<jats:title>Abstract</jats:title><jats:p>Bioassay‐guided fractionation of the dichloromethane extracts of the roots and the bark of <jats:italic>Zanthoxylum usambarense</jats:italic> led to the isolation of two physiologically active compounds, i.e. canthin‐6‐one <jats:bold>1</jats:bold> (fungicide) and pellitorine <jats:bold>4</jats:bold> (insecticide). Together with oxychelerythrine <jats:bold>2</jats:bold>, norchelerythrine <jats:bold>3</jats:bold>, (+)‐sesamin <jats:bold>5</jats:bold> and (+)‐piperitol‐3,3‐dimethylallyl ether <jats:bold>6</jats:bold>, they were isolated for the first time from this plant. Copyright © 2002 John Wiley & Sons, Ltd.