Medicine composite containing icaritin and demethylicaritin and its application

An estrogen receptor, methyl epimedium technology, which is applied in the directions of medical preparations containing active ingredients, drug delivery, endocrine system diseases, etc., to achieve the effect of significant theoretical and practical value and clear components

Inactive Publication Date: 2005-03-30
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0026] So far, there are no domestic and foreign research reports on the estrogen-like effects of icariin and demethylicariin on the pharmacological activity and as a selective estrogen receptor modulator

Method used

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  • Medicine composite containing icaritin and demethylicaritin and its application
  • Medicine composite containing icaritin and demethylicaritin and its application
  • Medicine composite containing icaritin and demethylicaritin and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 Estrogen-like activity of icariin and desmethyl icariin

[0044] In this experiment, MCF-7 estrogen-dependent breast cancer cells were used as the biological test carrier, and the estrogen-like activity was measured by the classic E-SCREEN method (the classic method for detecting the estrogen-like activity of compounds).

[0045] A. Routine culture of MCF-7 breast cancer cells

[0046] Culture conditions: DMEM medium containing 5% fetal bovine serum, 37°C, 5% CO2 incubator. Change the medium once every 2 to 3 days; try trypsin digestion and passage when the cells proliferate to 70% to 80% confluence.

[0047] B. Preparation of hormone-removed human serum

[0048] 5% activated carbon and 0.5% dextran T-70 were incubated at 4°C for 18-24 hours under stirring conditions, centrifuged to obtain dextran-coated activated carbon (DCC), DCC was mixed with serum at a concentration of 5%, Stir at 4°C for 1 hour, centrifuge at 5000×g for 15 minutes, filter and sterilize, then...

Embodiment 2

[0056] Example 2 Application of icariin and desmethyl icariin in the prevention and treatment of osteoporosis and menopausal syndrome

[0057] In view of the phytoestrogen-like activity of icariin and desmethyl icariin, these two compounds can be developed as effective drugs for the prevention and treatment of osteoporosis and menopausal syndrome. Basis: a. Phytoestrogens are structurally similar to endogenous estrogen and have an estrogen-like effect on bone tissue. Epidemiological investigations, animal tests, in vitro tests and human tests have found that phytoestrogens promote bone formation and inhibit bone Absorption plays an important role in preventing and treating osteoporosis caused by estrogen deficiency. The mature phytoestrogens genistein and daidzein have been used as food additives and adjuvant drugs for the prevention and treatment of osteoporosis and menopausal syndrome; structural analogues developed based on the structure of phytoestrogens. Ipriflavone has been ...

Embodiment 3

[0058] Example 3 Application as an alternative medicine for HRT

[0059] The purpose of hormone replacement therapy (HRT) in postmenopausal women is to control the symptoms caused by menopause and prevent osteoporosis and cardiovascular disease. At present, only 35%-40% of women receive HRT, and many people cannot insist on using it. The reason is that estrogen has many side effects as HRT drugs, such as breast cancer, increased risk of endometrial cancer, and vaginal bleeding. As a natural product, estrogen can selectively regulate the activity of estrogen receptors, and also exhibits estrogen activity and anti-estrogen-like activity. For example, it can antagonize the estrogen receptors in breast and vagina and other tissues, and stimulate the cardiovascular and bones. The estrogen receptor at the place. Therefore, research on cardiovascular protection, lowering blood cholesterol levels, controlling menopausal symptoms and preventing osteoporosis has shown promising prospects.

...

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Abstract

The present invention provides a medicine composition including icaritin and / or demethylicaritin as active component, medicinal carrier and / or excipient and having plant female hormone action, it can be used in the preparation of medicines for curing various diseases of hormone-dependend type cancers, cardiovascular diseases, after-menopausal osteoporosis, climacteric indisposition, senile dementia, hepatitis, diabetes and others, also can be used as precursor compound of the medicine.

Description

Technical field [0001] The present invention belongs to a pharmaceutical composition and its use, and mainly relates to a pharmaceutical composition with a phytoestrogen-like effect, in particular to a pharmaceutical composition containing icariin (Icaritin) and desmethylicaritin, and its use in Medical use. Background technique [0002] Phytoestrogens is a class of natural plant compounds with estrogen-like activity. It has anti-oxidation, anti-angiogenesis, and inhibition of cancer cell differentiation. Studies have shown that phytoestrogens are regulated by receptors and non-receptor regulatory pathways. (Such as anti-free radicals, regulating enzyme activity, ion channels) for hormone-dependent cancers, cardiovascular diseases, postmenopausal osteoporosis and menopausal discomfort, early Alzheimer's disease, liver inflammation, liver fibrosis, diabetes, hyperlipidemia, Immune system, virus infection and other diseases have better preventive and therapeutic effects. [0003] 1...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/7048A61P5/30A61P7/00A61P7/04A61P9/10A61P15/14
Inventor 楼宜嘉王志强叶海涌刘健朱丹雁
Owner ZHEJIANG UNIV
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