Here we describe the practical synthesis and biological properties of bergenin and its structural analogues. Synthetic bergenin compounds were prepared by acylation of bergenin. These compounds were then evaluated for suppression of lipopolysaccharide (LPS)-induced nitric oxide (NO) generation in cultured cells and anti-narcotic effects on morphine-dependent mice. We found that bergenin derivatives showed potent anti-inflammatory activity (suppression of NO generation) at concentrations ranging from 20-30 μM in vitro, and bergenin derivatives (10-20 mg/kg) exhibited significant anti-narcotic effects on morphine-dependence in mice. These results suggest the potential utility of bergenin and its analogues as anti-narcotic agents and the design of more potent anti-inflammatory compounds.