Compared with the parent compound resveratrol, pterostilbene has the phenolic hydroxyl groups at positions 3 and 5 replaced by methoxy groups. This structural change gives it higher lipid solubility, chemical stability and bioavailability, enabling it to more effectively penetrate the cell membrane and maintain a higher active concentration in the body. Therefore, it is hailed as "the second-generation resveratrol".

Pterostilbene has a wide range of biological activities, including strong antioxidant, anti-inflammatory, anti-tumor, anti-aging, neuroprotective and cardiovascular protective effects. Its mechanism of action mainly involves activating the nuclear factor-related factor 2 (Nrf2) signaling pathway, inhibiting the nuclear factor κB (NF-κB) inflammatory pathway, regulating the silent information regulator 1 (SIRT1) pathway and inducing autophagy in cells.