Ursolic acid (UA) is a pentacyclic
triterpenoid frequently found in medicinal herbs and plants, having numerous pharmacological effects. UA and its analogs treat multiple diseases, including
cancer,
diabetic neuropathy, and inflammatory diseases. UA inhibits
cancer proliferation,
metastasis, angiogenesis, and induced cell death, scavenging
free radicals and triggering numerous anti- and
pro-apoptotic proteins. The biochemistry of UA has been examined broadly based on the literature, with alterations frequently having been prepared on positions C-3 (
hydroxyl), C12-C13 (double bonds), and C-28 (
carboxylic acid), leading to several UA derivatives with increased potency, bioavailability and water solubility. UA could be used as a
protective agent to counter neural dysfunction via
anti-oxidant and anti-inflammatory effects. It is a potential therapeutic drug implicated in the treatment of
cancer and
diabetic complications diseases provide novel machinery to the anti-inflammatory properties of UA. The pharmacological efficiency of UA is exhibited by the therapeutic theory of one-drug → several targets → one/multiple diseases. Hence, UA shows promising therapeutic potential for
cancer and
diabetic neuropathy diseases. This review aims to discuss mechanistic insights into promising beneficial effects of UA. We further explained the pharmacological aspects, clinical trials, and potential limitations of UA for the management of
cancer and
diabetic neuropathy diseases.