Centro de Investigación en Biotecnología, Universidad Autónoma del Estado de Morelos, Avenida Universidad 1001, Colonia Chamilpa, Cuernavaca, Morelos 62210, Mexico.
J Ethnopharmacol. 2010 Feb 3;127(2):551-4. doi: 10.1016/j.jep.2009.11.020. Epub 2009 Nov 29.
Ternstroemia pringlei represents one of the most widely employed and commercially exploited medicinal plant in Mexico, used popularly as a tranquilizer and for the treatment of insomnia.
To investigate the sedative constituents of the plant through a bio-guided fractionation of extracts derived from calyx and fruits.
Crude extracts with different polarities (CHCl(3), AcOEt, MeOH, aqueous) were prepared and subjected to chromatographic fractionation, leading to the isolation of the sedative compound (1) from the MeOH crude extract. The identity of 1 was unequivocally established by means of 1D and 2D NMR spectroscopic analysis. The sleeping time induced by sodium pentobarbital and the elevated plus-maze models were performed on mice to determine the sedative and anxiolytic activities, respectively. Bioactivity was also investigated though in vitro GABA release experiments using mice brain slices.
The sedative compound was established as jacaranone (1), and its effect was clearly demonstrated through a dose-dependent response analysis (ED(50) = 25 mg/kg mouse weight). When tested in the elevated plus-maze model, none of the extracts from Ternstroemia pringlei displayed anxiolytic activity. GABA release experiments showed that the MeOH and aqueous crude extracts released this neurotransmitter at a ratio of 217 and 179 pmol/g protein, respectively, evidencing the presence of other bioactive constituents in the extracts apart of 1, whose activity was absent in this model.
Although 1 has been isolated and identified in a number of plant species, this is the first time that its sedative effect has been demonstrated. No previous record exists of other sedative compounds having been isolated from Ternstroemia pringlei.
植物在墨西哥被广泛应用于医疗用途，民间用作镇静剂和治疗失眠。本研究旨在通过对金缕梅科萼和果实提取物的生物导向分离，寻找该植物中的镇静成分。
不同极性（CHCl3、AcOEt、MeOH、水）的粗提取物经色谱分离后，从 MeOH 粗提取物中分离出镇静化合物 1。通过 1D 和 2D NMR 波谱分析明确了 1 的结构。通过戊巴比妥钠诱导的睡眠时间和高架十字迷宫模型，分别在小鼠体内确定了 1 的镇静和抗焦虑活性。通过体外 GABA 释放实验也研究了生物活性。
镇静化合物被鉴定为 jacaranone（1），并通过剂量依赖性反应分析清楚地证明了其效果（ED50 = 25mg/kg 小鼠体重）。当在高架十字迷宫模型中进行测试时，金缕梅属萼和果实的提取物均没有显示出抗焦虑活性。GABA 释放实验表明，MeOH 和水粗提取物分别以 217 和 179pmol/g 蛋白的比例释放这种神经递质，表明提取物中除 1 之外还存在其他生物活性成分，而 1 在该模型中没有活性。
尽管 1 已在许多植物物种中被分离和鉴定，但这是首次证明其镇静作用。以前从未从金缕梅属萼和果实中分离出其他镇静化合物。
