Abstract The full-length rat galanin (GWTLNSAGYLLGPHAIDNHRSFSDKHGLT-NH 2 , G29) was prepared by the solid phase peptide synthesis using the Fmoc-strategy. The peptide chain was elongated both by one amino acid and by a fragment condensation. Fragments with the C -terminal glycine residue were synthesized by the solid phase method on the 2-chlorotrityl chloride resin or by the method of conventional peptide synthesis in solution. After the reversed phase HPLC, galanin had the correct molecular weight and 98% purity. We studied the G29 cardioprotective properties on a model of acute myocardial infarction in rats. The G29 administration reduced the infarct size by 40% and decreased the activity of necrosis markers CK-MB (Creatine Kinase-MB) and LDH (Lactate Dehydrogenase) in the blood plasma. The peptide improved metabolic state of the infarcted heart, increased the ATP content, the total adenine nucleotide pool, phosphocreatine, and total creatine, and decreased the lactate level compared to a control. These results indicated the possibility of the G29 use as a drug for reducing the myocardial reperfusion injury. In addition, the mechanisms of the G29 action should be studied.

中文翻译：

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大鼠甘丙肽的聚合合成及其生物活性研究

摘要 采用Fmoc-策略通过固相肽合成制备全长大鼠甘丙肽(GWTLNSAGYLLGPHAIDNHRSFSDKHGLT-NH 2 , G29)。肽链被延长了一个氨基酸和片段缩合。C-末端甘氨酸残基的片段通过固相法在2-氯三苯甲基氯树脂上合成或通过常规肽在溶液中合成的方法合成。反相 HPLC 后，甘丙肽具有正确的分子量和 98% 的纯度。我们研究了 G29 对大鼠急性心肌梗塞模型的心脏保护特性。G29 给药使梗塞面积减少了 40%，并降低了血浆中坏死标志物 CK-MB（肌酸激酶-MB）和 LDH（乳酸脱氢酶）的活性。与对照相比，该肽改善了梗塞心脏的代谢状态，增加了 ATP 含量、总腺嘌呤核苷酸库、磷酸肌酸和总肌酸，并降低了乳酸水平。这些结果表明G29有可能用作减轻心肌再灌注损伤的药物。此外，应研究 G29 作用的机制。