Photodynamic therapy agent for relieving tumor hypoxia as well as preparation method and application thereof

A technology for photodynamic therapy and tumor, applied in the field of medicine, can solve problems such as affecting the therapeutic effect of photodynamic therapy, and achieve the effects of low cost, high yield and simple synthesis steps

Active Publication Date: 2021-01-22
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This therapy relies on local O 2 molecules to produce highly cytotoxic 1 o 2 , but the hypoxic microenvironment of solid tumors will affect the therapeutic effect of photodynamic therapy

Method used

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  • Photodynamic therapy agent for relieving tumor hypoxia as well as preparation method and application thereof
  • Photodynamic therapy agent for relieving tumor hypoxia as well as preparation method and application thereof
  • Photodynamic therapy agent for relieving tumor hypoxia as well as preparation method and application thereof

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Experimental program
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preparation example Construction

[0034] The preparation method of the above-mentioned photodynamic therapy agent comprises the following steps:

[0035] Step 1, prepare porphyrin ester and tetrakis (4-carboxyphenyl) porphyrin (H 2 TCPP).

[0036] (1) Preparation of porphyrin esters by high temperature solvothermal method

[0037] 6 g of pyridine, 14 g of methyl p-formylbenzoate, and 200 mL of propionic acid were added to a 500 mL round-bottomed flask, and after brief sonication, the mixture was condensed at reflux at 140 °C for 12 h. After cooling to room temperature, put it in the refrigerator for 6 hours, collect the product by suction filtration, collect the product by suction filtration while stirring with ethanol, and add a small amount of tetrahydrofuran (THF) for suction filtration and washing. Finally, the porphyrin ester was obtained by vacuum drying at 60° C. for 12 h.

[0038] (2) Acidification of porphyrin ester to obtain tetrakis (4-carboxyphenyl) porphyrin

[0039] 2 g of the synthesized por...

Embodiment 1

[0066] (1) Preparation of porphyrin ester

[0067] Add 6 g of pyridine, 14 g of methyl p-formylbenzoate, and 200 mL of propionic acid into a 500 mL round-bottomed flask. After a brief sonication, the mixture was refluxed at 140 °C for 12 h, cooled to room temperature, and placed Put it in the refrigerator for 6 hours, collect the product by suction filtration, wash the product by centrifugation with ethanol, collect the product by suction filtration while stirring, and add a small amount of tetrahydrofuran (THF) for suction filtration and washing. Finally, the porphyrin ester was obtained by vacuum drying at 60° C. for 12 h.

[0068] (2) Preparation of tetrakis (4-carboxyphenyl) porphyrin

[0069] 2 g of the synthesized porphyrin ester, 60 mL of THF, 60 mL of methanol and a prepared potassium hydroxide (KOH) solution (6.8 g of KOH plus 60 mL of water) were condensed and refluxed at 85 °C for 12 h. After cooling to room temperature, adjust the pH of the product to 6~7 with 1M...

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Abstract

The invention discloses a photodynamic therapy agent for relieving tumor hypoxia as well as a preparation method and application thereof, and belongs to the technical field of medicines. The photodynamic therapy agent is a metal-organic framework nano composite material loaded with O2. The metal-organic framework nano composite material is metal-organic framework nano particles Zr-TCPP (Fe), the interiors of nano frameworks of the nano particles Zr-TCPP (Fe) are modified with perfluorooctanoic acid, and meanwhile glucose oxidase GOx is further adsorbed in pore channels of the nano particles Zr-TCPP (Fe). According to the invention, a drug delivery system capable of catalyzing tumor to endogenously generate O2 is designed while O2 is delivered to tumor tissue, so that the hypoxic environment can be remarkably improved, and the photodynamic therapy effect is enhanced. In addition, the synthetic steps of the therapy agent are relatively simple, and the yield is relatively high; and a synthetic method is simple and relatively low in cost, so that the method is suitable for large-scale production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a photodynamic therapy agent for alleviating tumor hypoxia, a preparation method and application thereof. Background technique [0002] As we all know, malignant tumors seriously endanger human life and health. Among them, solid tumors account for more than 85% of clinical malignant tumors, and hypoxia is one of the important characteristics of solid tumors. Due to the existence of tumor hypoxic regions, the sensitivity of tumors to radiotherapy and chemotherapy is reduced, resulting in the formation of tumor angiogenesis and hypoxia-inducible factors, which induce tumor cell recurrence, invasion and metastasis, and become the fundamental reason why tumors are difficult to cure. Tumor hypoxic regions are characterized by insufficient oxygen content, and the therapeutic effects of existing tumor treatment technologies (radiotherapy, photodynamic therapy) are strongly ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61P35/00
CPCA61K41/0076A61P35/00
Inventor 黄悠悠吴灿晨汪洋姚勇
Owner NANTONG UNIVERSITY
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