Prim-O-glucosylcimifugin
Tšebeliso ea Prim-O-glucosylcimifugin
Prim-o-glucosylcimifugin e na le litlamorao tse matla tse thibelang ho ruruha.Polelo ea iNOS le COX-2 e ka thibeloa ka ho laola phetisetso ea lets'oao la JAK2 / STAT3.
Lebitso la Prim-O-glucosylcimifugin
Lebitso la Sechaena:Cimicifugin glycoside
Lebitso la Senyesemane:(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
SechaenaAlias:Cimicifugin
Bioactivity ea Prim-O-glucosylcimifugin
Tlhaloso:
prim-o-glucosylcimifugin e na le litlamorao tse matla tse thibelang ho ruruha.Polelo ea iNOS le COX-2 e ka thibeloa ka ho laola JAK2 / STAT3 transd signal.
Lihlopha tse amehang:
Tsela ea pontšo>> ho itšireletsa mafung le ho ruruha>> nitric oxide synthase
Sebaka sa lipatlisiso>> ho ruruha / ho itšireletsa mafung
Lihlahisoa tsa Tlhaho > > tse ling
Sepheo:iNOS
COX-2
Thuto ea In Vitro:
prim-o-glucosylglycine (POG) ke dikahare tse phahameng ka ho fetisisa tsa chromone le e 'ngoe ea likarolo tse ka sehloohong tse sebetsang ho Fangfeng (RS).Prim-o-glucosylglycine e bapala karolo e khahlanong le ho ruruha ho macrophages e tala ea 264.7 ka ho thibela phetisetso ea matšoao a JAK2 / STAT3 le ho thibela polelo ea iNOS le COX-2.Cytotoxicity ea prim-o-glucoside ho LPS e kentsoeng tšebetsong ea macrophage e tala ea 264.7 e ile ea lekanyetsoa.Sebelisa LPS (1 μ G / ml) le ho eketseha ha khatello ea prim-o-glucosylglycine (15, 50 le 100 μ G / ml) bakeng sa lihora tse 24, 'me ho sebetsa ha sele ho ile ha hlahlojoa ke tlhahlobo ea CCK-8.Ha ho bapisoa le lisele tse tšoaroang tsa DMSO (taolo), lihora tse 24 le ho pepeseha ho 15-100 μ Ka mor'a g / ml prim-o-glucoside, ho sebetsa ha sele ha hoa ka ha ameha haholo.E le ho ithuta ka phello e khahlanong le ho ruruha ea prim-o-glucosylglycine, hore na prim-o-glucosylglycine e ka ama NO synthesis e ile ea hlahlojoa LPS e entsoeng lisele tse tala tsa 264.7.Sebelisa LPS (1 μ G / ml) le likhakanyo tse fapaneng tsa prim-o-glucosylglycine (15, 50 le 100 μ G / ml) bakeng sa lihora tse 24.Boikutlo bo ne bo sa lekanngoe moetlong o matla ka ho fetesisa ka karabelo ea Griess.Khatello ea che ho setso sa supernatant e ile ea eketseha haholo ka ho pepeseha ha LPS, 'me prim-o-glucoside e thibetse haholo LPS ha ea ka ea hlahisa tlhahiso ka mokhoa o itšetlehileng ka mahloriso [1].
Thutong ea Vivo
Bronchoalveolar lavage fluid (BALF) e ile ea bokelloa lihora tse 7 ka mor'a tsamaiso ea lipopolysaccharide (LPS), 'me boemo ba cytokine ho BALF bo lekantsoe ka ELISA.Ha ho bapisoa le sehlopha sa taolo, TNF ho BALF- α, IL-1 β Le maemo a IL-6 a eketsehile haholo.Leha ho le joalo, pretreatment ka prime-o-glucosylglycine (2.5, 5 kapa 10 mg / kg) haholo e laoloang TNF- α, IL-1 β Le IL-6 ka mokhoa o itšetlehileng ka lethal dose (P <0.05, P <0.05, 0.01) ) [1].
Teko ea Cell
Cell counting Kit (CCK-8) e ile ea sebelisoa ho fumana hore na cytotoxic concentration ea prim-o-glucosylglycine ke efe.Ka bokhutšoanyane, lisele tse tala tsa 264.7 li ne li tšoaroa ka 1 ka seliba × Boima ba lisele tsa 104 bo ne bo kenngoa lilibeng tsa 96 'me bo kenngoa ka bosiu bo le bong.Ebe sebelisa 1 μ Lisele li ile tsa hlohlelletsoa ka g / ml LPS 'me tsa phekoloa ka mefuta e sa tšoaneng ea prim-o-glucosylglycine (15, 50 le 100 μ g/mL; Medchem express, Princeton, NJ, USA) kapa phekolo ea DMSO.Ka mor'a ho qhoqhoa ka 37 ℃ bakeng sa lihora tse 24, tharollo ea CCK-8 e ile ea eketsoa selibeng se seng le se seng 'me e kenngoa hora e' ngoe hape.Absorbance e ne e lekantsoe ho 450 nm ho sebelisa sebali sa microplate [1].
Teko ea Liphoofolo
litoeba [1] BALB / C litoeba tse tona, libeke tse 8, tse boima ba 18 ho isa ho 20g.Litoeba li ne li arotsoe ka lihlopha tsa 5: sehlopha sa taolo;sehlopha sa LPS;LPS + prime-o-glucosylglycine (2.5, 5 kapa 10mg / kg boima ba 'mele).Prime-o-glucosylglycine e ne e tsamaisoa ka intraperitoneally.Kamora hora e le 'ngoe, litoeba tsa sehlopha sa LPS le LPS + prime-o-glucosylglycine sehlopha li ile tsa fuoa 50 mg / L intranasal (in) (200 mg / L) μ LLPs ho baka kotsi e mpe ea matšoafo.Litoeba tsa taolo li ile tsa fuoa 50% intranasal (ka) ntle le LPS μ LPBS
[1]
Referense:
[1].Zhou J, le ba bang.Prim-O-glucosylcimifugin Attenuates LipopolysaccharideInduced Inflammatory Response ho RAW 264.7 Macrophages.Pharmacogn Mag.2017 Jul-Sep; 13(51): 378-384.
[2].Chen N, le ba bang.Prime-O-glucosylcimifugin e thibela kotsi e mpe ea matšoafo e bakoang ke lipopolysaccharide ho litoeba.Ho ea ka Immunopharmacol.2013 Jun;16(2):139-47.
Lintho tsa Physicochemical of Prim-O-glucosylcimifugin
Boima: 1.5 ± 0.1 g / cm3
Ntho e Belang: 736.9 ± 60.0 ° C ho 760 mmHg
Foromo ea molek'hule: C22H28O11
Boima ba 'mele: 468.451
Sebaka sa Flash: 255.0 ± 26.4 ° C
'Misa Hantle: 468.163147
PSA:168.28000
LogP: -1.35
Khatello ea Mouoane: 0.0 ± 2.5 mmHg ho 25 ° C
Index ea Refractive: 1.648
Lintlha tsa polokeho ea Prim-O-glucosylcimifugin
Polelo ea Tšireletseho (Yuropa): 24 / 25
Khoutu ya Dikgetho: 29389090
Lebitso la Senyesemane la 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-methoxy-, (2S)-
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
Prim-O-glucosylcimifugin