Centro de Química e Bioquímica, Faculdade de Ciências da Universidade de Lisboa, Campo Grande, 1749-016 Lisboa, Portugal.
Food Funct. 2011 Feb;2(2):130-6. doi: 10.1039/c0fo00070a. Epub 2010 Dec 13.
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.
本研究旨在确定普列兰（唇形科）草药茶作为脑乙酰胆碱酯酶（AChE）抑制剂的功能。为了实现这一目标，给实验室动物（大鼠）服用草药茶及其主要成分迷迭香酸，并评估其对大脑 AChE 活性的影响。研究了草药茶在血浆和大脑中的代谢物。草药水提取物通过灌胃和腹腔内给药。当植物提取物通过灌胃给药时，在大鼠血浆中存在普列兰提取物化合物的痕量代谢物，但在大脑中未发现，尽管检测到大脑乙酰胆碱酯酶活性抑制。然而，当普列兰提取物通过腹腔内给药时，其所有化合物都存在于血浆中，并且在大脑中发现了迷迭香酸。给药后 30 分钟检测到化合物/代谢物的最高浓度。腹腔内给药 30 和 60 分钟后，大脑乙酰胆碱酯酶活性分别抑制 29.0±2.3%和 24.9±3.7%。这些值高于预期值，考虑到在大脑中检测到的迷迭香酸的量，这表明可能存在其他活性提取物化合物或代谢物，但无法检测到。这些结果证明，普列兰水提取物的给药可以到达大脑并作为 AChE 抑制剂发挥作用。
