CN107080767A - Purposes of the radix tetrastigme general flavone in treatment anti-hepatic fibrosis medicines - Google Patents
Purposes of the radix tetrastigme general flavone in treatment anti-hepatic fibrosis medicines Download PDFInfo
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
- A61K2236/333—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
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Abstract
The present invention relates to treatment anti-hepatic fibrosis medicines technical field, a kind of purposes of radix tetrastigme general flavone in treatment anti-hepatic fibrosis medicines is disclosed, medicine is treatment anti-hepatic fibrosis medicines, the preparation technology of radix tetrastigme general flavone：Take 10 30kg radix tetrastigme stem tuber coarse powder, percent by volume is added to extract 3 times for 78 85% alcohol reflux, merge extract solution and ethanol is recovered under reduced pressure, filtered after standing overnight, filtrate crosses polyamide column with after 3 degreasings of petroleum ether extraction, is successively 90 95% ethanol elutions with water, percent by volume, ethanol is recovered under reduced pressure to dry for 90 95% ethanol eluate in percent by volume, radix tetrastigme general flavone is produced.Radix tetrastigme general flavone is radix tetrastigme main component, has good therapeutic effect to liver fibrosis.The present invention selects radix tetrastigme flavone in treating liver fibrosis, with multicomponent, Mutiple Targets, multipath and the advantage such as uneasy to recur.The present invention is a kind of efficient and less liver fibrosis new types of therapeutic agents of side effect.
Description
Technical field
Anti- liver fibre is being treated the present invention relates to treatment anti-hepatic fibrosis medicines technical field, more particularly to radix tetrastigme general flavone
Tie up the purposes in chemical drug thing.
Background technology
Liver fibrosis is dynamic process of the chronic liver injury to cirrhosis progress, shows as extracellular matrix (ECM) a large amount of
Synthesis, secretion, and absolute or relative deficiency of degrading, make ECM diffuse deposition in liver.It originates in liver cell (HC) necrosis,
It is inflammatory reaction, fiber generation medium release, HSCs (FSC) activation, finally with liver connective tissue elements therewith
Synthesis and obvious disequilibrium of degrading.Liver fibrosis is the common pathologic process of a variety of chronic liver diseases, is the important of influence prognosis
Factor.
Between past 20 years, the research of liver fibrosis makes significant progress, it was demonstrated that liver fibrosis and a certain degree of liver
Hardening is all reversible.Occur in that some Strategies of Anti-fibrosis Therapy methods successively in recent years, including chemical drugs, biological agent, in
Medicine and gene therapy etc., but preferably clinical treatment means still lack.The key of preventing and treating liver fiber is to be directed to and liver at present
The related link of stellate cell activator, mainly：Mitigate hepatic injury；Suppress stellate cell activator, reduce extracellular matrix and produce；
Adjust cell factor disorderly, promote activated hepatic stellate cells apoptosis；Suppress the fibroblastic propagation of liver and sternzellen
The a large amount of secretion fibroblastic propagation of induced liver of activation.
The content of the invention
The present invention in view of the shortcomings of the prior art, discloses use of the radix tetrastigme general flavone in treatment anti-hepatic fibrosis medicines
On the way.
In order to solve the above-mentioned technical problem, the present invention is addressed by following technical proposals.
Purposes of the radix tetrastigme general flavone in treatment anti-hepatic fibrosis medicines, medicine is treatment anti-hepatic fibrosis medicines, three
The preparation technology of leaf green grass or young crops general flavone：10-30kg radix tetrastigme stem tuber coarse powder is taken, percent by volume is added and is returned for 78-85% ethanol
Stream is extracted 3 times, merges extract solution and ethanol is recovered under reduced pressure, filtered after standing overnight, filtrate is with after 3 degreasings of petroleum ether extraction, mistake
Polyamide column, is successively 90-95% ethanol elutions with water, percent by volume, by the ethanol elution that percent by volume is 90-95%
Ethanol is recovered under reduced pressure to dry in liquid, produces radix tetrastigme general flavone.Radix tetrastigme general flavone for treating anti-hepatic fibrosis, uses volume
Percentage for 78-85% ethanol extract when, effective component extracting it is better.
Preferably, taking 20kg radix tetrastigme stem tuber coarse powder.
Extracted 3 times for 80% alcohol reflux preferably, adding percent by volume.Three for treating anti-hepatic fibrosis
Leaf green grass or young crops general flavone, using percent by volume for 80% ethanol extract when, effective component extracting it is better.
Preferably, crossing polyamide column, successively with water, 95% ethanol elution, percent by volume is washed for 95% ethanol
Ethanol is recovered under reduced pressure to dry in de- liquid.
Preferably, including setting up liver fibrosis mouse model, comprising the following steps, 18-22g male mices are taken, in hero
Property mouse peritoneal injects 2mg/kg carbon tetrachloride 3 times a week, continues six weeks, sets up liver fibrosis mouse model, is making respectively
Draw materials 1 week, 2 weeks, 4 weeks, 6 weeks of mould.
Compared with prior art, beneficial effects of the present invention are：Liver fibrosis is to the national economic development and health of people
Significant impact is caused, the life of the serious threat people, it has also become one of major issue of harm health in world wide, enter one
Step accelerates pathogenesis and the original new drug research and development of its early stage pathogenesis " liver fibrosis ", it appears very urgent.Domestic appearance
The hf resi stant medicine of property has colchicin, penicillamine, prostaglandin E2, Guadisu, hanfangchin A, peach kernel preparation, cordyceps sinensis
Preparation and compound red sage root preparation etc., but mostly curative effect is not obvious and side effect is larger.
Radix tetrastigme general flavone is radix tetrastigme main component, has good therapeutic effect to liver fibrosis.The present invention is selected
Radix tetrastigme flavone in treating liver fibrosis, with multicomponent, Mutiple Targets, multipath and the advantage such as uneasy to recur, will turn into the country
One main path of outer innovation medicine.The present invention is a kind of efficient and less liver fibrosis novel therapeutic medicine of side effect
Thing.
Brief description of the drawings
Fig. 1 is pathological section figure.Wherein, a, b, c, d, e, f are dyed with HE, and a is normal group, and b is model group, and c is autumn waters -- limid eyes
Celestial alkali group (positive drug), d is general flavone group (40mg/kg), and e is general flavone group (80mg/kg), and f is general flavone group (160mg/
kg)；
Wherein, a-1, b-1, c-1, d-1, e-1, f-1 are dyed with Masson, and a-1 is normal group, and b-1 is model group, c-1
It is colchicin group (positive drug), d-1 is general flavone group (40mg/kg), and e-1 is general flavone group (80mg/kg), and f-1 is total Huang
Ketone group (160mg/kg).
Embodiment
Embodiment 1
Purposes of the radix tetrastigme general flavone in treatment anti-hepatic fibrosis medicines, medicine is treatment anti-hepatic fibrosis medicines, three
The preparation technology of leaf green grass or young crops general flavone：20kg radix tetrastigme stem tuber coarse powder is taken, percent by volume is added and extracts 3 for 80% alcohol reflux
It is secondary, merge extract solution and ethanol is recovered under reduced pressure, filtered after standing overnight, filtrate crosses polyamide with after 3 degreasings of petroleum ether extraction
Post, is successively 95% ethanol elution with water, percent by volume, percent by volume is recovered under reduced pressure into second for 95% ethanol eluate
Alcohol produces radix tetrastigme general flavone to dry.
Also include setting up liver fibrosis mouse model, comprise the following steps, take 18-22g male mices, in male mice abdomen
Chamber injects 2mg/kg carbon tetrachloride 3 times a week, continues six weeks, sets up liver fibrosis mouse model, respectively in modeling 1 week, 2
Week, 4 weeks, 6 weeks draw materials.
1. radix tetrastigme general flavone anti-hepatic fibrosis drug action (as shown in Figure 1)：
Pathological examination result shows that radix tetrastigme general flavone composition various dose group can be effectively protected liver cell, prevent
Degeneration of liver cells, necrosis, you can prevent inflammatory cell infiltration, HSC activation and proliferation of fibrous tissue, cut off to liver fibrosis, liver
The pathologic process of development is hardened, and takes and liver function will not be had undesirable effect for a long time, there may be protection to liver on the contrary
Effect.
2. influence of the radix tetrastigme general flavone to liver fibrosis mice serum ALT, AST
Influence of the radix tetrastigme general flavone of table 1 to liver fibrosis mice serum ALT, AST
| Group | ALT(U/L) | AST(U/L) |
| Normal group | 27.45±6.32 | 64.78±9.64 |
| Model group | 146.21±12.09## | 124.98±9.94## |
| Colchicin (0.2mg/kg positive drugs) | 87.89±14.54** | 89.83±11.07** |
| General flavone low dosage (40mg/kg) | 135.76±10.79 | 102.76±12.12 |
| General flavone middle dosage (80mg/kg) | 112.33±15.68** | 115.06±11.25** |
| General flavone high dose (160mg/kg) | 86.39±9.24** | 89.56±16.19** |
Note：##P<0.01vs. normal groups；*P<0.05,**P<0.01vs. model groups
Shown in table 1, Liver Fibrosis Model rat blood serum ALT, AST is significantly raised compared with normal group, radix tetrastigme general flavone
Treatment group's transaminase declines, and positive controls colchicin also can substantially reduce model mice serum transaminase ALT, AST.
3. hepatic tissue is ground to form pasty state by influence (SOD, GSH-PX, MDA) of the radix tetrastigme general flavone to MDA
(9mL physiological saline/g hepatic tissues), 4000r/min centrifugation 10min, takes supernatant, produces 10% tissue homogenate.According to ELISA
Kit illustrates the content for detecting SOD, GSH-PX, MDA.
The liver fibrosis mouse liver homogenate MDA that the radix tetrastigme general flavone of table 2 is induced CCl4, SOD and GSH-Px levels
Influence
Note：##P<0.01vs. normal groups；*P<0.05,**P<0.01vs. model groups.
Shown in table 2, SOD and GSH-Px enzymatic activitys are remarkably decreased in model group mouse liver even slurry, and MDA contents significantly rise
It is high.Elevated MDA values can be significantly reduced by giving after radix tetrastigme flavone in treating, and significantly increased SOD and GSH-Px activity.Col
Group can significantly reduced content MDA, be remarkably improved GSH-Px enzymatic activitys.
3. influence of the radix tetrastigme general flavone to Hyp in hepatic tissue：Hepatic tissue is ground to form into pasty state (9mL physiological saline/g livers
Tissue), 4000r/min centrifugation 10min take supernatant, produce 10% tissue homogenate.According to ELISA kit explanation detection Hyp
Content.
Influence of the radix tetrastigme general flavone of table 3 to Hyp in hepatic tissue
Note：##P<0.01vs. normal groups；*P<0.05,**P<0.01vs. model groups.
Shown in table 3, liver Hyp is an important indicator for reflecting degree of hepatic fibrosis, is as a result shown, with Normal group
Compare, rat model liver tissue homogenate Hyp contents significantly increase (P<0.01) radix tetrastigme general flavone (80,160mg/kg-), is given
After colchicin (0.2mg/kg), liver homogenate Hyp contents (P can be significantly reduced<0.01).
4. influence of the radix tetrastigme general flavone to TNF-α in serum and IL-6：Each group mouse orbit takes and centrifuged after blood, standing,
Take serum, operating procedure to specifications, using the content of ELISA method detection relevant cell factor TNF-α and IL-6.
Influence of the radix tetrastigme general flavone of table 4 to TNF-α in serum and IL-6
| Group | TNF-α(fmol/mL) | IL-6(pg/mL) |
| Normal group | 18.59±3.56 | 131.05±21.34 |
| Model group | 46.01±7.49## | 412.78±28.92## |
| Colchicin (0.2mg/kg positive drugs) | 32.39±3.34** | 289.53±31.46** |
| General flavone low dosage (40mg/kg) | 39.96±6.79* | 310.31±15.38* |
| General flavone middle dosage (80mg/kg) | 33.03±5.67** | 268.25±27.51** |
| General flavone high dose (160mg/kg) | 25.67±4.33** | 263.06±44.74** |
Note：##P<0.01vs. normal groups；*P<0.05,**P<0.01vs. model groups.
The result of table 4 shows that model group rats TNF-α and IL-6 expression significantly raise (P compared with Normal group<0.01).Give
Give after radix tetrastigme general flavone (80,160mg/kg-) and colchicin (0.2mg/kg), model group rats TNF-α and IL-6
Expression is decreased obviously.
Embodiment 2
Purposes of the radix tetrastigme general flavone in treatment anti-hepatic fibrosis medicines, medicine is treatment anti-hepatic fibrosis medicines, three
The preparation technology of leaf green grass or young crops general flavone：10kg radix tetrastigme stem tuber coarse powder is taken, percent by volume is added and extracts 3 for 78% alcohol reflux
It is secondary, merge extract solution and ethanol is recovered under reduced pressure, filtered after standing overnight, filtrate crosses polyamide with after 3 degreasings of petroleum ether extraction
Post, is successively 90-% ethanol elutions with water, percent by volume, and percent by volume is recovered under reduced pressure for 90% ethanol eluate
Ethanol produces radix tetrastigme general flavone to dry.
Including setting up liver fibrosis mouse model, comprise the following steps, take 18-22g male mices, in male mice abdominal cavity
2mg/kg carbon tetrachloride is injected 3 times a week, is continued six weeks, is set up liver fibrosis mouse model, respectively in modeling 1 week, 2
Week, 4 weeks, 6 weeks draw materials.
Embodiment 3
Purposes of the radix tetrastigme general flavone in treatment anti-hepatic fibrosis medicines, medicine is treatment anti-hepatic fibrosis medicines, three
The preparation technology of leaf green grass or young crops general flavone：30kg radix tetrastigme stem tuber coarse powder is taken, percent by volume is added and extracts 3 for 85% alcohol reflux
It is secondary, merge extract solution and ethanol is recovered under reduced pressure, filtered after standing overnight, filtrate crosses polyamide with after 3 degreasings of petroleum ether extraction
Post, is successively 92% ethanol elution with water, percent by volume, percent by volume is recovered under reduced pressure into second for 92% ethanol eluate
Alcohol produces radix tetrastigme general flavone to dry.
Including setting up liver fibrosis mouse model, comprise the following steps, take 18-22g male mices, in male mice abdominal cavity
2mg/kg carbon tetrachloride is injected 3 times a week, is continued six weeks, is set up liver fibrosis mouse model, respectively in modeling 1 week, 2
Week, 4 weeks, 6 weeks draw materials.
In a word, presently preferred embodiments of the present invention, all equalizations made according to scope of the present invention patent be the foregoing is only
Change and modification, should all belong to the covering scope of patent of the present invention.
Claims (5)
1. purposes of the radix tetrastigme general flavone in treatment anti-hepatic fibrosis medicines, it is characterised in that：Medicine is the anti-liver fiber for the treatment of
Chemical drug thing, the preparation technology of radix tetrastigme general flavone：10-30kg radix tetrastigme stem tuber coarse powder is taken, addition percent by volume is 78-85%
Alcohol reflux extract 3 times, merge extract solution and ethanol be recovered under reduced pressure, filtered after standing overnight, filtrate is taken off with petroleum ether extraction 3 times
After fat, polyamide column is crossed, is successively 90-95% ethanol elutions with water, percent by volume, be 90-95%'s by percent by volume
Ethanol is recovered under reduced pressure to dry in ethanol eluate, produces radix tetrastigme general flavone.
2. purposes of the radix tetrastigme general flavone according to claim 1 in treatment anti-hepatic fibrosis medicines, it is characterised in that：
Take 20kg radix tetrastigme stem tuber coarse powder.
3. purposes of the radix tetrastigme general flavone according to claim 1 in treatment anti-hepatic fibrosis medicines, it is characterised in that：
Percent by volume is added to extract 3 times for 80% alcohol reflux.
4. purposes of the radix tetrastigme general flavone according to claim 1 in treatment anti-hepatic fibrosis medicines, it is characterised in that：
Polyamide column is crossed, successively with water, 95% ethanol elution, ethanol is recovered under reduced pressure extremely for 95% ethanol eluate in percent by volume
It is dry.
5. purposes of the radix tetrastigme general flavone according to claim 1 in treatment anti-hepatic fibrosis medicines, it is characterised in that：
Including setting up liver fibrosis mouse model, comprise the following steps, take 18-22g male mices, in male mice abdominal cavity 3 times a week
Inject 2mg/kg carbon tetrachloride, continue six weeks, set up liver fibrosis mouse model, respectively in modeling 1 week, 2 weeks, 4 weeks, 6
Week draws materials.
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| CN109303819A (en) * | 2018-11-24 | 2019-02-05 | 郎国忠 | A kind of processing technology of radix tetrastigme |
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| CN109303819A (en) * | 2018-11-24 | 2019-02-05 | 郎国忠 | A kind of processing technology of radix tetrastigme |
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Application publication date: 20170822 |