Synthesis and antitumor activity evaluation of glycoconjugates derived from natural product harmine / 中国药科大学学报

@#Based on our previous work, the study herein designed and synthesized eight glycoconjugates of natural product harmine (14a-14h)by introducing a cyclohexylmethyloxyl group at its C7 position and coupling a methyl-2-amino-β-D-glucopyranoside to the N9 position through different lengths of alkyl chains.In vitro anti-tumor activity screening and structure-activity relationship studies showed that the antitumor activity of the conjugates increased with the lengthening of the alkyl chain in the linker.Compound 14h exhibited significantly better proliferative inhibitory activity against MDA-MB-231 breast cancer cells than harmine.As compared to harmine, the introduction of the carbohydrate moiety improved the water solubility of compound 14h and enhanced its tumor cell selectivity through the Warburg effect.Mechanism of action studies revealed that compound 14h induced apoptosis and G0/G1 cell cycle arrest in MDA-MB-231 cells, and inhibited tumor cell migration by interfering with epithelial-mesenchymal transition process.This study provides a new approach for the development of antitumor drugs based on harmine.

Microbial monitoring of urban drinking water in Jiangxi Province from 2016 to 2020 / 上海预防医学

ObjectiveTo monitor the microbes in urban drinking water in Jiangxi from 2016 to 2020， to analyze the change in microbial qualification rate， and to provide a scientific basis for government decision-making. MethodsAccording to the Standard Examination Method for Drinking Water （GB/T 5750‒2006） and the Standards for Drinking Water Quality （GB 5749‒2006）， the water samples were collected， tested and evaluated for hygienic safety. The chi-square test was used to compare the qualification rates among different water periods， water source types， water supply modes， water samples， treatment processes， and disinfection methods. ResultsA total of 10 584 water samples were collected and examined from 2016 to 2020，with a qualification rate of 97.72%. The qualified rate of the microbiological index increased gradually over the years. There was no statistically significant difference in the microbiological qualification rate of water samples monitored in different water periods （χ2=0.718，P=0.398）， and the qualification rates were 97.85% and 97.60% in dry and abundant water periods respectively. There was a statistically significant difference in the qualification rates of water samples monitored in different water source types （χ2=79.560，P=0.398）， with groundwater having a higher qualification rate of 98.83% than surface water （97.70%）. The microbiological pass rate of water samples differed among different water supply methods （χ2=201.836，P<0.001）. The microbiological pass rates of municipal centralized water supply， self-built centralized water supply and secondary water supply were 97.51%， 88.94% and 96.56% respectively. The microbiological pass rates of water samples differed among different treatment processes. There were differences in the qualification rates of the water samples between different treatment processes（χ2=855.034，P<0.001）， with 98.22%， 67.19%， 95.60% and 53.13% of the conventionally treated， precipitated filtered， disinfected only and untreated water samples， respectively. The differences in the microbiological qualification rates of the monitored water samples between different disinfection methods were statistically significant （χ2=904.993，P<0.001）. Chlorination disinfection， chlorine dioxide disinfection， other disinfection methods and non-disinfected water samples had the pass rates of 98.35%， 98.19%， 84.38% and 60.16%， respectively. ConclusionThe qualified rate of the microbiological index of drinking water in Jiangxi increases year by year， but there are still some drinking water without appropriate disinfectants and water quality treatment processes. There is still a need to strengthen the purification， disinfection and monitoring of drinking water.

Contribution of basal and early phase insulin secretion to plasma glucose level in patients with type 2 diabetes / 中华内分泌代谢杂志

Objective To investigate the effects of basal and early phase insulin secretion on plasma glucose level in type 2 diabetes. Methods Plasma glucose and true insulin levels were measured at 0, 30, 60, 120 min during standard meal test in 81 patients with type 2 diabetes. Insulin sensitivity index (ISI) and insulin secretion index (?I 30 /?G 30 ) were calculated for evaluating the insulin sensitivity. Contributions of basal and early insulin secretion to plasma glucose level were evaluated by multivariate regression analysis with SAS software. Results ISI and ?I 30 /?G 30 showed nearly equal effects on plasma glucose levels by multivariate regression analysis. Among insulin levels of different time points during standard meal test, basal and postprandial 60 min insulin levels played important roles in changes of plasma glucose levels. The effect of fasting insulin on the area under plasma glucose curve was stronger than that of ?I 30 /?G 30 . Conclusion Both basal and early insulin secretions greatly contribute to glycemic control.