Synthesis of 2,3-Dialkyl-5-hydroxybenzofurans via a One-pot, Three-step Reaction Sequence of 2-Monosubstituted 1,3-Diketones and 1,4-Benzoquinones.

An economical one-pot, three-step reaction sequence of readily available 2-monosubstituted 1,3-diketones and 1,4-benzoquinones has been explored for the facile access of 2,3-dialkyl-5-hydroxybenzofurans. By using cheap K2CO3 and conc. HCl as the reaction promoters, the reaction occurs smoothly via sequential Michael addition, aromatization, retro-Claisen, deacylation, hemiketalization, and dehydration processes under mild conditions in a practical manner. Additionally, an interesting phenomenon was observed during the derivatization studies, where the dihydroquinoline was converted into tetrahydroquinoline and quinoline products, respectively, via a disproportionation process.

Biosimilar monoclonal antibodies in China: A patent review.

Biosimilars play an important role in reducing the burden on patients and increasing the market competition. Biosimilar monoclonal antibodies are currently one of the hotspots of research and development in China with policies support. With the continuous improvement of policies, the enthusiasm for the research and development of biosimilars has increased year by year. The policy requirements in different periods have different degrees of impact on the patent applications of pharmaceutical companies. This review introduces the biosimilar monoclonal antibodies market status and approval process in China, analyzes the patents in this field, and helps pharmaceutical companies protect their intellectual property rights.

CAR-T Cell Therapy for Breast Cancer: From Basic Research to Clinical Application.

Breast cancer rises as the most commonly diagnosed cancer in 2020. Among women, breast cancer ranks first in both cancer incidence rate and mortality. Treatment resistance developed from the current clinical therapies limits the efficacy of therapeutic outcomes, thus new treatment approaches are urgently needed. Chimeric antigen receptor (CAR) T cell therapy is a type of immunotherapy developed from adoptive T cell transfer, which typically uses patients' own immune cells to combat cancer. CAR-T cells are armed with specific antibodies to recognize antigens in self-tumor cells thus eliciting cytotoxic effects. In recent years, CAR-T cell therapy has achieved remarkable successes in treating hematologic malignancies; however, the therapeutic effects in solid tumors are not up to expectations including breast cancer. This review aims to discuss the development of CAR-T cell therapy in breast cancer from preclinical studies to ongoing clinical trials. Specifically, we summarize tumor-associated antigens in breast cancer, ongoing clinical trials, obstacles interfering with the therapeutic effects of CAR-T cell therapy, and discuss potential strategies to improve treatment efficacy. Overall, we hope our review provides a landscape view of recent progress for CAR-T cell therapy in breast cancer and ignites interest for further research directions.

LMX1B rs10733682 Polymorphism Interacts with Macronutrients, Dietary Patterns on the Risk of Obesity in Han Chinese Girls.

Previous studies have found that LMX1B rs10733682 polymorphism is associated with Body Mass Index (BMI) in European and American Indian adults. In this study, the association of rs10733682 polymorphism with obesity-related indicators, and its interaction with macronutrients and dietary patterns (DPs) were explored in Chinese children (n = 798). The rs10733682 polymorphism was genotyped by improved Multiple Ligase Detection Reaction (iMLDR). Four DPs were identified by factor analysis. The AA genotype had a higher incidence of overweight/obesity than GG+GA genotypes (P = 0.010) in girls (n = 398), but no difference in boys. The AA genotype in girls could interact with intake of energy, fat and carbohydrate, causing an increased triglyceride (TG), (P = 0.021, 0.003, 0.002, respectively), and also could interact with energy from protein, causing an elevated BMI (P = 0.023) and waist (P = 0.019). Girls inclining to the HED (high-energy density)-DP were associated with increased TG (P = 0.033), and girls inclining to the VEF (vegetables, eggs, and fishes based)-DP were associated with decreased total cholesterol (TC, P = 0.045) and decreased low density lipoprotein cholesterin (LDL, P = 0.016). The findings indicated that the AA genotype of rs10733682 and the HED-DP are potential risk factors of obesity in Chinese girls.

Interaction of the CMTM7 rs347134 Polymorphism with Dietary Patterns and the Risk of Obesity in Han Chinese Male Children.

A genome-wide association study (GWAS) in the Han Chinese population had found that single nucleotide polymorphism (SNP) on the CMTM7 gene rs347134 was significantly associated with Body Mass Index (BMI). In the present study, the association of the rs347134 SNP with obesity and its interaction with dietary patterns (DPs) were explored in Han Chinese children. This cross-sectional study group included 1292 children, in whom obesity-related indicators were evaluated, the rs347134 SNP was genotyped by improved Multiple Ligase Detection Reaction (iMLDR), and the DPs were identified by principal component factor analysis. The GG genotype exhibited higher odds of general overweight/obesity (P = 0.038) and central obesity (P = 0.039) than AA+GA genotypes in boys. Four DPs of boys were identified: healthy balanced (HBDP), nuts and sweets-based (NSDP), animal food-based (AFDP), and wheaten and dairy-based (WDDP). Boys with the GG genotype were significantly more inclined to AFDP (P = 0.028) and had a shorter sleep duration (P = 0.031). Significant interactions were observed; boys with the GG genotype displayed a higher LDL in AFDP (P = 0.031) and higher FBG in NSDP (P = 0.038), respectively. Our findings indicate for the first time that the GG genotype of CMTM7 rs347134 is potentially a novel obesity risk factor for Han Chinese male children and is associated with dietary patterns more or less.

The exposure of temple workers to polycyclic aromatic hydrocarbons.

Five temples, each a different size, were selected for this study. Two of the temples were located in Taichung City (in central Taiwan), and three were in Tainan City (in Southern Taiwan). Aerosols smaller than 10 microm aerodynamic diameter (PM(10)) were collected by using personal collection samplers during pilgrim days (the first and fifteenth day of each lunar month) and normal days (all other days). Regression analysis showed that about 1.6 microg/m(3) of PM(10) contributed to the workers' exposure in the temples for each joss stick increase in the censer. The concentrations of total polycyclic aromatic hydrocarbons (t-PAHs) and carcinogenic PAHs (car-PAHs) on pilgrim days were higher than those on normal days. Mean concentrations of urinary 1-hydroxypyrene (1-OHP) in the pre-shift and post-shift workers of the five temples on normal days were 1.20 and 1.61 microg/g creatinine, respectively. Furthermore, the post-shift concentrations of 1-OHP in the workers of temples on pilgrim days were all higher than those of the workers of corresponding temples on normal days. Significant relationships between the urinary concentrations of 1-OHP and the exposure concentrations of pyrene, total PAHs and BaP(eq) were found in the workers of the temples. Results of linear regression showed that the increase of unit concentration (1 ng/m(3)) of pyrene led to a 0.05 microg/g creatinine increase of urinary 1-OHP, while the increase of unit concentration (1 ng/m(3)) of BaP(eq) resulted in an increase of 0.03 microg/g creatinine of urinary 1-OHP.

Particle concentration effect in adsorption/desorption of Zn(II) on anatase type nano TiO2.

Adsorption/desorption in a new Zn(II)-TiO2 adsorption system was investigated at different particle concentrations (Cp). TEM, SEM and XRD analyses revealed that the TiO2 particles were an aggregation of nano-sized (approximately 10 nm) pure anatase-type TiO2. Adsorption experiments were carried out with particle concentrations of 100, 400 and 1000 mg/L, and their adsorption isotherms were found to decline successively, showing an obvious Cp effect. Desorption experiments indicated that adsorption in this system was irreversible, and the irreversibility increased with increasing Cp. These phenomena could be explained by the MEA (metastable equilibrium adsorption) theory and the Cp effect could be modeled well with an MEA-Freundlich-type Cp effect isotherm equation. This study may help understand environmental behavior of contaminants on ultrafine natural particles.