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Objective To investigate the role of nucleotide-binding oligomerization domain-containing protein 1 (NOD1) in inducing insulin resistance in differentiated human adipocytes.Methods Human preadipocytes obtained via liposuction were induced to differentiate into mature adipocytes.iE-DAP,a specific ligand for NOD1,was administered to human adipocytes in culture.NF-κB transcriptional activity and proinflammatory cytokines production were determined by luciferase assay and enzyme-linked immunosorbent assay.Glucose uptake in adipocytes was measured by 2-deoxy-D-[3 H] glucose uptake (P＜0.05).The expression of phosphatidylinositol-3-kinase p85 (PI-3K p85),insulin receptor substrate-1 (IRS-1) and Akt phosphorylations were detected by Western blotting.Results NF-κB transcriptional activity and cytokines such as interleukin (IL)-6,IL-8,and monocyte chemotactic protein 1 secretion were markedly increased after stimulation with iE-DAP (P＜0.05 or P＜0.01).Insulin-induced glucose uptake was decreased with the activation of NOD1 in a dose-and time-dependent fashion.NOD1 activation weakened insulin signal transduction as being revealed by increasing IRS-1 Ser307phosphorylation,reducing protein expression of PI-3K p85,and attenuating insulin-induced phosphorylation of Akt on Ser473 and Thr308in human adipocytes.Conclusion These results indicate that NOD1 activation induces inflammatory response and insulin resistance via IRS-1/PI3-K/Akt signaling pathway in human adipocytes.
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OBJECTIVE:To optimize the formulation of Compound pearl powder effervescent granule and study its release behavior in vitro. METHODS:The contents of anhydrous citric acid,sodium bicarbonate,and lactose in the formulation were optimized by uniform design method with the consumption of ethylenediamine tetraacetic acid(EDTA) as index meanwhile giving consideration to the foaming height and pH of the solution. The dissolution of calcium carbonate in Compound pearl powder effervescent granule,self-made calcium carbonate tablets and self-made pearl power in distilled water and hydrochloric acid were investigated. RESULTS:The optimized formulation of the Compound pearl powder effervescent granule was stated as follows:10.0 g anhydrous citric acid,2.5 g sodium bicarbonate,and 5.0 g lactose. There were significant differences across the 3 different preparations in dissolution rates. CONCLUSION:The prepared Compound pearl powder effervescent granule is characterized by fast and complete drug release. Its solution is acid and indicated for specific population.