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Application of biphenyl cyclooctadiene lignin in treatment of tumour medicine

A technology of biphenyl cyclooctadiene lignan and biphenyl cyclooctadiene, which is applied in the application field of biphenyl cyclooctadiene lignan in the preparation of drugs for treating tumors, and can solve the problem of anti-tumor multidrug resistance. Drugs, no anti-tumor reports, etc.

Inactive Publication Date: 2006-09-20
胡汛 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Biphenylcyclooctadiene lignans are Schisandra chinensis: the main component in the dry mature fruit of Magnoliaceae Schisandra chinensis (Turcz.) Baill. or Magnoliaceae Schisandra sphenanthera Rehd.et Wils. It is listed as the top grade in Materia Medica, and has the effects of astringent, astringent, nourishing qi and promoting body fluid, nourishing the kidney and calming the heart. It is a nourishing and strengthening drug commonly used in traditional Chinese medicine. In particular, there are no reports of antitumor multidrug resistance

Method used

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  • Application of biphenyl cyclooctadiene lignin in treatment of tumour medicine
  • Application of biphenyl cyclooctadiene lignin in treatment of tumour medicine
  • Application of biphenyl cyclooctadiene lignin in treatment of tumour medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0119] Example 1: Detection of P-glycoprotein (P-gp) and MRP1 in multidrug resistant cells.

[0120] (1) Experimental materials:

[0121] Cell lines: K562 / adr, MCF7 / adr and KBV200 multi-drug resistant cell lines are cells with high expression of Pgp protein. K562 / adr was induced by Zhejiang University Cancer Institute, and MCF-7 / adr and KBV200 multidrug-resistant cell lines were purchased from Institute of Hematology, Chinese Academy of Medical Sciences. HL60 / adr is a multidrug-resistant tumor cell line with high expression of MRP1, which was purchased from the Institute of Hematology, Chinese Academy of Medical Sciences.

[0122] Reagent: The monoclonal fluorescently labeled antibody of P-gp is R-PE-17F9 from BD Company, USA. MRP1 monoclonal fluorescent antibody was purchased from Santa Cruz, USA.

[0123] Instruments: culture flasks, culture plates, carbon dioxide incubators, flow cytometer (FACS Calibur, American Becton-Dickinson Company).

[0124] (2) Experimental meth...

Embodiment 2

[0134] Example 2: Reversal of P-glycoprotein-mediated tumor multidrug resistance by biphenyl cyclooctadiene lignans

[0135] In order to prove that the lignans with biphenylcyclooctadiene can reverse the P-glycoprotein-mediated tumor multidrug resistance, we used 10 kinds of biphenylcyclooctadiene lignans with different structures. studied. The 10 biphenylcyclooctadiene lignans are: Schisandrin A, Schisandrin B, Schisandrin C, Schisandrin Ester A, Schisandrin Ester B, Schisandrin Ester C, Schisandrin Ester D, Schisandrin E, Schisandrin A , and schisandrol B. These lignans were purchased from China Institute of Biological Products and Drug Identification and Chengdu Cisco Huasheng Biotechnology Co., Ltd.

[0136] Cell lines: K562 / adr, MCF7 / adr, KBV200 multi-drug resistant cell lines with high expression of Pgp protein as the main drug resistance mechanism.

[0137] Reagents: Dissolve various biphenylcyclooctadiene lignans in DMSO respectively to make 10 mg / ml as a mother sol...

Embodiment 3

[0144] Example 3: Biphenylcyclooctadiene Lignans Inhibit MRP1-Mediated Tumor Multidrug Resistance

[0145] (1) Experimental materials:

[0146] Cell line: HL60 / adr multi-drug resistant cell line has high expression of MRP1 protein as the main drug resistance mechanism.

[0147] Reagents: Dissolve various biphenylcyclooctadiene lignans in DMSO respectively to make 10 mg / ml as a mother solution, and then use RPMI-1640 to make a working solution; daunorubicin.

[0148] Instruments: flasks, plates, FCM.

[0149] (2) Experimental method:

[0150] FACS analysis of daunorubicin accumulation in cells: HL60 / adr cells were cultured in fresh medium without drugs. The experiment was divided into two groups, the control group and the reversal group. Add fresh culture medium to the control group, add biphenyl cyclooctadiene lignan to the final concentration of 10 μg / ml in the reversal group, add daunorubicin DNR after incubation for 1 hour, the concentration is 2 μg / ml, and incubate at 37...

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Abstract

An application of the biphenyl cyclooctadiene lignan in preparing the medicine for treating tumor by poisoning the tumor cells and reversing the resistance of tumor cells to multiple medicines is disclosed.

Description

(1) Technical field [0001] The invention relates to the application of biphenylcyclooctadiene lignans in the preparation of drugs for treating tumors, especially the application of biphenyl cyclooctadiene lignans in the preparation of anti-tumor cell multidrug resistance reversal agent drugs. (2) Background technology [0002] Tumor is one of the main causes of human death, and tumor chemotherapy is a major means of treating tumors. However, cancer chemotherapy will fail because tumor cells acquire drug resistance. [0003] There are many reasons for the multidrug resistance of tumor cells, the most important of which is the expression of ATP-binding transporters [ATP binding cassette (ABC) transporters] in tumor cells. P-glycoprotein (P-glycoprotein, P-gp), multidrug resistant associated protein 1 (MRP1) and breast cancer resistance protein (BCRP, also known as MXR or ABCG2), It is currently recognized as several major proteins that lead to tumor multidrug resistance. Th...

Claims

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Application Information

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IPC IPC(8): A61K31/075A61K31/216A61K31/36A61K45/06A61K9/08A61K9/16A61K9/20A61K9/48A61P35/00
Inventor 胡汛
Owner 胡汛
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