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An active ingredient isolated from Salvia miltiorrhiza and its application in the treatment of cerebrovascular diseases

An active ingredient, the technology from Salvia miltiorrhiza, applied in the field of active ingredients and its application in the treatment of cerebrovascular diseases, can solve problems such as elevation, and achieve obvious effects, protective effects, and simple separation and purification methods

Active Publication Date: 2019-11-01
YANGZHOU FIRST PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But even when niacin and statins are combined, they only raise HDL-C by about 30%

Method used

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  • An active ingredient isolated from Salvia miltiorrhiza and its application in the treatment of cerebrovascular diseases
  • An active ingredient isolated from Salvia miltiorrhiza and its application in the treatment of cerebrovascular diseases
  • An active ingredient isolated from Salvia miltiorrhiza and its application in the treatment of cerebrovascular diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] (1) Pulverization: get Salvia miltiorrhiza (1kg), pulverize to 20-100 mesh, get fine powder for subsequent use;

[0022] (2) Extraction: the fine powder obtained in step (1) is extracted by dichloromethane percolation to obtain a dichloromethane extract (0.96L), and the extract is concentrated to obtain a medicinal extract for subsequent use; wherein, the temperature of percolation extraction is At room temperature, the percolation extraction time is 8 hours, and the percolation rate is 2ml / min per kilogram of powder outflow rate;

[0023] (3) Purification: take the extract obtained in step (2), and first carry out normal phase silica gel column chromatography separation, stationary phase: 200-300 mesh silica gel, mobile phase is 30% ethyl acetate / petroleum ether mixed solvent, eluting 2 column volumes, the eluent is concentrated and separated by high performance liquid chromatography, stationary phase: semi-preparative C 18 Chromatographic column (Kromasil, 7 μm, 10 ×...

Embodiment 2

[0030] (1) Pulverization: get Salvia miltiorrhiza (1kg), pulverize to 20-100 mesh, get fine powder for subsequent use;

[0031] (2) Extraction: the fine powder obtained in step (1) is extracted by dichloromethane percolation to obtain dichloromethane extract (2.88L), and the extract is concentrated to obtain medicinal extract for subsequent use; wherein, the temperature of percolation extraction is At room temperature, the percolation extraction time is 16 hours, and the percolation rate is 3ml / min per kilogram of powder outflow rate;

[0032] (3) Purification: take the extract obtained in step (2), and first carry out normal phase silica gel column chromatography separation, stationary phase: 200-300 mesh silica gel, mobile phase is 40% ethyl acetate / petroleum ether mixed solvent, eluting 3 column volumes, the eluent is concentrated and separated by high performance liquid chromatography, stationary phase: semi-preparative C 18 Chromatographic column (Kromasil, 7 μ m, 10 × 2...

Embodiment 3

[0034] (1) Test the inhibitory activity of the active ingredient of Salvia miltiorrhiza with the structure of formula I of the present invention on CETP, and test the IC of the active ingredient of Salvia miltiorrhiza with the structure of formula I on CETP according to the method recorded in Chinese Patent Application No. 201610102917.1 50 , the results show that the IC of the active ingredient of Salvia miltiorrhiza with structure I of the present invention to CETP 50 The IC of positive control MK-0859 on CETP is 0.125μM 50 is 25nM. The above results show that the active ingredient of Salvia miltiorrhiza with the structure of formula I of the present invention has a strong inhibitory effect on CETP, and can be used to prevent and / or treat related diseases such as atherosclerosis.

[0035] (2) According to the method recorded in Chinese Patent Application No. 201710371901.5, the effect of the active ingredients of Salvia Miltiorrhiza with the structure of Formula I on the pl...

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Abstract

The invention relates to an active ingredient separated from salvia miltiorrhiza and application of the active ingredient in treatment of cerebrovascular diseases, in particular to application of a salvia miltiorrhiza active ingredient of a structure shown in a formula I, a stereoisomer, a tautomer or pharmaceutically acceptable salt thereof in preparation of a medicine used for preventing and / ortreating cerebrovascular diseases, wherein the structure shown in the formula I is described in the specification.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to an active ingredient isolated from Danshen and its application in treating cerebrovascular diseases. Background technique [0002] Salvia miltiorrhiza is the dry root and rhizome of Salvia miltiorrhiza Bge., a plant of the Labiatae family. It has the effects of promoting blood circulation and removing blood stasis, promoting menstrual flow and relieving pain, clearing the heart and eliminating troubles, cooling blood and eliminating carbuncles. [0003] Cerebrovascular disease is characterized by the "four highs" of high morbidity, high disability, high mortality and high recurrence rate, and has become the first major disease that seriously endangers human health. Among them, cerebral atherosclerosis and thrombosis are important causes of cerebrovascular diseases. Studies have shown that increasing high-density lipoprotein cholesterol (high-density lipoprotein cholesterol, H...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/06A61K31/4745A61P9/00A61P9/10
Inventor 唐铁钰张新江王英歌段作伟张海峰刘一辉
Owner YANGZHOU FIRST PEOPLES HOSPITAL
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