Theanine, an amino acid contained in green tea, is known to possess many pharmacological functions. In this paper, we investigated the absorption of theanine in the human intestinal epithelium, using a Caco-2 monolayer model. Different concentrations of either pure theanine or green tea extracts were administered to Caco-2 cells. The theanine content in the samples was analysed by high-performance liquid chromatography coupled with fluorescence detection. Cell permeation was also measured. The data revealed that the transport of pure theanine occurred in a manner consistent with passive diffusion. Surprisingly, pure theanine showed good absorption, whereas theanine in the green tea extract was poorly absorbed in the Caco-2 cell model. Furthermore, the transport of theanine in green tea extract in the basolateral (BL) to apical (AP) direction was much greater than that in the AP-BL direction, suggesting that green tea components profoundly affect the trans-epithelial transport of theanine in this Caco-2 cell model. (C) 2010 Elsevier Ltd All rights reserved.