Annona muricata L., Annonaceae, is extensively used in Mexican traditional medicine for the treatment of gastrointestinal disorders, diabetes mellitus, and as antitumor. The ethanol extract of the leaves from A. muricata was suspended in 10% ethanol water and fractionated by organic solvent extraction with chloroform. The chloroform and aqueous residual fractions were tested for antiprotozoal, antipropulsive, antihyperglycemic, and antilymphoma activities, as well as brine shrimp lethality. While for the antiprotozoal, antilymphoma, and antihiperglycemic activities as well as brine shrimp lethality the chloroform fraction was the most active, the aqueous residual fraction provided better result for the antipropulsive activity. The aqueous residual and chloroform fractions were purified by chromatographic methods to give rutin, nicotinflorin, narcissin, and cis-reticulatacin, as well as β-sitosterol.