Aster tataricus alleviates constipation by antagonizing the binding of acetylcholine to muscarinic receptor and inhibiting Ca2+ influx

Biomed Pharmacother. 2021 Jan:133:111005. doi: 10.1016/j.biopha.2020.111005. Epub 2020 Dec 11.

Abstract

Background: The dried root and rhizome of Aster tataricus (RA), is a traditional Chinese medicine has been used for more than 2000 years with the function of antitussive, expectorant and antiasthmatic. Ancient books and modern pharmacological researches demonstrated that RA may have the function of moistening intestines and relieving constipation, but there was a lack of systematic evidence. The aim of this study was to comprehensively evaluate the efficacy and possible mechanisms of ethanol extract of Aster tataricus (ATE) in treating constipation from in vivo to in vitro.

Methods: In vivo, the ATE was studied in loperamide-induced constipation of mice. In vitro, different concentrations of ATE was tested separately or cumulatively on spontaneous and agonists-induced contractions of isolated rat duodenum strips.

Results: In vivo, at doses of 0.16, 0.8 g/mL, ATE showed significantly promotion of the small intestinal charcoal transit, decrease of the amount of remnant fecal, and increase of the content of fecal water in colon. In addition, ATE could effectively relieve colonic pathological damage caused by loperamide as well. In vitro, with the cumulative concentration increase of ATE from 0.8 to 6.4 mg/mL, it could significantly decrease the contraction caused by KCl or Ach, and gradually restore to near base tension value.Meanwhile, it could also partially but significantly inhibit the contractions induced by Ach and CaCl2 on rat duodenum in a concentration related manner.

Conclusions: Taking all these findings together, it could be speculated that ATE may attenuate constipation mainly through antagonizing the binding of acetylcholine to muscarinic receptor, inhibiting Ca2+ influx and anti-inflammation.

Keywords: Anti-inflammation; Aster tataricus; Ca(2+)channel; Constipation; Muscarinic receptor.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / isolation & purification
  • Anti-Inflammatory Agents / pharmacology
  • Aster Plant* / chemistry
  • Calcium Signaling / drug effects*
  • Constipation / chemically induced
  • Constipation / drug therapy*
  • Constipation / metabolism
  • Constipation / physiopathology
  • Defecation / drug effects*
  • Disease Models, Animal
  • Duodenum / drug effects*
  • Duodenum / metabolism
  • Duodenum / physiopathology
  • Gastrointestinal Transit / drug effects*
  • Laxatives / isolation & purification
  • Laxatives / pharmacology*
  • Loperamide
  • Mice
  • Muscarinic Antagonists / isolation & purification
  • Muscarinic Antagonists / pharmacology*
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology*
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Anti-Inflammatory Agents
  • Laxatives
  • Muscarinic Antagonists
  • Plant Extracts
  • Loperamide