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6-Hydroxyflavone and Derivatives Exhibit Potent Anti-Inflammatory Activity among Mono-, Di- and Polyhydroxylated Flavones in Kidney Mesangial Cells
| Content Provider | Semantic Scholar |
|---|---|
| Author | Wang, Xing Wang, Zhiwei Sidhu, Preetpal Singh Desai, Umesh R. Zhou, Qibing |
| Copyright Year | 2015 |
| 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. |
| File Format | PDF HTM / HTML |
| DOI | 10.1371/journal.pone.0116409 |
| PubMed reference number | 25790236 |
| Journal | Medline |
| Volume Number | 10 |
| Alternate Webpage(s) | http://journals.plos.org/plosone/article/file?id=info:doi/10.1371/journal.pone.0116409.s003&type=supplementary |
| Alternate Webpage(s) | http://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0116409&type=printable |
| Alternate Webpage(s) | http://ftp.ncbi.nlm.nih.gov/pub/pmc/80/4c/pone.0116409.PMC4366162.pdf |
| Alternate Webpage(s) | https://scholarscompass.vcu.edu/cgi/viewcontent.cgi?article=1017&context=medc_pubs |
| Alternate Webpage(s) | https://doi.org/10.1371/journal.pone.0116409 |
| Journal | PloS one |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |