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Wilson Eik Filho,Bruna Juliana Wanczinski Ferrari,Marina Masetto Antunes,Patrícia Batista Travassos,Helenir Medri de Souza,Eniuce Menezes de Souza,Roberto Barbosa Bazotte 한국식품영양과학회 2021 Journal of medicinal food Vol.24 No.9
We compared the effect of oral glucose versus oral glucose combined with glycerol (glucose + glycerol) in promoting glucose recovery during hypoglycemia. These studies were carried out in two series of experiments. In the first series of experiments, 16 overnight fasted rats received an intraperitoneal injection of lispro insulin (1 IU/kg), and 25 min later, they received oral water (control), glucose (0.25 g/kg), glycerol (2.5 g/kg), or glucose (0.25 g/kg) + glycerol (2.5 g/kg). In the second series of experiments on 164 eligible type 1 diabetic (T1D) patients, 30 individuals with a history of hypoglycemia were recruited. Five volunteers did not meet the inclusion criteria and two subjects were excluded after starting the clinical investigation; 23 patients concluded the study. All patients with symptoms of hypoglycemia ingested oral glucose (15 g) or glucose (15 g) + glycerol (9.45 g). To treat hypoglycemia in T1D patients, preparations containing glucose alone or glucose + glycerol were used alternately (2 weeks/2 weeks) in a double-blind crossover scheme. Throughout the clinical research (4 weeks), glucose concentrations were assessed with a continuous glucose monitoring device and the results after the use of glucose alone or glucose + glycerol preparations were compared. Oral glucose combined with glycerol was more effective in promoting glucose recovery in comparison with glucose alone, not only in rats but also in T1D patients. Taken together, our experimental and clinical investigations reported the best performance of oral administration of glucose + glycerol in comparison with isolated glucose.
Lee, Hyosung,Park, Ki Duk,Torregrosa, Robert,Yang, Xiao-Fang,Dustrude, Erik T.,Wang, Yuying,Wilson, Sarah M.,Barbosa, Cindy,Xiao, Yucheng,Cummins, Theodore R.,Khanna, Rajesh,Kohn, Harold American Chemical Society 2014 Journal of medicinal chemistry Vol.57 No.14
<P/><P>We prepared 13 derivatives of <I>N</I>-(biphenyl-4′-yl)methyl (<I>R</I>)-2-acetamido-3-methoxypropionamide that differed in type and placement of a R-substituent in the terminal aryl unit. We demonstrated that the R-substituent impacted the compound’s whole animal and cellular pharmacological activities. In rodents, select compounds exhibited excellent anticonvulsant activities and protective indices (PI = TD<SUB>50</SUB>/ED<SUB>50</SUB>) that compared favorably with clinical antiseizure drugs. Compounds with a polar, aprotic R-substituent potently promoted Na<SUP>+</SUP> channel slow inactivation and displayed frequency (use) inhibition of Na<SUP>+</SUP> currents at low micromolar concentrations. The possible advantage of affecting these two pathways to decrease neurological hyperexcitability is discussed.</P>