Synthesis of Diverse -Trifluoromethyl Pyrazoles by Trapping of Transiently-Generated Trifluoromethylhydrazine.

A one-pot synthesis of functionalized -trifluoromethyl pyrazoles from readily available di-Boc trifluoromethylhydrazine and dialdehydes, diketones, carbonylnitriles, and ketoesters/amides/acids is described. F NMR studies were used to characterize the stability of trifluoromethylhydrazine HCl salt in solution and in solid form and identified a short solution-state half-life of ∼6 h. Optimization of cyclization conditions identified DCM, combined with a strong acid, as a key to suppress the undesired des-CF side products, which formed as a result of the instability of trifluoromethylhydrazine and related intermediates.

Causal relationships involving brain imaging-derived phenotypes based on UKB imaging cohort: a review of Mendelian randomization studies.

The UK Biobank (UKB) has the largest adult brain imaging dataset, which encompasses over 40,000 participants. A significant number of Mendelian randomization (MR) studies based on UKB neuroimaging data have been published to validate potential causal relationships identified in observational studies. Relevant articles published before December 2023 were identified following the PRISMA protocol.

[Retracted] Paclitaxel inhibits breast cancer metastasis via suppression of Aurora kinase‑mediated cofilin‑1 activity.

[This retracts the article DOI: 10.3892/etm.2017.

Bidirectional two-sample Mendelian randomization analyses support causal relationships between structural and diffusion imaging-derived phenotypes and the risk of major neurodegenerative diseases.

Previous observational investigations suggest that structural and diffusion imaging-derived phenotypes (IDPs) are associated with major neurodegenerative diseases; however, whether these associations are causal remains largely uncertain. Herein we conducted bidirectional two-sample Mendelian randomization analyses to infer the causal relationships between structural and diffusion IDPs and major neurodegenerative diseases using common genetic variants-single nucleotide polymorphism (SNPs) as instrumental variables. Summary statistics of genome-wide association study (GWAS) for structural and diffusion IDPs were obtained from 33,224 individuals in the UK Biobank cohort.

Mechanism and effectiveness of enzymatically induced phosphate precipitation (EIPP) in stabilizing coexisting lead, zinc, and cadmium in tailings.

Lead-zinc (Pb-Zn) tailings ponds carry the risk of multiple heavy metals (HMs) contamination and pile destabilization. This poses requirements for in-situ applicable, low-distribution, and effective stabilization/solidification (S/S) methods. For this, the novel enzymatically induced phosphate precipitation (EIPP) method was implemented in this study.

Genetic labeling reveals spatial and cellular expression pattern of neuregulin 1 in mouse brain.

Background: Where the gene is expressed determines the function of the gene. Neuregulin 1 (Nrg1) encodes a tropic factor and is genetically linked with several neuropsychiatry diseases such as schizophrenia, bipolar disorder and depression. Nrg1 has broad functions ranging from regulating neurodevelopment to neurotransmission in the nervous system.

Comparison of Diagnostic Value for Chronic Kidney Disease between 640-Slice Computed Tomography Kidney Scan and Conventional Computed Tomography Scan.

Objective: To explore the diagnostic value for chronic kidney disease (CKD) between 640-slice computed tomography (CT) kidney scan and conventional CT scan.

Methods: A total of 120 CKD patients who received kidney plain scan plus enhanced examination in the CT room of the Medical Imaging Department of our hospital from June 2019 to September 2019 were selected and randomly divided into the experimental group ( = 60) and the control group ( = 60). Patients in the control group received the conventional CT plain scan and enhanced scan, and for patients in the experimental group, CT plain scan was performed first, the range of 640-slice CT dynamic volume scan was determined, and after bolus injection of contrast agent, dynamic volume scan was performed for scanning in the cortical phase, myeloid phase, and secretory phase.

Dehydration effect of freeze-thaw on sludge: Temperature spatio-temporal distribution and multi-scale evaluation.

The freeze-thaw vacuum method for conditioning pretreated sludge has been proved that it not only has greater dewatering efficiency but also is more ecologically friendly. In this paper, the experiment is improved to address shortcomings in previous freeze-thaw vacuum approach for sludge treatment. The spatio-temporal distribution relationship of distance-time-temperature is developed and divided into two stages by numerically fitting the temperature change of freezing tubes in the sludge.

Comparison of the Application Value for Diagnosis of Chronic Kidney Disease between Color Doppler Flow Quantification Technique and Computed Tomography.

Objective: The aim of this study is to compare the application value for diagnosis of chronic kidney disease (CKD) between the color Doppler flow quantification (CDFQ) technique and computed tomography (CT).

Methods: The clinical data of 88 hospitalized patients treated in the Renal Medicine of our hospital and diagnosed with CKD after pathological examination from June 2020 to June 2021 were selected for the retrospective analysis, and 32 individuals with normal physical examination results in the same period were selected as the control group. All study subjects received CDFQ and 640-slice volume CT examination, and by plotting the ROC curves, the clinical value of different diagnostic modalities was analyzed.

Dynamic Functional Connectivity Alterations and Their Associated Gene Expression Pattern in Autism Spectrum Disorders.

Autism spectrum disorders (ASDs) are a group of heterogeneous neurodevelopmental disorders that are highly heritable and are associated with impaired dynamic functional connectivity (DFC). However, the molecular mechanisms behind DFC alterations remain largely unknown. Eighty-eight patients with ASDs and 87 demographically matched typical controls (TCs) from the Autism Brain Imaging Data Exchange II database were included in this study.

Insights into vacuum preloading consolidation of landfill sludge based on Fe-activated sodium persulfate.

To further reduce the in-situ sludge from landfill, Fe-activated sodium persulfate combined with vacuum preloading was first proposed. Firstly, the effects of optimal NaSO dosage on the landfill sludge (LS) were investigated by the vacuum filtration experiments. Then, vacuum preloading experiments were conducted on the sludge with different NaSO dosages to study the water content, water discharge, and settlement.

Freeze-thaw vacuum treatment of landfill sludge: Mechanism of uneven frost heaving and dewatering performance.

The method of freeze-thaw combined with vacuum pretreatment for landfill sludge (LS) has attracted extensive attention. However, most of the existing approaches are based on small-scale laboratory testing, and further testing studies must be performed to realize in situ treatment. To enhance the practicality of such approaches, the range of temperature effects on LS was analysed after field freeze-thaw model testing.

Co-treatment with miR-21-5p inhibitor and Aurora kinase inhibitor reversine suppresses breast cancer progression by targeting sprouty RTK signaling antagonist 2.

Numerous studies have reported the regulatory effects of miR-21-5p and reversine in human breast cancer (HBC). However, the mechanism of reversine and miR-21-5p has not been fully investigated in HBC. The aim of the current study was to assess the mechanism of action of reversine, with or without miR-21-5p, in HBC progression.

Overexpression of neuregulin 1 in GABAergic interneurons results in reversible cortical disinhibition.

Cortical disinhibition is a common feature of several neuropsychiatric diseases such as schizophrenia, autism and intellectual disabilities. However, the underlying mechanisms are not fully understood. To mimic increased expression of Nrg1, a schizophrenia susceptibility gene in GABAergic interneurons from patients with schizophrenia, we generated gtoNrg1 mice with overexpression of Nrg1 in GABAergic interneurons.

An urchin-like helical polypeptide-asparaginase conjugate with mitigated immunogenicity.

The use of asparaginase (ASNase), a first line drug for lymphoma treatment, is impaired by short circulation and notoriously high immunogenicity. Although PEGylation can prolong the circulating half-life of ASNase, however, it also induces anti-PEG antibodies that lead to accelerated blood clearance (ABC) and hypersensitivity reactions. Here, we create an urchin-like polypeptide-ASNase conjugate P(CB-EGGlu)-ASNase, in which the surface of ASNase is sufficiently shielded by an array of zwitterionic helical polypeptides through the labeling of the ε-amine of lysine.

Early Intervention of Gastrodin Improved Motor Learning in Diabetic Rats Through Ameliorating Vascular Dysfunction.

The mechanism of cognitive dysfunction in diabetes is still unclear. Recently, studies have shown that the cerebellum is involved in cognition. Furthermore, diabetes-induced cerebellar alterations is related to vascular changes.

Evaluation of the Chinese version of the swallowing screen in stroke patients with dysphagia.

Objective: The purpose of this study was to validate a Chinese version of the modified Standardized Swallowing Assessment (SSA) instrument used by nurses in stroke patients with dysphagia and explore the feasibility of the simplified instrument.

Materials And Methods: This study involved a cross-sectional design. Nurses independently applied the modified SSA to 127 patients with stroke before a complete dysphagia evaluation conducted by a speech-language pathologist.

Gastrodin Ameliorates Motor Learning Deficits Through Preserving Cerebellar Long-Term Depression Pathways in Diabetic Rats.

Cognitive dysfunction is a very severe consequence of diabetes, but the underlying causes are still unclear. Recently, the cerebellum was reported to play an important role in learning and memory. Since long-term depression (LTD) is a primary cellular mechanism for cerebellar motor learning, we aimed to explore the role of cerebellar LTD pathways in diabetic rats and the therapeutic effect of gastrodin.

A S-Sn Lewis Pair-Mediated Ring-Opening Polymerization of α-Amino Acid -Carboxyanhydrides: Fast Kinetics, High Molecular Weight, and Facile Bioconjugation.

The rapid and controlled generation of polypeptides with ultrahigh molecular weight (MW) and well-defined chain end functionality has been a great challenge. To tackle this problem, we report here an initiation system based on a S-Sn Lewis pair, trimethylstannyl phenyl sulfide (PhS-SnMe), for the ring-opening polymerization (ROP) of α-amino acid -carboxyanhydrides (NCAs). This initiator displays a strong solvent effect, and can yield polypeptides with high MW (>1.

Paclitaxel inhibits breast cancer metastasis via suppression of Aurora kinase-mediated cofilin-1 activity.

The main problem in breast cancer treatment is the recurrence of tumor growth and metastases. Previous studies have suggested that Paclitaxel is widely used to treat various cancers. The present study analyzed the potential signaling pathway of Paclitaxel-inhibited breast cancer metastasis.

Targeted delivery of a guanidine-pendant Pt(iv)-backboned poly-prodrug by an anisamide-functionalized polypeptide.

We describe here a novel targeting polyion complex (Tg-PIC) system for the delivery and intracellular release of cisplatin. Briefly, a guanidinium-pendant Pt(iv)-backboned poly-prodrug termed P(DSP-Gu) is prepared with excellent aqueous solubility, high drug-loading and high potency. To enable prolonged circulation and selective cellular internalization, P(DSP-Gu) is complexed with anisamide-end-capped poly(ethylene glycol)-block-poly(l-phosphotyrosine)-block-poly(l-leucine) (AA-PEG-PpY-PLeu) to yield Tg-PIC via electrostatic coacervation.

Harnessing Phosphato-Platinum Bonding Induced Supramolecular Assembly for Systemic Cisplatin Delivery.

To improve the therapeutic index of cisplatin (CDDP), we present here a new paradigm of drug-induced self-assembly by harnessing phosphato-platinum complexation. Specifically, we show that a phosphato-platinum cross-linked micelle (PpY/Pt) can be generated by using a block copolymer methoxy-poly(ethylene glycol)-block-poly(l-phosphotyrosine) (mPEG-b-PpY). Coating of PpY/Pt with a R-iRGD peptide by simple mixing affords a targeting micelle with near neutral-charged surface (iPpY/Pt).

Cloning and Characterisation of Two H+ Translocating Organic Pyrophos-phatase Genes in Salix and Their Expression Differences in Two Willow Varieties with Different Salt Tolerances.

Willows are one of the most important tree species for landscaping, biofuel and raw timber. Screening salt-tolerant willow varieties is an effective approach to balance wood supply and demand. However, more salt-tolerant willow varieties are required and little is known regarding the mechanism of salt tolerance at the gene expression level.

[Clinical evaluation of one-stage radical debridement combined with posterior pedicle internal fixation for brucellar spondylitis of the thoracic and lumbar vertebrae].

Objective: To discuss the surgical treatment method and effectiveness of brucellar spondylitis.

Methods: Between January 2002 and October 2010, 78 patients underwent one-stage radical debridement and posterior pedicle internal fixation, who were definitely diagnosed as having brucellar spondylitis of the thoracic and lumbar vertebrae. There were 42 males and 36 females, aged 24 to 65 years (mean, 45 years).