ABSTRACT
Flavonoids are compounds based on a 2-phenylchromonone scaffold. Flavonoids can be divided into flavonoids, flavonols, dihydroflavones, anthocyanins, chalcones and diflavones according to the oxidation degree of the central tricarbonyl chain, the connection position of B-ring (2-or 3-position), and whether the tricarbonyl chain forms a ring or not. There are a variety of biological activities about flavonoids, such as anti-inflammatory activity, anti-oxidation and anti-tumor activity, and the antiinflammatory activity is apparent. This paper reviews the anti-inflammatory activities and mechanisms of flavonoids and their derivatives reported in China and abroad from 2011 till date (2011-2020), in order to find a good drug scaffold for the study of anti-inflammatory activities.
Subject(s)
Anti-Inflammatory Agents/chemical synthesis , Anti-Inflammatory Agents/pharmacology , Drug Discovery , Flavones/chemical synthesis , Flavones/pharmacology , Anti-Inflammatory Agents/chemistry , Humans , Molecular Structure , Structure-Activity RelationshipABSTRACT
A series of novel 4-ferrocenylchroman-2-one derivatives were designed and synthesised to discover potent anti-inflammatory agents for treatment of arthritis. All the target compounds had been screened for their anti-inflammatory activity by evaluating the inhibition effect of LPS-induced NO production in RAW 264.7 macrophages. Among them, 4-ferrocenyl-3,4-dihydro-2H-benzo[g]chromen-2-one (3h) was found to be the most potent compound in inhibiting the productions of NO with low toxicity. This compound also exhibited significant inhibition of the productions of IL-6 and TNF-α in RAW 264.7 macrophages. Preliminary mechanism studies indicated that compound 3h could inhibit the activation of LPS-induced NF-κB and MAPKs signalling pathways. The in vivo anti-inflammatory effect of this compound was determined in the rat adjuvant-induced arthritis model.
