Application of hematoporphyrin derivative in treatment of bladder cancer together with chemical drug

A derivative, the technology of hematoporphyrin, applied in the field of medicine to increase the sensitivity of chemotherapeutic drugs, can solve the problems of limited application and low polarity of hematoporphyrin, and achieve the effect of easy method and broad application prospect

Pending Publication Date: 2021-03-26
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 in treatment of bladder cancer together with chemical drug
  • Application of hematoporphyrin derivative in treatment of bladder cancer together with chemical drug
  • Application of hematoporphyrin derivative in treatment of bladder cancer together with chemical drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Synthesis of Hematoporphyrin Derivative A2

[0038] Hematoporphyrin and verapamil fragments (3,4-dimethoxyphenethylamine) are catalyzed by BOP to synthesize the target product, namely hematoporphyrin derivative A2, through amide condensation reaction. The synthesis process is as follows:

[0039]

[0040] The specific operation is:

[0041] Dissolve 0.5 mmol of hematoporphyrin in a reaction vessel filled with 30 mL of dimethylformamide (DMF), and add 4 mmol of 3,4-dimethoxyphenethylamine and 0.5 mmol of benzotriazol-1-yloxy base tris(dimethylamino)phosphonium hexafluorophosphate (BOP), stirred at room temperature for 3 hours, and TLC detected the reaction progress; Precipitate a solid; suction filter the precipitated solid and dry to obtain a crude product; dissolve the crude product in ethyl acetate, add 200-300 mesh silica gel equivalent to three times the mass of the crude product, and vacuum rotary evaporate ethyl acetate ; In silica gel column chromatography ...

Embodiment 2

[0045] CCK8 kit detects hematoporphyrin derivative A2 and chemotherapeutic drugs to inhibit proliferation of bladder cancer cells

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Abstract

The invention belongs to the field of chemotherapeutic drug sensitivity enhancing medicine and particularly relates to use of a hematoporphyrin-verapamil-fragment-combined hematoporphyrin derivative A2 in tolerance and sensitivity enhancing of bladder cancer reversing chemotherapeutic drugs. The hematoporphyrin derivative A2 has different extents of chemotherapeutic-drug-sensitivity-enhanced bladder cancer cell proliferation inhibiting actions, and it is shown that the hematoporphyrin derivative A2 can be developed into chemotherapeutic-drug sensitizing agents or drug resistance reversing agents and is applied to treatment on bladder cancer sufferers.

Description

technical field [0001] The invention belongs to the field of medicine for increasing the sensitivity of chemotherapeutic drugs, and specifically relates to the use of a hematoporphyrin derivative A2 in combination with verapamil fragments in reversing the tolerance and sensitization of chemotherapeutic drugs for bladder cancer. [0002] technical background [0003] Bladder cancer is a common malignant tumor of the urinary system, once the disease will seriously affect the quality of life of patients. Chemotherapy is one of the important methods to treat bladder cancer, but during long-term chemotherapy, tumor cells will develop drug resistance, which will lead to treatment failure. When tumor cells become resistant to chemotherapy, their biological behavior will also change, which will affect the clinical efficacy of bladder cancer and eventually lead to the failure of bladder cancer treatment. [1] . How to overcome the multidrug resistance of bladder cancer has become an ...

Claims

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Application Information

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IPC IPC(8): A61K47/55A61K33/243A61K41/00A61K31/277A61P35/00
CPCA61K47/55A61K33/243A61K41/0071A61K31/277A61P35/00A61K2300/00
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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