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Methoxy-7-luteolin and preparation method and application thereof

A technology of luteolin and methoxy, which is applied in the direction of medical formulas, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problem that the medicinal value of Motherwort has not been fully developed, and achieve the synthesis rate of estradiol inhibitory effect

Inactive Publication Date: 2018-08-10
YUNNAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, some medicinal value of motherwort has not been fully developed at present.

Method used

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  • Methoxy-7-luteolin and preparation method and application thereof
  • Methoxy-7-luteolin and preparation method and application thereof
  • Methoxy-7-luteolin and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] 1. Preparation of Methoxy-7-Luteolin (I)

[0036] Extraction and separation of methoxy-7-luteolin:

[0037] Collect the whole motherwort, dry it in the shade at room temperature, pulverize, take 15.0kg of dry powder, extract 3 times with 95% ethanol at reflux, 2-3 hours each time, combine the ethanol extracts, filter, and concentrate under reduced pressure until there is no alcohol smell; The solution was suspended in an aqueous solution and extracted with petroleum ether, ethyl acetate and n-butanol in sequence. The ethyl acetate extracted part was dissolved and adsorbed on silica gel with chloroform-methanol, placed at room temperature to evaporate the solvent, pulverized, and subjected to silica gel column chromatography. 1:0→0:1 chloroform / methanol eluted to obtain 6 parts; of which, the second part was chromatographed on a reverse C-18 silica gel column with a 9:1→0:10 water / methanol gradient to obtain The compound methoxy-7-luteolin (I, 3.1 g). The structure of the c...

Embodiment 2

[0063] According to the method of Example 1, methoxy-7-luteolin was first prepared, and after dissolving in a small amount of DMSO, water for injection was added as usual, followed by precision filtration, potting and sterilization to prepare an injection solution.

Embodiment 3

[0065] Firstly, methoxy-7-luteolin was prepared according to the method of Example 1. After dissolving with a small amount of DMSO, dissolving it in sterile water for injection, stirring to dissolve, and filtering with a sterile suction filter funnel. The bacteria essence is filtered, divided into ampoules, freeze-dried at low temperature and then aseptically melt-sealed to obtain a powder injection.

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Abstract

The invention belongs to the technical field of medicines and particularly relates to methoxy-7-luteolin and preparation method and application thereof. The preparation method of the methoxy-7-luteolin includes: adopting 95% ethyl alcohol for reflux extraction from herba leonuri, sequentially subjecting concentrated extract liquid to extraction with petroleum ether, ethyl acetate and normal butanol, and eluting to obtain a compound namely the methoxy-7-luteolin. A pharmaceutical composition containing methoxy-7-luteolin is used for ovulation failure caused by breast cancers, hyperplasia of mammary glands and polycystic ovarian syndromes. According to researches, methoxy-7-luteolin has an evident inhibition effect on in-vitro estradiol synthesis ratio, is free of evident cytotoxicity and has a curative effect on ovulation failure caused by breast cancers, hyperplasia of mammary glands and polycystic ovarian syndromes.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to methoxy-7-luteolin and its preparation method and application. Background technique [0002] Malignant tumors have a major impact on social development, national economy, and people’s health. The prevention and control of tumors has become the focus of global health strategies. According to statistics from the World Health Organization (WHO), there were more than 14 million new tumor cases worldwide in 2012 alone, among which breast cancer is the most common malignant tumor with the highest incidence among women. There are more than 1.67 million new cases of breast cancer in women worldwide, accounting for the first place in the incidence of all malignant tumors in women. Almost 1 in 4 cases of female malignant tumors is breast cancer. Because the formation, growth and proliferation of breast tumors require estrogen stimulation, more than 60% of breast cancer patients are...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/30C07D311/40A61K31/352A61P35/00A61P15/08A61P15/14
CPCA61P15/08A61P15/14A61P35/00C07D311/30C07D311/40
Inventor 肖伟烈王飞张兴杰杜宝文张芮菡
Owner YUNNAN UNIV
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