Madecassoside is a triterpenoid found in Centella that exhibits anti-inflammatory, antioxidative, anti-fibrotic, neuroprotective, and cardioprotective activities. In animal models of cerebral ischemia/reperfusion, madecassoside downregulates expression of malondialdehyde, NO, and pro-inflammatory cytokines, prevents apoptosis, decreases infarct size, and attenuates cognitive deficits. Madecassoside protects neurons against amyloid-β (Aβ)-induced inflammation and autophagy; it also shows potential benefit in animal models of Parkinson’s disease. Additionally, madecassoside downregulates expression of α-smooth muscle actin and TGF-β1, attenuates phosphorylation of Smad2/3, decreases myeloperoxidase activity and malondialdehyde levels, and increases superoxide dismutase and glutathione levels, ameliorating pulmonary fibrosis. This compound also decreases infarct size, lowers levels of lactate dehydrogenase, malondialdehyde, and creatine kinase, and suppresses apoptosis, providing protection in myocardial ischemia/reperfusion models.