Plant triterpenoids, a vast and diverse group of natural compounds derived from six isoprene units, exhibit an extensive array of structural diversity and remarkable biological activities. In this review, we update the recent research progress in the catalytic mechanisms underlying triterpene synthesis and summarize the current insights into the biosynthetic pathways and regulatory mechanisms of triterpenoids. We emphasize the biosynthesis of pharmacologically active triterpenoids and the role of triterpenoid synthesis in plant growth, development, defense mechanisms, and plant-microbe interactions. This insight review offers a comprehensive perspective on the applications and future avenues of triterpenoid research.