The phytochemical analysis of Heliotropium undulatum [Heliotropium bacciferum] revealed the presence of alkaloids, saponins, tannins, steroids, terpenoids, flavonoids, glycosides, and phenols. While, Heliotropium europaeum was shown to contain three major alkaloids: heliotrine N-oxide 0.08%, lasiocarpine 0.09% and lasiocarpine N-oxide 0.05%; and four minor alkaloids: heliotrine 0.02%, europine 0.02%, acetyllasiocarpine 0.03% and a novel alkaloid acetyllasiocarpine N-oxide 0.05%. Twenty six compounds were identified in the essential oil of Heliotropium europaeum. The previous pharmacological studies showed that these species possessed antioxidant, antimicrobial, anti-inflammatory and hapatoprotective effects. However, pyrrolizidine alkaloids were toxic for animals and human. This review was designed to highlight the chemical constituents, pharmacological and toxic effects of Heliotropium undulatum [Heliotropium bacciferum] and Heliotropium europaeum. Keywords: chemical constituents, pharmacology, toxicology,Heliotropium undulatum, Heliotropium bacciferum, Heliotropium europaeum