Shigeta J, Takahashi S, Okabe S
Department of Applied Pharmacology, Kyoto Pharmaceutical University, Misasagi, Yamashina, Kyoto 607-8414, Japan.
J Pharmacol Exp Ther. 1998 Sep;286(3):1383-90.
To elucidate the role of cyclooxygenase (COX)-2 in ulcer healing, we compared the effects of NS-398 (COX-2-selective inhibitor) and indomethacin (nonselective COX inhibitor) on the healing of acetic acid-induced gastric ulcers in rats. Prostaglandin E2 (PGE2) production was elevated in ulcerated tissue, but remained unaffected in intact tissue. COX-2 mRNA was only detected in the ulcerated tissue, in which the COX-2 protein was found in fibroblasts, macrophages/monocytes and granulocytes. In contrast, COX-1 mRNA expression was not affected by ulceration. In an in vitro study, the increased PGE2 production was inhibited by NS-398; this had no effect on PGE2 production in the intact tissue. When NS-398 and indomethacin were administered to rats, 3 and 6 mg/kg NS-398 only reduced PGE2 production in the ulcerated tissue, but 10 mg/kg NS-398 and 0.5 to 2 mg/kg indomethacin inhibited the production in both the ulcerated and intact tissues. The healing of gastric ulcers was significantly impaired by 3 to 10 mg/kg NS-398 and 1 and 2 mg/kg indomethacin. The delay in ulcer healing was associated with the inhibition of PGE2 production in the ulcerated tissue. As observed upon histological analysis, regeneration of the mucosa, maturation of the ulcer base and angiogenesis in the base were significantly prevented by 6 mg/kg NS-398 and 2 mg/kg indomethacin, although the inhibitory effect of NS-398 was weaker than that of indomethacin. These results clearly indicate that COX-2 plays an important role in the healing of gastric ulcers in rats.
为阐明环氧化酶(COX)-2在溃疡愈合中的作用,我们比较了NS-398(COX-2选择性抑制剂)和吲哚美辛(非选择性COX抑制剂)对大鼠乙酸诱导的胃溃疡愈合的影响。溃疡组织中前列腺素E2(PGE2)的产生增加,但完整组织中的PGE2产生未受影响。COX-2 mRNA仅在溃疡组织中检测到,在该组织中,COX-2蛋白存在于成纤维细胞、巨噬细胞/单核细胞和粒细胞中。相比之下,COX-1 mRNA表达不受溃疡影响。在一项体外研究中,NS-398抑制了PGE2产生的增加;这对完整组织中的PGE2产生没有影响。当给大鼠施用NS-398和吲哚美辛时,3和6 mg/kg的NS-398仅降低了溃疡组织中PGE2的产生,但10 mg/kg的NS-398和0.5至2 mg/kg的吲哚美辛抑制了溃疡组织和完整组织中的PGE2产生。3至10 mg/kg的NS-398和1及2 mg/kg的吲哚美辛显著损害了胃溃疡的愈合。溃疡愈合延迟与溃疡组织中PGE2产生的抑制有关。如组织学分析所示,6 mg/kg的NS-398和2 mg/kg的吲哚美辛显著阻止了黏膜再生、溃疡底部成熟和底部血管生成,尽管NS-398的抑制作用比吲哚美辛弱。这些结果清楚地表明COX-2在大鼠胃溃疡愈合中起重要作用。