Pharmacological basis for the medicinal use of black pepper and piperine in gastrointestinal disorders

Malik Hassan Mehmood, Anwarul Hassan Gilani

Research output: Contribution to journalArticlepeer-review

75 Citations (Scopus)

Abstract

Dried fruits of Piper nigrum (black pepper) are commonly used in gastrointestinal disorders. The aim of this study was to rationalize the medicinal use of pepper and its principal alkaloid, piperine, in constipation and diarrhea using in vitro and in vivo assays. When tested in isolated guinea pig ileum, the crude extract of pepper (Pn.Cr) (1-10 mg/mL) and piperine (3-300 μM) caused a concentration-dependent and atropine-sensitive stimulant effect. In rabbit jejunum, Pn.Cr (0.01-3.0 mg/mL) and piperine (30-1,000 μM) relaxed spontaneous contractions, similar to loperamide and nifedipine. The relaxant effect of Pn.Cr and piperine was partially inhibited in the presence of naloxone (1 μM) similar to that of loperamide, suggesting the naloxone-sensitive effect in addition to the Ca2+ channel blocking (CCB)-like activity, which was evident by its relaxant effect on K+ (80 mM)-induced contractions. The CCB activity was confirmed when pretreatment of the tissue with Pn.Cr (0.03-0.3 mg/mL) or piperine (10-100 μM) caused a rightward shift in the concentration-response curves of Ca2+, similar to loperamide and nifedipine. In mice, Pn.Cr and piperine exhibited a partially atropine-sensitive laxative effect at lower doses, whereas at higher doses it caused antisecretory and antidiarrheal activities that were partially inhibited in mice pretreated with naloxone (1.5 mg/kg), similar to loperamide. This study illustrates the presence of spasmodic (cholinergic) and antispasmodic (opioid agonist and Ca2+ antagonist) effects, thus providing the possible explanation for the medicinal use of pepper and piperine in gastrointestinal motility disorders.

Original languageEnglish
Pages (from-to)1086-1096
Number of pages11
JournalJournal of Medicinal Food
Volume13
Issue number5
DOIs
Publication statusPublished - 2010
Externally publishedYes

Keywords

  • Piper nigrum
  • antidiarrheal
  • antispasmodic
  • laxative
  • pepper
  • piperine
  • spasmodic

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