胃泌素C-端四肽的N-乙酰化和糖化及其对泌酸活性的影响

本文报道了胃泌素C—端四肽N—乙酰化和糖化的方法,并用大白鼠胃灌流技术研究了它们对泌酸活性的影响。结果表明,乙酰化和糖化均可提高其泌酸活性,其中葡萄糖—1—脱氧果糖四肽(Glc—1—deoxyfru—Trp—Met—Asp—Phe—NH_2)的泌酸活性超过了商品五肽胃泌素(Boc—α—Ala—Trp—Met—Asp—Phe—NH_2)

N-Acetylation and Glycosylation of C-Terminal Tetrapeptide of Gastrin and Their Effects on Acid Stimulatory Activity

This Paper reports preparation of N-acetylated and glycosylated derivatives of C-terminal tetrapeptide of gastrin. An improved technique of perfusion of the stomach in rat was used to determine the of these derivatives on gastric secretion. The N-acetyl and glycosylated peptide exhibits an enhanced biological potency when compared with the parent peptides with free ammo groups. In particular, the acid stimulatory activity of glucosyl-deoxyfructosyl-tetragastrin was higher than that of pentagastrin (Boc-β-Ala-Trp-Met-Asp-Phe-NH2) and it was also characterized by a strong solubility in water. These properties suggest that N-glyco-sylated tetragastrin may be of great use in clinical practice.