ARA-290 ke peptide ea maiketsetso e entsoeng ka 11 li-amino acid, e nkiloeng mofuteng oa sebopeho sa mahlakore a mararo a homone ea endogenous erythropoietin (EPO). E etsisa sebopeho se tlamang sa erythropoietin receptor β-co-receptor (βcR), ka mokhoa o ikhethileng o kenya tšebetsong protheine ea receptor ea tokiso. Habohlokoa le ho feta, mochine ona o qoba likotsi tse ngata tse ka 'nang tsa amahanngoa le li-receptor tsa setso tsa EPO.
Ea pele e tlalehiloeng ka 2008, Ho hlaha ha ARA-290 ho bolela phetoho ea leano lipatlisisong tsa EPO ho tloha kalafong ea hematopoietic ho lebisa tlhokomelong ea tokiso ea lisele le immunomodulation.
Ka metjhini, ka ho tlama ka kamano e phahameng le IRR, ARA-290 e kenya tšebetsong litsela tsa mats'oants'o tse tlase, ho kenyeletsa JAK2-STAT3 le PI3K-Molao, e qetellang e fetola bahlahisi ba bohlokoa joalo ka NF-kB.
Ho feta mona, ARA-290 e bonts'a litlamorao tse matla tsa anti-inflammatory le immunomodulatory, e thusa ho lokisa methapo ea kutlo le ho kokobetsa bohloko ba neuropathic, e laola metabolism, mme e bonts'a bokhoni ba kalafo bakeng sa ho alafa methapo e nyane ea fiber, Lefu la Charcot-Marie-Tooth, le lefu la tsoekere la methapo ea kutlo.
Tatelano
H-Pyr-Glu-Gln-Leu-Glu-Arg-Ala-Leu-Asn-Ser-Ser-OH
Nomoro ea CAS
1208243-50-8
Foromo ea limolek'hule
C51H84N16O21
Boima ba Molek'hule
1257.3
Lipatlisiso tsa ARA-290
1.Ho Ntlafatsa Matla a Angiogenic le Matla a Ho Homing a Ho potoloha Lisele tsa Endothelial Progenitor:
- Ea pele, mafu a ischemic a tšoantšetsa mafu a senyang a vascular. Ka ho ata ha botenya le lefu la tsoekere, palo ea bakuli ba amehileng e ntse e eketseha. Ka lebaka leo, bakeng sa batho ba nang le lefu la vascular le matla, ho khaoloa e ntse e le khetho ea mantlha ea kalafo.
- Thutong e amehang, ARA-290 e ile ea fuoa litoeba ka ischemia ea maoto e sa foleng (CLI). Liphetho li bonts'itse hore ARA-290 e ntlafatsa haholo ho ata / ho falla le ho hanela apoptosis e bakoang ke hydrogen peroxide..
- Ho phaella moo, ente e le 'ngoe ea ARA-290 e ntlafalitse phallo ea mali ea maoto le matsoho.
Ka kopanelo, liphuputso tsena li bonts'a hore ho sebelisa ARA-290 joalo ka mothusi ho ka ntlafatsa thepa ea angiogenic ea kahare. Endothelial colony e etsa sele(ECFCs) le in vivo ea bona ho ea libakeng tsa ischemic, ka tsela eo e susumetsa angiogenesis. Kahoo, sena se fana ka mokhoa o sebetsang o mocha oa phekolo bakeng sa mafu a sa foleng a ischemic.
2.Ho ntlafatsa tlhahiso ea insulin le mamello ea tsoekere ka mofuta 2 Bakuli ba Lefu la tsoekere:
Sebakeng sa metabolic, ARA-290 e ntlafatsa haholo mamello ea tsoekere ho likhoto tsa lefu la tsoekere ntle le ho ama likhoto tse se nang lefu la tsoekere.. Ka ho toba, e hlasimolla e phahamisitsoe GSIS(Sekhahla sa Insulin e susumetsoang ke Glucose) maemo, qetellong ea ntlafatsa oxidation ea tsoekere le Adenosine triphosphate(ATP) tlhahiso. Ka mochine ona, ka ho susumetsa Mocha oa potasiamo o utloang ATP(KATSE) ho koaloa ha kanale, qetellong e ama tlhahiso ea insulin.
3.Anti-inflammatory le Neuroprotective Effects:
Ho hlahloba neuroinflammation, tekong ea phekolo e amang likhoto tsa Lewis le liteko tsa autoimmune encephalomyelitis (EAE), tsamaiso e tsoelang pele ea liente tsa ARA-290 e fokolitse haholo ho tiea ha EAE ho likhoto. Ka ho khetheha, Kalafo ena e ile ea fokotsa ho bokellana ha lisele tsa ho ruruha mokokotlong oa mokokotlo oa EAE le ho thibela ho ata le ho hlahisa li-cytokine tse kang interleukin., tumor necrosis factor-α, le innducible nitric oxide synthase ho EAE rat lesapo la mokokotlo.
Ho feta moo, Lithuto tsa in vitro li bontšitse hore ARA-290 e thibela Th1 le Th7 sele polarization ho EAE lymphocytes. Mmoho, teko ena e bontša hore ARA-290 e na le molemo oa phekolo bakeng sa multiple sclerosis.
4.Ho Khothalletsa ho Lokisoa ha Neural le ho Fokotsa Bohloko ba Neuropathic:
Ka ho khetheha, ARA-290 ka ho toba tšela le mokoallo oa mali-boko, ho e nolofalletsa ho sebetsa ka kotloloho mokokotlo oa motso oa ganglia le microglia. Mono, e hatella ho tsoa ho sa tloaelehang tsamaisong ea methapo e bohareng ea boko, fokotsa maikutlo a bohareng, 'me ka mafolofolo e fetola lintlha tsa neurotrophic ha e ntse e fokotsa ho ruruha ho dorsal root ganglia ho lokisa tsamaiso ea methapo e bohareng..
5.Ho Ntlafatsa ho Lokisoa ha Mahlaseli le Matla a Tsosoloso:
Qetellong, ARA-290 e sebetsa liseleng tsa tlhaho tsa 'mele tse hlahisang IRR, e khothalletsang ka matla polarization ea bona ho tloha ho pro-inflammatory M1 phenotype ho ea ho anti-inflammatory le pro-repair M2 phenotype. Ka hoo, e hatella likarabo tse feteletseng tsa ho ruruha ha e ntse e susumetsa secretion ea lintlha tse ngata tsa kgolo, ho hloekisa lisele tsa apoptotic, le ho theha methapo e mecha ea mali. Qetellong, sena se ntlafatsa botšepehi ba sebopeho le thepa ea mechine ea lisele tse lokisitsoeng.
COA
HPLC
MOF
