Background. Increasing antimicrobial resistance has led to an arduous search for new potent drugs from nature. In this search, plants have proved to be rich reservoirs of efficacious medicinal components that manage ailments. The current study is designed to investigate the phytochemical composition, antimicrobial activity, and the cytotoxicity of the crude root extracts of Croton dichogamus, a shrub that is commonly used in the eastern Africa for the management of infectious diseases. Methods. The roots of Croton dichogamus were obtained, dried, ground, and extracted using three solvents (acetone, distilled water, and 50% ethanol). The antimicrobial activity was tested using agar well diffusion and microbroth dilution techniques against five human pathogens. The brine shrimp lethality assay was used to assess the toxic effect. Results. The phytochemical screening indicated the presence of terpenoids, flavonoids, tannins, phenols, polyuronides, saponins, and anthracenes. The brine shrimp lethality assay indicated that all the extracts were highly cytotoxic with LC50 values below 100 μg/ml. Acetonic extract had an LC50 value of 4.148 μg/ml, hydroethanolic extract had 76.09 μg/ml, and aqueous extract had 42.61 μg/ml. All extracts showed the antibacterial activity against Gram-positive bacteria (B. cereus and S. aureus) and a fungal organism, C. albicans. The extracts showed no antibacterial effect on the Gram-negative bacterial strains (P. aeruginosa and E. coli) at a concentration of 250 mg/ml. The highest antimicrobial activity was demonstrated by the acetonic extract on B. cereus which had an MIC of 10.42 mg/ml and a zone of inhibition of 17.33 ± 0.58 at a concentration of 250 mg/ml. Conclusion. In this research work, we report that C. dichogamus had the antimicrobial activity confirming the folklore claim. The results made a strong case for isolation of novel anticancer lead compounds.