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Lf纳米分散体是一种具有强效α-葡萄糖苷酶和胰脂肪酶抑制作用的降血糖产品。

Lf nanodispersion is a hypoglycemic product with a potent α-glucosidase and pancreatic lipase inhibitor effect.

作者信息

Prada Ariadna Lafourcade, Keita Hady, de Souza Tatiane Pereira, Lima Emerson Silva, Acho Leonard Domingo Rosales, da Silva Márcia de Jesus Amazonas, Carvalho José Carlos Tavares, Amado Jesus Rafael Rodriguez

机构信息

Pharmacy Department, Faculty of Natural Sciences, University of Oriente, Patricio Lumumba s/n, Santiago de Cuba, CP 84500 Santiago de Cuba, Cuba.

Drug Research Laboratory, Federal University of Amapá, Rodovia Juscelino Kubitschek, km 2, Jardim Marco Zero, CEP: 68903-419 Macapá, AP, Brazil.

出版信息

Saudi Pharm J. 2019 Feb;27(2):191-199. doi: 10.1016/j.jsps.2018.10.003. Epub 2018 Oct 17.

Abstract

PURPOSE

This study aimed to evaluate the hypoglycemic effect, antioxidant, α-glucosidase and lipase inhibitory activity, and the cytotoxicity of the nanodispersion (CgND).

METHODS

The hypoglycemic effect was evaluated in alloxan-induced diabetic mice. The particle size, polydispersion index, ζ-potential, and conductivity, as well as the drug-loaded content, were monitored in shelf-live, along a year. The delivery profile was evaluated in simulated intestinal fluids at pH 6.5 and 7.4. The antioxidant effect was evaluated as DPPH and ABTS inhibition. The murine α-glucosidase inhibitory activity and the lipase-inhibitory effect were evaluated Cytotoxicity was evaluated by the Alamar blue test.

RESULTS

CgND remained stable for a year in shelf conditions. The hypoglycemic effect in a dose of 10 mg/kg was not statistically different from glibenclamide 25 mg/kg. Nanoparticles released 100% of extract in 120 min at pH 6.5 and 7.4. Nanodispersion exhibited a potent α-glucosidase and lipase-inhibitory effect with IC of 3.96 and 0.58 µg/mL, respectively. A strong antioxidant activity against DPPH (IC 0.65 µg/mL) and ABTS (0.48 µg/mL) was also observed. The hypoglycemic effect could occur, at least in part, via antioxidant and α-glucosidase inhibition. CgND is non-cytotoxic in MRC-5 line cell. This nanodispersion is a promising nanotechnological product that could be used in pharmaceuticals for the treatment of Type II diabetes and related complications as obesity.

摘要

目的

本研究旨在评估纳米分散体(CgND)的降血糖作用、抗氧化作用、α-葡萄糖苷酶和脂肪酶抑制活性以及细胞毒性。

方法

在四氧嘧啶诱导的糖尿病小鼠中评估降血糖作用。在一年的储存期内监测其粒径、多分散指数、ζ电位、电导率以及载药量。在pH值为6.5和7.4的模拟肠液中评估释放情况。通过DPPH和ABTS抑制来评估抗氧化作用。评估小鼠α-葡萄糖苷酶抑制活性和脂肪酶抑制作用。通过alamar蓝试验评估细胞毒性。

结果

CgND在储存条件下一年内保持稳定。10mg/kg剂量的降血糖作用与25mg/kg格列本脲相比无统计学差异。纳米颗粒在pH值为6.5和7.4时120分钟内释放100%的提取物。纳米分散体表现出强效的α-葡萄糖苷酶和脂肪酶抑制作用,IC50分别为3.96和0.58μg/mL。还观察到对DPPH(IC50 0.65μg/mL)和ABTS(0.48μg/mL)有很强的抗氧化活性。降血糖作用可能至少部分通过抗氧化和α-葡萄糖苷酶抑制发生。CgND对MRC-5细胞系无细胞毒性。这种纳米分散体是一种有前景的纳米技术产品,可用于制药治疗II型糖尿病及肥胖等相关并发症。

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