Kayayyaki

Tasirin kayan wanka akan P-glycoprotein atpase ayyuka: bambance-bambance a cikin rikice-rikice na basal da ayyukan dogaro da verapamil.

P-glycoprotein (P-gp), wani membrane glycoprotein na plasma wanda ke da alaƙa da phenotype na juriya da yawa, yana da alhakin zubar da tushen ATP na magungunan amphiphilic daban-daban.Yin amfani da vesicles na membrane da aka shirya daga layin salula mai juriya da yawa DC-3F / ADX, mun yi nazarin rikicewar basal (watau in babu magani) da ayyukan P-gp ATPase masu dogara da verapamil waɗanda masu wanke-wanke daban-daban suka jawo, a marasa narkewa, da kuma a solubilizing, maida hankali.Ana kula da solubilization na membrane na ci gaba tare da ƙara yawan abin da ake amfani da kayan wanka ta hanyar watsawar haske da gwaje-gwajen centrifugation.Don abubuwan da ba a warware su ba, duk abubuwan da aka gwada banda DOC sun haifar da wani ɓangare na hana aikin P-gp ATPase, wanda ba shi da alaƙa da adadin nau'in nau'in nau'in nau'i na gwajin da aka haɗa a cikin membranes.Binciken P-gp mai kunnawa na verapamil yana nuna cewa ayyukan P-gp ATPase an canza su daban-daban ta hanyar wanke-wanke daban-daban a abubuwan da ba su da ƙarfi.Don haka, ƙayyadaddun hulɗar tsakanin P-gp da abubuwan wanke-wanke suna iya faruwa fiye da lalata membrane na duniya.Bayan narkar da kayan wanke-wanke daban-daban da aka gwada, aikin basal P-gp ATPase kusan an hana shi gabaɗaya, sai dai a gaban CHAPS wanda ya sami damar adana wannan aikin a matakin daidai da wanda aka auna a cikin membranes na asali.Koyaya, an rasa kunnawa P-gp ATPase na verapamil a lokacin P-gp solubilization ta CHAPS, amma an dawo dashi bayan dilution na CHAPS ƙasa da mahimmancin tattarawar micellar.Waɗannan abubuwan lura suna nuna takamaiman hulɗa tsakanin P-gp da ƙwayoyin CHAPS a cikin gauraye micelles.Gabaɗaya, bayananmu da ke tabbatar da takamaiman hulɗar P-gp / kayan wanke-wanke sun yi daidai da wurin wuraren jigilar magunguna a kan yankuna masu canzawa na P-gp.