Journal of Ethnopharmacology 2020-Apr
Discovery of the active compounds of Smilacis Glabrae Rhizoma by utilizing the relationship between the individual differences in blood drug concentration and the pharmacological effect in rats.
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MATERIALS AND METHODS
A method was established to discover and identify the potential active compounds in drug-containing plasma from rats that were orally administered SGR extract, utilizing the relationship between the individual differences in blood drug concentrations in the rats and the resulting differences in pharmacological effect, and the method was denoted as the RID-PE method. For this method, we used high-performance liquid chromatography with a diode array detector combined with electrospray ionization ion trap time-of-flight multistage mass spectrometry (LC-MSn) to identify the compounds (the original constituents and metabolites) and to determine the peak areas of the compounds in drug-containing plasma following SGR treatment. The anti-inflammatory effect of SGR was evaluated using a carrageenan-induced inflammatory rat model. According to the percent inhibition of paw edema in each model rat (14 rats total) orally administered SGR extract, the plasma samples from the rats were sorted and divided into 7 groups. Each group consisted of two plasma samples, and their percent inhibition of paw edema were similar to each other. We performed an LC-MSn analysis on 3 plasma groups, which showed large differences in the inhibition rates, with percent inhibitions of 92.7%, 72.4% and 38.4%. The correlation coefficients (r) between the peak area of each compound and the pharmacological effect (inhibition ratio) of SGR in the three groups were analyzed using SPSS software. When the correlation coefficients of the compounds are greater than 0.8 (0.8 < r ≤1), these compounds are strongly and positively correlated with anti-inflammatory activity, making them potential anti-inflammatory active compounds.