Persea Americana Seeds Cause Ileal Smooth Muscle Relaxation Via Stimulation of α-1 Adrenoceptors

Drug Res (Stuttg). 2020 Feb;70(2-03):107-111. doi: 10.1055/a-1076-0703. Epub 2020 Jan 2.

Abstract

The effect of methanol extract of P. americana seeds on isolated ileal smooth muscle was studied for isometric response using 10 adult rabbits of both sexes. Reactivity and agonist-antagonist responses of rabbit ileum to the extract were determined in this study. The affinity, effective concentration to give 50% response (EC50) and maximum response were calculated from the concentration response curves (CRC) obtained. The result for the reactivity study showed the seed extract of P. americana caused concentration dependent relaxation of isolated rabbit ileum with threshold responses at concentration of 1×10-9 mg/ml and 120 mg/ml respectively. The extract-antagonist study showed an upward and right shift in CRC in the presence of phenoxybenzamine, a non-selective adrenergic antagonist, with the EC50 increased from 5.01 mg/ml to 12.59 mg/ml and affinity decreased from 0.20 to 0.08. Extract-antagonist study also showed a right and upward shift in the CRC with a greater magnitude in the presence of prazosin, an α1-adrenergic antagonist, with EC50 increased from 0.32 mg/ml to 25.12 mg/ml and a consequential decrease in the affinity from 3.13 to 0.04. In the presence of propranolol, a β-adrenergic antagonist, a downward and left shift in the CRC was observed with the EC50 and PA2 remaining constant at 0.1 mg/ml and 10 respectively. P. americana concentration-dependently reduced or inhibited gastric motility, increasing transit time which is important for food absorption, thus a pro-nutritive and antispasmodic effect. The interaction with α1-adrenoceptors is beneficially in heart failure management. The plant can be developed as a drug candidate for management of hypertension.

MeSH terms

  • Adrenergic alpha-1 Receptor Antagonists / pharmacology
  • Adrenergic beta-Antagonists / pharmacology
  • Animals
  • Dose-Response Relationship, Drug
  • Female
  • Ileum / drug effects
  • Ileum / metabolism
  • Male
  • Muscle Relaxation / drug effects*
  • Muscle, Smooth / drug effects
  • Muscle, Smooth / metabolism
  • Persea / chemistry*
  • Plant Extracts / administration & dosage
  • Plant Extracts / pharmacology*
  • Rabbits
  • Receptors, Adrenergic, alpha-1 / drug effects*
  • Receptors, Adrenergic, alpha-1 / metabolism
  • Seeds

Substances

  • Adrenergic alpha-1 Receptor Antagonists
  • Adrenergic beta-Antagonists
  • Plant Extracts
  • Receptors, Adrenergic, alpha-1