The genus Plectranthus, belonging to the Lamiaceae family, has emerged as a valuable source of bioactive natural products, particularly abietane-type diterpenoids. These compounds, rooted in traditional medicinal practices, have gained attention for their diverse pharmacological properties and potential as drug leads. Abietanes isolated from Plectranthus species exhibit a wide range of biological activities, including antimicrobial, anti-inflammatory, and anticancer effects, making them attractive scaffolds for therapeutic development.This presentation highlights the translational journey of Plectranthus-derived abietanes from ethnobotanical relevance to preclinical evaluation. Notable examples include Parvifloron D from P. ecklonii and 7α-acetoxy-6β-hydroxyroyleanone from P. grandidentatus, both demonstrating significant bioactivity. A particular focus is placed on dibenzoylroyleanone (RoyBz), a patented abietane diterpenoid with selective activation of protein kinase C (PKC) and potent antiproliferative effects in colon cancer models. Mechanistic studies reveal that RoyBz induces apoptosis via a PKCδ-mediated mitochondrial pathway and disrupts cancer cell metabolism, underscoring its promise as a drug candidate.By integrating phytochemical profiling, pharmacological screening, and molecular investigations, this work reinforces the role of Plectranthus species as a rich source of novel therapeutic agents. It also emphasizes the importance of preserving traditional knowledge and validating it through modern scientific approaches to support sustainable drug discovery from natural products.