Synthesis of andrographolide derivatives and their TNF-α and IL-6 expression inhibitory activities

The synthesis of a series of andrographolide derivatives was described and their inhibitory effects on TNF-α and IL-6 secretion in mouse macrophages were also evaluated. Most of the tested compounds showed inhibitory effects, and the compounds with the structure of 12-hydroxy-14-dehydroandrographolide showed better inhibitory activity than the compounds with the structure of isoandrographolide.

Andrographolide and its derivatives were evaluated in the ELISA for the inhibitory potency in the secretion of TNF-α and IL-6 of LPS-stimulated mouse macrophages. The derivatives 3e, 9e, 9f have better inhibitory effect than andrographolide.Figure optionsDownload as PowerPoint slide