keyword
https://read.qxmd.com/read/38838169/-bifidobacterium-bifidum-ameliorates-dss-induced-colitis-in-mice-by-regulating-microbial-metabolome-and-targeting-gut-microbiota
#1
JOURNAL ARTICLE
Mengzhen Han, Jingjing Liang, Mengxin Hou, Yuanye Liu, Hongcai Li, Zhenpeng Gao
Inflammatory bowel disease (IBD) is a recurrent inflammatory condition affecting the gastrointestinal tract, and its clinical treatment remains suboptimal. Probiotics have shown effectiveness in alleviating dextran sulfate sodium salt (DSS)-induced colitis, exhibiting strain-specific anti-inflammatory properties. In this study, we compared the therapeutic effects of five strains of Bifidobacterium bifidum isolated from healthy adult feces on DSS-induced colitis in mice. Additionally, we investigated the underlying mechanisms by examining gut microbiota composition and microbial metabolome...
June 5, 2024: Journal of Agricultural and Food Chemistry
https://read.qxmd.com/read/38837951/overcoming-secondary-mutations-of-type-ii-kinase-inhibitors
#2
REVIEW
Xiuqi Wang, Rosa Anna DeFilippis, Wei Yan, Neil P Shah, Hong-Yu Li
Type II kinase inhibitors bind in the "DFG-out" kinase conformation and are generally considered to be more potent and selective than type I inhibitors, which target a DFG-in conformation. Nine type II inhibitors are currently clinically approved, with more undergoing clinical development. Resistance-conferring secondary mutations emerged with the first series of type II inhibitors, most commonly at residues within the kinase activation loop and at the "gatekeeper" position. Recently, new inhibitors have been developed to overcome such mutations; however, mutations activating other pathways (and/or other targets) have subsequently emerged on occasion...
June 5, 2024: Journal of Medicinal Chemistry
https://read.qxmd.com/read/38837697/mining-the-dynamical-properties-of-substrate-and-fad-binding-pockets-of-lsd1-hints-for-new-inhibitor-design-direction
#3
JOURNAL ARTICLE
Kecheng Yang, Hongmin Liu
Lysine-specific demethylase 1 (LSD1), a highly sophisticated epigenetic regulator, orchestrates a range of critical cellular processes, holding promising therapeutic potential for treating diverse diseases. However, the clinical research progress targeting LSD1 is very slow. After 20 years of research, only one small-molecule drug, BEA-17, targeting the degradation of LSD1 and CoREST has been approved by the U.S. Food and Drug Administration. The primary reason for this may be the lack of abundant structural data regarding its intricate functions...
June 5, 2024: Journal of Chemical Information and Modeling
https://read.qxmd.com/read/38837604/discovery-total-synthesis-and-anti-inflammatory-evaluation-of-naturally-occurring-naphthopyrone-macrolide-hybrids-as-potent-nlrp3-inflammasome-inhibitors
#4
JOURNAL ARTICLE
Chunxiao Sun, Yuqi Jiang, Changlong Li, Simin Sun, Jiaqi Lin, Wenxue Wang, Luning Zhou, Liping Li, Mudassir Shah, Qian Che, Guojian Zhang, De Wang, Tianjiao Zhu, Dehai Li
Numerous clinical disorders have been linked to the etiology of dysregulated NLRP3 (NACHT, LRR, and PYD domain-containing protein 3) inflammasome activation. Despite its potential as a pharmacological target, modulation of NLRP3 activity remains challenging. Only a sparse number of compounds have been reported that can modulate NLRP3 and none of them have been developed into a commercially available drug. In this research, we identified three potent NLRP3 inflammasome inhibitors, gymnoasins A-C (1-3), with unprecedented pentacyclic scaffolds, from an Antarctic fungus Pseudogymnoascus sp...
June 4, 2024: Angewandte Chemie
https://read.qxmd.com/read/38837084/atomically-co-dispersed-nitrogen-doped-carbon-for-sensitive-electrochemical-immunoassay-of-breast-cancer-biomarker-ca15-3
#5
JOURNAL ARTICLE
Lei Han, Shuanglong Cai, Xiaogeng Chen
The development of an ultrasensitive and precise measurement of a breast cancer biomarker (cancer antigen 15-3; CA15-3) in complex human serum is essential for the early diagnosis of cancer in groups of healthy populations and the treatment of patients. However, currently available testing technologies suffer from insufficient sensitivity toward CA15-3, which severely limits early large-scale screening of breast cancer patients. We report a versatile electrochemical immunoassay method based on atomically cobalt-dispersed nitrogen-doped carbon (Co-NC)-modified disposable screen-printed carbon electrode (SPCE) with alkaline phosphatase (ALP) and its metabolite, ascorbic acid 2-phosphate (AAP), as the electrochemical labeling and redox signaling unit for sensitive detection of low-abundance CA15-3...
June 5, 2024: Mikrochimica Acta
https://read.qxmd.com/read/38837077/-177-lu-sn201-nanoparticle-shows-superior-anti-tumor-efficacy-over-conventional-cancer-drugs-in-4t1-orthotopic-model
#6
JOURNAL ARTICLE
Sujinna Lekmeechai, Kristian Pietras, Oskar Axelsson
In the current in-vivo study we demonstrate the potential of the radiolabeled nanoparticle 177 Lu-SN201 as an effective anticancer treatment, as evidenced by significantly prolonged survival and reduced tumor burden in the aggressive, triple negative 4T1 murine breast cancer model. We show with high statistical significance that 177 Lu-SN201 is superior at suppressing the tumor growth not only compared to vehicle but also to the commonly used cancer drugs paclitaxel, niraparib, carboplatin, and the combination of the immune checkpoint inhibitors anti PD-1 and anti-CTLA-4...
June 5, 2024: Investigational New Drugs
https://read.qxmd.com/read/38836746/three-dyes-for-use-in-tissue-marking-inks-for-biopsies-and-other-small-specimens
#7
JOURNAL ARTICLE
Zhenkun Zhu, Quan Li, Chunxiang Xiang, Hui Xing
In histological processing, the loss of a small biopsies can prevent diagnosis by the pathologist. Appropriate specimen marking dyes are helpful, but those sold for the purpose have trade-secret components. The purpose of this study is to find suitable dyes with known chemistry to improve the visibility of small specimens. Samples of various organs, including stomach, lung, nasopharynx, small intestine and sentinel lymph nodes, were labeled with Rose red D-FR (CI 282855, Direct red 227), Blue 2RL (CI 24315, Direct blue 80), and Purple D-5BL (CI 29120, Direct violet 66)...
June 5, 2024: Biotechnic & Histochemistry: Official Publication of the Biological Stain Commission
https://read.qxmd.com/read/38836578/fluorinated-bpa-derivatives-enhanced-10-b-delivery-in-tumors
#8
JOURNAL ARTICLE
Dandan Ding, Shushan Mo, Qishan Li, Fei Wang, Xueyi Wang, Caiwen Ou, Zhenhua Li
Boron neutron capture therapy (BNCT) is an emerging approach for treating malignant tumors with binary targeting. However, its clinical application has been hampered by insufficient 10 B accumulation in tumors and low 10 B concentration ratios of tumor-to-blood (T/B) and tumor-to-normal tissue (T/N). Herein, we developed fluorinated BPA derivatives with different fluorine groups as boron delivery agents for enabling sufficient 10 B accumulation in tumors and enhancing T/B and T/N ratios. Our findings demonstrated that fluorinated BPA derivatives had good biological safety...
June 5, 2024: Journal of Materials Chemistry. B, Materials for Biology and Medicine
https://read.qxmd.com/read/38836548/microfluidic-electrochemical-integrated-sensor-for-efficient-and-sensitive-detection-of-candida-albicans
#9
JOURNAL ARTICLE
Ying-Xue Liang, Yi-Ke Wang, Wei-Jie Meng, Qian Wang, Jia-Xin Li, Wei-Hua Huang, Min Xie
Traditional methods for the detection of pathogenic bacteria are time-consuming, less efficient, and sensitive, which affects infection control and bungles illness. Therefore, developing a method to remedy these problems is very important in the clinic to diagnose the pathogenic diseases and guide the rational use of antibiotics. Here, microfluidic electrochemical integrated sensor (MEIS) has been investigated, functionally for rapid, efficient separation and sensitive detection of pathogenic bacteria. Three-dimensional macroporous PDMS and Au nanotube-based electrode are successfully assembled into the modeling microchip, playing the functions of "3D chaotic flow separator" and "electrochemical detector," respectively...
June 5, 2024: Analytical Chemistry
https://read.qxmd.com/read/38836446/recent-advances-in-organic-small-molecule-fluorescent-probes-based-on-dicyanoisophorone-derivatives
#10
REVIEW
Liqiang Yan, Liting Tang, Xiongzhi Wu, Lin Li
Fluorescent probe technology holds great promise in the fields of environmental monitoring and clinical diagnosis due to its inherent advantages, including easy operation, reliable detection signals, fast analysis speed, and in situ imaging capabilities. In recent years, a wide range of fluorescent probes based on diverse fluorophores have been developed for the analysis and detection of various analytes, yielding significant achievement. Among these fluorophores, the dicyanoisophorone-based fluorophores have garnered significant attention...
June 5, 2024: Critical Reviews in Analytical Chemistry
https://read.qxmd.com/read/38836433/outcome-based-analytical-performance-specifications-current-status-and-future-challenges
#11
JOURNAL ARTICLE
Andrea Rita Horvath, Katy J L Bell, Ferruccio Ceriotti, Graham R D Jones, Tze Ping Loh, Sally Lord, Sverre Sandberg
Analytical performance specifications (APS) based on outcomes refer to how 'good' the analytical performance of a test needs to be to do more good than harm to the patient. Analytical performance of a measurand affects its clinical performance. Without first setting clinical performance requirements, it is difficult to define how good analytically the test needs to be to meet medical needs. As testing is indirectly linked to health outcomes through clinical decisions on patient management, often simulation-based studies are used to assess the impact of analytical performance on the probability of clinical outcomes which is then translated to Model 1b APS according to the Milan consensus...
June 6, 2024: Clinical Chemistry and Laboratory Medicine: CCLM
https://read.qxmd.com/read/38835152/stereoselective-synthesis-of-%C3%AE-s-glycosides-via-palladium-catalysis
#12
JOURNAL ARTICLE
Yixuan Liu, Yuan Wang, Jie Chen, Nengzhong Wang, Nianyu Huang, Hui Yao
S -Glycosides are more resistant to enzymatic and chemical hydrolysis and exhibit higher metabolic stability than common O -glycosides, demonstrating their widespread application in biological research and drug development. In particular, β- S -glycosides are used as antirheumatic, anticancer, and antidiabetic drugs in clinical practice. However, the stereoselective synthesis of β- S -glycosides is still highly challenging. Herein, we report an effective β- S -glycosylation using 3- O -trichloroacetimidoyl glycal and thiols under mild conditions...
June 4, 2024: Journal of Organic Chemistry
https://read.qxmd.com/read/38835132/mechanism-of-guigan-longmu-decoction-in-the-treatment-of-arrhythmias-based-on-network-pharmacology-and-untargeted-metabolomics-assays
#13
JOURNAL ARTICLE
Tuo Deng, Sheng Guo, Jie Yang, Xiao-Yu Huang, Xiao-Bin Lu, Jing Lu, Liang Liu, Ze Du
BACKGROUND: Guigan longmu decoction (GGLM), a traditional Chinese medicine compound, has demonstrated efficacy in treating rapid arrhythmia clinically. Nevertheless, its mechanism of action remains elusive. This study aims to elucidate the molecular mechanism underlying the efficacy of GGLM in treating arrhythmia utilizing non-targeted metabolomics, widely-targeted metabolomics, and network pharmacology, subsequently validated through animal experiments. METHODS: Initially, network pharmacology analysis and widely-targeted metabolomics were performed on GGLM...
June 3, 2024: Combinatorial Chemistry & High Throughput Screening
https://read.qxmd.com/read/38835129/circrna_0008668-sponges-mir-1301-3p-to-promote-the-inflammatory-response-in-allergic-rhinitis-by-upregulating-gata6-expression
#14
JOURNAL ARTICLE
Xiyan Xiao, Feng Zhai, Yue Yang, Jie Chen
AIMS: We aim to explore GATA6 modulation in allergic rhinitis (AR). BACKGROUND: Circular RNAs (circRNAs) and microRNAs (miRNAs) are involved in inflammatory responses; GATA6 is also known to regulate multiple inflammatory pathways. However, the mechanism of regulation of AR between them is unclear. OBJECTIVE: We expect that this study will provide new treatment options for AR from a GATA6 perspective. METHODS: In vitro, AR models were employed to examine the efficacy of our study, where we utilized monoclonal anti-2,4,6-dinitrophenyl immunoglobulin (Ig) E/human serum albumin (DNP-IgE/HSA) to induce rat basophilic leukemia cells (RBL-2H3 cells)...
June 3, 2024: Current Medicinal Chemistry
https://read.qxmd.com/read/38834378/bioisosterism-in-drug-discovery
#15
EDITORIAL
Maria Chatzopoulou
No abstract text is available yet for this article.
May 14, 2024: Bioorganic & Medicinal Chemistry
https://read.qxmd.com/read/38834280/quantitative-analysis-of-heme-and-hemoglobin-for-the-detection-of-intravascular-hemolysis
#16
JOURNAL ARTICLE
Marie-T Hopp, Sonali M Vaidya, Karina M Grimmig, Lasse J Strudthoff, Johanna C Clauser, Xiaojing Yuan, Sneha Singh, Jens Müller, Johannes Oldenburg, Iqbal Hamza, Diana Imhof
BACKGROUND: Intravascular hemolysis is associated with massive release of hemoglobin and consequently labile heme into the blood, resulting in prothrombotic and proinflammatory events in patients. Though heme is well-known to participate in these adverse effects, it is not monitored. Instead, haptoglobin and hemoglobin serve as clinical biomarkers. The quantification of labile heme together with hemoglobin, however, should be considered in clinical diagnosis as well, to obtain a complete picture of the hemolytic state in patients...
July 11, 2024: Analytica Chimica Acta
https://read.qxmd.com/read/38834279/cds-bi-2-s-3-nis-ternary-heterostructure-based-photoelectrochemical-immunosensor-for-the-sensitive-detection-of-carbohydrate-antigen-125
#17
JOURNAL ARTICLE
Shulei Wang, Jingxia Yuan, Chunfang Wang, Tingting Wang, Faqiong Zhao, Baizhao Zeng
The sensitive, accurate and rapid detection of carbohydrate antigen 125 (CA125) is essential for the early diagnosis and clinical management of ovarian cancer, but there is still challenge. Herein, a photoelectrochemical (PEC) immunosensor based on CdS/Bi2 S3 /NiS ternary sulfide heterostructured photocatalyst was presented for the detection of CA125. The CdS/Bi2 S3 /NiS was synthesized by a one-step hydrothermal approach. The heterojunction comprising of CdS and Bi2 S3 could separate photogenerated carriers, the introduced narrow bandgap NiS could act as electron-conducting bridge to facilitate the transfer of interfacial photogenerated electrons, thereby improving the photoelectric conversion efficiency...
July 11, 2024: Analytica Chimica Acta
https://read.qxmd.com/read/38834272/aptamer-based-hybrid-monolithic-pipette-tips-supported-by-melamine-sponge-for-enrichment-of-proteins
#18
JOURNAL ARTICLE
Yue-Lun Sun, Jie Cheng, Bin-Bin Liu, Jun-Qin Qiao, Ling-Yu Zhao, Hong-Zhen Lian, Li Mao
BACKGROUND: The convenient preparation and application of functionalized organic-inorganic hybrid monolithic materials have obtained substantial interest in the pretreatment of complex samples by solid-phase extraction (SPE). Compared to the in-tube solid-phase microextraction in fused-silica capillaries, micro SPE in plastic pipette tips have fascinating merits for the easily operated enrichment of trace target analytes from biological samples. However, the poor compatibility of organic-inorganic hybrid monoliths with plastics leads to the rare appearance of commercial hybrid monolithic pipette tips (HMPTs)...
July 11, 2024: Analytica Chimica Acta
https://read.qxmd.com/read/38834264/novel-electrospun-based-extractive-probes-for-rapid-determination-of-clinically-important-compounds-in-human-plasma
#19
JOURNAL ARTICLE
Ezgi Rana Temel, Ahmet E Eroğlu, Bekir Salih, Ezel Boyaci
BACKGROUND: Coated blade spray (CBS) represents an innovative approach that utilizes solid-phase microextraction principles for sampling and sample preparation. When combined with ambient mass spectrometry (MS), it can also serve as an electrospray ionization source. Therefore, it became a promising tool in analytical applications as it can significantly reduce the analysis time. However, the current CBS coatings are based on the immobilization of extractive particles in bulk polymeric glue, which constrains the diffusion of the analytes to reach the extractive phase; therefore, the full reward of the system cannot be taken at pre-equilibrium...
July 11, 2024: Analytica Chimica Acta
https://read.qxmd.com/read/38834261/urine-multi-index-intelligent-detection-based-on-polymer-paper-hybrid-microfluidic-biochip-for-hyperuricemia-monitoring
#20
JOURNAL ARTICLE
Cuicui Wang, Qing Xue, Haiqin Li, Hao Qi, Xiaochun Li
Hyperuricemia (HUA) has gradually become a public health burden as an independent risk factor for a variety of chronic diseases. Herein, a user-friendly point-of-care (POC) detection system (namely "Smart-HUA-Monitor") based on smartphone-assisted paper-based microfluidic is proposed for colorimetric quantification of HUA urinary markers, including uric acid (UA), creatinine (CR) and pH. The detection limits of UA and CR were 0.0178 and 0.5983 mM, respectively, and the sensitivity of pH were 0.1. The method was successfully validated in artificial urine samples and 100 clinical samples...
July 11, 2024: Analytica Chimica Acta
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