Salvianolic acid C
Injongo
I-Salvianolic acid C i-inhibitor engakhuphisaniyo ye-cytochrome p4502c8 (cyp2c8) kunye ne-inhibitor edibeneyo ye-cytochrome P4502J2 (CYP2J2) kunye nobukhulu obuphakathi.Amaxabiso ayo e-Ki ye-cyp2c8 kunye ne-CYP2J2 yi-4.82 ngokulandelanayo μ M kunye ne-5.75 μ M
Igama lesiNgesi
(2R)-3- (3,4-Dihydroxyphenyl) -2-({(2E)-3-[2-(3,4-dihydroxyphenyl)- 7-hydroxy-1-benzofuran-4-yl]-2- propenoyl}oxy)propanoic acid
IsiNgesi Alias
(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- propenoyl}oxy)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)-
Salvianolic acid C
Iimpawu zePhysicochemical yeSalvianolic Acid C
Ubuninzi: 1.6 ± 0.1 g / cm3
Indawo yokuBilisa: 844.2 ± 65.0 ° C kwi-760 mmHg
Ifomula yemolekyuli: C26H20O10
Ubunzima beMolekyuli: 492.431
Indawo edanyazayo: 464.4 ± 34.3 ° C
Ubunzima obuchanekileyo: 492.105652
PSA: 177.89000
LogP: 3.12
Uxinzelelo lomphunga: 0.0 ± 3.3 mmHg ku-25 ° C
Isalathiso se-refractive: 1.752
I-Bioactivity ye-Salvianolic Acid C
Inkcazo:
I-Salvianolic acid C i-inhibitor engakhuphisaniyo ye-cytochrome p4502c8 (cyp2c8) kunye ne-inhibitor edibeneyo ye-cytochrome P4502J2 (CYP2J2) kunye nobukhulu obuphakathi.Amaxabiso e-Ki e-cyp2c8 kunye ne-CYP2J2 yi-4.82 ngokulandelelanayo μ M kunye ne-5.75 μ M.
Iindidi ezifanelekileyo:
Indlela yokubonakalisa imiqondiso > > i-enzyme ye-metabolic / iprotease > > i-cytochrome P450
Indawo yophando > > umhlaza
Iimveliso zendalo > > abanye
Ekujoliswe kuko:
I-CYP2C8:4.82 μM (Ki)
CYP2J2:5.75 μM (Ki)
Isifundo se-In Vitro:
I-Salvianolic acid C yi-inhibitor edibeneyo edibeneyo ye-cyp2c8 inhibitor engakhuphisaniyo kunye ne-CYP2J2.I-KIS ye-cyp2c8 kunye ne-CYP2J2 yi-4.82 kunye ne-5.75 ngokulandelanayo μ M [1]。 I-1 kunye ne-5 μ M i-salvianolic acid C (SALC) inokunqanda ngokubonakalayo i-LPS eyenza ukuba akukho mveliso.I-Salvianolic acid C yanciphisa kakhulu ukubonakaliswa kwe-iNOS.I-Salvianolic acid C inqanda i-LPS eyenziwe nge-TNF- α, IL-1 β, IL-6 kunye ne-IL-10 yaveliswa kakhulu.I-Salvianolic acid C inqanda i-LPS eyenza i-NF- κ B isebenze.I-Salvianolic acid C nayo yandisa ukubonakaliswa kwe-Nrf2 kunye ne-HO-1 kwi-BV2 microglia [2].
Kwizifundo zeVivo:
Unyango lwe-Salvianolic acid C (20mg / kg) lunciphise kakhulu ukubaleka kokubaleka.Ukongeza, unyango lwe-SALC (10 kunye ne-20 mg / kg) lwandise kakhulu inani leqonga lokuwela xa kuthelekiswa neqela lemodeli ye-LPS.Xa kuthelekiswa neqela lemodeli, ukulawulwa kwenkqubo ye-salvianolic acid C phantsi kwengqondo elawulwayo ye-TNF- α, IL-1 β kunye ne-IL-6 amanqanaba.Amanqanaba e-iNOS kunye ne-COX-2 kwi-cortex ye-cerebral kunye ne-hippocampus yeegundane yayiphezulu kuneqela lokulawula, ngelixa unyango lwe-salvianolic acid C luphantsi kakhulu lulawula i-cortex kunye ne-hippocampus.I-Salvianolic acid C (i-5, i-10 kunye ne-20 mg / kg) unyango luye lwanda i-p-ampk, i-Nrf2, i-HO-1 kunye ne-NQO1 amanqanaba kwi-rat cerebral cortex kunye ne-hippocampus ngendlela exhomekeke kwi-dose [2].
Isalathiso:
[1].Xu MJ, et al.Iimpembelelo ze-Inhibitory zamacandelo e-Danshen kwi-CYP2C8 kunye ne-CYP2J2.I-Chem Biol Interact.2018 Jun 1;289:15-22 .
[2].Ingoma J, et al.Ukusetyenziswa kokubonakaliswa kwe-Nrf2 nge-salvianolic acid C inciphisa i-NF κ B i-mediated inflammatory response kokubili kwi-vivo kunye ne-vitro.I-Immunopharmacol.2018 Okt;63:299-310.
