Application of hematoporphyrin derivative combined with chemical drug in treatment of osteosarcoma

A derivative, the technology of hematoporphyrin, which is applied in the field of medicine to increase the sensitivity of chemotherapy drugs, can solve the problems of low polarity and limited application of hematoporphyrin, and achieve the effect of broad application prospects and easy mastery

Pending Publication Date: 2021-03-19
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 treatment of osteosarcoma
  • Application of hematoporphyrin derivative combined with chemical drug in treatment of osteosarcoma
  • Application of hematoporphyrin derivative combined with chemical drug in treatment of osteosarcoma

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 in an amount equivalent to three times the mass of the crude product, and vacuum rotary evaporate ethyl acetate Esters; in silica gel col...

Embodiment 2

[0045] CCK8 kit detects the activity of compound A2 and chemotherapeutic drugs in inhibiting the proliferation of osteosarcoma cells

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Abstract

The invention belongs to the field of medicine and pharmacology for improving chemotherapy drug sensitivity, and particularly relates to application of a hematoporphyrin-verapamil fragment compound A2in reversing the tolerance and sensitization of chemotherapy drugs for osteosarcoma. Different degrees of the sensitization chemotherapeutic drugs of the compound A2 inhibit the proliferation of osteosarcoma cells, which indicates that the compound A2 can be developed into a sensitizer or a reverse drug resistance of the chemotherapeutic drugs and is used for treating osteosarcoma patients.

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 hematoporphyrin-verapamil fragment compound A2 in reversing the tolerance and sensitization of chemotherapeutic drugs in osteosarcoma. [0002] technical background [0003] Malignant tumors are one of the major diseases that seriously affect human health and threaten human life in the world today. Malignant tumors are now the second leading cause of death in humans and are difficult to treat [1] . Osteosarcoma (OS) is the most common primary malignant tumor of bone. The age of onset is mostly between 15 and 25 years old. It is the most common malignant tumor in children and adolescents. There are more males than females. It usually presents as malignant growth of osteoblasts. [2] . It is characterized by rapid tumor progression, early lung metastasis, and extremely poor prognosis. The 5-year survival rate is...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K31/137A61K47/55A61K31/337A61P35/00
CPCA61K41/0071A61K31/137A61K47/55A61K31/337A61P35/00A61K2300/00
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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