Anti-Inflammatory Derivatives with Dual Mechanism of Action from the Metabolomic Screening of Poincianella pluviosa
| Autor: | João Henrique G. Lago, Bianca Gonçalves Vasconcelos de Alcântara, Marisi G. Soares, Tatiane C. S. Maiolini, Daniela Aparecida Chagas-Paula, Olívia da Silva Domingos, João L. Baldim, Danielle Ferreira Dias, Mario F.C. Santos |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2019 |
| Předmět: |
medicine.drug_class
Pharmaceutical Science Context (language use) Pharmacology 01 natural sciences Dual mechanism Anti-inflammatory Analytical Chemistry 03 medical and health sciences Rhuschalcone VI Metabolomics In vivo Drug Discovery medicine Potency Physical and Theoretical Chemistry 030304 developmental biology anti-inflammatory 0303 health sciences Poincianella pluviosa 010405 organic chemistry Chemistry Organic Chemistry metabolomics 0104 chemical sciences Chemistry (miscellaneous) flavonoids Molecular Medicine |
| Zdroj: | Molecules Volume 24 Issue 23 |
| ISSN: | 1420-3049 |
| DOI: | 10.3390/molecules24234375 |
| Popis: | Metabolomics approaches have become fundamental strategies for the analysis of complex mixtures, guiding the isolation of target compounds by focusing on unpublished or promising pharmacological properties. The discovery of novel anti-inflammatory agents is important due to several limitations regarding their potency, efficacy, and adverse effects. Thus, novel anti-inflammatory candidates are essential, aiming to find agents with better mechanisms of action. In this context, extracts from Poincianella pluviosa var. peltophoroides demonstrated significant in vivo anti-inflammatory potential. Thus, metabolomics analysis based on UHPLC-UV-HRFTMS data was performed for the identification of biomarkers with anti-inflammatory properties. Metabolomics-guided chromatographic process led to the isolation of novel compounds 4‴-methoxycaesalpinioflavone and 7-methoxycaesalpinioflavone, as well as known derivatives rhuschalcone VI and caesalpinioflavone. Isolated compounds caused edema inhibition and neutrophil recruitment. Two of them showed better efficacy than reference drugs (indomethacin and dexamethasone). Results of in vivo experiments corroborated those obtained through metabolomics and statistical analyses guiding the isolation of substances of interest. |
| Databáze: | OpenAIRE |
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