AIM: To study the absorption properties and mechanism of two important components, trolline and veratric acid, from the flowers of Trollius chinensis, in order to better understand the contribution of these two compou...AIM: To study the absorption properties and mechanism of two important components, trolline and veratric acid, from the flowers of Trollius chinensis, in order to better understand the contribution of these two compounds to the effectiveness of these flowers. METHOD: The human Caco-2 cell monolayer model was employed to study the transport of trolline and veratric acid from apical side(AP) to basal side(BL), and from BL to AP by determining the transport rates as the function of time and concentration and calculating apparent permeability coefficients(Papp). RESULTS: Trolline and veratric acid were transported across Caco-2 cell monolayer through different mechanisms in a concentration dependent manner.Trolline was transported at a Papp level of 10-6 cm·s-1 with a Papp AP→BL/Papp BL→AP ratio of more than 1.8 or less than 0.8, while veratric acid was transported at a Papp level of 10-5 cm·s-1 with a Papp AP→BL/Papp BL→AP ratio of close to 1.0. CONCLUSION: Trolline is moderately absorbed through an associative mechanism involving active and passive transport, and veratric acid is well-absorbed mainly through passive diffusion. These factors should be taken into account when chemically assessing the pharmacodynamic material basis of the flowers of T. chinensis.展开更多
The present study was designed to investigate the pharmacokinetics and tissue distributions of veratric acid following intravenous administration in rats.The concentrations of veratric acid in rat plasma at various ti...The present study was designed to investigate the pharmacokinetics and tissue distributions of veratric acid following intravenous administration in rats.The concentrations of veratric acid in rat plasma at various times after administrated at doses of 2.5,5,and 10 mg·kg–1 were quantified by HPLC.The tissue distributions of veratric acid at various times after a single intravenous dose of 2.5 mg·kg–1 were also analyzed.The plasma pharmacokinetic parameters at the three doses were as follows:t1/2,(86.23 ± 6.83),(72.66 ± 4.10) and(71.20 ± 2.90) min; C0,(11.10 ± 1.47),(23.67 ± 1.24) and(39.17 ± 3.90) μg·m L–1; and AUC0→∞,(1 240.90 ± 129.14),(2 273.84 ± 132.47) and(3 516.4 ± 403.37) min·μg·m L–1,respectively.The compound was distributed into tissues rapidly and extensively after intravenous administration and was mainly distributed into the liver,heart and kidneys.展开更多
基金supported by the National Sciences Foundation of China(Nos.81073018,81274044)
文摘AIM: To study the absorption properties and mechanism of two important components, trolline and veratric acid, from the flowers of Trollius chinensis, in order to better understand the contribution of these two compounds to the effectiveness of these flowers. METHOD: The human Caco-2 cell monolayer model was employed to study the transport of trolline and veratric acid from apical side(AP) to basal side(BL), and from BL to AP by determining the transport rates as the function of time and concentration and calculating apparent permeability coefficients(Papp). RESULTS: Trolline and veratric acid were transported across Caco-2 cell monolayer through different mechanisms in a concentration dependent manner.Trolline was transported at a Papp level of 10-6 cm·s-1 with a Papp AP→BL/Papp BL→AP ratio of more than 1.8 or less than 0.8, while veratric acid was transported at a Papp level of 10-5 cm·s-1 with a Papp AP→BL/Papp BL→AP ratio of close to 1.0. CONCLUSION: Trolline is moderately absorbed through an associative mechanism involving active and passive transport, and veratric acid is well-absorbed mainly through passive diffusion. These factors should be taken into account when chemically assessing the pharmacodynamic material basis of the flowers of T. chinensis.
文摘The present study was designed to investigate the pharmacokinetics and tissue distributions of veratric acid following intravenous administration in rats.The concentrations of veratric acid in rat plasma at various times after administrated at doses of 2.5,5,and 10 mg·kg–1 were quantified by HPLC.The tissue distributions of veratric acid at various times after a single intravenous dose of 2.5 mg·kg–1 were also analyzed.The plasma pharmacokinetic parameters at the three doses were as follows:t1/2,(86.23 ± 6.83),(72.66 ± 4.10) and(71.20 ± 2.90) min; C0,(11.10 ± 1.47),(23.67 ± 1.24) and(39.17 ± 3.90) μg·m L–1; and AUC0→∞,(1 240.90 ± 129.14),(2 273.84 ± 132.47) and(3 516.4 ± 403.37) min·μg·m L–1,respectively.The compound was distributed into tissues rapidly and extensively after intravenous administration and was mainly distributed into the liver,heart and kidneys.
