Pentacyclic triterpenoids represent a significant class of phytochemicals , categorized into oleanane, ursane, friedelane, and lupane. Among these, betulonic acid stands out as a lupane-type pentacyclic triterpenoid found in numerous plants. Its diverse biological properties, including anti-tumor, anti-viral, anti-inflammatory, anti-bacterial, and hepato-protective effects, have been extensively documented. To further explore the therapeutic potential of betulonic acid and its derivatives, we provide a comprehensive review of their sources, biological activities , and molecular mechanisms. We aim for this synthesis of data to stimulate fresh perspectives on betulonic acid and its potential in drug discovery . • Betulonic acid: A lupane-type triterpenoid with anti-tumor, anti-viral, anti-inflammatory, anti-bacterial effects. • Betulonic acid is sourced from plants, semi-synthesized, and can also be produced through microbial biotransformation. • Characterization of betulonic acid reveals overlooked biological properties. • Provides a novel insights, as well as a theoretical basis for the development of betulonic acid.