Intracellular calcium mobilization as a target for the spasmolytic action of scopoletin

Planta Med. 2001 Oct;67(7):605-8. doi: 10.1055/s-2001-17355.

Abstract

The coumarin scopoletin was isolated in a pure form from the roots of Brunfelsia hopeana Benth. (Solanaceae). In isolated rat aortic rings, scopoletin (26-520 microM) inhibited to approximately the same extent the contractions induced by a variety of substances, including phenylephrine, potassium chloride, serotonin and PGF(2) (alpha). The effect of the coumarin on phenylephrine-induced contractions was not affected by endothelium removal or NO-synthase blockade by L-NAME (100 microM). Scopoletin (78 - 590 microM) antagonized in a concentration-dependent manner (IC(50) = 300 +/- 20 microM, n = 5), transient contractions in Ca(2+)-free media induced by noradrenaline, but not those induced by caffeine. Also, scopoletin did not interfere with the refilling of noradrenaline-sensitive intracellular calcium stores. It is suggested that the non-specific spasmolytic action of scopoletin can be attributed, at least in part, to its ability to inhibit the intracellular calcium mobilization from the noradrenaline-sensitive stores.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aorta
  • Caffeine / pharmacology
  • Calcium / metabolism*
  • Coumarins / chemistry
  • Coumarins / isolation & purification
  • Coumarins / pharmacology
  • Dinoprost / agonists
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • In Vitro Techniques
  • Intracellular Membranes / metabolism
  • Male
  • Muscle Contraction / drug effects
  • Muscle, Smooth, Vascular / drug effects
  • Norepinephrine / pharmacology
  • Parasympatholytics / pharmacology*
  • Phenylephrine / agonists
  • Plant Extracts / pharmacology*
  • Plant Roots / chemistry
  • Potassium Chloride / agonists
  • Rats
  • Rats, Wistar
  • Scopoletin / antagonists & inhibitors
  • Scopoletin / chemistry
  • Scopoletin / isolation & purification
  • Scopoletin / pharmacology*
  • Serotonin / pharmacology
  • Solanaceae / chemistry*
  • Vasoconstriction / drug effects

Substances

  • Coumarins
  • Parasympatholytics
  • Plant Extracts
  • Phenylephrine
  • Serotonin
  • Caffeine
  • Potassium Chloride
  • Dinoprost
  • Scopoletin
  • Calcium
  • Norepinephrine