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Application of hematoporphyrin derivative combined chemical drug in liver cancer treatment

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

Pending Publication Date: 2021-03-16
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 chemical drug in liver cancer treatment
  • Application of hematoporphyrin derivative combined chemical drug in liver cancer treatment
  • Application of hematoporphyrin derivative combined chemical drug in liver cancer treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Synthesis of Hematoporphyrin Derivative A2

[0044] Dissolve 0.5 mmol of hematoporphyrin in 30 mL of DMF and stir on a magnetic stirrer, then add 2 mmol of 3,4-dimethoxyphenethylamine and 0.5 mmol of benzotriazol-1-yloxytri( Dimethylamino)phosphonium hexafluorophosphate (BOP), stirred at room temperature for 3 hours, and the reaction progress was detected by thin-plate chromatography (TLC). After the reaction was completed, 100 mL of water was added to the reaction system and stirred evenly, and then the reaction vessel was placed on ice to precipitate a solid. The precipitated solid was filtered off with suction and dried to give the crude product. The crude product was dissolved in ethyl acetate, 200-300 mesh silica gel equivalent to three times the mass of the crude product was added, the ethyl acetate was evaporated in vacuum, and then the sample was dry-loaded with dichloromethane:methanol volume ratio 50: 1 is the eluent and purified by silica gel column chromat...

Embodiment 2

[0048] CCK8 Kit Detects Hematoporphyrin Derivative A2 and Chemotherapeutic Drugs Inhibiting the Proliferation Activity of Liver Cancer Cells

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Abstract

The invention belongs to the field of medicine for increasing the sensitivity of chemotherapeutic drugs, and particularly relates to application of a hematoporphyrin derivative A2 of a hematoporphyrincombined verapamil fragment in tolerance and sensitization of liver cancer reverse chemotherapeutic drugs. The hematoporphyrin derivative A2 has the effect of inhibiting liver cancer cell proliferation of sensitization chemotherapeutic drugs of different degrees, and the hematoporphyrin derivative A2 can be developed into a sensitizer or a reverse drug-resistant agent of the chemotherapeutic drugs and used for treating liver cancer 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 a hematoporphyrin derivative A2 in combination with verapamil fragments in reversing the tolerance and sensitization of chemotherapeutic drugs for liver cancer. [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, and have become the second leading cause of human death [1] . Hepatocellular carcinoma (HCC) is a common solid tumor in my country, with the highest mortality rate among malignant tumors, which seriously endangers the health of our people. [2] . Due to the insidious onset and rapid progress of HCC, most patients are already in the middle and late stage when they are diagnosed, and the best time for surgical treatment is missed. This makes transcatheter arterial chemoembolization (TACE) an i...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K45/06A61P35/00A61K31/704A61K31/513A61K31/337
CPCA61K41/0071A61K45/06A61P35/00A61K31/704A61K31/513A61K31/337A61K2300/00
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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