Abstract
Inflammatory responses by kidney mesangial cells play a critical role in the glomerulonephritis. The anti-inflammatory potential of nineteen mono-, di- and polyhydroxylated flavones including fisetin, quercetin, morin, tricetin, gossypetin, apigenin and myricetin were investigated on rat mesangial cells with lipopolysaccharide (LPS) as the inflammatory stimuli. 6-Hydroxyflavone and 4',6-dihydroxyflavone exhibited high activity with IC50 in the range of 2.0 μM, a much better inhibition potential in comparison to the well-studied polyhydroxylated flavones. Interestingly, the anti-inflammatory activity was not due to direct quenching of NO radicals. Investigation on derivatives with methylation, acetylation or sulfation of 6-hydroxyl group revealed that 6-methoxyflavone was the most potent with an IC50 of 192 nM. Mechanistic study indicated that the anti-inflammatory activity of 6-methoxyflavone arose via the inhibition of LPS-induced downstream inducible NO synthase in mesangial cells. The identification of 6-hydroxyflavone and 6-methoxyflavone with potent anti-inflammatory activity in kidney mesangial cells provides a new flavone scaffold and direction to develop naturally derived products for potential nephritis prevention and ...Continue Reading
References
Dec 1, 2001·Journal of Medicinal Chemistry·M LiuM L Go
Nov 23, 2006·Chemical Research in Toxicology·Qibing ZhouJohn J Ryan
Jun 16, 2007·Rheumatology·H-A ShuiA Chen
Dec 17, 2008·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Dayong SiJ Paul Fawcett
Mar 19, 2009·Biochemical and Biophysical Research Communications·Liesbeth GeraetsGeja J Hageman
Jun 12, 2009·Current Medicinal Chemistry·Shu-Feng ZhouJian-Ping Cai
Jun 23, 2009·Bioorganic & Medicinal Chemistry Letters·Jenson VergheseUmesh R Desai
May 1, 2010·Pharmacognosy Research·Avani PatelN M Patel
Aug 9, 2011·Bioorganic & Medicinal Chemistry Letters·N PanduranganA Banerji
Nov 16, 2011·Clinical and Experimental Medicine·Filiz OzcanMutay Aslan
Dec 6, 2011·The Journal of Nutritional Biochemistry·Chenghui XieXianli Wu
Mar 15, 2012·Experimental Cell Research·Hanna E Abboud
Jun 26, 2012·Biochimica Et Biophysica Acta·Chan-Min LiuChao Cheng
Nov 17, 2012·Cell Communication and Signaling : CCS·I-Ta LeeChuen-Mao Yang
Jun 7, 2013·International Journal of Radiation Biology·Amitava KhanSanjit Dey
Jun 19, 2013·Toxicology·Robert DomitrovićMarko Škoda
Jun 20, 2014·Archives of Biochemistry and Biophysics·Subash C GuptaBharat B Aggarwal
Jul 16, 2014·European Journal of Medicinal Chemistry·Manjinder SinghOm Silakari
Aug 19, 2014·Archives of Biochemistry and Biophysics·Thao Anh TranSomi Kim Cho
Sep 6, 2014·Bioorganic & Medicinal Chemistry Letters·K AmruthaAsoke Banerji
Citations
Oct 14, 2018·Journal of Biomolecular Structure & Dynamics·Sourav DasAtanu Singha Roy
May 18, 2019·Zeitschrift Für Naturforschung. C, a Journal of Biosciences·Monika StomporJoanna Wietrzyk
Mar 18, 2020·Biomolecules·Mostafa AlilouHermann Stuppner
Nov 9, 2017·Zeitschrift Für Naturforschung. C, a Journal of Biosciences·Monika StomporJoanna Wietrzyk
Jun 25, 2019·Oxidative Medicine and Cellular Longevity·Fang-Fang SunLi-Dong Wu
Nov 10, 2020·The Journal of Physical Chemistry. a·Sinjan DasNitin Chattopadhyay