1. Tetrahydrocoptisine has effective effects in suppressing inflammation. 2. Tetrahydrocoptisine possesses a protective effect on LPS-induced ALI through inhibiting of NF-κB signaling pathways, which may involve the inhibition of pulmonary inflammatory process. 3. Tetrahydrocoptisine has gastroprotective activity, is attributed to reducing NO production and adjusting the pro-inflammatory cytokine, inhibited neutrophil accumulation and NF-κB expression. 4. Tetrahydrocoptisine is an active anti-inflammatory constituent by inhibition of TNF-α, IL-6 and NO production possibly via down-regulation of NF-κB activation, phospho-ERK1/2 and phospho-p38MAPK signal pathways.