Inhibitory effect of flavonoids on multidrug and toxin extrusion protein 1 function: Implications for food/herb-drug interaction and drug-induced kidney injury.

Multidrug and toxin extrusion protein 1 (MATE1), an efflux transporter mainly expressed in renal proximal tubules, mediates the renal secretion of organic cationic drugs. The inhibition of MATE1 will impair the excretion of drugs into the tubular lumen, leading to the accumulation of nephrotoxic drugs in the kidney and consequently potentiating nephrotoxicity. Screening and identifying potent MATE1 inhibitors can predict or minimize the risk of drug-induced kidney injury. Flavonoids, a group of polyphenols commonly found in foodstuffs and herbal products, have been reported to cause transporter-mediated food/herb-drug interactions. Our objective was to investigate the inhibitory effects of flavonoids on MATE1 in vitro and in vivo and to assess the effects of flavonoids on cisplatin-induced kidney injury. Thirteen flavonoids exhibited significant transport activity inhibition (>50%) on MATE1 in MATE1-MDCK cells. Among them, the six strongest flavonoid inhibitors, including irisflorentin, silymarin, isosilybin, sinensetin, tangeretin, and nobiletin, markedly increased cisplatin cytotoxicity in these cells. In cisplatin-induced in vivo renal injury models, irisflorentin, isosilybin, and sinensetin also increased serum creatinine and blood urea nitrogen levels to different degrees, especially irisflorentin, which exhibited the most potent nephrotoxicity with cisplatin. The pharmacophore model indicated that the hydrogen bond acceptors at the 3, 5, and 7 positions may play a critical role in the inhibitory effect of flavonoids on MATE1. Our findings provide helpful information for predicting the potential risks of flavonoid-containing food/herb-drug interactions and avoiding the exacerbation of drug-induced kidney injury via MATE1 mediation.

Rare earth elements applied to phytoremediation: Enhanced endocytosis promotes remediation of antimony contamination with different valence levels in Solanum nigrum L.

Antimony (Sb) pollution poses a noteworthy risk to human health and ecosystem sustainability, therefore effective, eco-friendly, and widely accepted restoration methods are urgently needed. This study introduces a new approach of using La(III) foliar application on Solanum nigrum L. (S. nigrum), a cadmium hyperaccumulator, to improve its photosynthetic and root systems under Sb stress, resulting in a higher biomass. Notably, La(III) also enhances endocytosis in root cells, facilitating efficient and non-selective remediation of both Sb(III) and Sb(V) forms. The absorption of Sb by root cell endocytosis was observed visually with a confocal laser scanning microscope. The subcellular distribution of Sb in the cell wall of S. nigrum is reduced. And the antioxidant enzyme activity system is improved, resulting in an enhanced Sb tolerance in S. nigrum. Based on the existing bibliometric analysis, this paper identified optimal conditions for S. nigrum to achieve maximum translocation and bioconcentration factor values for Sb. The foliar application of La(III) on plants treated with Sb(III), Sb(V), and a combination of both resulted in translocation factor values of 0.89, 1.2, 1.13 and bioconcentration factor values of 11.3, 12.81, 14.54, respectively. Our work suggests that La(III)-enhanced endocytosis of S. nigrum root cells is a promising remediation strategy for Sb-contaminated environments.

Tunable and highly sensitive fluorescent thermometers from La2CaZrO6:Cr3+ with a time-resolved technology.

Non-contact optical temperature measurement can effectively avoid the disadvantages of traditional contact thermometry and thus, become a hot research topic. Herein, a fluorescence intensity ratio (FIR) thermometry using a time-resolved technique based on La2CaZrO6:Cr3+ (LCZO) is proposed, with a maximum relative sensitivity (Sr - FIR) of 2.56% K-1 at 473 K and a minimum temperature resolution of 0.099 K. Moreover, the relative sensitivity and temperature resolution can be effectively controlled by adjusting the width of the time gate based on the time-resolved technique. Our work provides, to our knowledge, new viewpoints into the development of novel optical thermometers with adjustable relative sensitivity and temperature resolution on an as-needed basis.

Research progress in water quality prediction based on deep learning technology: a review.

Water, an invaluable and non-renewable resource, plays an indispensable role in human survival and societal development. Accurate forecasting of water quality involves early identification of future pollutant concentrations and water quality indices, enabling evidence-based decision-making and targeted environmental interventions. The emergence of advanced computational technologies, particularly deep learning, has garnered considerable interest among researchers for applications in water quality prediction because of its robust data analytics capabilities. This article comprehensively reviews the deployment of deep learning methodologies in water quality forecasting, encompassing single-model and mixed-model approaches. Additionally, we delineate optimization strategies, data fusion techniques, and other factors influencing the efficacy of deep learning-based water quality prediction models, because understanding and mastering these factors are crucial for accurate water quality prediction. Although challenges such as data scarcity, long-term prediction accuracy, and limited deployments of large-scale models persist, future research aims to address these limitations by refining prediction algorithms, leveraging high-dimensional datasets, evaluating model performance, and broadening large-scale model application. These efforts contribute to precise water resource management and environmental conservation.

Adjustable ultraviolet and white light dual emission phosphor Y2Sr(Ga1-yAly)4SiO12:xPr3+ for health lighting.

Mid-ultraviolet light (290-320 nm) can promote human vitamin D synthesis, which helps in the prevention and treatment of rickets and cartilage disease. For people who lack sufficient ultraviolet radiation all year round, it is significant to supplement the ultraviolet component in daily lighting sources. However, there are few luminous materials showing a combination of mid-ultraviolet light and white light emission on the market. Here, we designed a new material, Y2Sr(Ga1-yAly)4SiO12:xPr3+ (YSGAS:xPr3+), which achieves dual emission of 320 nm ultraviolet and white light from a single substrate with a single doped phosphor. Without Al3+ ions, the emission intensity of the Y2SrGa4SiO12:xPr3+ phosphor shows a contribution-dependent relationship, and concentration quenching due to exchange interaction. The crystal field environment was regulated by partially replacing Ga3+ ions with Al3+ ions. After introducing Al3+, YSGAS:xPr3+ phosphors exhibit dual ultraviolet emission (320 nm) and visible light emission. The emission color of YSGAS:xPr3+ can be adjusted by changing the Al3+ concentration, and Y2Sr(Ga0.6Al0.4)4SiO12:1%Pr3+ emits both ultraviolet light and white light. The LED device prepared by using the YSGAS:Pr3+ phosphor and chips shows a color temperature of 4858 K and appropriate CIE coordinates of (0.3474, 0.3390), indicating wide application prospects in the field of "health lighting" for particular populations.

A comprehensive review on the source, ingestion route, attachment and toxicity of microplastics/nanoplastics in human systems.

Microplastics (MPs)/nanoplastics (NPs) are widely found in the natural environment, including soil, water and the atmosphere, which are essential for human survival. In the recent years, there has been a growing concern about the potential impact of MPs/NPs on human health. Due to the increasing interest in this research and the limited number of studies related to the health effects of MPs/NPs on humans, it is necessary to conduct a systematic assessment and review of their potentially toxic effects on human organs and tissues. Humans can be exposed to microplastics through ingestion, inhalation and dermal contact, however, ingestion and inhalation are considered as the primary routes. The ingested MPs/NPs mainly consist of plastic particles with a particle size ranging from 0.1 to 1 µm, that distribute across various tissues and organs within the body, which in turn have a certain impact on the nine major systems of the human body, especially the digestive system and respiratory system, which are closely related to the intake pathway of MPs/NPs. The harmful effects caused by MPs/NPs primarily occur through potential toxic mechanisms such as induction of oxidative stress, generation of inflammatory responses, alteration of lipid metabolism or energy metabolism or expression of related functional factors. This review can help people to systematically understand the hazards of MPs/NPs and related toxicity mechanisms from the level of nine biological systems. It allows MPs/NPs pollution to be emphasized, and it is also hoped that research on their toxic effects will be strengthened in the future.

Shifting and state transformations-based adaptive tracking control for deferred full state-constrained uncertain nonlinear systems.

This paper concerns the tracking control problem of a class of uncertain nonlinear systems subject to deferred time-varying state constraints and external disturbances. The states of the system are free in the initial phase and are restricted by some time-varying constraints after a particular time. A class of novel shifting functions are defined, which make any initial states that beyond the constraint region move to the desired position (such as zero). Thereafter, a new state transformation is implemented for the shifted state, which transforms the state constraint problem into the boundedness of a new variable. Compared with the existing BLF method, this approach avoids feasibility test for virtual control variables. Adaptive backstepping control and dynamic surface control are used in system controller design and stability analysis, and the ideal tracking performance is achieved. Finally, simulation example and comparative studies are carried out to illustrate the effectiveness and outstanding characteristics of the proposed approach. Simulation results show that the proposed control scheme broadens the scope of application, shortens running time and improves control efficiency compared with the existing control strategies.

Lanthanum promotes Solanum nigrum L. growth and phytoremediation of cadmium and lead through endocytosis: Physiological and biochemical response, heavy metal uptake and visualization.

Rare earth elements (REEs) are important to enhance agricultural productivity. The utilization of phytoremediation as a green technology for addressing heavy metal (HMs) contamination in soil and wastewater has gained significant attention. In our research, we conducted indoor hydroponic experiments to examine the impacts of lanthanum (La) on the growth and enrichment capacity of Solanum nigrum L. (S. nigrum). S. nigrum was cultivated in 10 mg·L-1 of cadmium (Cd), 25 mg·L-1 of lead (Pb), and a mixture of both (5 mg·L-1 Cd + 15 mg·L-1 Pb). Additionally, S. nigrum were subjected to foliar spray or hydroponic supplementation of La(III). The treatment with La(III) significantly increased total fresh weight by 17.82 % to 42.20 %, compared to the treatment without La(III). Furthermore, La(III) facilitated the endocytosis of roots and enhanced Cd2+ flux ranging from 15.64 % to 75.99 % when compared to the treatment without La(III). Foliar and hydroponic application of La(III) resulted in an increase in the translocation factors (TF) in plants of Cd and Pb compared to treatments without La(III). These findings can offer valuable insights into the potential of La(III) to enhance the phytoremediation of soil or wastewater polluted with compounds.

Inhibitory interaction of flavonoids with organic anion transporter 3 and their structure-activity relationships for predicting nephroprotective effects.

The organic anion transporter 3 (OAT3), an important renal uptake transporter, is associated with drug-induced acute kidney injury (AKI). Screening and identifying potent OAT3 inhibitors with little toxicity in natural products, especially flavonoids, in reducing OAT3-mediated AKI is of great value. The five strongest OAT3 inhibitors from the 97 flavonoids markedly decreased aristolochic acid I-induced cytotoxicity and alleviated methotrexate-induced nephrotoxicity. The pharmacophore model clarified hydrogen bond acceptors and hydrophobic groups are the critical pharmacophores. These findings would provide valuable information in predicting the potential risks of flavonoid-containing food/herb-drug interactions and optimizing flavonoid structure to alleviate OAT3-related AKI.

Foliar spraying of lanthanum activates endocytosis in lettuce (Lactuca sativa L.) root cells, increasing Cd and Pb accumulation and their bioaccessibility.

Cadmium (Cd) and lead (Pb) accumulate easily in leafy vegetables and can harm human health. Lanthanum (La) have been used to improve agricultural yield and quality, but the effect of La application on Cd/Pb enrichment in leafy vegetables remains incomplete currently. A previous study reported that the endocytosis in lettuce leaf cells can be activated by La, leading to an increase in Pb accumulation in lettuce leaves. However, it has not been investigated whether foliar application of La enhances root cellular endocytosis and promotes its uptake of Cd and Pb. In this study, the influence of La on the uptake of Cd and Pb, Cd bioaccessibility, and the safety risks of cultivating lettuce under Cd and Pb stress were explored. It was found that La increased Cd (16-30 % in shoot, 16-34 % in root) and Pb (25-29 % in shoot, 17-23 % in root) accumulation in lettuce. The increased accumulation of Cd and Pb could be attributed to La-enhanced endocytosis. Meanwhile, La enhanced the toxicity of both Cd and Pb, inhibited lettuce growth, and aggravated the damage to the photosynthetic and antioxidant systems. Finally, gastrointestinal simulation experiments showed that La increased the Cd bioaccessibility in both gastric and intestinal phase by 7-108 % and 9-87 %, respectively. These results offer valuable insights into the safety of REEs for agricultural applications.

Cerebral neurotoxicity of amino-modified polystyrene nanoplastics in mice and the protective effects of functional food Camellia pollen.

Accumulating evidence suggests that nanoplastics contribute to an increased risk of brain damage, however, the precise underlying mechanisms remain unclear. Here, we subjected mice to long-term exposure to amino-modified polystyrene nanoplastics (APS-NPs). These nanoplastics were detected in the mouse brain; coupled with the observed upregulation of Alzheimer's disease-associated genes (APP and MAPT). To further explore nanoplastic damage mechanisms and the corresponding protective strategies against these mechanisms in vitro, we used hCMEC/D3 and HT22 cells. Results showed that APS-NPs disrupted tight junction proteins (Occludin and ZO-1) via TLR2/MMP9 axis, resulting in blood-brain barrier permeation; this was significantly mitigated by functional food Camellia pollen treatment. APS-NPs initiated iNOS and nNOS upregulation within neurons resulting in Sirtuin 1 deacetylase inactivation and CBP acetyltransferase stimulation, ultimately leading to Ac-Tau formation. This process was attenuated by Camellia pollen, which also ameliorated the APS-NPs-induced neuronal apoptosis mediated by the p53/Bax/Bcl-2 axis. Network pharmacology analysis of Camellia pollen offered a further theoretical understanding of its potential applications in preventing and treating nervous system disorders, such as Alzheimer's disease. This study established that Camellia pollen protects the brain against APS-NPs-mediated blood-brain barrier damage and alleviates neuronal apoptosis and Alzheimer's disease-like neurotoxicity. This study elucidates the mechanisms underlying polystyrene-induced brain damage and can be used to inform future prevention and treatment strategies.

Study on the mechanism of high energy transfer efficiency of blue light excited Cr3+, Nd3+ co-doped near infrared phosphors.

Although Cr3+ as activator for Near infrared (NIR) phosphors has been widely studied, the peaks of Cr3+ emission spectra in most hosts are less than 1000 nm. Nd3+ as an activator in many hosts has a wide distribution of absorption peaks in the Ultraviolet-visible-Near infrared (UV-vis-NIR) band, especially in the 650-900 nm band for effective NIR to NIR Stokes luminescence (4F3/2→4I9/2, 4F3/2→4I11/2 transitions). Therefore, Cr3+, Nd3+ co-doping to achieve the emission in the NIR II region (1000-1700nm) is very meaningful. Here, we report La2CaZrO6(LCZO): Cr3+, Nd3+ NIR phosphors with emission spectra covering an ultra-wide range of 700-1400 nm and reveal their luminescence mechanism. The energy transfer efficiency of Cr3+ for Nd3+ can be as high as 88.4% under 471 nm blue light excitation. In the same case, the integrated intensity of the emission spectra of Cr3+, Nd3+ co-doped can reach 847% of that of Nd3+ alone and 204% of that of Cr3+ alone. Finally, the combination of commercial blue light chips and Cr3+, Nd3+ co-doped NIR phosphors shows great potential for applications in face recognition, night lighting, and angiography.

A Meta-Analysis of Influencing Factors on the Activity of BiVO4-Based Photocatalysts.

With the continuous advancement of global industrialization, a large amount of organic and inorganic pollutants have been discharged into the environment, which is essential for human survival. Consequently, the issue of water environment pollution has become increasingly severe. Photocatalytic technology is widely used to degrade water pollutants due to its strong oxidizing performance and non-polluting characteristics, and BiVO4-based photocatalysts are one of the ideal raw materials for photocatalytic reactions. However, a comprehensive global analysis of the factors influencing the photocatalytic performance of BiVO4-based photocatalysts is currently lacking. Here, we performed a meta-analysis to investigate the differences in specific surface area, kinetic constants, and the pollutant degradation performance of BiVO4-based photocatalysts under different preparation and degradation conditions. It was found that under the loading condition, all the performances of the photocatalysts can be attributed to the single BiVO4 photocatalyst. Moreover, loading could lead to an increase in the specific surface area of the material, thereby providing more adsorption sites for photocatalysis and ultimately enhancing the photocatalytic performance. Overall, the construct heterojunction and loaded nanomaterials exhibit a superior performance for BiVO4-based photocatalysts with 136.4% and 90.1% improvement, respectively. Additionally, within a certain range, the photocatalytic performance increases with the reaction time and temperature.

Recent advancements on use of essential oils as preservatives against fungi and mycotoxins spoiling food grains.

Spoilage of grains by mycotoxigenic fungi poses a great threat to food security and human health. Conventionally used chemical agents to prevent grain fungi contamination cause increasingly significant problems such as microbial resistance, residual toxicity and environmental unfriendliness. In recent years, plant essential oils (EOs) have become a hot spot in the research of control of grain fungi and mycotoxins, due to their extensive sources, non-toxicity, environmental friendliness and good antifungal efficiency. The current review aims to provide an overview of the prevention of fungi and mycotoxins in grain through EOs. The antifungal and toxin inhibition efficiency of different EOs and their effective components are investigated. The inhibition mechanism of EOs on fungi and mycotoxins in grains is introduced. The influence of EOs treatment on the change of grain quality is also discussed. In addition, the formulations and techniques used to overcome the disadvantages of EOs application are introduced. The results of recent studies have confirmed that EOs provide great potential for controlling common fungi and mycotoxins in grains, and enhancing quantity and quality safety of grains.

Uptake, transport and accumulation of micro- and nano-plastics in terrestrial plants and health risk associated with their transfer to food chain - A mini review.

Waste plastics enter the environment (water, soil, and atmosphere) and degrade into micro- and nano-plastics (MNPs) through physical, chemical, or biological processes. MNPs are ubiquitous in the environment and inevitably interact with terrestrial plants. Terrestrial plants have become important potential sinks, and subsequently, the sources of MNPs. At present, many studies have reported the effects of MNPs on plant physiology, biochemistry, and their phototoxicity. However, the source, detection method, and the absorption process of MNPs in terrestrial plants have not been systematically studied. In order to better understand the continuous process of MNPs entering terrestrial plants, this review introduces the sources and analysis methods of MNPs in terrestrial plants. The uptake pathways of MNPs in terrestrial plants and their influencing factors were systematically summarized. Meanwhile, the transport pathways and the accumulation of MNPs in different plant organs (roots, stems, leaves, calyxes, and fruits) were explored. Finally, the transfer of MNPs through food chains to humans and their health risks were discussed. The aim of this work is to provide significant theoretical knowledge to understand the uptake, transport, and accumulation of MNPs in terrestrial plants and the potential health risks associated with their transfer to humans through food chain.

Super-resolution reconstruction, recognition, and evaluation of laser confocal images of hyperaccumulator Solanum nigrum endocytosis vesicles based on deep learning: Comparative study of SRGAN and SRResNet.

It is difficult for laser scanning confocal microscopy to obtain high- or ultra-high-resolution laser confocal images directly, which affects the deep mining and use of the embedded information in laser confocal images and forms a technical bottleneck in the in-depth exploration of the microscopic physiological and biochemical processes of plants. The super-resolution reconstruction model (SRGAN), which is based on a generative adversarial network and super-resolution reconstruction model (SRResNet), which is based on a residual network, was used to obtain single and secondary super-resolution reconstruction images of laser confocal images of the root cells of the hyperaccumulator Solanum nigrum. Using the peak signal-to-noise ratio (PSNR), structural similarity (SSIM) and mean opinion score (MOS), the models were evaluated by the image effects after reconstruction and were applied to the recognition of endocytic vesicles in Solanum nigrum root cells. The results showed that the single reconstruction and the secondary reconstruction of SRGAN and SRResNet improved the resolution of laser confocal images. PSNR, SSIM, and MOS were clearly improved, with a maximum PSNR of 47.690. The maximum increment of PSNR and SSIM of the secondary reconstruction images reached 21.7% and 2.8%, respectively, and the objective evaluation of the image quality was good. However, overall MOS was less than that of the single reconstruction, the perceptual quality was weakened, and the time cost was more than 130 times greater. The reconstruction effect of SRResNet was better than that of SRGAN. When SRGAN and SRResNet were used for the recognition of endocytic vesicles in Solanum nigrum root cells, the clarity of the reconstructed images was obviously improved, the boundary of the endocytic vesicles was clearer, and the number of identified endocytic vesicles increased from 6 to 9 and 10, respectively, and the mean fluorescence intensity was enhanced by 14.4% and 7.8%, respectively. Relevant research and achievements are of great significance for promoting the application of deep learning methods and image super-resolution reconstruction technology in laser confocal image studies.

Inhibitory interaction of flavonoids with organic cation transporter 2 and their structure-activity relationships for predicting nephroprotective effects.

Organic cation transporter 2 (OCT2) is mainly responsible for the renal secretion of various cationic drugs, closely associated with drug-induced acute kidney injury (AKI). Screening and identifying potent OCT2 inhibitors with little toxicity in natural products in reducing OCT2-mediated AKI is of great value. Flavonoids are enriched in various vegetables, fruits, and herbal products, and some were reported to produce transporter-mediated drug-drug interactions. This study aimed to screen potential inhibitors of OCT2 from 96 flavonoids, assess the nephroprotective effects on cisplatin-induced kidney injury, and clarify the structure-activity relationships of flavonoids with OCT2. Ten flavonoids exhibited significant inhibition (>50%) on OCT2 in OCT2-HEK293 cells. Among them, the six most potent flavonoid inhibitors, including pectolinarigenin, biochanin A, luteolin, chrysin, 6-hydroxyflavone, and 6-methylflavone markedly decreased cisplatin-induced cytotoxicity. Moreover, in cisplatin-induced renal injury models, they also reduced serum blood urea nitrogen (BUN) and creatinine levels to different degrees, the best of which was 6-methylflavone. The pharmacophore model clarified that the aromatic ring, hydrogen bond acceptors, and hydrogen bond donors might play a vital role in the inhibitory effect of flavonoids on OCT2. Thus, our findings would pave the way to predicting the potential risks of flavonoid-containing food/herb-drug interactions in humans and optimizing flavonoid structure to alleviate OCT2-related AKI.

The characteristics and metabolic potentials of the soil bacterial community of two typical military demolition ranges in China.

The response mechanism of soil microbiota in military polluted sites can effectively indicate the biotoxicity of ammunition. In this study, two military demolition ranges polluted soils of grenades and bullet were collected. According to high-throughput sequencing, after grenade explosion, the dominant bacteria in Site 1 (S1) are Proteobacteria (97.29 %) and Actinobacteria (1.05 %). The dominant bacterium in Site 2 (S2) is Proteobacteria (32.95 %), followed by Actinobacteria (31.17 %). After the military exercise, the soil bacterial diversity index declined significantly, and the bacterial communities interacted more closely. The indigenous bacteria in S1 were influenced more compared to those in S2. According to the environmental factor analysis, the bacteria composition can easily be influenced by heavy metals and organic pollutants, including Cu, Pb, Cr and Trinitrotoluene (TNT). About 269 metabolic pathways annotated in the Kyoto Encyclopedia of Genes and Genomes (KEGG) database were detected in bacterial communities, including nutrition metabolism (C, 4.09 %; N, 1.14 %; S, 0.82 %), external pollutant metabolism (2.52 %) and heavy metal detoxication (2.12 %), respectively. The explosion of ammunition changes the basic metabolism of indigenous bacteria, and heavy metal stress inhibits the TNT degradation ability of bacterial communities. The pollution degree and community structure influence the metal detoxication strategy at the contaminated sites together. Heavy metal ions in S1 are mainly discharged through membrane transporters, while heavy metal ions in S2 are mainly degraded through lipid metabolism and biosynthesis of secondary metabolites. The results obtained in this study can provide deep insight into the response mechanism of the soil bacterial community in military demolition ranges with composite pollutions of heavy metals and organic substances. CAPSULE: Heavy metal stress changed the composition, interaction and metabolism of indigenous communities in military demolition ranges, especially the TNT degradation process.

Inhibitory effects of flavonoids on glucose transporter 1 (GLUT1): From library screening to biological evaluation to structure-activity relationship.

Glucose transporter 1 (GLUT1) is mainly responsible for glucose uptake and energy metabolism, especially in the aerobic glycolysis process of tumor cells, which is closely associated with the advancement of tumors. Numerous studies have demonstrated that the inhibition of GLUT1 can decrease the growth of tumor cells and enhance drug sensitivity, so GLUT1 is considered to be a promising therapeutic target for cancer treatment. Flavonoids are a group of phenolic secondary metabolites present in vegetables, fruits, and herbal products, some of which were reported to increase cancer cells' sensitivity to sorafenib by inhibiting GLUT1. Our objective was to screen potential inhibitors of GLUT1 from 98 flavonoids and assess the sensitizing effect of sorafenib on cancer cells. and illuminate the structure-activity relationships of flavonoids with GLUT1. Eight flavonoids, including apigenin, kaempferol, eupatilin, luteolin, hispidulin, isosinensetin, sinensetin, and nobiletin exhibited significant inhibition (>50%) on GLUT1 in GLUT1-HEK293T cells. Among them, sinensetin and nobiletin showed stronger sensitizing effects and caused a sharp downward shift of the cell viability curves in HepG2 cells, illustrating these two flavonoids might become sensitizers to enhance the efficacy of sorafenib by inhibiting GLUT1. Molecular docking analysis elucidated inhibitory effect of flavonoids on GLUT1 was related to conventional hydrogen bonds, but not Pi interactions. The pharmacophore model clarified the critical pharmacophores of flavonoids inhibitors are hydrophobic groups in 3'positions and hydrogen bond acceptors. Thus, our findings would provide useful information for optimizing flavonoid structure to design novel GLUT1 inhibitors and overcome drug resistance in cancer treatment.

Effect of Sr2+ ions on the structure, up-conversion emission and thermal sensing of Er3+, Yb3+ co-doped double perovskite Ba(2-x)SrxMgWO6 phosphors.

Investigating the effect of different phases on the optical performance is crucial for thermal sensing phosphor materials. Ba(2-x)SrxMgWO6:Er3+, Yb3+, K+ double perovskite phosphors were successfully prepared using a high-temperature solid-phase method. The dominant up-conversion luminescent (UCL) mechanism was deduced by analyzing the power-dependence spectra and energy level diagrams. By X-ray diffraction tests and tolerance factor calculations, it was demonstrated that the substitution of Sr2+ ions for Ba2+ ions led to the phase changing from cubic to tetragonal. The phase transition led to a decrease in the crystallographic symmetry of the compounds and changes in the optical thermometric properties. The optical temperature sensing properties were investigated using the fluorescence intensity ratio of thermally coupled energy levels (2H11/2 and 4S3/2 to the ground state energy level 4I15/2) of Er3+ ions in Ba2MgWO6, BaSrMgWO6 and Sr2MgWO6. The maximum absolute sensitivities obtained for Ba2MgWO6, BaSrMgWO6 and Sr2MgWO6 doped with 7% Er3+, 2% Yb3+ and 9% K+ were 6.77 × 10-4 K-1, 10.09 × 10-4 K-1 and 23.4 × 10-4 K-1, respectively. The comparison revealed that the phase transition caused an increase in the luminescence intensity and absolute sensitivity. This provides a useful pathway for modulating the subsequent thermometric performance.