Discovery of gefitinib-1,2,3-triazole derivatives against lung cancer via inducing apoptosis and inhibiting the colony formation.

A series of 20 novel gefitinib derivatives incorporating the 1,2,3-triazole moiety were designed and synthesized. The synthesized compounds were evaluated for their potential anticancer activity against EGFR wild-type human non-small cell lung cancer cells (NCI-H1299, A549) and human lung adenocarcinoma cells (NCI-H1437) as non-small cell lung cancer. In comparison to gefitinib, Initial biological assessments revealed that several compounds exhibited potent anti-proliferative activity against these cancer cell lines. Notably, compounds 7a and 7j demonstrated the most pronounced effects, with an IC50 value of 3.94 ± 0.17 µmol L-1 (NCI-H1299), 3.16 ± 0.11 µmol L-1 (A549), and 1.83 ± 0.13 µmol L-1 (NCI-H1437) for 7a, and an IC50 value of 3.84 ± 0.22 µmol L-1 (NCI-H1299), 3.86 ± 0.38 µmol L-1 (A549), and 1.69 ± 0.25 µmol L-1 (NCI-H1437) for 7j. These two compounds could inhibit the colony formation and migration ability of H1299 cells, and induce apoptosis in H1299 cells. Acute toxicity experiments on mice demonstrated that compound 7a exhibited low toxicity in mice. Based on these results, it is proposed that 7a and 7j could potentially be developed as novel drugs for the treatment of lung cancer.

A review of novel research technology to explore the mystery of traditional Chinese medicine: Terahertz.

During the 2022 Annual National Terahertz Biophysics Conference, the hypothesis was proposed that bio frequency electromagnetic fields sensitive points, akin to acupuncture points, exist in the human body. This development has prompted numerous researchers to apply terahertz technology to the field of traditional Chinese medicine (TCM). In recent years, terahertz technology has achieved notable progress in the field of TCM, particularly concerning the meridian-collateral system. This review systematically presents the advancements in terahertz technology and its implications on TCM theory from a biophysical perspective. Additionally, it summarizes the utilization of terahertz waves in elucidating aspects of TCM, particularly focusing on the scientific connotation of Qi, the theoretical foundation of the meridian-collateral system, and moxibustion in diagnosing and treating diseases. We aimed to explore the innovative applications and distinct advantages of terahertz technology in TCM and its feasibility as a pioneering technological tool for the modernization of TCM.

Establishment of a predictive equation for pulmonary ventilation function in school-aged children in northeast China: a prospective study. / ä¸œåŒ—åœ°åŒºå­¦é¾„æœŸå„¿ç«¥è‚ºé€šæ°”åŠŸèƒ½é¢„è®¡æ–¹ç¨‹å¼å»ºç«‹çš„å‰çž»æ€§ç ”ç©¶.

OBJECTIVES: To establish a predictive equation for commonly used pulmonary ventilation function parameters in children aged 6-<16 years in northeast China. METHODS: A total of 504 healthy children from Liaoning, Jilin, and Heilongjiang provinces of China were selected for the prospective study, among whom there were 242 boys and 262 girls. The JAEGER MasterScreen Pneumo spirometer was used to measure pulmonary ventilation function. With the measured values of 10 parameters, including forced vital capacity (FVC), forced expiratory volume in 1 second (FEV1), FEV1/FVC ratio, and back-extrapolated volume (BEV), as dependent variables and age, body height, and body weight as independent variables, the stepwise multivariate regression method was used to establish the regression equation for children of different sexes. The mean of relative prediction error was used to evaluate the applicability of the predictive equation. RESULTS: The boys aged 9-<10 years and 15-<16 years had significantly higher body height, FVC, and FEV1 than the girls of the same age (P<0.05), and the boys aged 9-<10, 10-<11, 11-<12, and 13-<14 years had a significantly lower FEV1/FVC ratio than the girls of the same age (P<0.05). The correlation analysis showed that all parameters, except FEV1/FVC ratio and BEV/FVC ratio, were significantly positively correlated with age, body height, and body weight (P<0.001). Further regression analysis showed that age and body height were the influencing factors for most parameters, while body weight was less frequently included in the regression equation. Compared with the predictive equations from previous studies, the regression equation established in this study had relatively good applicability in the study population. CONCLUSIONS: A new predictive equation for the main pulmonary ventilation function parameters has been established in this study for children aged 6-<16 years in northeast China, which provides a basis for accurate judgment of pulmonary function abnormalities in clinical practice.

Syntheses and structures of three macrocyclic supramolecular complexes and one ZnII-containing coordination polymer generated from a semi-rigid multidentate N-containing ligand.

Semirigid organic ligands can adopt different conformations to construct coordination polymers with more diverse structures when compared to those constructed from rigid ligands. A new asymmetric semirigid organic ligand, 4-{2-[(pyridin-3-yl)methyl]-2H-tetrazol-5-yl}pyridine (L), has been prepared and used to synthesize three bimetallic macrocyclic complexes and one coordination polymer, namely, bis(µ-4-{2-[(pyridin-3-yl)methyl]-2H-tetrazol-5-yl}pyridine)bis[dichloridozinc(II)] dichloromethane disolvate, [Zn2Cl4(C12H10N6)2]·2CH2Cl2, (I), the analogous chloroform monosolvate, [Zn2Cl4(C12H10N6)2]·CHCl3, (II), bis(µ-4-{2-[(pyridin-3-yl)methyl]-2H-tetrazol-5-yl}pyridine)bis[diiodidozinc(II)] dichloromethane disolvate, [Zn2I4(C12H10N6)2]·2CH2Cl2, (III), and catena-poly[[[diiodidozinc(II)]-µ-4-{2-[(pyridin-3-yl)methyl]-2H-tetrazol-5-yl}pyridine] chloroform monosolvate], {[ZnI2(C12H10N6)]·CHCl3}n, (IV), by solution reaction with ZnX2 (X = Cl and I) in a CH2Cl2/CH3OH or CHCl3/CH3OH mixed solvent system at room temperature. Complex (I) is isomorphic with complex (III) and has a bimetallic ring possessing similar coordination environments for both of the ZnII cations. Although complex (II) also contains a bimetallic ring, the two ZnII cations have different coordination environments. Under the influence of the I- anion and guest CHCl3 molecule, complex (IV) displays a significantly different structure with respect to complexes (I)-(III). C-H...Cl and C-H...N hydrogen bonds, and π-π stacking or C-Cl...π interactions exist in complexes (I)-(IV), and these weak interactions play an important role in the three-dimensional structures of (I)-(IV) in the solid state. In addition, the fluorescence properties of L and complexes (I)-(IV) were investigated.

Deep Portrait Image Completion and Extrapolation.

General image completion and extrapolation methods often fail on portrait images where parts of the human body need to be recovered -a task that requires accurate human body structure and appearance synthesis. We present a twostage deep learning framework for tackling this problem. In the first stage, given a portrait image with an incomplete human body, we extract a complete, coherent human body structure through a human parsing network, which focuses on structure recovery inside the unknown region with the help of full-body pose estimation. In the second stage, we use an image completion network to fill the unknown region, guided by the structure map recovered in the first stage. For realistic synthesis the completion network is trained with both perceptual loss and conditional adversarial loss.We further propose a face refinement network to improve the fidelity of the synthesized face region. We evaluate our method on publicly-available portrait image datasets, and show that it outperforms other state-of-the-art general image completion methods. Our method enables new portrait image editing applications such as occlusion removal and portrait extrapolation. We further show that the proposed general learning framework can be applied to other types of images, e.g. animal images.

Tissue lipid metabolism and hepatic metabolomic profiling in response to supplementation of fermented cottonseed meal in the diets of broiler chickens.

This study investigated the effects of fermented cottonseed meal (FCSM) on lipid metabolites, lipid metabolism-related gene expression in liver tissues and abdominal adipose tissues, and hepatic metabolomic profiling in broiler chickens. One hundred and eighty 21-d-old broiler chickens were randomly divided into three diet groups with six replicates of 10 birds in each group. The three diets consisted of a control diet supplemented with unfermented cottonseed meal, an experimental diet of cottonseed meal fermented by Candida tropicalis, and a second experimental diet of cottonseed meal fermented by C. tropicalis plus Saccharomyces cerevisae. The results showed that FCSM intake significantly decreased the levels of abdominal fat and hepatic triglycerides (P<0.05 for both). Dietary FCSM supplementation down-regulated the mRNA expression of fatty acid synthase and acetyl CoA carboxylase in liver tissues and the lipoprotein lipase expression in abdominal fat tissues (P<0.05 for both). FCSM intake resulted in significant metabolic changes of multiple pathways in the liver involving the tricarboxylic acid cycle, synthesis of fatty acids, and the metabolism of glycerolipid and amino acids. These findings indicated that FCSM regulated lipid metabolism by increasing or decreasing the expression of the lipid-related gene and by altering multiple endogenous metabolites. Lipid metabolism regulation is a complex process, this discovery provided new essential information about the effects of FCSM diets in broiler chickens and demonstrated the great potential of nutrimetabolomics in researching complex nutrients added to animal diets.

[Determination of1-bromopropane in the workplace air by GC-FID].

OBJECTIVE: To establish a method for determination 1-bromopropane (1-BP) in workplace air by gas chromatography-flame ionization detector (GC-FID). METHOD: 1-bromopropane in workplace air was collected with activated charcoal tube, then desorbed by carbon disulfide and determined by GC-FID. 1-bromopropane was quantitatively measured using retention time and peak area. RESULTS: Linear regression formula was Y = 3353.4x-10064 in a range of 2.50 ∼ 500.00 µg/ml with regression coefficient R = 0.9998. Detection limit was 0.25 µg/ml and the lowest detection concentration of 1-brmopropane in air was 0.14 mg/m(3) (at air volume 1.8L). The mean recoveries of 1-BP were between 96.8% and 102.6%, and relative standard deviation of inter and intra-assay was less than 10%. The average desorption efficiencies were between 93.2% and 104.4%. The samples in activated charcoal tube could be stably stored for 5 days at room temperature. CONCLUSION: The method could be feasible to determine 1-bromopropane in workplace air.