Asid Salvianolik C
Objektif
Salvianolic asid C se yon inibitè ki pa konpetitif nan cytochrome p4502c8 (cyp2c8) ak yon inibitè melanje nan cytochrome P4502J2 (CYP2J2) ak entansite mwayen.Valè Ki li yo pou cyp2c8 ak CYP2J2 se 4.82 μ M ak 5.75 μ M respektivman.
Non angle
(2R)-3-(3,4-Dihydroxyphenyl)-2-({(2E)-3-[2-(3,4-dihydroxyphenyl)-7-hydroxy-1-benzofuran-4-yl]-2- propenoyl}oxy)propanoik asid
Alyas angle
(2R)-3-(3,4-Dihydroxyphenyl)-2-({(2E)-3-[2-(3,4-dihydroxyphenyl)-7-hydroxy-1-benzofuran-4-yl]prop-2 -enoyl}oxy)propanoik asid
(2R)-3-(3,4-Dihydroxyphenyl)-2-({(2E)-3-[2-(3,4-dihydroxyphenyl)-7-hydroxy-1-benzofuran-4-yl]-2- propenoyl}oxy)propanoik asid
Asid benzènpropanoik, α-[[(2E)-3-[2-(3,4-dihydroxyphenyl)-7-hydroxy-4-benzofuranyl]-1-oxo-2-propen-1-yl]oxy]-3, 4-dihydroxy-, (αR)-
Asid Salvianolik C
Pwopriyete fizikochimik asid Salvianolik C
Dansite: 1.6 ± 0.1 g / cm3
Pwen bouyi: 844.2 ± 65.0 ° C nan 760 mmHg
Fòmil molekilè: C26H20O10
Pwa molekilè: 492.431
Pwen flash: 464.4 ± 34.3 ° C
Mas egzak: 492.105652
PSA:177.89000
LogP: 3.12
Presyon vapè: 0.0 ± 3.3 mmHg nan 25 ° C
Endèks refraktif: 1.752
Byoaktivite asid Salvianolic C
Deskripsyon:
Salvianolic asid C se yon inibitè ki pa konpetitif nan cytochrome p4502c8 (cyp2c8) ak yon inibitè melanje nan cytochrome P4502J2 (CYP2J2) ak entansite mwayen.Valè Ki li yo pou cyp2c8 ak CYP2J2 se 4.82 respektivman μ M ak 5.75 μ M.
Kategori ki enpòtan:
Chemen siyal > > metabolik anzim / proteaz > > cytochrome P450
Domen rechèch > > kansè
Pwodwi natirèl >> lòt moun
Sib:
CYP2C8:4.82 μM (Ki)
CYP2J2:5.75 μM (Ki)
Etid in vitro:
Salvianolic asid C se yon inibitè modere melanje nan inibitè cyp2c8 ki pa konpetitif ak CYP2J2.KIS nan cyp2c8 ak CYP2J2 yo se 4.82 ak 5.75 respektivman μ M [1]。 1 ak 5 μ M asid salvianolic C (SALC) ka siyifikativman anpeche LPS pwovoke pa gen okenn pwodiksyon.Salvianolic asid C siyifikativman redwi ekspresyon iNOS.Salvianolic asid C inibit LPS pwovoke TNF-α， IL-1 β， IL-6 ak IL-10 te twòp pwodwi.Salvianolic asid C inibit LPS pwovoke deklanchman NF-κ B.Salvianolic asid C ogmante ekspresyon Nrf2 ak HO-1 nan microglia BV2 [2].
Etid In Vivo:
Salvianolic asid C (20mg / kg) tretman siyifikativman redwi latansi a chape.Anplis de sa, tretman SALC (10 ak 20 mg / kg) ogmante siyifikativman kantite travèse platfòm konpare ak gwoup modèl LPS.Konpare ak gwoup modèl la, administrasyon sistemik asid salvianolik C desann kontwole TNF-α nan sèvo, IL-1 β ak nivo IL-6.Nivo iNOS ak COX-2 nan cortical serebral la ak ipokanp nan rat yo te pi wo pase sa yo nan gwoup kontwòl la, pandan y ap tretman asid salvianolic C siyifikativman desann reglemante cortical a ak ipokanp.Salvianolic asid C (5, 10 ak 20 mg / kg) tretman ogmante p-ampk, Nrf2, HO-1 ak NQO1 nivo nan rat serebral cortical ak ipokanp nan yon fason ki depann de dòz [2].
Referans:
[1].Xu MJ, et al.Efè inhibition nan eleman Danshen sou CYP2C8 ak CYP2J2.Chem Biol Interact.2018 jen 1;289:15-22.
[2].Song J, et al.Aktivasyon nan siyal Nrf2 pa asid salvianolic C atenue NF κ B medyatè repons enflamatwa tou de nan vivo ak nan vitro.Int Immunopharmacol.2018 oktòb;63:299-310.
