Inspired by magnolol: design of NSAID-based compounds with excellent anti-inflammatory effects

Abstract

Magnolol is a major active constituent of Magnolia officinalis which is a natural traditional Chinese medicine. Inspired by magnolol which shows a wide diversity of bioactivities, a series of magnolol derivatives containing nonsteroidal anti-inflammatory drugs (NSAIDs) were designed, synthesized and screened for their anti-inflammatory activities by using a TPA-induced mouse ear edema model. These results indicated that in comparison with magnolol and ketoprofen, topical application of A10 (magnolol derivative containing ketoprofen) prior to TPA treatment markedly suppressed the expressions of IL-1β, IL-6 and TNF-α, respectively. Further mechanical investigations demonstrated that A10 inhibited IKK and IκBα phosphorylation, thereby suppressing the activation of p65. Accordingly, A10 may be a potent anti-inflammatory agent capable of preventing inflammation-associated edema.