Unveiling the multi-targeted therapeutic potentials of vernonia amygdalina: a comprehensive review of bioactive compounds, molecular mechanisms, and clinical opportunities

Abstract

Vernonia amygdalina (bitter leaf) has been used as traditional medicine across Africa and beyond because of its diverse pharmacological activities. While previous studies have validated its therapeutic potentials, a comprehensive understanding of the underlying molecular mechanisms driving these effects remains incomplete. This review critically examines the bioactive compounds present in V. amygdalina, their documented pharmacological effects, and the potential therapeutic applications of this plant, focusing specifically on elucidating the key molecular pathways modulated by its constituents. A systematic literature search was conducted using Web of Science, Scopus, PubMed, and ScienceDirect. Identification and analyses of a wide array of bioactive compounds, including sesquiterpene lactones (vernodalin, vernolepin), flavonoids (luteolin, apigenin), and saponins were carried out. Critical analyses revealed that these compounds exert their effects through multiple, interconnected pathways, including but not limited to: the method of extraction, their robust antioxidant and cytoprotective effects, and the direct cytotoxic effects on cancer cells through induction of apoptosis and cell cycle arrest. Bitter leaf used in the traditional treatment of: malaria, diabetes, and gastrointestinal disorders in light of these established mechanisms, its antimicrobial properties and its effectiveness in managing metabolic syndromes were discussed. However, significant challenges remain in translating V. amygdalina’s therapeutic benefits into standardized and safe clinical applications include: variability in bioactive compound concentrations due to environmental factors and preparation methods, limited data on human bioavailability and pharmacokinetics and a lack of rigorous clinical trials demonstrating efficacy and safety. Addressing these challenges through targeted research into optimized extraction techniques, formulation development, and well-designed clinical studies are crucial. Bitter leaf represents a promising source of novel drug leads, particularly for the development of multi-targeted therapies for complex diseases. Future research should prioritize the identification and validation of specific bioactive compounds responsible for the observed effects and the elucidation of their detailed molecular mechanisms of action.

Received on, 16 February 2025

Accepted on, 17 March 2025

Published on, 28 April 2025