I-Prim-O-glucosylcimifugin
Ukusetshenziswa kwe-Prim-O-glucosylcimifugin
I-Prim-o-glucosylcimifugin inemiphumela enamandla yokulwa nokuvuvukala.Inkulumo ye-iNOS ne-COX-2 ingavinjelwa ngokulawula ukudluliselwa kwesignali ye-JAK2 / STAT3.
Igama le-Prim-O-glucosylcimifugin
Igama lesiShayina:I-Cimicifugin glycoside
Igama lesiNgisi:(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-one
IsiShayinaAi-lias:Cimicifugin
I-Bioactivity ye-Prim-O-glucosylcimifugin
Incazelo:
I-prim-o-glucosylcimifugin inemiphumela enamandla yokulwa nokuvuvukala.Inkulumo ye-iNOS ne-COX-2 ingavinjelwa ngokulawula isignali ye-JAK2 / STAT3
Izigaba ezifanele:
Indlela yokubonisa > > ukungatheleleki nokuvuvukala > > i-nitric oxide synthase
Inkambu yocwaningo > > ukuvuvukala / ukungatheleleki
Imikhiqizo Yemvelo > > abanye
Ithagethi:I-iNOS
I-COX-2
Isifundo se-In Vitro:
I-prim-o-glucosylglycine (POG) iwukuqukethwe okuphezulu kakhulu kwekhromone kanye nengxenye eyinhloko esebenzayo ku-Fangfeng (RS).I-Prim-o-glucosylglycine idlala indima yokulwa nokuvuvukala kuma-macrophage angakahluzwa angama-264.7 ngokuvimbela ukudluliselwa kwesignali ye-JAK2 / STAT3 futhi ivimbele ukuvezwa kwe-iNOS ne-COX-2.I-cytotoxicity ye-prim-o-glucoside ku-LPS eyenziwe yasebenza eluhlaza engama-macrophage angu-264.7 ikaliwe.Sebenzisa i-LPS (1 μ G / ml) nokwandisa ukugxila kwe-prim-o-glucosylglycine (15, 50 kanye no-100 μ G / ml) amahora angu-24, futhi ukusebenza kwamaseli kwahlolwa ngokuhlolwa kwe-CCK-8.Uma kuqhathaniswa namaseli aphathwe i-DMSO (ukulawula), amahora angu-24 kanye nokuchayeka ku-15-100 μ Ngemva kwe-g/ml prim-o-glucoside, ukusebenza kweseli akuzange kuthinteke kakhulu.Ukuze kufundwe umphumela wokunqanda ukuvuvukala we-prim-o-glucosylglycine, ukuthi i-prim-o-glucosylglycine ingaba nomthelela AKUKHO yini ukuhlanganiswa kwahlolwa kumaseli e-LPS acushiwe angu-264.7.Sebenzisa i-LPS (1 μ G / ml) kanye nokugxila okuhlukahlukene kwe-prim-o-glucosylglycine (15, 50 kanye no-100 μ G / ml) amahora angu-24.Ukugxilisa ingqondo akuzange kukalwe kumasiko angaphezu kwamandla ngokusabela kukaGriess.Ukugxiliswa kwe-cha ku-supernatant yesiko kukhuphuke kakhulu ngokuchayeka kwe-LPS, futhi i-prim-o-glucoside evimbe kakhulu i-LPS ayizange ikhiqize ukukhiqizwa ngendlela encike ekugxilweni [1].
Esifundweni se-Vivo
I-bronchoalveolar lavage fluid (BALF) iqoqwe emahoreni angu-7 ngemva kokuphathwa kwe-lipopolysaccharide (LPS), futhi izinga le-cytokine ku-BALF likalwa nge-ELISA.Uma kuqhathaniswa neqembu lokulawula, i-TNF ku-BALF- α, IL-1 β Futhi amazinga e-IL-6 anda kakhulu.Kodwa-ke, ukwelashwa kwangaphambili nge-prime-o-glucosylglycine (2.5, 5 noma 10 mg / kg) kwehlisa kakhulu i-TNF- α, IL-1 β Kanye ne-IL-6 ngendlela encike kumthamo (P <0.05, P <0.05, 0.01 [1].
Ukuhlolwa Kweseli
Ikhithi yokubala yamaseli (CCK-8) yasetshenziselwa ukunquma ukugcwala kwe-cytotoxic ye-prim-o-glucosylglycine.Ngamafuphi, amangqamuzana angama-264.7 aluhlaza aphathwe nge-1 emthonjeni ngamunye × Ubuningi bamaseli angu-104 afakwe emithonjeni ye-96 futhi afakwe ubusuku bonke.Bese sebenzisa 1 μ Amaseli avuselelwa nge-g/ml LPS futhi aphathwa ngokugxilisa okuhlukahlukene kwe-prim-o-glucosylglycine (15, 50 kanye no-100 μ g/mL; i-Medchem express, Princeton, NJ, USA) noma ukwelashwa kwe-DMSO.Ngemva kokufukamela ku-37 ℃ amahora angu-24, isisombululo se-CCK-8 sanezelwa emthonjeni ngamunye futhi sifakwa elinye ihora.I-Absorbance ikalwa ku-450 nm kusetshenziswa isifundi se-microplate [1].
Ukuhlolwa Kwezilwane
amagundane [1] BALB / C male amagundane, anamaviki angu-8 ubudala, anesisindo esingaba ngu-18 kuya ku-20g.Amagundane ahlukaniswa ngokungahleliwe abe amaqembu e-5: iqembu lokulawula;Iqembu le-LPS;I-LPS + prime-o-glucosylglycine (2.5, 5 noma 10mg / kg isisindo somzimba).I-Prime-o-glucosylglycine ilawulwa ngaphakathi kwe-intraperitoneally.Ngemuva kwehora elingu-1, amagundane eqembu le-LPS neqembu le-LPS + prime-o-glucosylglycine anikezwa ama-50 mg / L intranasal (in) (200 mg / L) μ LLPs ukuze enze ukulimala okukhulu kwamaphaphu.Amagundane okulawula anikezwe u-50% we-intranasal (in) ngaphandle kwe-LPS μ LPBS
[1]
Ireferensi:
[1].UZhou J, et al.I-Prim-O-glucosylcimifugin Inciphisa i-Lipopolysaccharide Response Evuvukalayo ku-RAW 264.7 Macrophages.I-Pharmacogn Mag.2017 Jul-Sep;13(51):378-384.
[2].Chen N, et al.I-Prime-O-glucosylcimifugin inciphisa ukulimala kwamaphaphu okubangelwa i-lipopolysaccharide kumagundane.I-Immunopharmacol.2013 Jun;16(2):139-47.
Izakhiwo Ze-Physicochemical Of Prim-O-glucosylcimifugin
Ukuminyana: 1.5 ± 0.1 g / cm3
Indawo yokubilisa: 736.9 ± 60.0 ° C ku-760 mmHg
I-Molecular Formula: C22H28O11
Isisindo se-molecule: 468.451
I-Flash Point: 255.0 ± 26.4 ° C
IMisa ngqo: 468.163147
I-PSA: 168.28000
I-LogP:-1.35
I-Steam Pressure: 0.0 ± 2.5 mmHg ku-25 ° C
Inkomba ye-Refractive: 1.648
Ulwazi lokuphepha lwe-Prim-O-glucosylcimifugin
Isitatimende Sokuphepha (EYurophu): 24 / 25
Ikhodi Yempahla: 29389090
Isibizo sesiNgisi se-Prim-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- I-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- I-D-glucopyranoside
I-Prim-O-glucosylcimifugin