Polymethoxylated flavones from Orthosiphon stamineus leaves as antiadhesive compounds against uropathogenic E. coli
| Autor: | Andreas Hensel, Melanie Deipenbrock |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Phytochemicals
Chrysoeriol 01 natural sciences Flavones Bacterial Adhesion Hydroxylation chemistry.chemical_compound Cell Line Tumor Germany Drug Discovery Humans Uropathogenic Escherichia coli Sinensetin Orthosiphon Cytotoxicity Pharmacology chemistry.chemical_classification Flavonoids biology Molecular Structure 010405 organic chemistry Chemistry Orthosiphon stamineus General Medicine biology.organism_classification Diosmetin 0104 chemical sciences Plant Leaves 010404 medicinal & biomolecular chemistry Biochemistry |
| Zdroj: | Fitoterapia. 139 |
| ISSN: | 1873-6971 |
| Popis: | Aqueous and acetone extracts of O. stamineus leaves reduce the adhesion of uropathogenic E. coli (UPEC, strain UTI89) to T24 bladder cells significantly (IC25 ~ 524 mg/mL, resp. 40 μg/mL). The acteonic extract had no cytotoxic effects against UPEC in concentrations that inhibited the bacterial adhesion. The extract significantly reduced the gene expression of fimH, fimC, fimD, csgA and focG, which are strongly involved in the formation of bacterial adhesins. The antiadhesive effect was due to the presence of polymethoxylated flavones, enriched in the acetonic extract. Five flavones have been isolated by fast centrifugal partition chromatography, followed by preparative HPLC. Eupatorin, ladanein, salvigenin, sinensetin, 5,6,7,4′-tetramethoxyflavone and 5-hydroxy-6,7,3′,4′-tetramethoxyflavone were identified as the main polymethoxylated flavones. With the exception of eupatorin, all of these flavones reduced the bacterial adhesion in a concentration depending manner, indicating that B-ring hydroxylation and methoxylation seems to have a major impact on the antiadhesive activity. In addition, this was confirmed by investigation of the flavones chrysoeriol and diosmetin, which had only very weak antiadhesive activity. From these data, Orthosiphon extracts can be assessed to have a pronounced antiadhesive activity against UPEC, based on a variety of polymethoxylated flavones. |
| Databáze: | OpenAIRE |
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