CYCLIC PEPTIDE, PREPARATION METHOD THEREFOR AND USE THEREOF

• Main Authors: LU, Yunyu, WU, Gang, LEI, Xiaoxuan, CHENG, Liuxingxing, WU, Liyong
• Format: Patent
• Language: Chinese; English; French
• Published: 02.02.2023
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

A cyclic peptide, a preparation method therefor and a use thereof. The cyclic peptide is a sequence of head-to-tail cyclic peptide having a triazole ring prepared from a complete linear histatin sequence or a Hst1 truncated linear sequence subject to azide-alkyne cycloaddition reaction under specific conditions. The biological activity of the complete head-to-tail cyclic peptide sequence is more than 1000 times higher than that of linear histatin, and the dose-effect ratio and clinical efficacy of histatin is significantly improved compared to existing histatin cyclic peptides. For the Hst1 truncated sequence head-to-tail cyclic peptide, the molecular weight is only one-third that of linear Hst1, the biological activity is 15 times that of linear Hst1, and the cost to reach the same level of activity is only one-hundredth that of linear Hst1. The entire cyclization process is mild, simple and efficient, is capable of producing high-purity head-to-tail cyclic peptides, can be used to prepare aging-resisting an