The phytochemical investigations on Cleome droserifolia resulted in the isolation and characterization of a new indole alkaloid, 5-hydroxy-2-methoxy-1-methyl-1H-indole-3-carbaldehyde (1). The structure elucidation was carried out on the basis of 1D- and 2D-NMR techniques. In addition to 1, two known aromatic derivatives, veratrol (2) and 2-methoxy-4-methylacetophenone (3), were also obtained. All these compounds were purified by repeated column chromatography of the CH2Cl2 fraction obtained from MeOH extract of Cleome droserifolia. The structure of the new compound 1 was finally confirmed by the combined 1D (1H- and 13C-) and 2D (H-C correlations; HMBC and HSQC) NMR and IR spectroscopy, mass spectrometry (MS), and UV absorption spectroscopy techniques. The comparison of the physical and spectroscopic data with those in the literature provided evidence for the structure confirmation of known compounds. All the purified compounds were subjected to urease and α-glucosidase enzymes inhibition. The results showed that compound 1 was more potent with an IC50 value 11.97±2.067 μg/ml towards urease inhibition, while the activity of α-glucosidase enzyme was marginal. Copyright © 2015 Verlag Helvetica Chimica Acta AG, Zürich.