Emodin (1,3,8-trihydroxy-6-methylanthraquinone) has been identified to have the potential to improve lung fibrosis and lung cancer. To avoid the liver and kidney toxicities and the fast metabolism of emodin, emodin-loaded polylactic acid microspheres (ED-PLA-MS) were prepared and their characteristics were studied. ED-PLA-MS were prepared by the organic phase dispersion-solvent diffusion method. By applying an orthogonal design, our results indicated that the optimal formulation was 12 mg/mL PLA, 0.5% gelatin, and an organic phase:glycerol ratio of 1:20. Using the optimal experimental conditions, the drug loading and encapsulation efficiencies were (19.0 ± 1.8)% and (62.2 ± 2.6)%, respectively. The average particle size was 9.7 ± 0.7 μm. In vitro studies indicated that the ED-PLA-MS demonstrated a well-sustained release efficacy. The microspheres delivered emodin, primarily to the lungs of mice, upon intravenous injection. It was also detected by microscopy that partial lung inflammation was observed in lung tissues and no pathological changes were found in other tissues of the ED-PLA-MS-treated animals. These results suggested that ED-PLA-MS are of potential value in treating lung diseases in animals.

Objective: The second messenger inositol triphosphate (IP3) is involved in signal transduction in multiple cell types. We evaluated the effects of high-dose levocetirizine on chronic spontaneous urticaria (CSU) and examined the significance of serum IP3 level in the pathogenesis of CSU. Methods: Fifteen patients with refractory CSU were given oral levocetirizine at a dose of 15 mg once daily for 7 days, and treatment efficacy was determined using the Urticaria Activity Score and by evaluating wheal-and-erythema reactions and itching. The serum concentration of IP3 at specific time points was determined by enzyme-linked immunosorbent assay. Results: The mean serum concentration of IP3 was 43.54 ± 41.97 pg/mL prior to treatment, 18.40 ± 17.53 pg/mL after treatment, and 1.31 ± 0.92 pg/mL in a healthy control group. The mean concentration of IP3 was significantly higher before treatment than after treatment, and the level of IP3 in the patient group before and after treatment was significantly higher than that in the control group. Conclusion: High-dose levocetirizine was shown to be effective in the treatment of CSU. The level of serum IP3 was positively correlated with CSU activity, indicating that IP3 may play an important role in the pathogenesis of this condition.

Oxymatrine, one kind of alkaloids extracted from Sophora flavescens Ait, has been demonstrated to attenuate bleomycin-induced lung fibrosis. The mechanisms of this action are poorly known. This study aimed to use proteomics to provide new insights into the mechanisms of the pharmacological effects. Proteins from murine lung fibroblasts exposed to oxymatrine were separated by two-dimensional electrophoresis. Differentially expressed proteins were identified using mass spectrometry. A two-dimensional cell migration assay was used to study the effects of oxymatrine on fibroblast migration activity. Among these detectable protein spots on the 2-DE gel 9 protein, spots were significantly altered in oxymatrine treated cells. 5 proteins were successfully identified. All were down-regulated by oxymatrine. Mass spectrometer analysis indicated that one of these proteins is a metabolic enzyme, while others are related to cytoskeleton or involved in cellular transcription and translation. The attenuated expressions of mRNA and protein of the cytoskeleton-related protein, HSP27, were confirmed by Western blotting and RT-PCR analysis. Besides these, the migration activity of fibroblast was reduced by oxymatrine. It is suggested that regulation of HSP27 expression by oxymatrine is associated with its inhibitory effects on motility of lung fibroblasts, which contributes to the protective action of this drug against lung fibrosis. Key words: Oxymatrine, fibroblasts, proteomics, heat shock protein 27, motility.