Kenyelletso eaLi-Microsomesle s5
Tšimong ea metabolism le pharmacokinetics, ho utloisisa ka thata ha li-Micricies tsa sebete le S9 li bohlokoa haholo. Tsena litsamaisong tsa vitro li na le thuso ea mekhahlelo ea pele ea ho sibolla lithethefatsi, ho fana ka leseli ho hore na mekhabiso e mecha ea lik'hemik'hale e nchafalitsoe ke sebete. Bokhoni ba ho bolela botsitso le botsitso le ts'ebelisano ea lithethefatsi ke tsa bohlokoa haholo, ho boloka nako le lisebelisoa ho nts'etsopele ea li-pharmaticaucal tse ncha. Sengoliloeng sena se fetela liphapang pakeng tsa Microsos Micrososmes le S9 likoloing, ho lekola sebopeho sa bona, ts'ebetso ea melemo, menyetla le mefokolo.Sebopeho le sebopeho sa li-Microsomes tsa sebete
● Microsomemes e le karolo ea polokelo ea endoplasmic
Li-Microsomes li na le mafahla buspication Li thehiloe ha lisele li se li theotsoe nakong ea ts'ebetso ea homone, e leng e tlisoang ke sedimonetion ho itšireletsa ka tlung. Karolo ena e supang e rusolose ka membrane - E ngolisoang enzyme 'me e patisaneng ha e ithuta metabolism ea lithethefatsi, haholo-holo karolo kea u tsoela pele.● Enzymes ea bohlokoa e kenyelletsang: Cytochrome P450s le li-uggs
TLHOKOMELISO E FELENG EA CYOCHROME P450 Enzyme (Cyps) ka Microsomes tsa bona ke karolo ea tsona e hlalosang. Mekete ena e bapala karolo ea bohlokoa litabeng tse ngata tsa metabolism ea li-Xenbootic, ho kenyelletsa le lithethefatsi tsa tikoloho. Hape e le hantle, urfinesphate -Sebopeho le sebopeho sa S9
● S9 e le motsoako oa likaroloana tsa microssal le li-cytosolic
Karolo ea S9, hangata e ne e bitsoa 9000g e phahametseng karolo ea subcon e tsoang ka har'a litloloko tsa likolo tse fapaneng. Ho fapana le li-Microsomes tse nang le semumuso sa ho itšireletsana - li-storacme tsa S9, li kenyelletsa li-enzyme tsa microssomal le li-cytorolic tse khethehileng haholoanyane.● Lijo-thollo li fumaneha ka S9 ho kenyelletsa karolo ea i le II
S9 Lihlare li fana ka setlama se chesang se secha ke sekisetsa ka bobeli joalo ka cmzuros and gliculathine - S - Transfera - s. Mefuta ena e lumella liphetoho tse eketsehileng tsa metabolity, li tsamaisang sebete sa sebete se tikolohong ea vivo haholoanyane ho feta microsomes feela.Ts'ebetso: Phato I le phase II metabolismm
● Phapang ke ts'ebetso ea enzyme pakeng tsa Microsomemes le S9
Phapang ea mantlha e teng sebakeng sa enzymatic. Li-Micromes tsa sebete tsa mantlha li tšehetsana haholo-holo karolo eo ke e etsang, e amanang le oxidation, phokotso le hydrolysis. Boitšoaro bona bo hlahisa kapa ho pepesa lihlopha tse sebetsang ka har'a lingaka tsa lithethefatsi, li beha mekhoa ea bakeng sa karolo ea karolo ea karolo ea karolo. Ka lehlakoreng le leng, liqhoro tsa S9 li na le likarolo tse ka bobeli tsa I le II, ka tsela eo li tsamaisa liphetoho tse kopaneng tseo Microsomemes a ke keng a li etsa.● Bohlokoa ba Phato II le metabolism ea lithethefatsi
Tlhaho ea liemahale tsa mehleng ea I le II ea II ea II le II li totobatsa bohlokoa ba eona ho metabolism ea lithethefatsi. Karolo eo ke fetolang likarolo ka kakaretso ho lokisa likhamphani II, tse kenyelletsang ho sitisa ho eketsa qubu ea tharollo. Ho utloisisa mekhahlelo ena ho bohlokoa ho bolela botsitso ba lithethefatsi, ho sebetsa hantle le ho ba le chefo.Likopo tsa lithuto tsa lithethefatsi tsa metabolism tsa metabolism
● Sebelisa lithutong tsa Adme: Ho ameha, ho ajoa, metabolism, molumo
Sekepe Microsomes and s9 hills lithutong tse Anseme, tse hlahlobang metamo, li abōpeho, metabolism le ho felisoa ha mekete ea lithethefatsi. Lithuto tsena li bohlokoa ho etsa qeto ea ho khetha phapanyetsano ea pharmacokineetic, ho fana ka datha ea bohlokoa e u tsebisa data, tšebelisano-bohloko.● Lithuto tsa thuto: Microsoises vs. S9 ka ho sibolla lithethefatsi
Tlhahlobo e bapisang lipakeng tsa li-microsomes le S9 li bonts'a mekhoa ea eona, ho na le pono e 'ngoe ea metabolic e ntle ea metabolic. Lithuso tsena tse felletseng tsa ho ithuta ka ho tsebahala litseleng tsa metabolic tse ka 'nang tsa se ke tsa totobala ha u sa sebelise li-microsomemes tsa sebete feela.Melemo ea Li-Microsomes
● Litsenyehelo - E sebetsa le ho fumaneha
Li-Microsomes tsa sebete li hauheloa bakeng sa litšenyehelo tsa tsona - E sebetsa le ho fumaneha ka mokhoa o sa feleng. Tsamaiso ea litokisetso tsa bona le ts'ebeliso ea bona li hantle - e thehiloe, e etsa hore li khethoe ka li-laboratori tse ngata.● Khokahano e phahameng ea lihlahisoa le boits'oaro
Tsela e bonolo ea likhaba tsa likoti e etsa hore li khone ho kenya letsoho le ho kenella, ntho ea bohlokoa ea ho hlahloba lilaebrari tse kholo ka potlako. Monyetla ona o bohlokoa haholo ho tsamaisa sejana sa ho sibolla semelo se sibolotseng, se lumella ho tseba pele ho khethoa pejana.Melemo ea Lilemo tsa Lilsa S9
● Selelekela se Ikemetseng sa Metabolic
Ka karolo e ka bobeli ea I le II e enzymes, S9 hit e fana ka tlhahlobo e felletseng ea metabolic e felileng. Sepolelo sena se felletseng se na le thuso e khethehileng bakeng sa ho tsebahatsa metabooli ba metabooli ba opeloa pele ts'ebetsong ea lithethefatsi.● Kekehloang ke metabolismm ea metabolism le menahano ea theko
Ho kopanyelletsa le li-enzyme tsa II tsa II tse bolelang hore liqheleho tsa S9 li bolela hore lits'oants'o tsa S9 li ka fana ka leseli mabapi le mokhoa oa ho ts'oaroa, ho bolela hore na lithethefatsi li tla sebetsoa joang 'meleng. Le ha li kanna tsa hloka lits'oants'o tse ling tsa litlatsetso tse ling, li ntse li fana ka litšenyehelo tse ntle le ts'ebeliso tse tsoang litlhophisong tse phahameng.Meeli ea Li-Microsomes tsa sebete
● Ho ba sieo ha li-enzyme tsa cytorac tse amang data ea metabolism e felletseng
Moeli oa bohlokoa oa Microsomemes ea sebete ke khaello ea bona ea li-cytorolic, tse bohlokoa bakeng sa setšoantšo se felletseng sa metabolic. Ho ba sieo hona ho bolela hore metaballi ea mang e ka hlokomolohuoa, mekhoa e thata ea bohlokoa e bohlokoa bakeng sa ho utloisisa polokeho le katleho ea lithethefatsi le katleho.● TLHOKOMELISO HO ETSA LINTHO TSE LING TSA BOPHELO BA PROSE II
Ho ithuta merero ea II e sa sebetsoeng, litsamaiso tse eketsehileng kapa tlatsetso le li-enzyme tsa kantle / likokoana-hloko lia sebelisa Microsomes. Tlhokahalo ena e ka thatafatsa moralo oa ho buisana le ho toloka.Meeli ea Liver SCE
● Tlhokahalo ea CO - lintlha le ho phomola ha enzyme
Ho sa tsotellehe tlhaho ea bona ea tlhaho, hangata likaroloana hangata li hloka ho eketsoa ha likokoana-hloko tsa ho tšehetsa mesebetsi e meng ea enzzymatic. Tlhokeho ena e ka hlahisa phapang le ho rarahana ho assays. Ho feta moo, thiluoa ea enzyme ho S9 histering, ha ho bapisoa le litokisetso tsa tlhaho, e ka ama maikutlo a ho fumanoa bakeng sa karabelo e itseng ea metabolic.● Lithapelo tsa tokiso le litokiso tse kemileng tsa Microsomes
Ho hlophisoa le ho boloka likaroloana tsa S9 ho ka ba thata le ho feta ho Microsomes. Ho lokisa ka nepo ts'ebetsong ea enzzymatic ka ho boloka tlhokomelo e hlokolosi ke ea bohlokoa ho fumana litholoana tse tšepahalang, li thatafatsa ts'ebeliso ea tsona ho isa ho tse kholo -Phetha le likhothaletso
● Kakaretso ea ho fetisisa - sebelisa maemo a mokhoa o mong le o mong
Sekepe Microsomes and s9 hills e 'ngoe le e' ngoe e na le matla le bofokoli. Li-Microsomes tsa sebete li sebelisoa hamolemo ha li le theko - Karolo e sebetsang, karoloana ea ho hlahlojoa ha metabolism. Ka lehlakoreng le leng, likarolo tsa S9 li tšoaneloa ke lithuto tse felletseng tse hlokang ho utloisisa ho kenella ka har'a karolo ka bobeli. Ho khetha sistimi e nepahetseng ho latela litlhoko tse ikhethileng tsa lipatlisiso le lisebelisoa tse fumanehang.● Litlhahiso tsa tšebeliso e nepahetseng lits'ebetsong tse nepahetseng tsa lithethefatsi
Bakeng sa ba leng mahlakore a lithethefatsi a lithethefatsi, ba sebelisa matla Ha Patlisiso e ntse e tsoela pele, e kenyelletsasebete S9Likaroloana, mohlomong li hlophisitsoe fekthering ea sebete sa sebete, e tla fana ka setšoantšo se felletseng sa botsitso ba metabolic, ho bolela hore na tlhahlobo ea lithethefatsi ea metabolica e tlala.● Kenyelletso eaIphase
Kantle ho pota-poteroho ea North Wales, Pennsylvania, Bioscienvanies ke "e ikhethang" e ncha - Ho latela tsebo e batsi le takatso e pharaletseng bakeng sa lipatlisiso tsa mahlale ka bophara le ho thusa bafu molemong oa bona oa bokhachane ea ho thusa ho fihlela sepheo sa bona sa lipatlisiso. Ho phehella R & D Hantle ho Bakoahlauli ba Meholo, "Ho Sebetsa Bokamoso," Ikhulo e ile ea thehoa le balekane ba Mekete ho pholletsa le lefatše.
Nako ea poso: 2024 - 11 - 261 16:50:02