6-Hydroxyflavone and derivatives exhibit potent anti-inflammatory activity among mono-, di- and polyhydroxylated flavones in kidney mesangial cells

PloS One
Xing WangQibing Zhou

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

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Citations

May 18, 2019·Zeitschrift Für Naturforschung. C, a Journal of Biosciences·Monika StomporJoanna Wietrzyk
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

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Methods Mentioned

BETA
acetylation
protein assay
electrophoresis
chemical modification

Software Mentioned

Graphpad Prism

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