Application of hematoporphyrin derivative combined with chemical drug in breast cancer treatment

A kind of derivative, hematoporphyrin technology, which is applied in the field of medicine to increase the sensitivity of chemotherapeutic drugs, can solve the problems of low polarity of hematoporphyrin and limited application, and achieves the effect of broad application prospect and easy-to-mastery method.

Pending Publication Date: 2021-04-20
范平生 +5
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the low polarity of hematoporphyrin, it cannot be directly administered intravenously, which greatly limits its clinical application.

Method used

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  • Application of hematoporphyrin derivative combined with chemical drug in breast cancer treatment
  • Application of hematoporphyrin derivative combined with chemical drug in breast cancer treatment
  • Application of hematoporphyrin derivative combined with chemical drug in breast cancer treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040]Synthesis of hematoporphyrin derivative A2

[0041]Substrates, Torp porphyr derivatives A2 by amide condensation reaction by amide condensation reaction by amide condensation reaction by catalyzing hemptidin and Vivaimi fragment (3,4-dimethoxyethylenethylamine). The synthetic process is as follows:

[0042]

[0043]The specific operation is:

[0044]0.5 mmol hemolin is dissolved in a reaction vessel having 30 ml of dimethylformamide (DMF), and 4 mmol3,4-dimethoxytinethylamine and 0.5 mmol benzotriazole-1-oxygen were added. Basis (dimethylamino) phosphonium hexafluorophosphate (BOP), at room temperature for 3 hours, TLC detection reaction process; after the reaction is completed, 100 ml of water is added to the reaction vessel, and the reaction vessel is placed on ice waiting Preferred solids; extracting the solid and dried, i.e. to obtain a crude product; dissolve the crude product in ethyl acetate, add 200-300 weeks of silicate silicate, vacuum rotation, evaporation of ethyl acetate In s...

Embodiment 2

[0048]CCK8 kit detection testing hematoporphyrin derivative A2 and chemotherapeutic drug inhibits breast cancer cell value-added activity

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Abstract

The invention belongs to the field of medicine and pharmacology for increasing sensitivity of chemotherapeutic drugs, and particularly relates to application of a hematoporphyrin-verapamil fragment hematoporphyrin derivative A2 in tolerance reversing and sensitization of breast cancer chemotherapeutic drugs. The hematoporphyrin derivative A2 has different degrees of sensitization of the chemotherapeutic drugs for inhibiting breast cancer cell proliferation, which indicates that the hematoporphyrin derivative A2 can be developed into a sensitizer or a reverse drug-resistant agent of the chemotherapeutic drugs and used for treating breast cancer patients.

Description

Technical field[0001]The invention belongs to the use of a pharmaceutically acceptable drug sensitivity to increase chemotherapeutic drugs, and more particularly to the use of hematoporphyrin 骈 骈 拉帕米 片 fragment hematoporphyrin derivative A2 in tolerance and sensitization of breast cancer inversion.[0002]technical background[0003]Chemotherapy is one of the most effective methods in current breast cancer. Since the introduction of chemotherapy in the mid-1990s, the incidence and mortality caused by breast cancer have been greatly reduced, and the life of patients with breast cancer is extended.[1]. However, the development of drug resistance ultimately became a huge challenge for successful chemotherapy of breast cancer. It is estimated that a large amount of breast cancer patients (up to 50%) have no reaction to the current chemotherapy solution.[2]. Drug resistance to a single anti-tumor drug tends to trigger a multi-effect drug resistance of multiple structural and functionally ind...

Claims

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Application Information

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IPC IPC(8): A61K31/409A61P35/00C07D487/22A61K31/704A61K31/513
Inventor 范平生李增纪丽君张腾跃汪国兴钱立庭刘亚贝杨广山黄金翁呈韬樊高飞汤丽莉王旭杨国红何静段巧虹刘淼吴旸赵永欣何义富王敏刘彤彤方平孙瑾
Owner 范平生
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