Na Cocer Peptides 
ukwezi gushize
INGINGO ZOSE N'AMAKURU Y’IBICURUZWA BITANZWE KURI URU RUBUGA BISANZWE KUBONA AMAKURU N'INTEGO Z'UBUREZI.
Ibicuruzwa byatanzwe kururu rubuga bigenewe gusa mubushakashatsi bwa vitro. Mu bushakashatsi bwa vitro (Ikilatini: * mu kirahure *, bisobanura mu bikoresho by'ibirahure) bikorwa hanze y'umubiri w'umuntu. Ibicuruzwa ntabwo ari imiti, ntabwo byemejwe n’ikigo cy’Amerika gishinzwe ibiryo n’ibiyobyabwenge (FDA), kandi ntigomba gukoreshwa mu gukumira, kuvura, cyangwa gukiza indwara iyo ari yo yose y’ubuvuzi, indwara, cyangwa indwara. Birabujijwe rwose n'amategeko kwinjiza ibyo bicuruzwa mumubiri wabantu cyangwa inyamaswa muburyo ubwo aribwo bwose.
Incamake ya PE22-28
PE22-28 ni peptide 7-amino acide yashizweho ishingiye kubushakashatsi bwakozwe muri Spadin (PE 12-28). Kwiheba, indwara yo mu mutwe yibasira hafi 20% by'abatuye isi, kuri ubu ivurwa imiti igabanya ubukana ifite ibibazo nko gutinda gutangira ibikorwa n'ingaruka zikomeye. Spadin isobanurwa nka peptide ya endogenous ifite ibikorwa byo kurwanya antidepressant ihagarika cyane umuyoboro wa TREK-1, ariko ibikorwa byayo birashira nyuma yamasaha 7 nyuma yubuyobozi. Kugira ngo Spadin itere imbere kandi iboneka muri vivo, abashakashatsi berekanye ibigereranyo byayo n'ibiyikomokaho, biga ku bicuruzwa bitesha agaciro amaraso ya Spadin, hanyuma barangiza bakora PE22-28.
Igishushanyo 1 Spadin-igereranya yihariye. .
Igikorwa cya PE22-28
Ingaruka kumuyoboro wa TREK-1
Mu bushakashatsi bwa vitro ukoresheje tekinoroji ya patch-clamp kuri selile ya HTREK-1 / HEK yerekanye ko PE22-28 yerekana umwihariko hamwe nubusabane kumiyoboro ya TREK-1 ugereranije na Spadin. Amakuru yihariye yerekana ko IC₅₀ ya PE22-28 ari 0,12 nM, naho iya Spadin ni 40-60 nM. Ibi bivuze ko mubihe bimwe, PE22-28 irashobora gukora kumuyoboro wa TREK-1 neza cyane murwego rwo hasi, bityo ikagira ingaruka yibinyabuzima neza. Ubushakashatsi bwagaragaje kandi ko mu bihe bimwe, impinduka zitandukanye kuri N- cyangwa C-terminus ya PE22-28 zishobora gukomeza cyangwa gukuraho ibikorwa bya umuyoboro wa TREK-1 bitagize ingaruka ku mibanire y’umuyoboro wa TREK-1. Ubu buryo budasanzwe bwo kugenzura ibikorwa byumuyoboro hamwe nubusabane bitanga ibimenyetso byingenzi byubushakashatsi bwimbitse kubikorwa byabwo no guteza imbere ibiyobyabwenge.
Ingaruka zirwanya imiti muri vivo
Kwemeza icyitegererezo cyimyitwarire: Muburyo bwimyitwarire yo kwiheba nkikizamini cyo koga ku gahato, imiti igabanya ubukana bwa PE22-28 nibiyikomokaho byemejwe. Imbeba zavuwe hamwe na Spadin (harimo na PE22-28) zerekanye igabanuka ryinshi mugihe cyo kudahagarara. Igihe cya immobilisation nikimenyetso cyingenzi cyimyitwarire isa niyihebye mu mbeba mugihe cyo kwipimisha ku gahato, kandi kugabanuka kwigihe cyo kwimuka byerekana kugabanuka kwimyitwarire isa niyihebye, byerekana ko PE22-28 igira ingaruka zo kurwanya antidepressant. Mu kizamini cyo kugaburira udushya nyuma yiminsi 4 yo kuvura indwara zidasanzwe, PE22-28 yagabanije cyane igihe cyo gutinda kwimbeba kurya pelleti y'ibiryo. Ikizamini cyo kugaburira udushya ni uburyo bwo kugerageza gusuzuma ubushake bwimbeba zo kurya ahantu hashya. Igihe gito cyo gutinda cyerekana kugabanuka kwimyitwarire nimyitwarire ijyanye no kwiheba mu mbeba, bikomeza kwemeza ingaruka zo kurwanya antidepressant ya PE22-28.
Ingaruka kuri neurogenezi na synaptogenezi: Nyuma yiminsi 4 gusa yo kuvurwa, PE22-28 nibisa nayo byateye neurogenezi, hamwe na G / A-PE22-28 byerekana ingaruka zikomeye. Neurogenezi igira uruhare runini mu gutera indwara yo kwiheba no kuvura, kandi kubyara neuron nshya bifasha kunoza imikorere y’imitsi ndetse n’imiterere. Muri neuron yimbeba cortical neuron, PE22-28 nibiyikomokaho nabyo byongereye synaptogenez, nkuko byapimwe nurwego rwa PSD-95 rwiyongera. PSD-95 ni poroteyine ifitanye isano n'akarere ka postynaptic yuzuye, kandi kwiyongera k'urwego byerekana kwerekana uburyo bwo gukora synaps hamwe n'imikorere, byorohereza ihererekanyamakuru hagati ya neuron no kuvugurura imitsi, ibyo bikaba bifite akamaro kanini mu kunoza ibimenyetso byo kwiheba.
Ibyiza mugihe cyibikorwa: Ugereranije na Spadin, igihe cyibikorwa bya PE22-28 nibisa nabyo byateye imbere cyane. Spadin itakaza ibikorwa byayo nyuma yamasaha 7 nyuma yubuyobozi, mugihe igihe cyibikorwa bya PE22-28 gishobora kugera kumasaha 23. Igihe kirekire cyibikorwa bivuze ko ingaruka z’ibinyabuzima zishobora gukomeza igihe kirekire muri vivo, kugabanya inshuro z’ubuyobozi no kunoza iyubahirizwa ry’abarwayi, bifite akamaro gakomeye mu kuvura amavuriro.
Gusaba PE22-28
Ibishobora gukoreshwa mukuvura depression: Urebye imikorere myiza ya PE22-28 muburyo bwimyitwarire igabanya ubukana, uburyo bwihariye bwibikorwa kumuyoboro wa TREK-1, hamwe ningaruka nziza kuri neurogenezi na synaptogenez, byerekana molekile itanga ikizere cyo gusimbuza Spadin mukuvura depression. Kugaragara kwa PE22-28 bitanga uburyo bushya bwo kuvura depression. Byahindutse icyerekezo cyingenzi mugutezimbere igisekuru kizaza cyimiti igabanya ubukana. Binyuze mu bushakashatsi n’iterambere, hongerwaho uburyo bwo gufata imiti nuburyo bwo kuyobora, biteganijwe ko bizatanga uburyo bunoze bwo kuvura abarwayi bafite depression.
Inkomoko
[1] Djillani A, Pietri M, Moreno S, n'abandi. Kugereranya Spadin Kugereranya Kugaragaza Ibyiza TREK-1 Kubuza, Mubikorwa bya Vivo no Kurwanya Antidepressant [J]. Imipaka muri Farumasi, 2017,8: 643.DOI: 10.3389 / fphar.2017.00643.
Ibicuruzwa biboneka mubushakashatsi bukoreshwa gusa:
