Application of haematoporphyrin derivative to treatment of neuroblastoma

A technology for neuroblastoma and its 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: 2021-04-09
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 direc...

Method used

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  • Application of haematoporphyrin derivative to treatment of neuroblastoma
  • Application of haematoporphyrin derivative to treatment of neuroblastoma
  • Application of haematoporphyrin derivative to treatment of neuroblastoma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Synthesis of Hematoporphyrin Derivative A2

[0037] 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:

[0038]

[0039] The specific operation is:

[0040] 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

[0044] CCK8 kit detects the activity of compound A2 and chemotherapy drugs to inhibit the proliferation of neuroblastoma cells

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Abstract

The invention belongs to the field of medicine and pharmacology for sensitizing chemotherapy drug, in particular to application of a haematoporphyrin-verapamil fragment compound A2 to tolerance reversing and sensitization of chemotherapy drugs for neuroblastoma. The compound A2 sensitizes the chemotherapy drugs in different degrees to inhibit cell proliferation of the neuroblastoma, which indicates that the compound A2 can be developed into a sensitizer or a drug resistance reversing agent of the chemotherapy drugs for treating a patient with the neuroblastoma.

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 neuroblastoma. [0002] technical background [0003] Neuroblastoma (Neuroblastoma, NB) is the most common extracranial solid tumor in children. It originates from the neural crest and is a heterogeneous malignant solid tumor that occurs in the sympathetic and parasympathetic ganglia in early childhood. It accounts for all malignant tumors in adolescents under 15 years old. The annual incidence rate is 0.3 / 100,000-0.5 / 100,000, second only to leukemia and central nervous system tumors [1] . Because NB has the characteristics of hidden primary site, difficult early diagnosis, high degree of malignancy, rapid progression and easy early metastasis, the traditional treatment methods including surg...

Claims

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Application Information

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IPC IPC(8): A61K47/55A61K31/277A61K31/409A61K31/704A61P35/00
CPCA61K31/277A61K31/409A61K31/704A61K47/55A61P35/00A61K2300/00
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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