Potent relaxant effect of a Celastrus paniculatus extract in the rat and human ileum

Francesca Borrelli, Nicola Borbone, Raffaele Capasso, Domenico Montesano, Simona De Marino, Gabriella Aviello, Giovanni Aprea, Stefania Masone, Angelo A Izzo

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

ETHNOPHARMACOLOGICAL IMPORTANCE: Celastrus paniculatus Willd. (Celastraceae) is an Ayurvedic remedy used for the treatment of a number of diseases, including bowel spasms.

AIM OF THE STUDY: 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.

MATERIALS AND 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%).

CONCLUSION: 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.

Original languageEnglish
Pages (from-to)434-438
Number of pages5
JournalJournal of Ethnopharmacology
Volume122
Issue number3
Early online date11 Feb 2009
DOIs
Publication statusPublished - 21 Apr 2009

Fingerprint

Celastrus
Ileum
Spasm
Celastraceae
omega-Conotoxins
Tachykinins
Tetrodotoxin
Nifedipine
Acetylcholine
Seeds
Norepinephrine
Nitric Oxide
Adenosine Triphosphate
Pharmacology

Keywords

  • Animals
  • Calcium Channel Blockers
  • Celastrus
  • Dose-Response Relationship, Drug
  • Gastrointestinal Motility
  • Humans
  • Ileum
  • Muscle Relaxation
  • Muscle, Smooth
  • Neurotoxins
  • Nifedipine
  • Parasympatholytics
  • Plant Extracts
  • Plant Oils
  • Rats
  • Rats, Wistar
  • Seeds
  • Tetrodotoxin
  • omega-Conotoxins
  • Journal Article
  • Research Support, Non-U.S. Gov't

Cite this

Borrelli, F., Borbone, N., Capasso, R., Montesano, D., De Marino, S., Aviello, G., ... Izzo, A. A. (2009). Potent relaxant effect of a Celastrus paniculatus extract in the rat and human ileum. Journal of Ethnopharmacology, 122(3), 434-438. https://doi.org/10.1016/j.jep.2009.02.003

Potent relaxant effect of a Celastrus paniculatus extract in the rat and human ileum. / Borrelli, Francesca; Borbone, Nicola; Capasso, Raffaele; Montesano, Domenico; De Marino, Simona; Aviello, Gabriella; Aprea, Giovanni; Masone, Stefania; Izzo, Angelo A.

In: Journal of Ethnopharmacology, Vol. 122, No. 3, 21.04.2009, p. 434-438.

Research output: Contribution to journalArticle

Borrelli, F, Borbone, N, Capasso, R, Montesano, D, De Marino, S, Aviello, G, Aprea, G, Masone, S & Izzo, AA 2009, 'Potent relaxant effect of a Celastrus paniculatus extract in the rat and human ileum', Journal of Ethnopharmacology, vol. 122, no. 3, pp. 434-438. https://doi.org/10.1016/j.jep.2009.02.003
Borrelli F, Borbone N, Capasso R, Montesano D, De Marino S, Aviello G et al. Potent relaxant effect of a Celastrus paniculatus extract in the rat and human ileum. Journal of Ethnopharmacology. 2009 Apr 21;122(3):434-438. https://doi.org/10.1016/j.jep.2009.02.003
Borrelli, Francesca ; Borbone, Nicola ; Capasso, Raffaele ; Montesano, Domenico ; De Marino, Simona ; Aviello, Gabriella ; Aprea, Giovanni ; Masone, Stefania ; Izzo, Angelo A. / Potent relaxant effect of a Celastrus paniculatus extract in the rat and human ileum. In: Journal of Ethnopharmacology. 2009 ; Vol. 122, No. 3. pp. 434-438.
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abstract = "ETHNOPHARMACOLOGICAL IMPORTANCE: Celastrus paniculatus Willd. (Celastraceae) is an Ayurvedic remedy used for the treatment of a number of diseases, including bowel spasms.AIM OF THE STUDY: 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.MATERIALS AND 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{\%}).CONCLUSION: 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.",
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T1 - Potent relaxant effect of a Celastrus paniculatus extract in the rat and human ileum

AU - Borrelli, Francesca

AU - Borbone, Nicola

AU - Capasso, Raffaele

AU - Montesano, Domenico

AU - De Marino, Simona

AU - Aviello, Gabriella

AU - Aprea, Giovanni

AU - Masone, Stefania

AU - Izzo, Angelo A

N1 - This work was supported by Italian MIUR and the Enrico and Enrica Sovena Foundation.

PY - 2009/4/21

Y1 - 2009/4/21

N2 - ETHNOPHARMACOLOGICAL IMPORTANCE: Celastrus paniculatus Willd. (Celastraceae) is an Ayurvedic remedy used for the treatment of a number of diseases, including bowel spasms.AIM OF THE STUDY: 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.MATERIALS AND 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%).CONCLUSION: 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.

AB - ETHNOPHARMACOLOGICAL IMPORTANCE: Celastrus paniculatus Willd. (Celastraceae) is an Ayurvedic remedy used for the treatment of a number of diseases, including bowel spasms.AIM OF THE STUDY: 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.MATERIALS AND 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%).CONCLUSION: 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.

KW - Animals

KW - Calcium Channel Blockers

KW - Celastrus

KW - Dose-Response Relationship, Drug

KW - Gastrointestinal Motility

KW - Humans

KW - Ileum

KW - Muscle Relaxation

KW - Muscle, Smooth

KW - Neurotoxins

KW - Nifedipine

KW - Parasympatholytics

KW - Plant Extracts

KW - Plant Oils

KW - Rats

KW - Rats, Wistar

KW - Seeds

KW - Tetrodotoxin

KW - omega-Conotoxins

KW - Journal Article

KW - Research Support, Non-U.S. Gov't

U2 - 10.1016/j.jep.2009.02.003

DO - 10.1016/j.jep.2009.02.003

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VL - 122

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EP - 438

JO - Journal of Ethnopharmacology

JF - Journal of Ethnopharmacology

SN - 0378-8741

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