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

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 limited application, low polarity of hematoporphyrin, etc., and achieves 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 stomach cancer together with chemical drug
  • Application of hematoporphyrin derivative in treatment of stomach cancer together with chemical drug
  • Application of hematoporphyrin derivative in treatment of stomach cancer together with chemical drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Synthesis of Hematoporphyrin Derivative A2

[0042] 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:

[0043]

[0044] The specific operation is:

[0045] 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

[0049] CCK8 kit detects hematoporphyrin derivative A2 and chemotherapeutic drugs to inhibit the proliferation of gastric 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 stomach cancer reversing chemotherapeutic drugs. The hematoporphyrin derivative A2 has different extents of chemotherapeutic-drug-sensitivity-enhanced stomach 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 stomach 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 gastric cancer. [0002] technical background [0003] Stomach cancer is one of the most common cancers in Southeast Asia including China, Japan and South Korea, as well as Eastern Europe [1] . Although gastric cancer incidence and mortality have declined significantly in most developed countries over the past half century, it remains the second most common cause of cancer-related mortality in the world. About two-thirds of gastric cancer patients in China will develop advanced or metastatic disease, and more than 50% of patients will develop recurrence after surgery [2] . Systemic chemotherapy plays a vital role in the treatment of gastric cancer. Although surger...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K31/513A61P35/00
CPCA61K41/0071A61K31/513A61P35/00A61K2300/00
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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