N-Substituted Nipecotic Acids as (S)-SNAP-5114 Analogues with Modified Lipophilic Domains

Potential mGAT4 inhibitors derived from the lead substance (S)-SNAP-5114 have been synthesized and characterized for their inhibitory potency. Variations from the parent compound included the substitution of one of its aromatic 4-methoxy and 4-methoxyphenyl groups, respectively, with a more polar moiety, including a carboxylic acid, alcohol, nitrile, carboxamide, sulfonamide, aldehyde or ketone function, or amino acid partial structures. Furthermore, it was investigated how the substitution of more than one of the aromatic 4-methoxy groups affects the potency and selectivity of the resulting compounds. Among the synthesized test substances (S)-1-{2-[(4-formylphenyl)bis(4-methoxyphenyl)-methoxy]ethyl}piperidine-3-carboxylic acid, that features a carbaldehyde function in place of one of the aromatic 4-methoxy moieties of (S)-SNAP-5114, was found to have a pIC₅₀ value of 5.89±0.07, hence constituting a slightly more potent mGAT4 inhibitor than the parent substance while showing comparable subtype selectivity.     

餐饮废油生物柴油低温流动性的改进研究

使用气-质联用仪测定餐饮废油生物柴油(WCME)和-10号柴油(-10PD)的组成,使用冷滤点试验器和运动黏度试验器测定WCME的低温流动性,同时使用调合、添加低温流动性改进剂的方法改进WCME的低温流动性。实验结果表明,WCME主要由饱和脂肪酸甲酯和不饱和脂肪酸甲酯组成,质量分数分别为27.63%和71.81%;WCME冷滤点为0℃,运动黏度(40℃)为4.41mm2/s;WCME与-10PD调合后,冷滤点降低,其中B20的冷滤点最低,为-13℃,运动黏度随着WCME的体积分数的减少,逐渐接近-10PD的运动黏度。通过添加低温流动性改进剂,WCME,B10,B20的冷滤点分别从0,-8,-13℃降至-4,-26,-25℃。     

Characteristic of polysaccharides from Flammulina velutipes in vitro digestion under salivary,simulated gastric and small intestinal conditions and fermentation by human gut microbiota

In this study, in vitro digestion and fermentation of Flammulina velutipes -derived polysaccharides (FVP) were investigated. It was found that FVP mainly consisted of 48.45% glucose, 15.40% mannose, 14.60% xylose, 11.80% fucose and 9.90% galactose. The -human saliva, simulated gastric and small intestinal juices conditions did not break down the FVP. Based on in vitro fermentation tests, FVP modulated the composition of gut microbiota by elevating the amounts of Bifidobacteriaceae and Bacteroidaceae and reducing the numbers of genera Lachnospiraceae and Enterococcaceae. Meanwhile, FVP affected the synthesis of short-chain fatty acids derived from gut microbiota.