Antagonistic effects of 3 sesquiterpene lactones from Atractylodes macrocephala Koidz on rat uterine contraction in vitro.
OBJECTIVE
To study the effects of three sesquiterpene lactones: atractylenolide I (8,9-dehydroasterolide, B), 4,15-epoxy-8 beta-hydroxyasterolide (C), and atractylenolide III (8 beta-hydroasterolide, D) from Atractylodes macrocephala Koidz, on rat isolated uterus smooth muscle.


METHODS
Rat isolated uteri bathed in De Jalon I solution were used; acetylcholine (ACh), CaCl2, and oxytocin (Oxy) were used to evoke the contraction of uterus.


RESULTS
B, C, and D 28 or 56 mumol.L-1 inhibited the spontaneous movement of uterus, reducing their rest force, contractile force, and movement ability. B 28 or 56 mumol.L-1 also slowed down the frequency of uterus spontaneous contraction, but C or D did not. B, C, or D 28 and 56 mumol.L-1 inhibited the uterine spasm induced by Oxy and ACh. Likewise, Ver 0.28 mumol.L-1, B, C, and D 28 or 56 mumol.L-1 relieved the contraction mediated by CaCl2 in high-KCl solution, but B, C, or D had not marked influence on the maximal response of uterus to CaCl2.


CONCLUSIONS
B, C, and D inhibit the movement of uterus smooth muscle, and the mechanism is related to the inhibition of cholinergic system as well as Ca2+ movement.
Zhang
Y Q
YQ
Laboratory of Pharmacy & Pharmacology, Department of Pharmacy, School of Life Sciences, Guangzhou 510275, China.
Xu
S B
SB
Lin
Y C
YC
Li
Q
Q
Zhang
X
X
Lai
Y R
YR
D000109:Acetylcholine / Q000037:antagonists & inhibitors; D000818:Animals; D001693:Biological Transport, Active; D002118:Calcium / Q000378:metabolism; D018680:Cholinergic Antagonists; D004365:Drugs, Chinese Herbal / Q000737:chemistry; D005260:Female; D066298:In Vitro Techniques; D007783:Lactones / Q000494:pharmacology*; D010121:Oxytocin / Q000037:antagonists & inhibitors; D051381:Rats; D017207:Rats, Sprague-Dawley; D012717:Sesquiterpenes / Q000494:pharmacology*; D014590:Uterine Contraction / Q000187:drug effects*
C424803:4,15-epoxy-8-hydroxyasterolide; D018680:Cholinergic Antagonists; D004365:Drugs, Chinese Herbal; D007783:Lactones; D012717:Sesquiterpenes; C424804:atractylenolide I; C424802:atractylenolide III; D010121:Oxytocin; D000109:Acetylcholine; D002118:Calcium