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Use of 7-hydroxy-3-[(4-hydroxy)-3-((E)-3,7-dimethyl-octyl-2,6-diolefin)phenyl]-4H-1-benzopyran-4-ketone

A compound and pharmaceutical technology, applied in the field of medicine, can solve the problem of unclear function of non-classical estrogen membrane signaling pathway

Active Publication Date: 2008-03-12
BEIJING SHENOGEN BIOMEDICAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the role of the non-canonical estrogen membrane signaling pathway is still unclear

Method used

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  • Use of 7-hydroxy-3-[(4-hydroxy)-3-((E)-3,7-dimethyl-octyl-2,6-diolefin)phenyl]-4H-1-benzopyran-4-ketone
  • Use of 7-hydroxy-3-[(4-hydroxy)-3-((E)-3,7-dimethyl-octyl-2,6-diolefin)phenyl]-4H-1-benzopyran-4-ketone
  • Use of 7-hydroxy-3-[(4-hydroxy)-3-((E)-3,7-dimethyl-octyl-2,6-diolefin)phenyl]-4H-1-benzopyran-4-ketone

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Example 1 In Vitro Biological Test of Formula (I) Compound

[0033] Test 1-1:

[0034] Experimental method: pre-blot filter sheets containing breast cancer tissue proteins from different patients were purchased from ProSci Company (Poway, CA). Use an anti-ERα36 antibody specific to ERα36 [ER-α36-specific antibody (for 20 amino acids at the C-terminus of ER-α36) was prepared by Alpha Diagnostic International (San Antonio, TX), see Proc.Natl.Acad.Sci.USA, 2006, 103 (24): 9063-9068], HRP-labeled secondary antibody and enhanced chemiluminescence reagent (ECL, AmerShamPharmacia Biotech) detect the filter and develop color. After the membrane was eluted, the membrane piece was detected using anti-ERα antibody H222 (Novocastra Laboratories Ltd, UK), which can simultaneously detect three subtypes of ER (ERα66, ERα46 and ERα36). (See Figure 2)

[0035] Test results: ERα66, ERα46 and ERα36 were expressed in invasive ductal carcinoma (lane 2), invasive lobular carcinoma (lane ...

Embodiment 2

[0047] Example 2: In vivo antitumor pharmacodynamics test of the compound of formula (I)

[0048] 2-1 The effect on human breast cancer BCAP-37

[0049] Experimental method: 25 BALB / c-nu nude mice with an average body weight of 19-21 g were used. Before the experimental administration, the human breast cancer BCAP-37 tumor strain was transplanted into the axilla of the right forelimb of the nude mice. With reference to the antineoplastic drug "Tamoxifen (Tamoxifen) clinical human effective oral dose 10-20mg, orally, 2 times / day calculation, the compound (I) is established as a single dose group, namely: 33mg / kg (0.66mg / day / day) In addition, a positive drug tamoxifen control group (16.5mg / kg, 0.33mg / day / only) and a negative tumor-bearing nude mouse control group were set up. There were 9 nude mice in each treatment group, and the negative tumor-bearing nude mice Rat control group consisted of 7 nude mice, female. Oral gavage was used for administration, once a day. After th...

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Abstract

The present invention relates to the application of the 7-hydroxy-3-[(4-hydroxy)-3-((E)-3, 7-dimethyl-octyl-2, 6-alkenyl) phenyl]-4H-1-benzopyran-4-ketone, belonging to the medical field. The expression of ER alpha 66, ER alpha 46 and ER alpha 36 of the compound will not change under the low-concentration condition; the expression of ER alpha 66, ER alpha 46 and ER alpha 36 can be inhibited at the same time under the high-concentration condition. At the same time, the compound can kill the breast cancer cell MCF7 cell which can express the ER alpha 66, ER alpha 46 and ER alpha 36. Therefore, the compound can be used as regulator of the estrogen receptor FR alpha 36 used for treating the diseases caused by the abnormal expression of the estrogen receptor FR alpha 36, such as the tumor, osteoporosis, asthma, heart disease or Alzheimer's disease and other diseases.

Description

technical field [0001] The invention belongs to the field of medicine and relates to the application of natural compounds in the preparation of antitumor drugs, osteoporosis and senile dementia drugs. Background technique [0002] Estrogen is a steroid hormone produced by the endocrine system, which plays an important role in the reproductive system, bone tissue, cardiovascular system, immune system and central nervous system [J Cell Sci, 2003; 116(4): 585-586]. The estrogen signaling system plays an important role in the regulation of cell growth, differentiation and apoptosis. The occurrence and development of estrogen-dependent tumors, such as breast cancer, ovarian cancer and endometrial cancer, are closely related to estrogen [J Steroid Biochem.Mol.Biol., 2002, 81(1): 1-24 , J Mammary Gland Biol. Neoplasia, 1998, 3(1): 49-61, Curr. Drug Targets Immune Endocr. Metabol. Disord; 2001, 1(1): 1-12, Cancer Res., 1998, 58(23) : 5367-5373, J Psychiatry Neurosci, 2002; 27 (1)...

Claims

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Application Information

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IPC IPC(8): C07D311/34A61K31/352A61P35/00
Inventor 李靖孟坤
Owner BEIJING SHENOGEN BIOMEDICAL
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