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Medicine composite containing icaritin and demethylicaritin and its application

A technology of methyl epimedium and icariin is applied in the directions of drug combination, medical preparations containing active ingredients, drug delivery, etc., to achieve the effect of significant theoretical and application value and clear components

Inactive Publication Date: 2003-12-10
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0025] 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

[0042] Example 1 Estrogen-like activity of icariin and demethylicariin

[0043] In this experiment, MCF-7 estrogen-dependent breast cancer cells were used as the biological test carrier, and the classic E-SCREEN method (a classic method for detecting estrogen-like activity of compounds) was used to measure its estrogen-like activity.

[0044] A, Routine culture of MCF-7 breast cancer cells

[0045] Culture conditions: DMEM medium containing 5% fetal bovine serum, cultured in 37°C, 5% CO2 incubator. Change the medium once every 2-3 days; when the cells proliferate to 70%-80% confluent, trypsinize and passage.

[0046] B. Preparation of hormone-free human serum

[0047] 5% activated carbon and 0.5% dextran T-70 were co-incubated at 4°C for 18-24 hours under agitation, centrifuged to obtain dextran-coated activated carbon (DCC), and DCC was mixed with serum at a concentration of 5%. Stir at 4°C for 1 hour, centrifuge at 5000×g for 15 minutes, and filter to sterilize to remove ...

Embodiment 2

[0055] Example 2 Application of icariin and demethylicariin in the prevention and treatment of osteoporosis and menopausal syndrome

[0056] Given the phytoestrogen-like activities of icariin and desmethylicariin, these two compounds may be developed as effective drugs for the prevention and treatment of osteoporosis and menopausal syndrome. Basis: a. Phytoestrogens are structurally similar to endogenous estrogens, and have estrogen-like effects on bone tissue. Epidemiological investigations, animal experiments, in vitro experiments, and human experiments have found that phytoestrogens promote bone formation and inhibit bone formation. It plays an important role in the prevention and treatment of osteoporosis caused by estrogen deficiency. The more mature phytoestrogens genistein and daidzein have been used as food additives and auxiliary drugs for the prevention and treatment of osteoporosis and menopausal syndrome; structural analogs developed based on the structure of phyto...

Embodiment 3

[0057] Embodiment 3 as the application of HRT substitute medicine

[0058] The purpose of hormone replacement therapy (HRT) in postmenopausal women is to control symptoms caused by menopause and prevent osteoporosis and cardiovascular disease. At present, only 35%-40% of women accept HRT, and many of them cannot insist on using it. The reason is that estrogen has many side effects as HRT drugs, such as increased risk of breast cancer, endometrial cancer, vaginal bleeding, etc., while plants As a natural product, many estrogens have the activity of selectively regulating estrogen receptors, and at the same time exhibit estrogen activity and anti-estrogen-like activities, such as antagonizing estrogen receptors in tissues such as mammary glands and vagina, and stimulating cardiovascular and bone, etc. estrogen receptors. Therefore, studies on cardiovascular protection, lowering blood cholesterol levels, controlling menopausal symptoms and preventing osteoporosis show promising ...

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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 pharmaceutical composition and application thereof, mainly relates to the pharmaceutical composition of phytoestrogen-like effect, especially to the pharmaceutical composition containing Icaritin (Icaritin) and desmethylicaritin (Desmethylicaritin), and its Use in medicine. Background technique [0002] Phytoestrogens (Phytoestrogens) are a class of natural plant compounds with estrogen-like activity. They have anti-oxidation, anti-angiogenesis, and inhibition of cancer cell differentiation. (such as anti-free radicals, regulating enzyme activity, ion channels) for hormone-dependent cancers, cardiovascular diseases, postmenopausal osteoporosis and menopausal discomfort, early senile dementia, liver inflammation, liver fibrosis, diabetes, hyperlipidemia, It has good preventive and therapeutic effects on diseases such as immune system and viral infection. [0003] 1. Phytoestrogens and osteoporosis [0004] Osteoporosi...

Claims

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Application Information

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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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