From Traditional Use to Experimental Evidence: Phytochemistry, Pharmacological Activities, Safety and Therapeutic Potential of Anthocleista grandiflora Gilg

Anthocleista grandiflora Gilg is an African medicinal tree used traditionally for malaria, fever, diabetes, diarrhoea and other conditions. This review critically assessed its ethnomedicinal uses, phytochemistry, pharmacological activities and safety. Studies published between 1949 and December 2024 were searched in Scopus, Web of Science, PubMed, ScienceDirect, Google Scholar and SciFinder. Taxonomy and distribution were verified using botanical databases. The bark, roots, leaves and twigs are used medicinally, particularly for malaria and fever. Species-specific isolation studies confirmed grandifloroside, methylgrandifloroside, sweroside, scopoletin, baruol, 3-deacetylmongolenin, anthocleistone, 6-ketoanthocleistone, lupenone and (+)-de-O-methyllasiodiplodin as constituents of A. grandiflora. Additional triterpenoids have been reported in conference and secondary literature, while compounds identified only through GC-MS library matching remain tentative. The strongest pharmacological finding was the activity of a twig dichloromethane extract against Plasmodium falciparum NF54, with an IC50 value of 2.12 µg/mL and selectivity index of 26. Antimicrobial, antileishmanial, antiviral, alpha-glucosidase-inhibitory, analgesic and anti-inflammatory effects were also reported, although most evidence came from preliminary laboratory studies. Safety information was limited and extract-specific. A. grandiflora contains a chemically diverse group of confirmed constituents and shows promising preclinical activities. Standardised extraction, compound-directed bioassays, pharmacokinetic studies and in vivo safety and efficacy investigations are required before clinical development.