[Gastrointestinal inhibitory effects of sesquiterpene lactones from Atractylodes macrocephala].
Atractylenolide I (8,9-dehydroasterolide, B), 4,15-epoxy-8 beta-hydroxyasterolide (C) and atractylenolide III (8 beta-hydroasterolide, D) from Atractylodes macrocephala Koidz, 28.0, 56.0 mumol/L, inhibited the spontaneous movement of rat isolated ileum with contractile force decreased obviously (P < 0.001), but the rest force not affected (P > 0.05). B, C and D inhibited the spasm enhanced by Ach and His to rat ileum, rightly shifted the dose-response curves and reduced the maximal response (P < 0.05). Pretreatment with B, C or D 28.0, 56.0 mumol/L Ver 0.28 mumol/L significantly antagonized CaCl2-induced contraction of rat isolated ileum. Co bathing of B, C or D 56.0 mumol/L with Atr 0.19 mumol/L weakened the response of ileum to Ach. B, C or D 56.0 mumol/L restrained the spasm of ileum mediated by Neo 2.15 mumol/L. The modified Phenol Red Paste Model demonstrated that B, C or D in dose of 28.0 mg/kg inhibited the gastrointestinal prochoresis of mice significantly. These results suggested that B, C and D inhibit the gastrointestinal movement of rat and the spasm induced by the agonists. Their activities are related to the inhibition of cholinergic system and Ca2+.
Zhang
Y
Y
Zhongshan University, Guangzhou 510275.
Xu
S
S
Lin
Y
Y
D000818:Animals; D031174:Atractylodes / Q000737:chemistry*; D018680:Cholinergic Antagonists / Q000494:pharmacology; D005769:Gastrointestinal Motility / Q000187:drug effects; D007082:Ileum / Q000187:drug effects; D007783:Lactones / Q000302:isolation & purification / Q000494:pharmacology*; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects; D010946:Plants, Medicinal / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D027343:Rhizome / Q000737:chemistry; D012717:Sesquiterpenes / Q000302:isolation & purification / Q000494:pharmacology*
C424803:4,15-epoxy-8-hydroxyasterolide; D018680:Cholinergic Antagonists; D007783:Lactones; D012717:Sesquiterpenes; C424804:atractylenolide I; C424802:atractylenolide III