ABSTRACT
Objective: To compare the relationship of ingredients and pharmacokinetics of steamed Notoginseng Radix et Rhizoma (the roots of Panax notoginseng) with different time (0, 2, 4, and 8 h), and accompany with its anti-platelet aggregation activity. Methods: The components with different steaming duration were determined by HPLC method. Concentration of saponins in Notoginseng Radix et Rhizoma before and after steaming at different time points were detected by UPLC-MS/MS. Pharmacokinetic parameters of each compound were calculated using DAS 3.2.6 software. The anti-platelet aggregation activity was measured by platelet aggregation/clotting analyzer. Results: The results showed that the steaming process reduced the contents of certain bioactive substances (NG-R1, Rg1, Rd, Rb1, and Re) and produced some new components (Rh1, Rg3, Rk3, and Rh4). Ginsenoside Rg3, deglycosylated metabolites of ginsenoside Rb1 possessed lower tmax than ginsenoside Rb1 that indicated the course of deglycosylation made faster absorption. Steamed Notoginseng Radix et Rhizoma had stronger antiplatelet activity, following higher antiplatelet and anticoagulant activities with increasing steaming durations. Conclusion: The results inspire us that saponins may become more active ingredients after deglycosylation, saponins with deglycosylated in vitro become more and more active ingredients into the blood, which could make stronger anticoagulant activity.
ABSTRACT
HPLC analysis was performed to study the changes in chemical composition of ginseng extracts prepared from high quality ginseng with 0, 2, 4, 8 h of steamed times. An UFLC-MS/MS multiple-reaction monitoring (MRM) quantitative analysis was made to investigate the pharmacokinetic behavior differences of ginsenosides in mice ig administered of ginseng extracts with different steamed times in the negative ion mode, with Digoxin as the internal standard substance. The mice were injected with LPS to establish inflammation model after ig administration of ginseng for a week and the contents of tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) in mice plasma were detected by ELISA, in order to study on anti-inflammatory effects of ginseng with different steamed times. It was determined that levels of TNF-α and IL-1β were significantly decreased in inflammation model group ig administered of ginseng extracts with 8h of steamed time. The results showed that the chemical components in ginseng changed after steaming and the components into the blood changed, correspondingly. Ginseng with steamed 8 h contributes to anti-inflammatory effects. These results provided an experimental basis for revealing the active substance basis and dose-effect relationship of ginseng on anti-inflammatory effect.