Mechanism Of Inhibition Research Articles

The Role of MicroRNA-124-3p in Breast Cancer Stem Cell Inhibition by Benzyl Isothiocyanate.

We have shown previously that benzyl isothiocyanate (BITC) derived from cruciferous vegetables inhibits self-renewal of breast cancer stem-like cells (bCSC). The current study provides insights into the mechanism of bCSC inhibition by BITC. Quantitative real time-polymerase chain reaction and western blot analysis were performed to detect microRNAs(miRNAs) and Forkhead box Q1 (FoxQ1) protein expression, respectively. The bCSC were characterized by aldehyde dehydrogenase 1 activity and flow cytometric analysis of CD49f high/CD133high fraction. BITC treatment resulted in induction of miR-124-3p expression in MDA-MB-231 and MCF-7 cells. miR-124-3p did not affect BITC-mediated inhibition of cell migration or cell proliferation but it significantly regulated bCSC in response to BITC. We also found that miR-124-3p directly targets the 3'untranslated regions (UTR) of FoxQ1 and negatively regulates its expression. The BITC-mediated inhibition of bCSC was partially attenuated by miR-124-3p inhibitor. These findings indicate that miR-124-3p plays an important role in BITC-mediated inhibition of bCSC.

Inhibition of EREG/ErbB/ERK by Astragaloside IV reversed taxol-resistance of non-small cell lung cancer through attenuation of stemness via TGFβ and Hedgehog signal pathway.

Taxol is the first-line chemo-drug for advanced non-small cell lung cancer (NSCLC), but it frequently causes acquired resistance, which leads to the failure of treatment. Therefore, it is critical to screen and characterize the mechanism of the taxol-resistance reversal agent that could re-sensitize the resistant cancer cells to chemo-drug. The cell viability, sphere-forming and xenografts assay were used to evaluate the ability of ASIV to reverse taxol-resistance. Immunohistochemistry, cytokine application, small-interfering RNA, small molecule inhibitors, and RNA-seq approaches were applied to characterize the molecular mechanism of inhibition of epiregulin (EREG) and downstream signaling by ASIV to reverse taxol-resistance. ASIV reversed taxol resistance through suppression of the stemness-associated genes of spheres in NSCLC. The mechanism exploration revealed that ASIV promoted the K48-linked polyubiquitination of EREG along with degradation. Moreover, EREG could be triggered by chemo-drug treatment. Consequently, EREG bound to the ErbB receptor and activated the ERK signal to regulate the expression of the stemness-associated genes. Inhibition of EREG/ErbB/ERK could reverse the taxol-resistance by inhibiting the stemness-associated genes. Finally, it was observed that TGFβ and Hedgehog signaling were downstream of EREG/ErbB/ERK, which could be targeted using inhibitors to reverse the taxol resistance of NSCLC. These findings revealed that inhibition of EREG by ASIV reversed taxol-resistance through suppression of the stemness of NSCLC via EREG/ErbB/ERK-TGFβ, Hedgehog axis.

Defect inhibition mechanism of 3D‐printed ceramics via synergetic resin composition and debinding processing regulation

AbstractProducing ceramic parts by Vat Photopolymerization (VPP) additive manufacture with desired mechanical properties typically requires time‐consuming debinding steps. This study aims at optimizing composition and processing parameters with the use of dibutyl phthalate (DBP) in the resin formulation and debinding in an argon atmosphere for dental zirconia‐toughed alumina (ZTA). The method produces parts with fewer defects, and 67.7% higher flexural strength while increasing the debinding heating rate over 400% compared to standard formulations debinded in air. These improvements are attributed to pore formation at low temperatures and reduced heat release and gas evolution rates arising from use of the DBP and the inert atmosphere, respectively. While ZTA ceramics were studied, this method should be applicable to many ceramic systems with exciting possibilities for promoting the rapid development of VPP 3D‐printed high‐performance ceramics for various engineering applications.

Insight into the responses of the anammox granular sludge system to tetramethylammonium hydroxide (TMAH) during chip wastewater treatment

Tetramethylammonium hydroxide (TMAH), an extensively utilized photoresist developer, is frequently present in ammonium-rich wastewater from semiconductor manufacturing, and its substantial ecotoxicity should not be underestimated. This study systematically investigated the effects of TMAH on the anammox granular sludge (AnGS) system and elucidated its inhibitory mechanisms. The results demonstrated that the median inhibitory concentration of TMAH for anammox was 84.85 mg/L. The nitrogen removal performance of the system was significantly decreased after long-term exposure to TMAH (0–200 mg/L) for 30 days (p < 0.05), but it showed adaptability to certain concentrations (≤50 mg/L). Concurrently, the stability of the granules decreased dramatically, resulting in the breakdown of AnGS. Further investigations indicated that TMAH exposure increased the secretion of extracellular polymeric substances but weakened their defense function. The increase in reactive oxygen species resulted in damage to the cell membrane. Reduced activity of anammox bacteria, impeded electron transfer, and changes in enzyme activity suggested that TMAH affected the metabolic activity. Microbiological analysis revealed that TMAH caused a decrease in the abundance of anammox bacteria and a weakening of symbiotic interactions within the microbial community. These results provide valuable guidance for the AnGS system application in chip wastewater treatment.

Synthesis of silane-modified styrene-acrylic ester emulsion and its inhibition mechanism on whitening of calcium aluminate cement mortar

A new polymer, triethoxyvinylsilane-modified styrene-acrylic ester emulsion (TMSA), was synthesized through emulsion polymerization. The effect of TMSA on the whitening of calcium aluminate cement (CAC) mortar was investigated. The results showed that TMSA had an excellent inhibition effect on the whitening of the CAC mortar with only 0.8 % - 1.6 % addition. Analysis of the micro-morphology and Raman spectra revealed that the white deposits on the surface of the mortar were C4AC(_)H11 and CaCO3, whereas TMSA addition effectively inhibited the formation of C4AC(_)H11 and reduced the occurrence of CaCO3. Through investigating the hydration, Ca2+ concentration, capillary water absorption and pore structure, it was found that the effect of the CAC hydration on the whitening of the mortars was inessential, whereas there was a strong link among whitening, capillary water absorption and macro-capillary pores. The addition of TMSA not only reduced the concentration of Ca2+ which was the source of the whitening, but also reduced the formation of macro-capillary pores in the CAC mortar that led to a significant reduction in the capillary water absorption, thus weakening the mobility of pore solution in the mortar and hindering the migration of Ca2+ to the mortar surface. Based on these two aspects, TMSA effectively inhibited the whitening of the CAC mortar.

The molecular mechanisms of Caulophyllum robustum Maxim extract inhibition by regulating FAK/PI3K signaling pathway in gastric cancer HGC-27 cells

Ethnopharmacological relevanceCaulophyllumrobustum Maxim extract (CRME), as recorded in traditional Chinese medicine, has the function of dispelling Feng, regulating Qi and dredging collaterals, promoting blood circulation and regulating menstruation, gingering up and relieving pain, clearing heat simultaneously detoxifying, lowering blood pressure and hemostasis. CRME is often used as Chinese materia medica preparation for rheumatoid arthritis, traumatic injury, irregular menstruation, abdominal pain, and hypertension treatment. Since gastric cancer (GC) existed as a health problem of human over the years, we are committed to the development of potential components of Chinese herbal medicine curing cancer, and we found CRME is expected to be one of the effective anti-tumor traditional Chinese medicine preparations. Aims of the studyTo investigate the molecular mechanisms of CRME anticancer effects and the potential links between CRME and FAK. Materials and methodsCaulophyllumrobustum Maxim was extracted to obtain CRME, high-performance liquid chromatography (HPLC) was used for qualitative analysis. Information about CRME was collected from traditional Chinese medicine records and local surveys unpublished internationally. Series of cellular function experiments were applied to detect cell proliferation, migration, apoptosis, autophagy, cell cycle, angiogenesis. The xenograft model is employed in vivo. ResultsCRME can significantly inhibit HGC-27 cells on proliferation, migration and angiogenic capacity. Xenograft model indicated CRME inhibited cell proliferation in vivo. Annexin V-FITC/PI double staining assay and PI single staining assay depicted that CRME induces cell apoptosis, and arrests cell cycle at G0/G1 phase. AO (acridine orange) staining assay showed that CRME promoted autophagosome formation and inhibited autophagic flow. HPLC indicated Cauloside A and Cauloside C are components of CRME. Western blot indicated that FAK/PI3K signaling pathway is critical in the inhibition of CRME on HGC-27 cells. ConclusionsThe anti-tumor components of CRME, Cauloside A and Cauloside C, inhibited tumor progression in HGC-27 cells. This inhibition is achieved by decreasing the phosphorylation levels of FAK, thereby modulating PI3K/AKT signaling pathway.

Phytoconstituent and In silico Screening of Active Compounds from Red Ginger (Zingiber officinale var. rubrum Theilade) Rhizome and Avocado (Persea americana Mill.) Leaves Extracts as Novel Inhibitors of MRSA

Red ginger rhizome (Zingiber officinale var. Rubrum) and avocado leaves (Persea americana Mill.) are empirically known as one of the medicinal plants used in Taro Village, Gianyar Regency, Bali which have great potential in treating infectious diseases caused by antibiotic resistance, such as MRSA. This study aims to analyze the phytoconstituents and anti-MRSA potential contained in red ginger rhizome and avocado leaves extracts by assessing their inhibitory effects on three proteins related to MRSA resistance and virulence (PBAP2a, transglycosylase, and glycosyltransferase). Phytoconstituents of avocado leaf and red ginger extracts were analyzed using GC-MS. Molecular docking was performed in silico to determine the similarity properties of predicted drugs, bioactivity, toxicity, identification of active sites and validation of protein structures, and docking simulations were performed between compounds found in the extract and their target proteins. Phytoconstituent analysis revealed that avocado leaves and red ginger extracts as a whole have 43 types of compounds and 10 bioactive compounds each with beneficial drug-like properties. The compound 6,11-hexadecadien-1-ol from avocado leaves extracts was predicted to have hepatotoxic properties. There were at least 3 compounds, namely beta-bisabolene from avocado leaves extract, zingiberenol and gamma-curcumene from red ginger rhizome extract, showing the lowest binding affinity for the target protein. Red ginger rhizome and avocado leaves extracts showed valuable potential as anti-MRSA agents through the mechanism of inhibition of three resistance-related proteins, as predicted by in silico analysis.

Berberine modulates ovarian cancer autophagy and glycolysis through the LINC01123/P65/MAPK10 signaling axis

BackgroundBerberine, a readily accessible natural compound known for its ease of synthesis and low toxicity, exhibits anti-tumor properties by modulating inflammatory responses. Recent studies have revealed that berberine can also treat malignant tumors by influencing tumor metabolic reprogramming, making it a potential candidate for metabolic therapy in ovarian cancer. MethodsThe anti-proliferative and anti-metastatic effects of berberine on ovarian cancer cells were investigated using CCK-8 assays, scratch assays, EDU proliferation assays, and assays related to glycolysis and autophagy. Differentially expressed lncRNAs in ovarian cancer were identified using data from the TCGA database. A specific lncRNA's role was delineated through RNA pulldown assays, silver staining, mass spectrometry analysis, CHIP assays, and immunoprecipitation experiments, focusing on its involvement in glycolysis and autophagy regulation in ovarian cancer. Additionally, the inhibitory mechanism of berberine on ovarian cancer cells was validated through cell thermal shift assays and cycloheximide protein degradation experiments to confirm its interaction with key targets. ResultsIn vitro experiments revealed that berberine reduces glycolysis and autophagy levels, leading to the inhibition of ovarian cancer cell proliferation and metastasis. Bioinformatics analysis of TCGA data identified LINC00123 as associated with poor prognosis in ovarian cancer. Experimental validation, including RNA pulldown assays, confirmed that the LINC00123/P65/MAPK10 signaling axis regulates glycolysis and autophagy in ovarian cancer. Furthermore, at the molecular level, berberine inhibits the interaction between LINC00123 and P65, thereby reducing P65 protein stability and impeding its transcriptional regulation of downstream MAPK10. These findings were further validated in animal models. ConclusionOur study highlights berberine's dual benefits of anti-inflammatory effects and inhibition of ovarian cancer proliferation and metastasis by modulating autophagy and glycolysis levels. Mechanistically, berberine targets the LINC00123/P65/MAPK10 signaling pathway to regulate glycolysis and autophagy in ovarian cancer. These insights not only expand the potential of berberine in ovarian cancer therapy but also provide new targets and therapeutic strategies for metabolic therapy in this cancer type.

Synthesis, structural characterization, thermal analysis and anticorrosion properties of novel AZO-based imidazo[1,2-a]pyridine derivatives: Experimental study and theoretical approaches

In this study, innovative AZO-based imidazo[1,2-a]pyridine derivatives were synthesized using simple and efficient synthetic approach enabling large-scale production. Thermal analysis highlights their suitability for potential applications requiring resistance to moderate temperatures. These compounds were investigated as corrosion inhibitors for MS in a 1 M HCl-medium. Corrosion inhibition studies, including weight loss, PotentioDynamic polarization and electrochemical impedance spectroscopy methods, revealed that AZOs exhibited maximum corrosion inhibition efficiencies reaching 96.13 % and 94.07 %, respectively, at a concentration of 10−3 M and a temperature of 298 K, with both compounds acting as mixed-type inhibitors. The study also delved into the influence of temperature and immersion time on inhibitory performance, revealing stable inhibition within the temperature range of 298–328 K. The calculated standard free energy of adsorption was −42.06 and −40.62 kJ/mol for AZO 1 and AZO 2, respectively, suggesting mixed-type adsorption, with adsorption behavior following the Langmuir isotherm. Morphological analysis through SEM and AFM, showed a reduction in surface roughness in the presence of the inhibitors, while water contact angle measurements indicated a significant increase in surface hydrophobicity. UV–visible and FT-IR analyses confirmed the interaction of AZOs with the MS surface, suggesting the formation of a protective layer composed of adsorbed AZO molecules. Furthermore, computational investigations employing DFT, Monte Carlo, and Molecular Dynamic simulation revealed the formation of coordinate bonds between the studied inhibitors and the metal surface, confirming adsorption on the metallic surface. These findings align well with experimental outcomes, and a possible corrosion inhibition mechanism process was discussed.

Biological Activity of Ethanol Extract of Terminalia chebula Dried Carp against Bacterial Wilt of Lycopersicum esculentum and its Mechanism of Inhibition

Biological Activity of Ethanol Extract of Terminalia chebula Dried Carp against Bacterial Wilt of Lycopersicum esculentum and its Mechanism of Inhibition

Unveiling the Complexity of cis-Regulation Mechanisms in Kinases: A Comprehensive Analysis.

Protein cis-regulatory elements (CREs) are regions that modulate the activity of a protein through intramolecular interactions. Kinases, pivotal enzymes in numerous biological processes, often undergo regulatory control via inhibitory interactions in cis. This study delves into the mechanisms of cis regulation in kinases mediated by CREs, employing a combined structural and sequence analysis. To accomplish this, we curated an extensive dataset of kinases featuring annotated CREs, organized into homolog families through multiple sequence alignments. Key molecular attributes, including disorder and secondary structure content, active and ATP-binding sites, post-translational modifications, and disease-associated mutations, were systematically mapped onto all sequences. Additionally, we explored the potential for conformational changes between active and inactive states. Finally, we explored the presence of these kinases within membraneless organelles and elucidated their functional roles therein. CREs display a continuum of structures, ranging from short disordered stretches to fully folded domains. The adaptability demonstrated by CREs in achieving the common goal of kinase inhibition spans from direct autoinhibitory interaction with the active site within the kinase domain, to CREs binding to an alternative site, inducing allosteric regulation revealing distinct types of inhibitory mechanisms, which we exemplify by archetypical representative systems. While this study provides a systematic approach to comprehend kinase CREs, further experimental investigations are imperative to unravel the complexity within distinct kinase families. The insights gleaned from this research lay the foundation for future studies aiming to decipher the molecular basis of kinase dysregulation, and explore potential therapeutic interventions.

High temperature long-lasting corrosion inhibition mechanism of sodium dodecyldiphenyl ether disulfonate on ADC12 aluminum alloy in oxalic acid solution

The high temperature corrosion inhibition mechanism of sodium dodecyl diphenyl ether disulfonate (MADS) on ADC12 aluminum alloy in oxalic acid solution at 80 °C was investigated using electrochemical measurements, surface characterization and theoretical computations. The results manifested that MADS still had excellent performance in high-temperature oxalic acid solution, and was a highly efficient and long-lasting corrosion inhibitor with an optimal corrosion inhibition efficiency (ƞ) of 90.90 %. With increasing soaking time, the ƞ increased to 98.70 %. MADS molecule adsorbed on the aluminum alloy surface in an L-shaped walking scooter configuration through physicochemical adsorption to form a dense, thin and stable hydrophobic film, inhibiting the formation of aluminum oxalate and Al2O3, and protecting it from corrosion.

Biogenic synthesis of AgNPs via polyherbal formulation: Mechanistic neutralization and toxicological impact on acetylcholinesterase from Bungarus sindanus venom.

This study aims to examine the biogenic production, characterization, and anti-acetylcholinesterase (AAChE) properties of polyherbal formulation PHF-extract-synthesized silver nanoparticles (PHF-AgNPs). The Elapidae snake Bungarus sindanus has extremely dangerous venom for humans and contains a high amount of AChE (acetylcholinesterase). Inhibiting AChE leads to acetylcholine buildup, affecting neurotransmission. The study tested silver nanoparticles as AChE inhibitors using kinetics. Their production was confirmed through ultraviolet (UV) spectrometry at 425 nm (SPR peak of 1.94), and stabilizing functional groups were identified via Fourier transform infrared spectroscopy (FT-IR). The average length of 20 nm was confirmed by analyzing the scanning electron microscopy (SEM) data. Energy-dispersive X-ray spectroscopy (EDX) identified silver as the primary component of PHF-AgNPs (26%). Statistical analysis showed that the activity of AChE in krait venom decreased by up to 45% and 37% at a given dose of ACh (0.5 mM) by PHF and AgNPs, respectively. Utilizing the Lineweaver-Burk plot for kinetic analysis, a competitive type of inhibition is found. RESEARCH HIGHLIGHTS: Successfully synthesized PHF-extract-induced silver nanoparticles (PHF-AgNPs) demonstrated through UV spectrometry and characterized as crystalline with an average size of 45 nm by X-ray diffraction. PHF-AgNPs effectively inhibited acetylcholinesterase (AChE), an enzyme critical in neurotransmission, reducing its activity in krait venom by up to 45% at certain concentrations. Kinetic analysis revealed that the inhibition mechanism of AChE by PHF-AgNPs is competitive, offering potential for therapeutic applications in neurologically related conditions.

Prevention and control of cardiac arrhythmic by using therapeutic foods: A review.

Arrhythmia occurs as a common heart vascular disease. Functional food is a rich source of natural compounds with significant pharmacological, The aim of this paper is to explore its effect on arrhythmia. By reviewing the literature and summarising the findings, we described the role of functional foods in the alleviation of cardiac arrhythmias from different perspectives. Our study shows that functional foods have anti-arrhythmic effects through modulation of ion channels, oxidative stress, and Calmodulin-dependent protein kinase II. We summarize the mechanism of arrhythmia inhibition by the active ingredients of medicinal diets in this review article, intending to provide research ideas for dietary therapy to regulate arrhythmia.

Synergistic effects of thermally reduced graphene oxide/zinc oxide composite material on microbial infection for wound healing applications

Infections originating from pathogenic microorganisms can significantly impede the natural wound-healing process. To address this obstacle, innovative bio-active nanomaterials have been developed to enhance antibacterial capabilities. This study focuses on the preparation of nanocomposites from thermally reduced graphene oxide and zinc oxide (TRGO/ZnO). The hydrothermal method was employed to synthesize these nanocomposites, and their physicochemical properties were comprehensively characterized using X-ray diffraction analysis (XRD), High-resolution transmission electron microscopy (HR-TEM), Fourier-transform infrared (FT-IR), Raman spectroscopy, UV-vis, and field-emission scanning electron microscopy (FE-SEM) techniques. Subsequently, the potential of TRGO/ZnO nanocomposites as bio-active materials against wound infection-causing bacteria, including Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli, was evaluated. Furthermore, the investigated samples show disrupted bacterial biofilm formation. A reactive oxygen species (ROS) assay was conducted to investigate the mechanism of nanocomposite inhibition against bacteria and for further in-vivo determination of antimicrobial activity. The MTT assay was performed to ensure the safety and biocompatibility of nanocomposite. The results suggest that TRGO/ZnO nanocomposites have the potential to serve as effective bio-active nanomaterials for combating pathogenic microorganisms present in wounds.

Investigating the inhibition of xanthine oxidase by five catechins: Kinetic studies, spectroscopy, molecular docking, and dynamics simulations

Catechins compounds from tea have demonstrated significant inhibitory effects on xanthine oxidase (XOD). However, the precise inhibitory mechanisms of the main catechins on XOD remain to be fully elucidated. This study explored the inhibition mechanisms and binding characteristics of five catechins (GC, EGC, EC, EGCG, and ECG) on XOD through a combination of inhibition kinetics, multi-spectroscopy analysis, molecular docking, and dynamics simulations. Among the catechins, EGCG and ECG exhibited the most potent inhibitory activities against XOD. All five catechins were found to exhibit mixed inhibition, affecting the hydrophobic groups and secondary structure of XOD predominantly through hydrophobic interactions and hydrogen bonding. Molecular dynamics simulations revealed that a 3,4,5-trihydroxybenzoic acid moiety at C3 position significantly enhances the binding affinity of EGCG and ECG to XOD. Additionally, the decrease of β-sheet and random coil induced by EGCG and ECG was found to be crucial for enhancing inhibitory activity of XOD. In vitro cell experiments showed that EGCG and ECG significantly reduced high uric acid levels of BRL-3A cell. This study elucidates the inhibitory mechanisms of catechins on XOD, paving the way for their application as XOD inhibitors to combat hyperuricemia.

Exploring the anti-NSCLC mechanism of phillyrin targeting inhibition of theHSP90-AKT pathway.

Phillyrin (PHN), derived from the dried fruit of Forsythia suspensa (Thunb.) Vahl, is a kind of Chinese herbal medicine with the effect of clearing heat, and has been used in China for thousands of years in treating various tumors. However, the mechanism of its main components on non-small cell lung cancer (NSCLC) remains unclear. PHN is a distinct component extracted from Forsythia suspensa with promising anti-cancer activity against various tumor types. This study sought to elucidate the promising effects of PHN on NSCLC. Based on network pharmacology results, we identified potential PHN targets and pathways for NSCLC treatment. CCK-8 assay, wound healing assay, apoptosis assay, western blot, and in vivo experiments verified the inhibitory effect of PHN on NSCLC. Network pharmacology identified 160 potential PHN targets, 955 NSCLC-related targets, and 54 common targets, along with 132 pathways and 2 core genes. Biological experiments demonstrated that PHN significantly inhibited the growth and migration of A549 and LLC cells while promoting their apoptosis. Western blot analysis revealed down-regulation of AKT, HSP90AA1, and CDC37 expression, suggesting that PHN inhibits A549 and LLC cell proliferation by down-regulating the HSP90-AKT pathway. In vivo experiments confirmed that PHN significantly inhibited NSCLC growth with low toxicity. This study, using network pharmacology and biological experiments, verified the effectiveness of PHN against NSCLC through the HSP90-AKT pathway. These findings provide a foundation for further research and analysis.

The Impact of Amphimedon chloros Ethyl Acetate Extract on MDA-MB-231 Cell Lines' Expression of Bax, Cyclin D, Caspase 3, P21, C-myc, and Bcl2: Mechanism of inhibition of the Growth of Cancer Cells

The Impact of Amphimedon chloros Ethyl Acetate Extract on MDA-MB-231 Cell Lines' Expression of Bax, Cyclin D, Caspase 3, P21, C-myc, and Bcl2: Mechanism of inhibition of the Growth of Cancer Cells

Inhibitory effect of caffeic acid and dihydrocaffeic acid on the formation of advanced glycation end products: Mechanism analysis based on intermolecular interaction

The accumulation of advanced glycation end products (AGEs) generated from glycation reaction accelerates the development and deterioration of some diseases. Herein, the AGEs model of fructose-induced glycation of human serum albumin (HSA) was constructed and characterized. Both caffeic acid (CA) and dihydrocaffeic acid (DHCA) can inhibit the formation of AGEs, and the inhibitory effect of CA was more pronounced, as confirmed by fluorescence spectroscopy, gel electrophoresis, scanning electron microscopy, and carbonyl and thiol contents analysis. The binding of CA and DHCA to HSA was investigated by fluorescence spectroscopy and molecular docking. The primary inhibitory mechanism was the occupation of the glycation site LYS199 of HSA, and the more significant inhibitory effect of CA was related to its stronger binding affinity. Furthermore, the conformational changes caused by glycation and CA/DHCA binding were monitored using fluorescence, circular dichroism, and dynamic light scattering analysis. The results would help to elucidate the inhibitory mechanism of CA and DHCA on AGEs formation based on their different structures and inhibitory effects, and provide guidance for choosing natural inhibitors for diabetes.

Antifungal activity of 2-chloro-5-trifluoromethoxybenzeneboronic acid and inhibitory mechanisms on Geotrichum candidum from sour rot Xiaozhou mustard root tuber

Xiaozhou mustard (Brassica napiformis) root tuber, a traditional fermented vegetable, has a long history in Rongan County, Guangxi Province. However, the frequent occurrence of root tuber sour rot by Geotrichum candidum (G. candidum) has seriously reduced Xiaozhou mustard production and quality in recent years. The objective of the present study is to investigate the antifungal efficacy of 2-chloro-5-trifluoromethoxybenzeneboronic acid (Cl-F-BBA) against G. candidum and its possible mechanisms. The results revealed that a concentration of 0.25 mg/mL Cl-F-BBA completely halted mycelial growth and spore germination. Furthermore, a slightly lower concentration of 0.20 mg/mL was sufficient to compromise the integrity of the plasma membrane in mycelia and mitochondria, leading to a reduction in respiratory rate, activities of malate dehydrogenase (MDH), and succinate dehydrogenase (SDH), ATP content, and energy charge. This concentration also significantly disordered antioxidant metabolism, resulting in the accumulation of reactive oxygen species (ROS) and malondialdehyde (MDA), and caused intracellular leakage in mycelia. In vivo experiments further demonstrated that Xiaozhou mustard root tubers treated with Cl-F-BBA exhibited markedly lower decay rates and lesion diameters compared to the control group. In summary, Cl-F-BBA presents a promising solution for controlling root tuber sour rot in Xiaozhou mustard caused by G. candidum.