Design, synthesis, anticancer activity and molecular docking of quinoline-based dihydrazone derivatives.

Based on the biologically active heterocycle quinoline, we successfully synthesized a series of quinoline-based dihydrazone derivatives (3a-3d). H NMR, C NMR, ESI-HRMS, IR, element analysis, UV/Vis spectroscopy and fluorescence spectroscopy were performed to comprehensively characterize their chemical structures, spectral properties and stability. Nitrosamine impurities were not detected in 3a-3d, and the systemic toxicological assessment indicated that the toxicity of 3a-3d was lower.

Facile Fabrication of Novel S-scheme AgPO/g-CN/Zeolite Photocatalyst for Boosting Photocatalytic Tetracycline Degradation and Hydrogen Production.

This study presents a novel ternary AgPO/g-CN/zeolite composite for photocatalytic H production and TC degradation through S-scheme electron transport. The S-scheme AgPO/g-CN heterojunction was successfully constructed on zeolite surface through calcination and precipitation processes. The results indicated that AgPO/g-CN/zeolite-50 % presented dramatically enhanced photocatalytic TC degradation performance, and the TC degradation efficiency was up to 92.

FeO@MXene@PEI aerogel immobilized acetylcholinesterase for inhibitor screening from herbal plants.

Screening of acetylcholinesterase (AChE) inhibitors is a common strategy in drug discovery for treating Alzheimer's disease. Herein, AChE was immobilized onto magnetic polyethyleneimine-based MXene aerogels through both electrostatic interactions and covalent bonds, enabling its application in AChE activity assays and inhibitor screening of herbal plants. The composite was analyzed using a range of techniques, including scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), and Zeta potential analysis, to gain insight into its chemical and physical properties.

Proteomic analysis and experimental validation reveal the blood-brain barrier protective of Huanshaodan in the treatment of SAMP8 mouse model of Alzheimer's disease.

Background: Huanshaodan (HSD) is a Chinese Herbal Compound which has a definite clinical effect on Alzheimer's disease (AD), however, the underlying mechanism remains unclear. The aim of this study is to preliminarily reveal the mechanism of HSD in the treatment of AD model of SAMP8 mice.

Methods: Chemical composition of HSD and its drug-containing serum were identified by Q-Orbitrap high resolution liquid mass spectrometry.

The role of RRS1 in breast cancer cells metastasis and AEG-1/AKT/c-Myc signaling pathway.

Breast cancer is the most common malignant tumor in women. Recurrence, metastasis, and chemotherapy resistance are the main causes of death in breast cancer patients. The inhibition of breast cancer metastasis is of great significance for prolonging its survival.

Huanshaodan regulates microglial glucose metabolism reprogramming to alleviate neuroinflammation in AD mice through mTOR/HIF-1α signaling pathway.

Abnormal glucose metabolism in microglial is closely associated with Alzheimer's disease (AD). Reprogramming of microglial glucose metabolism is centered on regulating the way in which microglial metabolize glucose to alter microglial function. Therefore, reprogramming microglial glucose metabolism is considered as a therapeutic strategy for AD.

Light-promoted stereoselective late-stage difunctionalization and anti-tumor activity of oridonin.

The late-stage difunctionalization of diterpene oridonin by light-promoted direct oxyamination with various O-benzoylhydroxylamines was carried out to afford C16α-N-C17-OBz-oridonin derivatives (1-25) for the first time. Though as a radical reaction, it features high stereoselectivity to only produce C16α-N-C17-OBz-oridonins. The in vitro antiproliferative activity of these C16α-N-C17-OBz-oridonins against the human breast cancer cell lines (MCF-7) was evaluated by MTT assay, showing that most of the synthesized compounds possessed moderate anticancer activity against MCF-7 cell lines superior or similar to the parent compound oridonin.

Selective extraction and analysis of phenolic acids in herbal plants using FeO@MXene@PEI aerogel.

A magnetic MXene aerogel (FeO@MXene@PEI) was prepared by crosslinking amino modified MXene with polyethyleneimine using epichlorohydrin as a cross-linker. Adsorption properties of FeO@MXene@PEI aerogel for phenolic acids were evaluated by adsorption kinetics and isotherms experiments, showing that the high adsorption affinity was governed by multilayer chemisorption process. An efficient MSPE/HPLC method was developed for the determination of phenolic acids with excellent selectivity, good linearity (0.

[Effect of Huanglian Jiedu Decoction on TREM2/Akt/GSK3β pathway in cerebral cortex of APP/PS1 transgenic mice].

The Chinese medical mechanism of Huanglian Jieduo Decoction on treating Alzheimer's disease(AD) characterized by "toxin damaging brain collateral" is still unclear. This study aims to explore the mechanism of Huanglian Jieduo Decoction on regulating triggering receptor expressed on myeloid cells 2(TREM2)/protein kinase B(Akt)/glycogen synthase kinase 3β(GSK3β) pathway to improve the cognitive deficit in APP/PS1 transgenic mice. APP/PS1 mice of approximately nine months old were randomly divided into the model group, the low, medium, and high(2.

Regulator of Ribosome Synthesis 1 (RRS1) Stabilizes GRP78 and Promotes Breast Cancer Progression.

Regulator of ribosome synthesis 1 (RRS1), a crucial regulatory factor in ribosome biogenesis, exerts a remarkable impact on the progression of breast cancer (BC). However, the exact mechanisms and pathways have not yet been fully elucidated. To investigate the impact of RRS1 on BC growth and metastasis, along with its underlying mechanisms.

Long noncoding RNA SNHG1 promotes breast cancer progression by regulating the miR-641/RRS1 axis.

An increasing number of studies have indicated the crucial involvement of long non-coding RNAs (lncRNAs) in the onset and progression of malignancies. However, a complete understanding of the molecular mechanism underlying the effect of abnormally expressed lncRNAs on breast cancer (BC) remains elusive. This study aimed to elucidate the influence of the lncRNA small nucleolar RNA host gene 1 (SNHG1) on BC progression and its underlying mechanism.

Novel tetranuclear grid-like Zn(II) complexes derived from dihydrazone pyrimidine derivatives as antitumor agents.

Due to the antitumor properties, Zn(II) complexes have attracted more and more attention. Herein, three novel tetranuclear Zn(II) complexes 1-3 based on dihydrazone pyrimidine derivatives HL-HL were synthesized and characterized using IR spectroscopy, H NMR spectroscopy, single crystal X-ray diffraction analysis, XRD, TG and elemental analysis. Single crystal X-ray diffraction analysis revealed that 1-3 all displayed a [2 × 2] grid-like topology.

Ribosome Biogenesis Regulator 1 Homolog (RRS1) Promotes Cisplatin Resistance by Regulating AEG-1 Abundance in Breast Cancer Cells.

Many ribosomal proteins are highly expressed in tumors and are closely related to their diagnosis, prognosis and pathological characteristics. However, few studies are available on the correlation between ribosomal proteins and chemoresistance. RRS1 (human regulator of ribosome synthesis 1), a critical nuclear protein involved in ribosome biogenesis, also plays a key role in the genesis and development of breast cancer by protecting cancer cells from apoptosis.

Design, synthesis and in vitro/in vivo anticancer activity of tranylcypromine-based triazolopyrimidine analogs as novel LSD1 inhibitors.

Histone lysine specific demethylase 1 (LSD1) is responsible for the demethylation of mono-/dimethylated lysine residue on histone proteins. LSD1 plays an extensive and essential role in the pathogenesis and progression of many human diseases such as cancers, and thus is becoming an attractive therapeutic target for cancer treatment. Tranylcypromine (TCP) is an important chemical template for developing irreversible LSD1 inhibitors, representing a major chemotype of clinical candidates.

Radix Rehmanniae Praeparata (Shu Dihuang) exerts neuroprotective effects on ICV-STZ-induced Alzheimer's disease mice through modulation of INSR/IRS-1/AKT/GSK-3β signaling pathway and intestinal microbiota.

Radix Rehmanniae Praeparata (RRP, Shu Dihuang in Cinese) is widely used as primal medicine in Chinese herbal formula for the treatment of Alzheimer's disease (AD). However, the underlying mechanism of RRP for AD remains unclear. The aim of this study was to investigate the therapeutic effect of RRP on intracerebroventricular injection of streptozotocin (ICV-STZ)-induced AD model mice and its potential mechanism.

Synthesis, Biological Evaluation, DNA Binding, and Molecular Docking of Hybrid 4,6-Dihydrazone Pyrimidine Derivatives as Antitumor Agents.

In the present paper, on the basis of molecular hybridization, a series of 4,6-dihydrazone pyrimidine derivatives containing the pyridine moiety were synthesized, structurally characterized, and evaluated in vitro for their antitumor activity. According to the results, all the tested compounds demonstrated broad-spectrum antitumor activity against selected tumor cell lines (MCF-7, BGC-823, A549, and BEL-7402) and no obvious toxicity toward normal cells HL-7702. In particular, compounds and were found to be the most promising antitumor agents among the tested compounds against BGC-823 cells (IC = 9.

Pre-treatment systemic immune-inflammation index as a non-invasive biomarker for predicting clinical outcomes in patients with renal cell carcinoma: a meta-analysis of 20 studies.

Introduction: To systematically assess the predictive significance of systemic immune-inflammation index (SII) in renal cell carcinoma (RCC).

Methods: Relevant studies published before November 2022 were retrieved from public databases. Hazard ratio (HR), standardised mean difference (SMD) and relative risk (RR) were calculated to estimate associations of SII with prognosis, treatment responses and clinicopathological features.

Measuring Well-Being of Migrant Gig Workers: Exampled as Hangzhou City in China.

The consistent innovations and applications of information technology drive the vigorous development of the gig economy, and generate gig workers such as food delivery workers and couriers, and make a great contribution to stabilizing employment and increasing income. Gig workers, mostly made up of migrants, and suffer from job and status difficulties. Research on the well-being of migrant gig workers can reveal the practical problems and provide suggestions for narrowing the wealth gap to promote social fairness and justice.

Down-regulation of EVA1A by miR-103a-3p promotes hepatocellular carcinoma cells proliferation and migration.

Background: EVA1A (Eva-1 homolog A), a novel protein involved in autophagy and apoptosis, functions as a tumor suppressor in some human primary cancers, including hepatocellular carcinoma (HCC). While it is consistently downregulated in several cancers, its involvement in hepatocarcinogenesis is still largely unknown.

Methods: We first detected the expression of EVA1A in HCC tissues and cell lines using RT‒qPCR, immunohistochemistry and western blotting and detected the expression of miR-103a-3p by RT‒qPCR.

Multiplexed strategies toward clinical translation of extracellular vesicles.

Extracellular vesicles (EVs), of which exosomes are a representative subgroup, are naturally secreted nanoparticles with a variety of payloads. With the intrinsic merits of stability, biocompatibility, low immunogenicity, and large capacity, EVs are widely regarded as effective carriers of drug delivery. However, disadvantages, such as low yield, complicated isolation procedures, and low loading efficiency, hinder its clinical translation.

LiuweiDihuang improved cognitive functions in SAMP8 mice by inhibiting COX-2 expression and subsequent neuroinflammation.

Ethnopharmacological Relevance: LiuweiDihuang (LW) pills was mainly used to treatment of children's fontanelle incomplete closure, enuresis and nervous system development delays and other diseases.Following the deepening of pharmacological research, LW has a good effect on neurological diseases include senile dementia. However, the neuroprotection mechanism of LW on Alzheimer's disease (AD) through regulation of inflammation remains unclear.

Downregulated RRS1 inhibits invasion and metastasis of BT549 through RPL11‑c‑Myc‑SNAIL axis.

Regulator of ribosome synthesis 1 (RRS1) is a key factor in ribosome biosynthesis and other cellular functions. High level of RRS1 in breast cancer cell lines is associated with increased cell proliferation, invasion and migration. RRS1 controls the assembly of the 60s subunit and maturation of 25S rRNA during ribosome biosynthesis.

Identification of AGT and CD44 in methotrexate-resistant colorectal cancer and reversal of methotrexate-resistance.

This study aims to screen out hub genes in 2 methotrexate-resistant colorectal cancer (CRC) cells (HT29 and Caco2), compared with parental CRC cells and reverse methotrexate-resistance in methotrexate-resistant CRC. GEO database and R software were utilized to analyze the gene expression profiles GSE11440 and GSE16066. Venn diagram was used to identify intersection differentially expressed genes (DEGs) between GSE11440 and GSE16066.

The mining and construction of a knowledge base for gene-disease association in mitochondrial diseases.

Mitochondrial diseases are a group of heterogeneous genetic metabolic diseases caused by mitochondrial DNA (mtDNA) or nuclear DNA (nDNA) gene mutations. Mining the gene-disease association of mitochondrial diseases is helpful for understanding the pathogenesis of mitochondrial diseases, for carrying out early clinical diagnosis for related diseases, and for formulating better treatment strategies for mitochondrial diseases. This project researched the relationship between genes and mitochondrial diseases, combined the Malacards, Genecards, and MITOMAP disease databases to mine the knowledge on mitochondrial diseases and genes, used database integration and the sequencing method of the phenolyzer tool to integrate disease-related genes from different databases, and sorted the disease-related candidate genes.