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Application of cucurbitacin b and its analogues in the preparation of medicines for treating endometrial cancer

A technology for endometrial cancer, cucurbitacin, applied in the field of medicine

Active Publication Date: 2016-06-01
国药集团工业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But, up to now, also do not see the related report of cucurbitacin B treatment endometrial cancer, therefore, research and development a kind of cucurbitacin B and its analog as the application in the preparation for the treatment of endometrial cancer medicine has always been an urgent problem to be solved. new subject of

Method used

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  • Application of cucurbitacin b and its analogues in the preparation of medicines for treating endometrial cancer
  • Application of cucurbitacin b and its analogues in the preparation of medicines for treating endometrial cancer
  • Application of cucurbitacin b and its analogues in the preparation of medicines for treating endometrial cancer

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Inhibitory effect of cucurbitacin B on the autoactivity (phosphorylation) of epithelial growth factor receptor in cultured endometrial carcinoma.

[0020] 1. Human endometrial carcinoma expresses epithelial growth factor receptor.

[0021] experimental method:

[0022] Cell culture:

[0023] Fluorescence real-time quantitative PCR (Real-timePCR)

[0024] Cells were homogenized, RNA was extracted with Trizol, and then reverse-transcribed into cDNA using a kit (TaKaRa Biotechnology, Dalian, China), and amplified using a SYBRGreen fluorescent quantitative PCR kit (Agilent Technologies, NC, USA). The primers for epithelial growth factor receptor and housekeeping gene ?-actin were

[0025] F: 5'-TGATTGGGGATCTTGGAGTTTT-3

[0026] R: 5'-CTTGTGGCTTGTGCTCCTTG-3';

[0027] F:5'-TGGCACCCAGCACAATGAA-3'

[0028] R: 5'-CTAAGTCATAGTCCGCCTAGAAGCA-3'.

[0029] Prepare 20 μl standard PCR reaction system: 10 μl 2x SYBR green PCR mixture; 0.3 μl 500x ROX dye; 2 μl PCR front-strand ...

Embodiment 2

[0040] Cucurbitacin B inhibits the activation (phosphorylation) of epithelial growth factor receptors induced by epithelial growth factor in cultured endometrial carcinomas HEC-1-A and HEC-1-B in vitro.

[0041] experimental method:

[0042] Cell culture: Same as above.

[0043] There is no serum in the incubation solution, add 50, 100 and 200nM cucurbitacin B for 15 minutes, then add epithelial growth factor 10ng / ml, and detect the activity of epithelial growth factor receptor (Y1173 position) by immunogel electrophoresis and immunoprecipitation after 10 minutes point phosphorylation).

[0044] Immunogel electrophoresis and co-immunoprecipitation: same as above.

[0045] see results Figure 4 .

[0046] Experiments have confirmed that cucurbitacin B inhibits the activation of epithelial growth factor receptors caused by epithelial growth factor in human endometrial cancer HEC-1-A and HEC-1-B at concentrations above 50 nM.

Embodiment 4

[0048] Cucurbitacin B inhibited the proliferation of endometrial cancer HEC-1-B cultured in vitro.

[0049] experimental method:

[0050] Cell culture: Same as above.

[0051] MTT method to detect tumor cell growth inhibition rate:

[0052] Tumor cells were seeded in 96-well culture plates, 1×10 5 cells / well and incubated overnight to allow them to adhere to the wall.

[0053] Add 200μl cucurbitacin B incubation solution (concentrations are 0, 50, 100, 200, 400, 800nM respectively) and continue to incubate for 48h, add 20lMTT (5mg / mL) to incubate for 4h, discard the culture solution, dissolve with 100lDMSO, read the absorbance at 570nm wavelength of each well ( OD) value A. The culture medium was used instead of drugs as the control group. Calculate the cell inhibition rate according to the A value, and the calculation formula is inhibition rate=[(average A value of the control group-average A value of the blank control group)-(mean A value of the experimental group-avera...

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Abstract

The invention discloses an application of cucurbitacin B and analogs thereof in the preparation of drugs for treating endometrial cancer, wherein the analogs are generated by changing the groups in the R1, R2, R3, R4, R5, X, Y, a, and b positions in the cucurbitacin B molecule, and the drugs can be used to carry out an individualized treatment for endometrial cancer patients, wherein the endometrial cancer can be idiopathic or metastatic. Cucurbitacin B and analogs thereof can be any pharmaceutically acceptable cucurbitacin B and analogs thereof, the cucurbitacin B and analogs thereof have one or more components which have the function of inhibiting epidermal growth factor receptor (EGFR), the cucurbitacin B and analogs thereof can be individually used to cure cancer or can be used with other treatments or drugs, such as radiotherapy, chemotherapy, surgical therapy, other growth factor inhibitors and sex hormone inhibitors, and any drugs or methods for treating cancer. Through inhibiting the epidermal growth factor receptor (EGFR), the cucurbitacin B and analogs thereof inhibit the tumor cell proliferation so as to achieve the goal of individualized treatment, and the cucurbitacin B and analogs thereof can be individually used to treat cancer or used with other drugs or treatments for cancer treatment.

Description

technical field [0001] The invention relates to the application of cucurbitacin B and its analogs in the field of medical technology as a medicine for treating endometrial cancer. Background technique [0002] Cucurbitacin B and its analogues belong to a class of tetracyclic triterpenoids with a 19-methyl group appearing at the C-9 position. They are mainly distributed in Cucurbitaceae plants and are a class of natural substances with known structures. The plain tablet is used clinically for the treatment of hepatitis and liver cancer. The main ingredient in the cucurbitacin tablets currently on the market is cucurbitacin B. In vivo and in vitro experiments found that cucurbitacin B has anti-tumor effects (see review: Zhang Yanting et al., Chinese Journal of Pharmacology and Toxicology, 26:212-215, 2012). The research on its drug action mechanism is still inconclusive, and the main finding is the inhibition of intracellular STAT3 and MAPK signal transduction (see review: L...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/575A61P35/00A61P15/00
Inventor 黄荣
Owner 国药集团工业有限公司
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