I-Pepstatin yi-pentapeptide, i-aspartyl protease inhibitor eyenzeka ngokwemvelo, enokuthintela i-aspartic protease kunye ne-acid protease yee-microorganisms ezahlukeneyo.I-Pepstatin ikhutshwe kakhulu yi-Streptomyces iintlobo kwaye iveliswe yi-Streptomyces.Inokuthintela i-pepsin, i-pepsin D kunye ne-angiotensin-releasing enzyme, kwaye ineempembelelo zonyango kwi-gastric ulcer, i-renal hypertension, i-arthritis, i-carrageenan edema kunye nezinye izifo.
I-Pepstatin yi-inhibitor enamandla ye-aspartyl proteases ezifana ne-pepsin, i-cathepsin D, kunye ne-renin.Le pentapeptide yendalo eyodwa kwi-actinomycetes yayiyiminyaka emininzi i-classic renin inhibitor in vitro.Pepstatin ayithethi ngokuthe ngqo kwi-renin kwaye ayinyibiliki kakuhle emanzini.Izinto eziphuma kwisakhiwo se-pepstatin zandise ukunyibilika kwayo kunye nokuchaneka kwe-renin ngemiyalelo emininzi yobukhulu.I-Pepstatin iqulethe i-γ engaqhelekanga ye-amino acid statin enokuthi ithathe indawo yee-amino acids ezimbini kwibhondi ye-scissile ye-protein substrate kunye ne-block substrate cleavage ngenxa ye-analogue yesakhiwo. ukuya kwimeko yenguqu ye-peptide bond hydrolysis yi-aspartyl proteases.
Xa iprotein ikhutshwa kwiiseli ezaphukileyo, iiproteases zinokukhutshwa, ekufuneka zithintelwe ngokukhawuleza ukugcina iprotein ingawohloki.Kwinkqubo yokutsalwa kweeprotheyini, ii-protease inhibitors kufuneka zongezwe ukukhusela iproteolysis.I-Protease inhibitor ibhekisa ngokubanzi kwinto ebophelela kumaqela athile kwiziko elisebenzayo leemolekyuli zeprotease, ukuze umsebenzi weprotease wehle okanye ude uphele, kodwa ayijiki iprotein ye-enzyme.Uvakalelo lweeprotease ezahlukeneyo kwiiprotheyini ezahlukeneyo zahlukile, ngoko ke kuyimfuneko ukulungisa ukuxinana kweeproteases ezahlukeneyo.Ngenxa yokuba ukunyibilika kwe-protease inhibitor kulwelo kuphantsi kakhulu, kufuneka kunikwe ingqwalasela eyodwa kweso sithinteli seprotease kufuneka sixutywe ngokupheleleyo kwisithinteli ukunciphisa imvula ye-protease inhibitor.I-Pepstantin A inokuthintela iiprotease ze-asidi ezifana ne-pepsin, i-angiotensin, i-collagenase, i-cathepsin D kunye ne-chymosin.
I-Pepstatin A yi-inhibitor ye-cathepsin d kunye ne-e.Emva kokuba iiseli ze-HEK293 ziphathwe ngeendlela ezahlukeneyo ze-pepstatin A kwiiyure ze-24, ukubonakaliswa kwe-LC3Ⅱ kunye ne-p62 kwafunyanwa.Iziphumo zabonisa ukuba i-pepstatin A inokuphucula kakhulu ukubonakaliswa kwe-LC3Ⅱ kunye ne-P62 (P<0.05) ngendlela exhomekeke kumthamo.I-20μ g / ml i-pepstatin A yayisetyenziselwa ukunyanga i-HEK293 ngamaxesha ahlukeneyo, kunye nemiphumo yamaxesha ahlukeneyo kwintetho ye-LC3II kunye ne-p62 yabonwa.Iziphumo zibonise ukuba i-pepstatin A inokulawula ukubonakaliswa kwe-LC3II kunye ne-p62 ngexesha elixhomekeke kwixesha.
Singumenzi wepolypeptide eTshayina, esineminyaka eliqela yamava aqolileyo kwimveliso yepolypeptide.I-Hangzhou Taijia Biotech Co., Ltd. yingcali yomenzi we-polypeptide ekrwada, enokubonelela amashumi amawaka ezinto ezikrwada ze-polypeptide kwaye inokwenziwa ngokweemfuno.Umgangatho weemveliso ze-polypeptide ugqwesileyo, kwaye ukucoceka kunokufikelela kwi-98%, eye yaqatshelwa ngabasebenzisi emhlabeni wonke.
