Nachar Abir, Eid Hoda M, Vinqvist-Tymchuk Melinda, Vuong Tri, Kalt Wilhelmina, Matar Chantal, Haddad Pierre S
Natural Health Products and Metabolic Diseases Laboratory, Department of Pharmacology and Physiology, Université de Montréal, Station Centre-Ville, P.O. Box 6128, Montréal, Québec, H3C 3J7, Canada.
Canadian Institutes of Health Research Team in Aboriginal Antidiabetic Medicines and Montreal Diabetes Research Center, Montreal, Canada.
BMC Complement Altern Med. 2017 Mar 4;17(1):138. doi: 10.1186/s12906-017-1650-2.
We recently reported that blueberry juice fermented (FJ) with Serratia vaccinii bacterium has antidiabetic activities both in vivo and in vitro. The purpose of this project was to elucidate the effect of FJ on glucose homeostasis in liver and skeletal muscle cells and to identify active fractions/compounds responsible for this effect.
FJ was fractionated using standard chromatography procedures. Hepatic (H4IIE, HepG2) and skeletal muscle cells (C2C12) were treated with maximum non-toxic concentrations of FJ, fractions and isolated compounds thereof. Glucose-6-phosphatase (G6Pase) activity was measured using glucose oxidase method. To measure glucose uptake and glycogen synthase (GS) activity, radioactive assays were used.
Fractionation of FJ yielded seven fractions. FJ and its phenolic fractions F2, F3-1 and F3-2 respectively inhibited G-6Pase by 31, 45, 51 and 26%; activated GS by 2.3-, 2.3-, 2.2- and 2-fold; and stimulated glucose uptake by 19, 25, 18 and 15%, as compared to DMSO vehicle control. Subfractionation of the active fractions yielded 4 compounds (catechol, chlorogenic, gallic and protocatechuic acid). Catechol, yielding the greatest bioactivity in G6Pase and glucose uptake assays, decreased G6Pase activity by 54%, increased GS by 2-fold and stimulated glucose uptake by 44% at 45.5 μM.
This study identifies novel potential antidiabetic compounds that can help standardize FJ.
我们最近报道，用粘质沙雷氏菌发酵的蓝莓汁（FJ）在体内和体外均具有抗糖尿病活性。本项目的目的是阐明FJ对肝脏和骨骼肌细胞葡萄糖稳态的影响，并确定造成这种影响的活性成分/化合物。
采用标准色谱程序对FJ进行分离。用FJ、其分离组分及其分离出的化合物的最大无毒浓度处理肝脏（H4IIE、HepG2）和骨骼肌细胞（C2C12）。采用葡萄糖氧化酶法测定葡萄糖-6-磷酸酶（G6Pase）活性。使用放射性测定法测量葡萄糖摄取和糖原合酶（GS）活性。
FJ分离得到七个组分。与二甲基亚砜溶剂对照相比，FJ及其酚类组分F2、F3-1和F3-2分别使G-6Pase活性降低31%、45%、51%和26%；使GS活性分别提高2.3倍、2.3倍、2.2倍和2倍；使葡萄糖摄取分别增加19%、25%、18%和15%。对活性组分进行进一步细分得到4种化合物（儿茶酚、绿原酸、没食子酸和原儿茶酸）。在G6Pase和葡萄糖摄取试验中具有最大生物活性的儿茶酚，在浓度为45.5μM时，使G6Pase活性降低54%，使GS活性提高2倍，并使葡萄糖摄取增加44%。
本研究鉴定出了有助于使FJ标准化的新型潜在抗糖尿病化合物。
