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A kind of sterol derivative and its preparation method and application

A technology of sterols and methanol, applied in the field of sterol derivatives and their preparation, can solve the problems of restricting the scientific use of red yeast rice and hindering the wide application of red yeast rice, and achieve the effects of inhibiting platelet aggregation and improving vascular endothelial function.

Active Publication Date: 2016-04-06
BEIJING WBL PEKING UNIV BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the many components in red yeast rice, people still know little about the effects of each component in red yeast rice, which limits the scientific use of red yeast rice to a certain extent and hinders the wide application of red yeast rice.

Method used

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  • A kind of sterol derivative and its preparation method and application
  • A kind of sterol derivative and its preparation method and application
  • A kind of sterol derivative and its preparation method and application

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preparation example Construction

[0037] In a typical embodiment of the present invention, the method for preparing the above compound includes the following steps: taking a red yeast rice preparation, adding a solvent, and performing ultrasonic extraction, and concentrating the extract under reduced pressure to obtain a refined extract. The refined extract was separated by silica gel column chromatography. In the process of column chromatography, petroleum ether and ethyl acetate were used for gradient elution of the refined extract. During the gradient elution, the volume ratio of petroleum ether and ethyl acetate was 75:25. 50:50-25:75, 0:100, and the eluent obtained when the volume ratio of petroleum ether and ethyl acetate is 50:50-25:75. Preferably, petroleum ether and ethyl acetate are used in the gradient elution process. The volume ratio of ester is 75:25, 50:50, 25:75, 0:100. Take the eluent obtained when the volume ratio of petroleum ether and ethyl acetate is 25:75, and the volume ratio is 1: The mi...

Embodiment 1

[0055] Raw material: 2kg of Xuezhikang capsule produced by Beijing Peking University Weixin Biotechnology Co., Ltd.

Embodiment 2

[0057] Raw material: 3kg of commercially available red yeast rice powder.

[0058] 1. The method for preparing the sterol compound with structural formula (II) using the raw materials in Examples 1 and 2:

[0059] 1) Take 2kg of the contents of Xuezhikang capsules or about 3kg of red yeast rice powder, and ultrasonically extract 3 times with 2-6 times the volume of n-hexane as a solvent, 20-40 minutes each time, combine the extracts and concentrate under reduced pressure to obtain n-hexane essence Extract 84g.

[0060] 2) Take 50 g of the n-hexane refined extract, apply silica gel column chromatography for separation, and perform gradient elution with petroleum ether and ethyl acetate. The volume ratio of petroleum ether to ethyl acetate is 75:25, 50:50, 25:75, 0:100.

[0061] 3) Take 3.0 g of the extract obtained by the elution of petroleum ether-ethyl acetate at 25:75, and rotary evaporate the oily substance concentrated under reduced pressure. After dissolving with a trace amount...

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Abstract

The invention discloses a sterol derivative, and a preparation method and an application thereof. The sterol derivative comprises sterol compounds having a structural formula (I), or pharmaceutically acceptable salts of the sterol compounds, or extract products including the sterol compounds, or compositions including the sterol compounds. In the structural formula (I), R1 is -OH, =O, H, or a C1-C3 alkyl group; R2 is -OH, H, or a C1-C3 alkyl group; R3 is -OH, =O, H, or a C1-C3 alkyl group; R4 is -OH, H, or a C1-C3 alkyl group; and at least one of R1, R2, R3 and R4 is -OH. The compounds having the structural formula (I) can be used for preparing medicines having an HMG-CoA reductase activity inhibition effect, and the prepared medicines can effectively inhibit the activities of an HMG-CoA reductase.

Description

Technical field [0001] The invention relates to the field of pharmacy, in particular to a sterol derivative with the structural formula (I) and a preparation method and application thereof. Background technique [0002] Red yeast rice (Monascus-fermented rice) is a kind of purplish red rice yeast made from rice as raw material and fermented by Monascus. Monascus is called Danqu in ancient times. It is made by inoculating the mother of monascus or distiller's yeast on rice and fermenting. Its color is red, so it is also called red yeast, red rice, red rice and red grains. Fujian and other places. So it is also known as Fuqu, Fumi and so on. [0003] Red yeast rice is a traditional Chinese medicine with both diet and therapy. As early as ancient times, it has been widely used in food coloring, wine making, fermentation, and traditional Chinese medicine. "Drinking Zheng Yao" has red yeast rice "sweet, peaceful, non-toxic", "invigorating the spleen, nourishing qi, and warming the mi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J71/00A61K31/58A61P3/06A61P7/02A61P9/10
Inventor 段震文郭树仁李雪梅
Owner BEIJING WBL PEKING UNIV BIOTECH
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