Fujita T, Sakuma S, Yamamoto N, Fujimoto Y
Department of Hygienic Chemistry, Osaka University of Pharmaceutical Sciences, Japan.
Biochem Mol Biol Int. 1998 Sep;46(1):157-63. doi: 10.1080/15216549800203662.
The effects of eicosapentaenoic acid and its 15-hydroperoxy and 15-hydroxy adducts on the activity of glucosamine synthetase, the rate-limiting enzyme of mucus synthesis, in rabbit gastric antral mucosa were examined. 15-Hydroperoxy-eicosapentaenoic acid inhibited the glucosamine synthetase activity at concentrations of 10, 20 and 50 microM. The effect was concentration-dependent, and the concentration required for 50% inhibition was approximately 20 microM. Eicosapentaenoic acid and its 15-hydroxy adduct had no significant effect on the enzyme activity at the same concentration range. The experiment utilizing Fe2+ revealed that the inhibitory effect of 15-hydroperoxyeicosapentaenoic acid on the glucosamine synthetase activity is not due to hydroxy radical which is expected to be formed from the hydroperoxy adduct. These results suggest that 15-hydroperoxyeicosapentaenoic acid has the potential to reduce the synthesis of gastric mucus by inhibiting the glucosamine synthetase activity.
研究了二十碳五烯酸及其15 - 氢过氧化物和15 - 羟基加合物对兔胃窦黏膜中氨基葡萄糖合成酶（黏液合成的限速酶）活性的影响。15 - 氢过氧二十碳五烯酸在浓度为10、20和50微摩尔时抑制氨基葡萄糖合成酶活性。该效应呈浓度依赖性，50%抑制所需浓度约为20微摩尔。在相同浓度范围内，二十碳五烯酸及其15 - 羟基加合物对酶活性无显著影响。利用Fe2 +进行的实验表明，15 - 氢过氧二十碳五烯酸对氨基葡萄糖合成酶活性的抑制作用并非源于预期由氢过氧化物加合物形成的羟基自由基。这些结果表明，15 - 氢过氧二十碳五烯酸有可能通过抑制氨基葡萄糖合成酶活性来减少胃黏液的合成。
