Kawasaki K, Maeda M, Yamashiro Y, Mayumi T, Takahashi M, Kaneto H
Faculty of Pharmaceutical Sciences, Kobe-Gakuin University, Japan.
Chem Pharm Bull (Tokyo). 1993 Nov;41(11):2053-4. doi: 10.1248/cpb.41.2053.
The poly(ethylene glycol) hybrid of Leu-enkephalin (Tyr-Gly-Gly-Phe-Leu) was prepared and its analgesic activity was examined. Poly(ethylene glycol) #4000 was converted to amino-poly(ethylene glycol) and coupled with the N alpha-protected pentapeptide, followed by trifluoroacetic acid treatment to give the hybrid. The hybrid was soluble in water or various organic solvents. The analgesic activity of Leu-enkephalin was markedly potentiated by hybrid formation with poly(ethylene glycol).
制备了亮氨酸脑啡肽（Tyr-Gly-Gly-Phe-Leu）的聚乙二醇杂化物，并检测了其镇痛活性。将聚乙二醇#4000转化为氨基聚乙二醇，然后与Nα-保护的五肽偶联，再经三氟乙酸处理得到该杂化物。该杂化物可溶于水或各种有机溶剂。与聚乙二醇形成杂化物后，亮氨酸脑啡肽的镇痛活性显著增强。
