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Anti-inflammatory flavonoids from root bark of Broussonetia papyrifera in LPS-stimulated RAW264.7 cells
Institution:1. Department of Pharmacognosy, School of Pharmacy, Fudan University, Shanghai 201203, PR China;2. National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China;3. Institute of Analytical Chemistry, Han Dock Su Pyongyang University of Light Industry, Pyongyang 999093, DPR, Korea;1. College of Pharmacy and Research Center for Cell Fate Control, Sookmyung Women''s University, 52 Hyochangwon-Gil, Yongsan-Gu, Seoul 140–742, Republic of Korea;2. Natural Products Research Institute, College of Pharmacy, Seoul National University, 1 Gwanak-Ro, Gwanak-Gu, Seoul 151-742, Republic of Korea
Abstract:Broussonetia papyrifera has been used as a diuretic, tonic and suppressor of edema. Bioactivity-guided fractionation and metabolite investigation of root bark extracts of this plant resulted in the isolation and identification of six 1,3-diphenylpropanes (1, 2, 8, 10, 17, 20), flavanone (3), two chalcones (4, 5), five flavans (6, 11, 1416), dihydroflavonol (7) and five flavonols (9, 12, 13, 18, 19), including five new compounds (5, 7, 8, 19, 20) that inhibit NO production in LPS-induced RAW264.7 cells. The structures of compounds 120 were elucidated on the basis of spectroscopic data (1D and 2D NMR, MS, MS/MS, and HRMS). In particular, compounds 3, 5, 7, 12, and 20 exhibited significant inhibitory effects on the NO, iNOS, and pro-inflammatory cytokine (TNF-α and IL-6) production. Therefore, this study suggests that the flavonoid-rich products of B. papyrifera, including the new compounds, could be valuable candidates for the development of pharmaceuticals or functional foods in the prevention and treatment of anti-inflammatory disease.
Keywords:Dihydroflavonol  Diphenylpropane  Bioactivity-guided isolation  Anti-inflammatory
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