Carboxyreses (CES) mu mankhwala opatsirana a mankhwala: Zomwe zimachitika

Mawu osakira: Mankhwala - Kulumikizana Mabala (DDI), Carboxylesteraphse 2, CER1, CER STRYXMESEGE SUARIY, Kukhazikika kwa mankhwalawa.

Iphase Chopanga

Chiyambi

Carboxyreses (CES) ndi ma enrolytic a hydrolytic omwe akukhudzidwa ndi kagayidwe ka ester ya ester - Ndipo amide - wokhala ndi mankhwala osokoneza bongo. Mwa izi,Carboxylestrase 1 (CES1)ndiCarboxylesterase 2 (CES2)ndi otchuka kwambiri mwa anthu. Kugawa kwawo minofu ndi gawo lapansi kumapangitsa CES1 ndi Ces2 Pakati pa kumvetsetsa kwa kagayidwe,Kukhazikika kwa mankhwala osokoneza bongo, ndipoMankhwala - Zosintha Mankhwalapa sayansi yamankhwala.

CES1 ndi Cen2: Zojambula ndi Zosiyanasiyana

Carboxylestaft 1 (CES1) imafotokozedwa kwambiri m'chiwindi ndipo imatchulidwa kutiChiwindi carboxy. Enzyme imadziwika ndi gawo lalikulu kwambiri, mankhwala osokoneza bongo monga Osltamiviciiviric, methylphene, ndi clokomogl. Mosiyana ndi zimenezo, Carboxyletterase 2 (CES2) ndiwochuluka kwambiri m'matumbo, chifukwa nthawi zambiri amatchedwaMatumbo a carboxyyated. Kes2 amatenga gawo lofunika kwambiri pa kagayidwe ka anticancer monga Irinotecan ndi Prodrugs monga Capecitabine.

Njira yosinthira ya CES1 ndi Ces2 imawapangitsa mipata yovuta mu ADM (kuyamwa, kugawa kagayidwe, komanso kudzipereka). Onse a chiwindi carboxyserase (CES1) ndi matumbo a carboxyletrase (CES2) amayesedwa nthawi yayitali m'magawo oyamba a mankhwala.

Udindo wa Mankhwala Okhazikika Pakatikati

Kukhazikika kwa mankhwala osokoneza bongo ndi gawo lofunikira la pharmacokinetics. CES1 ndi Ces2 imathandizira kwambiri kukhazikika ndi theka - moyo wa elster - zomwe zimakhala ndi othandizira. CES1, kukhala kayendedwe ka chiwindi, kumapangitsa kuti kutsimikizika kwa chitsimikizo ndi plasma. CES2, ngati carboxylexyaset, makamaka imakhudza woyamba - Pass Hydrolysis a mankhwala ovomerezeka. Kuwunika momwe ma enzymes awa amathandizira ma molekyulu amathandiza kuti atseke mankhwala osokoneza bongo ndi kuperekera mankhwala.

Kuchita motsatira ma enzymes

Kuchita motsatirandikofunikira kuti mudziwe ma enzyme enieni a biotransforth. Onse a Kes 1 ndi Cent2 amatenga nawo mbali pamaphunzirowa kuti amvetsetse zopereka zawo. Kulondola molondola kumatha kudziwitsa kukula kwa Prodrugs komwe kumapangidwira ku Cent1 kapena CES2, kukuthandizani kutumiza mankhwala osokoneza bongo komanso kusintha bioavailability.

Ofufuzawo amagwiritsa ntchito zobwezeretsa zobwezera, mic2mes, microolumes (kwa ma microsumes (a chiwindi carboxyletrase ntchito), ndi ma microsomes (m'matumbo a carstades (a Carstade Carboxyresesp. Cholinga ndikuchepetsa kusiyanasiyana ndikuwonetsetsa kuti ma metabolic ndi bwino - zodziwika.

Ces enzyme zoletsa komanso mankhwala osokoneza bongo - mankhwala osokoneza bongo

Ces enzyme choletsandikuti nkhawa ikukula chifukwa cha kuthekera kwake kubweretsa mankhwala osokoneza bongo - Zogwirizana ndi Mankhwala. Kuletsa Cek1 imasokoneza kagayidwe kake kake, zomwe zimayambitsa kuchuluka kwa mankhwala osokoneza bongo. Mofananamo, zoletsa za CES2 zomwe zimalepheretsa matumbo zimatha kuchepetsa chiwonetsero cha Prodrug, kuchepetsa kuchiritsa.

Mankhwala ambiri achipembedzo komanso azachipatala - Maphunziro owonjezera amagwiritsa ntchito mankhwala osokoneza bongo tsopano amaphatikizapo kuwunika kwa CES enzyme. Izi zimathandizira kuneneratu za pharmacokinetic mabungwe atsopano komanso popanga njira zopangira zomwe zimachepetsa chiopsezo.

Mwachitsanzo, CO - Kugwiritsa ntchito CES1 Ofriton ndi methylpher angakweze plasma wogwira ntchito yogwira ntchito yogwira, ndikupanga chiopsezo cha zovuta. Mofananamo, zoletsa za CES2 pa kuphatikiza Chertherapy zimatha kusokoneza kutsegula kwa Irinotecan, kuchepetsa ntchito yake yoletsa.

Ntchito mu kafukufuku wa mankhwala

Carboxylesterase 1 (CES1) ndi Carboxylesterase 2 (Ces2) mwakhala zida zosafunikira mu kafukufuku wamakono. Kufunika kwawo:

• Kulosera kagayidwe ka mankhwala cakatibolic.
• Kuchita izi:
• Kuwunika kwa CES Enzyme kuletsa kwa mankhwala oneneratu - Zokhudza Mankhwala.
• Kupanga CES - adayambitsa ma prodrugs a kutumiza bwino.

Udindo wa CES1 monga gawo loyambirira la chiwindi ndi Cen2 popeza matumbo akuluakulu a matumbo ali bwino - Zolemba zonse za mafakitale ndi mafakitale. Pophatikizira CES yinde ntchito m'magulu a mankhwala masipu, asayansi amatha kupanga mankhwala otetezeka komanso ogwira ntchito bwino.

Mapeto

Pomaliza, Carboxylestaft 1 ndi Carboxyletterase 2 ndi oposa michere chabe yokha - ndi yofunika kwambiri ya mankhwala ndi chitetezo. Yang'anirani Pamodzi pa CES1 (Liver Carboxyretyase) ndi Cent2 (matumbo a cartastideltrase) mu metabolict) mu mankhwala a kagayidwe, a Centymeyme, odziwika bwino ogwiritsa ntchito mayesero. Kumvetsetsa kwakukulu kwa ntchito ya CES kumangothandizira kuti mankhwala opangidwa ndi mankhwala okha komanso kumawonjezeranso kuchuluka kwa ochiritsa othandizira omwe amagulitsa.