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

Wang X, Wang Z, Sidhu PS, Desai UR, Zhou Q - PLoS ONE (2015)

Bottom Line: 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.

View Article: PubMed Central - PubMed

Affiliation: Department of Nanomedicine and Biopharmaceuticals, College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan, Hubei, China.

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 treatment.

No MeSH data available.


Related in: MedlinePlus

Anti-inflammatory activity of mono-, di- and polyhydroxylated flavones on the LPS-induced NO production in rat kidney mesangial cells.All of the hydroxylated flavones were abbreviated as the positions of hydroxyl groups followed by—HO. The total production of nitrite in the treatment media was measured with Griess assay at 48 h post 10 ng/mL LPS stimulation. The nitrile level in the LPS treatment alone was used as 100%, and IC50 values were obtained using the dose-response analysis provided by the Graphpad Prism software as shown in parenthesis. Compounds of group 5 with IC50 >200 μM were not shown in the figure.
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pone.0116409.g001: Anti-inflammatory activity of mono-, di- and polyhydroxylated flavones on the LPS-induced NO production in rat kidney mesangial cells.All of the hydroxylated flavones were abbreviated as the positions of hydroxyl groups followed by—HO. The total production of nitrite in the treatment media was measured with Griess assay at 48 h post 10 ng/mL LPS stimulation. The nitrile level in the LPS treatment alone was used as 100%, and IC50 values were obtained using the dose-response analysis provided by the Graphpad Prism software as shown in parenthesis. Compounds of group 5 with IC50 >200 μM were not shown in the figure.

Mentions: A total of nineteen hydroxylated flavones including four monohydroxylated, four dihydroxylated, two trihydroxylated, four tetrahydroxylated, three pentahydroxylated and two hexahydroxylated flavones as representatives were screened for the potential anti-inflammatory activity on the LPS-induced NO production in kidney mesangial cells (Fig. 1). This compound list included several well reported bio-active hydroxylated flavones such as fisetin [15], quercetin [4,5], morin [2], tricetin [15], gossypetin [16], apigenin [2,4] and myricetin [2], which exhibit broad spectrum anti-inflammatory and anticancer effects.


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

Wang X, Wang Z, Sidhu PS, Desai UR, Zhou Q - PLoS ONE (2015)

Anti-inflammatory activity of mono-, di- and polyhydroxylated flavones on the LPS-induced NO production in rat kidney mesangial cells.All of the hydroxylated flavones were abbreviated as the positions of hydroxyl groups followed by—HO. The total production of nitrite in the treatment media was measured with Griess assay at 48 h post 10 ng/mL LPS stimulation. The nitrile level in the LPS treatment alone was used as 100%, and IC50 values were obtained using the dose-response analysis provided by the Graphpad Prism software as shown in parenthesis. Compounds of group 5 with IC50 >200 μM were not shown in the figure.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4366162&req=5

pone.0116409.g001: Anti-inflammatory activity of mono-, di- and polyhydroxylated flavones on the LPS-induced NO production in rat kidney mesangial cells.All of the hydroxylated flavones were abbreviated as the positions of hydroxyl groups followed by—HO. The total production of nitrite in the treatment media was measured with Griess assay at 48 h post 10 ng/mL LPS stimulation. The nitrile level in the LPS treatment alone was used as 100%, and IC50 values were obtained using the dose-response analysis provided by the Graphpad Prism software as shown in parenthesis. Compounds of group 5 with IC50 >200 μM were not shown in the figure.
Mentions: A total of nineteen hydroxylated flavones including four monohydroxylated, four dihydroxylated, two trihydroxylated, four tetrahydroxylated, three pentahydroxylated and two hexahydroxylated flavones as representatives were screened for the potential anti-inflammatory activity on the LPS-induced NO production in kidney mesangial cells (Fig. 1). This compound list included several well reported bio-active hydroxylated flavones such as fisetin [15], quercetin [4,5], morin [2], tricetin [15], gossypetin [16], apigenin [2,4] and myricetin [2], which exhibit broad spectrum anti-inflammatory and anticancer effects.

Bottom Line: 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.

View Article: PubMed Central - PubMed

Affiliation: Department of Nanomedicine and Biopharmaceuticals, College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan, Hubei, China.

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 treatment.

No MeSH data available.


Related in: MedlinePlus