Application of (E)-1-(2, 4-dihydroxy-5-(3-methyl-butyl-2-alkenyl) phenyl)-3-(4-hydroxy-phenyl) propylene-2-ketone-1 in medicine
A hydroxyphenyl and dihydroxy technology, which is applied in the field of preparing antitumor drugs, can solve the problems of unclear function of non-classical estrogen membrane signaling pathway, etc.
Active Publication Date: 2011-03-30
BEIJING SHENOGEN BIOMEDICAL
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However, the role of the non-canonical estrogen membrane signaling pathway is still unclear
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The invention relates to a chemical compound (E)-1-(2,4-dihydroxy- 5-(3-methyl-butyl-2-alkenyl) phenyl)-3-(4-hydroxyphenyl)-propylene-2-ketone-1 and the application of the salt and solvate thereof acceptable in pharmacy in preparing drugs used for treating diseases related to estrogen receptor ER-Alpha subtype and ER-Beta subtype, belonging to the field of pharmacology. The chemical compound does not change expressions of ER-Alpha 66, ER-Alpha 46 and ER-Alpha 36 under the low concentration condition, while the expressions can be simultaneously inhibited under high concentration condition; meanwhile, the compound can kill the breast cancer MCF7 cells which can express ER-Alpha 66, ER-Alpha 46 and ER-Alpha 36; therefore, the compound can be used as a moderator of estrogen receptor ER-Alpha36 for treating diseases such as tumor, osteoporosis, asthma, heart diseases, senile dementia, etc. caused by abnormal expression of estrogen receptor ER-Alpha 36.
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)...
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IPC IPC(8): A61K31/122A61K9/20A61K9/48A61K9/10A61K9/08A61P35/00A61P19/10A61P11/06A61P9/00A61P25/28
Inventor 李靖孟坤
Owner BEIJING SHENOGEN BIOMEDICAL