Flavonol derivatives containing pyrazole oxime ether: design, synthesis, and anti-TMV activity.

A series of flavonol derivatives containing pyrazole oxime ether moieties were designed and synthesized. In vivo antiviral assays revealed that some compounds exhibited remarkable inhibitory effects against tobacco mosaic virus (TMV). Among them, Both the curative activity (EC = 88.

Carbon Nanohorns and Polydopamine as Eco-Friendly Pesticide Carriers: Nanoencapsulation Based on Thiazoleamide Derivatives and Synergistic Antifungal Effects.

In this study, a nanodelivery system (CNH-Q7-PDA) based on van der Waals force-driven self-assembly was developed, where carbon nanohorns (CNH) adsorbed Q7 and were encapsulated by polydopamine (PDA) to enhance pesticide application efficiency. Simulated rainfall washoff experiments demonstrated that the incorporation of PDA significantly reduced the rolling and bouncing of carriers on plant leaves, effectively improving the deposition and retention rates of pesticides on the leaves. Meanwhile, antifungal experiments revealed that CNH-Q7-PDA exhibited superior fungicidal activity compared to Q7 and CNH-Q7.

Choroidal metastasis as the first sign of small cell lung cancer: A case report.

Metastases in the choroid originating from small cell lung cancer (SCLC) remain rare. The diagnosis of ocular metastases and primary lung tumors in individuals with SCLC can be challenging and time-consuming, particularly when their first symptoms present as ocular. The treatment of patients with ocular metastases of lung cancer is another clinical challenge in terms of primary tumor control and metastasis suppression.

Clinical outcomes of contezolid in treating complex tuberculosis: real-world evidence from 11 patients.

Background: Tuberculosis (TB) remains a major global health challenge, especially among patients with drug intolerance or comorbidities that limit treatment options. Although linezolid (Lzd), an oxazolidinone antibiotic, has demonstrated good efficacy against (MTB), its long-term use is frequently associated with serious adverse effects such as myelosuppression and peripheral neuropathy. Contezolid, a novel oxazolidinone with a more favorable safety profile, has shown comparable activity against MTB.

Corrigendum: Facile assembly of thermosensitive liposomes for active targeting imaging and synergetic chemo-/magnetic hyperthermia therapy.

[This corrects the article DOI: 10.3389/fbioe.2021.

Discovery of Potential Antifungal Agents: Chalcone Derivatives Containing Thiourea and Piperidine Moieties.

Twenty-two chalcone derivatives containing thiourea and piperidine moieties were synthesized. The in vitro antifungal activities of these compounds against nine fungi were evaluated. The results demonstrated that a majority of these compounds exhibited exceptional antifungal activities.

Effects of stigma on the quality of life in patients with epilepsy.

Background: This study was aimed to evaluate the stigma and quality of life (QoL) in adult patients with epilepsy (PWEs) and explore the relationship between stigma and QoL.

Methods: Two hundred and ninety-eight PWEs admitted to the Epilepsy Center of the First Affiliated Hospital of Chongqing Medical University during September 2020 and March 2021 were enrolled in this study. All participants completed self-reported questionnaires including the Stigma Scale for Epilepsy and the Quality of Life in Epilepsy Inventory-31 (QOLIE-31).

RRM1 O-GlcNAcylation inhibition suppresses pancreatic cancer via TK1-mediated replication stress.

O-GlcNAcylation of ribonucleotide reductase large subunit M1 (RRM1) at position 734 influences high glucose-induced genomic instability and cell transformation in normal pancreatic cells. By disrupting the ribonucleotide reductase complex, it reduces dNTPs. Although the impact of RRM1 O-GlcNAcylation on pancreatic cancer progression remains unexplored, our CRISPR knock-in technology created the RRM1-T734A mutation to minimize RRM1 O-GlcNAcylation.

Identification of PTGR2 inhibitors as a new therapeutic strategy for diabetes and obesity.

Peroxisome proliferator-activated receptor γ (PPARγ) is a master transcriptional regulator of systemic insulin sensitivity and energy balance. The anti-diabetic drug thiazolidinediones (TZDs) are potent synthetic PPARγ ligands with undesirable side effects, including obesity, fluid retention, and osteoporosis. 15-keto prostaglandin E2 (15-keto-PGE2) is an endogenous PPARγ ligand metabolized by prostaglandin reductase 2 (PTGR2).

Optimizing phage therapy for carbapenem-resistant bacteremia: insights into dose and timing.

The increase in multidrug-resistant (MDR) complex (ECC) infections, particularly those resistant to carbapenems, underscores the urgent need for alternative therapies. Phage therapy, with its specific bactericidal action, offers a promising solution. However, there remains a shortage of well-characterized ECC-targeting phages, and dosing and timing optimization for ECC-specific phage cocktails is largely unexplored.

Discovery of highly effective antiviral agents based on flavonoid-benzothiazole against TMV.

A series of flavonol derivatives containing benzothiazole were designed and synthesized. The structures of all the compounds were characterized by NMR and HRMS. The results of the activity assay showed that some of the target compounds possessed outstanding in vivo antiviral activity against the tobacco mosaic virus (TMV).

Innovative cyclic peptide disrupts IL-17RB-MLK4 interaction for targeted pancreatic cancer therapy.

The IL-17B/IL-17RB oncogenic signaling axis promotes pancreatic cancer progression through interaction with mixed-lineage kinase 4 (MLK4). Here, we improved the effectiveness of a therapeutic peptide (TAT-IL17RB, loop peptide) that disrupted IL-17RB/MLK4 interaction by converting its linear structure into a cyclic form. The modified cyclic peptide with higher uptake efficiency inhibited pancreatic cancer cell growth and metastasis, outperforming the original linear peptide both in vitro and in an orthotopic mouse model.

An Injectable Hydrogel Bioimplant Loaded with Engineered Exosomes and Triple Anti-Tuberculosis Drugs with Potential for Treating Bone and Joint Tuberculosis.

Purpose: Treatment for bone and joint tuberculosis (BJTB) is challenging due to its refractory and recurrent nature. This study aimed to develop a bioimplantable scaffold with osteoinductive and antituberculosis characteristics to treat BJTB.

Methods: This scaffold is built on oxidized hyaluronic acid and carboxymethyl chitosan hydrogel mixed with hydroxyapatite as a bone tissue engineered material.

Anti-TMV activity based flavonol derivatives containing piperazine sulfonyl: Design, synthesis and mechanism study.

A series of flavonoid derivatives containing piperazine sulfonate were designed and synthesized. The results of antiviral experiments in vivo showed that some target compounds had good inhibitory effect on tobacco mosaic virus (TMV). The EC values of S15 and S19 curative activity were 174.

Discovery of novel flavonoid derivatives containing benzothiazole as potential antifungal agents.

Background: Fungal diseases of plants have a serious impact on the quality and yield of crops, and some traditional pesticides can no longer cope with this problem. Therefore, it is of great significance to develop new pesticides with high efficiency and low toxicity.

Results: A series of flavonoid derivatives containing benzothiazole were designed and synthesized.

Tacrolimus regulates extracellular vesicle secretion from T cells via autophagy-lysosomal pathway.

Extracellular vesicles (EVs) derived from T cells have been proposed to mediate intercellular communication and orchestrate immune responses. The immunosuppressive drug, tacrolimus (TAC), suppresses T cell activity; however, the impact of TAC on T cell-derived EVs remains primarily unexplored. In this study, human primary T cells purified from healthy donors were used to investigate TAC-mediated regulation of EV secretion by T cells.

Digital boundaries: A study on WeChat parent-child relationships among Chinese college students and their association with family factors.

Objective: This study aims to investigate the current state of WeChat parent-child relationships among college students and their association with family factors.

Methods: Using convenient sampling, 6159 students,age from 18 to 25,the participants were selected from colleges of Chengdu to complete a questionnaire survey on response and attitudes towards parents' WeChat friend requests, Family APGAR Index,Parental Management Scale,Family Conflict Scale,were used as measurement tools.

Results: Responses to parental WeChat friend requests showed significant positive correlations with higher levels of family function satisfaction (r = 0.

Antifungal activity of chalcone derivatives containing 1,2,3,4-tetrahydroquinoline and studies on them as potential SDH inhibitors.

Background: A large number of pathogenic fungi have caused serious damage to the global crop yield, and drug resistance is always a topic that cannot be avoided for traditional fungicides. Therefore, finding efficient, green, and low-toxic fungicides is our primary task, which brings opportunities for the development of natural product green pesticides.

Results: Twenty chalcone derivatives containing 1,2,3,4-tetrahydroquinoline were designed and synthesized, and the compounds were tested for their fungicidal effects against eight plant pathogenic fungi in vitro.

SEMA7A-mediated juxtacrine stimulation of IGFBP-3 upregulates IL-17RB at pancreatic cancer invasive front.

Tumor invasion is the hallmark of tumor malignancy. The invasive infiltration pattern of tumor cells located at the leading edge is highly correlated with metastasis and unfavorable patient outcomes. However, the regulatory mechanisms governing tumor malignancy at the invasive margin remain unclear.

Novel Flavonol Derivatives Containing Quinoxaline: Insights into the Antifungal Mechanism against .

In this study, 12 pairs of tautomeric flavonol derivatives containing quinoxaline were synthesized. The results of antifungal activity showed that in the enol-keto tautomerism, the target compounds containing keto ( series) had better inhibitory activity against (.) than compounds containing enol ( series).