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Application of imperatorin in preparing antineoplastic drugs with multi-drug resistance (MDR)

A multi-drug resistance, imperatorin technology, applied in anti-tumor drugs, drug combinations, active ingredients of heterocyclic compounds, etc., can solve problems such as no report on inhibiting proliferation.

Inactive Publication Date: 2011-02-09
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has a wide range of sources and has a variety of biological activities, such as: anti-mutagenic, analgesic, sedative, anti-epilepsy, anti-hepatitis, anti-osteoporosis, etc. It has also been found to have anti-cancer effects recently, but imperatorin has many Inhibition of proliferation of drug-resistant tumor cells has not been reported

Method used

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  • Application of imperatorin in preparing antineoplastic drugs with multi-drug resistance (MDR)
  • Application of imperatorin in preparing antineoplastic drugs with multi-drug resistance (MDR)
  • Application of imperatorin in preparing antineoplastic drugs with multi-drug resistance (MDR)

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Separation and purification of imperatorin from the traditional Chinese medicine Angelica dahurica and identification of its structure

[0021] experimental method

[0022] 1. Separation and purification: the dried roots of Angelica dahurica are ground into powder in a grinder, and weighed to obtain 3 kg of dried Angelica dahurica powder. Soak the powder in petroleum ether and ethyl acetate solvent for 48h, wherein the volume ratio of petroleum ether and ethyl acetate is 2:1. Then pour it into a round-bottomed flask, heat and reflux at about 100°C in a jacketed thermostat for about 2 hours, connect a condenser tube to the top of the round-bottomed flask and continue to pass water to achieve the purpose of condensation and reflux. After cooling, pour out the liquid and filter it, and leave the filter residue in the round bottom flask, and then add an appropriate amount of petroleum ether and ethyl acetate solvent, continue to heat and reflux the Angelica dahu...

Embodiment 2

[0025] 2. Structural identification of imperatorin: white cotton-like substance, 1H NMR (500Hz, DMSO) main chemical shift: 1H-NMR: δppm: 7.764 (1H, d, J=9.6Hz, C4-H), 7.691 (1H , d, J=2.0Hz, C12-H), 7.359 (1H, s, C5-H), 6.814 (1H, d, J=2.0Hz, C11-H), 6.370 (1H, d, J=9.6Hz , C3-H), 5.613 (1H, m, C2′-H), 5.007 (2H, d, J=7.2Hz, C1′-H), 1.744, 1.722 (3H each, s, 2×CH3), according to These data are compared with the literature, and it is determined that the monomer compound is imperatorin (Imperatorin), and the molecular formula is C16H1404. figure 1 It is a liquid chromatographic analysis of imperatorin extracted from the traditional Chinese medicine Angelica dahurica. Example 2 Comparison of the Sensitivity of Liver Cancer HepG2 Cells and R-HepG2 to Clinical Antineoplastic Drugs and the Expression of P-glycoprotein

[0026] Experimental materials and methods:

[0027] Liver cancer cell HepG2 was purchased from the American Type Culture Collection in the United States. The drug...

Embodiment 3

[0037] Example 3 Inhibition of imperatorin on proliferation of HepG2 and R-HepG2 in vitro

[0038] Experimental materials and methods: cell source and MTT method are the same as in Example 2

[0039] The experimental results are attached image 3 .

[0040] The inhibition of imperatorin on the proliferation of HepG2 cells and R-HepG2 cells in vitro was dose-dependent, and R-HepG2 cells were more sensitive to it. The half-inhibitory concentration of imperatorin on HepG2 and R-HepG2 after 48 hours of action IC 50 They were 43.3 μM and 28.1 μM respectively, and the drug resistance index RI was 0.65, which was much smaller than that of adriamycin 50 (Table 1), indicating that R-HepG2 had no resistance to imperatorin.

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Abstract

The invention provides the application of imperatorin in preparing antineoplastic drugs with multi-drug resistance (MDR), wherein the imperatorin is extracted from angelica roots. The oncolytic effect of the imperatorin on tumor cells with MDR is obviously better than that of normal clinical medicines such as adriamycin, cis-platinum and the like, and the mechanism of killing high-expression P-glycoprotein tumor cells by the imperatorin is not affected by the high-expression P-glycoprotein tumor cells, the imperatorin induces the apoptosis of tumor cells with MDR and then ensure the tumor cells with MDR to be consistent with parental drug sensitive cells. Because currently, the medicines which can reverse the MDR of tumor cells clinically are lacking, the imperatorin has a good application prospect in preparing antineoplastic drugs with MDR.

Description

technical field [0001] The invention belongs to the technical field of pharmacy and relates to a new application of imperatorin, that is, the application of imperatorin in the preparation of anti-tumor multi-drug resistance drugs. Background technique [0002] Cancer chemotherapy is a basic means of treating tumors, but the effect of tumor chemotherapy will fail because tumor cells acquire drug resistance. Multidrug resistance (MDR) refers to the development of tumor cells to multiple drugs with different structures and mechanisms Cross-resistance is the main reason for the failure of chemotherapy. The mechanism of MDR is complex, one of which is related to the overexpression of the product encoded by the MDR1 gene - ATP energy-dependent drug efflux pump P-glycoprotein (P-glycoprotein, P-gp), resulting in increased drug efflux, intracellular drug In addition, it is also related to the process of apoptosis. The lack of apoptosis protein Bax or overexpression of anti-apoptosi...

Claims

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Application Information

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IPC IPC(8): A61P35/00A61K31/37
Inventor 刘非燕郭添德罗可望吴平冯国培
Owner ZHEJIANG UNIV
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