Application of modified peptide in preparation of medicine for inhibiting pancreatic islet from secreting insulin and modification method

Abstract

The invention belongs to the technical field of peptide modification, and discloses application of a modified peptide in the preparation of a medicine for inhibiting insulin secretion of pancreas islet and a modification method. The method comprises the following steps: selecting a closed COX52-69 tail end; carrying out N-terminal acetylation and C-terminal amidation modification on the tail end of the closed COX52-69; performing methylation modification on an amido bond between valine and leucine, adding cysteine to the head end and the tail end of polypeptide, enabling the polypeptide to be connected into a ring through a disulfide bond, and forming a rigid molecule. According to the invention, the original linear polypeptide is modified to form the annular polypeptide COX52-69, so that the mode of only injection administration in the past is changed into an oral administration mode, and the annular polypeptide COX52-69 also has the function of inhibiting glucose-induced insulin secretion. The modified annular polypeptide realizes an oral administration route, and the more linear peptide COX52-69 has the same function of inhibiting pancreas islet from secreting insulin. The oral administration way of the polypeptide is realized.

Description

Technical field [0001] The present invention belongs to the field of peptide-modified techniques, and more particularly to a modified peptide in the preparation of use and modification methods of inhibiting insulin drugs. Background technique [0002] Currently, short peptide COX 52-69 It is a polypeptide containing 18 amino acids, initially separated from the small intestine of the pig, and found that it is completely overlapping from the 52nd to 69 of the cytochrome oxidase VII from the small intestine of the pig. So COX 52-69 . The sequence is Llpagwvlshldsykkre. Purified Cox by biochemical separation 52-69 The polypeptide makes functions experiments that the polypeptide can inhibit the secretion of insulin caused by glucose, which is currently applying for the Chinese invention patent on October 11, 2013, and the application number is 201310471571.9. Thereafter, a short peptide Cox having biologically active is obtained by a method of solid phase synthesis. 52-69 This technol...

AI Technical Summary

Problems solved by technology

[0004] (1) Linear peptide COX synthesized by solid-phase synthesis 52-69 Inability to function by oral administration;

[0005] (2) There is no linear peptide COX in the prior art 52-69 Methods for modifying the molecular structure that affect COX 52-69 Applications

[0009] Due to their instability and low bioavailability, peptide drugs are mostly administered by injection, which brings great pain to patients

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