprotective effects were found. In pH 3.5 medium-induced damage, the three drugs had marked protective
effects on gastric cells, however, when the concentration of drugs was high (0.25 mg/ml), only (+)-PAN·Na had
significant cytoprotection. We concluded that the cytoprotective mechanisms of (-)-PAN·Na and (+)-PAN·Na
are different. The results of in vitro experiments were not in complete accordance with the
in vivo results, suggesting that the effects of the three drugs on ulcer inhibition are mainly due to the effects of acid inhibition
rather than cytoprotection.
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