Andrographolide

Andrographolide is a diterpene lactone and bioactive phytochemical derived from Andrographis paniculata. It is being investigated primarily in preclinical pharmacology, including studies of inflammation, cancer, pulmonary injury, enzyme inhibition, metabolism, and drug-delivery systems. Reported activities include modulation of inflammatory signaling and inhibition of acetylcholinesterase (AChE); in extracts of A. paniculata, andrographolide showed an AChE-inhibitory activity with an IC₅₀ of 97.1 μM.

Recent studies describe several context-dependent mechanisms. In an allergic-rhinitis mouse model, andrographolide alleviated nasal mucosal inflammation through inhibition of the IL-17/NF-κB pathway and downregulation of MUC5AC expression. In acute lung injury research, a neutrophil-targeted andrographolide liposome was developed to inhibit neutrophil extracellular trap formation (NETosis). Anticancer studies have examined andrographolide in combination with paclitaxel, cytarabine, vincristine, berbamine, or gemcitabine, with reported investigations involving apoptosis, reactive oxygen species, mitochondrial dysfunction, RRM2, and JAK/STAT3 signaling. Its lipophilicity and resulting low plasma concentrations have prompted investigation of nanoemulsions, liposomes, and other delivery systems. In mice, its hepatic metabolism has been associated with CYP2D22 and CYP2C29, including during analysis of Liandan Xiaoyan Formula metabolism in ulcerative-colitis models.