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- W1983291282 abstract "Flavonoids and chalcones are natural plant derived compounds with inherent therapeutic value for a range of human pathologies. In this study, a series of 24 substituted chalcones and flavones were synthesized and subsequently screened for anti-inflammatory effects on lipopolysaccharide (1 µg/ml)-activated BV-2 microglial cells by assessing initial production/release of nitric oxide (NO). The data obtained eliminate the majority of compounds as weak or non-effective, whereas 2′-hydroxy-3,4,5,3′,4′-pentamethoxychalcone (1) and 2′-hydroxy-3,4,5-trimethoxychalcone (2) were potent, having an IC50 of 1.10 and 2.26 μM, respectively; with greater potency than L-N6-(1-iminoethyl)lysine selective iNOS inhibitor (IC50 = 3.1 μM) but less than steroidal dexamethasone (IC50 < 200 nM). The most potent compound (chalcone 1) attenuated NO parallel to reducing iNOS protein expression, events also corresponding to reduction of IL-1α, IL-10 and IL-6 pro-inflammatory cytokines. These findings suggest that the presence of electron donating groups OH and OCH3 on both A and B rings of synthetic compounds correlate to stronger anti-inflammatory potency." @default.
- W1983291282 created "2016-06-24" @default.
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- W1983291282 date "2014-09-07" @default.
- W1983291282 modified "2023-09-25" @default.
- W1983291282 title "Biological evaluation of synthetic chalcone and flavone derivatives as anti-inflammatory agents" @default.
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- W1983291282 doi "https://doi.org/10.1007/s00044-014-1214-7" @default.
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