Bipolar photosensitizer and preparation method thereof

Abstract

The invention discloses a bipolar photosensitizer and a preparation method thereof. The bipolar photosensitizer is ammonium salt. The chemical structural formula of positive ions in the ammonium saltis shown in the specification. The bipolar photosensitizer further comprises glycerol acyl residues, the bipolar photosensitizer is adopted as a lyophobic group to be bounded with an EtNBSe photosensitizer to form a structure with one hydrophilic and one lyophobic end, the structure is similar to an essential ingredient-phosphatidylcholine for forming a biological film, due to the principle that like dissolves like, the bipolar photosensitizer can more easily enter cancer cells, the intake rate of the bipolar photosensitizer is greatly increased and is increased by about 46.1%, the weight percentage in bipolar photosensitizer medicine can be properly lowered, and therefore the treatment effect of the bipolar photosensitizer can be improved while the side effect of drugs is lowered.

Description

technical field [0001] The invention relates to a bipolar photosensitizer and a preparation method thereof, in particular to EtNBSe derivatives used as a photosensitizer to kill specific tumor cells by photodynamic effect, and to improve the killing effect by combining with an AMPK signaling pathway activator , belonging to the field of biomedicine. Background technique [0002] Due to environmental and bad living habits and other reasons in recent years, the prevalence of skin cancers, led by squamous cell carcinoma, has increased in the population. Squamous cell carcinoma is one of the skin cancers with high incidence. In severe cases, it can spread to deep tissues and endanger life. It has become a common disease that endangers human life and health. Therefore, rapid and effective interventional treatment is particularly important. [0003] Photodynamic therapy is a new technology for the treatment of cancer in recent years. It uses laser light of a specific wavelength ...

AI Technical Summary

Problems solved by technology

However, the first and second generation photosensitizers, such as hematoporphyrin derivatives, have complex components and a smaller wavelength of maximum absorption light, and the light waves with smaller wavelengths can only penetrate human tissues to a limited depth, making it impossible to treat deeper tissue cells.

For example, in the invention patent "Preparation Method of a Novel Photosensitizer Hypocretin B" (Application No.: 200910154644.5, Publication No.: CN 102070432 A), the main absorption wavelength of Hypocretin B is relatively short, and it absorbs at the wavelength of near-infrared light. Weak ability, difficult to target deep tissue treatment

Secondly, there are also problems such as low rate of entry into tumor cells, which is not conducive to the accumulation of photosensitizers in tumor cells.

Such as the composition of 5-aminolevulinic acid and its derivatives in the invention patent "composition and use of 5-aminolevulinic acid and its derivatives" (application number: 200810044109.X, publication number: CN 101745102 A) The hydrophilicity affects the efficiency of photosensitizers entering cells through the cell membrane, and the targeting selectivity is low, making it difficult to accumulate photosensitizers in tumor cells in large quantities to achieve the desired therapeutic effect

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