Medicinal plants remain vital resources for drug discovery, and Heliotropium species are recognized for their extensive ethnomedicinal use and diverse bioactive compounds. Despite their therapeutic potential, safety concerns related to pyrrolizidine alkaloids necessitate critical evaluation. This review synthesizes the literature on the taxonomy, ethnobotanical applications, phytochemistry, pharmacology, and toxicology of Heliotropium species. A systematic literature search was conducted following the principles of PRISMA (Preferred Reporting Items for Systematic Reviews and Meta-Analyses). Relevant publications were retrieved from major scientific databases, including Scopus, Web of Science, PubMed, Google Scholar, and ScienceDirect. Peer-reviewed articles, ethnopharmacological surveys, and toxicological studies published between 2000 and 2025 were screened and evaluated. After the removal of duplicates and the application of predefined inclusion criteria, relevant studies were selected for qualitative synthesis. More than 325 Heliotropium species are distributed worldwide, many of which are traditionally used to treat inflammatory conditions, infections, gastrointestinal disorders, and skin ailments. Phytochemical analyses reveal abundant secondary metabolites, including alkaloids, flavonoids, terpenoids, and phenolic acids. These compounds underpin diverse pharmacological effects, such as antioxidant, antimicrobial, anticancer, anti-ulcer, and anti-inflammatory activities. Essential oils from several species exhibit unique chemotypes with ecological and therapeutic significance. However, toxicological evidence indicates that pyrrolizidine alkaloids pose hepatotoxic and genotoxic risks, thereby limiting the safe clinical use of these plants. Heliotropium represents both an opportunity and a challenge: a valuable reservoir of novel bioactive compounds for drug discovery, yet one that requires cautious therapeutic application due to associated toxicity risks.
Adedoyin et al. (Sat,) studied this question.
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