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
| Autor: | XuanWang, Yi-Fan Zhang, Gegentana, Shu-Jie Shen, Feng Xu, Guang-Xue Liu, Shao-Qing Cai, Feng-Chun Li, Ming-Ying Shang, Ping Yang, Yao-Li Li, Xin-Xin Yang |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Male
Spectrometry Mass Electrospray Ionization medicine.drug_class Electrospray ionization Anti-Inflammatory Agents Blood drug concentration Pharmacology Smilax glabra Anti-inflammatory Rats Sprague-Dawley 03 medical and health sciences 0302 clinical medicine Chromatography detector In vivo Blood drug Drug Discovery medicine Animals Edema Chromatography High Pressure Liquid 030304 developmental biology Inflammation 0303 health sciences biology Plant Extracts Chemistry Metabolism biology.organism_classification Rats Disease Models Animal 030220 oncology & carcinogenesis Smilax Rhizome Drugs Chinese Herbal |
| Zdroj: | Journal of Ethnopharmacology. 258:112886 |
| ISSN: | 0378-8741 |
| Popis: | Ethnopharmacological relevance This study addresses the rapid discovery of the active compounds (the original constituents and/or metabolites) of a traditional Chinese drug, Smilacis Glabrae Rhizoma (SGR). Aim of the study The aim of this study was to develop a new method to find out the active compounds of traditional drugs in vivo. 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 Results Fifty-eight potential anti-inflammatory compounds (0.8 Conclusions The RID-PE method can be used to discover and identify the active constituents and metabolites of SGR systematically and in vivo. Furthermore, these findings enhance our understanding of the metabolism and effective forms of SGR. |
| Databáze: | OpenAIRE |
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