Recently, we identified a novel ginseng-derived lysophosphatidic acid (LPA) receptor ligand, called gintonin. We showed that gintonin induces [Ca2+]i transient-mediated morphological changes, proliferation, and migration in cells expressing LPA receptors and that oral administration of gintonin exhibits anti-Alzheimer’s disease effects in model mice. However, little is known about the intestinal absorption of gintonin. The aim of this study was to investigate gintonin absorption using two model systems.