The present invention relates to a pharmaceutical composition and a health food composition for the prevention and treatment of immune- and autoimmune diseases such as septic shock, hemorrhagic shock, rheumatoid arthritis, osteoarthritis, inflammatory bowel disease and multiple sclerosis, and metabolic diseases such as arteriosclerosis and type II diabetes, and an inducible nitric oxide synthase (iNOS) inhibitor composition containing theopederin derivatives as an active ingredient. The composition of the present invention can be effective in the prevention and treatment of immune diseases and metabolic diseases by inhibiting the excessive generation of NO by inhibiting the activity of iNOS.