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Application of cyclo-icaritin aglycone in preparation of anti-inflammatory and antimicrobial medicaments

A technology of cyclic icariin and aglycone, which is applied in the field of natural medicine extraction, can solve problems such as unreported biological activity research, and achieve the effects of simple and feasible operation, high purity, and improvement of estrogen levels.

Inactive Publication Date: 2015-03-25
ANKANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The research on the medicinal components of Epimedium is currently mainly focused on the total glycosides of Epimedium and icariin, and there is no report on the derivatives and biological activities of the main components in Epimedium

Method used

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  • Application of cyclo-icaritin aglycone in preparation of anti-inflammatory and antimicrobial medicaments
  • Application of cyclo-icaritin aglycone in preparation of anti-inflammatory and antimicrobial medicaments
  • Application of cyclo-icaritin aglycone in preparation of anti-inflammatory and antimicrobial medicaments

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0046] 3.3.1 Preparation of inflammatory model: inflammatory substance: pure egg white; positive control substance: indomethacin. Subcutaneously inject 0.1mL of pure egg white into the toes of rats, and the paws of the rats will appear red, hot, swollen, and painful within 0.5 hours, and the experimental observation will start after 0.5 hours.

[0047] 3.3.2 Effect of cyclic icariin aglycon on toe swelling of rats induced by pure egg white: 20 rats weighing 200g-220g were randomly divided into 4 groups, 5 rats in each group. They were high-dose cycloicariin aglycone group (0.448 mg / 100g), low-dose group (0.224 mg / 100g), distilled water control group, and indomethacin control group (1 mg / 100g). The first two groups of cycloicariin aglycone were injected with high-dose and low-dose cycloicariin aglycon suspension 1.0mL / 100g respectively through the tail vein each time, and the latter two groups were injected with the same volume of normal saline and indole respectively through t...

Embodiment 1

[0059] Crush or cut 100g of dried Epimedium, heat and extract twice with water as solvent, add 8 times the amount of water for the first time, heat and extract for 2 hours, add 6 times the amount of water for the second time, heat and extract for 1 hour, filter the extract, and concentrate , purified by chromatography on LSA-20 resin (provided by Xi’an Lanxiao Resin Co., Ltd.), put it on the column and let it stand for 2-3h. After the resin is fully absorbed, wash it with water until the eluent is colorless, discard it, and use Elute with 30% ethanol, collect the eluate, recover ethanol, and dry. Add 500mL of methanolic hydrochloric acid solution (485mL of methanol solution, 15mL of 38% hydrochloric acid) to the dry matter, and reflux in the water bath for 5h. Methanol was recovered under reduced pressure, the concentrated solution was extracted with ethyl acetate, and the solvent was evaporated to obtain the crude cycloicariin aglycone. Add appropriate amount of ethanol to t...

Embodiment 2

[0061] Grind or cut 100g of dried Epimedium, heat and extract twice with water as solvent, add 10 times the amount of water for the first time, heat and extract for 2 hours, add 8 times the amount of water for the second time, heat and extract for 1 hour, filter the extract, and concentrate , purified by chromatography on D101 resin (provided by Xi’an Lanxiao Resin Co., Ltd.), put it on the column and let it stand for 2-3h. Eluted with ethanol, collected eluate, recovered ethanol, and dried. Add 500mL of methanolic sulfuric acid (475mL of methanol solution, 25mL of 38% hydrochloric acid) to the dry matter, and reflux in the water bath for 6h. Methanol was recovered under reduced pressure, the concentrated solution was extracted with chloroform, and the solvent was evaporated to obtain the crude cycloicariin aglycon. Add appropriate amount of ethyl acetate to the obtained cycloicariin aglycone crude product, heat to dissolve, place and crystallize to obtain 1.28 g of high-puri...

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Abstract

The invention discloses cyclo-icaritin aglycone with a structural formula shown as follows. A preparation method of the cyclo-icaritin aglycone comprises the following steps of: (1) crushing and cutting dried epimedium herbs into sections, adding water, heating for extraction, and filtering an extract to obtain a concentrated solution; (2) performing chromatographic purification on the concentrated solution on macroporous resin, eluting with water until the eluant is colorless after sufficient adsorption of the resin, discarding the resin, eluting with 20 to 50 percent methanol or ethanol, collecting the eluant, recovering the methanol or ethanol, and drying; and (3) adding the dried object obtained in the step (2) into a strong acid methanol or ethanol solution in a volume ratio of (2-6):100, fully stirring, then refluxing by heating, reducing the pressure to recover the methanol or ethanol, extracting the concentrated solution by using ethyl acetate, and steaming out a solvent to obtain a crude product of the cyclo-icaritin aglycone. The prepared cyclo-icaritin aglycone can be used for preparing anti-inflammatory and antimicrobial medicaments.

Description

technical field [0001] The invention relates to cycloicariin aglycone, a preparation method thereof and an application in the preparation of medicines and health care products, and belongs to the technical field of natural medicine extraction. Background technique [0002] Epimedium has a long history of medicinal use. There are five kinds of Epimedium currently used in Chinese Pharmacopoeia: Epimedium, Epimedium Cardiac, Epimedium Sagittarius, Epimedium Korean and Epimedium Wushan. [0003] The research on the medicinal components of Epimedium is currently mainly focused on the total glycosides of Epimedium and icariin, and there is no report on the derivatives of the main components in Epimedium and their biological activities. Contents of the invention [0004] The object of the present invention is to provide a kind of cyclic icariin aglycon isolated and extracted from Epimedium. [0005] Another object of the present invention is to provide a preparation method of th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/353A61P29/00A61P31/00A61P31/04A61P39/06A61P9/00A61P19/10A61P37/04A61P5/30A23L1/30C07D493/04
Inventor 谢娟平向纪明王浩东
Owner ANKANG UNIV
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