Genipin is an iridoid glycoside compound found in zhishi or Gardenia jasminoides; it is most well known for its protein cross-linking ability. Genipin displays anti-amnestic, wound healing, anticancer, neuroprotective, cognition enhancing, anti-inflammatory, and antioxidative activities. In animal models, genipin inhibits acetylcholine esterase (AChE) , attenuating scopolamine-induced memory impairment. In ex vivo and in vivo models, genipin increases wound healing by inducing cross-linking of collagen. Genipin also exerts anticancer activity, as it increases the Bax/Bcl-2 ratio and induces PARP cleavage and caspase-3- and caspase-9-mediated apoptosis in non-small cell lung cancer (NSCLC) cells. In animal models, this compound upregulates nNOS and decreases acute inflammation through inhibition of LPS-induced NF-κB activity. Additionally, genipin inhibits Toll-like receptor (TLR) signaling and the production of pro-inflammatory cytokines, preventing sepsis and increasing survival in animal models of infection. Genipin also upregulates mitochondrial uncoupling protein 2 (UCP2) levels in the kidney, postponing progression of diabetic neuropathy in vivo.