Compounds and methods for treating estrogen receptor-related diseases

A compound and disease technology, applied in the fields of botanical equipment and methods, active ingredients of heterocyclic compounds, sexual diseases, etc., can solve the problem of unclear Herba Epimedii

Active Publication Date: 2009-09-09
BEIJING SHENOGEN PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Compounds and methods for treating estrogen receptor-related diseases
  • Compounds and methods for treating estrogen receptor-related diseases
  • Compounds and methods for treating estrogen receptor-related diseases

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0169] Example 1. Expression of ER-alpha variants in human breast cancer samples

[0170] Membranes pre-blotted with human breast cancer tissue were purchased from ProSci Corporation (Poway, CA). The membrane was detected with an anti-ER-[alpha]36 antibody that specifically recognizes ER-[alpha]36 and a HRP-conjugated secondary antibody, and visualized with an enhanced chemiluminescence (ECL) detector (Amersham Pharmacia Biotech). The same membrane stripping was detected with the anti-estrogen receptor-α antibody H222 (Novocastra Laboratories Ltd, UK), which recognizes all three subtypes of ER-α - ER-α66, ER-α46 and ER-α36. figure 1 It is shown that ER-α66, ER-α46 and ER-α36 were not expressed in normal breast tissue (lane 1) but in one specimen of invasive ductal carcinoma (lane 2), one specimen of invasive lobular carcinoma (lane 5). ) and non-invasive ductal carcinoma (lane 7). In addition, ER-[alpha]36 was expressed in invasive ductal carcinoma (lane 4) and in another sa...

Embodiment 2

[0171] Example 2. ER-α36 is expressed in ER-negative breast cancer cell line MDA-MB-231

[0172] The MDA-MB-231 cell line is known to lack ER-α66 and ER-α46 (Relevance of breast cancer cell lines as models for breast tumors: an update. Marc Lacroix, Guy Leclercq, Brest Cancer Research and Treatment 83: 249-289 (2004)) . MDA-MB-231 cells were obtained from the American Type Culture Collection (ATCC). MDA-MB-231 cells at 37 °C, 5% CO 2 Grow for 12 hours in Dulbecco's modified Eagle's medium (DMEM) and 10% fetal bovine serum on atmospheric 8-well BIOCOAT chamber slides (BDScience Discovery Labware). The cells were then washed twice with sterile phosphate buffered saline (PBS) and fixed with 4% paraformaldehyde in PBS (pH 7.4) for 30 minutes at room temperature. Thereafter, the cells were washed with PBS and permeabilized with 0.5% (v / v) Triton X-100 for 10 minutes. The cells were then washed with PBS and blocked with 3% serum in PBS for 1 hour at room temperature. The chambe...

Embodiment 3

[0173] Example 3. Icaritin induces cell death in ER-negative breast cancer MDA-MB-231 cells

[0174] Keep MDA-MB-231 cells at 37 °C, 5% CO 2 Atmosphere of DMEM and 10% FBS. The cells were 1×10 in each 60mm dish 5 Cell density spot plate. MDA-MB-231 cells were treated with icariin dissolved in DMSO at concentrations of 0, 1 μM, 5 μM and 10 μM. Epimedium was purchased from Shanghai Yousi Biotechnology Co., Ltd. The treated cells were detected under a Nikon TS100 inverted microscope and the morphological changes were photographed. image 3 It was shown that when treated with 10 μM icariin, the cells exhibited characteristics of apoptotic cells and the number of viable cells was significantly reduced.

[0175] In addition, MDA-MB-231 cells were treated with tamoxifen, ICI 182,780, luteolin, and icariin at concentrations of 0, 5 μM, 10 μM, 20 μM, 30 μM, 40 μM and 50 μM to detect the effects of these compounds on MDA - Effect on growth of MB-231 cells. Tamoxifen and Luteolin ...

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Abstract

The invention provides, in certain embodiments, compounds, pharmaceutical compositions and methods for modulating the functions of estrogen receptor alpha 36, for preventing and/or treating diseases related to estrogen receptor alpha 36, for preventing and/or treating respiratory diseases such as asthma, for inducing cell death and/or inhibiting cell proliferation and for preventing and/or treating diseases involving abnormal cell proliferation such as cancers.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of US Provisional Patent Application No. 60 / 862,984, filed October 25, 2006, the entire contents of which are incorporated herein by reference. technical field [0003] The present invention relates to compounds, pharmaceutical compositions and methods for preventing and / or treating diseases associated with estrogen receptors. Background technique [0004] Estrogens are a group of hormones involved in many key physiological functions in the body. Estrogen functions include developing the female sex organs, conditioning the mammary glands and uterus for pregnancy and breastfeeding after childbirth. Estrogen also plays an important role in maintaining normal cardiovascular function and bone density. Estrogen is known to promote cell proliferation and may increase a woman's risk of developing cancer, especially breast and uterine cancers. [0005] Estrogen binds to estrogen receptors...

Claims

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Application Information

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IPC IPC(8): A01N43/42A61K31/44
CPCA61K31/352A61P1/02A61P1/04A61P11/00A61P11/06A61P11/08A61P15/08A61P15/10A61P17/00A61P19/08A61P19/10A61P25/00A61P25/14A61P25/16A61P25/20A61P25/22A61P25/24A61P25/28A61P27/16A61P29/00A61P3/04A61P35/00A61P35/02A61P3/06A61P37/02A61P43/00A61P9/00A61P9/10A61P9/12
Inventor 李靖孟坤
Owner BEIJING SHENOGEN PHARMA GRP
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