CN111729038A - Application of dendrobium extract in preparation of cholesterol-lowering medicine - Google Patents
Application of dendrobium extract in preparation of cholesterol-lowering medicine Download PDFInfo
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- CN111729038A CN111729038A CN202010793414.XA CN202010793414A CN111729038A CN 111729038 A CN111729038 A CN 111729038A CN 202010793414 A CN202010793414 A CN 202010793414A CN 111729038 A CN111729038 A CN 111729038A
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Abstract
The invention discloses an application of a dendrobium huoshanense extract in preparing a cholesterol-reducing medicine, wherein the dendrobium huoshanense extract comprises a dendrobium huoshanense aqueous extract, a dendrobium huoshanense aqueous extract and a dendrobium huoshanense alcohol extract, the dendrobium huoshanense extract realizes the effect of reducing cholesterol level by inhibiting the activity of beta-hydroxy-beta-methylglutaryl coenzyme A reductase, a key regulating factor for regulating the expression of the beta-hydroxy-beta-methylglutaryl coenzyme A reductase is sterol regulatory element binding protein, the sterol regulatory element binding protein is specifically bound with a sterol regulatory element, and the sterol regulatory element is an enhancer of genes such as a low-density lipoprotein receptor and the beta-hydroxy-beta-methylglutaryl coenzyme A reductase. The dendrobium huoshanense extract disclosed by the invention has an inhibiting effect on the synthesis of cholesterol and a promoting effect on the metabolic degradation of the cholesterol, so that the effect of treating the cholesterol is good, and the drug toxicity caused by long-term use of western medicines can be avoided.
Description
Technical Field
The invention relates to the field of pharmacy, in particular to application of a dendrobium extract in preparing a cholesterol-lowering medicine.
Background
Cholesterol is a steroid compound, is indispensable to the metabolism of the body, and plays an important role in the composition of cell membranes and the synthesis of hormones, in particular. Cholesterol is mainly derived from the body's own synthesis, partly from food. The human body can synthesize cholesterol in the liver, and also can ingest exogenous cholesterol through diet. In coronary heart disease and atherosclerosis, atheromatous plaques are formed by the deposition of lipids such as cholesterol. In the body, cholesterol is bound to proteins, mainly in the form of lipoproteins, and is transported in the body mainly in the form of high-density lipoprotein cholesterol (HDL) and low-density lipoprotein cholesterol (LDL-C), wherein HDL-C is called good cholesterol because studies show that an increase in serum HDL-C level has the effect of cleaning atherosclerosis and has a protective effect on cardiovascular vessels.
Dendrobium huoshanense, commonly known as dendrobium huoshanense, is a herbaceous plant of dendrobium of orchidaceae, is a special Chinese first-level protective plant. [1] Stem is upright, fleshy, not branched, with 3-7 nodes, yellowish green, sometimes with purplish red spots, and dry, yellowish. 2-3 leaves of the leaf leathers alternate on the upper part of the stem, are inclined out and are in a tongue-shaped long circle. 1-3 total inflorescences with 1-2 flowers are formed and come out from the upper part of the old stem with fallen leaves; the flower is light yellow and green, and the development is carried out; the petal is oval, the tip is blunt, 5 pulses are provided; the labial lobe is nearly rhomboid, and the length and the width are approximately equal. The flowering period is 5 months.
China national geographic marking products. The mountain trees mainly produced in Huoshan counties of Anhui province in Dabie mountain areas mostly grow between cliff stones in cloud and fog-filled cliff and on ancient trees in the mountain forests and on valley rocks. The dendrobium huoshanense can greatly improve the SOD (main substance for delaying senility) level in a human body, and is very suitable for people who often stay up all night, use brain, smoke and wine excessively, and have weak and hypodynamia. The dendrobium huoshanense has the effects of improving eyesight, regulating yin and yang, tonifying yang and kidney, and maintaining beauty and keeping young, so that the effects of health care and prolonging life are achieved.
Disclosure of Invention
The invention aims to solve the defects in the prior art, and provides application of a dendrobium extract in preparing a cholesterol-lowering medicine.
In order to achieve the purpose, the invention adopts the following technical scheme:
the application of the dendrobium huoshanense extract in preparing the cholesterol-lowering medicine comprises a dendrobium huoshanense aqueous extract, a dendrobium huoshanense aqueous extract and a dendrobium huoshanense alcohol extract.
Preferably, the dendrobium huoshanense extract achieves the effect of reducing cholesterol levels by inhibiting the activity of beta-hydroxy-beta-methylglutaryl coenzyme A reductase.
Preferably, the key regulator for regulating the expression of the beta-hydroxy-beta-methylglutaryl coenzyme A reductase is sterol regulatory element binding protein, the sterol regulatory element binding protein is specifically bound with a sterol regulatory element, the sterol regulatory element is an enhancer of genes such as low density lipoprotein receptor and beta-hydroxy-beta-methylglutaryl coenzyme A reductase, the sterol regulatory element binding protein stimulates the expression enhancement of the gene containing the sterol regulatory element, activates the expression of the beta-hydroxy-beta-methylglutaryl coenzyme A reductase gene and reduces the cholesterol level.
Preferably, the dendrobium huoshanense extract increases the expression of scavenger receptor type B I, the scavenger receptor type B I prevents excessive accumulation of free cholesterol to cause atherosclerosis, and the SR-BI binds to high density lipoprotein to return excess cholesterol to the liver for further metabolism and promote cholesterol degradation.
Preferably, the dendrobium huoshanense extract is used for treating patients with insufficient low-density lipoprotein cholesterol reduction, so that a low-density lipoprotein receptor is degraded, the plasma low-density lipoprotein cholesterol level is increased, and the cholesterol level is reduced.
Preferably, the dendrobium huoshanense extract increases the expression of low density lipoprotein, wherein the low density lipoprotein is acted by lysosomal enzyme, and cholesterol ester in the low density lipoprotein is hydrolyzed into free cholesterol and fatty acid.
Preferably, the dendrobium huoshanense extract increases the expression of high-density lipoprotein and has the effect of reversing cholesterol to be transported back to the liver.
The invention has the beneficial effects that: the dendrobium huoshanense aqueous extract, the dendrobium huoshanense aqueous extract and the dendrobium huoshanense alcohol extract not only have an inhibiting effect on the synthesis of cholesterol, but also have a promoting effect on the metabolic degradation of the cholesterol, and are applied to medicines, so that the effect of treating the cholesterol is good, and the drug toxicity caused by long-term use of western medicines can be avoided.
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FIG. 1 shows the mRNA expression levels of the dendrobium huoshanense extract on beta-hydroxy-beta-methylglutaryl coenzyme A reductase (HMGCR), sterol regulatory element binding protein (SCAP), cholesterol Sensor (SCAP) and INSIG2 genes.
FIG. 2 shows the mRNA expression levels of the extract of Dendrobii caulis of the present invention on Lecithin Cholesterol Acyltransferase (LCAT), Low Density Lipoprotein Receptor (LDLR), proprotein convertase subtilisin/kexin 9 type (PCSK 9), scavenger receptor type B I (SRB 1).
FIG. 3 shows a positive control group according to the present invention.
FIG. 4 is an irrelevant control group of the present invention.
Detailed Description
The technical solutions in the embodiments of the present invention will be clearly and completely described below with reference to the drawings in the embodiments of the present invention, and it is obvious that the described embodiments are only a part of the embodiments of the present invention, and not all of the embodiments.
Referring to fig. 1 to 4, the application of the dendrobium huoshanense extract in preparing the cholesterol-lowering drug includes dendrobium huoshanense aqueous extract, dendrobium huoshanense aqueous extract and dendrobium huoshanense alcoholic extract, the dendrobium huoshanense extract achieves the effect of lowering cholesterol level by inhibiting the activity of beta-hydroxy-beta-methylglutaryl coenzyme a reductase (HMG-CoA reductase), a key regulatory factor for regulating the expression of beta-hydroxy-beta-methylglutaryl coenzyme a reductase is sterol regulatory element binding protein, the sterol regulatory element binding protein is specifically bound with a sterol regulatory element (SRE-1), the sterol regulatory element (SRE-1) is an enhancer of genes of Low Density Lipoprotein Receptor (LDLR) and beta-hydroxy-beta-methylglutaryl coenzyme a reductase, the combination protein of the sterol regulatory element stimulates the gene expression enhancement containing the sterol regulatory element (SRE-1), activates the gene expression of beta-hydroxy-beta-methylglutaryl coenzyme A reductase (HMGCR), reduces the cholesterol level, the dendrobium huoshanense extract increases the expression of scavenger receptor B type I (SRB 1), the scavenger receptor B type I (SRB 1) prevents the excessive accumulation of free cholesterol to cause atherosclerosis, the scavenger receptor B type I (SRB 1) is combined with High Density Lipoprotein (HDL), the surplus cholesterol is returned to the liver for further metabolism, the cholesterol degradation is promoted, the dendrobium huoshanense extract treats the patients with insufficient low density lipoprotein cholesterol (LDL-C) reduction, the low density lipoprotein receptor (LDL-R) is degraded, the level of plasma low density lipoprotein cholesterol (LDL-C) is increased, the dendrobium huoshanense extract for reducing cholesterol level increases the expression of low-density lipoprotein (LDL), the low-density lipoprotein (LDL) is acted by lysosomal enzyme, cholesterol ester in the low-density lipoprotein (LDL) is hydrolyzed into free cholesterol, the dendrobium huoshanense extract for increasing the expression of high-density lipoprotein (HDL) is used for reversing the cholesterol and transporting the cholesterol back to the liver.
Example 1:
application of dendrobium huoshanense extract in preparation of cholesterol-lowering drugs, and influence of dendrobium huoshanense extract on HUH7cells cholesterol synthesis
After HUH7cells were recovered, they were transferred to a culture dish in DMEM (high-sugar) medium containing 10% FBS, cultured at 37 ℃ under 5% CO2 for 6-12h with cell synchronization, and randomly divided into 6 groups: a blank control group; ② irrelevant control group: ethanol; positive control group: simvastatin; fourthly, the dry dendrobium huoshanense aqueous extract group; fifthly, preparing a dendrobium huoshanense aqueous extract group; sixthly, the dendrobium huoshanense alcohol extract group. Administration: after serum-free culture synchronization is carried out for 12 hours, pre-dosing is carried out for 12 hours respectively for dosing groups, then cholesterol is added or not added to a blank control group, an irrelevant control group, a positive control group, a dendrobium huoshanense aqueous extract group, a fresh dendrobium huoshanense aqueous extract group and a dendrobium huoshanense alcoholic extract group, after 24 hours of action, a culture medium is sucked, stimulation is stopped, and relevant detection is carried out. The measured correlation index: beta-hydroxy-beta-methylglutaryl coenzyme A reductase (HMGCR), sterol regulatory element binding protein (SCAP), cholesterol Sensor (SCAP), mRNA expression of INSIG 2. And (3) experimental data statistics: the water extract of the dendrobium stem has obvious inhibition effect on the mRNA expression level of beta-hydroxy-beta-methylglutaryl coenzyme A reductase (HMGCR) gene and shows concentration-dependent tolerance. The dendrobium huoshanense aqueous extract has obvious inhibition effect on the mRNA expression level of beta-hydroxy-beta-methylglutaryl coenzyme A reductase (HMGCR) and cholesterol Sensor (SCAP) genes, and the concentration depends on tolerance. The dendrobium huoshanense alcohol extract has obvious inhibition effect on the mRNA expression level of INSIG2 gene and can inhibit the synthesis of cholesterol.
The experimental results show that a bar chart 1 of the influence of the dry dendrobium water extract on the cholesterol metabolism related genes of HUH7cells, the influence of the fresh dendrobium water extract on the cholesterol metabolism related genes of HUH7cells and the influence of the dendrobium huoshanense alcohol extract on the cholesterol metabolism related genes of HUH7cells is obtained, and the dendrobium huoshanense extract has an inhibiting effect on cholesterol synthesis in HUH7cells induced by cholesterol.
Example 2
Application of dendrobium huoshanense extract in preparation of cholesterol-lowering drugs, and influence of dendrobium huoshanense extract on HUH7cells cholesterol metabolism
After HUH7cells were recovered, they were transferred to a culture dish in DMEM (high-sugar) medium containing 10% FBS, cultured at 37 ℃ under 5% CO2 for 6-12h with cell synchronization, and randomly divided into 6 groups: a blank control group; ② irrelevant control group: ethanol; positive control group: simvastatin; fourthly, the dry dendrobium huoshanense aqueous extract group; fifthly, preparing a dendrobium huoshanense aqueous extract group; sixthly, the dendrobium huoshanense alcohol extract group. Administration: after serum-free culture synchronization is carried out for 12 hours, pre-dosing is carried out for 12 hours respectively for dosing groups, then cholesterol is added or not added to a blank control group, an irrelevant control group, a positive control group, a dendrobium huoshanense aqueous extract group, a fresh dendrobium huoshanense aqueous extract group and a dendrobium huoshanense alcoholic extract group, after 24 hours of action, a culture medium is sucked, stimulation is stopped, and relevant detection is carried out. The measured related indices Lecithin Cholesterol Acyltransferase (LCAT), Low Density Lipoprotein Receptor (LDLR), proprotein convertase subtilisin/kexin 9 type (PCSK 9), scavenger receptor class B type I (SRB 1) mRNA expression. And (3) experimental data statistics: the aqueous extract of the dendrobium stem has obvious effect of enhancing the mRNA expression level of a low-density lipoprotein receptor (LDLR) gene and shows concentration dependence. The dendrobium huoshanense aqueous extract has obvious inhibition effect on the mRNA expression level of a low-density lipoprotein receptor (LDLR) gene and concentration dependence. The dendrobium huoshanense alcohol extract has obvious effect of enhancing the mRNA expression level of Lecithin Cholesterol Acyltransferase (LCAT), Low Density Lipoprotein Receptor (LDLR) and scavenger receptor B type I (SRB 1) genes, and can promote the metabolic degradation of cholesterol.
And a bar chart 2 of the influence of the dry dendrobium water extract on the HUH7cell cholesterol metabolism related gene, the influence of the fresh dendrobium water extract on the HUH7cell cholesterol metabolism related gene and the influence of the dendrobium huoshanense alcohol extract on the HUH7cell cholesterol metabolism related gene is obtained after experimental results, and the dendrobium huoshanense extract has an enhancement effect on cholesterol metabolism degradation in HUH7cells induced by cholesterol.
Comparing the positive control in fig. 3 with the irrelevant control in fig. 4, the present invention compares: beta-hydroxy-beta-methylglutaryl coenzyme A reductase (HMGCR), sterol regulatory element binding protein, cholesterol Sensor (SCAP), and inhibition of mRNA expression level of INSIG2 gene are obvious, and enhancement of mRNA expression level of Lecithin Cholesterol Acyltransferase (LCAT), Low Density Lipoprotein Receptor (LDLR), proprotein convertase subtilisin/kexin 9 type (PCSK 9), scavenger receptor type B I (SRB 1) is obvious.
The invention has the beneficial effects that: the extract of Dendrobium huoshanense can inhibit the synthesis of cholesterol, and promote the metabolic degradation of cholesterol.
The above description is only for the preferred embodiment of the present invention, but the scope of the present invention is not limited thereto, and any person skilled in the art should be considered to be within the technical scope of the present invention, and the technical solutions and the inventive concepts thereof according to the present invention should be equivalent or changed within the scope of the present invention.
Claims (7)
1. The application of the dendrobium huoshanense extract in preparing the cholesterol-lowering medicine is characterized in that the dendrobium huoshanense extract comprises a dendrobium huoshanense aqueous extract, a dendrobium huoshanense aqueous extract and a dendrobium huoshanense alcohol extract.
2. The use of the dendrobium extract as claimed in claim 1, in the preparation of a cholesterol lowering medicament, wherein the dendrobium huoshanense extract achieves the effect of lowering cholesterol levels by inhibiting the activity of beta-hydroxy-beta-methylglutaryl coenzyme A reductase.
3. The use of the dendrobe extract in the preparation of a cholesterol lowering medicament according to claim 2, wherein the key regulator for regulating the expression of β -hydroxy- β -methylglutaryl coenzyme a reductase is sterol regulatory element binding protein, the sterol regulatory element binding protein specifically binds to sterol regulatory element, the sterol regulatory element is an enhancer of genes including low density lipoprotein receptor and β -hydroxy- β -methylglutaryl coenzyme a reductase, the sterol regulatory element binding protein stimulates the expression of the gene containing the sterol regulatory element, activates the expression of the β -hydroxy- β -methylglutaryl coenzyme a reductase gene, and lowers cholesterol levels.
4. The use of the dendrobe extract of claim 1 in the preparation of a cholesterol lowering medicament, wherein the dendrobe extract increases the expression of scavenger receptor class B I, which prevents atherosclerosis due to excessive accumulation of free cholesterol, and SR-BI binds to high density lipoprotein to return excess cholesterol to the liver for further metabolism and promote cholesterol degradation.
5. The use of the extract of Dendrobii caulis as defined in claim 1 for the preparation of a cholesterol lowering medicament, wherein the extract of Dendrobii caulis treats patients with inadequate LDL-cholesterol lowering, degrades LDL-receptors, elevates plasma LDL-cholesterol levels, and lowers cholesterol levels.
6. The use of the extract of Dendrobii caulis of claim 1 for the preparation of a cholesterol lowering medicament, wherein the extract of Dendrobii caulis increases the expression of low density lipoproteins that are acted upon by lysosomal enzymes, wherein cholesterol esters are hydrolyzed to free cholesterol and fatty acids.
7. The use of the dendrobium huoshanense extract as claimed in claim 1 in the preparation of a cholesterol lowering medicament, wherein the dendrobium huoshanense extract increases the expression of high density lipoprotein and has the effect of transporting cholesterol back to the liver.
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CN103272125A (en) * | 2013-06-22 | 2013-09-04 | 武汉久源生物医药科技有限公司 | Traditional Chinese medicine composition containing dendrobium huoshanense and having hypoglycemic effect, and preparation method thereof |
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CN103272125A (en) * | 2013-06-22 | 2013-09-04 | 武汉久源生物医药科技有限公司 | Traditional Chinese medicine composition containing dendrobium huoshanense and having hypoglycemic effect, and preparation method thereof |
Non-Patent Citations (2)
Title |
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XIAO-YU WANG ET AL: "The effects of daily supplementation of Dendrobium huoshanense polysaccharide on ethanol-induced subacute liver injury in mice by proteomic analysis", 《FOOD & FUNCTION》 * |
戴亚峰等: "霍山石斛提取物降血脂作用研究", 《安徽农业科学》 * |
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