Prim-O-glucosylcimifugin
Gushyira mu bikorwa Prim-O-glucosylcimifugin
Prim-o-glucosylcimifugin igira ingaruka zikomeye zo kurwanya inflammatory.Imvugo ya iNOS na COX-2 irashobora guhagarikwa mugutwara ibimenyetso bya JAK2 / STAT3.
Izina rya Prim-O-glucosylcimifugin
Izina ry'igishinwa:Cimicifugin glycoside
Izina ry'icyongereza:(2S) -2- (2-hydroxypropan-2-yl) -4-mikorerexy-7 - [ -2-yl] oxymethyl] -2,3-dihydrofuro [3,2-g] chromen-5-imwe
IgishinwaAkubeshya:Cimicifugin
Bioactivite ya Prim-O-glucosylcimifugin
Ibisobanuro:
prim-o-glucosylcimifugin ifite ingaruka zikomeye zo kurwanya inflammatory.Imvugo ya iNOS na COX-2 irashobora guhagarikwa mugutegeka ibimenyetso bya JAK2 / STAT3 transd
Ibyiciro bijyanye:
Inzira yerekana inzira >> ubudahangarwa no gutwika >> synthase ya nitric
Umwanya wubushakashatsi >> gutwika / ubudahangarwa
Ibicuruzwa bisanzwe >> ibindi
Intego:iNOS
COX-2
Mu Kwiga Vitro:
prim-o-glucosylglycine (POG) nicyo kintu kinini cya chromone kandi nikimwe mubice byingenzi bigize Fangfeng (RS).Prim-o-glucosylglycine igira uruhare mu kurwanya inflammatory muri macrophage mbisi 264.7 muguhagarika kwanduza ibimenyetso bya JAK2 / STAT3 no kubuza imvugo ya iNOS na COX-2.Cytotoxicity ya prim-o-glucoside kuri LPS yakoresheje macrophage mbisi 264.7.Koresha LPS (1 μ G / ml) no kongera imbaraga za prim-o-glucosylglycine (15, 50 na 100 μ G / ml) mu masaha 24, kandi ubushobozi bwa selile bwasuzumwe na CCK-8.Ugereranije na DMSO ivura selile (kugenzura), amasaha 24 no guhura na 15-100 μ Nyuma ya g / ml prim-o-glucoside, ubuzima bwa selile ntabwo bwagize ingaruka zikomeye.Kugirango twige ingaruka zo kurwanya inflammatory ya prim-o-glucosylglycine, niba prim-o-glucosylglycine ishobora kugira ingaruka NTA synthesis yasuzumwe muri LPS ikora selile 264.7.Koresha LPS (1 μ G / ml) hamwe nubushakashatsi butandukanye bwa prim-o-glucosylglycine (15, 50 na 100 μ G / ml) mumasaha 24.Kwibanda ntabwo byapimwe mumico ndengakamere na Griess reaction.Ubwinshi bwa oya mu muco ndengakamere bwiyongereye ku buryo bugaragara hamwe na LPS, kandi prim-o-glucoside yabujije cyane LPS nta musaruro watangaga mu buryo bushingiye ku kwibanda ku [1].
Mu Kwiga Vivo
Bronchoalveolar lavage fluid (BALF) yakusanyijwe nyuma yamasaha 7 nyuma yubuyobozi bwa lipopolysaccharide (LPS), kandi urugero rwa cytokine muri BALF rwapimwe na ELISA.Ugereranije nitsinda rishinzwe kugenzura, TNF muri BALF- α , IL-1 β Na IL-6 urwego rwiyongereye cyane.Nyamara, kwitegura hamwe na prime-o-glucosylglycine (2.5, 5 cyangwa 10 mg / kg) byagabanutse cyane TNF- α , IL-1 β na IL-6 muburyo buterwa na dose (P <0.05, P <0.05, 0.01 ) [1].
Ubushakashatsi bwakagari
kubara selile Kit (CCK-8) yakoreshejwe kugirango hamenyekane ubukana bwa cytotoxic ya prim-o-glucosylglycine.Muri make, selile mbisi 264.7 zavuwe hamwe 1 kuri buri riba × Ubucucike bwa selile 104 bwatewe mumariba 96 kandi bwaraye bwije.Noneho koresha 1 μ Ingirabuzimafatizo zashizwemo na g / ml LPS hanyuma zivurwa hamwe nubushakashatsi butandukanye bwa prim-o-glucosylglycine (15, 50 na 100 μ g / mL; Express ya Medchem, Princeton, NJ, USA) cyangwa kuvura DMSO.Nyuma yubushakashatsi kuri 37 ℃ kumasaha 24, igisubizo cya CCK-8 cyongewe kuri buri riba hanyuma kongerwaho andi masaha.Absorbance yapimwe kuri 450 nm ukoresheje umusomyi wa microplate [1].
Ubushakashatsi ku nyamaswa
imbeba [1] Imbeba zabagabo BALB / C, ibyumweru 8, ipima nka 18 kugeza 20g.Imbeba zagabanyijwemo amatsinda 5: itsinda rishinzwe kugenzura;Itsinda rya LPS;LPS + prime-o-glucosylglycine (uburemere bw'umubiri 2,5, 5 cyangwa 10mg / kg).Prime-o-glucosylglycine yatanzwe muburyo budasanzwe.Nyuma yisaha 1, imbeba zo mumatsinda ya LPS na LPS + prime-o-glucosylglycine zahawe 50 mg / L intranasal (muri) (200 mg / L) μ LLPs kugirango bikomeretsa ibihaha bikabije.Imbeba zo kugenzura zahawe 50% intranasal (muri) idafite LPS μ LPBS
[1]
Reba:
[1].Zhou J, n'abandi.Prim-O-glucosylcimifugin Yongerera Lipopolysaccharideinduced Inflammatory Igisubizo muri RAW 264.7 Macrophage.Pharmacogn Mag.2017 Nyakanga-Nzeri; 13 (51): 378-384.
[2].Chen N, n'abandi.Prime-O-glucosylcimifugin yongerera lipopolysaccharide iterwa no gukomeretsa cyane ibihaha mu mbeba.Int Immunopharmacol.2013 Jun; 16 (2): 139-47.
Ibyiza bya fiziki ya Himiki ya Prim-O-glucosylcimifugin
Ubucucike: 1.5 ± 0.1 g / cm3
Ingingo yo guteka: 736.9 ± 60.0 ° C kuri 760 mmHg
Inzira ya molekulari: C22H28O11
Uburemere bwa molekuline: 468.451
Ingingo ya Flash: 255.0 ± 26.4 ° C.
Misa nyayo: 468.163147
PSA: 168.28000
LogP: -1.35
Umuvuduko wamazi: 0.0 ± 2,5 mmHg kuri 25 ° C.
Ironderero ridakuka: 1.648
Prim-O-glucosylcimifugin amakuru yumutekano
Itangazo ry'umutekano (Uburayi): 24/25
Kode ya gasutamo: 29389090
Icyongereza Alias cya Prim-O-glucosylcimifugin
5H-Furo [3,2-g] [1] benzopyran-5-imwe, 7 - [((β 4-mikorerexy-, (2S) -
HMS2196A10
[(2S) -2- (2-Hydroxypropan-2-yl) -4-mikorerexy-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-mikorerexy-5-oxo-2,3-dihydro-5H-furo D-glucopyranoside
Prim-O-glucosylcimifugin