title: Antispasmodic effects of myrrh due to calcium antagonistic effects in inflamed rat small intestinal preparations.
abstract: Myrrh is the oleo-gum resin of mainly Commiphora molmol and as a powdered substance, one compound in the traditional medicinal product Myrrhinil-Intest®, which has been used for the treatment of unspecific, inflammatory intestinal disorders. The aim of the present study was to evaluate the antispasmodic effect of myrrh under healthy and inflamed conditions, and to evaluate a calcium-antagonistic effect as a possible mode of action. Therefore, an ethanolic myrrh extract was tested for its effects on muscle tone and acetylcholine-induced contractions in untreated and inflamed rat ileum/jejunum preparations. Inflammation was experimentally induced by 2,4,6-trinitrobenzene sulfonic acid (10 mM, 30 min). Additionally, the effect of the calcium channel agonist Bay K8644 in the presence of varying myrrh extract concentrations was examined. Myrrh extract (0.99 mg/mL) suppressed the acetylcholine-induced contraction down to 25.8 % in untreated and 15.2 % in inflamed preparations. Myrrh extract (0.15; 0.25 and 0.35 mg/mL) induced a concentration-dependent rightward shift of the Bay K8644 concentration-response curve in untreated and inflamed preparations with a significant EC50 shift. Schild analysis resulted in a pA2 value of 0.93 for untreated preparations. Increasing myrrh extract concentrations induced a concentration-dependent decrease of the agonistic maximum effect in untreated and inflamed preparations down to 15.8 % and 25.8 %, respectively, for the highest concentration leading to a pD2 value of 0.58. Myrrh extract reduced intestinal muscle tone and acetylcholine-induced contraction of untreated and inflamed ileum/jejunum preparations based on dual calcium antagonism characterized by a right shift of the agonistic dose-response curve and a depression of the maximum effect. The resulting reduction of intestinal motility and spasmolytic effects provide a rationale for the symptom treatment of intestinal disorders such as irritable bowel syndrome.
authors.affiliation: University of Leipzig, Institute of Pharmacy, Leipzig, Germany.
authors.forename: Cica
authors.initials: C
authors.lastname: Vissiennon
authors.affiliation: REPHA GmbH Biologische Arzneimittel, Langenhagen, Germany.
authors.forename: Karl-Heinz
authors.initials: KH
authors.lastname: Goos
authors.affiliation: REPHA GmbH Biologische Arzneimittel, Langenhagen, Germany.
authors.forename: Ole
authors.initials: O
authors.lastname: Goos
authors.affiliation: University of Leipzig, Institute of Pharmacy, Leipzig, Germany.
authors.forename: Karen
authors.initials: K
authors.lastname: Nieber
mesh_terms: D000109:Acetylcholine / Q000009:adverse effects; D000818:Animals; D002118:Calcium / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D029744:Commiphora / Q000737:chemistry*; D004195:Disease Models, Animal; D004751:Enteritis / Q000188:drug therapy*; D005260:Female; D005769:Gastrointestinal Motility / Q000187:drug effects; D007082:Ileum / Q000187:drug effects / Q000473:pathology; D007583:Jejunum / Q000187:drug effects / Q000473:pathology; D008297:Male; D010276:Parasympatholytics / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D010936:Plant Extracts / Q000494:pharmacology / Q000627:therapeutic use; D051381:Rats; D017208:Rats, Wistar; D013729:Terpenes / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D014301:Trinitrobenzenes / Q000009:adverse effects
chemical_list: D002121:Calcium Channel Blockers; D010276:Parasympatholytics; D010936:Plant Extracts; D013729:Terpenes; D014301:Trinitrobenzenes; C029222:sym-trinitrobenzene; C014119:myrrh oil; D000109:Acetylcholine; D002118:Calcium