Platycodi radix beverage ameliorates postprandial lipemia response through lipid clearance of triglyceride-rich lipoprotein: A randomized controlled study in healthy subjects with a high-fat load

BACKGROUND/OBJECTIVES: Elevation of postprandial lipemia characterized by a rise in triglyceride (TG)-rich lipoproteins can increase the risk of atherogenesis. The objective of this study was to investigate postprandial lipemia response to a single dietary fat/sugar load test and monitor beneficial changes induced by the consumption of Platycodi radix (AP) beverage in healthy subjects. SUBJECTS/METHODS: A total of 52 subjects were randomly assigned to either placebo or AP beverage group with a high-fat shake in a randomized controlled crossover trial. Postprandial blood was collected at 0, 1, 2, 4, and 6 h and analyzed for TG and lipoprotein lipase mass. Inhibition of pancreatic lipase was determined in vitro. RESULTS: AP inhibited pancreatic lipase activity in vitro (IC₅₀ = 5 mg/mL). Compared to placebo beverage, AP beverage consumption with a high-fat shake induced significant increase of plasma lipoprotein lipase mass (P = 0.0111, β estimate = 4.2948) with significant reduction in very low-density lipoprotein (VLDL) TG concentration (P = 0.038, β estimate = −52.69) at 6 h. Based on significant correlation between high-fat dietary scores MEDFICTS and postprandial TG responses in VLDL (P = 0.0395, r = 0.2127), subgroup analysis revealed that 6 h-postprandial VLDL TG response was significantly decreased by AP consumption in subjects with MEDFICTS ≥ 40 (P = 0.0291, β estimate = −7214). CONCLUSIONS: AP beverage might have potential to alleviate postprandial lipemia through inhibiting pancreatic lipase activity and elevating lipoprotein lipase mass. Subgroup analysis revealed that subjects with high-fat dietary pattern could be classified as responders to AP beverage among all subjects.

An HPLC-MS/MS method for the quantitative determination of platycodin D in rat plasma and its application to the pharmacokinetics of Platycodi Radix extract / 中国天然药物

AIMS@#To develop an HPLC-MS/MS method for the quantification of platycodin D (PD) in rat plasma, and to acquire the main pharmacokinetic parameters of PD after oral administration of pure PD or of Platycodi Radix extract (PRE) containing PD.@*METHOD@#Plasma samples were pretreated with solid-phase extraction using an Oasis® HLB SPE cartridge. Madecassoside was used as the internal standard (IS). Chromatographic separation was achieved on an ODS column (100 mm × 2.1 mm i.d., 3.5 μm) with a mobile phase consisting of acetonitrile/water (30 : 70, V/V) containing 0.1 mmol·L(-1) ammonium acetate at a flow rate of 0.25 mL·min(-1). The detection was performed on a triple quadruple tandem mass spectrometer using an electrospray ionization (ESI) source with a chromatographic run time of 3.0 min. The detection was operated by multiple reaction monitoring (MRM) of the transitions of m/z 1 223.6→469.2 for PD and of m/z 973.6→469.2 for madecassoside (IS), respectively.@*RESULTS@#The calibration curve was linear from 5 to 2 000 ng·mL(-1) (r(2) >0.99) with a lower limit of quantification (LLOQ) of 5 ng·mL(-1). The intra- and inter-day precision (relative standard deviation, RSD) values were below 15% and the accuracy (relative error, RE) was from -15% to +15% at three quality control (QC) levels. Plasma concentrations of PD were determined for 24 h after i.v. administration of PD, and oral administration of PD and PRE, respectively. The absolute oral bioavailability of PD in rats was found to be (0.48 ± 0.19)% when administered PD, and to be (1.81 ± 0.89)% when administered PRE.@*CONCLUSION@#The developed HPLC-MS/MS method was successfully applied to assess the pharmacokinetic parameters and oral bioavailability of PD in rats after administration of PD and Platycodi Radix extract.