Ramirez Guillermo, Zamilpa Alejandro, Zavala Miguel, Perez Julia, Morales Dulce, Tortoriello Jaime
Centro de Investigación Biomédica del Sur, Instituto Mexicano del Seguro Social (IMSS), Argentina 1, 62790 Xochitepec, Morelos, Mexico.
Centro de Investigación Biomédica del Sur, Instituto Mexicano del Seguro Social (IMSS), Argentina 1, 62790 Xochitepec, Morelos, Mexico.
J Ethnopharmacol. 2016 Jun 5;185:1-8. doi: 10.1016/j.jep.2016.03.014. Epub 2016 Mar 10.
Tecoma stans is traditionally used by several ethnical groups in Mexico and Central America to treat diabetes. This species is mentioned in the majority of the ethnopharmacological studies compiled in Mexico focused in medicinal plants used as anti-diabetic treatment.
Recently, this plant was found to display a high level of pancreatic lipase inhibitory activity, in addition to the several action mechanisms already described. Here we show the phytochemical and in vitro pharmacological characterization of some of the compounds responsible for the antilipase activity.
Starting with a hydroalcoholic extract, fractions were obtained by liquid-liquid separation and successive processes of column chromatography purifications. Lipase inhibitory activity was measured employing a spectrophotometric analysis. For structural elucidation (1)H and (13)C NMR experiments were used. HPLC was used to quantify and confirm the identity of the bioactive compounds.
Bio-guided chemical purification of the hydroalcoholic extract produced an organic fraction (ethyl acetate, TsEA), flavone fractions (TsC1F13), (TsC1F15), (TsC1F16) and isolated compounds (chrysoeriol, apigenin, luteolin, and verbascoside) with the capability to inhibit the activity of pancreatic lipase. The most active fraction (TsC2F6B) was constituted by a mixture of Chrysoeriol (5,7-dihydroxy-2-[4-hydroxy-3-methoxyphenyl]chromen-4-one, 96% ) and Apigenin (4%). This flavone mixture displayed a percentage of inhibition of 85% when it was eavaluated at 0.25mg/mL. Luteolin and chrysoeriol produced a noncompetitive and mixed inhibition with values of IC50=63 and 158µM respectively. The content of chrysoeriol was also quantified in the hydroalcoholic extract (TsHAE) and organic fraction (TsEA) as 1% and 7% respectively. All of this confirms that high proportion of both flavones produce an increase of the biological activity due to they show the highest inhibition of lipase enzyme in a concentration dependant way.
These results evidence that the medicinal use of T. stans could be in part because of its lipase inhibitory activity allowing to adapt the administration of this plant before meals. Also this data could help to develop a novel phytopharmaceutical drug (standardized in luteolin, chrysoeriol, and apigenin) auxiliary for the Type 2 Diabetes mellitus.
在墨西哥和中美洲，几个民族群体传统上使用黄花梧桐树来治疗糖尿病。在墨西哥编纂的大多数民族药理学研究中，该物种被提及，这些研究集中于用作抗糖尿病治疗的药用植物。
最近，除了已经描述的几种作用机制外，还发现这种植物具有高水平的胰脂肪酶抑制活性。在此，我们展示了一些负责抗脂肪酶活性的化合物的植物化学和体外药理学特征。
从水醇提取物开始，通过液 - 液分离和柱色谱纯化的连续过程获得馏分。采用分光光度分析测量脂肪酶抑制活性。使用（1）H和（13）C NMR实验进行结构解析。使用HPLC定量并确认生物活性化合物的身份。
水醇提取物的生物导向化学纯化产生了具有抑制胰脂肪酶活性能力的有机馏分（乙酸乙酯，TsEA）、黄酮馏分（TsC1F13）、（TsC1F15）、（TsC1F16）和分离的化合物（白杨素、芹菜素、木犀草素和毛蕊花糖苷）。活性最高的馏分（TsC2F6B）由白杨素（5,7 - 二羟基 - 2 - [4 - 羟基 - 3 - 甲氧基苯基]色原酮 - 4 - 酮，96%）和芹菜素（4%）的混合物组成。当以0.25mg/mL进行评估时，这种黄酮混合物显示出85%的抑制率。木犀草素和白杨素分别产生非竞争性和混合性抑制，IC50值分别为63和158μM。水醇提取物（TsHAE）和有机馏分（TsEA）中白杨素的含量也分别定量为1%和7%。所有这些都证实，这两种黄酮的高比例会导致生物活性增加，因为它们以浓度依赖性方式表现出对脂肪酶的最高抑制作用。
这些结果表明，黄花梧桐树的药用部分原因可能是其脂肪酶抑制活性，这使得可以在饭前服用这种植物。此外，这些数据有助于开发一种新型植物药（以木犀草素、白杨素和芹菜素标准化）作为2型糖尿病的辅助药物。
