iridoids and scoparone

Yīn-Chén-Hāo decoction (YCHD) is a traditional Chinese medicine formula composed of capillaris (

Topics: Animals; Anthraquinones; Anti-Inflammatory Agents; Antiviral Agents; Artemisia; Ascites; Chlorogenic Acid; Clinical Trials as Topic; Coumarins; Drugs, Chinese Herbal; Emodin; Fatty Liver; Gardenia; Humans; Iridoids; Liver Diseases; Plant Extracts; Rheum

Topics: Animals; Anthraquinones; Chromatography, Liquid; Coumarins; Drug Evaluation, Preclinical; Herbal Medicine; Iridoids; Male; Rats; Reproducibility of Results; Sensitivity and Specificity; Tandem Mass Spectrometry

Topics: Anthraquinones; Chromatography, High Pressure Liquid; Coumarins; Drugs, Chinese Herbal; Iridoids; Microscopy; Spectrometry, Mass, Electrospray Ionization; Tandem Mass Spectrometry

Increasing evidence has demonstrated that multidrug combinations could amplify the therapeutic efficacies of each agent. Interestingly, the pharmacological effect of traditional Chinese medicine (TCM) is usually attributed to the drug-interaction property (synergism) of multiple active constituents. Pharmacokinetics is a useful means of evaluating the drug interactions of major active compounds in TCM. A simple, sensitive and reliable RP-HPLC-DAD method has been developed to simultaneously quantify 6,7-dimethylesculetin (D), geniposide (G) and rhein (R), which are the active ingredients in Yin-Chen-Hao-Tang (YCHT), performing drug-interaction pharmacokinetics studies in vivo. Plasma samples were prepared using methanolic precipitation, a filtration step, and then injection of the methanolic extract onto a Nova-Pak C₁₈ Guard-Pak™ guard column with a gradient mobile phase. Triple-wavelength diode array detection was set at λ(max) values of 343 nm for D, 241 nm for the G, and 259 nm for R. Our results successfully demonstrate that this method has excellent and satisfactory selectivity, sensitivity, linearity, precision, accuracy and recovery. In healthy rats, the estimated pharmacokinetic parameters (i.e. C(max) , AUC and Cl) of D, G and R, when administered with COC (a combination of D, G and R), were C(max) 16.05 mg/L, AUC 108.96 mg h/L and Cl 0.36 L/h for D; C(max) 9.35 mg/L, AUC 64.71 mg h/L and Cl 0.88 L/h for G; and C(max) 14.18 mg/L, AUC 57.98 mg h/L and Cl 1.77 L/h for R. Here, we report that the COC combination could significantly increase the plasma level and slow the elimination rate compared with any one or two of the three individual compounds, which may indicate a drug-drug interaction.

Topics: Animals; Anthraquinones; Chromatography, High Pressure Liquid; Chromatography, Reverse-Phase; Coumarins; Drug Synergism; Drugs, Chinese Herbal; Iridoids; Linear Models; Male; Models, Chemical; Rats; Rats, Wistar; Reproducibility of Results; Sensitivity and Specificity

A method for the rapid and simultaneous determination of 6,7-dimethylesculetin (CAS 120-08-1) and geniposide (CAS 24512-63-8) in rat plasma has been developed, using validated high performance liquid chromatography (HPLC) with solid phase extraction (SPE). The HPLC analysis was performed on a commercially available column (200 mm x 4.6 mm, 5 microm) with acetonitrile-methanol-0.1% aqueous formic acid as mobile phase and the UV detection at 343 nm and 238 nm for 6,7-dimethylesculetin and geniposide, respectively. The calibration curves for 6,7-dimethylesculetin and geniposide were linear over the range 0.4-25.6 microg/mL and 1.12-71.68 microg/mL, respectively. The lower limits of quantitation were 0.40 microg/ mL and 1.12 microg/mL, and the lower limits of detection were 0.06 microg/mL and 0.09 microg/ mL, respectively. The intra-day and inter-day precision for 6,7-dimethylesculetin and geniposide were < 5%, whereas the absolute recovery percentages were > 74%. A successful application of the developed HPLC analysis was demonstrated for the pharmacokinetic study of a Traditional Chinese Medicine formula of Yin Chen Hao Tang preparation.

Topics: Algorithms; Animals; Calibration; Chromatography, High Pressure Liquid; Coumarins; Drugs, Chinese Herbal; Half-Life; Iridoids; Male; Rats; Rats, Wistar; Reproducibility of Results

Yin Chen Hao Tang preparation (YCHTP) is a classic traditional Chinese medicine formula, which is commonly used for clinical treatment of hepatological diseases. In this study, a rapid and validated high-performance liquid chromatography (HPLC) method was developed to simultaneously identify 6,7-dimethylesculetin and geniposide in rat plasma. This assay was performed on a Dikma Diamonsil RP(18) column (200 mm×4.6 mm, 5 μm) with acetonitrile-methanol-water (0.1% formic acid) as the mobile phase, showing acceptable linearity, intra- and inter-day precision and accuracy (R.S.D.=5%), and absolute recovery for two analytes (74%); the limits of quantitation were 0.4 and 1.12 μg/ml, and the limits of detection were 0.06 and 0.09 μg/ml for two analytes. The developed method was successfully applied to study the effect of formula compatibility on the pharmacokinetics of 6,7-dimethylesculetin and geniposide in YCHTP when orally administrating an effective human daily dose of YCHTP to rats. We surmise that formula compatibility can significantly influence the pharmacokinetics of YCHTP, and we have elucidated and validated the compatible administration of YCHTP.

Topics: Administration, Oral; Animals; Calibration; Chromatography, High Pressure Liquid; Coumarins; Drugs, Chinese Herbal; Iridoids; Limit of Detection; Male; Rats; Rats, Wistar; Reproducibility of Results