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Application of fulvestrant in preparing antimicrotubular chemotherapeutic drug resistance reversal agent

A technology of fulvestrant and chemotherapeutic drugs, which is applied in the field of preparation of anti-microtubule chemotherapeutic drug resistance reversal agent of fulvestrant, achieving effects of less side effects, good clinical application prospects, and good patient tolerance

Inactive Publication Date: 2011-08-17
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no published literature showing that fulvestrant has any application prospects in reversing multidrug resistance in breast cancer

Method used

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  • Application of fulvestrant in preparing antimicrotubular chemotherapeutic drug resistance reversal agent
  • Application of fulvestrant in preparing antimicrotubular chemotherapeutic drug resistance reversal agent
  • Application of fulvestrant in preparing antimicrotubular chemotherapeutic drug resistance reversal agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: BCap37, Bats-72 and Bads-200P-glycoprotein and ER-α expression detection

[0022] (1) Experimental materials

[0023] Cell lines: paclitaxel-sensitive cell line BCap37 (purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences), two new cell lines Bats-72 and Bads-200 (strain numbers are CCTCC No: C201065 and CCTCC No: C201066, which have been in the prior application 201010502654.6 As a new cell line protection), the P-gp positive cell line MCF7 / ADR (purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences), and the estrogen receptor alpha positive cell line is MCF-7 (purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences);

[0024] Reagent consumables: 1640 culture medium (Hangzhou Jinuo Biomedical Technology Co., Ltd.), 0.25% trypsin (Hangzhou Jinuo), super neonatal bovine serum (Shanghai Yikesai Biological Products Co., Ltd.), PBS, Tween-20, 100mm culture Dishes (Corning), protein lysate (Beiyuntian), BCA ...

Embodiment 2

[0034] Example 2: Detection of drug resistance of Bats-72 and Bads-200 (taking paclitaxel as an example).

[0035] (1) Experimental materials

[0036] Cell lines: Paclitaxel-sensitive cell line BCap37, novel cell lines Bats-72 and Bads-200

[0037] Reagent consumables: 1640 culture medium (Hangzhou Gino), 0.25% trypsin (Hangzhou Gino), super neonatal bovine serum (Shanghai Ekesai), 100mm culture dish (Corning), 96-well plate (Corning), DMSO (Shanghai Sinopharm), MTT, Paclitaxel.

[0038] Instruments: cell incubator, ultra-clean bench, hemocytometer, microplate reader.

[0039] (2) Experimental method

[0040]BCap37 and Bads-200 were inoculated on 100mm culture dishes, cultivated for 72 hours, replaced with fresh culture medium, digested with 0.25% trypsin, collected cells, counted cells, prepared single cell suspension at a concentration of 20000 cells / ml, and inoculated 0.2ml per well The single cell suspension was transferred to a 96-well plate with 4000 cells per total,...

Embodiment 3

[0045] Example 3: Toxicity detection of fulvestrant on Bats-72 and Bads-200 cells.

[0046] (1) Experimental materials

[0047] Cell lines: new cell lines Bats-72 and Bads-200;

[0048] Reagent consumables: 1640 culture medium (Hangzhou Gino), 0.25% trypsin (Hangzhou Gino), super neonatal bovine serum (Shanghai Ekesai), 100mm culture dish (Corning), 96-well plate (Corning), DMSO (Shanghai Sinopharm), MTT, Paclitaxel.

[0049] Instruments: cell incubator, ultra-clean bench, hemocytometer, microplate reader.

[0050] (2) Experimental method

[0051] Bats-72 and Bads-200 were inoculated on 100mm culture dishes, cultured 72, replaced with fresh culture medium, digested with 0.25% trypsin, collected cells, counted cells, prepared a single cell suspension with a concentration of 20000 / ml, inoculated 0.2 ml single cell suspension to 96-well plate, each total cell number is 4000, cultivate overnight, add fulvestrant to treat the concentration gradient of 0, 10, 20, 50, 100, 200, 5...

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Abstract

The invention provides application of fulvestrant in preparing an antimicrotubular chemotherapeutic drug resistance reversal agent. The fulvestrant reverts antimicrotubular chemotherapeutic drug resistance of breast cancer cells without relying whether estrogen receptors are expressed or not and also without relying whether the function of restricting P-glycoprotein is achieved or not. The fulvestrant and the antitumor drugs which are used together can accelerate the antitumor drugs to induce apoptosis of drug-resistance cells of breast cancer with negative estrogen receptors. The fulvestrant has been approved to be used for clinics and has the advantages of less side effects, good tolerance of a patient, less cross drug resistance with other estrogen receptor regulators or chemotherapeutic drugs, and the like, has clinical operability while being collaboratively used with common chemotherapeutic drugs for clinically treating the breast cancer, such as taxol, adriamycin, vinorelbine, and the like and has favorable clinical application prospect as the antimicrotubular chemotherapeutic drug resistance reversal agent for treating the drug-resistance breast cancer.

Description

(1) Technical field [0001] The invention relates to a new application of fulvestrant in the preparation of an anti-microtubule chemotherapeutic drug resistance reversal agent. (2) Background technology [0002] Malignant tumor is currently one of the leading causes of death in many countries in the world including China (CA Cancer J Clin. 2005, 55: 74-108.). The World Health Organization (WHO) warned at the 2008 International Oncology Annual Meeting held in Atlanta, USA that by 2010 cancer will replace cardiovascular disease as the disease with the largest number of deaths in the world. According to statistics from the Ministry of Health of my country, there are 1.6 to 1.7 million new cancer patients in my country every year, and the total number of existing cancer patients is about 4.5 million, ranking first among the deadly diseases. Breast cancer has also become the number one "killer" of women's health today. [0003] Microtubules are involved in the mitotic process. I...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/566A61K31/337A61K31/475A61P35/00
Inventor 范伟民蒋东海隋梅花
Owner ZHEJIANG UNIV
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