Zogulitsa

Zotsatira za zotsukira pa P-glycoprotein atpase ntchito: kusiyana kwa zosokoneza za ntchito zodalira basal ndi verapamil.

P-glycoprotein (P-gp), plasma membrane glycoprotein yolumikizidwa ndi multidrug resistance phenotype, ndi amene amachititsa kuti ATP-amadalira efflux osiyanasiyana amphiphilic mankhwala.Kugwiritsa ntchito nembanemba vesicles okonzedwa kuchokera multidrug kusamva cell mzere DC-3F/ADX, tinaphunzira perturbation wa woyambira (ie, pakalibe mankhwala) ndi verapamil amadalira P-gp ATPase ntchito chifukwa ndi zotsukira zosiyanasiyana, pa sanali solubilizing, komanso pa solubilizing, ndende.Kuchuluka kwa membrane solubilization ndi kuchuluka kwa zotsukira kumawunikidwa ndi kuyesa kubalalika komanso kuyesa kwa centrifugation.Pazinthu zotsukira zosasungunuka, zotsukira zonse zoyesedwa kupatula DOC zinapangitsa kulepheretsa pang'ono kwa P-gp ATPase ntchito, zomwe sizinali zogwirizana ndi kuchuluka kwa zotsukira zosiyanasiyana zoyesedwa zophatikizidwa mu nembanemba.Kuwunika kwa kutsegulira kwa P-gp yopangidwa ndi verapamil kumawonetsa kuti zochita za P-gp ATPase zimasinthidwa mosiyanasiyana ndi zotsukira zosiyanasiyana zomwe sizisungunuka.Chifukwa chake, kuyanjana kwapadera pakati pa P-gp ndi zotsukira ndizosavuta kuchitika m'malo mosokoneza nembanemba yapadziko lonse lapansi.Pambuyo pa kusungunuka ndi zotsukira zosiyanasiyana zoyesedwa, ntchito yoyambira ya P-gp ATPase inali yoletsedwa kotheratu, kupatula pamaso pa CHAPS yomwe inatha kusunga ntchitoyi pamlingo wofanana ndi womwe umayesedwa mu nembanemba zakomweko.Komabe, kutsegulira kwa P-gp ATPase kopangidwa ndi verapamil kudatayika panthawi ya P-gp solubilization ndi CHAPS, koma idachira pambuyo pakuchepetsedwa kwa CHAPS pansi pa micellar yake yovuta kwambiri.Izi zikuwonetsa kuyanjana kwapadera pakati pa mamolekyu a P-gp ndi CHAPS mkati mwa micelles yosakanikirana.Pazonse, deta yathu yomwe ikuwonetsa kuyanjana kwapadera kwa P-gp / zotsukira zimagwirizana ndi malo omwe amanyamula mankhwala pazigawo za P-gp transmembrane.