Convergent Synthesis of the Rat Galanin and Study of Its Biological Activity

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...

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Bibliographic Details
Published in:Russian journal of bioorganic chemistry 2020, Vol.46 (1), p.32-42
Main Authors: Sidorova, M. V., Palkeeva, M. E., Avdeev, D. V., Molokoedov, A. S., Ovchinnikov, M. V., Azmuko, A. A., Serebryakova, L. I., Veselova, O. M., Studneva, I. M., Pisarenko, O. I.
Format: Article
Language:English
Subjects:
Adenine
Adenosine triphosphate
Biochemistry
Biological activity
Biomedical and Life Sciences
Biomedicine
Bioorganic Chemistry
Blood plasma
Creatine
Glycine
Injury prevention
Kinases
Lactate dehydrogenase
Life Sciences
Myocardial infarction
Necrosis
Nucleotides
Organic Chemistry
Peptides
Solid phases
Synthesis
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Summary: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.
ISSN:1068-1620
1608-330X
DOI:10.1134/S1068162020010100