Kakino Mamoru, Izuta Hiroshi, Ito Tetsuro, Tsuruma Kazuhiro, Araki Yoko, Shimazawa Masamitsu, Oyama Masayoshi, Iinuma Munekazu, Hara Hideaki
Department of Biofunctional Evaluation, Molecular Pharmacology, Gifu Pharmaceutical University, Gifu, Japan.
Biosci Biotechnol Biochem. 2010;74(8):1550-5. doi: 10.1271/bbb.100122. Epub 2010 Aug 7.
Agarwood (Aquilaria sinensis, Aquilaria crasna) is well known as an incense in the oriental region such as Thailand, Taiwan, and Cambodia, and is used as a digestive in traditional medicine. We investigated the laxative effects and mechanism of agarwood leaves extracted with ethanol (EEA-1, Aquilaria sinensis; EEA-2, Aquilaria crasna). EEA-1, EEA-2, the main constituents of EEAs (mangiferin, and genkwanin-5-O-primeveroside), and senna increased the frequency and weight of stools in loperamide-induced constipation model mice. EEA-1 and EEA-2 did not induce diarrhea as a side effect, but senna induced severe diarrhea. EEA-1 and senna increased gastro-intestinal (GI) transit in the model mice. EEA-1, but not senna, also increased the intestinal tension of isolated jejunum and ileum in guinea pigs, and the tension increase was blocked by atropine, a muscarinic receptor antagonist, but not by other inhibitors (granicetron, pyrilamine, or bradykinin-antagonist peptide). Furthermore, the increase in frequency and weight of stools induced by EEA-1 were blocked by pre-administration of atropine in the model mice. These findings indicate that EEAs exerted a laxative effect via acetylcholine receptors in the mouse constipation model.
沉香（白木香、土沉香）在泰国、台湾和柬埔寨等东方地区作为香料而闻名，并在传统医学中用作消化剂。我们研究了用乙醇提取的沉香叶（EEA-1，白木香；EEA-2，土沉香）的通便作用及其机制。EEA-1、EEA-2、EEAs的主要成分（芒果苷和芫花素-5-O-樱草糖苷）以及番泻叶均增加了洛哌丁胺诱导的便秘模型小鼠的粪便频率和重量。EEA-1和EEA-2未引起腹泻副作用，但番泻叶引起严重腹泻。EEA-1和番泻叶增加了模型小鼠的胃肠（GI）转运。EEA-1而非番泻叶还增加了豚鼠离体空肠和回肠的肠张力，且张力增加被毒蕈碱受体拮抗剂阿托品阻断，而非被其他抑制剂（格拉司琼、苯吡胺或缓激肽拮抗剂肽）阻断。此外，在模型小鼠中预先给予阿托品可阻断EEA-1诱导的粪便频率和重量增加。这些发现表明，在小鼠便秘模型中，EEAs通过乙酰胆碱受体发挥通便作用。
