Galdino Pablinny M, Carvalho Adryano A V, Florentino Iziara F, Martins José L R, Gazola Andressa C, de Paula José R, de Paula Joelma A M, Torres Luce M B, Costa Elson A, de Lima Thereza Christina M
Laboratório de Neurofarmacologia, Farmacologia, CCB, UFSC, Florianópolis, SC, Brazil; Laboratório de Farmacologia de Produtos Naturais, ICB, UFG, Goiânia, GO, Brazil.
Laboratório de Farmacologia de Produtos Naturais, ICB, UFG, Goiânia, GO, Brazil.
J Ethnopharmacol. 2015 Jul 21;170:218-25. doi: 10.1016/j.jep.2015.05.015. Epub 2015 May 14.
Lafoensia pacari A. St.-Hil. (Lythraceae), known popularly as "pacari" or "mangaba-brava" is popularly used in the state of Goiás, Brazil. The stem bark or leaves are used to treat cancer, gastric disorders, inflammation and as a tonic to treat loss of enthusiasm.
Previous results suggest that the ethanol:water 7:3 extract of the stem bark of L. pacari (PEx) has antidepressant-like activity in male mice. Our aim was to perform the PEx׳s bioguided fractionation and evaluate the monoaminergic system involvement in the antidepressant effect as well as progress in the study of L. pacari mechanism of action.
Mice (30-35g) orally treated (24, 5 and 1h) with PEx (100, 300 or 1000mg/kg), chloroform (ChloF-70mg/kg), ethyl acetate (180mg/kg), n-butanol (370mg/kg) and aqueous (1g/kg) fractions were submitted to the forced swimming test. To assess the mechanism of action, different groups of mice were pretreated with p-chlorophenylalanine (PCPA-100mg/kg, 4 days, i.p.) and alpha-methyl-p-tyrosine (AMPT-100mg/kg, 4h, i.p.) to assess the involvement of serotoninergic and catecholaminergic systems in the ChloF effects, respectively. A putative in vitro inhibition of monoamine oxidase (MAO) activity as well as the ex vivo hippocampal brain-derived neurotrophic factor (BDNF) quantification were carried out. Phytochemical screening, spectroscopy and chromatography analysis were used for identification of compounds present in ChloF.
After the fractionation, the ChloF 70mg/kg was the most active fraction, reducing the immobility time by 22%. Pre-treatments with both PCPA and AMPT abolished the ChloF effects, suggesting that ChloF antidepressant-like effect is dependent on serotonergic and catecholaminergic systems. ChloF did not inhibited MAO-A or MAO-B activity, excluding this as possible mechanism of action. ChloF augmented hippocampal BDNF level, which could be accounted for its antidepressant-like effect. Phytochemical screening showed the presence of saponins, tannins, steroids and triterpene in the PEx, and the presence of triterpene and steroids in ChloF. The spectroscopy and chromatography analysis identified lupeol, β-sitosterol and stigmasterol in ChloF.
ChloF is the fraction that better retained the crude extract active constituents. ChloF presents antidepressant-like effect that involves both serotonergic and catecholaminergic systems without inhibiting MAO enzymatic activity; this fraction also increases the hippocampal BDNF levels.
拉福恩西亚帕卡里A.圣-希尔（千屈菜科），俗称“帕卡里”或“野生番樱桃”，在巴西戈亚斯州被广泛使用。其茎皮或叶子用于治疗癌症、胃部疾病、炎症，并作为滋补剂治疗精神萎靡。
先前的结果表明，拉福恩西亚帕卡里茎皮的乙醇：水7:3提取物（PEx）在雄性小鼠中具有抗抑郁样活性。我们的目的是对PEx进行生物导向分级分离，并评估单胺能系统在抗抑郁作用中的参与情况，以及推进对拉福恩西亚帕卡里作用机制的研究。
对体重30 - 35克的小鼠口服给予PEx（100、300或1000毫克/千克）、氯仿（ChloF - 70毫克/千克）、乙酸乙酯（180毫克/千克）、正丁醇（370毫克/千克）和水相（1克/千克）分级部分（分别在24、5和1小时给药），然后进行强迫游泳试验。为评估作用机制，不同组的小鼠分别用对氯苯丙氨酸（PCPA - 100毫克/千克，腹腔注射，4天）和α-甲基-对酪氨酸（AMPT - 100毫克/千克，腹腔注射，4小时）预处理，以分别评估5-羟色胺能和儿茶酚胺能系统在ChloF作用中的参与情况。进行了单胺氧化酶（MAO）活性的体外假定抑制以及海马脑源性神经营养因子（BDNF）的体内定量分析。采用植物化学筛选、光谱学和色谱分析来鉴定ChloF中存在的化合物。
分级分离后ChloF 70毫克/千克是活性最高的部分，使不动时间减少了22%。PCPA和AMPT预处理均消除了ChloF的作用，表明ChloF的抗抑郁样作用依赖于5-羟色胺能和儿茶酚胺能系统。ChloF未抑制MAO - A或MAO - B活性，排除了这作为可能的作用机制之一。ChloF提高了海马BDNF水平，这可能解释了其抗抑郁样作用。植物化学筛选显示PEx中存在皂苷、单宁、类固醇和三萜，ChloF中存在三萜和类固醇。光谱学和色谱分析鉴定出ChloF中的羽扇豆醇、β-谷甾醇和豆甾醇。
ChloF是更好地保留了粗提物活性成分的分级部分。ChloF呈现出抗抑郁样作用，涉及5-羟色胺能和儿茶酚胺能系统且不抑制MAO酶活性；该分级部分还增加了海马BDNF水平。
