Background:
Paederia scandens (Lour.) Merrill, belonging to the Rubiaceae family, was
one of the Traditional Chinese Medicines that has been generally used to treat aches and pains, inflammation,
bacillary dysentery, piles and rheumatic arthritis. The four iridoid glycosides that
Paederosidic acid, Paederoside, Paederosidic acid methyl ester, and Asperuloside from Paederia
scandens are considered to be the main bioactive constituents. However, their pharmacokinetics and
action mechanisms of these iridoid glycosides still remain unknown. In this study, a method of simultaneous
determination of four iridoid glycosides components in rat plasma with LC-MS/MS has been
established and successfully applied to a pharmacokinetic study in rats, which would be favourable for
further exploration.
Methods:
In this study, a sensitive, rapid, accurate bioanalytical method of simultaneous determination
of four iridoid glycosides components from Paederia scandens extract in rat plasma with LCMS/
MS has been established. It is easy and rapid for LC-MS/MS to accurately separate and simultaneously
quantify the analytes because of its high sensitivity, selectivity and accuracy. This validated
method was successfully applied to a pharmacokinetic study in rats with intravenous and oral administrations
of Paederia scandens extract.
Results:
The resulting data are fully satisfied for the selectivity and the sensitivity. Their lower limit
of quantitation are in 0.25-0.5 ng/mL. Intra- and interday precisions were less than 15.0% with accuracy
in the range of -15.0% to 15.0%. In the stability measurements including repeated Freeze-thaw, 4
hours at 4°C, 24 hours at 4°C, and 30 days at -80°C, the variations between the measurements and the
nominated values of these compounds in plasma were detected to be less than 15.0%. The extraction
recoveries of the compounds were from 85.4% to 105.6%. The bioavailability (F) of the four iridoid
glycosides were 1.74% to 3.36%.
Conclusion:
In summary, a simple, rapid, precise, and sensitive LC-MS/MS method has been established
and validated to determine the four iridoid glycosides from Paederia scandens extract in rat
plasma, which was successfully applied to pharmacokinetic study in rats. The information obtained
from the study will facilitate further exploration on Paederosidic acid, Paederoside, Paederosidic acid
methyl ester as well as Asperuloside and these may provide valuable pharmacokinetic reference for
human applications.
Synthesis and Antiproliferative Evaluation of Novel Hybrids of Dehydroabietic Acid Bearing 1,2,3-Triazole Moiety
