Tsis zoo siv: Tus paagulin, tseem hu ua Pleuromutilin, yog cov tshuaj tiv thaiv diterpene diterpene tau txais los ntawm cov fungusPleurotus mutilusCov. Qhov no ua ke thiab nws cov derivatives pom cov kab mob antibacterial muaj ntau yam ntawm cov kab mob gram-zoo, mypsplasmas, thiab qee cov kab mob gram-tsis zoo. Cov ntawv no tshawb txog cov me nyuam antimicrobial ntawm cov pauromulinism ntawm cov qib siab thiab kev tsim kho cov cim tseem ceeb thiab nce qib hauv nws cov synthesis thiab application.
Khoom Code: BM -2-5-121
Lus Askiv Lub Npe: Pleuromulin
CAS TSIS MUAJ.: 125-65-5
Molecular Cov Qauv: C22H34O5
Molecular hnyav: 378.5
Eineecs tsis muaj.: 204-747-5
MDL No.:MFCD28154633
Analysis items: HPLC>99. {{0%, lc-ms
Kev Lag Luam Tseem Ceeb: Tebchaws Asmeskas, Australia, Nyij Pooj, Tebchaws Yelemees, Indonesia, UK, New Zealand, Canada thiab lwm yam.
Chaw tsim tshuaj paus: BLOOM Tech Changzhou Hoobkas
Kev Pab Technology: R & Dept. {-4
Peb muab cov Pleuromulin Cas 125-65-5, Thov saib mus rau lub vev xaib hauv qab no kom cov ncauj lus kom ntxaws thiab cov ntaub ntawv cov ntaub ntawv.
Lo lus tseem ceeb: Pleuromulin; antimicrobial meincial mechanism; keeb kwm txhim kho; Gram-zoo cov kab mob; Pleurotus mutilus
Lub hauv paus rau phau ntawv
Cov tshuaj tua kab mob tau ua lub pob kws ntawm cov khoom siv niaj hnub, ua kom cov kab mob zoo ntawm cov kab mob. Txawm li cas los xij, nce ntawm cov tshuaj tua kab mob tiv thaiv ua rau muaj kev hem thawj tseem ceeb rau kev noj qab haus huv ntiaj teb. Qhov kev tshawb pom thiab kev txhim kho cov tshuaj tua kab tshiab nrog cov kev sib cav tswv yim ntawm kev ua yog qhov tseem ceeb los tiv thaiv qhov kev sib tw no.Tus paagulin, cov tshuaj tua kab mob diterpene, sawv cev rau ib qho kev sib tw zoo li no. Cov lus no rho tawm mus rau hauv antimicrobial mechanism ntawm aluromulinism thiab nws keeb kwm kev loj hlob, ua rau lub peev xwm los ua lub peev xwm kho yav tom ntej.
Antimicrobial mechanism ntawm pleuromulin
Pleuromulin belongs rau cov Pleuromutilin chav kawm ntawm cov tshuaj tua kab mob, uas yog tus cwj pwm los ntawm lawv cov qauv tshuaj tshwj xeeb thiab hom kev ua. Cov antimicrobial kev ua si ntawm pleuromulin yog feem ntau yog vim nws muaj peev xwm cuam tshuam cov kab mob proteter proteisis, cov txheej txheem tseem ceeb rau cov kab mob muaj sia nyob thiab rov ua dua.
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Inhibition ntawm peptidyl hloov
Pleuromulin ntau zog nws cov nyhuv antibacterial los ntawm kev sib tw Peptidyl kev hloov chaw (PTC) ntawm cov kab mob khaub racosome. Tus ribosome yog ib lub tshuab molecular uas muaj lub luag hauj lwm rau protein synthesis hauv txhua lub cev. Lub PTC yog qhov tseem ceeb heev ntawm cov ribosome, catalying qhov tsim ntawm peptide bonds ntawm amino acids thaum lub sij hawm protein elongation.
Pleuromulin khi rau PTC thiab inhibits nws cov haujlwm, yog li tiv thaiv kev tsim cov peptide butters thiab tso cov protein synthesis. Qhov kev siv tshuab ntawm kev nqis tes ua no yog qhov sib txawv ntawm qhov ntawm lwm cov tshuaj tua kab mob, xws li cov kab mob cora-lactams thiab macrolides, uas lub hom phiaj sib txawv, uas yog cov khoom siv protein, ntsig txog. Qhov tshwj xeeb khi cov duab ntawm Pleuromulin ntawm Ribosome ua rau nws tsis tshua muaj cov chav kawm ua rau muaj kev kho mob rau cov kab mob multidrug-resistant.
Dav-spectrum kev ua ub no
Pleuromulin ua yeeb yam dav-spectrum cov tshuaj tua kab mob antibacterial, ua tau zoo nyob rau cov kab mob gram-zoo, suav nrog Methicillin-resistantStaphylococcus aureus(MRSA),Streptococcus priceaie, thiabEnterococcus faecalisCov. Nws tseem qhia txog kev ua si rau myCoopsmas thiab qee cov kab mob gram-tsis zoo, txawm hais tias nws txoj kev ua tau zoo tiv thaiv tom kawg feem ntau qis dua.
Cov kev ua dav dav ntawm Pleuromulin tuaj yeem raug rau kev txuag ntawm Ribosomal PTC hla cov kab mob sib txawv. Los ntawm kev sib tw muaj kev txuag thiab tseem ceeb ntawm cov kab ke ntawm cov kab ke ntawm cov kab ke ntawm cov kab mob antimicrobial thoob plaws ntawm cov kab mob.
Kev Tawm Tsam
Txawm hais tias nws cov cim tshwj xeeb ntawm kev txiav txim, tsis kam ntawm pawg neeg tau pom nyob hauv qee cov kab mob. Kev tawm tsam tuaj yeem tshwm sim los ntawm kev hloov pauv ntawm cov kev sib hloov pauv ntawm cov chaw muaj protein lossis RRNA, uas hloov lub tsev kawm ntawv khi thiab txo nws ib qho kev sib txawv rau PTC. Tsis tas li ntawd, EFFLUX twj, uas yog kev thauj khoom-ua rau thauj cov tshuaj uas nthuav tawm ntawm lub cell, tuaj yeem pab txhawb rau Pleuromulin tsis kam.
Txawm li cas los xij, tus nqi ntawm kev tiv thaiv kev loj hlob rau cov pauromulin zoo li tsis tshua muaj qhov piv rau lwm cov chav tua kab mob. Qhov no tuaj yeem yog vim muaj kev nyab xeeb tus nqi cuam tshuam nrog kev sib pauv uas contfer tsis kam rau kev sib hloov, raws li cov kev hloov pauv no feem ntau cuam tshuam qhov tseem ceeb rau kev sib tw.
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Kev loj hlob keeb kwm ntawm Pleuromulin
Kev txhim kho keeb kwm ntawm Pleuromulin Spans ntau xyoo caum, cim los ntawm qhov kev nce qib tseem ceeb hauv nws cov kev sib cais, hluavtaws, thiab cov ntaub ntawv thov.
Pleuromulin tau raug cais thawj zaug hauv xyoo 1950 los ntawm fungusPleurotus mutilus, ib hom tsiaj ntawm Basidiomycete pom nyob hauv av thiab hais tias poob ntoo. Qhov sib xyaw ua ke tau pib txheeb raws li tus metabolite theem nrab nrog cov kev ua tau zoo. Nws cov qauv tshuaj lom neeg tshwj xeeb, cov cim los ntawm Trricyclic diterpene skeleton nrog yim chair charet, nyiam cov kev txaus siab los ntawm cov kws tshawb fawb.
Kev rho tawm ntawm cov pauromulin los ntawm cov chaw ua pov thawj ua pov thawj tias yog qhov nyuaj vim nws cov kev nplua nuj ntau hauv cov fungus. Txawm li cas los xij, kev kho siab nyob rau hauv fermentation cov tswv yim thiab cov txheej txheem ua kom huv siv tau tsim cov loj-teev ntau lawm ntawm cov pleuromulin rau kev tshawb fawb ntxiv.
Cov qauv nyuaj ntawm cov pauromulin posed cov nyom nyuaj rau nws cov tshuaj synthesis. Kev sim thaum ntxov ntawm cov synthesis tau ntsib nrog kev ua tiav tsawg, feem ntau vim muaj kev tswj hwm ntawm cov chaw khaws nyiaj ntau chairal. Txawm li cas los xij, ntau pawg neeg tshawb fawb tau tsim cov kev ua hluavtaws muaj txiaj ntsig zoo rau cov pauromulin thiab nws cov derivatives.
Ib qho tseem ceeb tshaj plaws hauv kev siv cuam tshuam nrog kev siv cov khoom siv hluav taws xob modular, uas cov complex molecule tau tsim los ntawm cov yooj yim dua, ua ntej tsim cov khoom lag luam. Lub tswv yim no tau qhib cov synthesis ntawm ntau ntau ntawm cov pauromulin analogs nrog cov qib kev ua haujlwm ntawm cov tshuaj tua kabmob thiab cov khoom siv pharmacological.
Kev txhim kho ntawm catalytic asymmetric synthesis tseem ua si tseem ceeb lub luag haujlwm nyob rau hauv synthesis ntawm pleuromulin. Cov hau kev no tso cai rau kev xaiv xaiv ntawm chairal chaw, ua kom cov khoom siv ntshiab kom huv. Qhov no yog tshwj xeeb yog qhov tshwj xeeb tshaj yog rau kev ua si, raws li nws cov kev ua haujlwm muaj roj ntsha tau nce siab ntawm nws cov kev sib tw.
Cov kev txhim kho kev txhim kho ntawm cov pauromulin tau tsom mus rau nws cov derivatives, tsis yog niam txiv qhov sib xyaw nws tus kheej. Qhov no yog vim cov khoom siv tsis zoo ntawm cov pauromulin, suav nrog qhov ncauj qis dua thiab cov metabolism sai sai.
Ib qho ntawm cov txiaj ntsig zoo tshaj plaws ntawm Pleuromulin yog Retapamulin pom zoo rau kev kho mob ntawm impetigo thiab lwm yam kab mob ntawm daim tawv nqaij. Retapamulin yog c {1}} recified analog ntawm pleuromulin, tsim los txhim kho nws cov kev ua haujlwm tua kab mob.
Lwm cov derivatives ntawm pleuromulin, xws li Valnemulin thiab Tiamulin, tau tsim rau kev siv tsiaj txhu. Cov tebchaw no tau siv los kho kev ua pa thiab cov kab mob plab zom mov hauv npua thiab nqaij qaib, feem. Lawv txoj kev ua tau zoo thiab kev nyab xeeb hauv cov tsiaj tau coj mus rau lawv qhov kev siv thoob plaws hauv kev lag luam kws kho tsiaj.
Txawm hais tias muaj kev ua tiav hauv kev txhim kho Pleuromulin derivatives, Kev tshawb nrhiav txuas ntxiv txuas ntxiv mus tshawb cov khoom tshiab nrog cov khoom uas tau txhim kho tshiab. Cov kws tshawb nrhiav tau zoo tshaj rau kev tsim cov kab sib txuas nrog cov kab mob ua kom zoo nkauj, nrog rau cov uas tau txhim kho cov chaw muag tshuaj cov ntaub ntawv siv.
Tsis tas li ntawd, tus cim tshwj xeeb ntawm kev ua ntawm pleuromulin tau ua rau muaj kev txaus siab rau nws cov peev xwm ua cov tshuaj txhuas uas nyiam ua haujlwm. Los ntawm kev nkag siab cov kev sib txuas lus molecular ntawm cov pob zeb thiab cov kws tshaj lij kev sib txuas lus, kev cia siab cia siab rau cov chaw tshiab tab sis nrog kev xaiv tau ntau lub potency thiab xaiv tau.
Tag
Pleuromulin, ib qho tshuaj tua kab mob diterpene tau txais los ntawm cov fungusPleurotus mutilus, sawv cev rau cov neeg sib tw cog lus rau kev kho mob ntawm kab mob. Nws cov txheej txheem tshwj xeeb ntawm kev nqis tes ua, kev sib tw Peptidyl hloov chaw ntawm cov kab mob ribosome, cov chav tua kab mob thiab txo qis kev pheej hmoo ntawm tus ntoo khaub lig-resistance.
Kev txhim kho keeb kwm ntawm Pleuromulin tau cim los ntawm qhov kev nce qib tseem ceeb hauv nws cov kev sib cais, hluavtaws, thiab cov ntaub ntawv thov. Thaum tus niam txiv compound muaj cov khoom siv tshuaj tsawg tsawg, nws cov derivatives tau qhia cov lus cog tseg hauv tib neeg thiab cov nkauj kho tsiaj.
Kev tshawb fawb txuas ntxiv txuas ntxiv mus tshawb cov phab ntsa tshiab ntawm cov pauromulin nrog kev txhim kho cov khoom, ua rau nthuav dav nws cov kev kho mob. Lub cim kev tshwj xeeb thiab hom kev ua ntawm pleuromulin ua rau nws lub hom phiaj ntxim nyiam rau kev txhim kho cov tshuaj tua kab mob uas nyiam ua rau tshuaj tiv thaiv kab mob.
Raws li cov thoob ntiaj teb kev noj qab haus huv cov pob qij txha tsis zoo nrog kev tiv thaiv kev tiv thaiv, kev tshawb pom thiab kev nthuav dav ntawm cov kev ua haujlwm tshiab ntawm kev ua yog qhov tseem ceeb. Pleuromulin thiab nws cov derivatives sawv cev rau ib txoj kev ntawm kev tshawb fawb no, muab kev cia siab rau lub neej tom ntej ntawm cov tshuaj kho yav tom ntej.