Morales Dulce, Ramirez Guillermo, Herrera-Arellano Armando, Tortoriello Jaime, Zavala Miguel, Zamilpa Alejandro
Facultad de Medicina, Universidad Autónoma del Estado de Morelos, Cuernavaca 62350, Mexico.
Centro de Investigación Biomédica del Sur, Instituto Mexicano del Seguro Social, Xochitepec 62790, Mexico.
Evid Based Complement Alternat Med. 2018 Jul 16;2018:8781352. doi: 10.1155/2018/8781352. eCollection 2018.
Current antiobesity and antidiabetic tools have been insufficient to curb these diseases and frequently cause side effects; therefore, new pancreatic lipase and -glucosidase inhibitors could be excellent aids for the prevention and treatment of these diseases. The aim of this study was to identify, quantify, and characterize the chemical compounds with the highest degree of inhibitory activity of these enzymes, contained in a hydroalcoholic extract. Chemical purification was performed by liquid-liquid separation and column chromatography. Inhibitory activities were measured , employing acarbose, orlistat, and a hydroalcoholic extract as references. For structural elucidation, Nuclear Magnetic Resonance was carried out, and High Performance Liquid Chromatography was used to quantify the compounds. For -glucosidases, hydroalcoholic extract and its ethyl acetate fraction showed half-maximal Inhibitory Concentration (IC) values of 700 and 250 g/mL, for lipase, 480 and 718 g/mL, while showed 260 and 587 g/mL. The most active compounds were identified as ethyl gallate (, IC 832 M) and gallic acid (, IC 969 M); both displayed competitive inhibition of -glucosidases and isoorientin (, IC 201 M), which displayed uncompetitive inhibition of lipase. These data could be useful in the development of a novel phytopharmaceutical drug.
目前的抗肥胖和抗糖尿病药物不足以控制这些疾病，且经常会引起副作用；因此，新型胰脂肪酶和α-葡萄糖苷酶抑制剂可能是预防和治疗这些疾病的理想辅助药物。本研究的目的是鉴定、定量并表征水醇提取物中对这些酶具有最高抑制活性的化合物。通过液-液分离和柱色谱法进行化学纯化。以阿卡波糖、奥利司他和水醇提取物作为对照，测定抑制活性。采用核磁共振进行结构解析，并用高效液相色谱法对化合物进行定量。对于α-葡萄糖苷酶，水醇提取物及其乙酸乙酯馏分的半数抑制浓度（IC）值分别为700和250 μg/mL，对于脂肪酶，分别为480和718 μg/mL，而[此处原文缺失对照物质名称]分别为260和587 μg/mL。最具活性的化合物被鉴定为没食子酸乙酯（[此处原文缺失具体数值]，IC 832 μM）和没食子酸（[此处原文缺失具体数值]，IC 969 μM）；二者均对α-葡萄糖苷酶表现出竞争性抑制作用，而异荭草素（[此处原文缺失具体数值]，IC 201 μM）对脂肪酶表现出非竞争性抑制作用。这些数据可能有助于开发一种新型植物药。
