In the present study, we analyzed the antioxidant, antiplatelet aggregation, anti-inflammatory, and tyrosinase inhibitory activities of a variety of solvent extracts of Elaeagnus multiflora Thunb. (Family Elaeagnaceae). Among the solvent extracts of E. multiflora, the ethyl acetate extract (EE) exhibited the highest 1,1-diphenyl-2-picrylhydrazyl radical and xanthine oxidase inhibition activity, as well as the greatest tyrosinase inhibition activity. Only the chloroform extract (CE) inhibited platelet aggregation, and that was a weak effect with 19.29% inhibition at 250 microg/mL, as compared to controls. The CE was also the most potent inhibitor of nitric oxide production among the tested fractions, with almost 100% inhibition at 500 microg/mL. We also detected 2,4-bis(1,1-dimethylethyl)phenol in the CE and EE, via a gas chromatography-mass spectrometry assay. In conclusion, we found that E. multiflora Thunb. has antioxidant and antiplatelet aggregation effects to some extent, and its CE and EE possess potent inhibitory effects on nitric oxide production and tyrosinase activity.

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Pharmacokinetics, metabolism and excretion of two sequential inactive metabolites of the soft corticosteroid loteprednol etabonate (LE), Delta1-cortienic acid etabonate (AE) and Delta1-cortienic acid (A), have been investigated in rats. Pharmacokinetic studies (two-compartment model, 10 mg kg(-1) intra-venous bolus of AE or A) found the elimination of both AE (t(1/2)(beta), 12.46 +/- 1.18 min; CL total, 101.94 +/- 5.80 mL min(-1) kg(-1); and K el, 0.24 +/- 0.02 min(-1)) and A (t(1/2)(beta), 14.62 +/- 0.46 min; CL total, 53.80 +/- 1.40 mL min(-1) kg(-1); and K el, 0.18 +/- 0.02 min(-1)) to be significantly faster than that previously determined for the parent LE (t(1/2)(beta), 43.41 +/- 7.58 min; CL total, 67.40 +/- 11.60 mL min(-1) kg(-1); and K el, 0.071 +/- 0.024 min(-1)). For metabolism and excretion evaluations, 1 and 10 mg kg(-1) of either AE or A were intravenously administered, and the urine and bile were collected. AE and A rapidly reached their peak concentrations in the bile and urine, and most of them were eliminated within one hour. Total cumulative excretions at 4 h after 1 and 10 mg kg(-1) injections were 85.51 +/- 3.38% and 67.50 +/- 2.67% for AE, and 71.90 +/- 3.72% and 37.73 +/- 2.69% for A in bile; and 4.84 +/- 1.87% and 13.85 +/- 3.27% for AE, and 24.28 +/- 8.44% and 22.35 +/- 1.12% for A in urine, respectively. After AE administration, the excretion of AE was > 90%, and A was < 10% in all cases, indicating that the elimination of AE was much faster than its metabolism (to A). In a manner similar to that seen for LE, dose-dependent elimination was observed both in AE and A. These results suggested that both AE and A were ideal leads for the design of soft steroids based on the inactive metabolite approach.

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