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Use of 7-hydroxyl-3-[(4-hydroxyl)-3-(3-methyl- butyl-2- alkenyl) phenyl]-4H-1-benzopyran-4-ket

A compound and pharmaceutical technology, applied in the field of medicine, can solve the problems such as unclear role of non-classical estrogen membrane signaling pathway

Active Publication Date: 2010-04-14
BEIJING SHENOGEN BIOMEDICAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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-hydroxyl-3-[(4-hydroxyl)-3-(3-methyl- butyl-2- alkenyl) phenyl]-4H-1-benzopyran-4-ket
  • Use of 7-hydroxyl-3-[(4-hydroxyl)-3-(3-methyl- butyl-2- alkenyl) phenyl]-4H-1-benzopyran-4-ket
  • Use of 7-hydroxyl-3-[(4-hydroxyl)-3-(3-methyl- butyl-2- alkenyl) phenyl]-4H-1-benzopyran-4-ket

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Experimental program
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Effect test

Embodiment 1

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

[0033] 1.1 Test:

[0034] Experimental method: pre-blot filter sheets containing different human breast cancer tissue proteins were purchased from ProSci (Poway, CA). Anti-ERα36 antibody specific to ERα36 was used [ER-α36-specific antibody (20 amino acids on ER-α36 C-terminus) was prepared by Alpha Diagnostic International (San Antonio, TX). Proc. Natl. Acad. Sci. USA, 2006, 103(24):9063-9068], HRP-labeled secondary antibody and enhanced chemiluminescence reagent (ECL, AmerSham PharmaciaBiotech) 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 5) and non-invasive duc...

Embodiment 2

[0046] Example 2 In vivo antitumor pharmacodynamics test of the compound of formula (I)

[0047] 2.1 The effect on human breast cancer BCAP-37

[0048] 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 the...

Embodiment 4

[0075] The pharmacodynamics test of embodiment 4 formula (I) compound formula (I) to senile dementia

[0076] Estrogen receptors are widely distributed in the basal forebrain, diencephalon, midbrain, hippocampus, amygdala, cerebral cortex, and cerebellar cortex, with gender differences. Alzheimer's Disease is the most common type of senile dementia, and the incidence of AD in elderly women is 1.5 to 3 times that of men of the same age. Epidemiological data show that among healthy postmenopausal women who have previously received or are currently receiving estrogen replacement therapy, the incidence of AD is lower than that of women who have never received it, and the level of estrogen in postmenopausal women is related to AD. The incidence is inversely proportional (Aging Clin.Exp.Res.2007,19(2):165-168; Alzheimer Disease Associated Disorder 200620(4):322-323; Proc.Natl.Acad.Sci.USA.2006103(45): 16983-16988.

[0077] J Alzheimers Dis.20069(3):273-278). PC-12 cell is a common...

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Abstract

The invention relates to a usage of 7- hydroxy-3-[(4-hydroxy-3-(3-methyl-butyl-2-alkenyl) phenyl)]-4H-1-benzopyranyl-4-ketone and application of the compound or acceptable salt or flux mixture on thecompound pharmacy to preparing treat and relative disease of deestrogen receptor ER-alpha, which is characterized by the following: keeping not changing expression of ERalpha66, ERalpha46 and ERalpha36in concentration condition through experiment to prove; inhibiting the expression of the three through the high concentration compound at the same time; killing the MCF7 cells of breast cancer cellst hat expressing ERalpha6, ERalpha46 and ERalpha36 through the compound. So the compound can be conditioning agent of the ERalpha36 for treating the diseases because of the expression of ERalpha36, suchas tumor, osteoporosis, asthma and heart diseases or senile dementia symptoms.

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, 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 BiochemMol 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, JPsychiatry Neurosci, 2002, 27(1): 1-27], so ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61K9/00A61P35/00A61P19/10A61P9/00A61P25/28A61P11/06C07D311/36
Inventor 孟坤李靖
Owner BEIJING SHENOGEN BIOMEDICAL
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