CN104873491A - Application of schisandrin b and schizandrin c in preparation of anti-hepatic fibrosis drug - Google Patents

Application of schisandrin b and schizandrin c in preparation of anti-hepatic fibrosis drug Download PDF

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CN104873491A
CN104873491A CN201510257521.XA CN201510257521A CN104873491A CN 104873491 A CN104873491 A CN 104873491A CN 201510257521 A CN201510257521 A CN 201510257521A CN 104873491 A CN104873491 A CN 104873491A
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schisandrin
hepatic fibrosis
schizandrin
group
application
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CN104873491B (en
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张海
张国庆
柴逸峰
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Second Military Medical University SMMU
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Second Military Medical University SMMU
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Abstract

The invention relates to the technical field of medicines; the main characteristic component of schisandra chinensis as the traditional Chinese medicine is a lignan component; the lignan component comprises schisandrin a, schisandrin b, schisandrin c and the like; and modern pharmacological tests prove that the lignan component has multiple pharmacological activities for protecting liver, resisting oxidization and the like. The invention provides novel medical application of schisandrin b and schizandrin c, and in particular provides application of schisandrin b and schizandrin c in preparation of an anti-hepatic fibrosis drug. Pharmacodynamics researches show that schisandrin b and schizandrin c can be used for obviously reducing the concentration of ALT (Alanine Aminotransferase) and AST (Aspartate Transaminase) in rat serum of a hepatic fibrosis model induced by common bile duct ligation and CCL4 and improving hepatic fibrosis symptoms, and have good anti-hepatic fibrosis activity; and therefore, schisandrin b and schizandrin c can be used for preparing anti-hepatic fibrosis drugs or health-care foods.

Description

Schisandrin B, schisandrin C are preparing the application in anti-hepatic fibrosis medicines
Technical field:
The present invention relates to medical art, be specifically related to schisandrin B, schisandrin C is preparing the application in anti-hepatic fibrosis medicines or health food.
Background technology:
Liver cirrhosis is one of commonly encountered diseases of serious harm human health, and the incidence rate of current China still remains on higher level.The pathologic basis of liver cirrhosis is hepatic fibrosis, the latter is the liver injury that causes of various damage liver factor (as the damage of viral hepatitis, alcoholic liver disease, some metabolic disease, medicine and chemical toxicant and hepatic parasitosis etc.) and inflammation, so cause chronic hepatopathy to develop into liver cirrhosis must through pathological process.Hepatic fibrosis is the common pathological characters of most of chronic hepatopathy, is also chronic hepatitis, the liver cirrhosis important intermediate link that further develops, worsen.Modern study shows: have the patient of 20% to 40% finally can develop into liver cirrhosis in patients with liver fibrosis, even hepatocarcinoma.Therefore the generation of hepatic fibrosis is effectively blocked, to treatment hepatic disease important in inhibiting.“
Be instruct the fibrosis research carried out in recent years with Chinese medical theory, its toxic and side effects possessed is little, the feature that therapeutic effect is good, has been widely used in experiment and clinical research.Chinese medicine Schisandra chinensis begins to be loaded in Shennong's Herbal, and is listed in top grade.The primary efficacy of Fructus Schisandrae Chinensis is astringed the lung, and nourishing kidney is promoted the production of body fluid, and receives antiperspirant, arresting seminal emission.Modern pharmacological research shows: Fructus Schisandrae Chinensis has antiinflammatory, protection and strengthens the effect such as heart body, expansion blood vessel.Main in Fructus Schisandrae Chinensis containing Fructus Schisandrae Polysaccharide, volatile oil and lignan component, wherein lignin composition has hepatoprotective effect, but wherein which chemical composition plays effect of anti hepatic fibrosis and has no pertinent literature report.
Summary of the invention:
The object of the invention is to which chemical composition in deep parsing Fructus Schisandrae Chinensis and there is effect of anti hepatic fibrosis, another object of the present invention is to the medical usage providing schisandrin B, schisandrin C new.
The present inventor studies and finds schisandrin B, schisandrin C has significant effect of anti hepatic fibrosis.The present invention proves through zoopery: adopt deoxyschizandrin, schisandrin B, schisandrin C constituents effect of anti hepatic fibrosis research experiment, and discovery schisandrin B, schisandrin C can reduce the index such as HA, LN, collagen type v in rat blood serum; Adopt CCl 4the Rat Liver Fibrosis Model experiment of induction, discovery schisandrin B, schisandrin C significantly can reduce the concentration of ALT, AST in rat blood serum, improve hepatic tissue pathology symptom, reduce the content of rat liver type III collagen, there is good effect of anti hepatic fibrosis, therefore schisandrin B, schisandrin C play therapeutical effect to hepatic fibrosis, and deoxyschizandrin does not have remarkable therapeutical effect to fibrosis.
The invention provides schisandrin B, schisandrin C is preparing the application in anti-hepatic fibrosis medicines or health food.
Anti-hepatic fibrosis of the present invention, refers to prevention or treatment hepatic fibrosis.
The pharmaceutical composition that medicine of the present invention is made up of active constituents of medicine schisandrin B, schisandrin C and pharmaceutically acceptable adjuvant.
Pharmaceutical composition of the present invention can adopt the method for medical domain routine, using schisandrin B, schisandrin C as active component, make pharmaceutical preparation with pharmaceutically acceptable adjuvant, in described pharmaceutical preparation, the weight content of active component is 0.1% ~ 99.9%.
The present invention not only specify that in Fructus Schisandrae Chinensis, which chemical composition has effect of anti hepatic fibrosis, and provides new means for hepatic fibrosis clinical treatment.
Accompanying drawing illustrates:
HE colored graph after Fig. 1: CCL4 modeling administration, wherein A is model group, and B is deoxyschizandrin group, and C is schisandrin B group, and D is schisandrin C group;
S-red colored graph after Fig. 2: CCL4 modeling administration, wherein A is model group, and B is deoxyschizandrin group, and C is schisandrin B group, and D is schisandrin C group.
Detailed description of the invention:
Below in conjunction with accompanying drawing and concrete enforcement, the invention will be further described.Should be understood that following enforcement only for illustration of the present invention but not for limiting scope of the present invention.
Embodiment 1: deoxyschizandrin, schisandrin B, schisandrin C are to the therapeutical effect of common bile duct ligation Liver Fibrosis Model rat
Common bile duct ligation hepatic fibrosis experiment (Xu Shuyun, Bian Rulian, Chen Xiu. pharmacological experimental methodology, the 3rd edition [M]. Beijing: People's Health Publisher, 2002:807).Concrete grammar is as follows:
SD rat, male and female half and half, in 6 ~ 8 week age, body weight 200 ± 10g, Second Military Medical University, PLA's Experimental Animal Center provides.
Receptacle temperature 18-22 DEG C, relative humidity 60%-75%, artificial mixed fodder is fed.
Random packet, often organizes 10 rats: blank group, model group, deoxyschizandrin group (25mg/kgd), deoxyschizandrin group (50mg/kgd), deoxyschizandrin group (75mg/kgd), schisandrin B group (25mg/kgd), schisandrin B group (50mg/kgd), schisandrin B group (75mg/kgd), schisandrin C group (25mg/kgd), schisandrin C group (50mg/kgd), schisandrin C group (75mg/kgd).Sham operated rats is abdominal incision only, is separated common bile duct, does not do common bile duct ligation, then sew up.Common bile duct ligation group three days after surgery, administration group carries out administration, the normal saline of blank group gavage equivalent.
After administration 3w, put to death mouse in the 25th day.Hepatic portal vein gets blood, after static, and centrifuging and taking serum.Detect HA (hyaluronidase), LN albumen, type III collagenous amino-tenminal, collagen type v, total protein, total bilirubin.
The results are shown in Table 1.
From table 1, indices in model group is all significantly higher than sham operated rats, proof modeling success, relative to sham operated rats and model group, dosage is that the schisandrin B of 25mg/mL and the biochemical detection indexes of schisandrin C group raise, but along with the increasing of dosage, schisandrin B, schisandrin C group significantly can reduce the indexs such as HA (hyaluronidase), LN albumen, type III collagenous amino-tenminal, collagen type v, total protein, total bilirubin, but these indexs of deoxyschizandrin group do not have reducing effect.
Experimental result shows, schisandrin B, schisandrin C have inhibitory action to common bile duct ligation hepatic fibrosis, and deoxyschizandrin does not have anti-fibrosis effect significantly.
Embodiment 2: deoxyschizandrin, schisandrin B, schisandrin C are to CCL 4the rat therapeutical effect of the Liver Fibrosis Model of induction
CCL 4the Liver Fibrosis Model of inducing is tested (Xu Shuyun, Bian Rulian, Chen Xiu. pharmacological experimental methodology, the 3rd edition [M]. Beijing: People's Health Publisher, 2002:807).Concrete grammar is as follows:
SD rat, male and female half and half, in 6 ~ 8 week age, body weight 200 ± 10g, Second Military Medical University, PLA's Experimental Animal Center provides.
Receptacle temperature 18-22 DEG C, relative humidity 60%-75%, artificial mixed fodder is fed.
Random packet, often organize 10 rats: blank group, model group, deoxyschizandrin group (25mg/kgd), deoxyschizandrin group (50mg/kgd), deoxyschizandrin group (75mg/kgd), schisandrin B group (25mg/kgd), schisandrin B group (50mg/kgd), schisandrin B group (75mg/kgd), schisandrin C group (25mg/kgd), schisandrin C group (50mg/kgd), schisandrin C group (75mg/kgd).To the CCL of each group of rat according to the injected dose lumbar injection 35% of 2ml/kg 4peanut oil solution, 2 times weekly, injects 6w altogether, the formation of induction Liver Fibrosis Model.Administration group gastric infusion from the 7th week, the normal saline of model group and blank group gavage equivalent.Administration three weeks, put to death mouse after three weeks altogether.Getting same area hepatic tissue neutral formalin to fix, for doing paraffin section, carrying out HE and S-red dyeing, all the other hepatic tissue liquid nitrogen cryopreservations.Hepatic portal vein gets blood, after static, and centrifuging and taking serum.Detect HA (hyaluronidase), Piii, TBIl index.The results are shown in Table 2, Fig. 1, Fig. 2.
Table 2:CCL 4administration biochemical detection indexes after modeling
From table 2, indices in model group is all significantly higher than sham operated rats, proof modeling success, along with schisandrin B, the increase of schisandrin C dosage, TBIl value after modeling, HA (hyaluronidase) value significantly reduces, but these indexs of deoxyschizandrin group do not reduce, and composition graphs 1, 2 is visible, schisandrin B, the collage synthesis amount of schisandrin C group comparatively model group obviously reduces, the collage synthesis amount of deoxyschizandrin group does not reduce, schisandrin B is described, schisandrin C has inhibitory action to hepatic fibrosis, deoxyschizandrin does not have anti-fibrosis effect significantly.
Above-mentioned experimental result shows, schisandrin B, schisandrin C significantly can reduce the concentration of ALT, AST in rat blood serum, improve hepatic tissue pathology symptom, reduce the content of rat liver type III collagen, and deoxyschizandrin does not have the effect of fibrosis.Schisandrin B is described, schisandrin C effectively suppresses hepatic fibrosis that there is the novelty teabag that treatment hepatic fibrosis is relevant.
Below the preferred embodiment of the invention is illustrated, but the invention is not limited to described embodiment, those of ordinary skill in the art also can make all equivalent modification or replacement under the prerequisite without prejudice to the invention spirit, and these equivalent modification or replacement are all included in the application's claim limited range.
Experimental result shows, deoxyschizandrin does not have therapeutical effect to anti-hepatic fibrosis, and schisandrin B, schisandrin C have the novelty teabag for the treatment of hepatic fibrosis.
Below the preferred embodiment of the invention is illustrated, but the invention is not limited to described embodiment, those of ordinary skill in the art also can make all equivalent modification or replacement under the prerequisite without prejudice to the invention spirit, and these equivalent modification or replacement are all included in the application's claim limited range.

Claims (3)

1. schisandrin B, schisandrin C are preparing the application in anti-hepatic fibrosis medicines or health food.
2. schisandrin B according to claim 1 and 2, schisandrin C are preparing the application in anti-hepatic fibrosis medicines or health food, it is characterized in that, the pharmaceutical composition that described medicine is made up of active constituents of medicine schisandrin B, schisandrin C and pharmaceutically acceptable adjuvant.
3. schisandrin B according to claim 1 and 2, schisandrin C are preparing the application in anti-hepatic fibrosis medicines or health food, it is characterized in that, described pharmaceutical composition can adopt the method for medical domain routine, using schisandrin B, schisandrin C as active component, pharmaceutical preparation is made with pharmaceutically acceptable adjuvant, in described pharmaceutical preparation, the weight content of active component is 0.1% ~ 99.9%.
CN201510257521.XA 2015-05-19 2015-05-19 The application of deoxyschizandrin, schisandrin C in anti-hepatic fibrosis medicines are prepared Active CN104873491B (en)

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109157534A (en) * 2018-08-09 2019-01-08 杜彬 Purposes of the deoxyschizandrin in preparation prevention or treatment renal fibrosis drug
CN110585193A (en) * 2017-09-13 2019-12-20 北京理工大学 Application of diaryl butyrolactone lignan compound in preparation of anti-hepatic fibrosis medicine
CN112107575A (en) * 2020-08-10 2020-12-22 中国人民解放军总医院第五医学中心 Lignan compound combined with furocoumarin compound for treating hepatic fibrosis
CN113274385A (en) * 2021-07-13 2021-08-20 中国人民解放军总医院第五医学中心 Pharmaceutical composition for treating chronic liver injury and application thereof
CN114394890A (en) * 2022-01-19 2022-04-26 上海市第一人民医院 Schizandrol A metabolite and application thereof in preparation of medicine for resisting idiopathic pulmonary fibrosis

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CN103860565A (en) * 2012-12-10 2014-06-18 中国人民解放军军事医学科学院毒物药物研究所 Medicinal composition for treating diabetes hepatic fibrosis

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Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110585193A (en) * 2017-09-13 2019-12-20 北京理工大学 Application of diaryl butyrolactone lignan compound in preparation of anti-hepatic fibrosis medicine
CN110585193B (en) * 2017-09-13 2022-08-02 北京理工大学 Application of diaryl butyrolactone lignan compound in preparation of anti-hepatic fibrosis medicine
CN109157534A (en) * 2018-08-09 2019-01-08 杜彬 Purposes of the deoxyschizandrin in preparation prevention or treatment renal fibrosis drug
CN112107575A (en) * 2020-08-10 2020-12-22 中国人民解放军总医院第五医学中心 Lignan compound combined with furocoumarin compound for treating hepatic fibrosis
CN113274385A (en) * 2021-07-13 2021-08-20 中国人民解放军总医院第五医学中心 Pharmaceutical composition for treating chronic liver injury and application thereof
CN114394890A (en) * 2022-01-19 2022-04-26 上海市第一人民医院 Schizandrol A metabolite and application thereof in preparation of medicine for resisting idiopathic pulmonary fibrosis

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