Antidiarrheal activity of methanol extract of Sophora tonkinensis in mice and spasmolytic effect on smooth muscle contraction of isolated jejunum in rabbits

Pharm Biol. 2019 Dec;57(1):477-484. doi: 10.1080/13880209.2019.1645701.

Abstract

Context: In China, the herb Sophora tonkinensis Gagnep. (Fabaceae, ST) (Committee of National Pharmacopeia. 2015) exhibits anti-inflammatory, antitumor, and antiviral effects. However, to date, there have been few studies on its gastrointestinal effect. Objective: The gastrointestinal effect of the methanol extract of ST rhizome (STR) was evaluated. Materials and methods: Study was conducted from February to December 2018. In vivo, antidiarrheal activity of STR (125, 250 and 500 mg/kg; orally) in castor oil-induced diarrheal mice was studied. In vitro, the effects of STR (0.01-10 mg/mL) on the isolated tissue preparations of rabbit jejunum were also investigated, the rabbit jejunum stripes were pre-contracted with Ach (10-5 M), K+ (60 mM) and tested in the presence of STR, the possible spasmolytic effect was analyzed in the pretreatment of the jejunum preparations with STR or verapamil in Ca2+-free high-K+ (60 mM) solution containing EDTA. Results: STR (125, 250 and 500 mg/kg) exhibited antidiarrheal activity. STR (0.01-10 mg/mL) completely relaxed spontaneously contracting, Ach (10-5 M) and high K+ (60 mM) induced contracted jejunum with an EC50 value of 0.66 (0.49-0.96), 0.39 (0.28-0.44) and 0.17 (0.10-0.21), similar to verapamil. Concentration-response curves of CaCl2 could be significantly moved to the right and down in the presence of STR (0.3, 1 mg/mL). Discussion and conclusions: Results suggest the presence of antidiarrheal activity and spasmolytic effects of STR, possibly mediated through Ca2+ channel blocking activity, providing the pharmacological basis for its traditional uses in gastrointestinal disorders.

Keywords: antidiarrheal; spasmolytic.

MeSH terms

  • Animals
  • Antidiarrheals / isolation & purification
  • Antidiarrheals / therapeutic use*
  • Antidiarrheals / toxicity
  • Asteraceae / chemistry*
  • Castor Oil
  • Diarrhea / drug therapy*
  • Dose-Response Relationship, Drug
  • Gastrointestinal Motility / drug effects
  • In Vitro Techniques
  • Jejunum / drug effects*
  • Lethal Dose 50
  • Male
  • Methanol
  • Mice
  • Muscle Contraction / drug effects*
  • Muscle, Smooth / drug effects
  • Parasympatholytics / isolation & purification
  • Parasympatholytics / pharmacology*
  • Parasympatholytics / toxicity
  • Plant Extracts / isolation & purification
  • Plant Extracts / therapeutic use*
  • Plant Extracts / toxicity
  • Rabbits

Substances

  • Antidiarrheals
  • Parasympatholytics
  • Plant Extracts
  • Castor Oil
  • Methanol

Grants and funding

This work was supported by the undergraduate innovation project of Sichuan Province Education Department (201810634167, 201810634168, 201810634166) and the Applied Basic Research Programs of Science and Technology Department of Sichuan Province (2016JY0032).