Application of combination of hematoporphyrin derivative and chemical drug in colon cancer treatment

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 limited application and low polarity of hematoporphyrin, and achieve the effect of easy method and broad application prospect

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 combination of hematoporphyrin derivative and chemical drug in colon cancer treatment
  • Application of combination of hematoporphyrin derivative and chemical drug in colon cancer treatment
  • Application of combination of hematoporphyrin derivative and chemical drug in colon cancer treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Synthesis of Hematoporphyrin Derivative A2

[0039] 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:

[0040]

[0041] The specific operation is:

[0042] 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

[0046] CCK8 kit detects hematoporphyrin derivative A2 and chemotherapeutic drugs to inhibit the proliferation of colon cancer cells

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Abstract

The invention belongs to the field of medicines for improving the sensitivity of chemotherapeutic drugs, and particularly relates to application of a hematoporphyrin-verapamil fragment hematoporphyrinderivative A2 in tolerance reversion and sensitivity improvement of a colon cancer chemotherapeutic drug. The hematoporphyrin derivative A2 has the effect of improving the sensitivity of the chemotherapeutic drug for inhibiting the proliferation of colon cancer cells to different degrees, and it is indicated that the hematoporphyrin derivative A2 can be developed into a sensitizer or a drug tolerance reversion agent of the chemotherapeutic drug and is used for treating patients with colon cancer.

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 colon cancer. [0002] technical background [0003] Colon cancer, a disease in which malignant tumors form in the tissues of the colon, is the third most common cancer and one of the leading causes of cancer-related death worldwide [1-3] . Currently, surgery and chemotherapy are the two main treatment options for colon cancer, depending on the stage of the cancer, the location of the tumor at diagnosis, and individual patient characteristics [4] . Chemotherapy can generally be carried out at different stages of treatment. Patients with advanced colon cancer usually receive adjuvant therapy after surgery, and it can also be used before surgery to shrink tumors and f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K47/55A61K31/277A61K31/513A61P35/00
CPCA61K41/0071A61K31/513A61K47/55A61K31/277A61K9/0019A61P35/00A61K2300/00
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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