Abstract
The roots of Litsea cubeba (Lour.) Pers have been used for the treatment of rheumatic. In the previous study, we extracted and isolated the natural product dibenzylbutane lignan LCA with anti-inflammatory activity. With LCA as the lead compound, two series of LCA derivatives with imide structure and butadiene structure were designed and synthesized. Among them, compounds 10c and 16a showed stronger inhibitory effect on LPS-induced NO and ROS production in RAW264.7 cells. Further studies showed that compound 16a not only reduced the levels of inflammatory cytokines IL-6, TNF-α, and IL-1β, but also significantly reduced the expression levels of iNOS and COX-2. Preliminary mechanism of action studies suggests that 16a may exert anti-inflammatory effects by inhibiting the NF-κB signalling pathway. Overall, compound 16a may be used as a promising anti-inflammatory drug to enrich the compound library. In addition, the study of 16a could provide research ideas and methods for the development of anti-inflammatory drugs.