AUTHOR=Bawazeer Saud , Rauf Abdur , Bawazeer Sami 

TITLE=Gastrointestinal Motility, Muscle Relaxation, Antipyretic and Acute Toxicity Screening of Amyrin Type Triterpenoid (Daturaolone) Isolated From Datura metel Linnaeus (Angel’s Trumpet) Fruits

JOURNAL=Frontiers in Pharmacology

VOLUME=11

YEAR=2020

URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2020.544794

DOI=10.3389/fphar.2020.544794

ISSN=1663-9812

ABSTRACT=<p><italic>Datura metel</italic> Linn is used traditionally for the treatment of various diseases including relaxation of smooth muscles, relief of fever, as well as gastrointestinal disorder. This study deals with the bio-guided isolation of an active, amyrin-type triterpenoid, namely 3-oxo-6-<italic>β</italic>-hydroxy-<italic>β</italic>-amyrin (daturaolone; <bold>1</bold>), from the chloroform fraction of <italic>Datura metel</italic> L. (Angel’s trumpet) fruits and its gastrointestinal motility, antipyretic, and muscle relaxation effects in animal models. The chemical structure of daturaolone (<bold>1</bold>) was elucidated by NMR spectroscopy and crystallography techniques. The chloroform fraction and daturaolone (<bold>1</bold>) were assessed for the GIT motility test. Data exhibited in charcoal meal GI transit test show that chloroform fraction and daturaolone (<bold>1</bold>) significantly reduce GIT motility and increased intestinal transit time, comparable to the standard (atropine), a muscarinic receptor blocking agent. Muscle relaxant potency of the extract and daturaolone (<bold>1</bold>) was assessed in various animal paradigms. In the inclined plane screening test, it produced a significant (P &lt; 0.05) muscle relaxation potential in a dose-dependent manner after 30, 60, and 90 min. Likewise, the muscle relaxation potential of the extract and daturaolone (<bold>1</bold>) was strongly complemented by the chimney and traction test, representing a dominant effect after 60 min of sample administration. The chloroform fraction showed good antipyretic activity, and while daturaolone (<bold>1</bold>) exhibited significant activity at a higher dose, the maximum effect (84.64%) was at 20 mg/kg i.p. In acute toxicity screening test, the chloroform extract (100, 250, 500, and 1,000 mg/kg) and daturaolone (<bold>1</bold>) (5, 10, 20, and 50 mg/kg) were found safe. In conclusion, the chloroform extract and daturaolone (<bold>1</bold>) exhibited strong gastrointestinal motility, muscle relaxation, and antipyretic activity in different animal models and intestinally, was found safe at higher tested doses.</p>