A standardized, combined flavonoid extracts of Scutellaria baicalensis and Acacia catechu, UP446, demonstrates favorable anti-inflammatory properties. In this study, DNA microarray, quantitative polymerase chain reaction (QPCR), and enzyme-linked immunosorbent assay (ELISA) were used to study the effect of UP446 on the lipopolysaccharide (LPS)-induced pro-inflammatory gene regulation of both animal and human immortalized cell lines and also primary human cells. One consistent result from microarray was that the gene expression levels stimulated or suppressed by LPS were returned to normal levels by the UP446 co-treatment. This normalization effect from UP446 was also shown for pro-inflammatory genes cyclooxygenase (COX)-2, tissue necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6 using QPCR, and TNF-α using ELISA. The controlling transcriptional factor of these genes, NFκB, was also down-regulated by UP446 in the LPS-induced cell models. Microarray analysis for numerous genes, including cytokines, chemokines, receptors, transcriptional factors, caspase, growth factors, and phosphatases, suggests not only a genomic anti-inflammatory activity for UP446 but also signaling pathways of cell proliferation, cell death, and lipid metabolism demonstrated on different types of cells.
This study was performed to investigate whether magnolol enhances pentobarbital-induced sleeping behaviors through the GABAergic systems. Magnolol prolonged the sleeping time induced by pentobarbital. In addition, magnolol increased chloride influx in primary cultured cerebellar granule cells. The expression of the GABA(A) receptor alpha-subunit was increased selectively by magnolol, but magnolol had no effect on the abundance of beta- or gamma-subunits. The expression of glutamic acid decarboxylase (GAD) was not influenced by magnolol. It is suggested that magnolol may enhance pentobarbital-induced sleeping behaviors through the activation of GABAergic systems.
We aimed to find antiallergic agents from natural sources using mast cells activated during allergic reaction. We screened over 2000 plants for blockade of histamine release and identified two of them, S. baicalenesis and P. edulis. Bioassay-guided fractionation led to two main constituent flavonoids, baicalin from S. baicalenesis roots and isoorientin from P. edulis leaves. Based on these two compounds, two standardized extracts (SSBE and SPEE) and a combined standardized herb composition (SHC) were developed. SSBE, SPEE, and SHC remarkably inhibited histamine and leukotriene release from mast cells activated by anti-OVA/OVA binding, and SHC showed a stronger inhibition than either extract alone. SHC also showed greater inhibition potency than either aspirin or cromolyn, which are known antiallergic agents. Our results suggest that SHC reduce degranulation during mast cell activation and could be a promising candidate for the treatment of immune/allergic diseases related to mast cells.
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