Division of Food Science and Biotechnology, Graduate School of Agriculture, Kyoto University, Gokasho Uji, Kyoto, Japan.
J Neurochem. 2012 Jul;122(2):356-62. doi: 10.1111/j.1471-4159.2012.07777.x. Epub 2012 May 30.
We found that tryptic digest of ovalbumin after oral (p.o.) and intraperitoneal (i.p.) administration exhibited anxiolytic-like activity in mice, and then searched for orally active low-molecular-weight peptides with anxiolytic-like activity in the tryptic digest. Val-Tyr-Leu-Pro-Arg, named ovolin, corresponding to ovalbumin (280-284), mimicked the anxiolytic-like activity after p.o. and i.p. administration. The anxiolytic-like activity of ovolin was inhibited by indomethacin, a cyclooxygenase (COX) inhibitor, or BWA868C, an antagonist of the DP1 receptor for prostaglandin (PG) D2 . Ovolin-induced anxiolytic-like activity was also blocked by SCH58261 or bicuculline, antagonists of the adenosine A2A and GABAA receptors, respectively. Ovolin has no affinity for the DP1 , A2A and GABAA receptors. Taken together, ovolin may exhibit anxiolytic-like activity in a manner dependent on the PGD2 -DP1 system coupled to the A2A and GABAA receptors.
我们发现，经口（p.o.）和腹腔内（i.p.）给予卵清蛋白的胰蛋白酶消化产物在小鼠中具有抗焦虑样活性，然后在胰蛋白酶消化产物中寻找具有抗焦虑样活性的口服活性低分子量肽。Val-Tyr-Leu-Pro-Arg，命名为ovo lin，对应于卵清蛋白（280-284），在 p.o. 和 i.p. 给药后模拟抗焦虑样活性。ovo lin 的抗焦虑样活性被环加氧酶 (COX) 抑制剂吲哚美辛或前列腺素 (PG) D2 的 DP1 受体拮抗剂 BWA868C 抑制。DP1、A2A 和 GABAA 受体拮抗剂 SCH58261 或bicuculline 也可阻断 ovo lin 诱导的抗焦虑样活性。ovo lin 对 DP1、A2A 和 GABAA 受体没有亲和力。综上所述，ovo lin 可能通过与 A2A 和 GABAA 受体偶联的 PGD2-DP1 系统表现出抗焦虑样活性。
