Momordicine I is a natural cucurbitane-type triterpene exhibiting antihypertensive, anti-inflammatory, anti-hypertrophic, anti-fibrotic, and antioxidant properties. Its mechanisms of action include regulating insulin signalling, inducing cancer cell apoptosis, and modulating NO, ACE, PI3K/Akt, NF-kappaB, Nrf2, c-Met/STAT3 pathways, and may be applied in cardiovascular diseases and inflammation.