Discovery and development of thiazolidine-2,4-dione derivatives as Bcl-2/Mcl-1 dual inhibitors.

Increasing the levels of antiapoptotic Bcl-2 proteins is an important way that cancer cells utilize to get out of apoptosis, underscoring their significance as promising targets for anticancer therapies. Lately, a primary compound 1 bearing thiazolidine-2,4-dione was discovered to exhibit comparable Mcl-1 inhibitory activity in comparison to WL-276. Herein, thirty-nine thiazolidine-2,4-dione analogs were yielded through incorporating different biphenyl moieties (R), amino acid side chains (R) and sulfonamides (R) on 1.

Prevention of supercritical carbon dioxide fluid extract from Linnén on cutaneous squamous cell carcinomas progression following UV irradiation in mice.

Linnén (), a medicinal and food herb with various bioactive components, may be of beneficial use in cosmetics and the treatment of skin-related diseases. However, to date, few studies have been reported on its potential preventive and therapeutic effects on skin cancer. Therefore, the present study aimed to investigate the effect and potential mechanism of action of supercritical carbon dioxide extract from (CI) on UV-induced skin cancer in a mouse model.

Recent Advances in Photoswitchable Fluorescent and Colorimetric Probes.

In recent years, significant advancements have been made in the research of photoswitchable probes. These probes undergo reversible structural and electronic changes upon light exposure, thus exhibiting vast potential in molecular detection, biological imaging, material science, and information storage. Through precisely engineered molecular structures, the photoswitchable probes can toggle between "on" and "off" states at specific wavelengths, enabling highly sensitive and selective detection of targeted analytes.

Surface property and toxicity effect of insoluble particles given by protein corona: Implication for PM cytotoxicity assessment.

toxicological assessment helps explore key fractions of particulate matter (PM) in association with the toxic mechanism. Previous studies mainly discussed the toxicity effects of the water-soluble and organic-soluble fractions of PM. However, the toxicity of insoluble fractions is relatively poorly understood, and the adsorption of proteins is rarely considered.

Mechanical Behavior of Closed-Cell Ethylene-Vinyl Acetate Foam under Compression.

The static and dynamic compressions of closed-cell ethylene-vinyl acetate (EVA) foams with different densities were conducted under various strain rates. The stress-strain curves were processed to determine the corresponding curves of energy absorption per unit volume and energy absorption efficiency, and energy absorption diagrams were produced. The influences of density and strain rate on the elastic modulus, yield strength, energy absorption per unit volume, optimal strain, densification strain, and energy absorption diagrams were analyzed and discussed.

Reconnoitering correlation between human papillomavirus infection-induced vaginal microecological abnormality and squamous intraepithelial lesion (SIL) progression.

Objective: This study aims to investigate the relationship between abnormal vaginal microecology and human papillomavirus (HPV) infection, as well as the squamous intraepithelial lesions (SIL) progression.

Methods: A total of 383 patients diagnosed with HPV infection in our hospital between March 2017 and February 2022 were selected as the experimental group. In addition, several volunteers (n = 898) who underwent physical examination during the same period were randomly selected as the control group.

Heterologous Production in the Chassis Suggests the Biosynthetic Pathway of Astaxanthin in Cyanobacteria.

Astaxanthin is a carotenoid species with the highest antioxidant capability. Its natural resource is very rare. The biosynthesis of astaxanthin from β-carotene includes a hydroxylation step and a ketolation step, for which the corresponding enzymes have been characterized in a few species.

Azaindole derivatives as potential kinase inhibitors and their SARs elucidation.

Currently, heterocycles have occupied an important position in the fields of drug design. Among them, azaindole moiety is regarded as one privileged scaffold to develop therapeutic agents. Since two nitrogen atoms of azaindole increase the possibility to form hydrogen bonds in the adenosine triphosphate (ATP)-binding site, azaindole derivatives are important sources of kinase inhibitors.

Admission Heart Rate and Mortality in Critically Ill Patients with Acute Aortic Dissection.

The association between admission heart rate (HR) and the mortality of critically ill patients with acute aortic dissection (AAD) remains unclear.The data were extracted from the Medical Information Mart for Intensive Care (MIMIC-III) database. Cox regression models and Kaplan-Meier (KM) survival curve were used to explore the association between admission HR and 90-day, 1-year, and 3-year mortality in patients with AAD.

Degradation of deoxynivalenol in wheat by double dielectric barrier discharge cold plasma: identification and pathway of degradation products.

Background: Deoxynivalenol (DON) produced during the onset of fusarium head blight not only affects the quality and safety of wheat but also causes serious harm to human and livestock health. However, due to the high stability of DON, it is difficult to eliminate it or reduce it naturally after it has been produced. Cold plasma technology is a non-thermophysical processing technology that has been widely used for microbial inactivation and mycotoxin degradation.

Degradation of carbendazim in aqueous solution by dielectric barrier discharge cold plasma: Identification and toxicity of degradation products.

Dielectric barrier discharge (DBD) cold plasma, as a new nonthermal technology, has attracted increasing attention in pesticide degradation. In this study, DBD plasma was used to degrade carbendazim (MBC) in aqueous solution. Under the optimal conditions (160 kv, 50 Hz), MBC solution (0.

Benzoxazine: A Privileged Scaffold in Medicinal Chemistry.

Background: Benzoxazine is one of the most important privileged scaffolds in medicinal chemistry. Compounds bearing benzoxazine moiety usually have a variety of biological activities, such as anti-inflammatory, anti-microbial, anti-tuberculosis, anti- oxidant and anti-cancer activities. The fascinating bioactivity profile of benzoxazine scaffold in various fields has prompted medicinal chemists to design and discover novel benzoxazine derivatives as potential therapeutic candidates with the desired biological properties.

A Linear Piezoelectric Actuator Using "A-Shaped" Structure.

A new design of linear piezoelectric actuator using "A-shaped" structure was proposed, designed, fabricated, and tested. By fusion design of the piezoelectric transducer and the mechanical structure, the proposed actuator only uses the first bending vibration of the center piezoelectric transducer to work. Frequency degeneration is no longer needed, which enables the actuator to adjust its structural parameters according to the application conditions.

Protocol update for late endothelial progenitor cells identified by double-positive staining.

Endothelial progenitor cells (EPCs), which are precursors of endothelial cells (ECs), have the capacity to circulate, proliferate and differentiate into mature ECs. EPCs are primarily identified by the uptake of 1,1-dioctadecyl-3,3,3,3-tetramethylindocarbocyanine-labelled acetylated low-density lipoprotein (Dil-acLDL) and the binding of fluorescein-isothiocyanate (FITC)-conjugated Ulex europaeus agglutinin lectin (FITC-UEA-I). However, the cytoplasm and nucleus are usually stained by FITC-UEA-I via a typical method to double-stain late EPCs.

Sulfonamide derivatives as potential anti-cancer agents and their SARs elucidation.

Currently, the arise of drug resistance and undesirable off-target effects of anti-cancer agents are major challenges for cancer treatment, which energizes medicinal chemists to develop more anti-cancer agents with high efficiency and low toxicity continuously. Sulfonamide derivatives are a class of promising compounds with diverse biological activities including anti-cancer, and parts of them have been marketed for cancer therapy, such as Belinostat, ABT-199 and Amsacrine. In this review, we summed up the recent advances of sulfonamide derivatives as potential anti-cancer agents based on the anti-cancer targets, such as aromatase, carbonic anhydrase (CA), anti-apoptotic B-cell lymphoma-2 (Bcl-2) proteins, topoisomerase and phosphatidylinositol 3-kinase (PI3K), and elucidated the corresponding structure-activity relationships (SARs) of most sulfonamide derivatives.

Polysaccharides from Ganoderma Sinense - rice bran fermentation products and their anti-tumor activities on non-small-cell lung cancer.

Background: Non-small-cell lung cancer (NSCLC) accounts more than 80% of the lung cancer cases. Polysaccharides in rice bran and its fermentation products have been proven to suppress many cancers. However, the report on inhibiting NSCLC is few.

A theoretical model of the intermittent contact of piezoelectric actuator based on Greenwood-Williamson theory.

A theoretical model of the intermittent contact mechanism of linear piezoelectric actuator was proposed, in which the microscopic characteristics of the contact surfaces were taken into account. Greenwood-Williamson (GM) theory was involved for the first time to describe the microscopic characteristics of the contact surfaces in which the contact surfaces were considered as random rough surfaces that were composed of large amounts of asperities and the heights of the asperities conformed to a Gauss distribution. The developed theoretical model gives an insight into the influence of the microscopic properties, as well as the macroscopic and material properties on the output performance of the actuator, which may provide guidance for the design of such type of piezoelectric actuator.

Effect of ABO Blood Groups on the Response to Warfarin.

Background: Numerous studies have demonstrated that patients with non-O blood groups have a higher risk for venous thromboembolism than those with the O blood group. However, the effect of ABO blood groups on warfarin dose requirements in patients receiving anticoagulation in the Chinese Han population remains unknown. This study aimed to investigate the influence of ABO blood groups on warfarin dose requirements in a Chinese Han population.

A SNP of bacterial blc disturbs gut lysophospholipid homeostasis and induces inflammation through epithelial barrier disruption.

Background: Alteration of commensal bacterial composition is associated with many inflammatory diseases. However, few studies have pinpointed the specific bacterial genes that may suppress host immune responses against microbes and maintain homeostasis in the host intestine.

Methods: High-throughput screening was performed in Caenorhabditis elegans with a single gene knockout ut screening was performed in Caenorhabditis elegans with a single gene knockout Escherichia coli (E.

A Bifunctional Luminescent Metal-Organic Framework for the Sensing of Paraquat and Fe Ions in Water.

The hydrothermal reaction of Zn ions with a mixture of two ligands, Hcptpy and H btc (Hcptpy=4-(4-carboxyphenyl)-2,2':4',4''-terpyridine; H btc=1,3,5-benzenetricarboxylic acid), led to the formation of a 3D metal-organic framework (MOF) with 1D channels, [Zn (cptpy)(btc)(H O)] (1), which was structurally characterized by using single-crystal X-ray diffraction (SXRD). In MOF 1, two independent Zn ions were interconnected by btc ligands to form a 1D chain, whilst adjacent Zn ions were alternately bridged by cptpy ligands to generate a 2D sheet, which was further linked by 1D chains to form a 3D framework with a new (3,3,4,4)-connected topology. Furthermore, compound 1 also exhibited excellent stability towards air and water and, more importantly, luminescence experiments indicated that it could serve as a probe for the sensitive detection of paraquat (PAQ) and Fe ions in aqueous solution.

Inhibition of Quorum Sensing and Virulence in Serratia marcescens by Hordenine.

Serratia marcescens NJ01 is a pathogenic bacterium isolated from diseased tomato leaves. Here, we report on the development of a tomato- S. marcescens host-pathogen system as a model to evaluate the effects of hordenine on quorum sensing (QS)-mediated pathogenicity under native conditions.

Antioxidant capacity of phenolics in Camellia nitidissima Chi flowers and their identification by HPLC Triple TOF MS/MS.

Camellia nitidissima Chi (CNC) is a valuable medicinal and edible plant in China. In this study, CNC flowers were extracted with 95% ethanol, then partitioned into dichloromethane, ethyl acetate, n-butanol, and water fractions, with the antioxidant capacity of flavonoids and other phytochemicals in CNC flowers investigated for the first time. Results showed that the ethyl acetate fraction exhibited the strongest antioxidant capacity and highest total phenolic content (TPC) compared with the other fractions.