RESUMO
The observation area of a point target, which is usually inaccessible, is a necessary condition when utilizing the conventional single-band infrared radiometric thermometry method, as the image gray level inevitably undergoes dispersion. Otherwise, significant errors will be generated, seriously affecting the applicability of infrared radiometric thermometry for distant point targets in the external field. To address the above issue, the infrared radiometric thermometry method for point targets has been researched. A point target radiometric thermometry method based on dual-band infrared imaging is proposed, which can effectively measure radiance and temperature when the area of the point target is unknown. The experimental results show that, compared with conventional single-band algorithms, the proposed dual-band point target thermometry algorithm has a maximum error of 11.18°C under the condition of unknown area, which can meet the needs of infrared radiometric thermometry of point targets at long distances in the external field.
RESUMO
Multiple studies have confirmed that acid sphingomyelinase (ASM) activity is associated with depression. The discovery of direct inhibitors against ASM is of great significance for exploring antidepressants and their mechanisms of action. Herein, a series of novel phenylpyrazole analogues were rationally designed and synthesized. Among them, compound 46 exhibited potent inhibitory activity (IC50 = 0.87 µM) and good drug-like properties. In vivo studies demonstrated that compound 46 was involved in multiple antidepressant mechanisms of action, which were associated with a decline of ceramide, including increasing the Bcl-2/Bax ratio and BDNF expression, down-regulating caspase-3 and caspase-9, ameliorating oxidative stress, reducing the levels of proinflammatory cytokines such as TNF-α, IL-1ß, and IL-6, and elevating 5-HT levels in the brains of mice, respectively. These meaningful results reveal for the first time that direct inhibitors exhibit remarkable antidepressant effects in the CUMS-induced mouse model through multiple mechanisms of antidepressant action.
Assuntos
Antidepressivos , Pirazóis , Esfingomielina Fosfodiesterase , Animais , Antidepressivos/farmacologia , Antidepressivos/química , Antidepressivos/síntese química , Pirazóis/farmacologia , Pirazóis/química , Pirazóis/síntese química , Camundongos , Esfingomielina Fosfodiesterase/antagonistas & inibidores , Esfingomielina Fosfodiesterase/metabolismo , Relação Estrutura-Atividade , Masculino , Depressão/tratamento farmacológico , Depressão/metabolismo , Descoberta de Drogas , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/síntese química , Humanos , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Estresse Oxidativo/efeitos dos fármacosRESUMO
Ageratina adenophora can enhance its invasive ability by using beneficial rhizosphere bacteria. Bacillus cereus is able to promote plant growth and provide a positive feedback effect to A. adenophora. However, the interaction between A. adenophora and B. cereus under the influence of native polyphagous insect feeding is still unclear. In this study, Eupatorium lindleyanum, a local species closely related to A. adenophora, was used as a control, aimed to compare the content of B. cereus in the roots of A. adenophora and rhizosphere soil after different densities of Aphis gossypii feeding, and then investigated the variations in the population of A. gossypii and soil characteristics after the addition of B. cereus. The result showed that B. cereus content in the rhizosphere soil and root of A. adenophora increased significantly under A. gossypii feeding compared with local plants, which also led to the change of α-diversity and ß-diversity of the bacterial community, as well as the increase in nitrate nitrogen (NO3 -N) content. The addition of B.cereus in the soil could also inhibit the population growth of A. gossypii on A. adenophora and increase the content of ammonium nitrogen (NH4 +-N) in the soil. Our research demonstrated that B. cereus enhances the ability of A. adenophora to resist natural enemy by increasing soil ammonium nitrogen (NH4 +-N) and accumulating other beneficial bacteria, which means that rhizosphere microorganisms help invasive plants defend themselves against local natural enemies by regulating the soil environment.
RESUMO
Fucosylated chondroitin sulfate is a unique glycosaminoglycan isolated from sea cucumbers, with excellent anticoagulant activity. The fucosyl branch in FCS is generally located at the 3-OH of D-glucuronic acid but, recently, a novel structure with α-L-fucose linked to the 6-OH of N-acetyl-galactosamine has been found. Here, using functionalized monosaccharide building blocks, we prepared novel FCS tetrasaccharides with fucosyl branches both at the 6-OH of GalNAc and 3-OH of GlcA. In the synthesis, the protective group strategy of selective O-sulfation, as well as stereoselective glycosylation, was established, which enabled the efficient synthesis of the specific tetrasaccharide compounds. This research enriches knowledge on the structural types of FCS oligosaccharides and facilitates the exploration of the structure-activity relationship in the future.
Assuntos
Sulfatos de Condroitina , Oligossacarídeos , Pepinos-do-Mar , Sulfatos de Condroitina/química , Sulfatos de Condroitina/síntese química , Sulfatos de Condroitina/farmacologia , Animais , Oligossacarídeos/síntese química , Oligossacarídeos/química , Pepinos-do-Mar/química , Glicosilação , Fucose/química , Anticoagulantes/farmacologia , Anticoagulantes/química , Anticoagulantes/síntese química , Relação Estrutura-Atividade , Acetilgalactosamina/química , Acetilgalactosamina/análogos & derivadosRESUMO
BACKGROUND: Insects use odor detection to sense their surroundings. Use of volatile compounds, such as essential oils (EOs) of plants, to repel pests and disrupt their olfaction-driven behaviors has great practical potential for use in integrated pest management. Despite the available information on the repellent effects of EOs on herbivorous insects, the olfaction-based mechanisms remain unknown. RESULTS: Y-tube olfactometer tests showed that the EOs of three Lamiaceae plants - Mentha arvensis L., Mentha piperita L. and Lavandula angustifolia Mill. - were significantly repellent to winged cotton aphid, Aphis gossypii Glover. Electrical penetration graph (EPG) tests indicated the EOs reduced phloem feeding and increased the level of non-productive probing by the aphids. The EOs also reduced the fecundity of winged Aphis gossypii. Electrophysiological bioassays and gas chromatography-mass spectrometry (GC-MS) identified five physiologically active volatiles, that is menthone, isomenthone, neomenthol and menthol from Mentha piperita; menthone and menthol from Mentha arvensis; and linalool from L. angustifolia. Behavioral tests confirmed that all five compounds repelled winged Aphis gossypii. Under field conditions, the growth rate of aphid populations after 7 days was significantly lower in fields treated with these compounds than in the control fields. CONCLUSION: Our findings demonstrated that three EOs not only repelled winged Aphis gossypii but also interfered with the aphid's feeding behavior and reduced its fecundity. These EOs and their active constituents have great potential as eco-friendly control products for use against Aphis gossypii. The effects of these EOs also exceed other repellents that only keep pests away from host plants. © 2024 Society of Chemical Industry.
Assuntos
Afídeos , Comportamento Alimentar , Fertilidade , Repelentes de Insetos , Óleos Voláteis , Animais , Afídeos/efeitos dos fármacos , Afídeos/fisiologia , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Repelentes de Insetos/farmacologia , Comportamento Alimentar/efeitos dos fármacos , Fertilidade/efeitos dos fármacos , Lavandula/química , Mentha piperita/química , Mentha/química , Lamiaceae/químicaRESUMO
BACKGROUND: Piriformospora indica is an endophytic fungus that can promote the growth and confer resistance against diverse stresses in host plants by root colonization. However, the effects of P. indica colonization on improving plant resistance to insect pests are still less explored. The brown planthopper (BPH) Nilaparvata lugens is a serious monophagous pest that causes extensive damage to rice plants. Here, we aimed to evaluate the effects of P. indica colonization on rice resistance against BPH. RESULTS: The colonization of P. indica in rice roots resisted damage from BPH. Age-stage, two-sex life table analyses showed that feeding on P. indica-colonized rice plants affected BPH's female adult longevity, oviposition period, fecundity, population parameters and population size. BPH female adults feeding on P. indica-colonized plants excreted less honeydew. P. indica colonization remarkably increased the duration of np, N2, and N3 waveform, as well as the occurrences of N1 and N2, and decreased the duration of N4-b for BPH on rice plants. Meanwhile, the weight of BPH on the colonized plants was significantly lower than the control. In addition, the feeding and oviposition preferences of BPH to P. indica-colonized plants were reduced. qRT-RCR analyses revealed that P. indica colonization induced the expressions of jasmonic acid (JA)- and salicylic acid (SA)-related genes in rice plants. CONCLUSION: P. indica colonization can reduce BPH performance on rice plants with potential inhibitory effects on population growth. Collectively, these results support the potential for endophytically colonized P. indica as an effective strategy to improve insect resistance of crops. © 2024 Society of Chemical Industry.
Assuntos
Basidiomycota , Hemípteros , Oryza , Animais , Hemípteros/fisiologia , Hemípteros/microbiologia , Oryza/microbiologia , Oryza/parasitologia , Basidiomycota/fisiologia , Feminino , Oviposição , Endófitos/fisiologia , Herbivoria , Raízes de Plantas/microbiologia , Defesa das Plantas contra Herbivoria , MasculinoRESUMO
Biological studies on the endocannabinoid system (ECS) have suggested that monoacylglycerol lipase (MAGL), an essential enzyme responsible for the hydrolysis of 2-arachidonoylglycerol (2-AG), is a novel target for developing antidepressants. A decrease of 2-AG levels in the hippocampus of the brain has been observed in depressive-like models induced by chronic stress. Herein, employing a structure-based approach, we designed and synthesized a new class of (piperazine-1-carbonyl) quinolin-2(1H)-one derivatives as potent, reversible and selective MAGL inhibitors. And detailed structure-activity relationships (SAR) studies were discussed. Compound 27 (IC50 = 10.3 nM) exhibited high bioavailability (92.7%) and 2-AG elevation effect in vivo. Additionally, compound 27 exerted rapid antidepressant effects caused by chronic restraint stress (CRS) and didn't show signs of addictive properties in the conditioned place preference (CPP) assays. Our study is the first to report that reversible MAGL inhibitors can treat chronic stress-induced depression effectively, which may provide a new potential therapeutic strategy for the discovery of an original class of safe, rapid antidepressant drugs.
Assuntos
Inibidores Enzimáticos , Monoacilglicerol Lipases , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/uso terapêutico , Monoacilglicerol Lipases/metabolismo , Depressão/tratamento farmacológico , Monoglicerídeos , Relação Estrutura-Atividade , Antidepressivos/farmacologia , Antidepressivos/uso terapêutico , EndocanabinoidesRESUMO
Novel hybrids of selective COX-2 inhibitors (coxibs) and active derivatives of free radical scavenger edaravone were designed to overcome the risk of cardiovascular events and stroke increased by NSAIDs (nonsteroidal anti-inflammatory drugs) in this study. All the hybrids were assayed for the COX-2 inhibitory and DPPH (2, 2-diphenyl-1-picrylhydrazyl) free radical scavenging activities in vitro. Finally, we found a series of hybrids with good inhibitory activity and selectivity of COX-2 and excellent free radical scavenging activity in vitro. The most promising compound 6a (WYZ90) exhibited very potent COX-2 inhibitory activity (COX-2, IC50 = 75 nM), weak COX-1 inhibitory activity (COX-1, IC50 = 5734 nM), better free radical scavenging activity (DPPH, IC50 = 19.9 µM) than edaravone, moderate drug-likeness and ADME properties in silico, acceptable pharmacokinetic properties (T1/2 = 4.16 h, 10 mg/kg, o.p.) and oral bioavailability (F% = 36.03 %) in mice. In addition, compound WYZ90 showed similar analgesic activity to the selective COX-2 inhibitor celecoxib in acetic acid-induced mice and better antioxidant activity in Fe2+-induced lipid peroxidation in mouse liver tissue homogenate than edaravone. In conclusion, this study provided a novel class of coxibs containing edaravone moiety as COX-2 selective NSAIDs with free radical scavenging activity and the candidate compound WYZ90 showed not only similar selective COX-2 inhibitory and analgesic activity to celecoxib but also better free radical scavenging and antioxidant activity than edaravone.
Assuntos
Anti-Inflamatórios não Esteroides , Inibidores de Ciclo-Oxigenase 2 , Camundongos , Animais , Anti-Inflamatórios não Esteroides/farmacologia , Inibidores de Ciclo-Oxigenase 2/farmacologia , Edaravone/farmacologia , Ciclo-Oxigenase 2 , Celecoxib , Antioxidantes , Analgésicos/farmacologia , Radicais Livres/químicaRESUMO
The quality of electrophysiological (EP) signals heavily relies on the electrode's contact with the skin. However, motion or exposure to water can easily destabilize this connection. In contrast to traditional methods of attaching electrodes to the skin surface, this study introduces a skin-integration strategy inspired by the skin's intergrown structure. A highly conductive and room-temperature curable composite composed of silver microflakes and polydimethylsiloxane (Ag/PDMS) is applied to the skin. Before curing, the PDMS oil partially diffuse into the stratum corneum (SC) layer of the skin. Upon curing, the composite solidifies into an electrode that seamlessly integrated with the skin, resembling a natural extension. This skin-integration strategy offers several advantages. It minimizes motion artifacts resulting from relative electrode-skin displacement, significantly reduces interface impedance (67% of commercial Ag/AgCl gel electrodes at 100 Hz) and withstands water flushes due to its hydrophobic nature. These advantages pave the way for promising advancements in EP signal recording, particularly during motion and underwater conditions.