The purpose of this review article is to comprehensively summarize the anticancer potential of Ursolic Acid (UA) by elucidating its underlying molecular mechanisms, therapeutic efficacy, and formulation advancements. It aims to highlight UA’s multifunctional role in modulating key cancer-related pathways and discuss recent progress in nano-formulation strategies designed to overcome its poor solubility and bioavailability, thereby facilitating its clinical translation. This review employs a comprehensive analysis of existing preclinical and limited clinical studies on UA, focusing on its molecular mechanisms and anticancer activities. It systematically examines literature related to key signalling pathways, therapeutic effects, and formulation advancements. Additionally, it evaluates nano-formulation approaches and combination therapies aimed at improving UA’s bioavailability and clinical applicability. The review reveals that UA demonstrates strong anticancer potential by inducing apoptosis, autophagy, and cell cycle arrest through modulation of key pathways like PI3K/Akt/mTOR, STAT3, and NF-κB. It suppresses metastasis, angiogenesis, and epithelial-mesenchymal transition, enhances antioxidant defence, and triggers ROS-mediated apoptosis. UA’s epigenetic modulation contributes to its anti-proliferative effects, while nano formulations improve its solubility, bioavailability, and targeted delivery, with early clinical studies showing good tolerance and preliminary signs of therapeutic benefit.UA emerges as a promising natural anticancer agent capable of targeting multiple molecular pathways involved in tumor growth and progression. Despite its broad preclinical efficacy, its poor solubility and low bioavailability limit clinical application. Advances in nano-formulation strategies have shown potential to overcome these challenges. However, extensive clinical investigations and standardized formulations are essential for successful therapeutic translation.
Patil et al. (Fri,) studied this question.