Carvalho Fabiano B, Boligon Aline A, Athayde Margareth L, Rubin Maribel A, Ferreira Juliano, Trevisan Gabriela
Programa de Pós-graduação em Ciências Biológicas: Bioquímica Toxicológica, Centro de Ciências Naturais e Exatas, Universidade Federal de Santa Maria (UFSM), 97105-900 Santa Maria, RS, Brazil.
Programa de Pós-graduação em Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal de Santa Maria (UFSM), 97105-900 Santa Maria, RS, Brazil.
J Ethnopharmacol. 2016 Feb 17;179:45-54. doi: 10.1016/j.jep.2015.12.035. Epub 2015 Dec 21.
Scutia buxifolia is a tree native to South America and is used as a cardiotonic agent; however, this property has not been associated with a clear mechanism or a specific compound.
Given the importance of Na(+),K(+)-ATPase as a drug target in the treatment of heart failure, this study aimed to investigate the possible inhibitory effect of S. buxifolia crude extract and fractions (dichloromethane, ethyl acetate, and butanolic fractions), and identified compounds with effects on the activity of Na(+),K(+)-ATPase in vitro.
First, we characterized the crude extract and fractions by high-performance liquid chromatography, and then monitored their effects on the activity of Na(+),K(+)-ATPase obtained from heart muscle and brain membranes of adult male Wistar rats.
We identified gallic acid, chlorogenic acid, caffeic acid, rutin, quercitrin, quercetin, and ursolic acid in S. buxifolia stem bark and leaves; quercitrin and ursolic acid were the main compounds in the ethyl acetate and dichloromethane fractions from leaves and stem bark. The crude extract (3 and 30mg/ml), and the ethyl acetate and dichloromethane fractions (0.1 and 1mg/ml) of both the stem bark and leaves inhibited Na(+),K(+)-ATPase activity in heart and brain samples. We found that, of the identified compounds, only ursolic acid (0.1mg/ml) was able to diminish Na(+), K(+)-ATPase activity in heart and brain samples.
These data indicated that the cardiotonic effects of S. buxifolia may be due to the inhibition of Na(+),K(+)-ATPase activity in heart muscle, supporting the popular use of this plant as a treatment for heart failure.
南美鼠李是一种原产于南美的树木，被用作强心剂；然而，这一特性尚未与明确的作用机制或特定化合物相关联。
鉴于钠钾ATP酶作为治疗心力衰竭药物靶点的重要性，本研究旨在探究南美鼠李粗提物及其馏分（二氯甲烷、乙酸乙酯和正丁醇馏分）可能的抑制作用，并鉴定体外对钠钾ATP酶活性有影响的化合物。
首先，我们通过高效液相色谱对粗提物及其馏分进行表征，然后监测它们对成年雄性Wistar大鼠心肌和脑膜中钠钾ATP酶活性的影响。
我们在南美鼠李的茎皮和叶片中鉴定出了没食子酸、绿原酸、咖啡酸、芦丁、槲皮苷、槲皮素和熊果酸；槲皮苷和熊果酸是叶片和茎皮乙酸乙酯和二氯甲烷馏分中的主要化合物。粗提物（3和30mg/ml）以及茎皮和叶片的乙酸乙酯和二氯甲烷馏分（0.1和1mg/ml）均抑制了心脏和脑样本中的钠钾ATP酶活性。我们发现，在鉴定出的化合物中，只有熊果酸（0.1mg/ml）能够降低心脏和脑样本中的钠钾ATP酶活性。
这些数据表明，南美鼠李的强心作用可能是由于其对心肌中钠钾ATP酶活性的抑制，这支持了该植物在治疗心力衰竭方面的广泛应用。
