Targeted cell-penetrating peptide photosensitizer and preparation method and application thereof

Abstract

The invention discloses a targeted cell-penetrating peptide photosensitizer and a preparation method and application thereof. The targeted cell-penetrating peptide photosensitizer has higher targetingability and can be used for interaction of a targeted cell transmembrane peptide of a squamous carcinoma cell cytomembrane and a translocator on the squamous carcinoma cell cytomembrane so that the photosensitizer molecules enter and are gathered in squamous carcinoma cells. The targeted cell-penetrating peptide photosensitizer can activate a PERK-eIF signaling pathway in the squamous carcinoma cell to induce autophagy of tumor cells and can promote squamous carcinoma cell killing through inducing autophagy effects. The targeted cell-penetrating peptide photosensitizer improves molar light absorptivity of the squamous carcinoma cell to a photosensitizer and fully transforms lights into cytotoxic substances. The targeted cell-penetrating peptide photosensitizer satisfies the biological characteristics of the tumor cells and has better targeting effects on squamous carcinoma cells.

Description

Technical field [0001] The invention relates to a targeted cell-penetrating peptide photosensitizer and its preparation method and application. Background technique [0002] Cell-penetrating peptide is a kind of short peptide molecule that can carry different biologically active substances through the cell membrane and into the cell or even the nucleus without damaging the membrane structure. Its length generally does not exceed 30 amino acids. Cell penetrating peptides can carry a variety of substances including proteins, amino acids, polypeptides, nucleic acids and oligonucleotides into the cell, and their penetrating ability does not rely on classical endocytosis. At present, after studying the chemical structure and biological properties of natural cell penetrating peptides, some common characteristics of cell penetrating peptides have been gradually grasped, such as: cell penetrating peptides are rich in basic amino acids such as arginine and lysine Both the residue and its...

AI Technical Summary

Problems solved by technology

However, so far, the photosensitizers developed still have deficiencies, such as low molar absorptance, which cannot fully convert light into cytotoxic substances; photosensitizers cannot be effectively enriched in specific tumor cells; photosensitizers Poor targeting of different types of tumor cells, etc.

Such as Chinese invention, application number: 201210169784.1; authorization announcement number: CN 103193782B The photosensitizer chlorophyllin sodium salt and its derivatives are not modified and transformed in combination with the biological characteristics of tumors, so that they can be used in the targeted treatment of tumors. There is room for improvement in terms of performance and effectiveness; another example is the paper (Fang Qian. Synthesis and optical properties of benzophenoxazine (O, S, Se) water-soluble photosensitizers [D]. Central South University, 2012.) Although the selenium-containing benzophenoxazine photosensitizers studied in the study have high-efficiency photodynamic effects, they are only high-efficiency photosensitizers obtained directly from industrial dyes, and they have not been able to better adapt to different diseases and uses in biology. features

Images