<jats:title>Abstract</jats:title><jats:p>This paper describes the chemical investigation on BuOH‐soluble EtOH extract from the aerial part of <jats:italic>Sauropus androgynus</jats:italic>. This study led to the characterization of six bioactive ingredients including three nucleosides—adenosine (1), 5′‐deoxy‐5′‐methylsulphinyl‐adenosine (<jats:bold>2</jats:bold>), and uridine (<jats:bold>3</jats:bold>), two flavonol dioside — 3‐<jats:italic>O</jats:italic>‐β‐D‐glucosyl‐7‐<jats:italic>O</jats:italic>‐α‐L‐rhamnosyl‐kaempferol (<jats:bold>4</jats:bold>), 3‐<jats:italic>O</jats:italic>‐β‐D‐glucosyl‐(1→6)‐β‐D‐glucosyl‐kaempferol (<jats:bold>5</jats:bold>), and one rare flavonol trioside — 3‐<jats:italic>O</jats:italic>‐β‐D‐glucosyl‐(1→6)‐β‐D‐glucosyl‐7‐<jats:italic>O</jats:italic>‐α‐L‐rhamno‐syl‐kaempferol (<jats:bold>6</jats:bold>). Their structures were determined on the basis of spectral analysis.