Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm pleuromulin cas 125-65-5 hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo pleuromulin cas 125-65-5 muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Pleuromulinyog ib qho tshwj xeeb tricyclic diterpene tshuaj tua kab mob uas tau pib cais tawm ntawm cov kab mob siab dua (xws li Pleurotus mutilus, tam sim no hu ua Clitopilus passeckerianus) hauv xyoo 1950. Nws cov txheej txheem tshuaj tua kab mob yog qhov tshwj xeeb, los ntawm kev khi nrog kev sib raug zoo siab rau peptidyl transferase chaw nruab nrab ntawm 50S subunit ntawm cov kab mob ribosomes (sib koom qee qhov chaw sib tshooj nrog lincomycin thiab truncated cephalosporin), ncaj qha inhibiting kev tsim ntawm peptide bonds thaum lub sij hawm protein synthesis, tab sis muaj me ntsis cuam tshuam nrog cov mites ntawm cov protein ntau. xaiv xaiv.
|
Tshuaj Formula |
C22H34O5 |
|
Exact Mass |
378 |
|
Molecular Luj |
379 |
|
m/z |
378 (100.0%), 379 (23.8%), 380 (2.7%), 380 (1.0%) |
|
Elemental Analysis |
C, 69.81; H, 9.05; O, 21.13 |
Txoj kev loj hlob ntawm cov tshuaj no thiab nws cov series ntawm semi-synthetic derivatives (xws li lefamulin) feem ntau yog tsom rau cov teeb meem loj zuj zus ntawm cov tshuaj tua kab mob hauv Gram- cov kab mob zoo, tshwj xeeb tshaj yog qhia muaj zog tiv thaiv ntau- tshuaj- tiv taus Streptococcus pneumoniae, Staphylococcus a MR (Staphylococcus arrhythmia). faecalis, thiab tuaj yeem nkag mus rau biofilms zoo. Vim nws lub hom phiaj tshiab thiab qhov nyuaj ntawm kev hla- tawm tsam nrog lwm cov tshuaj tua kab mob, nws suav tias yog ib qho tshuaj tshwj xeeb rau kev tawm tsam cov tshuaj tua kab mob- tiv thaiv kab mob hauv cov kws kho tsiaj thiab tib neeg cov tshuaj (tshwj xeeb tshaj yog rau kev kho mob hauv zos xws li kab mob ntawm daim tawv nqaij), thiab nws cov qauv kev sib tw thiab cov kev sib tw hluavtaws txuas ntxiv mus rau hauv{7} cov tshuaj organic.
Pleuromulin yog ib chav kawm ntawm cov tshuaj tua kab mob uas muaj zog ua ntej raug rho tawm los ntawm cov nceb noj Clitophilus scyphoides hauv xyoo 1951, nrog rau cov txheej txheem tshwj xeeb ntawm inhibiting kab mob protein synthesis los ntawm kev khi rau 50S ribosomal subunit, yog li tsis txhob hla -ua hauj lwm nrog rau lwm yam tshuaj tua kab mob loj. Nws cov ntawv thov tau muab faib ua cov tshuaj kho tsiaj thiab tib neeg cov tshuaj, nrog cov khoom siv hluavtaws ua lub luag haujlwm tseem ceeb hauv ob qho tib si. Hauv cov kws kho tsiaj, nws tau siv dav los kho cov kab mob kab mob hauv cov zaub mov- tsim cov tsiaj, tshwj xeeb tshaj yog npua thiab nqaij qaib.
Derivatives zoo li tiamulin thiab valnemulin muaj txiaj ntsig zoo tiv thaiv swine dysentery, porcine proliferative enteropathy, thiab enzootic pneumonia, nrog rau cov kab mob Mycoplasma hauv cov nqaij qaib thiab epizootic luav enteropathy, nrog rau cov koob tshuaj tshwj xeeb kho rau cov tsiaj sib txawv thiab kev tswj hwm kev noj haus, dej haus, thiab kev txhaj tshuaj intramuscular. Hauv tib neeg cov tshuaj, kev tsim cov derivatives tau nthuav dav nws daim ntawv thov: retapamulin yog siv tshuaj pleev xim rau cov kab mob ntawm daim tawv nqaij, thaum lefamulin, pom zoo los ntawm FDA hauv 2019, yog thawj cov kab mob pleuromutilin rau kev kho cov zej zog - kis tau cov kab mob ntsws thiab kab mob ntawm daim tawv nqaij mob. Tshwj xeeb tshaj yog, Pleuromulin muaj qhov hloov pauv tsis tshua muaj tshwm sim thiab kev txhim kho tsis zoo, ua rau nws muaj txiaj ntsig hauv kev sib ntaus sib tua tshuaj - cov kab mob tiv thaiv, txawm hais tias nws siv yuav tsum tau saib xyuas kom zoo los tiv thaiv qhov tshwm sim tshwm sim.
Pleurotus truncatus thiab nws cov derivatives tuaj yeem cuam tshuam cov synthesis ntawm cov kab mob proteins ntawm qib ribosome, thiab muaj kev cuam tshuam tshwj xeeb rau ntau Gram - cov kab mob zoo thiab kab mob mycoplasma.
Xyoo 1951, Kavanagh et al. Ua ntej tshaj tawm cov kev sib cais thiab cov yam ntxwv ntawm crystalline antibacterial tshuaj ntawm truncated pleuridin.
Xyoo 1974, Sandoz lub koom haum tau pom ib qho derivative ntawm tylosin, uas yog 10-100 lub sij hawm siab dua li ntawm Pleurotus truncated. Cov tshuaj no hloov C-14 hydroxyl ntawm truncated Pleurotus nrog (diethylaminoethyl) sulfhydryl. Ntxiv nrog rau cov tshuaj tua kab mob ntawm truncated Pleurotus, nws qhia tau hais tias muaj zog tiv thaiv kab mob tiv thaiv Shigella, Klebsiella thiab Escherichia coli, thiab yog ib qho ntawm cov tshuaj tua kab mob uas nquag siv nyob rau hauv khw muag tshuaj veterinary tam sim no, Nws tsuas yog kho cov kab mob hauv plab thiab ua pa ntawm cov tsiaj nyeg thiab cov nqaij qaib.
Xyoo 1976, Knausederf et al. Ua tiav txoj kev tshawb fawb ua ntej ntawm fermentation tej yam kev mob, tshuaj qauv thiab biosynthetic txoj kev ntawm truncated pleurotin ua cov kab mob. Valnemulin, uas tau tsim tawm tom qab, kuj tseem siv los ua tsiaj tshwj xeeb tshuaj tua kab mob los kho cov kab mob ua pa hauv npua thiab qaib thiab kab mob enteritis hauv luav. Valnemulin yog ib tiam tshiab ntawm cov tshuaj tua kab mob semi hluavtaws ntawmpleuromulin tshuaj. Nws belongs rau diterpenes thiab belongs rau tib chav kawm ntawm cov tshuaj xws li tylosin. Nws yog ib qho tshuaj tua kab mob tshwj xeeb rau tsiaj. Nws yog siv los tiv thaiv thiab kho tus kab mob Mycoplasma thiab gram- cov kab mob zoo hauv npua, nyuj, yaj thiab nqaij qaib. Nws yog feem ntau yog concentrated nyob rau hauv lub ntsws thiab yog ib tug zoo tagnrho tshuaj rau kev kho mob ntawm lub ntsws kab mob los ntawm ntau yam pwm lub cev.
Hauv xyoo 2007, ze li ntawm 50 xyoo tom qab qhov kev tshawb pom ntawm pleurotin truncated pleurotin, thawj pleurotin tshuaj tua kab mob retapamulin tau pom zoo rau kev kho mob, thiab nws tsuas yog siv los ua cov tshuaj hauv zos los kho pustulosis los ntawm Staphylococcus aureus thiab Streptococcus pyogenes rau cov neeg laus thiab cov menyuam hnub nyoog tshaj 9 hli.
Hauv 2019, tom qab ze li ntawm 60 xyoo ntawm txoj kev loj hlob, lefamulin (bc-3781), cov tshuaj pleurotin tshiab kawg, ua tiav theem 3 kev sim tshuaj hauv xyoo 2018 thiab xa daim ntawv thov tshuaj tshiab rau FDA thaum Lub Ob Hlis 2019. Nws xav tias yuav dhau los ua thawj tib neeg truncated pleurotin cov kab mob siv tshuaj tua kab mob hauv zej zog uas tuaj yeem siv tshuaj tua kab mob hauv zej zog. (intravenous los yog qhov ncauj noj).
Pleuromulinyog ib qho dav -spectrum diterpene tshuaj tua kab mob uas tsim los ntawm Pleurotus ostreatus.
1. Nws tuaj yeem cuam tshuam cov synthesis ntawm cov kab mob protein, thiaj li ua tiav cov nyhuv ntawm inhibiting kab mob loj hlob. Nws hom kev ua yog txawv ntawm lwm hom tshuaj tua kab mob.
2. Nyob rau hauv cov nqe lus ntawm mechanism ntawm kev txiav txim. Truncated Pleurotus tshuaj tua kab mob feem ntau ua rau cov qib ribosome ntawm cov kab mob. Nws thaiv cov synthesis ntawm cov kab mob proteins los ntawm inhibiting cov kev ua ntawm peptidyl transferase, thiaj li ua tau ib tug dav -spectrum antibacterial nyhuv.
Cov tshuaj truncated Pleurotus ostreatus yog tsim los ntawm peb lub nplhaib, tsim cov pob txha loj, thiab nws cov qauv yooj yim yog yim lub nplhaib; Pab pawg carbonyl ntawm tsib lub nplhaib thiab pawg hydroxyl ntawm C-11 yog pab pawg tsim nyog rau kev ua si. Feem ntau ntawm cov kev tshawb fawb txawv teb chaws yog kev hloov kho tshuaj ntawm C-14 los txhim kho nws cov tshuaj tua kab mob thiab bioavailability. Vim tias C-14 ntawm cov tshuaj pleurotin truncated muaj hydroxyl dawb, nws tsis muaj kev ua si; Los ntawm kev hloov kho cov qauv ntawm C-14 rau hauv, derivatives nrog kev ua kom muaj zog tiv thaiv kab mob tiv thaiv kab mob thiab mycoplasma tuaj yeem tau txais.
Tsis tas li ntawd, cov tshuaj tua kab mob ntawm cov tebchaw nrog cov pab pawg nruab nrab lossis cov kua qaub txuas nrog C-14 sab chains yog tsawg heev, thiab kev ua haujlwm ntawm kev sib txuas ntawm ob txoj hlua sab hauv tseem tsawg heev; Txawm li cas los xij, kev ua haujlwm ntawm thioether sab saw derivatives txuas nrog lub hauv paus chaw tau raug txiav txim siab zoo dua. Piv txwv li, tamoxin fumarate yog ib yam tshuaj uas muaj thioether sab chains. Txawm li cas los xij, yog tias sulfur atom hauv Thioether Group hloov los ntawm oxygen atom, kev ua haujlwm ntawm cov tshuaj pleurotin raug txiav yuav txo qis. Yog tias lwm cov khoom hloov pauv yooj yim, xws li guanidine lossis thawj amine, ntxiv rau cov saw hlau sab ntawm C-14 txoj haujlwm, qhov kev ua haujlwm ntawm thioether derivatives tsis tuaj yeem ncav cuag, thiab nws yooj yim rau hydrolyze thiab inactivate hauv vivo. Yog li, acylation hloov kho ntawm C-14 txoj hauj lwm ntawm truncated pleurotin compound tuaj yeem txo qhov tsawg kawg nkaus inhibitory concentration thiab txhim kho cov tshuaj tua kab mob.
1. Cov yam ntxwv ntawm cov qauv molecular
Cov qauv molecular ntawmPleuromulinmuaj plaub lub voj voog, raws li pom hauv daim duab. Ntawm lawv, thawj lub nplhaib yog lub nplhaib benzo, lub nplhaib thib ob yog lub nplhaib oxygen heterocyclic, lub nplhaib thib peb yog lub nplhaib nitrile heterocyclic, thiab lub nplhaib thib plaub yog lub nplhaib pyrrole. Lawv sib txuas los ntawm C-C thiab C-N ib daim ntawv cog lus, tsim cov qauv molecular complex. Pawg no ntawm polycyclic compounds feem ntau hu ua polycyclic ketones lossis polycyclic lactones.
2. Kev tshuaj xyuas cov qauv molecular
Cov qauv molecular ntawm nws tuaj yeem txiav txim siab los ntawm ntau yam kev tshuaj ntsuam xyuas, suav nrog spectroscopy, huab hwm coj spectrometry, thiab X-ray crystallography.
(1) Spectroscopic tsom xam
Ultraviolet spectroscopy tuaj yeem muab cov ntaub ntawv ntawm cov qauv hluav taws xob ntawm cov khoom. Nws nthuav tawm ob qhov sib txawv qhov siab tshaj plaws nyob rau hauv cheeb tsam ultraviolet, nyob ntawm 246 nm thiab 279 nm, feem. Cov peaks no tuaj yeem raug ntaus nqi rau lawv π - π * kev hloov pauv thiab n - π * kev hloov pauv. Nyob ze infrared spectroscopy tuaj yeem muab cov ntaub ntawv hais txog cov qauv kev vibrational molecular ntawm cov khoom. Qhov ze ntawm -infrared spectroscopy qhia cov vibrational bands ntawm ntau pawg ua haujlwm, xws li carbonyl, hydroxyl, amino, thiab oxygen pawg.
Nuclear magnetic resonance (NMR) thev naus laus zis tuaj yeem muab cov ntaub ntawv qauv molecular ntawm cov khoom. Feem ntau, ^ 1H NMR spectroscopy thiab ^ 13C NMR spectroscopy yog siv los txiav txim nws cov qauv. Nyob rau hauv lub ^ 1H NMR spectrum, nws qhia ntau yam tshuaj hloov peaks, thiab qhov sib txawv ntawm cov peaks no yuav siv tau los txiav txim txoj hauj lwm ntawm txawv protons nyob rau hauv lub molecule. Piv txwv li, nws qhia peb lub ncov ntawm methylene protons, nrog ib lub ncov ntawm 0.8 ppm tshwm sim los ntawm thawj methylene proton, thiab ob lub ncov ntawm 1.2 ppm tshwm sim los ntawm qhov thib ob thiab thib peb methylene protons.
(2) Mass spectrometry tsom xam
Mass spectrometry yog ib qho cuab yeej tseem ceeb heev uas tuaj yeem muab qhov hnyav molecular thiab cov ntaub ntawv ntawm cov qauv molecules. Nyob rau hauv huab hwm coj spectrometers, nws yog feem ntau soj ntsuam siv siab -kev daws teeb meem kua chromatography-mass spectrometry (LC-MS). Electro spray ionization (ESI) lossis atmospheric siab tshuaj ionization (APCI) feem ntau yog siv ionization technologies. Nyob rau hauv qhov loj spectrum, nws qhia tau hais tias lub molecular ion ncov [M + H] ^ + ntawm m / z 372, uas ua raws li nws cov qauv molecular.
(3) X-ray crystallographic tsom xam
X-ray crystallography yog cov txheej txheem siv los txiav txim siab cov qauv siv lead ua los ntawm kev ua cov khoom siv lead ua rau hauv lub teeb hluav taws xob, khaws cov ntaub ntawv tawg, thiab siv cov txheej txheem suav los txheeb xyuas cov qauv molecular. Thaum siv cov tshuab no,Pleuromulinyuav tsum tau crystallized thiab tsim rau hauv ib lub pob zeb. Tom qab ntawd, cov qauv siv lead ua yog txiav txim siab los ntawm kev ntsuas qhov tawg ntawm cov siv lead ua hauv qab X-ray beam. Thaum kawg, X-ray crystallography thev naus laus zis tuaj yeem muab cov ncauj lus kom ntxaws txog kev coj ntawm molecular flow, atomic nrug, thiab lub kaum ntse ntse.
Pleuroutilin, tshuaj tua kab mob diterpene muab los ntawm cov kab mob fungus Pleurotus utilis, ua ib qho tseem ceeb ua ntej rau lub semi-synthetic kev loj hlob ntawm truncated Pleurotus tshuaj. Cov tshuaj tua kab mob no, tshwj xeeb tshaj yog cov tshuaj tua kab mob Pleurotus truncatus, sawv cev rau kev vam meej hauv kev kho tshuaj tua kab mob.
Cov tshuaj tua kab mob tshiab no nthuav tawm cov tshuaj tua kab mob zoo kawg nkaus, muaj peev xwm tiv thaiv cov kab mob dav dav. Qhov tshwj xeeb, lawv ua kom pom muaj zog tiv thaiv Gram- cov kab mob zoo, mycoplasma, thiab txawm tias qee hom kab mob Gram- cov kab mob tsis zoo. Qhov dav -spectrum kev ua haujlwm no yog qhov muaj txiaj ntsig zoo hauv chaw kho mob uas kis tau los ntawm ntau hom kab mob tuaj yeem nyuaj rau kev kho.
Ntxiv mus, cov tshuaj tua kab mob Pleurotus truncatus sawv tawm rau lawv cov tshuaj tiv thaiv. Raws li cov kab mob kab mob nce zuj zus tuaj yeem tiv taus cov tshuaj tua kab mob ib txwm muaj, kev tshawb pom ntawm cov neeg ua haujlwm tshiab uas tuaj yeem kov yeej qhov kev tiv thaiv no yog qhov tseem ceeb rau kev tswj xyuas cov kev kho mob zoo. Lub peev xwm ntawm cov tshuaj tua kab mob no khaws lawv cov kev ua tau zoo ntawm cov kab mob resistant underscores lawv lub peev xwm raws li muaj txiaj ntsig ntxiv rau cov tshuaj tua kab mob.
Lub semi-synthetic derivatives ntawm Pleuroutilin, raws li nws cov qauv tshuaj tshwj xeeb, muab cov sijhawm ntxiv rau kev ua kom zoo dua qub thiab txhim kho cov kab mob tua kab mob. Cov kws tshawb fawb tuaj yeem hloov kho cov txheej txheem ua ntej los tsim cov tebchaw tshiab nrog cov tshuaj kho mob zoo dua qub, xws li muaj zog ntxiv, txo cov tshuaj lom, lossis txhim kho bioavailability.
Hauv cov ntsiab lus, Pleuroutilin thiab nws cov semi-synthetic derivatives sawv cev rau cov chav kawm tshiab ntawm cov tshuaj tua kab mob uas muaj kev ua haujlwm dav dav, tiv thaiv tshuaj tiv thaiv, thiab muaj peev xwm ua kom zoo dua ntxiv. Cov cwj pwm no ua rau lawv cov neeg sib tw txaus nyiam rau kev txhim kho cov kev kho tshiab rau cov kab mob sib kis, tshwj xeeb yog cov tshwm sim los ntawm ntau hom - tshuaj tiv thaiv kab mob.
Cov kev mob tshwm sim ntawm cov tshuaj no yog dab tsi?
Gastrointestinal cov tshuaj tiv thaiv:Cov tsos mob ntawm plab hnyuv tsis xis nyob xws li xeev siab, ntuav, thiab raws plab yuav tshwm sim. Cov tsos mob no feem ntau yog me me thiab maj mam zoo dua tom qab txiav cov tshuaj.
Kev tsis haum tshuaj:Qee tus neeg yuav muaj kev fab tshuaj rau cov tshuaj, tshwm sim ua pob liab liab, khaus khaus, urticaria, thiab lwm yam tsos mob. Kev tsis haum tshuaj hnyav tuaj yeem suav nrog ua pa nyuaj, laryngeal edema, poob siab, thiab lwm yam, yuav tsum tau kho mob tam sim.
Neurological teb:Qee zaum, nws yuav ua rau cov tsos mob tsis xis nyob xws li kiv taub hau, mob taub hau, thiab tsaug zog. Cov tsos mob no yuav cuam tshuam rau tus neeg mob lub neej txhua hnub thiab kev ua haujlwm.
Lub siab thiab lub raum puas:Lub sij hawm ntev los yog siv ntau dhau ntawm cov tshuaj no tuaj yeem ua rau lub siab thiab lub raum ua haujlwm puas. Cov neeg mob uas muaj lub siab thiab lub raum tsis ua haujlwm yuav tsum tau ceev faj tshwj xeeb thaum siv nws thiab kho cov tshuaj raws li tus kws kho mob qhia.
Lwm yam teebmeem:Tej zaum muaj xws li kub taub hau, ua daus no, thiab mob ntawm qhov chaw txhaj tshuaj. Qee tus neeg mob me me tuaj yeem ntsib cov kab mob ntshav tsis zoo xws li leukopenia thiab thrombocytopenia.
FAQ
pleuromutilin yog dab tsi?
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Pleuromutilins yogtshuaj tua kab mob uas xaiv inhibit kab mob txhais lusthiab yog semisynthetic derivatives ntawm ib txwm tshwm sim tricyclic diterpenoid pleuromutilin, uas tau txais nws lub npe los ntawm pleuromutilin - tsim cov fungus Pleurotus mutilus.
Dab tsi yog pleuromutilin derivatives?
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Pleuromutilin derivatives xa mus rauCov tshuaj tua kab mob tau muab los ntawm fungal metabolite pleuromutilin, uas ua los ntawm inhibiting protein synthesis thiab muaj cov ntawv thov hauv kev kho cov kab mob, suav nrog cov uas tshwm sim los ntawm methicillin -resistant Staphylococcus aureus (MRSA).s hlau tsis zoo li cov khoom siv ntxhia, tom qab siv tau tuaj yeem tso qee yam tshuaj los txhawb tib neeg kev nqus.
Cim npe nrov: pleuromulin cas 125-65-5, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom