Autor: |
Napagoda M; Department of Biochemistry, Faculty of Medicine, University of Ruhuna, Galle 80000, Sri Lanka., Gerstmeier J; Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, Philosophenweg 14, D-07743 Jena, Germany., Butschek H; Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, Philosophenweg 14, D-07743 Jena, Germany., Lorenz S; Research Group Mass Spectrometry and Proteomics, Max Planck Institute for Chemical Ecology, Hans-Knoell-Strasse 8, D-07745 Jena, Germany., De Soyza S; Department of Biochemistry, Faculty of Medicine, University of Ruhuna, Galle 80000, Sri Lanka., Qader M; Natural Products Research Division, National Institute of Fundamental Studies, Hantana Road, Kandy 20000, Sri Lanka., Nagahawatte A; Department of Microbiology, Faculty of Medicine, University of Ruhuna, Galle 80000, Sri Lanka., Wijayaratne GB; Department of Microbiology, Faculty of Medicine, University of Ruhuna, Galle 80000, Sri Lanka., Schneider B; Research Group Biosynthesis/NMR, Max Planck Institute for Chemical Ecology, Hans-Knoell-Strasse 8, D-07745 Jena, Germany., Svatoš A; Research Group Mass Spectrometry and Proteomics, Max Planck Institute for Chemical Ecology, Hans-Knoell-Strasse 8, D-07745 Jena, Germany., Jayasinghe L; Natural Products Research Division, National Institute of Fundamental Studies, Hantana Road, Kandy 20000, Sri Lanka., Koeberle A; Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, Philosophenweg 14, D-07743 Jena, Germany.; Michael Popp Institute and Center for Molecular Biosciences Innsbruck (CMBI), University of Innsbruck, Mitterweg 24, A-6020 Innsbruck, Austria., Werz O; Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, Philosophenweg 14, D-07743 Jena, Germany. |
Abstrakt: |
Plectranthus zeylanicus Benth is used in Sri Lankan folk medicine as a remedy for inflammatory conditions and microbial infections. Our previous investigations revealed potent 5-lipoxygenase (5-LO) inhibitory activity in lipophilic extracts of this plant, supporting its anti-inflammatory potential. In-depth studies on the antimicrobial activity have not been conducted and the bioactive ingredients remained elusive. As a continuation of our previous work, the present investigation was undertaken to evaluate the antimicrobial activity of different extracts of P. zeylanicus and to isolate and characterize bioactive secondary metabolites. Different organic extracts of this plant were analyzed for their antibacterial activity, and the most active extract, i.e., dichloromethane extract, was subjected to bioactivity-guided fractionation, which led to the isolation of 7α-acetoxy-6β-hydroxyroyleanone. This compound displayed strong antibacterial activity against methicillin-resistant Staphylococcus aureus with a minimum inhibitory concentration of 62.5 µg/mL, and its disinfectant capacity was comparable to the potency of a commercial disinfectant. Moreover, 7α-acetoxy-6β-hydroxyroyleanone inhibits 5-LO with IC 50 values of 1.3 and 5.1 µg/mL in cell-free and cell-based assays, respectively. These findings rationalize the ethnopharmacological use of P. zeylanicus as antimicrobial and anti-inflammatory remedy. |