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1.
Int J Biol Macromol ; 265(Pt 2): 130795, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38492696

RESUMO

The utilization of biomass-based conductive polymer hydrogels in wearable electronics holds great promise for advancing performance and sustainability. An interpenetrating network of polyacrylamide/2-hydroxypropyltrimethyl ammonium chloride chitosan (PAM/HACC) was firstly obtained through thermal-initiation polymerization of AM monomers in the presence of HACC. The positively charged groups on HACC provide strong electrostatic interactions and hydrogen bonding with the PAM polymer chains, leading to improved mechanical strength and stability of the hydrogel network. Subsequently, the PAM/HACC networks served as the skeletons for the in-situ polymerization of polypyrrole (PPy), and then the resulting conductive hydrogel demonstrated stable electromagnetic shielding performance (40 dB), high sensitivity for strain sensing (gauge factor = 2.56). Moreover, the incorporation of quaternary ammonium chitosan into PAM hydrogels enhances their antimicrobial activity, making them more suitable for applications in bacterial contamination or low-temperature environments. This conductive hydrogel, with its versatility and excellent mechanical properties, shows great potential in applications such as electronic skin and flexible/wearable electronics.


Assuntos
Resinas Acrílicas , Compostos de Amônio , Quitosana/análogos & derivados , Compostos de Amônio Quaternário , Polímeros , Pirróis , Antibacterianos/farmacologia , Condutividade Elétrica , Hidrogéis
2.
Adv Mater ; 36(16): e2311817, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38226720

RESUMO

Transparent bulk glass is highly demanded in devices and components of daily life to transmit light and protect against external temperature and mechanical hazards. However, the application of glass is impeded by its poor functional performance, especially in terms of thermal isolation and impact resistance. Here, a glass composite integrating the nacre-inspired structure and shear stiffening gel (SSG) material is proposed. Benefiting from the combination of these two elements, this nacre-inspired SSG/glass composite (NSG) exhibits superior thermal insulation and impact resistance while maintaining transparency simultaneously. Specifically, the low thermal conductivity of the SSG combined with the anisotropic heat transfer capability of the nacre-inspired structure enhances the out-of-plane thermal insulation of NSG. The deformations over large volumes in nacre-inspired facesheets promote the deformation region of the SSG core, synergistic effect of tablet sliding mechanism in nacre-inspired structure and strain-rate enhancement in SSG material cause the superior impact resistance of overall panels in a wide range of impact velocities. NSG demonstrates outstanding properties such as transparency, light weight, impact resistance, and thermal insulation, which are major concerns for the application in engineering fields. In conclusion, this bioinspired SSG/glass composite opens new avenues to achieve comprehensive performance improvements for transparent structural materials.

3.
Oncol Lett ; 26(3): 412, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37614658

RESUMO

[This corrects the article DOI: 10.3892/ol.2015.3336.].

4.
Plants (Basel) ; 12(11)2023 May 24.
Artigo em Inglês | MEDLINE | ID: mdl-37299065

RESUMO

The rhizosphere plays a vital role in the exchange of materials in the soil-plant ecosystem, and rhizosphere microorganisms are crucial for plant growth and development. In this study, we isolated two strains of Pantoea rhizosphere bacteria separately from invasive Alternanthera philoxeroides and native A. sessilis. We conducted a control experiment to test the effects of these bacteria on the growth and competition of the two plant species using sterile seedlings. Our findings showed that the rhizobacteria strain isolated from A. sessilis significantly promoted the growth of invasive A. philoxeroides in monoculture compared to native A. sessilis. Both strains significantly enhanced the growth and competitiveness of invasive A. philoxeroides under competition conditions, regardless of their host source. Our study suggests that rhizosphere bacteria, including those from different host sources, can contribute to the invasion of A. philoxeroides by significantly enhancing its competitiveness.

5.
Nanomicro Lett ; 15(1): 88, 2023 Apr 07.
Artigo em Inglês | MEDLINE | ID: mdl-37029266

RESUMO

Highly ordered and uniformly porous structure of conductive foams is a vital issue for various functional purposes such as piezoresistive sensing and electromagnetic interference (EMI) shielding. With the aids of Kevlar polyanionic chains, thermoplastic polyurethane (TPU) foams reinforced by aramid nanofibers (ANF) with adjustable pore-size distribution were successfully obtained via a non-solvent-induced phase separation. In this regard, the most outstanding result is the in situ formation of ANF in TPU foams after protonation of Kevlar polyanion during the NIPS process. Furthermore, in situ growth of copper nanoparticles (Cu NPs) on TPU/ANF foams was performed according to the electroless deposition by using the tiny amount of pre-blended Ti3C2Tx MXene as reducing agents. Particularly, the existence of Cu NPs layers significantly promoted the storage modulus in 2,932% increments, and the well-designed TPU/ANF/Ti3C2Tx MXene (PAM-Cu) composite foams showed distinguished compressive cycle stability. Taking virtues of the highly ordered and elastic porous architectures, the PAM-Cu foams were utilized as piezoresistive sensor exhibiting board compressive interval of 0-344.5 kPa (50% strain) with good sensitivity at 0.46 kPa-1. Meanwhile, the PAM-Cu foams displayed remarkable EMI shielding effectiveness at 79.09 dB in X band. This work provides an ideal strategy to fabricate highly ordered TPU foams with outstanding elastic recovery and excellent EMI shielding performance, which can be used as a promising candidate in integration of satisfactory piezoresistive sensor and EMI shielding applications for human-machine interfaces.

6.
Bioorg Med Chem Lett ; 85: 129218, 2023 04 01.
Artigo em Inglês | MEDLINE | ID: mdl-36894107

RESUMO

A series of mono- and bisnaphthalimides derivatives containing 3-nitro and 4-morpholine moieties were designed, synthesized, and evaluated for their in vitro anticancer activities against four cancer cell lines. Some compounds exhibited relatively good antiproliferative activity on the cell lines tested, in comparison with mitonafide and amonafide. It is noteworthy that bisnaphthalimide A6 was identified as the most potent compound in anti-proliferation against MGC-803 cells, with an IC50 lowered to 0.09 µM, a far greater potency than that of mono-naphthalimide A7, mitonafide, and amonafide. A gel electrophoresis assay revealed that DNA and Topo I were the potential targets of compounds A6 and A7. The treatment of CNE-2 cells with compounds A6 and A7 resulted in an S phase cell cycle arrest, accompanied by the upregulation of the expression levels of the antioncogene p27 and the down-regulation of the expression levels of CDK2 and cyclin E. In addition, compounds A6 and A7-induced apoptosis was further confirmed by flow cytometry, ROS generation assay, and Hoechst 33,258 staining. In particular, in vivo antitumor assay results revealed that bisnaphthalimide A6 exhibited potent anticancer efficiency in an MGC-803 xenograft tumor model, in comparison with mitonafide, and had lower toxicity than mono-naphthalimide A7. In brief, the results suggested that bisnaphthalimide derivatives containing 3-nitro and 4-morpholine moieties might serve as DNA binding agents for the development of new antitumor agents.


Assuntos
Antineoplásicos , Humanos , Ensaios de Seleção de Medicamentos Antitumorais , Antineoplásicos/química , Apoptose , DNA/química , Morfolinas/farmacologia , Linhagem Celular Tumoral , Proliferação de Células , Relação Estrutura-Atividade , Estrutura Molecular
7.
Front Pharmacol ; 14: 1086813, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36814489

RESUMO

Hepatocellular carcinoma (HCC) is one of the most common digestive malignancies. HCC It ranges as the fifth most common cause of cancer mortality worldwide. While The prognosis of metastatic or advanced HCC is still quite poor. Recently, locoregional treatment, especially local ablation therapies, plays an important role in the treatment of HCC. Radiofrequency ablation (RFA) and high-intensity focused ultrasound (HIFU) ablation are the most common-used methods effective and feasible for treating HCC. However, the molecular mechanisms underlying the actions of ablation in the treatments for HCC and the HCC recurrence after ablation still are poorly understood. Hypoxia-inducible factor (HIF), the key gene switch for adaptive responses to hypoxia, has been found to play an essential role in the rapid aggressive recurrence of HCC after ablation treatment. In this review, we summarized the current evidence of the roles of HIF in the treatment of HCC with ablation. Fifteen relevant studies were included and further analyzed. Among them, three clinical studies suggested that HIF-1α might serve as a crucial role in the RAF treatment of HCC or the local recurrence of HCC after RFA. The remainder included experimental studies demonstrated that HIF-1, 2α might target the different molecules (e.g., BNIP3, CA-IX, and arginase-1) and signaling cascades (e.g., VEGFA/EphA2 pathway), constituting a complex network that promoted HCC invasion and metastasis after ablation. Currently, the inhibitors of HIF have been developed, providing important proof of targeting HIF for the prevention of HCC recurrence after IRFA and HIFU ablation. Further confirmation by prospective clinical and in-depth experimental studies is still warranted to illustrate the effects of HIF in HCC recurrence followed ablation treatment in the future.

8.
ACS Nano ; 17(4): 3620-3631, 2023 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-36715341

RESUMO

In nature, many insects have evolved sclerotic cuticles to shelter their soft bodies, which are considered as "body armor". For beetles, the epidermis is composed of cross-linked intertwined fiber structures; such a fiber network structure could provide an anti-impact function for composites. Aramid nanofibers (ANFs) are of great interest in various applications due to their 1D nanoscale, high aspect ratio, excellent strength and modulus, and impressive chemical and thermal stability. In this paper, a kind of ANF network is prepared by a layer-by-layer assembly method. The enhancing ANF networks are developed by introducing carboxylated chitosan acting as a hydrogen-bondin donors as well as a soft interlocking agent (C-ANFs). As a result of the formation of a nanostructure and the hydrogen-bond interactions, the assembled C-ANF networks presented a high tensile strength (551.4 MPa) and toughness (4.0 MJ/m2), which is 2.41 times and 32.69 times those of neat ANF networks, respectively. The excellent mechanical properties endow C-ANF networks with distinguished anti-impact performance. The specific dissipated energy after mass normalization reaches 7.34 MJ/kg, which is significantly superior to traditional protective materials such as steel and Kevlar composites. A nonlinear spring model is also used to explain the mechanical behavior of C-ANF networks. In addition to anti-impact protection, C-ANF networks can realize more than 99% of UV irradiation absorption and have excellent thermal stability. The chemical stability of C-ANF networks make them survive in acid and alkali environments. The above characteristics show that C-ANF networks have great application value in multiscale protection scenarios under an extreme environment.

9.
Plants (Basel) ; 11(23)2022 Dec 04.
Artigo em Inglês | MEDLINE | ID: mdl-36501409

RESUMO

The role of the interactions between endophytes and host plants is unclear in invasive plants from different geographical latitudes. In this study, we aimed to explore the relationship between endophytic microbes and the functional traits of the invasive plant Wedelia trilobata. We explored the relationship between endophytes and the clonal growth traits of the invasive clonal plant Wedelia trilobata from different geographical latitudes using high-throughput sequencing technology and a common garden-planting experiment. We found that: (1) Different W. trilobata populations had similar endophytic fungi but different endophytic bacteria. However, no latitudinal variation pattern of the overall microbial community was found; (2) plant clonal growth performance (i.e., spacer length) was significantly correlated with endophytic bacterial diversity but not fungal diversity; and (3) the latitudinal variation pattern of the plant clonal growth performance of W. trilobata populations was found in pre-cultivated (i.e., wild) individuals but disappeared in post-cultivated W. trilobata. Our results suggest both environmental adaptability and the endophytic bacterial community are linked to the functional traits of the invasive clonal plant W. trilobata, and these functional traits tend to increase its invasiveness, which may enhance its invasion success.

10.
Opt Express ; 30(14): 25907-25917, 2022 Jul 04.
Artigo em Inglês | MEDLINE | ID: mdl-36237110

RESUMO

Guided-mode resonance (GMR) bandpass filters have many important applications. The tolerance of fabrication errors that easily cause the transmission wavelength to shift has been well studied for one-dimensional (1D) anisotropic GMR gratings. However, the tolerance of two-dimensional (2D) GMR gratings, especially for different design architectures, has rarely been explored, which prevents the achievement of a high-tolerance unpolarized design. Here, GMR filters with common 2D zero-contrast gratings (ZCGs) were first investigated to reveal their differences from 1D gratings in fabrication tolerance. We demonstrated that 2D ZCGs are highly sensitive to errors in the grating linewidth against the case of 1D gratings, and the linewidth orthogonal to a certain polarization direction has much more influence than that parallel to the polarization. By analyzing the electromagnetic fields, we found that there was an obvious field enhancement inside the gratings, which could have a strong effect on the modes in the waveguide layer through the field overlap. Therefore, we proposed the introduction of an etch-stop (ES) layer between the gratings and the waveguide-layer, which can effectively suppress the interaction between the gratings and modal evanescent fields, resulting in 4-fold increased tolerance to the errors in the grating linewidth. Finally, the proposed etch-stop ZCGs (ES-ZCGs) GMR filters were experimentally fabricated to verify the error robustness.

11.
ACS Nano ; 16(11): 19067-19086, 2022 11 22.
Artigo em Inglês | MEDLINE | ID: mdl-36302097

RESUMO

Pervasive mechanical impact is growing requirement for advanced high-performance protective materials, while the electromagnetic interference (EMI) confers severe risk to human health and equipment operation. Bioinspired structural composites achieving outstanding safeguards against a single threat have been developed, whereas the synergistic implementation of impact/EMI coupling protection remains a challenge. This work proposes the concept of nacre-mimetic hierarchical composite duplicating the "brick-and-mortar" arrangement, which consists of freeze-drying constructed chitosan/MXene lamellar architecture skeleton embedded in a shear stiffening polyborosiloxane matrix. The resulting composite effectively attenuates the impact force of 85.9%-92.8% with extraordinary energy dissipation capacity, in the coordinative manner of strain-rate enhancement, structural densification, lamella dislocation and crack propagation. Attributed to the alternate laminated structure promoting the reflection loss of electromagnetic waves, it demonstrates an ultraefficient EMI shielding effectiveness of 47.2-71.8 dB within extremely low MXene loadings of 1.1-1.3 wt %. Furthermore, it serves favorably in impact monitoring and wireless alarm systems and accomplishes performance optimization through the combination of multiple biomimetic strategies. In conclusion, this function-integrated structural composite is shown to be a competitive candidate for sophisticated environments by resisting impact damage and EMI hazards.


Assuntos
Nácar , Humanos , Nácar/química , Biomimética , Fenômenos Mecânicos , Fenômenos Eletromagnéticos
12.
J Environ Manage ; 323: 116296, 2022 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-36261968

RESUMO

Phytoremediation is currently an active field of research focusing chiefly on identifying and characterizing novel and high chelation action super-accumulators. In the last few years, molecular tools have been widely exploited to understand better metal absorption, translocation, cation, and tolerance mechanisms in plants. Recently more advanced CRISPR-Cas9 genome engineering technology is also employed to enhance detoxification efficiency. Further, advances in molecular science will trigger the understanding of adaptive phytoremediation ability plant production in current global warming conditions. The enhanced abilities of nucleases for genome modification can improve plant repair capabilities by modifying the genome, thereby achieving a sustainable ecosystem. The purpose of this manuscript focuses on biotechnology's fundamental principles and application to promote climate-resistant metal plants, especially the CRISPR-Cas9 genome editing system for enhancing the phytoremediation of harmful contamination and pollutants.


Assuntos
Sistemas CRISPR-Cas , Poluentes Ambientais , Biodegradação Ambiental , Ecossistema , Plantas/genética , Metais , Tecnologia
13.
J Anal Methods Chem ; 2022: 5607347, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36248054

RESUMO

Diosgenin, a steroidal sapogenin, has attracted attention worldwide owing to its pharmacological properties, including antitumor, cardiovascular protective, hypolipidemic, and anti-inflammatory effects. The current diosgenin analysis methods have the disadvantages of long analysis time and low sensitivity. The aim of the present study was to establish an efficient, sensitive ultrahigh-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) approach for pharmacokinetic analysis of diosgenin amorphous solid dispersion (ASD) using tanshinone IIA as an internal standard (IS). Male Sprague-Dawley rats were orally administered diosgenin ASD, and orbital blood samples were collected for analysis. Protein precipitation was performed with methanol-acetonitrile (50 : 50, v/v), and the analytes were separated under isocratic elution by applying acetonitrile and 0.03% formic acid aqueous solution at a ratio of 80 : 20 as the mobile phase. MS with positive electron spray ionization in multiple reaction monitoring modes was applied to determine diosgenin and IS with m/z 415.2⟶271.2 and m/z 295.2⟶277.1, respectively. This approach showed a low limit of quantification of 0.5 ng/ml for diosgenin and could detect this molecule at a concentration range of 0.5 to 1,500 ng/ml (r = 0.99725). The approach was found to have intra- and inter-day precision values ranging from 1.42% to 6.91% and from 1.25% to 3.68%, respectively. Additionally, the method showed an accuracy of -6.54 to 4.71%. The recoveries of diosgenin and tanshinone IIA were 85.81-100.27% and 98.29%, respectively, with negligible matrix effects. Diosgenin and IS were stable under multiple storage conditions. Pharmacokinetic analysis showed that the C max and AUC0⟶t of diosgenin ASD were significantly higher than those of the bulk drug. A sensitive, simple, UPLC-MS/MS analysis approach was established and used for the pharmacokinetic analysis of diosgenin ASD in rats after oral administration.

14.
Chem Biodivers ; 19(7): e202200449, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-35680557

RESUMO

Zanthoxylum nitidum (Roxb.) DC., is one of Guangxi's characteristic national medicines, and is the classic Laoban medicine of Yao people "Ru Shan Hu" and Zhuang medicine "Liang Bei Zhen". It has been used as an anti-inflammatory, analgesic and haemostatic medicine for thousands of years. In this study, four new sesquiterpenoids (1-4), along with six previously described coumarins (5-10), were isolated from 95 % EtOH extract of Zanthoxylum nitidum. Comprehensive spectroscopic analyses (NMR and HR-ESI-MS) were used to elucidate the structures of these isolates. The absolute configurations of nitidumine A-D (1-4) were established by electronic circular dichroism (ECD). Their cytotoxicity of all the isolates against five cancer cell lines (T24, HeLa, MGC-803, A549, and HepG2) was evaluated by MTT experiment and found not to be cytotoxicity.


Assuntos
Medicamentos de Ervas Chinesas , Sesquiterpenos , Zanthoxylum , China , Cumarínicos/farmacologia , Medicamentos de Ervas Chinesas/química , Humanos , Estrutura Molecular , Sesquiterpenos/farmacologia , Zanthoxylum/química
15.
Int J Mol Sci ; 23(2)2022 Jan 11.
Artigo em Inglês | MEDLINE | ID: mdl-35054970

RESUMO

The voltage-gated calcium channel (VGCC) ß subunit (Cavß) protein is a kind of cytosolic auxiliary subunit that plays an important role in regulating the surface expression and gating characteristics of high-voltage-activated (HVA) calcium channels. Ditylenchus destructor is an important plant-parasitic nematode. In the present study, the putative Cavß subunit gene of D. destructor, namely, DdCavß, was subjected to molecular characterization. In situ hybridization assays showed that DdCavß was expressed in all nematode tissues. Transcriptional analyses showed that DdCavß was expressed during each developmental stage of D. destructor, and the highest expression level was recorded in the third-stage juveniles. The crucial role of DdCavß was verified by dsRNA soaking-mediated RNA interference (RNAi). Silencing of DdCavß or HVA Cavα1 alone and co-silencing of the DdCavß and HVA Cavα1 genes resulted in defective locomotion, stylet thrusting, chemotaxis, protein secretion and reproduction in D. destructor. Co-silencing of the HVA Cavα1 and Cavß subunits showed stronger interference effects than single-gene silencing. This study provides insights for further study of VGCCs in plant-parasitic nematodes.


Assuntos
Canais de Cálcio Tipo L/genética , Inativação Gênica , Fenótipo , Subunidades Proteicas/genética , RNA de Cadeia Dupla/genética , Tylenchida/fisiologia , Sequência de Aminoácidos , Animais , Canais de Cálcio Tipo L/química , Quimiotaxia/genética , Técnicas de Silenciamento de Genes , Estudos de Associação Genética , Locomoção/genética , Modelos Moleculares , Biossíntese de Proteínas , Conformação Proteica , Subunidades Proteicas/química , Interferência de RNA , Reprodução/genética , Relação Estrutura-Atividade , Tylenchida/genética , Tylenchida/crescimento & desenvolvimento
16.
J Leg Med ; 42(3-4): 123-141, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-38377336

RESUMO

The legal protection of biometric data is becoming an increasingly important issue in the information society. China attaches importance to the legal protection of biometric data. Over the past decades, the rapid development of digital technology has profoundly influenced Chinese information society. However, digital technology may also trigger substantial risks. In this article, we provide an in-depth examination of existing Chinese laws protecting biometric data. We explore general laws and facial recognition laws, administrative regulations, sector-based rules, judicial interpretations, regulatory documents, policy documents, and (draft) national standards. We find gaps in laws in China. Building on this analysis, we elaborate on five principles for the legal protection of biometric data: (1) legality, propriety, and necessity; (2) integrity; (3) purpose; (4) minimization; and (5) controllability. We provide three policy recommendations for the legal protection of biometric data: (1) sufficiently considering the purpose of the collection of biometric data, (2) creating controllable mechanisms, and (3) implementing regulatory compliance programs.

17.
ACS Appl Mater Interfaces ; 13(5): 6575-6584, 2021 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-33517653

RESUMO

A novel shock-resistant, self-generating triboelectric nanogenerator (SS-TENG) with high-speed impact energy-harvesting and safeguarding properties was developed by assembling Kevlar fiber and conductive shear-stiffening gel. The SS-TENG with energy-harvesting property generated a maximum power density of 5.3 mW/m2 with a voltage of 13.1 V under oscillator compression and could light up light-emitting diode arrays. Owing to the energy absorption effect, the as-designed SS-TENG could dissipate impact forces from 2880 to 1460 N, showing anti-impact performance under the drop hammer impact. It also sensed the loading forces by outputting 36.4 V. Functionalized as a self-powered sensor, SS-TENG monitored various human movements and provided protection from hammer impact. Interestingly, a wearable sole array with high sensitivity and a fast response could distinguish toe in/out motions. More importantly, this functional SS-TENG presented excellent anti-impact behavior, which dissipated 94% of kinetic energy under bullet-shooting excitation. It also gathered high speed ballistic energy, which outputted a maximum power density of 3 mW/m2. To this end, this SS-TENG with a protection effect and the ability to harvest various impact energy showed promising applications in new power sources, intelligent wearable systems, and safeguard areas.

18.
Int J Neuropsychopharmacol ; 24(1): 64-76, 2021 01 20.
Artigo em Inglês | MEDLINE | ID: mdl-33000169

RESUMO

BACKGROUND: Neuropathic pain is a multifaceted and ubiquitous disease across the globe. Mood disorders, such as anxiety and depression, are frequently observed in patients suffering from neuropathic pain. Both neuropathic pain and comorbid mood disorders seriously impact quality of life. Accumulated evidence shows that activation of the NOD-like receptor protein 3 (NLRP3) inflammasome is involved in the neuroinflammatory pathogenesis of neuropathic pain, anxiety, and depression. However, the role of the NLRP3 inflammasome in the pathological process of anxiety and depression under the neuropathic pain state has not been fully described. Albiflorin, a monoterpene glycoside, may be a potential regulator of the NLRP3 inflammasome, but it is not clear whether albiflorin relates to NLRP3 inflammasome activation. METHODS: We used a systematic pharmacological method to confirm whether the activation of the NLRP3 inflammasome in the hippocampus was involved in the development of neuropathic pain associated with mood disorders and whether albiflorin could be an effective treatment for these symptoms. RESULTS: The NLRP3 inflammasome contributed to the neuropathic pain and comorbid anxiety and depression-like behaviors induced by chronic constriction injury of the sciatic nerve, and albiflorin may relieve these symptoms via inhibition of the NLRP3 inflammasome activity. Moreover, albiflorin enhanced the translocation of the nuclear factor erythroid 2-related factor 2 into the nucleus and suppressed nuclear factor-kappa B activity in the hippocampus. CONCLUSIONS: Albiflorin, as a potential therapeutic agent, might greatly improve the overall symptoms of neuropathic pain.


Assuntos
Ansiedade/tratamento farmacológico , Hidrocarbonetos Aromáticos com Pontes/farmacologia , Depressão/tratamento farmacológico , Hipocampo/efeitos dos fármacos , Inflamassomos/efeitos dos fármacos , Proteína 3 que Contém Domínio de Pirina da Família NLR/efeitos dos fármacos , Neuralgia/tratamento farmacológico , Animais , Comportamento Animal/efeitos dos fármacos , Constrição , Modelos Animais de Doenças , Masculino , Neuralgia/etiologia , Traumatismos dos Nervos Periféricos/complicações , Ratos , Ratos Sprague-Dawley
19.
Drug Des Devel Ther ; 14: 2959-2975, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32801637

RESUMO

BACKGROUND AND PURPOSE: The traditional Chinese medicine, diosgenin (Dio), has attracted increasing attention because it possesses various therapeutic effects, including anti-tumor, anti-infective and anti-allergic properties. However, the commercial application of Dio is limited by its extremely low aqueous solubility and inferior bioavailability in vivo. Soluplus, a novel excipient, has great solubilization and capacity of crystallization inhibition. The purpose of this study was to prepare Soluplus-mediated Dio amorphous solid dispersions (ASDs) to improve its solubility, bioavailability and stability. METHODS: The crystallization inhibition studies were firstly carried out to select excipients using a solvent shift method. According to solubility and dissolution results, the preparation methods and the ratios of drug to excipient were further optimized. The interaction between Dio and Soluplus was characterized by differential scanning calorimetry (DSC), fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), powder X-ray diffraction (PXRD) and molecular docking. The pharmacokinetic study was conducted to explore the potential of Dio ASDs for oral administration. Furthermore, the long-term stability of Dio ASDs was also investigated. RESULTS: Soluplus was preliminarily selected from various excipients because of its potential to improve solubility and stability. The optimized ASDs significantly improved the aqueous solubility of Dio due to its amorphization and the molecular interactions between Dio and Soluplus, as evidenced by dissolution test in vitro, DSC, FT-IR spectroscopy, SEM, PXRD and molecular docking technique. Furthermore, pharmacokinetic studies in rats revealed that the bioavailability of Dio from ASDs was improved about 5 times. In addition, Dio ASDs were stable when stored at 40°C and 75% humidity for 6 months. CONCLUSION: These results indicated that Dio ASDs, with its high solubility, high bioavailability and high stability, would open a promising way in pharmaceutical applications.


Assuntos
Diosgenina/farmacocinética , Desenvolvimento de Medicamentos , Medicamentos de Ervas Chinesas/farmacocinética , Excipientes/farmacocinética , Polietilenoglicóis/farmacocinética , Polivinil/farmacocinética , Administração Oral , Animais , Disponibilidade Biológica , Cromatografia Líquida de Alta Pressão , Cristalografia por Raios X , Diosgenina/administração & dosagem , Composição de Medicamentos , Estabilidade de Medicamentos , Medicamentos de Ervas Chinesas/administração & dosagem , Excipientes/administração & dosagem , Masculino , Medicina Tradicional Chinesa , Conformação Molecular , Simulação de Acoplamento Molecular , Polietilenoglicóis/administração & dosagem , Polivinil/administração & dosagem , Ratos , Ratos Sprague-Dawley , Solubilidade , Espectrometria de Massas em Tandem
20.
Inflammopharmacology ; 28(6): 1495-1508, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32596762

RESUMO

Neuropathic pain remains one of the most common pain conditions worldwide. Accumulating evidence shows that activation of the NOD-like receptor protein 3 (NLRP3) inflammasome contributes to the pathogenesis of neuropathic pain, although the role of the NLRP3 inflammasome in neuropathic pain has not yet been fully elucidated. In animal models of neuropathic pain, paeoniflorin (PF) was shown to have analgesic, anti-inflammatory, and antidepressant effects. However, the role of the NLRP3 inflammasome in the analgesic properties of PF has not yet been studied. In this study, we aimed to confirm whether activation of the NLRP3 inflammasome in the spinal cord was involved in the development of neuropathic pain and whether PF could be an effective treatment for this type of pain. We found that activation of the NLRP3 inflammasome mediated the development of neuropathic pain following chronic constriction injury of the sciatic nerve and that PF attenuated neuropathic pain by inhibiting NLRP3 inflammasome activation. Moreover, PF enhanced the translocation of the transcription factor nuclear factor erythroid 2-related factor 2 into the nucleus and suppressed nuclear factor-kappa B activity in the spinal cord. These results suggest that PF may be a potential therapeutic agent for neuropathic pain.


Assuntos
Glucosídeos/farmacologia , Inflamassomos/efeitos dos fármacos , Monoterpenos/farmacologia , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Neuralgia/tratamento farmacológico , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Constrição , Hiperalgesia/tratamento farmacológico , Hiperalgesia/metabolismo , Inflamassomos/metabolismo , Fator 2 Relacionado a NF-E2/metabolismo , NF-kappa B/metabolismo , Neuralgia/metabolismo , Ratos , Ratos Sprague-Dawley , Nervo Isquiático/efeitos dos fármacos , Nervo Isquiático/metabolismo , Medula Espinal/efeitos dos fármacos , Medula Espinal/metabolismo
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