CN103919774A - Application of demethyleneberberine in preparation of hypolipidemic drug - Google Patents
Application of demethyleneberberine in preparation of hypolipidemic drug Download PDFInfo
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- CN103919774A CN103919774A CN201310717234.3A CN201310717234A CN103919774A CN 103919774 A CN103919774 A CN 103919774A CN 201310717234 A CN201310717234 A CN 201310717234A CN 103919774 A CN103919774 A CN 103919774A
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- berberine
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- demethyleneberberine
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Abstract
The invention provides a hypolipidemic compound demethyleneberberine. The demethyleneberberine is derived from a main in-vivo metabolite of natural medicine berberine. The researches on model animals with hyperlipidemia find that the demethyleneberberine has good drug effects of reducing cholesterol, triglyceride, low density lipoprotein (LDL) and the like, and has no obvious side effects for 6 weeks of continuous medication. The discovery can lead to discovery of a new hypolipidemic drug, and provides another alternative medicine for clinic treatment of hyperlipidemia, lipid metabolism disorder and high fat and obese patients and related people wanting to lose weight.
Description
Technical field
What the present invention relates to have blood fat reducing pharmacological action goes methylene berberine and potential clinical practice thereof, be specifically related to methylene berberine and on hyperlipidemia model animal, demonstrate good effect for reducing fat, being expected to becomes a class original new drug by further research and development, loses weight for clinical blood fat reducing with for obese people.
Background technology
Hyperlipidemia is the main hazard factor that causes cardiovascular and cerebrovascular disease, is a key factor of harm humans health.Although the medicine such as Statins has good effect for reducing fat clinically, may there is the toxic and side effects such as hepatotoxicity, rhabdomyolysis in life-time service, and liver Chinese medicine metabolic enzyme is had to considerable influence.And the expression of liver Chinese medicine metabolic enzyme may exert an influence to pharmacokinetics in the body of combination with medication with active variation, cause drug interaction and cause drug effect to reduce or occur toxic and side effects.Going methylene berberine to derive from natural drug Rhizoma Coptidis, there is effect for reducing fat, have again the very berberine of high security in the present invention, for berberine interior metabolism product, research is found to go methylene berberine to have effect for reducing fat, be expected to by further research and development, become a class original new drug, lose weight for clinical blood fat reducing with for obese people.
Summary of the invention
Inventor, by berberine interior metabolism product is studied, finds that one of berberine interior metabolism product goes methylene berberine to have good effect for reducing blood fat.Be expected to through research for clinical reduction blood fat, fat-reducing etc.
Beneficial effect of the present invention
The invention provides methylene berberine in the application of preparing in blood lipid-lowering medicine, experimental results show that methylene berberine has good effect for reducing fat, provide more choices for preparing fat-reducing medicament.
Brief description of the drawings
Accompanying drawing 1 is for going methylene berberine to high blood lipid model mice effect for reducing fat figure.Wherein, C is normal feedstuff matched group; H is high lipid food model group (giving CMC-Na solution); BBR is that berberine gavage group (120mg/Kgd), M2 (i.g.) are for going methylene berberine gavage group (120mg/Kgd); M2 (i.p.) is for removing methylene berberine lumbar injection group (20mg/Kgd) .TG: total triglyceride in serum; TC: T-CHOL; HDL-C: low-density lipoprotein cholesterol LDL-C: low-density lipoprotein cholesterol.* P < 0.05, * * P < 0.01vs hyperlipidemia model group.
Detailed description of the invention
The present invention carries out detailed explanation by the following examples, but and does not mean that the present invention only limits to this.
Go methylene berberine effect for reducing fat experimentation
Example removes methylene berberine effect for reducing fat
Employing C57BL/6 mice (30, purchased from Military Medical Science Institute, body weight 18 ± 2g) test.With AIN93 standard feed (by calorific value calculation, fatty 10%, carbohydrate 75.9%, protein 14.1%, 3601 kcal/kg) and feeding standard environment under (free diet and drinking-water, day alternates with night, each 12 hours), adaptability is raised one week.Subsequently, be divided at random 5 groups by body weight, one group is continued to give normal feedstuff, other four groups all give high lipid food (by calorific value calculation, fatty 60%, carbohydrate 25.9%, protein 14.1%, heat is 5018 kcal/kg) (Nantong Te Luofei feed technology company limited), all rats all can freely drink water.Above-mentioned 5 treated animal the same terms are raised, during to 3 weeks, get blood, separation of serum slurry, measure total triglyceride (TG), T-CHOL (TC), HDL-C (HDL) and low-density lipoprotein cholesterol (LDL) in serum according to test kit explanation (the safe clinical reagent of Beijing Northization company limited), confirm hyperlipidemia model success.
High fat treated animal is divided into four groups, be divided into matched group (giving CMC-Na blank solution), berberine gavage group (BBR, 120mg/Kgd), go methylene berberine gavage group (120mg/Kgd), go methylene berberine lumbar injection group (20mg/Kgd), within every 3 days, weigh once.Respectively within after administration 6 weeks, getting blood, separation of serum, measure total triglyceride (TG), T-CHOL (TC), HDL-C (HDL) and low-density lipoprotein cholesterol (LDL) in serum with said method, and carry out statistical analysis (Student ' sttest, table 1, Fig. 1).
Measurement result shows, 3 weeks high lipid foods of model group process feeding, and animal lipid obviously raises, and modeling success is described.And berberine gavage group, go methylene berberine lumbar injection significantly to reduce Mouse Weight and lipid parameter, as total triglyceride (TG), T-CHOL (TC), low-density lipoprotein cholesterol (LDL) in serum.Prompting goes methylene berberine to have better effect for reducing fat.
After table 1 goes the administration of methylene berberine, mice index of correlation changes (n=6)
* P < 0.05, * * P < 0.01vs hyperlipidemia model group
#p < 0.05vs matched group.
Claims (8)
1. be used for the treatment of hyperlipidemia and relevant disease suc as formula the methylene berberine that goes shown in I.
Molecular formula: [C
19h
18nO
4]+; Molecular weight: 324.35
Formula I
2. except removing methylene berberine in claim 1, can also be in conjunction with the salt forming with acceptable acid pharmaceutically.Pharmaceutically acceptable acid can be organic acid, mineral acid, aminoacid.The kind of acid is as all kinds of organic and mineral acids such as citric acid, maleic acid, succinic acid, fumaric acid, malic acid, hydrobromic acid, nitric acid, tartaric acid, oxalic acid, tannic acid, methanesulfonic acid, pantothenic acid, hydrochloric acid, sulphuric acid, sulfurous acid, pyrosulfurous acid, hydrosulphuric acid, phosphoric acid, dihydrogen phosphoric acid, sulfurous acid, acetone acid, nicotinic acid, lactic acid, orotic acid, ascorbic acid, folic acid, formic acid, acetic acid, propanoic acid, butanoic acid, valeric acid, glyceric acid, glycolics.And aminoacid, as taurine, glycine, arginine, glutamic acid, lysine etc.
3. a compositions for blood lipid-lowering medicine, by shown in formula I go described in methylene berberine or claim 2 salt and one or more pharmaceutically acceptable carrier make.
4. according to the pharmaceutical composition described in salt in claim 2 and 3, it is characterized in that: also contain one or more other hypolipidemic activity compositions.
5. pharmaceutical composition according to claim 4, is characterized in that: in pharmaceutical composition, the purity of formula I compound is greater than 95%.
6. according to the pharmaceutical composition described in any one in claim 5, it is characterized in that: compositions is made into acceptable dosage form clinically, comprise the various dosage forms of oral and parenteral form.For example tablet, capsule, oral liquid, syrup, granule, drop pill, oral cavity disintegration tablet, slow releasing tablet, patch, micropill, microcapsule, liposome, microsphere, sustained-release preparation; Controlled release preparation; All kinds of solids, semisolid, liquid, Emulsion or the mixed suspension preparations such as liquid drugs injection, freeze-dried powder, aseptic powder injection, transfusion.
7. pharmaceutical composition according to claim 6, is characterized in that: described pharmaceutically acceptable carrier is selected from filler, binding agent, lubricant, disintegrating agent, cosolvent, absorption carrier; Solvent, antioxidant, adsorbent, osmotic pressure regulator, pH adjusting agent.
8. according to the purposes in claim 1, except can be used for hyperlipidemia patient, can also cause blood fat, disorders of lipid metabolism patient for diseases such as obesity, diabetes, and need other crowds of fat-reducing, blood fat reducing.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310717234.3A CN103919774A (en) | 2013-12-20 | 2013-12-20 | Application of demethyleneberberine in preparation of hypolipidemic drug |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310717234.3A CN103919774A (en) | 2013-12-20 | 2013-12-20 | Application of demethyleneberberine in preparation of hypolipidemic drug |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103919774A true CN103919774A (en) | 2014-07-16 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| CN201310717234.3A Pending CN103919774A (en) | 2013-12-20 | 2013-12-20 | Application of demethyleneberberine in preparation of hypolipidemic drug |
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| CN (1) | CN103919774A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105362268A (en) * | 2015-12-15 | 2016-03-02 | 上海壹志医药科技有限公司 | Pharmaceutical application of demethyleneberberine |
| CN111493080A (en) * | 2017-11-20 | 2020-08-07 | 华南农业大学 | Application of berberine compounds as herbicide |
| CN115215858A (en) * | 2022-07-08 | 2022-10-21 | 哈尔滨医科大学 | 2,3-disubstituted berberine derivatives, and preparation method and application thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010104595A1 (en) * | 2009-03-11 | 2010-09-16 | Xintria Pharmaceutical Corporation, Inc. | Methods and compositions for the treatment of metabolic and cardiovascular disorders |
-
2013
- 2013-12-20 CN CN201310717234.3A patent/CN103919774A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010104595A1 (en) * | 2009-03-11 | 2010-09-16 | Xintria Pharmaceutical Corporation, Inc. | Methods and compositions for the treatment of metabolic and cardiovascular disorders |
Non-Patent Citations (2)
| Title |
|---|
| SHIJIE CAO等: "Berberine metabolites exhibit triglyceride-lowering effects via activation of AMP-activated protein kinase in HepG2 cells", 《JOURNAL OF ETHNOPHARMACOLOGY》 * |
| 曹阳 等: "原小檗碱类化合物的药理作用研究进展", 《现代药物与临床》 * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105362268A (en) * | 2015-12-15 | 2016-03-02 | 上海壹志医药科技有限公司 | Pharmaceutical application of demethyleneberberine |
| CN111493080A (en) * | 2017-11-20 | 2020-08-07 | 华南农业大学 | Application of berberine compounds as herbicide |
| CN111493080B (en) * | 2017-11-20 | 2021-07-09 | 华南农业大学 | Application of berberine compounds as herbicide |
| CN115215858A (en) * | 2022-07-08 | 2022-10-21 | 哈尔滨医科大学 | 2,3-disubstituted berberine derivatives, and preparation method and application thereof |
| CN115215858B (en) * | 2022-07-08 | 2023-08-11 | 哈尔滨医科大学 | 2, 3-disubstituted berberine derivative, and preparation method and application thereof |
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| PB01 | Publication | ||
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20140716 |