Salvianolic acid C
Purpose
Salvianolic acid C is a non competitive inhibitor of cytochrome p4502c8 (cyp2c8) and a mixed inhibitor of cytochrome P4502J2 (CYP2J2) with medium intensity. Its Ki values for cyp2c8 and CYP2J2 are 4.82 respectively μ M and 5.75 μ M
English Name
(2R)-3-(3,4-Dihydroxyphenyl)-2-({(2E)-3-[2-(3,4-dihydroxyphenyl)- 7-hydroxy-1-benzofuran-4-yl]-2-propenoyl}oxy)propanoic acid
English 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
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
Physicochemical Properties Of Salvianolic Acid C
Density: 1.6 ± 0.1 g / cm3
Boiling Point: 844.2 ± 65.0 ° C at 760 mmHg
Molecular Formula: C26H20O10
Molecular Weight: 492.431
Flash point: 464.4 ± 34.3 ° C
Exact Mass: 492.105652
PSA:177.89000
LogP: 3.12
Steam Pressure: 0.0 ± 3.3 mmHg at 25 ° C
Refractive index: 1.752
Bioactivity Of Salvianolic Acid C
Description:
Salvianolic acid C is a non competitive inhibitor of cytochrome p4502c8 (cyp2c8) and a mixed inhibitor of cytochrome P4502J2 (CYP2J2) with medium intensity. Its Ki values for cyp2c8 and CYP2J2 are 4.82 respectively μ M and 5.75 μ M。
Relevant categories:
Signaling pathway > > metabolic enzyme / protease > > cytochrome P450
Research field > > cancer
Natural Products > > others
Target:
CYP2C8:4.82 μM (Ki)
CYP2J2:5.75 μM (Ki)
In Vitro Study:
Salvianolic acid C is a moderate mixed inhibitor of non competitive cyp2c8 inhibitor and CYP2J2. The KIS of cyp2c8 and CYP2J2 are 4.82 and 5.75 respectively μ M[1]。 1 and 5 μ M salvianolic acid C (SALC) can significantly inhibit LPS induced no production. Salvianolic acid C significantly reduced the expression of iNOS. Salvianolic acid C inhibits LPS induced TNF- α， IL-1 β， IL-6 and IL-10 were overproduced. Salvianolic acid C inhibits LPS induced NF- κ B activation. Salvianolic acid C also increased the expression of Nrf2 and HO-1 in BV2 microglia [2].
In Vivo Studies:
Salvianolic acid C (20mg / kg) treatment significantly reduced the escape latency. In addition, SALC (10 and 20 mg / kg) treatment significantly increased the number of platform crossings compared with LPS model group. Compared with the model group, systemic administration of salvianolic acid C down regulated brain TNF- α， IL-1 β And IL-6 levels. The levels of iNOS and COX-2 in the cerebral cortex and hippocampus of rats were higher than those in the control group, while salvianolic acid C treatment significantly down regulated the cortex and hippocampus. Salvianolic acid C (5, 10 and 20 mg / kg) treatment increased p-ampk, Nrf2, HO-1 and NQO1 levels in rat cerebral cortex and hippocampus in a dose-dependent manner [2].
Reference:
[1]. Xu MJ, et al. Inhibitory Effects of Danshen components on CYP2C8 and CYP2J2. Chem Biol Interact. 2018 Jun 1; 289:15-22.
[2]. Song J, et al. Activation of Nrf2 signaling by salvianolic acid C attenuates NF κ B mediated inflammatory response both in vivo and in vitro. Int Immunopharmacol. 2018 Oct; 63:299-310.
