A Method for the Synthesis of Thioindoles through Copper-Catalyzed C-S Bond Coupling Reaction.

We herein report the copper-catalyzed C-S bond coupling reaction of indoles with N-thiosuccinimides, resulting in moderate to excellent yields of mono- and bis-sulfenylated compounds such as arylthioindoles, alkylthioindoles, selenylated indoles, and cysteine-substituted indoles. Thioarylation and thioglycosylation at the C2 position of indole alkaloids in the Radix Isatidis were achieved via structural modification. The first total syntheses of isatindigotindolosides III and IV have been successfully carried out. The electrophilic sulfenyl bromides generated in situ can play an important role in the catalytic cycle.

Hypervalent Iodine(III)-Mediated Umpolung Dialkoxylation of N-Substituted Indoles.

Herein, we report dialkoxylation of N-substituted indoles through a hypervalent iodine-mediated umpolung strategy, affording trans-2,3-dimethoxyindolines with up to 95% yield. In addition, C5-selective bromination of 2,3-dialkoxyindoline via NBS-mediated rearomatization was achieved. DFT calculation of the sequence of electrophilic addition and nucleophilic substitution pathway of N-substituted indoles has also been investigated.

[Multiphase Spatial Distribution Characteristics of Cd Morphology in Typical Intertidal Zones in the Guangdong-Hong Kong-Macao Greater Bay Area and Its Influencing Factors].

Simultaneous sampling and observation were conducted at 14 stations in typical intertidal zones of the Guangdong-Hong Kong-Macao greater bay area. The spatial distribution characteristics of Cd morphology in surface water, pore water, suspended matters, and sediments at each sampling site were analyzed, and the influencing factors of Cd morphology changes in each medium were discussed using statistical analyses based on environmental factors. The results showed that the total contents of Cd in surface water, pore water, suspended matters, and sediments in each intertidal zone ranged from 0.41-15.03 µg·L-1, 0.41-27.54 µg·L-1, 0.41-4.88 mg·kg-1, and 0.20-5.30 mg·kg-1, respectively. The contents of Cd in Shajiao Bay were significantly higher than those in other sampling sites, which should be related to the developed electronics and manufacturing industries in Dongguan. The concentration of Cd in surface water was slightly lower than that in pore water, whereas the content of Cd in suspended matter was comparable to that in sediment at the same sampling site. The results of morphological analysis showed that the ionic-state Cd was dominant in both surface water and pore water, accounting for 67.23%-97.56% and 33.33%-97.16%, respectively. In suspended matter and sediment, Cd was mainly in the residual state, accounting for 45.45%-96.36% and 45.80%-97.27%, respectively. Pearson correlation analysis showed that the complex-state Cd in the aqueous phase was negatively correlated with oxidation reduction potential (ORP) and pH and positively correlated with total organic carbon. The bioavailable Cd in solid sediment was significantly positively correlated with the proportion of clay, ORP, and solid organic carbon and significantly negatively correlated with pH. The single factor linear regression analysis showed that ORP had the greatest effect on the complex-state Cd in the aqueous phase, with regression coefficients of 0.864 and 0.824, respectively. The bioavailable Cd in solid sediment at different depths was significantly affected by the proportion of clay, and the regression coefficients were 0.968, 0.980, 0.977, and 0.877, respectively. The above results indicate that the distribution of total Cd content in the typical intertidal environment of the Greater Bay Area was affected by the characteristics of urban economic development, whereas the allocation of Cd morphology was closely related to environmental factors.

Early changes in pulmonary function and intrarenal haemodynamics and the correlation between these sets of parameters in patients with T2DM.

PURPOSE: The main objectives of this study were to assess the early changes in pulmonary function and intrarenal haemodynamics and to determine the correlation between pulmonary function and intrarenal haemodynamics in patients with type 2 diabetes mellitus (T2DM). METHODS: 96 patients with T2DM (diabetes group) without diabetes kidney disease (DKD) and 33 healthy subjects (control group) were enrolled in studies intended to assess the early changes in pulmonary function and intrarenal haemodynamics associated with diabetes, as well as to determine the correlation between pulmonary function and intrarenal haemodynamics. RESULTS: Pulmonary functional parameters were negatively correlated with HbA1c levels and diabetes duration (P< 0.05). Moreover, renal functional parameters were positively correlated with HbA1c levels and diabetes duration (P<0.05). Additionally, pulmonary functional parameters were negatively correlated with renal functional parameters (P<0.05). Multiple linear regression analysis of the relationship between pulmonary functional parameters and the bilateral kidney arterial resistivity index (RI) showed that all the pulmonary functional parameters were significantly correlated with the arterial RI (P< 0.05). CONCLUSIONS: Patients displayed changes in pulmonary function and intrarenal haemodynamics during the preclinical stages of DKD. Regulating glycaemia may improve intrarenal haemodynamics in the bilateral interlobular renal arteries. Moreover, during the preclinical stages of DKD, the right kidney RI is a effective predictor of early changes in pulmonary function in adult T2DM patients. TRIAL REGISTRATION: ClinicalTrials.gov (NCT02798198); registered 8 June 2016.

Longitudinal follow-up study of the retrobulbar and intrarenal hemodynamics in patients with T2DM.

OBJECTIVE: The primary aim of this study is to examine the hemodynamics of retrobulbar and intrarenal in the changes of early stage of type 2 diabetes mellitus (T2DM) patients from 2000 to 2015 and to assess incidence associated with diabetic kidney disease (DKD) and diabetic retinopathy (DR). METHOD: Our study contained 60 subjects newly diagnosed of T2DM were divided into 2 groups base on the mean resistive index (RI) (≤0.7 and >0.7) of hemodynamic and to compare between-group differences of the early changes in hemodynamics of retrobulbar and intrarenal and also to conclude the incidences of diabetic kidney disease (DKD) and diabetic retinopathy (DR)subsequently with a long follow-up duration(2000-2015). First, to compare the mean RI of central retinal artery (CRA) between 2 groups. Second, to compare the mean RI of intrarenal hemodynamics in the bilateral interlobular renal arteries, renal function parameters (blood urea nitrogen (BUN), creatinine (Cr), blood glucose parameters (glycosylated hemoglobinA1c (HbA1c), fasting plasma glucose (FBG), and 2-hour postprandial blood glucose (2hPBG)), glomerular filtration rate (GFR), albumin excretion rate (AER), and urine albumin-to-creatinine ratio (UACR) between 2 groups. RESULTS: First part of our follow-up studies was to compare hemodynamic RI index of retrobulbar in years of 2000 and 2015, both renal function and blood glucose parameters were fund significantly enhanced in subject group RIs ≤0.7. Incidence of DKD and DR was notably lower in group RIs ≤0.7 than group RIs > 0.7, difference was statistically significant (P < .05). Incidence of HbA1c ≤7% was higher in group RIs ≤0.7 than group RIs >0.7, but difference was not statistically significant (P > .05). Incidence of proliferative diabetic retinopathy (PDR) was notably lower in group RIs ≤0.7 than group RIs >0.7, but the difference was not statistically significant (P > .05). Second part of our follow-up studies was to compare hemodynamic RI index of interlobular renal in years of 2000 and 2015, both renal function and blood glucose parameters were fund significantly enhanced in subject group RIs ≤0.7. Compared data of various incidences from first part of study were coherent with second part. (Incidence of DKD and DR was notably lower in group RIs ≤0.7 than group RIs >0.7, difference was statistically significant (P < .05). Incidence of HbA1c ≤7% was higher in group RIs ≤0.7 than group RIs >0.7, but difference was not statistically significant (P > .05). Incidence of PDR was notably lower in group RIs ≤0.7 than group RIs >0.7, but the difference was not statistically significant (P > .05). CONCLUSIONS: RIs of retrobulbar and interlobular renal which would serve as a good predictors for the hemodynamics changes in retrobulbar and intrarenal would assess incidence of DKD and DR during the preclinical stage in long-term range excluding renal function and HbA1c in T2DM patients.

[Study on the Optimization Models of Nitrogen,Phosphorus and Potassium Application of Atractylodes japonica].

Objective: To optimize the nitrogen, phosphorus and potassium fertilization models of Atractylodes japonica to offer a scientific basis for its standard cultivation and the specialty fertilizers. Methods: Annual and biennial Atractylodes japonica were chosen in the experiment. By using three-factors, quadratic saturation-D optimal design, the effects of nitrogen, phosphorus and potassium on height, rhizome traits and active constituents of Atractylodes japonica were studied. Results: Considering the production and active constituents,the optimum plan of nitrogen, phosphorus and potassium fertilization model was selected as N0P2K2（ N 0 g/m2,P2O540. 227 g / m2,K2O 40. 227 g / m2） and N1P3K3（ N15. 939 g/m2,P2O567. 467 g / m2,K2O 67. 467 g / m2）. By means of regression equation with nitrogen, phosphorus and potassium ratio and production（ rhizome fresh weight） of Atractylodes japonica, potassium was the major factor in nitrogen, phosphorus and potassium single effect, and nitrogen came second. According to the regression model, the best combination of nitrogen, phosphorus and potassium was obtained. The highest fresh weight of Atractylodes japonica rhizome was 27. 4066 g when the fertilization level of nitrogen, phosphorus and potassium were 38. 4301 kg / hm2,181. 4750 kg/hm2,128. 5584 kg/hm2,respectively. The target fresh weight of Atractylodes japonica was selected as 26. 00 27. 41 g per plant according to the model optimization results, and the target production was 1 040. 0 1 096. 4 kg / hm2. In 95% confidence interval, the best fertilizer combinations were X1=-0. 2912± 0. 0825,X2= 0. 2764 ± 0. 1054 and X3= 0. 1325 ± 0. 0645. Conclusion: According to the yield and active constituents of Atractylodes japonica, which suggest that the fertilizing amount of Atractylodes japonica artificial planting is nitrogen 46. 951 59. 320 kg / hm2,phosphorus 131. 673 155. 377 kg / hm2 and potassium 120. 091 134. 597 kg / hm2.

[Effect of obesity intervention with socio-ecological model on anthropometric measurements of children and adolescents].

OBJECTIVE: To study whether the socio-ecological model based on "student-school-family" three-level strategy is effective in obesity prevention. METHODS: A total of 3 175 students aged 7 to 18 from 16 schools (4 urban primary schools, 4 rural primary schools, 4 urban secondary schools and 4 rural secondary schools, of which 2 intervention schools were selected, respectively) were recruited by stratified cluster sampling method. A three-month intervention using "student-school-family" socio-ecological model was conducted through health education and environment improvement. The intervention contents included knowledge on obesity, healthy diet and physical activities. Their anthropometric indexes were recorded. RESULTS: The intervention prevented obesity (OR=1.12, P<0.05), and was effective in waist circumference (WC) and waist-hip ratio (WHR) (adjusted difference=0.63, 0.02, P<0.05). WC and WHR were reduced in girls (adjusted difference=0.52 & 0.02, P<0.05), and obesity was prevented in girls (OR=1.18, P<0.05). WC and WHR were reduced in boys (adjusted difference=0.73, 0.01, P<0.05). WHR were reduced in urban areas (adjusted difference=0.01, P<0.05). WC and WHR were reduced (adjusted difference=1.05, 0.02, P<0.05) and obesity was prevented (OR=1.18, P<0.05) in rural areas. WHR were reduced (adjusted difference=0.01, P<0.05) and obesity was prevented (OR=1.21, P<0.05) in primary schools. WHR were reduced in secondary schools (adjusted difference=0.02, P<0.05).The intervention effect was better in girls than in boys, in rural areas than in urban areas, and in primary schools than in secondary schools. The overweight and obesity prevalence went down after the intervention (χ2=11.01, P<0.01). CONCLUSION: Intervention strategy is effective in central obesity indexes such as WC and WHR, and it can be used widely.