Abstract
Datura metel 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-β-hydroxy-β-amyrin (daturaolone; 1), from the chloroform fraction of Datura metel L. (Angel’s trumpet) fruits and its gastrointestinal motility, antipyretic, and muscle relaxation effects in animal models. The chemical structure of daturaolone (1) was elucidated by NMR spectroscopy and crystallography techniques. The chloroform fraction and daturaolone (1) were assessed for the GIT motility test. Data exhibited in charcoal meal GI transit test show that chloroform fraction and daturaolone (1) 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 (1) was assessed in various animal paradigms. In the inclined plane screening test, it produced a significant (P < 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 (1) 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 (1) 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 (1) (5, 10, 20, and 50 mg/kg) were found safe. In conclusion, the chloroform extract and daturaolone (1) exhibited strong gastrointestinal motility, muscle relaxation, and antipyretic activity in different animal models and intestinally, was found safe at higher tested doses.
Highlights
Datura metel is a member of the family Solanaceae and is an erect shrub with spreading branches
The muscle relaxation activity of the chloroform fraction and daturaolone (1) was performed using the chimney and inclined plane model according to the standard method (Rauf et al, 2018)
Animals were divided into various groups (n = 6); each group was administered with distilled water (10 ml/kg), standard drug (1 mg/kg), chloroform fraction at the doses 10, 25, 50, 100, and 200 mg/kg, i.p., and daturaolone (1) at the doses 2.5, 5, 10, 20, 40 mg/kg, i.p
Summary
Datura metel is a member of the family Solanaceae and is an erect shrub with spreading branches. In Ayurvedic medicinal systems, its seeds are used to cure ulcers, jaundice, diabetes, skin rashes, and bronchitis (Monira and Munan, 2012) Further to these uses, its flowers are involved in cigarette production, while the seeds are used in making tea with potent sedative action in Brazil (Agra et al, 2007). Other tropane alkaloids isolated from D. metel are used as antispasmodic, mydriatic, and sedative agents (Nuhu, 2002) It is an important source of withanolides, which is used to cure pain and has hallucinogenic potency (Abubakar et al, 2009; Yang et al, 2014; Arjun et al, 2015). The current study deals with the isolation of a triterpenoid, namely daturaolone (1), and the in vivo gastrointestinal motility, antipyretic, and muscle relaxation as well as acute toxicity study of the chloroform extract and the isolated daturaolone (1)
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