title: Biological evaluation of synthetic chalcone and flavone derivatives as anti-inflammatory agents.
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 IC50of 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 OCH3on both A and B rings of synthetic compounds correlate to stronger anti-inflammatory potency.
authors: College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL 32307, USA.
authors: Nelly
authors: N
authors: Mateeva
authors: College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL 32307, USA.
authors: Madhavi
authors: M
authors: Gangapuram
authors: College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL 32307, USA.
authors: Elizabeth
authors: E
authors: Mazzio
authors: College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL 32307, USA.
authors: Suresh
authors: S
authors: Eyunni
authors: College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL 32307, USA.
authors: Karam F A
authors: KF
authors: Soliman
authors: Division of Research, Florida A&M University, 410 Foote-Hilyer Administration Center, Tallahassee, FL 32307, USA kinfe.redda@famu.edu.
authors: Kinfe K
authors: KK
authors: Redda
keywords: Chalcones; Cytokines; Flavonoids; Microglial cells; Nitric oxide