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Application of Calycosin Derivatives in Preparation of Drugs for Treating ER-Negative Breast Cancer

A breast cancer and drug technology, applied in the field of medicine, can solve the problems of high effective concentration and unclear target

Active Publication Date: 2019-11-15
GUILIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Existing studies have shown that calycosin has the functions of anti-oxidative stress, anti-virus and regulation of cell apoptosis, but its disadvantage is that its effective concentration is relatively large, and the target is not clear

Method used

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  • Application of Calycosin Derivatives in Preparation of Drugs for Treating ER-Negative Breast Cancer
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  • Application of Calycosin Derivatives in Preparation of Drugs for Treating ER-Negative Breast Cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1: the synthesis of the compound shown in the formula (I) used in the following each experimental examples of the application:

[0033] Synthesized according to the following synthetic route:

[0034]

[0035] Among them, the chemical name of compound 1 is: 7-hydroxy-3-(3-hydroxy-4-methoxy)-4H-benzopyran-4-one, and the chemical name of compound 2 is: 1,2-di Bromoethane, the chemical name of intermediate product 3 is: 7-(2-bromoethoxy)-3-(3-(2-bromoethoxy)-4-methoxyphenyl)-4H-benzo Pyran-4-one, the chemical name of compound 4 is: morpholine; the chemical name of compound 5 is: 3-(4-methoxy-3-(2-morpholinoethoxy)phenyl)-7 -(2-Morpholinoethoxy)-4H-benzopyran-4-one.

[0036] The specific synthesis method is:

[0037]1) Take 7-hydroxy-3-(3-hydroxy-4-methoxy)-4H-benzopyran-4-one (300mg) and 1,2-dibromoethane in a molar ratio of 1:8 Dissolve in 13mL of acetone, then use triethylamine to adjust the pH of the system to 10, react at room temperature for 8h, spin...

experiment example 1

[0049] Experimental example 1: Detection of endothelial cell proliferation by MTT method

[0050] Take SKBR3, MDA-MB-468 that has reached 90% confluence, wash and digest, and make cell suspension. After counting, press 1x10 4 Each well was seeded in a 96-well plate, and cultured for 24 hours until the cells were completely adhered to the wall. In the experimental group, different concentrations of CAG002 (1 μM ~ 15 μM) were added to the groups, and each group had 9 replicate wells, and 200 μl / well of the low serum culture medium containing the drug was added. Two groups of controls were set at the same time, the blank control group was 0.1% DMSO culture solution, and the positive control was 15 μM calycosin.

[0051] MTT results showed that CAG002 could inhibit the proliferation of ER-negative breast cancer cells (SKBR3, MDA-MB-468) in a dose-dependent manner. Among them, when the drug concentration was 15 μM, the inhibitory effect was the most obvious. Compared with the bl...

Embodiment 2

[0052] Example 2: Long-chain non-coding chip detection CAG002 affects SKBR3 gene expression in ER-negative breast cancer cells

[0053] SKBR3 cultured in 10cm 2 Petri dish to 90% confluent. After the original culture solution was removed, it was treated with a culture solution containing 15 μM CAG002 for 48 hours, and 0.1% DMSO was used as a blank control. According to the instructions of TRIZOL reagent, the total cellular RNA was extracted, and the samples were sent to Huada Genomics Company for long-chain non-coding chip detection. The drug down-regulated 116 long-chain non-coding RNAs, of which 10 long-chain non-coding RNAs such as MALAT1 were the most obvious, and MALAT1 It is 0.192 of the control group, and the results are shown in Table 1.

[0054] Table 1: Long-chain non-coding microarray detection of CAG002 affecting SKBR3 gene expression in ER-negative breast cancer cells

[0055]

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Abstract

The invention discloses application of a calycosin derivative in preparation of a drug for treating an ER feminine breast cancer. An applicant finds through an experiment that the calycosin derivativecan lower the expression levels of MALAT1 and GPR30, inactivate ERK1 / 2 and Akt phosphorylation levels and inhibit cell proliferation of the ER negative breast cancer. An MTT experiment shows that theproliferation effect of inhibiting SKBR3 and MDA-MB-468 of the compound shown in a formula (I) is most obvious when the amount is 15 microns, while the same concentration of calycosin (15 microns) has no obvious effect on cell proliferation of SKBR3 and MDA-MB-468. The structure of the calycosin derivative is represented in the following formula (I) (shown in the description).

Description

technical field [0001] The invention relates to the application of a calycosin derivative in the preparation of a medicine for treating ER-negative breast cancer, and belongs to the technical field of medicine. Background technique [0002] Breast cancer accounts for approximately 30% of all adult female tumors. In the United States, breast cancer is the second leading cause of death among all gynecological cancers. According to the phenotypic differences of estrogen receptor (ER), breast cancer can be divided into two subtypes: ER positive and ER negative. Clinically, ER-negative breast cancer is more difficult to treat. ER is a member of the nuclear receptor superfamily and is divided into two subtypes: ERα and ERβ. Preliminary experiments have shown that ERα mediates endothelial cell proliferation and angiogenesis through classical genomic and rapid non-genomic effects. For ER-negative breast cancer, non-genomic effects play a more important role in its growth and deve...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/5377A61P35/00
CPCA61K31/5377
Inventor 陈健夏春波田晶王勇叶雨
Owner GUILIN MEDICAL UNIVERSITY
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