Agarwood induced laxative effects via acetylcholine receptors on loperamide-induced constipation in mice.
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.
Kakino
Mamoru
M
Department of Biofunctional Evaluation, Molecular Pharmacology, Gifu Pharmaceutical University, Gifu, Japan.
Izuta
Hiroshi
H
Ito
Tetsuro
T
Tsuruma
Kazuhiro
K
Araki
Yoko
Y
Shimazawa
Masamitsu
M
Oyama
Masayoshi
M
Iinuma
Munekazu
M
Hara
Hideaki
H
D000818:Animals; D001285:Atropine / Q000494:pharmacology; D018680:Cholinergic Antagonists / Q000494:pharmacology; D003248:Constipation / Q000139:chemically induced* / Q000188:drug therapy* / Q000378:metabolism; D003967:Diarrhea / Q000139:chemically induced; D000431:Ethanol / Q000737:chemistry; D005260:Female; D005772:Gastrointestinal Transit / Q000187:drug effects; D006168:Guinea Pigs; D007422:Intestines / Q000187:drug effects / Q000503:physiopathology; D054368:Laxatives / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D008139:Loperamide / Q000494:pharmacology*; D008297:Male; D051379:Mice; D010936:Plant Extracts / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D018515:Plant Leaves / Q000737:chemistry; D011950:Receptors, Cholinergic / Q000378:metabolism*; D029645:Thymelaeaceae / Q000737:chemistry*
D018680:Cholinergic Antagonists; D054368:Laxatives; D010936:Plant Extracts; D011950:Receptors, Cholinergic; D000431:Ethanol; D008139:Loperamide; D001285:Atropine