Potent relaxant effect of a Celastrus paniculatus extract in the rat and human ileum.
BACKGROUND
Celastrus paniculatus Willd. (Celastraceae) is an Ayurvedic remedy used for the treatment of a number of diseases, including bowel spasms.


OBJECTIVE
To investigate the mode of the relaxing action of a methanolic extract prepared from the seeds of Celastrus paniculatus (CPE, 0.0001-10 microg/mL) in the rat ileum and to try to confirm on human tissues the intestinal pharmacological activity of the extract.


METHODS
The relaxant effect of CPE was studied in vitro by evaluating its effect on the spontaneous contractions of the isolated ileum.


RESULTS
CPE exerted a tetrodotoxin- and omega-conotoxin-resistant inhibitory effect on rat ileum motility (IC(50): 0.24+/-0.02 microg/mL; E(max): 99.0+/-0.60%). The inhibitory effect was reduced by nifedipine but not by cyclopiazonic acid. Experiments with specific antagonists enabled us to exclude the involvement of the main endogenous spasmogenic (i.e. acetylcholine and tachykinins) and relaxing (noradrenaline, nitric oxide, ATP) compounds. CPE also relaxed the isolated human ileum (IC(50): 0.26+/-0.02 microg/mL; E(max): 99.1+/-0.46%).


CONCLUSIONS
It is concluded that (i) CPE exerted a powerful myogenic and L-type Ca(2+)-dependent relaxing effect in the isolated rat ileum and that (ii) the human ileum is sensitive to the inhibitory effect of CPE. If confirmed in vivo, our data could explain the traditional use of this herb in the treatment of intestinal spasms.
Borrelli
Francesca
F
Dipartimento di Farmacologia Sperimentale, Università degli Studi di Napoli Federico II, Napoli, Italy.
Borbone
Nicola
N
Capasso
Raffaele
R
Montesano
Domenico
D
De Marino
Simona
S
Aviello
Gabriella
G
Aprea
Giovanni
G
Masone
Stefania
S
Izzo
Angelo A
AA
D000818:Animals; D002121:Calcium Channel Blockers / Q000494:pharmacology; D031247:Celastrus; D004305:Dose-Response Relationship, Drug; D005769:Gastrointestinal Motility / Q000187:drug effects*; D006801:Humans; D007082:Ileum / Q000187:drug effects*; D009126:Muscle Relaxation / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects*; D009498:Neurotoxins / Q000494:pharmacology; D009543:Nifedipine / Q000494:pharmacology; D010276:Parasympatholytics / Q000494:pharmacology*; D010936:Plant Extracts / Q000494:pharmacology*; D010938:Plant Oils / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D012639:Seeds; D013779:Tetrodotoxin / Q000494:pharmacology; D020960:omega-Conotoxins / Q000494:pharmacology
D002121:Calcium Channel Blockers; D009498:Neurotoxins; D010276:Parasympatholytics; D010936:Plant Extracts; D010938:Plant Oils; D020960:omega-Conotoxins; D013779:Tetrodotoxin; D009543:Nifedipine