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A kind of sterol derivative and its preparation method and application

A technology of sterols and derivatization reactions, applied in the field of sterol derivatives and their preparation, can solve problems such as hindering the wide application of red yeast rice and restricting the scientific use of red yeast rice, and achieve the goal of improving vascular endothelial function, inhibiting effect, and inhibiting proliferation Effect

Active Publication Date: 2017-02-15
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

Examples

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preparation example Construction

[0052] In a typical embodiment of the present invention, the preparation method of the above-mentioned compound comprises the following steps: taking a preparation of red yeast rice, adding a solvent, performing ultrasonic extraction, and concentrating the extract under reduced pressure to obtain a fine extract. The fine extract is separated by silica gel column chromatography, and petroleum ether and ethyl acetate are used to carry out gradient elution to the fine extract during the column chromatography separation process. During the gradient elution, the volume ratio of petroleum ether and ethyl acetate is successively 75:25, 50:50~25:75, 0:100, take the eluent obtained when the volume ratio of petroleum ether and ethyl acetate is 50:50~25:75, preferably, petroleum ether and ethyl acetate in the gradient elution process The volume ratio of esters is 75:25, 50:50, 25:75, and 0:100 in turn, and the eluent obtained when the volume ratio of petroleum ether and ethyl acetate is 2...

Embodiment 1

[0082] Raw materials: Xuezhikang capsules produced by Beijing Beida Weixin Biotechnology Co., Ltd. content 2kg.

Embodiment 2

[0084] Raw materials: commercially available red yeast rice powder 3kg.

[0085] The method for preparing the sterol compounds with structural formula (II) using the raw materials in Examples 1 and 2 respectively:

[0086]1) Take 2kg of Xuezhikang capsule content or about 3kg of red yeast rice powder, and use 2-6 times the volume of n-hexane as a solvent to ultrasonically extract 3 times, each time for 20-40 minutes, combine the extracts, concentrate under reduced pressure to obtain n-hexane essence Extract 84g.

[0087] 2) Take 50 g of n-hexane fine extract, and separate it by silica gel column chromatography, and carry out gradient elution with petroleum ether and ethyl acetate. The volume ratio of petroleum ether-ethyl acetate is 75:25, 50:50, 25:75, 0:100 in sequence.

[0088] 3) Take 3.0 g of the extract obtained by eluting with petroleum ether-ethyl acetate at a ratio of 25:75, and rotatively evaporate the oily substance concentrated under reduced pressure. After diss...

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Abstract

The invention discloses a sterol derivative, a preparation method and application thereof. The sterol derivatives include sterol compounds with structural formula (I) or pharmaceutically acceptable salts thereof, or extracts containing them, or compositions containing them. In structural formula (I), wherein, R1 is -OH, =O, H, or C1-C3 alkyl; R2 is -OH, H, or C1-C3 alkyl; R3 is -OH, =O, H, or C1-C3 alkyl; R4 is -OH, H, or C1-C3 alkyl, and at least one of R1, R2, R3, R4 is -OH. The compound with the structural formula (I) can be used to prepare a drug with HMG-CoA reductase activity inhibitory effect, and the prepared drug can effectively inhibit HMG-CoA reductase activity or be used to prepare a drug with anticancer effect.

Description

technical field [0001] The present invention relates to the field of pharmacy, in particular to a sterol derivative with structural formula (I) and its preparation method and application. Background technique [0002] Monascus-fermented rice is a purple-red rice koji made from rice as raw material and fermented by Monascus. Red koji was called Danqu in ancient times, and it was fermented by inoculating koji or distiller's yeast based on Monascus on rice. Its color is red, so it is also called red koji, red rice, red rice, and red rice. Fujian and other places. Therefore, it is also known as Fuqu, Fumi, etc. [0003] Red yeast rice is a traditional Chinese medicine that combines both diet and therapy. As early as in 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, flat, non-toxic", "invigorating the spleen, replenishing qi, and warming the middle"; Evil blo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J71/00C07J75/00A61K31/58A61K35/00A61P3/06A61P9/10A61P7/02
CPCA61K31/58A61K36/064A61K36/88A61K36/899A61K2236/00A61P3/06A61P7/02A61P9/10A61P35/00C07J71/0005A61K31/357
Inventor 段震文郭树仁李雪梅
Owner BEIJING WBL PEKING UNIV BIOTECH
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