ABSTRACT
Three new dibenzofurans, 2-hydroxy-3,4-dimethoxydibenzofuran (1), 2,8-dihydroxy-3,4,9-trimethoxydibenzofuran (5) and 2-hydroxy-3,4,6,8-tetramethoxydibenzofuran (6), together with three known dibenzofurans 1-hydroxy-2,3,4-trimethoxydibenzofuran (2), 2-hydroxy-3,4,6-trimethoxydibenzofuran (3) and 1,6-dihydroxy-2,3,4-trimethoxydibenzofuran (4), were isolated from the twigs and leaves of Crataegus oresbia. Their structures were identified by the comprehensive analyses of the physicochemical properties and spectroscopic data (NMR and HR-ESI-MS). Compounds 1-3 showed significant in vitro lipid-lowering activities, especially compound 3 was stronger than simvastatin.
Subject(s)
Asteraceae , Crataegus , Crataegus/chemistry , Dibenzofurans , Plant Leaves/chemistry , Lipids/analysis , Molecular StructureABSTRACT
Phloridzin is a lead compound of the prestigious antidiabetic gliflozins. The present study found that phloridzin highly accumulated in Malus rockii Rehder. The content of phloridzin in M. rockii was the highest among wild plants, with the percentage of 15.54% in the dry leaves. The structure of phloridzin was revised by proton exchange experiments and extensive 2D NMR spectra. Phloridzin exhibited significant hypolipidemic activity in golden Syrian hamsters maybe by increasing the expression of CYP7A1, at the doses of 50 mg/kg and 200 mg/kg. The total performance of anti-hyperlipidemic effect of phloridzin may be superior to that of lovastatin, though lovastatin was more active than phloridzin. In addition, phloridzin exhibited moderate antimalarial activity with inhibition ratio of 31.3 ± 10.9% at a dose of 25 mg/kg/day, and showed moderate analgesic activity with 28.0% inhibition at a dose of 50 mg/kg.
Subject(s)
Antimalarials , Malus , Sodium-Glucose Transporter 2 Inhibitors , Phlorhizin/pharmacology , Phlorhizin/chemistry , Malus/chemistry , Sodium-Glucose Transporter 2 Inhibitors/metabolism , Protons , Lovastatin/metabolismABSTRACT
Additive manufacturing enabled the fabrication of porous titanium (PT) with customized porosity and mechanical properties. However, functionalization of PT surfaces with bioactive coatings is being challenged due to sophisticated geometry and highly porous structure. In this study, a facile flow-casting technique was developed to produce homogeneous 45S5 bioactive glass (BG) coatings on the entire surface of PT. The coating weight as a function of BG concentration in a BG-PVA slurry was investigated to achieve controllable coating yield without blocking macropore structure. The annealing-treated BG coating not only exhibited compact adhesion confirmed by qualitative sonication treatment, but also enhanced the mechanical properties of PT scaffolds. Moreover, in-vitro assessments of BG-coated PT cultured with MC3T3-E1 cells was carried out having in mind their potential as bioactive bone implants. The experimental results in this study offer a simple and versatile approach for the bio-functionalization of PT and other porous biomedical devices.