Inhibitory effect of the herbal antidepressant St. John's wort (Hypericum perforatum) on rat gastric motility

Raffaele Capasso, Francesca Borrelli, Gabriella Aviello, Francesco Capasso, Angelo A Izzo

Research output: Contribution to journalArticle

15 Citations (Scopus)

Abstract

St. John's wort (Hypericum perforatum) is a highly popular and effective herbal antidepressant that clinically interacts with a number of conventional drugs. Because alterations in gastric emptying can cause pharmacokinetic interactions, in the present study we evaluated the effect of a standardized extract prepared from the flowering tops of Hypericum perforatum (SJW extract) on rat gastric motility. Orally administered SJW extract delayed gastric emptying in vivo. In vitro studies showed that SJW extract was significantly more active in inhibiting acetylcholine (or prostaglandin E2)-induced contractions than electrical field stimulation (EFS)-induced contractions. The effect of SJW extract on EFS-induced contractions was unaffected by drugs that inhibit intrinsic inhibitory nerves or by tachykinin antagonists, but it was reduced by the 5-hydroxytryptamine antagonist methysergide. The inhibitory effect of SJW extract on acetylcholine-induced contractions was reduced by the sarcoplasmic reticulum Ca2+-ATPase inhibitor cyclopiazonic acid, but not by the L-type Ca2+ channel blocker nifedipine or by methysergide. Among the chemical constituents of SJW extract tested, hyperforin and, to a lesser extent, the flavonoids kaempferol and quercitrin, inhibited acetylcholine-induced contractions. It is concluded that SJW has a direct inhibitory effect on smooth muscle and could also possibly modulate gastric neurotransmission. If extended to humans, the inhibitory effect of SJW extract on gastric emptying in vivo could contribute, at least in part, to the clinical pharmacokinetic interactions between conventional medicines and this herbal antidepressant.

Original languageEnglish
Pages (from-to)407-414
Number of pages8
JournalNaunyn-Schmiedeberg's Archives of Pharmacology
Volume376
Issue number6
DOIs
Publication statusPublished - Feb 2008

Fingerprint

Hypericum
Gastric Emptying
Antidepressive Agents
Acetylcholine
Methysergide
Stomach
Electric Stimulation
Flowering Tops
Pharmacokinetics
Tachykinins
Serotonin Antagonists
Calcium-Transporting ATPases
Herbal Medicine
Sarcoplasmic Reticulum
Nifedipine
Dinoprostone
Flavonoids
Synaptic Transmission
Pharmaceutical Preparations
Smooth Muscle

Keywords

  • Analysis of Variance
  • Animals
  • Antidepressive Agents
  • Dose-Response Relationship, Drug
  • Flowering Tops
  • Gastric Emptying
  • Hypericum
  • In Vitro Techniques
  • Male
  • Muscle, Smooth
  • Plant Extracts
  • Rats
  • Rats, Wistar
  • Stomach
  • Journal Article
  • Research Support, Non-U.S. Gov't

Cite this

Inhibitory effect of the herbal antidepressant St. John's wort (Hypericum perforatum) on rat gastric motility. / Capasso, Raffaele; Borrelli, Francesca; Aviello, Gabriella; Capasso, Francesco; Izzo, Angelo A.

In: Naunyn-Schmiedeberg's Archives of Pharmacology, Vol. 376, No. 6, 02.2008, p. 407-414.

Research output: Contribution to journalArticle

Capasso, Raffaele ; Borrelli, Francesca ; Aviello, Gabriella ; Capasso, Francesco ; Izzo, Angelo A. / Inhibitory effect of the herbal antidepressant St. John's wort (Hypericum perforatum) on rat gastric motility. In: Naunyn-Schmiedeberg's Archives of Pharmacology. 2008 ; Vol. 376, No. 6. pp. 407-414.
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T1 - Inhibitory effect of the herbal antidepressant St. John's wort (Hypericum perforatum) on rat gastric motility

AU - Capasso, Raffaele

AU - Borrelli, Francesca

AU - Aviello, Gabriella

AU - Capasso, Francesco

AU - Izzo, Angelo A

N1 - This work was supported by PRIN, Regione Campania, and “Fondazione Enrico ed Enrica Sovena”.

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N2 - St. John's wort (Hypericum perforatum) is a highly popular and effective herbal antidepressant that clinically interacts with a number of conventional drugs. Because alterations in gastric emptying can cause pharmacokinetic interactions, in the present study we evaluated the effect of a standardized extract prepared from the flowering tops of Hypericum perforatum (SJW extract) on rat gastric motility. Orally administered SJW extract delayed gastric emptying in vivo. In vitro studies showed that SJW extract was significantly more active in inhibiting acetylcholine (or prostaglandin E2)-induced contractions than electrical field stimulation (EFS)-induced contractions. The effect of SJW extract on EFS-induced contractions was unaffected by drugs that inhibit intrinsic inhibitory nerves or by tachykinin antagonists, but it was reduced by the 5-hydroxytryptamine antagonist methysergide. The inhibitory effect of SJW extract on acetylcholine-induced contractions was reduced by the sarcoplasmic reticulum Ca2+-ATPase inhibitor cyclopiazonic acid, but not by the L-type Ca2+ channel blocker nifedipine or by methysergide. Among the chemical constituents of SJW extract tested, hyperforin and, to a lesser extent, the flavonoids kaempferol and quercitrin, inhibited acetylcholine-induced contractions. It is concluded that SJW has a direct inhibitory effect on smooth muscle and could also possibly modulate gastric neurotransmission. If extended to humans, the inhibitory effect of SJW extract on gastric emptying in vivo could contribute, at least in part, to the clinical pharmacokinetic interactions between conventional medicines and this herbal antidepressant.

AB - St. John's wort (Hypericum perforatum) is a highly popular and effective herbal antidepressant that clinically interacts with a number of conventional drugs. Because alterations in gastric emptying can cause pharmacokinetic interactions, in the present study we evaluated the effect of a standardized extract prepared from the flowering tops of Hypericum perforatum (SJW extract) on rat gastric motility. Orally administered SJW extract delayed gastric emptying in vivo. In vitro studies showed that SJW extract was significantly more active in inhibiting acetylcholine (or prostaglandin E2)-induced contractions than electrical field stimulation (EFS)-induced contractions. The effect of SJW extract on EFS-induced contractions was unaffected by drugs that inhibit intrinsic inhibitory nerves or by tachykinin antagonists, but it was reduced by the 5-hydroxytryptamine antagonist methysergide. The inhibitory effect of SJW extract on acetylcholine-induced contractions was reduced by the sarcoplasmic reticulum Ca2+-ATPase inhibitor cyclopiazonic acid, but not by the L-type Ca2+ channel blocker nifedipine or by methysergide. Among the chemical constituents of SJW extract tested, hyperforin and, to a lesser extent, the flavonoids kaempferol and quercitrin, inhibited acetylcholine-induced contractions. It is concluded that SJW has a direct inhibitory effect on smooth muscle and could also possibly modulate gastric neurotransmission. If extended to humans, the inhibitory effect of SJW extract on gastric emptying in vivo could contribute, at least in part, to the clinical pharmacokinetic interactions between conventional medicines and this herbal antidepressant.

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KW - Animals

KW - Antidepressive Agents

KW - Dose-Response Relationship, Drug

KW - Flowering Tops

KW - Gastric Emptying

KW - Hypericum

KW - In Vitro Techniques

KW - Male

KW - Muscle, Smooth

KW - Plant Extracts

KW - Rats

KW - Rats, Wistar

KW - Stomach

KW - Journal Article

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

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DO - 10.1007/s00210-007-0230-2

M3 - Article

VL - 376

SP - 407

EP - 414

JO - Naunyn-Schmiedeberg's Archives of Pharmacology

JF - Naunyn-Schmiedeberg's Archives of Pharmacology

SN - 0028-1298

IS - 6

ER -