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Drug combination containing prunetin and application thereof in drugs

A composition, the technology of prunus, which is applied in the direction of drug combination, medical preparation containing active ingredients, pharmaceutical formula, etc.

Inactive Publication Date: 2010-03-17
SHANGHAI INST OF PHARMA IND +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] So far, there are no domestic and foreign research reports on red cloverin, prunin or their glycosides as selective estrogen receptor modulators and related medical applications

Method used

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  • Drug combination containing prunetin and application thereof in drugs
  • Drug combination containing prunetin and application thereof in drugs
  • Drug combination containing prunetin and application thereof in drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Estrogen-like activities of pratensein and prunetin

[0034] In this experiment, MCF-7 estrogen-dependent breast cancer cells were used as the biological test carrier, and the estrogen-like activity was determined by the classic E-SCREEN method.

[0035] In this experiment, DMSO solvent control group (negative), 1nM estradiol control group (positive), red cloverin group (1uM, 10uM) and peraxanthin group (1uM, 10uM) were set.

[0036] The results show that: red cloverin and prunus can significantly promote the proliferation of MCF-7 cells, and have estrogen-like effects, but their activity is only 10 times that of estradiol. -5 -10 -3 .

Embodiment 2

[0038] Molecular simulation of the interaction between pratensein and prunetin and estrogen receptor

[0039] Using computer-aided drug design method, using estrogen receptor (ER β, ER α) as the target model, the active conformation of pratensein and prunetin molecules was obtained by molecular mechanics optimization, and the molecular docking program was used to calculate the relationship between the receptor and the ligand. interaction.

[0040] The results showed that both pratensein and prunetin could enter the binding cavity of estrogen receptor, and the results also indicated that the binding force of both pratensein and prunetin was 7-10 times stronger than that of ER α. In addition, some positions on the molecule are substituted, which has a certain influence on its activity.

[0041] Due to the differences in tissue distribution of human ER β and ER α, ER β mainly exists in the brain, bone, bladder and vascular epithelial tissues, suggesting that pratensein and prune...

Embodiment 3

[0043] Effects of pratensein and prunetin on osteoblasts cultured in vitro

[0044] Separation of osteoblasts from newborn 1-3 day old SD rat skulls by enzymatic digestion, the third generation cells were observed by MTT method and methylthymol blue (MTB) colorimetric method to observe the effect of red cloverin and prunin on in vitro culture. Effects of osteoblast proliferation, cellular matrix calcium, and mineralized nodular calcium.

[0045] The results showed that: red cloverin and prunus at concentrations of 0.1-10umol / L can significantly promote the proliferation of osteoblasts, and can significantly increase the calcium in the cell matrix and calcium in mineralized nodules. The specific results are shown in the table below:

[0046]

[0047] *P△ P△△ P<0.01 compared with NaF

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PUM

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Abstract

The invention relates to a drug combination containing pratensein and / or prunetin, which has the effects of preventing and treating cardiovascular systems, osteoporosis and the like via the effects ofselective estrogen receptor modulators widely distributed in the bodies. The combination can be used for preparing the drugs for treating cancers and lead compounds. The combination can be orally taken by the patients or be applied to the patients who need the treatment by nasal inhalation or in an external rectal, parenteral or local manner. The daily dose of the combination is 1mg-4mg / kg and the combination can be applied once or more times. The combination can be prepared into solid preparations, liquid preparations, creams, ointments, patches, spraying agents, subcutaneous implants and the like, and can be especially prepared into sustained release tablets, coated tablets and the like having effects on intestinal canals.

Description

[0001] This application is a divisional application of the patent application titled "A Pharmaceutical Composition Containing Trifolium Trifolium and Piraxanthin and Its Application in Medicine", application number 200510031097.3, and application date of October 25, 2005 . technical field [0002] The invention relates to a pharmaceutical composition and its application, in particular to a pharmaceutical composition containing pratensein and prunetin and its application in medicine. Background technique [0003] Isoflavones are widely found in plants and have a variety of biological activities, such as anti-cancer, lowering blood lipids, phytoestrogens-like effects, and improving body immunity. The related research on flavonoids has always been valued by scholars at home and abroad And keep going deeper. [0004] Red clover (Trifolium pretense L.), also known as clover, red clover, etc., is mostly used as pasture. The whole grass contains a variety of flavonoids and isoflav...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P19/10A61P9/00A61P35/00A61P5/30
Inventor 华茉莉方建平
Owner SHANGHAI INST OF PHARMA IND
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