Napagoda Mayuri, Gerstmeier Jana, Butschek Hannah, Lorenz Sybille, De Soyza Sudhara, Qader Mallique, Nagahawatte Ajith, Wijayaratne Gaya Bandara, Schneider Bernd, Svatoš Aleš, Jayasinghe Lalith, Koeberle Andreas, Werz Oliver
Department of Biochemistry, Faculty of Medicine, University of Ruhuna, Galle 80000, Sri Lanka.
Department of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, Philosophenweg 14, D-07743 Jena, Germany.
Pharmaceuticals (Basel). 2022 Mar 31;15(4):436. doi: 10.3390/ph15040436.
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 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 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 values of 1.3 and 5.1 µg/mL in cell-free and cell-based assays, respectively. These findings rationalize the ethnopharmacological use of as antimicrobial and anti-inflammatory remedy.
Benth在斯里兰卡民间医学中用作治疗炎症和微生物感染的药物。我们之前的研究表明,该植物的亲脂性提取物具有强大的5-脂氧合酶(5-LO)抑制活性,支持了其抗炎潜力。尚未对其抗菌活性进行深入研究,生物活性成分也尚不明确。作为我们之前工作的延续,本研究旨在评估该植物不同提取物的抗菌活性,并分离和鉴定生物活性次生代谢产物。分析了该植物不同的有机提取物的抗菌活性,最具活性的提取物,即二氯甲烷提取物,进行了生物活性导向的分级分离,从而分离出7α-乙酰氧基-6β-羟基瑞香酮。该化合物对耐甲氧西林菌显示出强大的抗菌活性,最低抑菌浓度为62.5μg/mL,其消毒能力与市售消毒剂相当。此外,在无细胞和基于细胞的试验中,7α-乙酰氧基-6β-羟基瑞香酮分别以1.3和5.1μg/mL的IC值抑制5-LO。这些发现为该植物作为抗菌和抗炎药物的民族药理学用途提供了理论依据。