Paeoniflorin is found in Paeonia; it exhibits anti-inflammatory, antioxidative, neuromodulatory, antidepressant, analgesic, and anticancer chemotherapeutic activities. In animal models of DSS-induced colitis, paeoniflorin decreases expression of toll-like receptor 4 (TLR4), inhibits production of IL-6 and TNF-α, and suppresses activity of myeloperoxidase. Paeoniflorin also scavenges ROS by inhibiting expression of NADPH oxidase, decreasing oxidative stress in animal models. Paeoniflorin decreases immobility in animals undergoing the forced swim test and tail suspension test and increases levels of 5-HT in the hippocampus. Additionally, paeoniflorin inhibits cell and tumor growth and induces G1 phase cell cycle arrest in cellular and animal models of colorectal cancer. This compound also decreases hyperalgesia in animal models and inhibits L-type voltage-gated Ca2+ channels.