Self-assembly short peptide and use thereof in antineoplastic medicine preparation

Abstract

A self-assembly short peptide R418 consists of an anti-tumor bioactive peptide section S18, a self-assembly peptide section RADA16-I and a connection peptide section, and the amino acid sequence is described in sequence table SEQ ID NO.1. The characterizations of an atomic force microscope and a transmission electron microscope prove that R418 molecule has the characteristic of forming nano fiber through self assembly in a solution. In vitro cell experiment shows that the self-assembly short peptide R418 can remarkably cause the death of tumor cells K562, Jurkat and MDA-MB-435S and has lower cytotoxicity on NIH3T3 cell. Beastie living body imaging experiments show that: after self assembly, the holding time of the local concentration of the R418 in an in vivo tumor region is much longer than the holding time of the local concentration of the S18. In accordance with beastie living body imaging experiments, animal tumor inhibition experiments show that: the self-assembly short peptide R418 has better tumor inhibition effect as compared with short peptide S18.

Description

technical field [0001] The invention belongs to the field of self-assembled short peptides, in particular to a self-assembled short peptide and its application in preparing antitumor drugs. Background technique [0002] Self-assembled short peptides are a new type of nano-biological material. Since its appearance in the 1990s, it has received extensive attention and has been developed rapidly. A variety of self-assembled short peptides with different structures have been synthesized, and they can be used in cells. Three-dimensional culture and preparation of hydrophobic drug carriers, hemostatic drugs, burn treatment drugs, antibacterial drugs, etc. However, the preparation of more self-assembled short peptides and the expansion of the application range of self-assembled short peptides are still issues of concern to scientific and technological workers. [0003] Cancer is one of the major diseases affecting human health. About seven million patients die of cancer every year...

AI Technical Summary

Problems solved by technology

However, the vast majority of anticancer drugs are in a state of free diffusion in the body. On the one hand, the drug cannot reach the concentration required for treatment in the lesion area, resulting in weakened efficacy; on the other hand, the free diffusion of anticancer drugs is bound to affect the body's Other normal tissues and organs cause certain side effects (see Sinha R, KimGJ, Nie S, & Shin DM (2006) Mol Cancer Ther 5, 1909-1917. LerouxJ-C, Allemann E, DeJaeghere F, Duelker E & Gurny R.( 1996) J Control Release 30, 339-50.)

[0005] In 2001, Shin S.Y. et al. disclosed a short peptide S18 (see Shin S, Lee S, Yang S, Park E, Lee D, Lee M, Eom S, Song W, Kim Y, Hahm K, et al.( 2001) J PEPT RES 58, 504-514. It is the P18 peptide in this document), according to the literature, the S18 short peptide has the characteristics of killing tumor cells K562, Jurkat, MDA-MB-361, and has the effect on normal cells NIH 3T3's killing effect is very weak

However, the literature only reported the anti-tumor effect of this peptide at the cellular level in vitro, and no in vivo animal experiments were carried out.

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