Cov Qauv Txheej Txheem ntawm Laxogenin ntsiav tshuaj yog Laxogenin (Chemes Npe: {} nws molecular formula yog c₂₇h₄₂o₄, nrog txoj kev molecular hnyav ntawm 430.62. Lub taw tes melting yog {}}℃ntawm chav thiab hauv ib lub teeb dawb crystalline ntawm {}}℃{{8}
Tshuaj Tshuaj Muaj Zog
Cov qauv ntawm Laxogenin zoo ib yam li ntawm cov tsiaj cov tshuaj steriid, tab sis kev txhim kho cov kab ke ntawm cov nroj tsuag ntawm cov nroj tsuag ntawm cov nroj tsuag ntawm kev txhawb nqa steroids (xws li Hepatotoxicity thiab Cov Hormonal Qib tsis muaj kev tsis txaus siab), ua rau nws muaj cov khoom noj muaj txiaj ntsig zoo hauv kev ua si kis las {}}
Kev sib raug zoo nrog 5 - hydroxy-liaxogenin
Nws yog ib qho tsim nyog kom meej qhia qhov txawv laxogenin los ntawm 5 - hydumbenin {}} Txawm li cas los xij, qee cov neeg siv khoom yuav tsum paub meej tias cov ntawv tshaj tawm tiag tiag los ntawm cov ntawv ceeb toom (xws li Heplc-ms) .
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Laxogenin Hmoov Coa
Technological tog
Cov qauv kev ua kom zoo: los ntawm ntuj sterols rau cov txiaj ntsig ua ntej
Cov khoom siv tseem ceeb ntawm cov ntsiav tshuaj Laxogenin, {}} hydrot derivateghy yog thawj zaug kev hloov kho ntawm cov qauv molecular:
5 - hydroxyl ua haujlwm pab pawg qhia
Los ntawm cov txheej txheem organic, cov pab pawg hydroxyl tau muab cov khoom siv sib xyaw ua ke nrog cov khoom siv sib xyaw ua ke nrog Glycolipid metabolism ntau dua hauv cov kev cai ntawm cov teeb meem syndromes (xws li ntshav qab zib thiab rog) .
C -3 hydroxyl lub zog
Khaws cov qauv hydroxyl ntawm c-3 txoj hauj lwm los muab cov tshuaj tiv thaiv kev sib txuas ua ke rau kev sib txuas ntawm cov tshuaj yeeb yaj kiab ntawm 2023 (cn} Kuv yog cov roj av Kev cuam tshuam zoo ua rau muaj teebmeem rau indomethacin hauv cov qauv kev raug mob nas, thiab cov plab zom mov ntawm cov qauv ntawm kev ncua ntev ntawm 60% .
Ntau hom phiaj synergy: los ntawm ib qho kev txiav txim mus rau txoj kev cai qub
Cov thev naus laus zis ntawm Laxogenin ntsiav tshuaj nyob hauv nws cov phiaj xwm ntau, npog plaub txoj cai, kev tiv thaiv protabolic, kev nyab xeeb ntawm kev nyab xeeb {}}
Ua kom muaj protein synthesis
mtor pathway actformation: Laxogenin txhim kho Biosynthesis thiab protein txhais lus {}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}, nrog cov nyhuv piv rau ntawm insulin (100nm) .
Nce Leucine Incorporationion tus nqi: los ntawm kev txhim kho cov leucine Transporter (Lat1), cov Leucine Incloting cov leeg nqaij muaj protein synthesis.
Anti-inars thiab rov ua kom zoo dua
NF-κb txoj kev inhibition inibition inibition: Laxogenin tuaj yeem inhibit qhov kev ua haujlwm ntawm NF-κB)} txo qis dua 40% ntawm kev xav ntawm 10μm.
Oxidative halex kev pab tswj: Hauv lub h₂o₂le -inducation oxidination oxidin txo cov antioxidant Ros qib (sod, miv) los ntawm 30% .
Cov Kev Cai Tswj Cov Mean
Txhim kho cov roj ua kom muaj rog: activ hormone-pantotes lipase (HSL), txhawb nqa cov ntaub so ntswg rau hauv cov roj ua kom muaj zog rau kev siv hluav taws xob rau kev siv hluav taws xob}
Cov kev cai ntawm glycolipid metabolism: los ntawm kev khi rau pepars, nws tswj cov ntsiab lus ntawm Glycolip Assulte muaj peev xwm ua kom muaj peev xwm ua rau lub peev xwm 2022}} l1 adipocytes, thiab cov mechanism yuav cuam tshuam nrog mus rau kev ua kom qhib ntawm ampk txoj kev thiab cov kev txhawb nqa ntawm Glut4 transpor qhia .
Tsis-hormonal kev nyab xeeb zoo
Tsis muaj cov tshuaj tiv thaiv kab ke: Laxogenin tsis khi rau Androgen Recetors lossis tshuaj estrogen recetors, yog li zam cov hormonal qib kev tsis txaus siab .
Kev Kawm Txog Kev Kawm Txog Kev Kawm Txog Kev Tshawb Fawb Txog Kev Kawm Txog Lub Siab lossis Lub raum ua haujlwm tau pom nyob rau hauv ntev kev sim ntev Kev sim ntev (13 lub lis piam
Muaj Synthesis: los ntawm chav kuaj kom loj-teev ntau lawm
Lub thev naus laus zis ntawmLaxogenin ntsiav tshuajKuj tseem muaj kev cuam tshuam hauv kev tsim kho tshiab ntawm cov txheej txheem muaj synthesis:
Txhim kho cov khoom siv hluavtaws
Lub tuam txhab Chemshutle siv Dioscin raws li qhov pib tsim los ntawm theem kev soj ntsuam ntawm cov tshuaj tiv thaiv kev ua haujlwm ntawm kev siv tshuaj ntsuab ntxiv rau cov tshuaj tiv thaiv tshuaj ntxiv rau kev siv tshuaj ntxiv rau kev sib txuas lus
Cov qauv hloov kho tau yooj yim
Txhawb kev hloov kho txheej txheem ntawm c -17 sab saws, xws li qhia txog qib siab (HPLCT} Cov txheej txheem synthesis thiab nce cov txiaj ntsig ntawm cov khoom lag luam.
Daim Ntawv Thov ntawm Green Chemistry Technistry Technis
Los ntawm kev ua kom zoo dua cov kev tshwm sim (xws li tsawg npaum li cas-hydration thiab catality hydrogenation thiab cov txheej txheem kab ke tsis tshua muaj zog) thiab qhia cov txheej txheem los txuas ntxiv rau cov khoom siv tshuaj tsis muaj roj av {2}
Cov Ntawv Pov Ntawv Pov Hwm Cov Lus Qhia: Los ntawm Kev Tshawb Fawb Yooj Yim rau Kev Tsim Tshuaj
Cov thev naus laus zis ntawm Laxogenin ntsiav tshuaj muaj qhov tau rau nws daim ntawv thov hauv ntau daim teb kho:
Kev Kho Mob Metabolic Kho:Raws li ib tug ua ntej PARp agonist analogues, nws tuaj yeem siv los tsim cov tshuaj kho mob ntshav qab zib thiab rog rog}}}
Kev Kho Mob Qaum:Nws c -3 hydroxyl pawg tuaj yeem txuas nrog cov leeg nqaij tawv (EPRITAXT) estive estive esting 3 .} 2 zaug piv nrog cov tshuaj pub dawb hauv nas mis mis nyuj ua ke, thiab lub neej ib nrab-lub neej tau ntev txog 48 teev.
Cov Kab Mob autoimmune:Los ntawm inhibiting lub maturation ntawm dendionic cell thiab txo cov kev zais ntawm cov qhab nia ntawm Chukai Qauv .
Cov yam ntxwv ntawm cov chaw ua ke
Kuv {.}}}} use nqus: qhov sib npaug ntawm cov pib sai thiab bioavailability
Laxogenin ntsiav tshuaj yog nqus tau sai sai tom qab cov kev sim ntawm 2%, tab sis nws tuaj yeem muaj kev cuam tshuam ntawm lub qhov ncauj pib ntawm 2}}}}}}}}} LC-MS / MS) {{. Qhov sib txawv ntawm daim siab canned ntawm lub siab cannium, ua rau hauv cov metabolism hauv cov tshuaj ua ntej lawv nkag mus rau hauv cov kev ncig ua ntej.
Cov Nta Tseem Ceeb:
Peak Lub Sij Hawm: Tom qab kev tswj hwm kev noj qab haus huv, nws yuav siv tau rau 4 mus rau 5 teev, tab sis nws tsis cuam tshuam rau tag nrho cov khoom nqus .
Dose-dependent: Within the dose range of 100-400mg, the blood drug concentration increases linearly. However, at high doses (>600mg), kev nqus cov piv txwv yuav txo qis vim yog kev thauj khoom ntawm cov hnyuv thauj {}}
Kev nqus tau cov dej num muaj kev phom sij: Thaum noj cov protein lossis carbohydrates, nws tuaj yeem nce bioavailability los ntawm kev ncua plab zom mov thiab txhim kho txoj hnyuv permeability.
Ii {{. Faib: Cov ntaub mos uas nkag siab zoo thiab cov protein
Laxounenin tau faib dav hauv lub cev thiab tuaj yeem nkag rau nws cov ntshav lub hlwb, li 430 teev thiab cov licid lipid solubility (logp≈2 {}}}} 5).
Cov Nta Tseem Ceeb:
Protein Binding tus nqi: 95% ntawm cov tshuaj los ntawm Plasma Proteins tom qab kev nqus cov tshuaj, tab sis nws kuj tseem tuaj yeem ua rau muaj kev sib tw nrog lwm cov tshuaj uas muaj cov protein ntau tus nqi, xws li warfarin .
Cov ntaub so ntswg faib: Nws muaj qhov siab ntawm lub siab, cov leeg nqaij thiab cov ntaub so ntswg uas tau txhawb nqa cov nqaij tawv nqaij muaj txiaj ntsig protein synthesis.
Lub peev xwm hla kev muaj peev xwm: Cov kev sim tsiaj tau pom tias Laxogenin tuaj yeem dhau los ntawm cov ntshav ntshav, tshwj xeeb tshaj plaws nyob rau hauv cov dej ntshav, tshwj xeeb tshaj yog nce thaum lub sij hawm meningeal o.
III {. metabolism: Yooj taus ntawm ntau cov tshuab thiab cov qauv hloov kho
Cov metabolism ntawm Laxogenin yog qhov tseem ceeb ntawm cov kev tshawb fawb ntawm lub siab?
Cov Nta Tseem Ceeb:
Metabolites: plaub metabolites loj yog tsim, suav nrog ob lub pyridine analogues tau nqis tes ua ib feem zuj zus tab sis tau ua rau ntau nrawm nrawm dua.
Kev ua haujlwm metabolic enzyme induction / Inhibition: CYP3A4 Intucers (xws li ketoconazole (xws li CYP3A4 cov tshuaj uas yuav tsum tau hloov kho Ua tib zoo .
Cov Txheej Txheem Hloov Qauv Muaj Peev Xwm: nws c {0} itherification pab pawg solubility thiab glycosylation los tsim cov khoom siv produgs lossis glycosylation los txhim kho nrog fatty acids tuaj yeem txhim kho cov cuab yeej phiaj ntawm adipose nqaij .
Iv {. excretion: biliary khib nyiab - kev pab los ntawm cov quav nrog kev pab ntawm lub raum
Lub excretion ntawm Laxogenin feem ntau yog los ntawm Biliary - Kev Pab Nyiaj Txiag
Cov Nta Tseem Ceeb:
Kev Ua Kom Zoo Siab: Hauv 72 teev tom qab kev tswj hwm, kwv yees li ntawm cov hnyuv los ntawm kev ua kom zoo nkauj rau 40% ntawm cov roj ntsha ua kom tiav rau 30% {.
Urine excretion: tsuas yog 5% rau 10% ntawm cov tshuaj pleev ib ce yog ua tsis muaj cov zis ntawm cov neeg mob ib nrab-lub neej nrog cov neeg mob raum tsis txaus (GFr<30 mL/min) may be prolonged to 24-30 hours.
Terminal Ib Nrab-Lub Neej: Lub Terminal Ib Nrab-Lub Neej Ntawm Lub Xeev khov kho ntawm 1 txog 30 teev, thiab cov koob tshuaj yuav tsum tau raug txo kom zoo {}
V . hloov kho cov tshuaj siv tshuaj hauv cov neeg tshwj xeeb
Cov neeg mob uas tsis muaj nuj nqi
Rau cov neeg mob uas muaj menyuam yaus-p, vim yog cov tshuaj liaxogenin tau nce ntxiv los ntawm {}}}}}}}}}}} {}}}}
Cov neeg mob uas muaj tus tsis muaj npe tsis txaus
Txij li nws yog feem ntau yog cais los ntawm kev kub plab, cov neeg mob uas tsis muaj lub npe dua tsis xav tau kho qhov ua tsis tiav (GFR<15 mL/min) need to monitor the risk of metabolite accumulation.
Cov menyuam yaus thiab cov hluas
Cov kws ua pharmerkininetics ntawm cov hluas hnub nyoog 12-18}} Txawm li cas los xij, vim yog cov menyuam yaus tsis muaj 12 xyoos
Cim npe nrov: Laxogenin ntsiav tshuaj, cov xa khoom, chaw tsim khoom, Hoobkas, lag luam wholesale, yuav, nqe, loj, loj, rau muag