Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm mycophenolic acid CAS 24280-93-1 hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo mycophenolic acid cas 24280-93-1 muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Mycophenolic acid, chemical formula C17H20O6, yog mis nyuj dawb hmoov uas yog soluble nyob rau hauv methanol thiab ethanol, me ntsis soluble nyob rau hauv ether thiab chloroform, insoluble nyob rau hauv benzene thiab toluene, thiab yuav luag insoluble nyob rau hauv dej txias. Mycophenlic acid ester, raws li lub ntsiab tiv thaiv kab mob, tau siv dav hauv tsev thiab txawv teb chaws los tiv thaiv thiab kho mob tsis zoo ntawm cov kab mob hloov pauv. Ua los ntawm fermentation metabolism ntawm Penicillium Brevi compactum, nws yog ib qho tshuaj tua kab mob nrog cov tshuaj tiv thaiv kab mob.
|
|
|
|
Tshuaj Formula |
C17H20O6 |
|
Exact Mass |
320 |
|
Molecular Luj |
320 |
|
m/z |
320 (100.0%), 321 (18.4%), 322 (1.6%), 322 (1.2%) |
|
Elemental Analysis |
C, 63.74; H, 6.29; O, 29.97 |
Nws tau raug rho tawm thawj zaug hauv xyoo 1896 thiab muaj cov haujlwm xws li tshuaj tiv thaiv- qog nqaij hlav, tshuaj tiv thaiv kab mob, tshuaj tiv thaiv kab mob, tiv thaiv psoriasis, thiab tiv thaiv- mob, nrog rau kev ua haujlwm tiv thaiv kab mob tshwj xeeb. Lub bioavailability ntawm mycophenlic acid yog qhov tsawg, thiab tau sim los txhim kho bioavailability thiab tshwj xeeb ntawm MPA los ntawm kev tsim nws cov derivatives. Mycophenolate mofetil (MMF) thiab Mycophenolate sodium (MPS) yog ob qho tseem ceeb derivatives ntawm Jatropha curcas, uas tau ntawv pov thawj los ntawm US FDA nyob rau hauv 1998 thiab 2004. Lawv tsuas yog siv rau kev tiv thaiv thiab kev kho mob ntawm acute rejection tshua nyob rau hauv lub cev hloov. Mycophenolate mofetil yog ib qho derivative ntawm MPA's 2-morpholinoethyl ester (Mycophenlic Acid) ester. MPA yog ib qho kev thim rov qab ntawm xanthine monophosphate dehydrogenase I / II (IMPDH), uas tuaj yeem tsis sib tw khi rau hypoxanthine mononucleotide dehydrogenase, ib qho tseem ceeb enzyme koom nrog de novo synthesis ntawm guanine nucleotides thaum lub sij hawm T thiab B lymphocyte proliferation. MMF tau siv dav hauv kev hloov pauv hauv nruab nrog cev ob qho tib si hauv tebchaws thiab thoob ntiaj teb hauv kev kho mob.
Mycophenolic acidyog bioactive compound uas tuaj yeem siv rau hauv cov tshuaj tom qab esterification. Nws ua lub luag haujlwm tseem ceeb hauv de novo purine synthesis txoj hauv kev uas tsis muaj kev sib tw thim rov qab inhibitor ntawm inosine monophosphate dehydrogenase (IMPDH). Keeb kwm tsim los ua ib qho tshuaj precursor rau mycophenolate mofetil los txhim kho nws qhov ncauj bioavailability. Mycophenolate mofetil, tam sim no feem ntau hu ua Mycophenolate mofetil (MMF), yog ib daim ntawv ester ntawm mycophenolate mofetil thiab tau siv dav hauv kev kho mob.
Daim ntawv thov nyob rau hauv lub tshav pob ntawm lub cev yog ib qho ntawm nws cov tseem ceeb tshaj plaws kev siv. Tom qab kev hloov pauv hauv nruab nrog cev, cov kabmob txawv teb chaws uas tsis yog cov ntaub so ntswg ntawm tib neeg lub cev tuaj yeem ua rau lub cev tsis muaj zog thiab ua rau mob hauv zos, ua rau muaj kev tsis lees paub. Los ntawm inhibiting qhov kev loj hlob thiab kev ua haujlwm ntawm T thiab B hlwb, lub cev tiv thaiv kab mob txo qis, tiv thaiv kev tsis lees paub.
(1) Kev hloov pauv raum: Nws yog ib qho ntawm cov tshuaj nyiam rau kev tiv thaiv kab mob tom qab hloov lub raum. Nws tuaj yeem txo qhov tshwm sim ntawm kev tsis lees paub mob hnyav thiab txhim kho txoj sia nyob ntawm cov raum hloov pauv. Tsis tas li ntawd, nws tseem tuaj yeem siv ua ke nrog lwm cov tshuaj tiv thaiv kab mob txhawm rau txhim kho cov nyhuv immunosuppressive.
(2) Lub plawv, lub ntsws, daim siab thiab lwm yam kev hloov pauv hauv nruab nrog cev: Ntxiv rau kev hloov lub raum, nws kuj tau siv dav rau kev kho mob tom qab kev tiv thaiv kab mob plawv, ntsws, siab thiab lwm yam kabmob. Nws kuj tseem tuaj yeem txo cov kev tsis lees paub thiab txhim kho cov ciaj sia ntawm cov kabmob hloov pauv.Tsis tsuas yog siv tau rau kev tiv thaiv kab mob tom qab hloov khoom nruab nrog cev, tab sis nws kuj tuaj yeem siv los kho ntau yam kab mob autoimmune. Cov kab mob no feem ntau tshwm sim raws li kev mob ntev uas yuav tsum tau siv sijhawm ntev - kho thiab tswj.
Kev siv rau hauv cov kab mob autoimmune
(1) Systemic lupus erythematosus (SLE): Nws yog ib qho tshuaj tseem ceeb hauv kev kho mob SLE. Nws alleviates cov tsos mob ntawm tus kab mob (xws li daim tawv nqaij ua pob ua pob, mob pob qij txha thiab qaug zog) los ntawm kev ua kom lub cev tsis muaj zog thiab txo qis kev tsim cov autoantibodies uas ua rau lub cev puas tsuaj rau cov ntaub so ntswg thiab kab mob. Tsis tas li ntawd, nws tseem tuaj yeem siv ua ke nrog lwm cov tshuaj xws li glucocorticoids los txhim kho cov txiaj ntsig kho mob thiab pab txo cov kev mob tshwm sim los ntawm kev siv sijhawm ntev ntawm -glucocorticoids.
(2) Sjogren's Syndrome: Sjogren's Syndrome yog ib hom kab mob autoimmune mob uas feem ntau cuam tshuam nrog cov qog exocrine, tshwj xeeb tshaj yog cov qog qaub ncaug thiab cov qog lacrimal. Nws tuaj yeem txhim kho cov tsos mob tsis zoo xws li lub qhov ncauj qhuav thiab qhov muag hauv cov neeg mob los ntawm kev tawm tsam qhov txawv txav ntawm lub cev tiv thaiv kab mob ntawm cov qog exocrine thiab txo qis glandular o thiab irreversible puas.
(3) Rheumatoid mob caj dab: Nws kuj tseem siv tau los ua kev kho mob ntxiv rau kev mob caj dab rheumatoid, kab mob autoimmune ntev uas tshwm sim los ntawm kev sib koom ua ke. Nws txhim kho lub neej zoo ntawm cov neeg mob los ntawm tshwj xeeb inhibiting qhov txawv txav ntawm kev loj hlob thiab kev ua haujlwm ntawm T thiab B hlwb, yog li txo qis kev sib koom ua ke, o thiab cov ntaub so ntswg puas, thiab ncua kev loj hlob ntawm kev sib koom tes.
(4) Lwm yam kab mob autoimmune: Ntxiv rau cov kab mob saum toj no, nws kuj tuaj yeem siv los kho ntau yam kab mob autoimmune, xws li pemphigus vulgaris, refractory systemic lupus erythematosus, immunoglobulin A nephropathy, me me vasculitis, thiab psoriasis. Kev kho mob ntawm cov kab mob autoimmune no feem ntau yuav tsum tau siv sijhawm ntev - noj tshuaj tsis tu ncua, thiab kev saib xyuas tus neeg mob qhov kev hloov pauv thiab qhov tshwm sim tsis zoo yog qhov tsim nyog thaum lub sijhawm kho mob los kho cov tshuaj hauv lub sijhawm. Ntxiv rau cov tshuaj tiv thaiv kab mob, nws kuj muaj qhov dav - cov teebmeem xws li tshuaj tua kab mob, tshuaj tua kab mob, tshuaj tua kab mob, thiab tshuaj tua kab mob. Cov yam ntxwv no ua rau nws muaj txiaj ntsig zoo rau kev kho mob ntawm ntau yam kab mob.
Antiviral, antifungal, antibacterial, thiab anticancer teebmeem
(1) Cov nyhuv Antiviral: Nws tuaj yeem cuam tshuam zoo rau kev rov ua dua thiab sib kis ntawm cov kab mob sib kis ntawm ntau yam kab mob, suav nrog tus kab mob herpes, cytomegalovirus thiab lwm yam kab mob sib kis. Qhov tshwj xeeb tshuaj tiv thaiv kab mob no tso cai rau nws los qhia cov peev txheej zoo hauv kev kho mob ntawm cov kab mob sib kis.
(2) Cov nyhuv Antifungal: Nws kuj muaj qee yam cuam tshuam rau qee cov kab mob fungi, thiab tuaj yeem siv los pab kho cov kab mob los ntawm cov kab mob no. Txawm li cas los xij, nws yuav tsum tau muab sau tseg tias nws cov tshuaj tiv thaiv kab mob yog qhov tsis muaj zog, thiab nws feem ntau yuav tsum tau ua ke nrog lwm cov tshuaj tiv thaiv kab mob siab - kom ua tau raws li qhov xav tau kev kho mob.
(3) Cov nyhuv Antibacterial: Nws kuj muaj qee yam cuam tshuam rau qee cov kab mob tshwj xeeb, tab sis nws cov kab mob tua kab mob yog qhov nqaim, thiab nws tsis zoo tiv thaiv kab mob feem ntau. Yog li ntawd, nyob rau hauv kev kho mob ntawm cov kab mob kab mob, nws yog feem ntau yog siv raws li ib tug adjuvant therapy tshuaj pab nyob rau hauv kev txhim kho cov nyhuv kho.
(4) Los tiv thaiv- cov nyhuv mob qog noj ntshav: Hauv xyoo tas los no, cov kev tshawb fawb cuam tshuam tau pom tias nws muaj peev xwm siv tau rau hauv kev kho mob ntawm qee hom qog. Nws ua haujlwm los tiv thaiv- mob qog noj ntshav los ntawm tshwj xeeb inhibiting qhov txawv txav thiab kev ua haujlwm ntawm cov qog hlwb, thiab ua rau apoptosis ntawm cov qog hlwb. Txawm li cas los xij, hais txog nws qhov tshwj xeeb ntawm daim ntawv thov, kev siv ntau npaum li cas thiab cov txiaj ntsig kho mob tiag tiag hauv kev kho mob qog noj ntshav, ntxiv rau hauv - kev tshawb fawb tob thiab kev tshawb fawb soj ntsuam tseem xav tau.
nqus
Bullingham et al. ntseeg hais tias txawm hais tias tsis hais qhov ncauj los yog tso zis, MMF tuaj yeem nqus tau sai thiab dav los ntawm lub cev thiab metabolized tag rau hauv nws cov khoom nquag MPA ua ntej kev ncig. CovMycophenolic Acidkev tswj xyuas lub sij hawm nkhaus ntawm ob txoj kev ntawm kev tswj hwm yog qhov zoo sib xws. Qhov nruab nrab MPA lub sijhawm siab tshaj (tmax) yog li 1 teev. Qhov nruab nrab ib nrab -lub neej (t1/2) ntawm MPA yog li ntawm 17 teev, qhia tau hais tias ob zaug tshuaj txhua hnub yog qhov tsim nyog dua.
Tsis muaj qhov sib txawv tseem ceeb hauv cheeb tsam nyob rau hauv lub sij hawm nkhaus (AUC ∞) ntawm MPA ntawm ob txoj kev tswj hwm, uas yog kwv yees li 105 mg / L.
Metabolize
MPA yog metabolized los ntawm uridine diphosphate glucosyltransferase (UGT) rau inactive mycophenolate glucuronide (MPAG). Lub siab yog lub cev muaj zog tshaj plaws rau UGT thiab qhov chaw tseem ceeb rau MPA metabolism.
Bullingham et al. pom tias nyob rau hauv 1 teev tom qab noj tshuaj, cov ntshav plasma concentration ntawm MPAG qis dua MPA concentration nyob rau tib lub sijhawm, tab sis tom qab ntawd nws tau ntau dua. Qhov nruab nrab MPAGt1/2 zoo ib yam li MPA, thaum tag nrho MPAGAUC yog plaub mus rau tsib npaug siab dua MPA, thiab sib xws, nws qhov nruab nrab plasma clearance tus nqi yog plaub mus rau tsib npaug qis dua MPA.
Muab piv rau cov theem pib ntawm MPAG thiab MPA cov duab, ob qho tib si muaj cov duab zoo sib xws, tab sis qhov qub tau qeeb thiab nthuav dav piv rau yav dhau los.
Nyob rau hauv lub lig 1990s, Shipkova et al. cais ob lwm cov metabolites ntawm MPA los ntawm cov ntshav ntawm cov neeg tau txais kev hloov pauv: mycophenlic acid acyl gluconic acid (AcMPAG) thiab mycophenlic acid phenyl gluconic acid (MPAG1s). MPAG1s tsis muaj kev cuam tshuam rau IMPDH thiab tsis koom nrog hauv kev tiv thaiv kab mob; Kev sim hauv vitro tau pom tias AcMPAG tuaj yeem cuam tshuam tib neeg hom II IMPDH (rh IMPDH-II) thiab inhibit lymphocyte proliferation (3,4). Ntawm qhov tod tes, AcMPAG tuaj yeem khi rau cov plasma proteins thiab lwm yam macromolecules, uas yog suav tias yog lawv lub cev tiv thaiv kab mob thiab tshuaj lom.
Enterohepatic ncig
Multidrug resistance txuam nrog protein 2 (MRP2) yog qhia nyob rau saum npoo ntawm daim siab hlwb, thiab nws txoj hauj lwm yog kom tshem tawm endogenous conjugates thiab tshuaj metabolites rau hauv cov kua tsib. Kobayashi et al. paub tseeb tias cov kua tsib excretion ntawm MPAG cia siab rau MRP2 kom tiav. Dawb MPA (fMPA) kuj yog ib qho substrate rau MRP2, tab sis nws zoo nkaus li tias MRP2 nyiam MPAG tshaj MPA.Thaum cov kua tsib nkag mus rau hauv cov hnyuv, MPAG tau degraded rau hauv MPA raws li kev ua ntawm cov kab mob thiab reabsorbed rau hauv cov kab mob.
Cov txheej txheem no hu ua enterohepatic circulation (EHC) ntawm MPA, uas qhia tau hais tias lub ncov thib ob (me dua thawj lub ncov) tshwm sim 6-12 teev tom qab kev tswj hwm ntawm lub sijhawm tshuaj. Nws tau raug lees paub tias EHC tuaj yeem nce MPA-AUC los ntawm qhov nruab nrab ntawm 37%. Cov yam ntxwv uas cuam tshuam rau cov kua tsib thiab tso tawm hauv lub cev, xws li colitis, raws plab, thiab tshuaj tua kab mob, tuaj yeem hloov cov plab hnyuv ua haujlwm thiab / lossis cov plab hnyuv microbiota, tag nrho cov no yuav ua rau muaj kev hloov pauv loj hauv vivo metabolism ntawm MMF.
Tshem tawm
MPAG yog secreted thiab tawm mus rau hauv cov zis los ntawm lub raum tubules. Kev tswj hwm qhov ncauj ntawm radiolabeled MMF tuaj yeem rov ua tiav cov tshuaj noj, nrog 93% tshwm sim hauv cov zis thiab 6% hauv cov quav. Feem ntau ntawm nws raug tso tawm hauv cov zis hauv daim ntawv ntawm MPAG, thiab cov khoom me me tau tawm hauv cov zis hauv daim ntawv ntawm MPA.
Shaw et al. ntseeg tias peb yam tswj hwm MPA tshem tawm tus nqi: (1) UGT hauv daim siab thiab plab hnyuv; (2) MPA-EHC; (3) MPA dissociation degree. Cov yam ntxwv uas tuaj yeem ua rau muaj kev hloov pauv tseem ceeb hauv MPA tshem tawm tus nqi lossis muaj feem cuam tshuam nrog nws muaj xws li mob raum lossis mob raum tsis txaus, cov tshuaj tiv thaiv kab mob sib xyaw xws li CsA thiab corticosteroids, thiab lub sijhawm tom qab hloov pauv. Lwm qhov ua tau yog qhov sib txawv ntawm haiv neeg.
Dawb MPA
Kev khi tus nqi ntawmMycophenolic Acidrau albumin yog kwv yees li 97%, thiab cov neeg mob hloov pauv ruaj khov 'fMPA tso nyiaj rau 1-3% ntawm tag nrho MPA. Qhov inhibition ntawm IMPDH thiab inhibition ntawm mitogen stimulated lymphocyte proliferation nyob ntawm qhov concentration ntawm fMPA. Cov yam ntxwv ntawm kev khi rau albumin thiab cov neeg mob yam tuaj yeem hloov pauv fMPA thiab fMPA AUC.
Shaw et al. ntseeg tias kev ntsuas cov MPA dawb thiab tag nrho MPA concentration tuaj yeem pab ntsuas MPA raug, thiab cov hauv qab no tuaj yeem txo qhov kev sib txuas ntawm MPA rau albumin: (1) cov neeg mob uas lub raum tsis ua haujlwm ntxov tom qab hloov lub raum; (2) Cov neeg mob uas lub raum tsis ua haujlwm ntev; (3) Cov neeg mob thaum ntxov postoperative tom qab hloov daim siab; (4) Cov neeg mob uas tsis tshua muaj albumin thiab/lossis siab bilirubin.Nyob rau hauv kev tshawb fawb ntawm kev hloov hauv lub raum, nws tau pom tias fMPA AUC yog ib qho tseem ceeb ua rau MMF muaj feem cuam tshuam, nrog rau kev pheej hmoo ntawm leukopenia lossis kab mob thaum koob tshuaj ntau dua 0.4 mg / L.
Mechanism ntawm kev ua:
MPA (mycophenolate mofetil los yog nws cov nquag metabolite mycophenolate mofetil), ua tau zoo heev, xaiv, thim rov qab, thiab tsis muaj kev sib tw inhibitor ntawm inosine dehydrogenase (IMPDH), tau qhia dav dav hauv kev ua liaj ua teb thiab tshuaj. IMPDH yog ib qho tseem ceeb enzyme nyob rau hauv de novo synthesis txoj kev ntawm purine nucleotides, lub luag hauj lwm rau catalyzing hloov ntawm xanthine monophosphate (IMP) rau xanthine monophosphate (GMP) los yog adenosine monophosphate (AMP), uas yog ib qho tseem ceeb kauj ruam nyob rau hauv lub synthesis ntawm guanine adenineotides thiab nucleotides. MPA ua haujlwm zoo thaiv txoj kev sib xyaw ua ke ntawm IMPDH tshwj xeeb los ntawm inhibiting nws, ua rau txo qis ntawm guanine nucleotides (xws li GTP) thiab adenine nucleotides (xws li ATP) hauv lub cell.
Kev loj hlob ntawm T thiab B lymphocytes yog nyob ntawm de novo synthesis ntawm purine nucleotides, thiab MPA cuam tshuam qhov kev loj hlob ntawm cov hlwb los ntawm inhibiting cov txheej txheem no. Nws yog ib qho tsim nyog sau cia tias lwm hom hlwb, xws li macrophages lossis fibroblasts, feem ntau tuaj yeem tso siab rau txoj hauv kev khaws cia (xws li siv exogenous purine nucleotides lossis hauv paus) los tsim cov purines uas yuav tsum tau ua, thiab yog li ntawd tsis tshua cuam tshuam los ntawm MPA. Qhov kev xaiv inhibitory no ua rau MPA cov cuab yeej kho tau zoo rau kev tswj hwm lub cev tiv thaiv kab mob, tshwj xeeb tshaj yog tiv thaiv kab mob autoimmune thiab kev hloov pauv tsis lees paub. Los ntawm thaiv txoj kev de novo synthesis ntawm DNA hauv T thiab B lymphocytes, MPA ua rau muaj zog tiv thaiv kab mob.
MPA (los yog MMF, tseem hu ua mycophenolate mofetil, cov tshuaj ua ntej ntawm MPA) nthuav tawm ntau yam kev ua ub no uas tsis yog tshuaj tiv thaiv kab mob. Nws tuaj yeem cuam tshuam kev loj hlob ntawm cov hlwb mesangial thiab cov leeg nqaij du, uas ua lub luag haujlwm tseem ceeb hauv ntau yam txheej txheem pathological, xws li glomerulonephritis, atherosclerosis, thiab lwm yam. Los ntawm inhibiting qhov kev loj hlob ntawm cov hlwb, MPA yuav pab txo qis kev loj hlob ntawm tus kab mob. Nyob rau tib lub sijhawm, MPA tseem tuaj yeem cuam tshuam kev loj hlob ntawm vascular endothelial hlwb, uas yog cov kauj ruam tseem ceeb hauv kev kho cov hlab ntsha tom qab raug mob thiab tsim cov atherosclerosis, yog li pab tswj cov qauv thiab kev ua haujlwm ntawm cov hlab ntsha.
MPA tawm dag zog los tiv thaiv- cov teebmeem inflammatory los ntawm inhibiting cov kev ua ntawm adhesion molecules xws li selectins, integrins, thiab cov tswv cuab ntawm cov immunoglobulin superfamily, txo cov kev sib cuam tshuam ntawm cov hlwb inflammatory thiab endothelial hlwb, txo cov neeg nrhiav neeg thiab infiltration ntawm inflammatory cells. Cov tshuaj tiv thaiv no yog qhov tseem ceeb rau kev kho mob ntawm ntau yam kab mob, xws li glomerulonephritis thiab autoimmune kab mob siab. Tsis tas li ntawd, los ntawm kev txo qis kev tsim cov kab mob thiab fibrosis ntsig txog yam,Mycophenolic Acidtuaj yeem cuam tshuam cov txheej txheem ntawm cov ntaub so ntswg fibrosis, tiv thaiv lub cev ua haujlwm, thiab txhim kho lub neej zoo ntawm cov neeg mob.
Mycophenolic acid (MPA) yog ib yam khoom ntuj tsim nrog cov tshuaj tseem ceeb, pib cais tawm ntawm cov fungi. Raws li cov tshuaj tiv thaiv kab mob, nws yog dav siv hauv kev kho mob tsis lees paub tom qab hloov pauv hauv nruab nrog cev, thiab tseem muaj ntau yam kev ua ub no xws li tshuaj tiv thaiv kab mob, tiv thaiv- qog, thiab tiv thaiv - cov teebmeem. Qhov kev tshawb pom ntawm MPA tuaj yeem taug qab rov qab mus rau lub xyoo pua puv 19, thaum cov kws tshawb fawb pib kawm cov metabolites ntawm fungi. Xyoo 1893, tus kws tshawb fawb Italian Bartolomeo Gosio thawj zaug cais cov tshuaj nrog tshuaj tua kab mob los ntawm kab lis kev cai nruab nrab ntawm Penicillium fungi thaum kawm nws.
Gosio tshawb pom tias cov khoom no tuaj yeem cuam tshuam qhov kev loj hlob ntawm Bacillus anthracis, tab sis vim muaj kev txwv hauv kev tshuaj ntsuam xyuas thaum lub sijhawm, nws tsis tuaj yeem txheeb xyuas nws cov qauv tshuaj. Cov tshuaj no tom qab tau lees paub tias yog MPA, tab sis vim Gosio txoj kev tshawb fawb tsis tau nthuav dav, cov neeg tshawb nrhiav tseeb ntawm MPA feem ntau suav tias yog cov kws tshawb fawb tom qab. Thaum pib ntawm lub xyoo pua 20th, nrog rau kev loj hlob ntawm microbiology thiab organic chemistry, cov kws tshawb fawb tau pib kawm cov kab mob fungal metabolites.
Xyoo 1913, Asmeskas cov kws tshawb fawb Alsberg thiab Dub tau cais cov tshuaj acidic los ntawm kab lis kev cai nruab nrab ntawm Penicillium stolonifera thiab hu ua "mycophenolic acid", uas txhais tau tias "phenolic acid tsim los ntawm fungi". Lawv tau piav qhia ua ntej nws cov tshuaj tua kab mob, tab sis lawv cov qauv meej tseem tsis tau txiav txim siab. Kev txheeb xyuas cov qauv tshuaj ntawm MPA tau dhau los ntawm cov txheej txheem ntev. Nyob rau xyoo 1940 thiab 1950, nrog rau kev txhim kho ntawm cov tshuab chromatographic thiab spectroscopic tsom xam (xws li ultraviolet, infrared, thiab nuclear magnetic resonance), cov kws tshawb fawb tuaj yeem txheeb xyuas cov qauv ntawm cov khoom ntuj tsim.
Xyoo 1945, British chemist Raistrick thiab nws pab neeg tau tshawb fawb ntxiv ntawm MPA thiab tau npaj qee yam ntawm nws cov qauv. Xyoo 1952, Birch thiab Donovan thaum kawg txiav txim siab ua tiav cov qauv ntawm MPA los ntawm kev sim tshuaj degradation thiab synthesis. MPA yog ib qho phenolic compound nrog cov pob txha benzopyran tshwj xeeb thiab ib qho enol ether sab saw (Daim duab 1). Qhov kev tshawb pom no tau tsim lub hauv paus rau kev hloov kho tshuaj lom neeg thiab kev tsim tshuaj.
Tom qab cov qauv ntawm MPA tau txiav txim siab, cov kws tshawb fawb tau pib kawm txog nws txoj haujlwm lom neeg. Cov kev tshawb fawb thaum ntxov pom tias MPA muaj cov tshuaj tua kab mob thiab tshuaj tua kab mob, tab sis nws cov tshuaj tua kab mob yog nqaim, txwv tsis pub nws daim ntawv thov hauv kev kho cov kab mob sib kis. Txawm li cas los xij, xyoo 1969, cov kws tshawb fawb pom tias MPA tuaj yeem cuam tshuam cov lymphocyte proliferation, qhia tias nws yuav muaj kev tiv thaiv kab mob. Nyob rau xyoo 1970, cov kws tshawb fawb tau piav qhia ntxiv txog kev ua haujlwm ntawm MPA.
Xyoo 1977, Allison thiab cov npoj yaig tau tshawb pom tias MPA yog ib qho kev xaiv inhibitor ntawm inosine monophosphate dehydrogenase (IMPDH). IMPDH yog ib qho enzyme tseem ceeb hauv guanine nucleotide synthesis, thiab kev loj hlob ntawm T thiab B lymphocytes yog nyob ntawm txoj kev no. Yog li, MPA tuaj yeem xaiv cov lymphocytes, txo cov tshuaj tiv thaiv kab mob, thiab muaj kev cuam tshuam me ntsis rau lwm cov hlwb. Qhov kev tshawb pom no muab lub hauv paus theoretical rau kev kho mob ntawm MPA ua ib qho tshuaj tiv thaiv kab mob.
Mycophenolic acid sawv cev rau kev hloov pauv hauv kev tiv thaiv kev tiv thaiv kab mob, sib txuas cov phiaj xwm kev ua haujlwm nrog ntau yam kev siv tshuaj kho mob. Kev tshawb fawb tsis tu ncua txuas ntxiv nthuav dav nws txoj kev kho mob pem hauv ntej thaum hais txog cov kev txwv los ntawm kev tsim kho tshiab thiab cov tswv yim txhaj tshuaj precision. Raws li kev nkag siab ntawm MPA's multi-faceted pharmacology tob zuj zus, qhov sib xyaw no tau npaj kom nyob twj ywm tseem ceeb hauv kev hloov pauv thiab tshuaj autoimmune rau ntau xyoo tom ntej.
FAQ
Dab tsi yog mycophenolic acid siv rau?
+
-
Mycophenolic acid (Myfortic) thiab nws cov derivative, mycophenolate mofetil (CellCept), yog cov tshuaj tiv thaiv kab mob feem ntau siv los tiv thaiv kev tsis lees paub hauv lub raum, lub plawv, thiab lub siab hloov cov neeg mob. Lawv kuj raug siv tawm ntawm - daim ntawv lo los kho cov kab mob autoimmune xws li lupus, rheumatoid mob caj dab, vasculitis, thiab psoriasis.
Puas yog mycophenolic acid ua rau qhov hnyav nce?
+
-
Feem ntau cov kev mob tshwm sim ntawm mycophenolate yog raws plab, mob, ntuav, ntshav siab, thiab o ntawm ob txhais ceg, ko taw, thiab pob taws. Lwm cov kev mob tshwm sim muaj xws li: qhov hnyav nce lossis poob. Teeb meem pw tsaug zog lossis pw tsaug zog.
Dab tsi yog qhov txawv ntawm mycophenolate thiab mycophenolic acid?
+
-
Mycophenolate mofetil (CellCept) thiab mycophenolic acid (Myfortic) yog ob qho tib si tshuaj tiv thaiv kab mob siv los tiv thaiv lub cev tsis zoo los ntawm inhibiting T- thiab B-lymphocyte proliferation. MMF yog ib qho tshuaj uas hloov mus rau MPA nquag, thaum Myfortic yog enteric-coated los txo cov kev mob tshwm sim ntawm plab hnyuv. Thaum 1g ntawm MMF yog kwv yees li 720mg ntawm Myfortic, lawv tsis tuaj yeem hloov pauv ncaj qha.
Dab tsi yog cov kev mob tshwm sim ntawm mycophenolic acid?
+
-
Feem ntau cov kev mob tshwm sim ntawm mycophenolic acid (Myfortic) suav nrog cov teeb meem hauv plab hnyuv xws li zawv plab, ntuav, xeev siab, mob plab, thiab cem quav, nrog rau kev kis kab mob (vim kev tiv thaiv kab mob), cov ntshav suav hloov ( ntshav ntshav, leukopenia), qaug zog, mob taub hau, thiab insomnia. Nws yog ib qho tseem ceeb uas yuav tau saib xyuas cov kev mob tshwm sim loj xws li kev kis kab mob, raws plab, lossis kab mob ntawm daim tawv nqaij tshiab. RxList +4
Cim npe nrov: mycophenolic acid CAS 24280-93-1, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom