Compound grandifoliol, its preparation method and its application

A kind of technology of rattanol and compound, which is applied in the field of medicine and can solve problems such as liver and kidney function damage

Inactive Publication Date: 2012-10-17
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Currently used lipid-lowering drugs and anti-platelet drugs mainly have two problems: first, they block the functions of materials required for normal physiological operations, such as the important physiological functions of HMG-CoA reductase in the human body, while HMG The use of -CoA reductase inhibitors will inhibit the normal physiological functions of this enzyme in the human body; second, this type of drug will cause huge damage to the liver and kidney functions, and long-term use will inevitably cause liver and kidney damage. disease

Method used

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  • Compound grandifoliol, its preparation method and its application
  • Compound grandifoliol, its preparation method and its application
  • Compound grandifoliol, its preparation method and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1 extracts and isolates the method for the separation compound grandifoliol (grandifoliol) from Salvia grandiflorum:

[0044] 5 kg of Sage herb medicinal material was extracted three times with 95% ethanol to obtain 386 g of extract, which was quickly eluted by silica gel column chromatography, and the eluent was sequentially selected from petroleum ether, chloroform, ethyl acetate, and methanol, and roughly divided into four parts . Chloroform part 21.8g, separated by silica gel column chromatography for many times, sherwood oil-ethyl acetate and sherwood oil-acetone gradient elution, every 250ml is a distillate, obtains grandifoliol (grandifoliol) crude product in the 63rd part, Purified by preparative HPLC (80% methanol-water, flow rate 6ml / min, 254nm wavelength detection), 500 μL sample was taken, and 35 mg of the compound grandifoliol was obtained at tR=69.6min, which was light yellow powder.

[0045] The physical and chemical properties and spectral d...

Embodiment 2

[0052] Example 2 Inhibitory effect of the compound grandifoliol on the proliferation of vascular smooth muscle cells induced by serum

[0053] The proliferation and phenotypic changes of vascular smooth muscle cells (VSMC) are the main pathological basis of atherosclerosis. In this experiment, a serum (FBS)-induced VSMC cell proliferation model was established, and the inhibitory activity of the compound of the present invention on FBS-induced VSMC proliferation was further observed. The primary cultured vascular smooth muscle cells were digested with 0.125% trypsin, seeded in 96-well plates, and cultured for 24 hours until subconfluent state. Change to serum-free culture for 24h to make the cells tend to rest (G 0 period), after the sample was treated for 4 hours, 10% FBS was added and cultured for 48 hours. Use the MTT method to detect the proliferation of the cells, and calculate the inhibition rate of the sample to FBS-induced VSMC cell proliferation. When the inhibition...

Embodiment 3

[0058] Example 3 The protective effect experiment of compound grandifoliol (grandifoliol) on hydrogen peroxide injury of human umbilical vein endothelial cells

[0059] with H 2 o 2 The vascular endothelial cells were damaged, and the mitochondrial activity of the cells was measured by MTT method. According to the change of optical density value, observe the sample pair H 2 o 2 Protective effect on vascular endothelial cell injury. CRL-1730 human umbilical vein endothelial cells were counted and cultured in 96-well flat-bottom culture plates. After 24 hours, the cells were first treated with the compound of the present invention for 4h, and then treated with H 2 o 2 Treated for 20 hours to create a model of cell oxidative damage, and use the MTT method to measure the mitochondrial activity of vascular endothelial cells to observe the effect of the sample on H 2 o 2 For the protective effect of oxidative damage on vascular endothelial cells, re-screening (5, 0.5, 0.05, ...

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Abstract

The invention relates to a novel compound grandifoliol extracted by salvia miltiorrhizae plant Salvia grandifolia, its preparation method, a pharmaceutical composition containing the compound and an application of the pharmaceutical composition containing the compound in prevention and / or treatment of cardiovascular and cerebrovascular diseases like Atherosclerosis.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a new compound grandifoliol extracted from Salvia genus Salvia grandifoliol, a preparation method thereof, a pharmaceutical composition containing the compound and its Application in prevention and / or treatment of cardiovascular and cerebrovascular diseases such as atherosclerosis. Background technique [0002] Sage is a plant of the genus Salvia in the Labiatae family, and its roots are used as medicine for salvia. Salvia can dilate coronary arteries, increase coronary flow, improve microcirculation, and protect the heart. It can inhibit and relieve platelet aggregation, improve the body's ability to withstand hypoxia, and has anti-hepatitis, anti-parasite, anti-tumor, and anti-virus activities. [0003] Atherosclerosis (AS) is a systemic disease related to lipid metabolism disorder and characterized by lipid deposition in the intima of large and medium arteries, atheroscler...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C49/737C07C45/79A61K31/122A61P9/10A61P9/08A61P9/12
Inventor 陈若芸方莲花肖磊郭晶王洪庆杜冠华刘超李保明
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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