ARA-290 bụ peptide sịntetịt mejupụtara 11 amino asịd, ewepụtara site n'ụdị nhazi akụkụ atọ nke homonụ endogenous erythropoietin (EPO). Ọ na-eṅomi njikọ njikọ nke erythropoietin receptor β-co-receptor (βcR), na-ahọrọ na-arụ ọrụ protein nnabata mmezi. Nke ka mkpa, Usoro a na-agafe ihe egwu na-agbasawanye nwere ike jikọta ya na ndị na-anabata EPO omenala.
Mbụ kọrọ na 2008, mpụta nke ARA-290 na-egosi mgbanwe dị mkpa na nyocha EPO site na ọgwụgwọ hematopoietic maka nrụzi anụ ahụ ezubere iche na immunomodulation.
Mechanistically, site na ijikọ njikọ dị elu na IRR, ARA-290 na-ahọrọ ụzọ nrịbama ala ala, gụnyere JAK2-STAT3 na PI3K-Iwu, nke n'ikpeazụ modulate oké egwu mmetụta dị ka NF-κB.
E wezụga nke a, ARA-290 na-egosiputa mmetụta mgbochi mkpali na immunomodulatory dị ike, na-akwalite nrụzi akwara ma na-ebelata mgbu neuropathic, na-achịkwa metabolism, ma gosipụta ikike ọgwụgwọ maka ịgwọ obere eriri neuropathy, Charcot-Marie-Tooth ọrịa, na ọrịa shuga neuropathy.
Usoro
H-Pyr-Glu-Gln-Leu-Glu-Arg-Ala-Leu-Asn-Ser-Ser-OH
Nọmba CAS
1208243-50-8
Usoro ihe omimi
C51H84N16O21
Ibu molekụla
1257.3
Nnyocha nke ARA-290
1.Ịkwalite ikike Angiogenic nwere ike ime na ime ụlọ nke Selụ Endothelial Progenitor Na-ekesa:
- Mbụ, Ọrịa ischemic na-akpata ọrịa vaskụla na-emebi emebi. Na oke ibu na ọrịa shuga, ọnụ ọgụgụ ndị ọrịa metụtara na-aga n'ihu na-arị elu. N'ihi ya, maka ndị nwere ọrịa vaskụla siri ike, ebipụ ka bụ nhọrọ ọgwụgwọ bụ isi.
- N'ime ọmụmụ ihe dị mkpa, Enyere ARA-290 na ụmụ oke ischemia na-adịghị ala ala (CLI). Nsonaazụ gosipụtara na ARA-290 na-akwalite mmụba/mbugharị nke ukwuu yana iguzogide apoptosis nke hydrogen peroxide kpatara..
- Na mgbakwunye, otu ogwu ogbugba nke ARA-290 na-eme ka oruru ọbara nke akụkụ aka na njupụta capillary.
Na mkpokọta, Nchọpụta ndị a na-egosi na iji ARA-290 dị ka adjuvant nwere ike ịkwalite ihe angiogenic dị n'ime ya. Endothelial colon na-emepụta cell(ECFCs) na ha in vivo homing na saịtị ischemic, si otú ahụ na-akpali angiogenesis. Ya mere, Nke a na-enye usoro ọgwụgwọ ọhụrụ bara uru maka ọrịa ischemic na-adịghị ala ala.
2.Imelite mwepụta insulin na nnabata glucose n'ụdị 2 Ndị ọrịa shuga:
Na ngalaba nke metabolic, ARA-290 na-akwalite nnabata glucose na oke ndị ọrịa mamịrị na-emetụtaghị oke ndị na-abụghị ọrịa shuga.. Kpọmkwem, ọ na-akpali elu GSIS(Ihe nzuzo insulin na-akpali glucose) ọkwa, N'ikpeazụ na-emeziwanye glucose oxidation na Adenosine triphosphate(ATP) mmepụta. Site na usoro a, site na-emetụta Ọwa potassium nwere mmetụta ATP(CAAT) mmechi ọwa, N'ikpeazụ ọ na-emetụta mmepụta insulin.
3.Mgbochi mkpali na Neuroprotective Mmetụta:
Iji nyochaa neuroinflammation, na ọgwụgwọ ọgwụgwọ metụtara Lewis oke na nnwale autoimmune encephalomyelitis (EAE), nchịkwa na-aga n'ihu nke injections ARA-290 na-ebelata oke nke EAE na oke. Ọ kachasị, ọgwụgwọ a na-ebelata mkpokọta mkpụrụ ndụ na-egbu egbu na eriri afọ EAE ma gbochie mmụba na nkwupụta nke cytokines dị ka interleukin., ụbụrụ necrosis factor-α, na inducible nitric oxide synthase na EAE oke ọkpụkpụ azụ azụ.
Ọzọkwa, ọmụmụ in vitro gosipụtara na ARA-290 na-egbochi Th1 na Th7 cell polarization na EAE lymphocytes. Ọnụ, Nnwale a na-egosi na ARA-290 nwere uru ọgwụgwọ maka otutu sclerosis.
4.Na-akwalite mmezi Neural na ibelata mgbu Neuropathic:
Karịsịa, ARA-290 nwere ike gafere ozugbo mgbochi ụbụrụ ọbara, na-enyere ya aka ime ihe ozugbo dorsal mgbọrọgwụ ganglia na microglia. Ebe ahụ, ọ na-egbochi mpụta na-adịghị mma na sistemụ ụjọ ụbụrụ nke ụbụrụ, na-ebelata Central uche, ma na-arụsi ọrụ ike na-agbanwe ihe neurotrophic ka ọ na-ebelata mbufụt na mgbọrọgwụ ganglia dorsal iji mezie sistemu ụjọ nke etiti..
5.Na-eme ka mmezi anụ ahụ na ike nweghachi:
N'ikpeazụ, ARA-290 na-arụ ọrụ na mkpụrụ ndụ na-alụso ọrịa ọgụ na-egosipụta IRR, nke na-akwalite ike ha site na pro-inflammatory M1 phenotype na mgbochi mkpali na pro-mmezi M2 phenotype.. N'ihi ya, ọ na-egbochi mmeghachi omume mkpali dị ukwuu ma na-akpali nzuzo nke ihe na-eto eto dị ukwuu, na-ehichapụ mkpụrụ ndụ apoptotic, na imepụta arịa ọbara ọhụrụ. N'ikpeazụ, nke a na-eme ka iguzosi ike n'ezi ihe na arụ ọrụ nke anụ ahụ arụziri.
COA
HPLC
MS
