Application of hematoporphyrin derivative combined with chemical drug in cervical 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: 2021-03-09
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 directly administered intravenously, which greatly limits its clinical application.

Method used

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  • Application of hematoporphyrin derivative combined with chemical drug in cervical cancer treatment
  • Application of hematoporphyrin derivative combined with chemical drug in cervical cancer treatment
  • Application of hematoporphyrin derivative combined with chemical drug in cervical 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 proliferation of cervical cancer cells

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Abstract

The invention belongs to the field of medicine and pharmacology for improving the sensitivity of chemotherapeutic drugs, and particularly relates to application of a hematoporphyrin-verapamil fragmenthematoporphyrin derivative A2 in reversing tolerance and sensitization of cervical cancer chemotherapeutic drugs. The hematoporphyrin derivative A2 has the effect of sensitive chemotherapeutics at different degrees for inhibiting proliferation of cervical cancer cells, which indicates that the hematoporphyrin derivative A2 can be developed into a sensitizer or a reversal resistance agent of the chemotherapeutics for treating patients with cervical 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 cervical cancer. [0002] technical background [0003] Cervical cancer (CC) is one of the common gynecological malignancies, ranking first among reproductive tract malignancies, and seriously threatening the health of women worldwide. In the early stage of cervical cancer, there may be no symptoms, but as the disease progresses, late symptoms of cervical cancer may include abnormal vaginal discharge, vaginal bleeding, contact bleeding and pelvic pain, etc. [1,2] . Cervical cancer is the most common malignant tumor of the female reproductive tract. According to the statistical report released in 2019, the United States is expected to have 13,170 new cases and 4,250 ...

Claims

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Application Information

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