RESUMO
The purpose of this study was to investigate whether intravenous crotalphine produces significant sedation, as well as physiological changes, in healthy standing horses. Six mares, aged 8 years and weighing 415kg underwent three different treatments in a crossover design: TA (acepromazine: 50μg.kg-1), TC (crotalphine: 0.01μg.kg-1) and TX (xylazine: 1000μg.kg-1), intravenously. At various time points over 60 minutes, physiologic variables were recorded: heart rate, respiratory rate, and rectal temperature. The head height from the ground (HHG) was evaluated in centimeters. Data were analyzed using ANOVA followed by Dunnett’s test or Friedman followed by Dunn’s test, under 5% significance. Heart rate decreased significantly at M5 and M10 compared with Mb in TX (28±7, 26±6 and 40±8 beats/minute-1, respectively; p=0.0004). Respiratory rate and rectal temperature did not differ among groups or time points. The HHG significantly decreased in all groups compared with Mb at various time points (p<0.0001). In conclusion, crotalphine did not produce reliable and durable sedation in healthy standing mares and did not influence cardiorespiratory variables in a clinically relevant manner.
O objetivo deste estudo foi investigar se a administração de crotalfina intravenosa produz sedação significativa e alterações fisiológicas em equinos saudáveis. Seis éguas, idade média de oito anos e peso médio de 415kg, foram submetidas a três tratamentos distintos: TA (acepromazina: 50μg/kg), TC (crotalfina: 0,01μg/kg) e TX xilazina: 1000μg/kg), por via intravenosa. Em vários momentos, ao de longo de 60 minutos, as variáveis fisiológicas registradas foram frequência cardíaca, frequência respiratória e temperatura retal. A altura de cabeça ao solo (ACS) foi avaliada em centímetros. Os dados foram analisados pela ANOVA, seguida pelo teste de Dunnett ou de Friedman e, depois, pelo teste de Dunn, sob 5% de significância. A frequência cardíaca diminuiu significativamente em M5 e M10 em comparação com Mb em TX (28±7, 26±6 e 40±8 bpm, respectivamente; P=0,0004). A frequência respiratória e a temperatura retal não diferiram entre os grupos ou os pontos de tempo. O HHG diminuiu significativamente em todos os grupos em comparação com Mb em vários momentos (P <0,0001). Em conclusão, a crotalfina não produziu sedação confiável e durável em éguas saudáveis e não influenciou as variáveis cardiorrespiratórias de maneira clinicamente relevante.
RESUMO
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-ß-hydroxy-ß-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.
