This study aims to determine the function of Plectranthus barbatus (Lamiaceae) herbal tea as inhibitor of the brain acetylcholinesterase (AChE) activity. To accomplish this objective the herbal tea as well as its main component, rosmarinic acid were administered to laboratory animals (rats) and the effect on the brain AChE activity was evaluated. The study of the herbal tea metabolites in the plasma and also in the brain was undertaken. The herbal water extract was administered intragastrically and also intraperitoneally. When the plant extract was intragastrically administered, vestigial amounts of metabolites from P. barbatus extract compounds were present in rat plasma, but none were found in brain, although inhibition of brain acetylcholinesterase activity was detected. However, when P. barbatus extract was administered intraperitoneally, all its compounds were found in plasma, and rosmarinic acid was found in brain. The highest concentrations of compounds/metabolites were found 30 min after administration. An inhibition of 29.0 ± 2.3% and 24.9 ± 3.7% in brain acetylcholinesterase activity was observed 30 and 60 min after intraperitoneal administration, respectively. These values were higher than those expected, taking into account the quantity of rosmarinic acid detected in the brain, which suggests that other active extract compounds or metabolites may be present in non-detectable amounts. These results prove that the administration of P. barbatus aqueous extract can reach the brain and act as AChE inhibitor.