I-Prim-O-glucosylcimifugin
Ukusetyenziswa kwePrim-O-glucosylcimifugin
I-Prim-o-glucosylcimifugin ineempembelelo ezinamandla ezichasayo.Ukubonakaliswa kwe-iNOS kunye ne-COX-2 kunokuvinjelwa ngokulawula i-JAK2 / STAT3 yokutshintshwa kwesignali.
Igama le-Prim-O-glucosylcimifugin
Igama lesiTshayina:Cimicifugin glycoside
Igama lesiNgesi:(2S)-2-(2-hydroxypropan-2-yl)-4-methoxy-7-[[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan -2-yl]oxymethyl]-2,3-dihydrofuro[3,2-g]chromen-5-enye
IsiTshayinaAilis:Cimicifugin
I-Bioactivity ye-Prim-O-glucosylcimifugin
Inkcazo:
I-prim-o-glucosylcimifugin ineempembelelo ezinamandla zokuchasa ukudumba.Ukubonakaliswa kwe-iNOS kunye ne-COX-2 kunokuvinjelwa ngokulawula i-JAK2 / STAT3 isignali yokudluliselwa
Iindidi ezifanelekileyo:
Indlela yokubonakalisa imiqondiso > > ukukhuseleka kunye nokuvuvukala > > i-nitric oxide synthase
Inkalo yophando > > ukudumba / ukunganyangeki
Iimveliso zendalo > > abanye
Ekujoliswe kuko:INOS
COX-2
Isifundo se-In Vitro:
I-prim-o-glucosylglycine (POG) ngowona mxholo uphezulu we-chromone kunye nenye yezinto eziphambili ezisebenzayo kwi-Fangfeng (RS).I-Prim-o-glucosylglycine idlala indima echasene nokuvuvukala kwi-macrophages eluhlaza ye-264.7 ngokuvimbela ukuhanjiswa kwesignali ye-JAK2 / STAT3 kunye nokuthintela ukubonakaliswa kwe-iNOS kunye ne-COX-2.I-cytotoxicity ye-prim-o-glucoside kwi-LPS evuliwe ekrwada ye-264.7 macrophages yalinganiswa.Sebenzisa i-LPS (i-1 μ G / ml) kunye nokwanda koxinzelelo lwe-prim-o-glucosylglycine (15, 50 kunye ne-100 μ G / ml) kwiiyure ezingama-24, kunye nokusebenza kweeseli kwavavanywa ngovavanyo lweCCK-8.Xa kuthelekiswa neeseli eziphathwayo ze-DMSO (ulawulo), iiyure ezingama-24 kunye nokuvezwa kwi-15-100 μ Emva kwe-g / ml prim-o-glucoside, ukusebenza kweseli akuzange kuchaphazeleke kakhulu.Ukuze ufunde i-anti-inflammatory effect ye-prim-o-glucosylglycine, nokuba i-prim-o-glucosylglycine inokuchaphazela i-NO synthesis yavavanywa kwi-LPS evuliwe ekrwada iiseli ezingama-264.7.Sebenzisa i-LPS (1 μ G / ml) kunye neentlobo ezahlukeneyo ze-prim-o-glucosylglycine (15, 50 kunye ne-100 μ G / ml) kwiiyure ezingama-24.Ugxininiso aluzange lulinganiswe kwinkcubeko ephezulu ngokuphendula kukaGriess.Uxinaniso lwe-no kwinkcubeko ephezulu lunyuke kakhulu ngokuvezwa kwe-LPS, kwaye i-prim-o-glucoside ithintele kakhulu i-LPS yenze ukuba kungabikho mveliso ngendlela exhomekeke kugxininiso [1].
KwiSifundo seVivo
I-bronchoalveolar lavage fluid (BALF) yaqokelelwa kwiiyure ze-7 emva kokulawulwa kwe-lipopolysaccharide (LPS), kunye nenqanaba le-cytokine kwi-BALF yalinganiswa ngu-ELISA.Xa kuthelekiswa neqela lolawulo, i-TNF kwi-BALF- α, IL-1 β Kwaye amanqanaba e-IL-6 anyuke kakhulu.Nangona kunjalo, ukunyangwa kwangaphambili nge-prime-o-glucosylglycine (2.5, 5 okanye 10 mg / kg) iphantsi kakhulu elawulwa yi-TNF- α, IL-1 β kunye ne-IL-6 ngendlela exhomekeke kwidosi (P <0.05, P <0.05, 0.01) ) [1].
Uvavanyo lweSeli
I-cell counting Kit (CCK-8) yayisetyenziselwa ukumisela i-cytotoxic concentration ye-prim-o-glucosylglycine.Ngamafutshane, iiseli eziluhlaza ze-264.7 zaphathwa nge-1 ngequla ngalinye × Ubuninzi beeseli ze-104 zahlanjululwa kumaqula angama-96 kwaye zifakwe ubusuku bonke.Emva koko sebenzisa i-1 μ Iiseli zavuselelwa nge-g / ml ye-LPS kwaye ziphathwe ngokugxininiswa okuhlukeneyo kwe-prim-o-glucosylglycine (15, 50 kunye ne-100 μ g / mL; iMedchem express, Princeton, NJ, USA) okanye unyango lwe-DMSO.Emva kokufukanyelwa kwi-37 ℃ iiyure ezingama-24, isisombululo seCCK-8 songezwa kwiqula ngalinye kwaye sifakelwe enye iyure.I-Absorbance ilinganiswa kwi-450 nm usebenzisa i-microplate reader [1].
Animal Experiment
iimpuku [1] BALB / C inkunzi iimpuku, 8 iiveki ubudala, ubunzima malunga 18 ukuba 20g.Iigundane zahlulwa ngokungenamkhethe zibe ngamaqela e-5: iqela lokulawula;Iqela le-LPS;LPS + prime-o-glucosylglycine (2.5, 5 okanye 10mg / kg ubunzima bomzimba).I-Prime-o-glucosylglycine ilawulwa nge-intraperitoneally.Emva kweyure eyi-1, iimpuku kwiqela le-LPS kunye ne-LPS + iqela le-prime-o-glucosylglycine lanikwa i-50 mg / L intranasal (in) (200 mg / L) μ LLPs ukubangela ukwenzakala okukhulu kwemiphunga.Iigundane zokulawula zanikwa i-50% ye-intranasal (in) ngaphandle kwe-LPS μ LPBS
[1]
Isalathiso:
[1].UZhou J, kunye nabanye.I-Prim-O-glucosylcimifugin Iyanciphisa i-Lipopolysaccharide i-Inflammatory Response kwi-RAW 264.7 Macrophages.Pharmacogn Mag.2017 Jul-Sep;13(51):378-384.
[2].UChen N, kunye nabanye.I-Prime-O-glucosylcimifugin ithoba i-lipopolysaccharide-induced acute lung injury kwiimpuku.I-Immunopharmacol.2013 Jun;16(2):139-47.
Iimpawu zePhysicochemical yePrim-O-glucosylcimifugin
Ubuninzi: 1.5 ± 0.1 g / cm3
Indawo yokuBilisa: 736.9 ± 60.0 ° C kwi-760 mmHg
Ifomula yemolekyuli: C22H28O11
Ubunzima beMolekyuli: 468.451
Indawo edanyazayo: 255.0 ± 26.4 ° C
Ubunzima obuchanekileyo: 468.163147
PSA:168.28000
I-LogP:-1.35
Uxinzelelo lomphunga: 0.0 ± 2.5 mmHg ku-25 ° C
Refractive Index: 1.648
Ulwazi lokhuseleko lwe-Prim-O-glucosylcimifugin
Ingxelo yoKhuseleko (iYurophu): 24 / 25
Ikhowudi yeCustoms: 29389090
Isibizo sesiNgesi sePrim-O-glucosylcimifugin
5H-Furo[3,2-g][1]benzopyran-5-one,7-[(β-D-glucopyranosyloxy)methyl]-2,3-dihydro-2-(1-hydroxy-1-methylethyl)- 4-indlela-, (2S)-
I-HMS2196A10
[(2S)-2-(2-Hydroxypropan-2-yl)-4-methoxy-5-oxo-2,3-dihydro-5H-furo[3,2-g]chromen-7-yl]methyl β- D-glucopyranoside
N1606
[(2S)-2-(2-Hydroxy-2-propanyl)-4-methoxy-5-oxo-2,3-dihydro-5H-furo[3,2-g]chromen-7-yl]methyl β- D-glucopyranoside
I-Prim-O-glucosylcimifugin