CN105343058A - Pharmacological purpose of artemisinin - Google Patents
Pharmacological purpose of artemisinin Download PDFInfo
- Publication number
- CN105343058A CN105343058A CN201510932840.6A CN201510932840A CN105343058A CN 105343058 A CN105343058 A CN 105343058A CN 201510932840 A CN201510932840 A CN 201510932840A CN 105343058 A CN105343058 A CN 105343058A
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- CN
- China
- Prior art keywords
- dpp
- artemisinin
- present
- inhibitor
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Classifications
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- 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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
Abstract
The invention relates to artemisinin or a solvate, which is acceptable in pharmacology, of the artemisinin and a purpose of the artemisinin which is used as a therapeutic agent and particularly as a DPP (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 artemisinin 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 artemisinin 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 artemisinin is 10.67% when concentration is 20 μ g/mL to the inhibitory action of DPP-IV.
Conclusion: the compound artemisinin 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. compound artemisinin is preparing the application in DPP IV (DPP-IV) inhibitor medicaments.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510932840.6A CN105343058A (en) | 2015-12-15 | 2015-12-15 | Pharmacological purpose of artemisinin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510932840.6A CN105343058A (en) | 2015-12-15 | 2015-12-15 | Pharmacological purpose of artemisinin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105343058A true CN105343058A (en) | 2016-02-24 |
Family
ID=55319224
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510932840.6A Pending CN105343058A (en) | 2015-12-15 | 2015-12-15 | Pharmacological purpose of artemisinin |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105343058A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1921856A (en) * | 2004-02-20 | 2007-02-28 | 诺瓦提斯公司 | Dpp-iv inhibitors for treating neurodegeneration and cognitive disorders |
| CN103230392A (en) * | 2013-04-10 | 2013-08-07 | 上海交通大学 | Purposes of artemisinin compounds in preparing anti-atherosclerotic medicaments |
-
2015
- 2015-12-15 CN CN201510932840.6A patent/CN105343058A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1921856A (en) * | 2004-02-20 | 2007-02-28 | 诺瓦提斯公司 | Dpp-iv inhibitors for treating neurodegeneration and cognitive disorders |
| CN103230392A (en) * | 2013-04-10 | 2013-08-07 | 上海交通大学 | Purposes of artemisinin compounds in preparing anti-atherosclerotic medicaments |
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| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160224 |
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| WD01 | Invention patent application deemed withdrawn after publication |