I-Salvianolic acid C
Inhloso
I-Salvianolic acid C iyi-inhibitor engaqhudelani ye-cytochrome p4502c8 (cyp2c8) kanye ne-mix inhibitor ye-cytochrome P4502J2 (CYP2J2) enamandla aphakathi.Amanani ayo e-Ki e-cyp2c8 kanye ne-CYP2J2 angu-4.82 ngokulandelanayo μ M kanye no-5.75 μ M
Igama lesiNgisi
(2R)-3-(3,4-Dihydroxyphenyl)-2-({(2E)-3-[2-(3,4-dihydroxyphenyl)- 7-hydroxy-1-benzofuran-4-yl]-2- i-propenoyl}oxy) i-propanoic acid
Isibizo sesiNgisi
(2R)-3-(3,4-Dihydroxyphenyl)-2-({(2E)-3-[2-(3,4-dihydroxyphenyl)-7-hydroxy-1-benzofuran-4-yl]prop-2 -enoyl}oxy) propanoic acid
(2R)-3-(3,4-Dihydroxyphenyl)-2-({(2E)-3-[2-(3,4-dihydroxyphenyl)-7-hydroxy-1-benzofuran-4-yl]-2- i-propenoyl}oxy) i-propanoic acid
I-Benzenepropanoic acid, α--[[(2E)-3-[2-(3,4-dihydroxyphenyl)-7-hydroxy-4-benzofuranyl]-1-oxo-2-propen-1-yl]oxy]-3, 4-dihydroxy-, (αR)-
I-Salvianolic acid C
Izici ze-Physicochemical Of Salvianolic Acid C
Ukuminyana: 1.6 ± 0.1 g / cm3
Indawo yokubilisa: 844.2 ± 65.0 ° C ku-760 mmHg
I-Molecular Formula: C26H20O10
Isisindo se-molecule: 492.431
Iphoyinti elikhanyayo: 464.4 ± 34.3 ° C
IMisa ngqo: 492.105652
I-PSA: 177.89000
I-LogP: 3.12
I-Steam Pressure: 0.0 ± 3.3 mmHg ku-25 ° C
Inkomba ye-refractive: 1.752
I-Bioactivity ye-Salvianolic Acid C
Incazelo:
I-Salvianolic acid C iyi-inhibitor engaqhudelani ye-cytochrome p4502c8 (cyp2c8) kanye ne-mix inhibitor ye-cytochrome P4502J2 (CYP2J2) enamandla aphakathi.Amanani ayo e-Ki e-cyp2c8 kanye ne-CYP2J2 angu-4.82 ngokulandelana kwawo μ M kanye no-5.75 μ M.
Izigaba ezifanele:
Indlela yokubonisa > > i-enzyme ye-metabolic / i-protease > > i-cytochrome P450
Umkhakha wocwaningo > > umdlavuza
Imikhiqizo Yemvelo > > abanye
Ithagethi:
I-CYP2C8:4.82 μM (Ki)
I-CYP2J2:5.75 μM (Ki)
Isifundo se-In Vitro:
I-Salvianolic acid C iyi-inhibitor exubile emaphakathi ye-cyp2c8 inhibitor engancintisani ne-CYP2J2.I-KIS ye-cyp2c8 ne-CYP2J2 yi-4.82 kanye ne-5.75 ngokulandelanayo μ M[1]。 I-1 kanye ne-5 μ M i-salvianolic acid C (SALC) ingavimbela ngokuphawulekayo i-LPS eyenza kungabikho ukukhiqizwa.I-Salvianolic acid C inciphise kakhulu inkulumo ye-iNOS.I-Salvianolic acid C ivimbela i-LPS eyenziwe i-TNF- α, IL-1 β, IL-6 ne-IL-10 yakhiqizwa ngokweqile.I-Salvianolic acid C ivimbela i-LPS eyenziwe i-NF- κ B kusebenze.I-Salvianolic acid C iphinde yandisa inkulumo ye-Nrf2 ne-HO-1 ku-BV2 microglia [2].
Ezifundweni ze-Vivo:
Ukwelashwa kwe-Salvianolic acid C (20mg/kg) kunciphise kakhulu ukubambezeleka kokuphunyuka.Ngaphezu kwalokho, ukwelashwa kwe-SALC (10 kanye no-20 mg/kg) kwenyuse kakhulu inani lokuwela inkundla uma kuqhathaniswa neqembu eliyimodeli ye-LPS.Uma kuqhathaniswa neqembu lamamodeli, ukuphathwa okuhlelekile kwe-salvianolic acid C phansi okulawulwayo kobuchopho TNF- α, IL-1 β kanye namazinga e-IL-6.Amazinga e-iNOS kanye ne-COX-2 ku-cerebral cortex kanye ne-hippocampus yamagundane ayephakeme kunalawo aseqenjini elilawulayo, kuyilapho ukwelashwa kwe-salvianolic acid C kuphansi kakhulu kwalawula i-cortex ne-hippocampus.Ukwelashwa kwe-Salvianolic acid C (5, 10 kanye ne-20 mg / kg) kukhuphule amazinga e-p-ampk, Nrf2, HO-1 kanye ne-NQO1 ku-rat cerebral cortex kanye ne-hippocampus ngendlela encike kumthamo [2].
Ireferensi:
[1].Xu MJ, et al.Imithelela Evimbelayo yezingxenye ze-Danshen ku-CYP2C8 ne-CYP2J2.I-Chem Biol Interact.2018 Jun 1;289:15-22.
[2].Ingoma J, et al.Ukusebenza kokubonisa i-Nrf2 nge-salvianolic acid C kunciphisa i-NF κ B impendulo yokuvuvukala ephakathi nendawo kokubili ku-vivo kanye ne-vitro.I-Immunopharmacol.2018 Okthoba;63:299-310.
