Zeolite imidazolate framework(ZIF)-derived bimetallic sulfides and layered double hydroxides(LDHs)have emerged as promising electrode materials for supercapacitors,owing to their porous layered structures,high electro...Zeolite imidazolate framework(ZIF)-derived bimetallic sulfides and layered double hydroxides(LDHs)have emerged as promising electrode materials for supercapacitors,owing to their porous layered structures,high electrochemical activity,tun-able molecular architectures,low cost,and high specific capacitance.In this study,a unique composite material comprising ZIF-derived ZnCo bimetallic sulfide and LDH with a honeycomb-like structure was in situ grown on nickel foil(NF)via a con-trolled self-sacrificial template strategy.In contrast to previous reports,the resulting ZnS@Co_(3)S_(4)@MXene@Ni-LDH/NF compos-ite integrates the advantages of MXene,LDH,and sulfides,leading to significantly enhanced conductivity,structural stability,and catalytic activity.The ZnS@Co_(3)S_(4)@MXene@Ni-LDH/NF electrode exhibits a uniform network structure with a thickness of approximately 1μm coated on NF,and delivers a high specific capacitance of 1356.1 F·g^(-1)at a current density of 2 A·g^(-1).Further-more,an asymmetric supercapacitor assembled with ZnS@Co_(3)S_(4)@MXene@Ni-LDH/NF as the positive electrode and activated car-bon as the negative electrode achieves a high energy density of 34.08 Wh·kg^(-1)and a power density of 742.3 W·kg^(-1)at 1 A·g^(-1).This device successfully powers LED lights for 5 min,demonstrating its practical applicability.These results underscore the out-standing electrochemical performance of the ZnS@Co_(3)S_(4)@MXene@Ni-LDH/NF electrode,highlighting its potential for applica-tions in supercapacitors and related energy storage fields.展开更多
Deep learning has made significant progress in the field of oriented object detection for remote sensing images.However,existing methods still face challenges when dealing with difficult tasks such as multi-scale targ...Deep learning has made significant progress in the field of oriented object detection for remote sensing images.However,existing methods still face challenges when dealing with difficult tasks such as multi-scale targets,complex backgrounds,and small objects in remote sensing.Maintaining model lightweight to address resource constraints in remote sensing scenarios while improving task completion for remote sensing tasks remains a research hotspot.Therefore,we propose an enhanced multi-scale feature extraction lightweight network EM-YOLO based on the YOLOv8s architecture,specifically optimized for the characteristics of large target scale variations,diverse orientations,and numerous small objects in remote sensing images.Our innovations lie in two main aspects:First,a dynamic snake convolution(DSC)is introduced into the backbone network to enhance the model’s feature extraction capability for oriented targets.Second,an innovative focusing-diffusion module is designed in the feature fusion neck to effectively integrate multi-scale feature information.Finally,we introduce Layer-Adaptive Sparsity for magnitude-based Pruning(LASP)method to perform lightweight network pruning to better complete tasks in resource-constrained scenarios.Experimental results on the lightweight platform Orin demonstrate that the proposed method significantly outperforms the original YOLOv8s model in oriented remote sensing object detection tasks,and achieves comparable or superior performance to state-of-the-art methods on three authoritative remote sensing datasets(DOTA v1.0,DOTA v1.5,and HRSC2016).展开更多
In recent years,our understanding of photoaging and photoprotection has significantly advanced,with photoaging now widely recognized as a key factor affecting both the health and aesthetic quality of the skin.This pap...In recent years,our understanding of photoaging and photoprotection has significantly advanced,with photoaging now widely recognized as a key factor affecting both the health and aesthetic quality of the skin.This paper explores the underlying mechanisms of skin damage caused by various bands of the light spectrum,along with the classical biological targets associated with photoaging.It proposes innovative strategies for effective photoprotection,including:(1)broadening protection beyond the ultraviolet(UV)spectrum;(2)tailoring sunscreen formulations to match different skin phototypes;and(3)adopting a comprehensive photoprotective approach that integrates prevention,defense,and repair.These strategies offer a theoretical foundation for the development of next-generation photoprotective products,contributing to the mitigation of photoaging and the maintenance of skin health.展开更多
Cerium oxide nanoparticles(CeO_(2)NPs)have attracted great interest recently in the field of cosmetics due to their excellent biomedical properties to treat diseases caused by reactive oxygen species(ROS).However,a re...Cerium oxide nanoparticles(CeO_(2)NPs)have attracted great interest recently in the field of cosmetics due to their excellent biomedical properties to treat diseases caused by reactive oxygen species(ROS).However,a realizable synthesis approach for the large-scale synthesis of CeO_(2)NPs reaching the quality requirements of cosmetic grade is still in desperate demand.This work reports a robust solvothermal approach for the mass production of self-assembled CeO_(2)microsphere(SA CeO_(2))up to 1000 g at a time.Depending on the concentration of initial precursors,the re sulting particle sizes can be precisely tuned to obtain micro spherical samples of SA CeO_(2)-145 nm,SA CeO_(2)-420 nm and SA CeO_(2)-680 nm.Typically,the mesoporous SA CeO_(2)-420 nm with the largest specific surface area exhibits greatly enhanced number of oxygen vacancies(Ce^(3+)cations)proved by X-ray photoelectro n spectro scopy and electron paramagnetic resonance analysis.Moreover,Turbiscan stability test reveals the superior physical stability of SA CeO_(2)-420 nm suspension based on multiple light scattering technology,which contributes to reduced in-vitro cytotoxicity assessed via MTT viability assay.Therefore,SA CeO_(2)-420 nm exhibits excellent antioxidant performance with a high DPPH free radical scavenging ratio of more than 90% at a low concentration below 1 mg/mL.Importantly,SA CeO_(2)-420 nm can effectively inhibit the in-vitro release of reactive oxygen species in mitochondria caused by UVB irradiation in HaCaT cells,exerting good antioxidant activity at the cellular level.As a consequence,a significant increase in skin color and brightness can be observed after 28 d of application of the emulsion containing SA CeO_(2)-420 nm,demonstrating the potential whitening effect.This work provides a facile and readily scalable synthetic strategy of CeO_(2)microsphere and subsequently offers an innovative avenue for their cosmetic application.展开更多
Idiopathic pulmonary fibrosis(IPF)is a progressive lung disease and its incidence rate is rapidly rising.However,effective therapies for the treatment of IPF are still lacking.Phosphodiesterase 4(PDE4)inhibitors were ...Idiopathic pulmonary fibrosis(IPF)is a progressive lung disease and its incidence rate is rapidly rising.However,effective therapies for the treatment of IPF are still lacking.Phosphodiesterase 4(PDE4)inhibitors were reported to be potential anti-fibrotic agents.Herein,structure-based hit-to-lead optimization of natural isoaurostatin(8.98μmol/L)resulted in several potent inhibitors of PDE4 with half maximal inhibitory concentration(IC_(50))values ranging from 35 nmol/L to 126 nmol/L.Co-crystal structures revealed that isoaurostatin compounds exhibited different binding patterns from the classic PDE4 inhibitor rolipram and the analogues would favor to be Z configurations other than the corresponding E isomers.Finally,lead 2–9 showed remarkable in vitro/in vivo anti-fibrotic effects indicating its potential as a novel anti-IPF agent.展开更多
The purpose of this study was to prepare glycyrrhizic acid nanoliposomes and evaluate the encapsulation efficiency and other properties of glycyrrhizic acid nanoliposomes, which would provide a reference for further r...The purpose of this study was to prepare glycyrrhizic acid nanoliposomes and evaluate the encapsulation efficiency and other properties of glycyrrhizic acid nanoliposomes, which would provide a reference for further research on Glycyrrhizic Acid in the treatment of liver diseases. Firstly, the preparation conditions of glycyrrhizic acid liposomes were optimized by the orthogonal design method. Then, glycyrrhizic acid liposomes were prepared by ultrasonic-film dispersion method and the encapsulation efficiency was determined by the HPLC method. Finally, the properties of glycyrrhizic acid nanoliposomes were also studied. The results showed that the optimal preparation conditions of liposomes were as follows: the ratio of drug to lipid was 1:30;Lecithin: cholesterol = 1:1;Hydration medium: pure water;Ultrasonic time: 120 s. The encapsulation efficiency of liposomes was about 90%. The final liposomes were round and uniform in distribution, with an average particle size of about 50 nm and absolute zeta potential of −28.9 mV. In this study, glycyrrhizic acid liposomes were prepared and the optimal preparation conditions were optimized. The encapsulation efficiency of the liposomes under the optimized conditions was determined. The evaluation of the morphology, size, particle size and stability of the liposomes was completed.展开更多
Phospholipids have the characteristics of excellent biocompatibility and a especial amphiphilicity.These unique properties make phospholipids most appropriate to be employed as important pharmaceutical excipients and ...Phospholipids have the characteristics of excellent biocompatibility and a especial amphiphilicity.These unique properties make phospholipids most appropriate to be employed as important pharmaceutical excipients and they have a very wide range of applications in drug delivery systems.The aim of this review is to summarize phospholipids and some of their related applications in drug delivery systems,and highlight the relationship between the properties and applications,and the effect of the species of phospholipids on the efficiency of drug delivery.We refer to some relevant literatures,starting from the structures,main sources and properties of phospholipids to introduce their applications in drug delivery systems.The present article focuses on introducing five types of carriers based on phospholipids,including liposomes,intravenous lipid emulsions,micelles,drug-phospholipids complexes and cochleates.展开更多
The glymphatic system plays a pivotal role in maintaining cerebral homeostasis.Chronic cerebral hypoperfusion,arising from small vessel disease or carotid stenosis,results in cerebrometabolic disturbances ultimately m...The glymphatic system plays a pivotal role in maintaining cerebral homeostasis.Chronic cerebral hypoperfusion,arising from small vessel disease or carotid stenosis,results in cerebrometabolic disturbances ultimately manifesting in white matter injury and cognitive dysfunction.However,whether the glymphatic system serves as a potential therapeutic target for white matter injury and cognitive decline during hypoperfusion remains unknown.Here,we established a mouse model of chronic cerebral hypoperfusion via bilateral common carotid artery stenosis.We found that the hypoperfusion model was associated with significant white matter injury and initial cognitive impairment in conjunction with impaired glym・phatic system function.The glymphatic dysfunction was associated with altered cerebral perfusion and loss of aquaporin 4 polarization.Treatment of digoxin rescued changes in glymphatic transport,white matter structure,and cognitive function.Suppression of glymphatic functions by treatment with the AQP4 inhibitor TGN-020 abolished this protective effect of digoxin from hypoperfusion injury.Our research yields new insight into the relationship between hemodynamics,glymphatic transport,white matter injury,and cognitive changes after chronic cerebral hypoperfusion.展开更多
Although active constituents extracted from plants show robust in vitro pharmacological effects, low in vivo absorption greatly limits the widespread application of these compounds. A strategy of using phyto-phospholi...Although active constituents extracted from plants show robust in vitro pharmacological effects, low in vivo absorption greatly limits the widespread application of these compounds. A strategy of using phyto-phospholipid complexes represents a promising approach to increase the oral bioavailability of active constituents, which is consist of ‘‘label-friendly'phospholipids and active constituents. Hydrogen bond interactions between active constituents and phospholipids enable phospholipid complexes as an integral part. This review provides an update on four important issues related to phyto-phospholipid complexes: active constituents, phospholipids, solvents, and stoichiometric ratios. We also discuss recent progress in research on the preparation, characterization, structural verification, and increased bioavailability of phyto-phospholipid complexes.展开更多
This paper presents an experimental investigation on the effect of protrusion radial position and height on the sealing performance and flow structure in the rotor-stator cavity. The rotormounted protrusions are assem...This paper presents an experimental investigation on the effect of protrusion radial position and height on the sealing performance and flow structure in the rotor-stator cavity. The rotormounted protrusions are assembled at three radial positions and are set to three heights. The cavity is equipped with three rim seals: a radial seal, an axial seal and a seal with double fins on the stator.The annulus Reynolds number is set at 4:39 ×10;and the rotational Reynolds number ranges from 7:51×10;to 1:20×10;. Heat and mass transfer analogy is applied. Pressure and CO;concentration are measured. The experimental results show that in cavities with different rim seals, radial distributions of the sealing efficiency, pressure and swirl ratio are basically the same. The sealing performance is improved by protrusions compared with the cavity without protrusion and improves with the increase of protrusion radial position and height. The effect of protrusion increases with the increase of the rotational Reynolds number. The windage loss and the flow resistance introduced by protrusions are investigated. It is found that induced windage loss and flow resistance decrease with the increase of protrusion radial position but increase with the protrusion height.展开更多
Rho-associated kinase（ROCK） is a key regulatory protein involved in inflammatory secretion in microglia in the central nervous system.Our previous studies showed that ROCK inhibition enhances phagocytic activity in ...Rho-associated kinase（ROCK） is a key regulatory protein involved in inflammatory secretion in microglia in the central nervous system.Our previous studies showed that ROCK inhibition enhances phagocytic activity in microglia through the extracellular signal-regulated kinase（ERK） signaling pathway,but its effect on microglial migration was unknown.Therefore,in this study,we investigated the effects of the ROCK inhibitors Y27632 and fasudil on the migratory activity of primary cultured microglia isolated from the spinal cord,and we examined the underlying mechanisms.The microglia were treated with Y27632,fasudil and/or the ERK inhibitor U0126.Cellular morphology was observed by immunofluorescence.Transwell chambers were used to assess cell migration.ERK levels were measured by incell western blot assay.Y27632 and fasudil increased microglial migration,and the microglia were irregularly shaped and had many small processes.These inhibitors also upregulated the levels of phosphorylated ERK protein.The ERK inhibitor U0126 suppressed these effects of Y27632 and fasudil.These findings suggest that the ROCK inhibitors Y27632 and fasudil promote microglial migration in the spinal cord through the ERK signaling pathway.展开更多
In this paper, the effect of different amount of protrusion on various parameters in rotor–stator system was experimentally studied by measuring CO_2 concentration and pressure, in order to obtain the optimal protrus...In this paper, the effect of different amount of protrusion on various parameters in rotor–stator system was experimentally studied by measuring CO_2 concentration and pressure, in order to obtain the optimal protrusion amount.The parameters of different dimensionless sealing flow were measured under the condition that the annulus Reynolds number was 4.39 × 10~5 and the rotating Reynolds number was 1.05 × 10~6.The results show that the change of the amount of protrusions has little effect on the static pressure in the cavity, and the static pressure change near the sealing ring is almost negligible.But the total pressure and sealing efficiency increase first and then decrease with the increase of the amount of protrusion.The variation of power consumption is the same.A complex vortex structure will appear at the high radius region when the protrusion is installed.On the other hand, the protrusion can effectively reduce the minimum sealing flow of the rotor–stator cavity.Furthermore, considering the sealing efficiency and power consumption,the best range of the protrusion amount is about 36.The ratio near this range can optimally balance the alleviation of the gas ingestion and the reduction of the power consumption.展开更多
The windage loss caused by protrusion in a rotor–stator cavity has been studied in detail,and there are abundant fitting formulas that have been summarized to calculate the moment coefficients.Some other theorists ha...The windage loss caused by protrusion in a rotor–stator cavity has been studied in detail,and there are abundant fitting formulas that have been summarized to calculate the moment coefficients.Some other theorists have emphasized its effect on the sealing efficiency,proposing that installation of protrusion could alleviate gas ingestion.However,the protrusion shape which is an influential factor on the sealing efficiency has not been focused in previous research.Using the experimental method of measuring CO2 volume fraction,cavity pressure,and power consumption,we investigated the effects of several typical protrusion shapes on various parameters for two sealing structures,in order to obtain the optimal shape.Results showed that a variation of the protrusion shape had little impact on the static pressure,but the total pressure and the sealing efficiency increased in different degrees.Furthermore,even though the hexagon shape resulted in the highest sealing efficiency,we observed that the drop shape had the best overall performance in all of the eight models,which could result in higher efficiency of the turbine cavity.The combination of a radial seal structure and protrusion could improve sealing efficiency better.展开更多
PEGylated liposomes are potential candidates to improve the pharmacokinetic characteristics of encapsulated drugs, to extend their circulation half-life and facilitate their passive accumulation at tumour sites. Howev...PEGylated liposomes are potential candidates to improve the pharmacokinetic characteristics of encapsulated drugs, to extend their circulation half-life and facilitate their passive accumulation at tumour sites. However, PEG-modified liposomes can induce accelerated blood clearance(ABC) upon repeated administration, and the extent of ABC phenomenon on the cytotoxic drugs-containing PEGylated liposomes is related to the dose of the cytotoxic drugs.In this study, EPI served as a model cytotoxic drug, a hydrophilic surfactant molecule,monosialylganglioside(GM1) was chosen and modified on the liposomes together with PEG.It was shown that upon mixed modification, when GM1 contents reached 10% or 15% mol,the ABC phenomenon of the PEGylated liposomal EPI significantly reduced. We also found that GM1 played an important role in abrogating the ABC phenomenon in both the induction phase and the effectuation phase. The results suggested that GM1 incorporation unfortunately did not avoid occurrence of ABC phenomenon completely, but GM1 modification on PEGylated liposomes may provide a significant improvement in clinical practice of PEGylated liposomes. Further study must be necessary.展开更多
The properties of modified biomaterial are gaining more and more importance in drug delivery systems.Sialic acid(SA)and polysialic acid(PSA)serve as endogenous substances,which are non-immunogenic and biodegradable.At...The properties of modified biomaterial are gaining more and more importance in drug delivery systems.Sialic acid(SA)and polysialic acid(PSA)serve as endogenous substances,which are non-immunogenic and biodegradable.At the same time,SA modification of the drugs/carriers can enhance the uptake of tumor cell and retention in brain;PSA modifi-cation can reduce the immunogenicity of the proteins or polypeptides and increase circulation time of the modified drugs/carriers in the blood,thus achieving active targeting effect.These properties offer a variety of opportunities for applications in drug delivery systems.This article summarizes the biological functions of SA and PSA and presents the technologies of SA/PSA modified small molecule drugs,proteins and carriers in drug delivery systems.展开更多
Grey matter(GM)alterations may contribute to cognitive decline in individuals with white matter hyperintensities(WMH)but no consensus has yet emerged.Here,we investigated cortical thickness and grey matter volume in 2...Grey matter(GM)alterations may contribute to cognitive decline in individuals with white matter hyperintensities(WMH)but no consensus has yet emerged.Here,we investigated cortical thickness and grey matter volume in 23 WMH patients with mild cognitive impairment(WMH-MCI),43 WMH patients without cognitive impairment,and 55 healthy controls.Both WMH groups showed GM atrophy in the bilateral thalamus,fronto-insular cortices,and several parietal-temporal regions,and the WMH-MCI group showed more extensive and severe GM atrophy.The GM atrophy in the thalamus and fronto-insular cortices was associated with cognitive decline in the WMH-MCI patients and may mediate the relationship between WMH and cognition in WMH patients.Furthermore,the main results were well replicated in an independent dataset from the Alzheimer's Disease Neuroimaging Initiative database and in other control analyses.These comprehensive results provide robust evidence of specific GM alterations underlying WMH and subsequent cognitive impairment.展开更多
The aim of the study was to prepare berberine hydrochloride long-circulating liposomes and optimize the formulation and process parameters,and investigate the influence of different factors on the encapsulation effici...The aim of the study was to prepare berberine hydrochloride long-circulating liposomes and optimize the formulation and process parameters,and investigate the influence of different factors on the encapsulation efficiency.Berberine hydrochloride liposomes were prepared in response to a transmembrane ion gradient that was established by ionophore A23187.Free and liposomal drug were separated by cation exchange resin,and then the amount of intraliposomal berberine hydrochloride was determined by UV spectrophotometry.The optimized encapsulation efficiency of berberine hydrochloride liposomes was 94.3%2.1%when the drug-to-lipid ratio was 1:20,and the mean diameter was 146.9 nm3.2 nm.As a result,the ionophore A23187-mediated ZnSO_(4)gradient method was suitable for the preparation of berberine hydrochloride liposomes that we could get the desired encapsulation efficiency and drug loading.展开更多
Microglia are immunocompetent cells in the cen- tral nervous system that take up tissue debris and pathogens. Rho-associated kinase （ROCK） has been identified as an important regulator of uptake, proliferation, secr...Microglia are immunocompetent cells in the cen- tral nervous system that take up tissue debris and pathogens. Rho-associated kinase （ROCK） has been identified as an important regulator of uptake, proliferation, secretion, and differentiation in a number of cell types. Although ROCK plays critical roles in the microglial secretion of inflammatory factors, naigration, and morphology, its effects on microglial uptake activity have not been well characterized. In the present study, we found that treatment of BV2 microglia and primary microglia with the ROCK inhibitors Y27632 and fasudil increased uptake activity and was associated with morpholog- ical changes. Furthermore, western blots showed that this increase in uptake activity was mediated through the extracel- lular-signal-regulated kinase （ERK） signaling cascade, indi- cating the importance of ROCK in regulating microglial uptake activity.展开更多
基金support by NSFC(No.61704047)Natural Science Foundation of Henan Province(No.242300420271)Key Research Project of Henan Provincial Higher Education(No.24A430008).
文摘Zeolite imidazolate framework(ZIF)-derived bimetallic sulfides and layered double hydroxides(LDHs)have emerged as promising electrode materials for supercapacitors,owing to their porous layered structures,high electrochemical activity,tun-able molecular architectures,low cost,and high specific capacitance.In this study,a unique composite material comprising ZIF-derived ZnCo bimetallic sulfide and LDH with a honeycomb-like structure was in situ grown on nickel foil(NF)via a con-trolled self-sacrificial template strategy.In contrast to previous reports,the resulting ZnS@Co_(3)S_(4)@MXene@Ni-LDH/NF compos-ite integrates the advantages of MXene,LDH,and sulfides,leading to significantly enhanced conductivity,structural stability,and catalytic activity.The ZnS@Co_(3)S_(4)@MXene@Ni-LDH/NF electrode exhibits a uniform network structure with a thickness of approximately 1μm coated on NF,and delivers a high specific capacitance of 1356.1 F·g^(-1)at a current density of 2 A·g^(-1).Further-more,an asymmetric supercapacitor assembled with ZnS@Co_(3)S_(4)@MXene@Ni-LDH/NF as the positive electrode and activated car-bon as the negative electrode achieves a high energy density of 34.08 Wh·kg^(-1)and a power density of 742.3 W·kg^(-1)at 1 A·g^(-1).This device successfully powers LED lights for 5 min,demonstrating its practical applicability.These results underscore the out-standing electrochemical performance of the ZnS@Co_(3)S_(4)@MXene@Ni-LDH/NF electrode,highlighting its potential for applica-tions in supercapacitors and related energy storage fields.
基金funded by the Hainan Province Science and Technology Special Fund under Grant ZDYF2024GXJS292.
文摘Deep learning has made significant progress in the field of oriented object detection for remote sensing images.However,existing methods still face challenges when dealing with difficult tasks such as multi-scale targets,complex backgrounds,and small objects in remote sensing.Maintaining model lightweight to address resource constraints in remote sensing scenarios while improving task completion for remote sensing tasks remains a research hotspot.Therefore,we propose an enhanced multi-scale feature extraction lightweight network EM-YOLO based on the YOLOv8s architecture,specifically optimized for the characteristics of large target scale variations,diverse orientations,and numerous small objects in remote sensing images.Our innovations lie in two main aspects:First,a dynamic snake convolution(DSC)is introduced into the backbone network to enhance the model’s feature extraction capability for oriented targets.Second,an innovative focusing-diffusion module is designed in the feature fusion neck to effectively integrate multi-scale feature information.Finally,we introduce Layer-Adaptive Sparsity for magnitude-based Pruning(LASP)method to perform lightweight network pruning to better complete tasks in resource-constrained scenarios.Experimental results on the lightweight platform Orin demonstrate that the proposed method significantly outperforms the original YOLOv8s model in oriented remote sensing object detection tasks,and achieves comparable or superior performance to state-of-the-art methods on three authoritative remote sensing datasets(DOTA v1.0,DOTA v1.5,and HRSC2016).
文摘In recent years,our understanding of photoaging and photoprotection has significantly advanced,with photoaging now widely recognized as a key factor affecting both the health and aesthetic quality of the skin.This paper explores the underlying mechanisms of skin damage caused by various bands of the light spectrum,along with the classical biological targets associated with photoaging.It proposes innovative strategies for effective photoprotection,including:(1)broadening protection beyond the ultraviolet(UV)spectrum;(2)tailoring sunscreen formulations to match different skin phototypes;and(3)adopting a comprehensive photoprotective approach that integrates prevention,defense,and repair.These strategies offer a theoretical foundation for the development of next-generation photoprotective products,contributing to the mitigation of photoaging and the maintenance of skin health.
基金Project supported by the National Natural Science Foundation of China(22301012)the R&D Program of Beijing Municipal Education Commission(KM202310011005)。
文摘Cerium oxide nanoparticles(CeO_(2)NPs)have attracted great interest recently in the field of cosmetics due to their excellent biomedical properties to treat diseases caused by reactive oxygen species(ROS).However,a realizable synthesis approach for the large-scale synthesis of CeO_(2)NPs reaching the quality requirements of cosmetic grade is still in desperate demand.This work reports a robust solvothermal approach for the mass production of self-assembled CeO_(2)microsphere(SA CeO_(2))up to 1000 g at a time.Depending on the concentration of initial precursors,the re sulting particle sizes can be precisely tuned to obtain micro spherical samples of SA CeO_(2)-145 nm,SA CeO_(2)-420 nm and SA CeO_(2)-680 nm.Typically,the mesoporous SA CeO_(2)-420 nm with the largest specific surface area exhibits greatly enhanced number of oxygen vacancies(Ce^(3+)cations)proved by X-ray photoelectro n spectro scopy and electron paramagnetic resonance analysis.Moreover,Turbiscan stability test reveals the superior physical stability of SA CeO_(2)-420 nm suspension based on multiple light scattering technology,which contributes to reduced in-vitro cytotoxicity assessed via MTT viability assay.Therefore,SA CeO_(2)-420 nm exhibits excellent antioxidant performance with a high DPPH free radical scavenging ratio of more than 90% at a low concentration below 1 mg/mL.Importantly,SA CeO_(2)-420 nm can effectively inhibit the in-vitro release of reactive oxygen species in mitochondria caused by UVB irradiation in HaCaT cells,exerting good antioxidant activity at the cellular level.As a consequence,a significant increase in skin color and brightness can be observed after 28 d of application of the emulsion containing SA CeO_(2)-420 nm,demonstrating the potential whitening effect.This work provides a facile and readily scalable synthetic strategy of CeO_(2)microsphere and subsequently offers an innovative avenue for their cosmetic application.
基金supported by the Natural Science Foundation of China(Nos.22277019,82150204,22307031,22377023,22077143,and 82003594)Key Project of Guangdong Natural Science Foundation(No.2016A030311033)+2 种基金Fundamental Research Funds for Hainan University(Nos.KYQD(ZR)-21031,KYQD(ZR)-21108,KYQD(ZR)-23003,and XTCX2022JKA01)Guangdong Provincial Key Laboratory of Construction Foundation(No.2023B1212060022)Science Foundation of Hainan Province(Nos.KJRC2023B10,824YXQN420,and 324MS018)。
文摘Idiopathic pulmonary fibrosis(IPF)is a progressive lung disease and its incidence rate is rapidly rising.However,effective therapies for the treatment of IPF are still lacking.Phosphodiesterase 4(PDE4)inhibitors were reported to be potential anti-fibrotic agents.Herein,structure-based hit-to-lead optimization of natural isoaurostatin(8.98μmol/L)resulted in several potent inhibitors of PDE4 with half maximal inhibitory concentration(IC_(50))values ranging from 35 nmol/L to 126 nmol/L.Co-crystal structures revealed that isoaurostatin compounds exhibited different binding patterns from the classic PDE4 inhibitor rolipram and the analogues would favor to be Z configurations other than the corresponding E isomers.Finally,lead 2–9 showed remarkable in vitro/in vivo anti-fibrotic effects indicating its potential as a novel anti-IPF agent.
文摘The purpose of this study was to prepare glycyrrhizic acid nanoliposomes and evaluate the encapsulation efficiency and other properties of glycyrrhizic acid nanoliposomes, which would provide a reference for further research on Glycyrrhizic Acid in the treatment of liver diseases. Firstly, the preparation conditions of glycyrrhizic acid liposomes were optimized by the orthogonal design method. Then, glycyrrhizic acid liposomes were prepared by ultrasonic-film dispersion method and the encapsulation efficiency was determined by the HPLC method. Finally, the properties of glycyrrhizic acid nanoliposomes were also studied. The results showed that the optimal preparation conditions of liposomes were as follows: the ratio of drug to lipid was 1:30;Lecithin: cholesterol = 1:1;Hydration medium: pure water;Ultrasonic time: 120 s. The encapsulation efficiency of liposomes was about 90%. The final liposomes were round and uniform in distribution, with an average particle size of about 50 nm and absolute zeta potential of −28.9 mV. In this study, glycyrrhizic acid liposomes were prepared and the optimal preparation conditions were optimized. The encapsulation efficiency of the liposomes under the optimized conditions was determined. The evaluation of the morphology, size, particle size and stability of the liposomes was completed.
文摘Phospholipids have the characteristics of excellent biocompatibility and a especial amphiphilicity.These unique properties make phospholipids most appropriate to be employed as important pharmaceutical excipients and they have a very wide range of applications in drug delivery systems.The aim of this review is to summarize phospholipids and some of their related applications in drug delivery systems,and highlight the relationship between the properties and applications,and the effect of the species of phospholipids on the efficiency of drug delivery.We refer to some relevant literatures,starting from the structures,main sources and properties of phospholipids to introduce their applications in drug delivery systems.The present article focuses on introducing five types of carriers based on phospholipids,including liposomes,intravenous lipid emulsions,micelles,drug-phospholipids complexes and cochleates.
基金supported by Grants from the National Natural Science Foundation of China(81873749 and 81801072)。
文摘The glymphatic system plays a pivotal role in maintaining cerebral homeostasis.Chronic cerebral hypoperfusion,arising from small vessel disease or carotid stenosis,results in cerebrometabolic disturbances ultimately manifesting in white matter injury and cognitive dysfunction.However,whether the glymphatic system serves as a potential therapeutic target for white matter injury and cognitive decline during hypoperfusion remains unknown.Here,we established a mouse model of chronic cerebral hypoperfusion via bilateral common carotid artery stenosis.We found that the hypoperfusion model was associated with significant white matter injury and initial cognitive impairment in conjunction with impaired glym・phatic system function.The glymphatic dysfunction was associated with altered cerebral perfusion and loss of aquaporin 4 polarization.Treatment of digoxin rescued changes in glymphatic transport,white matter structure,and cognitive function.Suppression of glymphatic functions by treatment with the AQP4 inhibitor TGN-020 abolished this protective effect of digoxin from hypoperfusion injury.Our research yields new insight into the relationship between hemodynamics,glymphatic transport,white matter injury,and cognitive changes after chronic cerebral hypoperfusion.
文摘Although active constituents extracted from plants show robust in vitro pharmacological effects, low in vivo absorption greatly limits the widespread application of these compounds. A strategy of using phyto-phospholipid complexes represents a promising approach to increase the oral bioavailability of active constituents, which is consist of ‘‘label-friendly'phospholipids and active constituents. Hydrogen bond interactions between active constituents and phospholipids enable phospholipid complexes as an integral part. This review provides an update on four important issues related to phyto-phospholipid complexes: active constituents, phospholipids, solvents, and stoichiometric ratios. We also discuss recent progress in research on the preparation, characterization, structural verification, and increased bioavailability of phyto-phospholipid complexes.
文摘This paper presents an experimental investigation on the effect of protrusion radial position and height on the sealing performance and flow structure in the rotor-stator cavity. The rotormounted protrusions are assembled at three radial positions and are set to three heights. The cavity is equipped with three rim seals: a radial seal, an axial seal and a seal with double fins on the stator.The annulus Reynolds number is set at 4:39 ×10;and the rotational Reynolds number ranges from 7:51×10;to 1:20×10;. Heat and mass transfer analogy is applied. Pressure and CO;concentration are measured. The experimental results show that in cavities with different rim seals, radial distributions of the sealing efficiency, pressure and swirl ratio are basically the same. The sealing performance is improved by protrusions compared with the cavity without protrusion and improves with the increase of protrusion radial position and height. The effect of protrusion increases with the increase of the rotational Reynolds number. The windage loss and the flow resistance introduced by protrusions are investigated. It is found that induced windage loss and flow resistance decrease with the increase of protrusion radial position but increase with the protrusion height.
基金supported by the National Natural Science Foundation of China,No.81471200,81771341
文摘Rho-associated kinase（ROCK） is a key regulatory protein involved in inflammatory secretion in microglia in the central nervous system.Our previous studies showed that ROCK inhibition enhances phagocytic activity in microglia through the extracellular signal-regulated kinase（ERK） signaling pathway,but its effect on microglial migration was unknown.Therefore,in this study,we investigated the effects of the ROCK inhibitors Y27632 and fasudil on the migratory activity of primary cultured microglia isolated from the spinal cord,and we examined the underlying mechanisms.The microglia were treated with Y27632,fasudil and/or the ERK inhibitor U0126.Cellular morphology was observed by immunofluorescence.Transwell chambers were used to assess cell migration.ERK levels were measured by incell western blot assay.Y27632 and fasudil increased microglial migration,and the microglia were irregularly shaped and had many small processes.These inhibitors also upregulated the levels of phosphorylated ERK protein.The ERK inhibitor U0126 suppressed these effects of Y27632 and fasudil.These findings suggest that the ROCK inhibitors Y27632 and fasudil promote microglial migration in the spinal cord through the ERK signaling pathway.
文摘In this paper, the effect of different amount of protrusion on various parameters in rotor–stator system was experimentally studied by measuring CO_2 concentration and pressure, in order to obtain the optimal protrusion amount.The parameters of different dimensionless sealing flow were measured under the condition that the annulus Reynolds number was 4.39 × 10~5 and the rotating Reynolds number was 1.05 × 10~6.The results show that the change of the amount of protrusions has little effect on the static pressure in the cavity, and the static pressure change near the sealing ring is almost negligible.But the total pressure and sealing efficiency increase first and then decrease with the increase of the amount of protrusion.The variation of power consumption is the same.A complex vortex structure will appear at the high radius region when the protrusion is installed.On the other hand, the protrusion can effectively reduce the minimum sealing flow of the rotor–stator cavity.Furthermore, considering the sealing efficiency and power consumption,the best range of the protrusion amount is about 36.The ratio near this range can optimally balance the alleviation of the gas ingestion and the reduction of the power consumption.
文摘The windage loss caused by protrusion in a rotor–stator cavity has been studied in detail,and there are abundant fitting formulas that have been summarized to calculate the moment coefficients.Some other theorists have emphasized its effect on the sealing efficiency,proposing that installation of protrusion could alleviate gas ingestion.However,the protrusion shape which is an influential factor on the sealing efficiency has not been focused in previous research.Using the experimental method of measuring CO2 volume fraction,cavity pressure,and power consumption,we investigated the effects of several typical protrusion shapes on various parameters for two sealing structures,in order to obtain the optimal shape.Results showed that a variation of the protrusion shape had little impact on the static pressure,but the total pressure and the sealing efficiency increased in different degrees.Furthermore,even though the hexagon shape resulted in the highest sealing efficiency,we observed that the drop shape had the best overall performance in all of the eight models,which could result in higher efficiency of the turbine cavity.The combination of a radial seal structure and protrusion could improve sealing efficiency better.
基金supported by the National Natural Science Foundation of China (Grant No.81373334)
文摘PEGylated liposomes are potential candidates to improve the pharmacokinetic characteristics of encapsulated drugs, to extend their circulation half-life and facilitate their passive accumulation at tumour sites. However, PEG-modified liposomes can induce accelerated blood clearance(ABC) upon repeated administration, and the extent of ABC phenomenon on the cytotoxic drugs-containing PEGylated liposomes is related to the dose of the cytotoxic drugs.In this study, EPI served as a model cytotoxic drug, a hydrophilic surfactant molecule,monosialylganglioside(GM1) was chosen and modified on the liposomes together with PEG.It was shown that upon mixed modification, when GM1 contents reached 10% or 15% mol,the ABC phenomenon of the PEGylated liposomal EPI significantly reduced. We also found that GM1 played an important role in abrogating the ABC phenomenon in both the induction phase and the effectuation phase. The results suggested that GM1 incorporation unfortunately did not avoid occurrence of ABC phenomenon completely, but GM1 modification on PEGylated liposomes may provide a significant improvement in clinical practice of PEGylated liposomes. Further study must be necessary.
基金the National Natural Science Foundation of China(Grant No.81373334).
文摘The properties of modified biomaterial are gaining more and more importance in drug delivery systems.Sialic acid(SA)and polysialic acid(PSA)serve as endogenous substances,which are non-immunogenic and biodegradable.At the same time,SA modification of the drugs/carriers can enhance the uptake of tumor cell and retention in brain;PSA modifi-cation can reduce the immunogenicity of the proteins or polypeptides and increase circulation time of the modified drugs/carriers in the blood,thus achieving active targeting effect.These properties offer a variety of opportunities for applications in drug delivery systems.This article summarizes the biological functions of SA and PSA and presents the technologies of SA/PSA modified small molecule drugs,proteins and carriers in drug delivery systems.
基金This work was supported by the National Natural Science Foundation of China(81801146,81871438,and 81771341)the Natural Science Foundation of Hubei Province(2017CFB392)+2 种基金Beijing Natural Science Funds for Distinguished Young Scholars(JQ200036)the Flagship Program of Tongji Hospital,China(2019CR106).Data collection and sharing for this project was funded by the Alzheimer's Disease Neuroimaging Initiative(ADNI)(National Institutes of Health Grant U01 AG024904)DOD ADNI(Department of Defense Award number W81XWH-12-2-0012).
文摘Grey matter(GM)alterations may contribute to cognitive decline in individuals with white matter hyperintensities(WMH)but no consensus has yet emerged.Here,we investigated cortical thickness and grey matter volume in 23 WMH patients with mild cognitive impairment(WMH-MCI),43 WMH patients without cognitive impairment,and 55 healthy controls.Both WMH groups showed GM atrophy in the bilateral thalamus,fronto-insular cortices,and several parietal-temporal regions,and the WMH-MCI group showed more extensive and severe GM atrophy.The GM atrophy in the thalamus and fronto-insular cortices was associated with cognitive decline in the WMH-MCI patients and may mediate the relationship between WMH and cognition in WMH patients.Furthermore,the main results were well replicated in an independent dataset from the Alzheimer's Disease Neuroimaging Initiative database and in other control analyses.These comprehensive results provide robust evidence of specific GM alterations underlying WMH and subsequent cognitive impairment.
文摘The aim of the study was to prepare berberine hydrochloride long-circulating liposomes and optimize the formulation and process parameters,and investigate the influence of different factors on the encapsulation efficiency.Berberine hydrochloride liposomes were prepared in response to a transmembrane ion gradient that was established by ionophore A23187.Free and liposomal drug were separated by cation exchange resin,and then the amount of intraliposomal berberine hydrochloride was determined by UV spectrophotometry.The optimized encapsulation efficiency of berberine hydrochloride liposomes was 94.3%2.1%when the drug-to-lipid ratio was 1:20,and the mean diameter was 146.9 nm3.2 nm.As a result,the ionophore A23187-mediated ZnSO_(4)gradient method was suitable for the preparation of berberine hydrochloride liposomes that we could get the desired encapsulation efficiency and drug loading.
基金supported by grants from the National Natural Science Foundation of China(81471200 and81000521)the National Basic Research Development Program of China(2011CB504403)
文摘Microglia are immunocompetent cells in the cen- tral nervous system that take up tissue debris and pathogens. Rho-associated kinase （ROCK） has been identified as an important regulator of uptake, proliferation, secretion, and differentiation in a number of cell types. Although ROCK plays critical roles in the microglial secretion of inflammatory factors, naigration, and morphology, its effects on microglial uptake activity have not been well characterized. In the present study, we found that treatment of BV2 microglia and primary microglia with the ROCK inhibitors Y27632 and fasudil increased uptake activity and was associated with morpholog- ical changes. Furthermore, western blots showed that this increase in uptake activity was mediated through the extracel- lular-signal-regulated kinase （ERK） signaling cascade, indi- cating the importance of ROCK in regulating microglial uptake activity.
