CN105326822A - Medical purpose of shikimic acid - Google Patents
Medical purpose of shikimic acid Download PDFInfo
- Publication number
- CN105326822A CN105326822A CN201510932837.4A CN201510932837A CN105326822A CN 105326822 A CN105326822 A CN 105326822A CN 201510932837 A CN201510932837 A CN 201510932837A CN 105326822 A CN105326822 A CN 105326822A
- Authority
- CN
- China
- Prior art keywords
- dpp
- shikimic acid
- present
- medical purpose
- compound
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
Abstract
The invention relates to shikimic acid or solvate, acceptable on pharmacy, of shikimic acid, and purpose of shikimic acid as a treatment agent especially dipeptidyl peptidase-IV inhibitor.
Description
Technical field
The present invention relates to medical art, specifically, the present invention relates to the medicinal usage that compound shikimic acid is used as DPP IV (DPP-IV) inhibitor.
Background technology
DPP IV (IUBMB enzyme nomenclature EC.3.4.14.5) is a kind of II type memebrane protein, mention with multiple title in the literature, comprise DPP4, DP4, DAP-IV, FAP β, ADCP 2, ABP (ADAbp), Dipeptidylaminopeptidase IV, Xaa-Pro-bis-peptidyls-amino peptidase, Gly-Pro naphthyl amidase, rear proline (postproline) Dipeptidylaminopeptidase IV, lymphocyte antigen CD26, Glycoprotein G P110, DPP IV, glycyl Prolyl iminopeptidase, glycyl Prolyl iminopeptidase, X-prolyl pipeptidyl base amino peptidase, pepX, human leucocyte antigen CD26, glycylprolyl Dipeptidylaminopeptidase, two peptidyl-peptide hydrolase, glycylprolyl amino peptidase, two peptidyls-amino peptidase IV, DPPIV/CD26, aminoacyl-prolyl pipeptidyl base amino peptidase, T cell Triggering molecules Tp103, X-PDAP.DPP IV is referred to herein as " DPP-IV ".
DPP-IV is a kind of non-classical serine aminopeptidase, and its amino terminal from peptide and protein (N-end) removes Xaa-Pro dipeptides.Some naturally occurring peptide has also reported the DPP-IV dependency slow releasing of X-Gly or X-Ser type dipeptides.
The present invention relates to and can suppress dipeptidyl peptidase-IV (DipeptidylpeptidaseIV, DPP-IV) active compound and/or pharmaceutically acceptable solvate, this compounds can be used for treating diabetes, as type 2 diabetes mellitus, hyperglycemia, metabolic syndrome, hyperinsulinemia, fat, cardiovascular disease and exception are as atherosclerosis, cerebrovascular disease, central nervous system disease or exception comprise schizophrenia, anxiety neurosis, two-way depression, depression, insomnia, cognitive disorder, gastrointestinal disease and exception, cancer, inflammation and inflammatory diseases, respiratory system disease and exception, skeletal muscle is abnormal, osteoporosis, menopause syndrome or exception, periodontal is as gingivitis, with various immunoregulatory disorder.
DPP-IV belongs to serine peptidases family, jointly belongs to DPP2, DPP8, DPP9, FAP and POP etc. in addition of this family with it.Animal model experiment result shows, suppress DPP8/9 can cause the toxic reaction [LankasGR such as such as anemia, alopecia, thrombocytopenia and splenomegaly, LeitingB, etal.DipeptidylpeptidaseIVinhibitionforthetreatmentoftyp e2diabetes:potentialimportanceofselectivityoverdipeptidy lpeptidases8and9.Diabetes, 2005,54:2988-2994].Therefore, for the significant [BhumikaDP of design and development of the selective depressant of the single target spot of DPP-IV, ManJunathDG.Recentapproachestomedicinalchemistryandthera peuticpotentialofdipeptidylpeptidase-4 (DPP-4) inhibitors.EuropeanJournalofMedicinalChemistry, 2014,74:574-605], this is also difficult point and the key point of the research and development of new selective DPP-IV inhibitor.
Therefore, this area selective DPP-IV inhibitors that still Structure of need is novel, activity is strong is to meet the demand of clinical treatment.
Summary of the invention
DPP IV (DipeptidylpeptidaseIV, DPP-IV, CD26, EC3.4.14.5) is the serine protease of a class energy specific for hydrolysis polypeptide or protein N-terminal Xaa-Pro or Xaa-Ala dipeptides.DPP-IV is atypical serine proteinases, and the Ser-Asp-His catalytic triads in its C-terminal region is different from typical serine protease, for reversing.DPP-IV is II type integral membrane protein, is distributed widely in mammal and respectively organizes.DPP-IV at the differentiation surface epithelial cell of intestinal, liver, Renal proximal tubular, prostate, corpus luteum and leukocyte sub-type as lymphocyte and Expression of Macrophages.There is the soluble protein form of DPP-IV in serum, its 26S Proteasome Structure and Function is identical with embrane-associated protein form but lack hydrophobic transmembrane domain.
Suppress DPP-IV can become type 2 diabetes mellitus and fat attractive therapy.Although DPP-IV inhibitor effectively can improve the carbohydrate tolerance of type 2 diabetes mellitus patient, the half-life of many inhibitor is shorter, or toxicity is larger.Therefore, the DPP-IV inhibitor needing exploitation to have more advantage at pharmaceutically active, stability, selectivity, toxicity, pharmacokinetics or medicine at least one for characteristic is treated for type 2 diabetes mellitus.Therefore, the invention provides a class novel DPP-IV inhibitors.
Detailed description of the invention
Following test example is for illustration of of the present invention.
The present invention's compound shikimic acid used is mm Suppliers gained.
Biological assessment
Test example 1
The compounds of this invention is tested DPP-IV enzyme inhibition activity:
Instrument:
Microplate reader, Envision (PerkinElmer, USA).
Material:
People source DPP-IV, obtains in expressed in insect cells for utilizing baculovirus expression system.
Substrate, Ala-Pro-AMC.
Process:
DPP-IV can generate product A MC, the AMC utilizing emitted light through the ultraviolet excitation generation 460nm of 355nm by specific for hydrolysis substrate A la-Pro-AMC, and in the kinetic measurement unit interval, 460nm wavelength place fluorescent value linear change, calculates DPP4 activity.Experiment adopts MERK-0431 compound in contrast.
Sample DMSO dissolves, cryopreservation, and the concentration of DMSO in final system controls within the scope not affecting detection of active.
The inhibitory action of compound MERK-0431 to DPP-IV is IC50 [nM] is 17.57.
Compound shikimic acid is 11.65% when concentration is 20 μ g/mL to the inhibitory action of DPP-IV.
Conclusion: the compound shikimic acid in the present invention has certain inhibitory action to DPP-IV enzyme.
The present invention can summarize with other the concrete form without prejudice to spirit of the present invention or principal character.Therefore, no matter from which point, above-mentioned embodiment of the present invention all can only be thought explanation of the present invention and can not limit the present invention.
Claims (1)
1. the application in DPP IV (DPP-IV) inhibitor medicaments prepared by compound shikimic acid.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510932837.4A CN105326822A (en) | 2015-12-15 | 2015-12-15 | Medical purpose of shikimic acid |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510932837.4A CN105326822A (en) | 2015-12-15 | 2015-12-15 | Medical purpose of shikimic acid |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105326822A true CN105326822A (en) | 2016-02-17 |
Family
ID=55277730
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510932837.4A Pending CN105326822A (en) | 2015-12-15 | 2015-12-15 | Medical purpose of shikimic acid |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105326822A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107496396A (en) * | 2017-10-09 | 2017-12-22 | 广东工业大学 | The application of shikimic acid |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101723930A (en) * | 2009-12-02 | 2010-06-09 | 中国科学院上海药物研究所 | Shikimic acid compound and preparation method and application thereof |
| CN103338760A (en) * | 2010-11-15 | 2013-10-02 | 贝林格尔.英格海姆国际有限公司 | Vasoprotective and cardioprotective antidiabetic therapy |
-
2015
- 2015-12-15 CN CN201510932837.4A patent/CN105326822A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101723930A (en) * | 2009-12-02 | 2010-06-09 | 中国科学院上海药物研究所 | Shikimic acid compound and preparation method and application thereof |
| CN103338760A (en) * | 2010-11-15 | 2013-10-02 | 贝林格尔.英格海姆国际有限公司 | Vasoprotective and cardioprotective antidiabetic therapy |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107496396A (en) * | 2017-10-09 | 2017-12-22 | 广东工业大学 | The application of shikimic acid |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN105362272A (en) | Pharmaceutical application of rotundine | |
| CN105497028A (en) | Medicinal application of berberrubine | |
| CN107362167A (en) | Orthosphenic acid A medicinal usage | |
| CN107260738A (en) | The medicinal usage of corydalmine alkali | |
| CN107115348A (en) | The medicinal usage of cucurbatacin E | |
| CN105326822A (en) | Medical purpose of shikimic acid | |
| CN105343116A (en) | Medicine application of naringin | |
| CN105456282A (en) | Medicinal application of ginsenoside Rg1 | |
| CN105534974A (en) | Medicament application of mangiferin | |
| CN105497027A (en) | Medical application of palmatine | |
| CN105412096A (en) | Drug application of jateorhizine | |
| CN105497012A (en) | Medicinal application of bilobalide A | |
| CN105343117A (en) | Medicinal application of neohesperidin | |
| CN105343045A (en) | Medicine application of levodopa | |
| CN105343069A (en) | Pharmaceutical use of vincamine | |
| CN105362268A (en) | Pharmaceutical application of demethyleneberberine | |
| CN105343068A (en) | Pharmacological purpose of sophocarpidine | |
| CN105343058A (en) | Pharmacological purpose of artemisinin | |
| CN105343093A (en) | Pharmacological purpose of ciprofloxacin | |
| CN107913274A (en) | The medicinal usage of De Kalin alkali | |
| CN106983757A (en) | The A of cucurbitacin II medicinal usage | |
| CN107496406A (en) | The medicinal usage of scutellarin | |
| CN107252425A (en) | The medicinal usage of Dehydrocorydaline | |
| CN107714690A (en) | The medicinal usage of dihydromyricetin | |
| CN107375294A (en) | The medicinal usage of dehydroevodiamine |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160217 |
|
| WD01 | Invention patent application deemed withdrawn after publication |