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Homoplantaginin

CAS No. : 17680-84-1

MCE 站：Homoplantaginin

产品活性：Homoplantaginin是来自中药Salvia plebeia的具有抗炎和抗氧化活性的类黄酮。

研究领域：Apoptosis  |  NF-κB

作用靶点：TNF Receptor  |  NF-κB

In Vitro: Homoplantaginin shows IC₅₀ of reduction level of DPPH radical at 0.35 μg/mL. In human hepatocyte HL-7702 cells exposed to H₂O₂, the addition of 0.1-100μg/mL of homoplantaginin significantly reduces lactate dehydrogenase leakage, and increases glutathione, glutathione peroxidase and superoxide dismutase in supernatant. Homoplantaginin (0.1, 1, 10 μM) dose-dependently reduces expression of toll-like receptor-4 evoked by palmitic acid (100 μM). Homoplantaginin tightly controlls palmitic acid-induced reactive oxygen species to prevent nucleotide-binding domain-like receptor 3 (NLRP3) inflammasome activation by suppressing reactive oxygen species-sensitive thioredoxin-interacting protein, NLRP3, and caspase-1. Pre-treatment of homoplantaginin on human umbilical vein endothelial cells significantly inhibits palmitic acid induced TNF-α and IL-6 mRNA expression, and IKKβ and NF-κB p65 phosphorylation. Homoplantaginin significantly modulates the Ser/Thr phosphorylation of IRS-1, improves phosphorylation of Akt and endothelial nitric oxide synthase, and increases NO production in the presence of insulin.

In Vivo: Homoplantaginin(25-100mg/kg) significantly reducesthe increase in serum alanine aminotranseferase and aspartate aminotransferase, decreases the levels of TNF-α and IL-1. The same treatment also reduces the content of thiobarbituric acid-reactive substances, elevates the levels of GSH, GSH-Px and SOD in hepatic homogenate. Homoplantaginin is rapidly absorbed (Tmax=16.00±8.94min), reaching a mean Cmax between 0.77 and 1.27nmol/mL. The absolute oral bioavailability is calculated to be only 0.75%.

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