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Multiple In vitro biological effects of phenolic compounds from Morus alba root bark

Authors Culenova, Marie; Sychrova, Alice; Hassan, Sherif T. S.; Berchova-Bimova, Katerina; Svobodova, Petra; Helclova, Alexandra; Michnova, Hana; Hosek, Jan; Vasilev, Hristo; Suchy, Pavel; Kuzminova, Gabriela; Svajdlenka, Emil; Gajdziok, Jan; Cizek, Alois; Suchy, Vaclav; Smejkal, Karel

Journal JOURNAL OF ETHNOPHARMACOLOGY , FEB 10 2020,:248

DOI 10.1016/j.jep.2019.112296 PubMed 31610262

Abstract Ethnopharmacological relevance: Morus alba L. is used in traditional Chinese medicine for the treatment of various diseases, including bacterial infections and inflammation. As a rich source of phenolic compounds, the plant is an object of many phytochemical and pharmacological studies.Aim of the study: The aim of the study was to isolate and evaluate possible parallel antiviral, antibacterial, and anti-inflammatory activities of phenolic mulberry compounds.Materials and methods: Extensive chromatographic separation of mulberry root bark extract and in vitro biological screening of 26 constituents identified promising candidates for further pharmacological research. Selected compounds were screened for anti-infective and anti-inflammatory activities. Antiviral activity was determined by the plaque number reduction assay and by the titer reduction assay, antibacterial using broth microdilution method, and anti-inflammatory activity using COX Colorimetric inhibitor screening assay kit. One compound was evaluated in vivo in carrageenan-induced paw-edema in mice.Results: Five prenylated compounds 1, 2, 8, 9, and 11, together with a simple phenolic ester 13, exhibited inhibitory activity against the replication of herpes simplex virus 1 (HSV-1) or herpes simplex virus 2 (HSV-2), with IC50 values ranging from 0.64 to 1.93 mu g/mL, and EC50 values 0.93 and 1.61 mu g/mL. Molecular docking studies demonstrated the effects of the active compounds by targeting HSV-1 DNA polymerase and HSV-2 protease. In antibacterial assay, compounds 1, 4, 11, and 17 diminished the growth of all of the Gram-positive strains tested, with MIC values of 1-16 mu g/mL. The anti-inflammatory ability of several compounds to inhibit cyclooxygenase 2 (COX-2) was tested in vitro, and compound 16 displayed greater activity than the indomethacin, positive control. Mulberrofuran B (11) showed anti-inflammatory activity in vivo against carrageenan-induced paw-edema in mice.Conclusions: Experimental investigation showed promising antiviral, antibacterial, and/or anti-inflammatory activities of the phenolic mulberry constituents, often with multiple inhibitory effects that might be used as a potential source of new medicine.

Species covered 桑 Morus alba