CN103494975A - Pathology application of schizocapsa total saponins - Google Patents
Pathology application of schizocapsa total saponins Download PDFInfo
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- CN103494975A CN103494975A CN201310478700.7A CN201310478700A CN103494975A CN 103494975 A CN103494975 A CN 103494975A CN 201310478700 A CN201310478700 A CN 201310478700A CN 103494975 A CN103494975 A CN 103494975A
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- total saponins
- dehiscent fruit
- diabetes
- fruit potato
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Abstract
The invention relates to pathology application of schizocapsa total saponins in preparing medicine for treating liver damage secondary to diabetes. The schizocapsa total saponins is capable of inhibiting CYP2E1specifically so as to treat liver function damages secondary to the diabetes, and is a hepatoprotective medicine with high medical and economic value.
Description
Technical field
The present invention relates to medical pathologies, be specifically related to the purposes in the dehiscent fruit potato total saponins medicine impaired at the liver function of preparation treatment diabetes with secondary.
Background technology
Liver is the major organs that body carries out all kinds of Substance Transformation metabolism, expresses the enzyme system of multiple participation substance metabolism, wherein the most important thing is Cytochrome P450 (being called for short CYPs).In CYPs, hypotype 2E1 (CYP2E1) main metabolic micromolecular compound, comprise that multi-medicament, halogenated hydrocarbon, alcohols, ketone and endogenous material are as arachidonic acid, fatty acid etc.CYP2E1 is considered to affect the important determiner of body to various poisonous substance infringements and carcinogenecity sensitivity, especially aspect the mediation hepar damnification.Known, at the liver lobule, be positioned at hepatocyte CYP2E1 expression around central vein and exceed 30 times than portal area CYP2E1 level.
Insecondary liver CYP2E1 high expression level can occur in diabetic, cause liver dysfunction.CYP2E1 excessively expresses and can cause intracellular mitochondrial injury, makes intracellular oxidation, Antioxidation Mechanism disequilibrium.CYP2E1, by strengthening oxidative stress, reducing antioxidant, increases the weight of lipid peroxidation, causes the generation of free radical to increase.But any molecule in the free radical attack cells, by a series of pathological processes, finally cause the infringement of hepatocyte structure and function.Simultaneously, the active oxygen produced by CYP2E1, by diffusion, can activate hepatic stellate cell and form hepatic fibrosis.On the other hand, in hepatic cell line, the CYP2E1 of overexpression can reduce the tyrosine phosphorylation of Insulin receptor INSR IRS21 and IRS22, thereby causes that insulin signaling descends, and makes the synthetic Developmental and Metabolic Disorder that reaches of fatty acid, promotes the formation of fatty liver.
For the hepatic injury case of diabetes with secondary, general nonspecific hepatic treatment for multiselect at present, lack for machine-processed specific treatment measure clinically.By the pathomechanism of research diabetes with secondary hepatic injury, the effect of CYP2E1 is familiar with gradually, for finding specific drug, protects treatment that foundation is provided.
The dehiscent fruit potato, Liliopsida, Liliidae, Liliales ， Rhizoma amorphophalli potato section, dehiscent fruit potato platymiscium, Latin formal name used at school: Schizocapsa plantaginea Hance.Be born on limit, ditch, ridge meadow more.Be distributed in the provinces and regions such as Jiangxi, Hunan, Guangdong, Guangxi and Guizhou.Be used as medicine with tuber, cure mainly laryngopharynx swelling and pain, acute gastroenteritis, urinary tract infection, toothache, chronic gastritis, Stomach duodenum ulcer, rheumatic arthritis, menoxenia, malaria, traumatic injury; Sore swollen toxin is controlled in external, traumatic hemorrhage.ZL201310072951 discloses the application of dehiscent fruit potato total saponins aspect the treatment cancer, and discloses its preparation method, at this, introduces in full the present invention.The report of dehiscent fruit potato total saponins aspect the hepatic injury for the treatment of diabetes with secondary also do not arranged so far.
Summary of the invention
Therefore, aspect first, provide the application of dehiscent fruit potato total saponins in the medicine of the hepatic injury of preparation treatment diabetes with secondary of the present invention.
In another aspect of the present invention, a kind of pharmaceutical composition for the treatment of the hepatic injury of diabetes with secondary is provided, comprise dehiscent fruit potato total saponins and pharmaceutically acceptable carrier.
Pharmaceutical composition of the present invention is applicable to being mixed with preparation, and these preparations are suitable for oral administration (for example, as tablet, capsule) and for the form of parenteral injection (as sterile solution or suspension).
Usually, can prepare in a usual manner with pharmaceutical carriers or diluent by above-mentioned preparation.In treatment, comprise in people's mammal, every daily dose of dehiscent fruit potato total saponins of the present invention is about 0.01 to 250mg/kg body weight when oral administration, when parenteral, is about 0.001 to 250mg/kg body weight.The civil day dosage of active component can change in a big way, and will depend on various factors, such as route of administration, and patient's age, body weight and sex, and can rule of thumb be come to determine by the doctor.
Dehiscent fruit potato total saponins of the present invention can be used separately, but usually will be with the form administration of pharmaceutical preparation, the acceptable diluent or carrier combination of wherein said compound and pharmacy.According to administering mode, described pharmaceutical preparation can comprise that 0.05 to 99%w/w, for example 0.10 to 80%w/w active component.
This pharmaceutical composition or pharmaceutical preparation can contain pharmaceutical acceptable carrier for example or diluent, correctives, sweetener, antiseptic, dyestuff, binding agent, dispersant, coloring agent, disintegrating agent, excipient, film former, lubricant, plasticizer, edible oil or above-mentioned two or more any combination.
Suitable pharmaceutical acceptable carrier or diluent include but not limited to, ethanol, water, glycerol, propylene glycol, magnesium carbonate, potassium phosphate, vegetable oil, animal wet goods.
Suitable binding agent includes but not limited to, starch, gelatin, glucose, sucrose, lactose, arabic gum, tragakanta, sodium alginate, carboxymethyl cellulose, hydroxypropyl emthylcellulose, Polyethylene Glycol, polyvinylpyrrolidone, wax etc.
Suitable disintegrating agent includes but not limited to, starch, methylcellulose, agar, Bentonite, xanthan gum, sodium starch glycolate, crospolyvinylpyrrolidone etc.
Suitable lubricant includes but not limited to, enuatrol, sodium stearate, stearyl fumarate, magnesium stearate, sodium benzoate, sodium acetate, sodium chloride etc.
Suitable dispersant includes but not limited to, plant gum, Tragacanth, arabic gum, alginate, glucosan, sodium carboxymethyl cellulose, methylcellulose, polyvinylpyrrolidone and gelatin.
Suitable film former includes but not limited to, hydroxypropyl emthylcellulose, ethyl cellulose and polymethacrylates.
Suitable plasticizer includes but not limited to, the Polyethylene Glycol of different molecular weight and propylene glycol.
Suitable coloring agent includes but not limited to, iron oxides, titanium dioxide etc.
Suitable edible oil includes but not limited to, Oleum Gossypii semen, Oleum sesami, Oleum Cocois and Oleum Arachidis hypogaeae semen.
The example of other additives includes but not limited to, Sorbitol, Pulvis Talci, stearic acid, calcium phosphate and polydextrose.
Preferred preparation can be tablet or injectable form.Tablet can comprise in addition disintegrating agent and/or can coating (for example, use enteric coating, or with coating materials such as the hydroxypropyl emthylcellulose coating).
The specific embodiment
embodiment 1
The mensuration of dehiscent fruit potato total saponins to CYP2E1 inhibition of enzyme activity constant
CYP2E1 catalysis aniline hydroxylation reaction, therefore the probe that AH is CYP2E1 is measured the AH activity and can be indicated the CYP2E1 activity level.Get normal swine liver: in vivo, measure the AH activity, the AH activity increases with concentration of substrate, is the saturation kinetics feature, meets the Michaelis-Menten equation.K as calculated
m95% credibility interval of value is 22.18 to 43.24 μ mol/L, V
maxvalue is 0.48 μ mol/min/mg.
According to experimental result, selecting concentration of aniline is 50 μ mol/L, carries out dehiscent fruit potato total saponins IC
50value (half-inhibition concentration) determination experiment.By the water-soluble Concentraton gradient that is configured to of dehiscent fruit potato total saponins, add external incubation system.The result demonstration, dehiscent fruit potato total saponins is concentration dependent and suppresses the AH activity, and the final concentration height of its inhibition degree and the configuration of dehiscent fruit potato total saponins is closely related.The semilog linear regression analysis shows dehiscent fruit potato total saponins IC
50value is 0.17mmol/L.
embodiment 2
The experimentation of dehiscent fruit potato total saponins to the liver injury protection effect of diabetes with secondary
With the matched group ratio, diabetes rats serum glutaminic acid aminotransferase (sALT), aspartate aminotransferase (sAST) and CYP2E1 (AH) activity all obviously raise (P all<0.05), show that secondary lesion appears in liver.
With the diabetic groups ratio; dehiscent fruit potato total saponins group liver CYP2E1 is active, serum glutaminic acid aminotransferase (sALT) and aspartate aminotransferase (sAST) all obviously reduce (P all<0.05), shows that dehiscent fruit potato total saponins can protect the liver secondary damage occurred because of diabetes.
Table 2 dehiscent fruit potato total saponins affects .n (number of cases)=15, x ± s (mean ± standard deviation) to the diabetes with secondary hepatic injury
Annotate: * P<0.01; * P<0.05
embodiment 3
Dehiscent fruit potato total saponins suppresses the experiment in vitro research of the high CYP2E1 activity of diabetes institute secondary
Diabetes rats, hepatomicrosome CYP2E1 activity is that the AH activity is 0.82 ± 0.05 μ mol/min/g, than matched group AH activity, 0.35 ± 0.12 μ mol/min/g raises 2.3 times.In the incubated in vitro system, add the dehiscent fruit potato total saponins (get dehiscent fruit potato total saponins crude drug, be diluted to variable concentrations, add external incubation system) of variable concentrations, diabetic groups CYP2E1 activity is obviously suppressed, and is concentration dependent.
Above these experimental results show, dehiscent fruit potato total saponins has the impaired effect of liver function for the treatment of diabetes with secondary, can be for clinical treatment.
Claims (4)
1. dehiscent fruit potato total saponins is preparing treatment because of the application in the medicine of the hepatic injury of diabetes with secondary.
2. a pharmaceutical composition for the treatment of the hepatic injury of diabetes with secondary, comprise dehiscent fruit potato total saponins and pharmaceutically acceptable carrier.
3. the pharmaceutical composition of claim 2, wherein said pharmaceutical composition is applicable to being mixed with preparation, and these preparations are suitable for oral administration (for example, as tablet, capsule) and for the form of parenteral injection (as sterile solution or suspension).
4. the pharmaceutical composition of claim 3, every daily dose of dehiscent fruit potato total saponins is about 0.01 to 250mg/kg body weight when oral administration, when parenteral, is about 0.001 to 250mg/kg body weight.
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| CN201310478700.7A CN103494975B (en) | 2013-10-15 | 2013-10-15 | Pathology application of schizocapsa total saponins |
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| CN201310478700.7A CN103494975B (en) | 2013-10-15 | 2013-10-15 | Pathology application of schizocapsa total saponins |
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| CN103494975A true CN103494975A (en) | 2014-01-08 |
| CN103494975B CN103494975B (en) | 2015-05-06 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105147883A (en) * | 2015-07-23 | 2015-12-16 | 广西医科大学 | Application of Schizocapsa plantaginea Hance total saponins in cell microtubule resistant effect |
| CN109172585A (en) * | 2018-07-31 | 2019-01-11 | 广西医科大学 | Pharmacodynamics application of the dehiscent fruit potato saponin(e in preparation treatment hepatic fibrosis medicines |
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| WO2000071563A2 (en) * | 1999-05-21 | 2000-11-30 | University Of Hawaii | Taccalonolide microtubule stabilizing agents |
| CN101574418A (en) * | 2009-06-16 | 2009-11-11 | 何奎 | Traditional Chinese medicine tea for treating high blood pressure, hyperlipoidemia and hyperglycosemia |
| CA2838401A1 (en) * | 2011-06-06 | 2012-12-13 | The Board Of Regents Of The University Of Texas System | Taccalonolide microtubule stabilizers |
| CN103142774A (en) * | 2013-03-07 | 2013-06-12 | 广西医科大学 | Application of total saponin extract of lobedfruit schizocapsarhizome in treatment of liver cancer and nasopharyngeal carcinoma |
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2013
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000071563A2 (en) * | 1999-05-21 | 2000-11-30 | University Of Hawaii | Taccalonolide microtubule stabilizing agents |
| CN101574418A (en) * | 2009-06-16 | 2009-11-11 | 何奎 | Traditional Chinese medicine tea for treating high blood pressure, hyperlipoidemia and hyperglycosemia |
| CA2838401A1 (en) * | 2011-06-06 | 2012-12-13 | The Board Of Regents Of The University Of Texas System | Taccalonolide microtubule stabilizers |
| CN103142774A (en) * | 2013-03-07 | 2013-06-12 | 广西医科大学 | Application of total saponin extract of lobedfruit schizocapsarhizome in treatment of liver cancer and nasopharyngeal carcinoma |
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| 陈仲良等: "箭根薯属(Tacca)苦味成分的研究——箭根酮内酯A和B的结构", 《化学学报》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105147883A (en) * | 2015-07-23 | 2015-12-16 | 广西医科大学 | Application of Schizocapsa plantaginea Hance total saponins in cell microtubule resistant effect |
| CN105147883B (en) * | 2015-07-23 | 2019-11-05 | 广西医科大学 | Dehiscent fruit potato total saposins are in the active application of anti-cell micro-pipe |
| CN109172585A (en) * | 2018-07-31 | 2019-01-11 | 广西医科大学 | Pharmacodynamics application of the dehiscent fruit potato saponin(e in preparation treatment hepatic fibrosis medicines |
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| CN103494975B (en) | 2015-05-06 |
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