Pharmacokinetics of CZN (15 mg/kg,i.v) after a 1 day and 7 day treatment with baicalin (450 mg/kg,i.v).

*<p><i>vs</i> control <i>P</i><0.05.</p>**<p><i>vs</i> control <i>P</i><0.01.</p><p>ΔΔ<i>vs</i> single <i>P</i><0.01.</p

Pharmacokinetics of CZN (15 mg/kg,i.v) after treatment with different doses of baicalin (225 and 450 mg/kg,i.v).

**<p><i>vs</i> control <i>P</i><0.01.</p

Mean plasma concentration–time profiles of baicalin in rats.

<p>(A) after i.v. administration baicalin at 225 mg/kg and 450 mg/kg. (B) after i.v. administration baicalin at 450 mg/kg/day for 1 day and 7 days in rats (mean ± SD, n = 9).</p

Plots of percentage of control in parameters of CZN versus C_max or AUC of baicalin.

<p>(A) (B) The rats treated with single dose of baicalin at 225 mg/kg (n = 9). (C) (D)The rats treated with single dose of baicalin at 450 mg/kg (n = 18, 9 rats were in different doses and 9 rats were in multiple dose). (E) (F) The rats treated with multiple dose of baicalin at 450 mg/kg (n = 9).</p

Effect of baicalin treatment on CZN pharmacokinetics.

<p>(A) (B)The concentration-time profile of CZN (15 mg/kg,iv) after treatment with saline (control) or baicalin in rats. (C) (D) The changes in CZN (15 mg/kg, i.v) concentrations (%) after treatment with baicalin compared with control. (A) (C) treatment with baicalin (225 or 450 mg/kg, i.v). (B) (D) 1 day-treatment or 7 day-treatment with baicalin (450 mg/kg/day, i.v). Each point represent the mean±SD (n = 9).</p

plasma protein binding of CZN.

<p>(A) The concentration of unbound CZN (%) in pooled plasma samples at different sampling times from rats after treatment with baicalin (450 mg/kg, iv, n = 9) (B) Effect of baicalin in concentration from 125–2500 mg/L on concentration of unbound CZN (%) in pooled rat plasma (n = 5). Total CZN concentration was 50 mg/L. * indicates a significant (<i>P</i><0.05) increase in concentration of unbound CZN (%) from blank values.</p

Correlation of changes in CZN concentrations and corresponding baicalin concentrations in rats.

<p>(A), (C), (E) Correlation coefficient of changes in CZN concentrations in different sampling times and corresponding baicalin concentrations in rats. (B), (D), (F) Plot of mean changes in CZN concentrations after baicalin treatment versus mean baicalin concentrations in rats. (A), (B) The rats treated with single dose of baicalin at 225 mg/kg (n = 9). (C), (D) The rats treated with single dose of baicalin at 450 mg/kg (n = 18, 9 rats were in different doses and 9 rats were in multiple dose). (E), (F) The rats treated with baicalin at 450 mg/kg/d for 7 days (n = 9). * <i>P</i>>0.05 in correlation analysis.</p

Inhibition of CYP2E1 activities by baicalin.

<p>(A) Inhibition of CYP2E1 activities by baicalin in pooled rat liver microsomes, presented as percentage of control activities (the concentration of CZN is 50 µM). (B) Lineweaver-Burk plots of the effect of baicalin on 6-hydroxychlorzoxazone formation in rat liver microsomes. Reactions were performed in the presence of CZN (6.25, 12.5, 25, 50, 100, 200 µM) and various concentrations of baicalin (0, 50, 100, 200µM) in the microsome (0.375 mg/mL) and NADPH-generating system in 100 mM phosphate buffer (pH 7.4), in a final volume of 200µL at 37°C for 30 min. All the data presented are from an analysis of the means of three separate experiments.</p

Additional file 1: of Evaluation of High-Performance Curcumin Nanocrystals for Pulmonary Drug Delivery Both In Vitro and In Vivo

An additional file showing the particle size with different milling times in more detail. (XLSX 10 kb

HRMS of compound from One-pot domino syntheses of 3-alkyl-3-<i>N</i>-substituted aminobenzofuran- 2(3<i>H</i>)-ones based on alkali-promoted Michael addition and lactonization

In this paper, a novel cascade reaction of caesium carbonate-promoted Michael addition and lactonization for the one-pot synthesis of 3-alkyl-3-N-substituted aminobenzofuran-2(3H)-one derivatives has been established based on the screening of the alkaline catalysts and optimization of reaction conditions, in which the N-substituted (ortho-hydroxy) aryl glycine esters were used as the Michael donors to react with different α, β-unsaturated carbonyl compounds. Besides racemic enantiomers, the obtained epimers were successfully separated by conventional chromatography in the case of using the asymmetric raw material. In addition, the possible reaction mechanisms were suggested and the absolute configuration of the epimer was analysed. All the chemical structures of unreported benzofuran- 2(3H)-one derivatives were characterized by IR, 1H NMR, 13C NMR spectra and HRMS spectra