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1.
Cell ; 186(24): 5363-5374.e16, 2023 11 22.
Artigo em Inglês | MEDLINE | ID: mdl-37972591

RESUMO

Cav1.2 channels play crucial roles in various neuronal and physiological processes. Here, we present cryo-EM structures of human Cav1.2, both in its apo form and in complex with several drugs, as well as the peptide neurotoxin calciseptine. Most structures, apo or bound to calciseptine, amlodipine, or a combination of amiodarone and sofosbuvir, exhibit a consistent inactivated conformation with a sealed gate, three up voltage-sensing domains (VSDs), and a down VSDII. Calciseptine sits on the shoulder of the pore domain, away from the permeation path. In contrast, when pinaverium bromide, an antispasmodic drug, is inserted into a cavity reminiscent of the IFM-binding site in Nav channels, a series of structural changes occur, including upward movement of VSDII coupled with dilation of the selectivity filter and its surrounding segments in repeat III. Meanwhile, S4-5III merges with S5III to become a single helix, resulting in a widened but still non-conductive intracellular gate.


Assuntos
Canais de Cálcio Tipo L , Venenos Elapídicos , Humanos , Canais de Cálcio Tipo L/química , Canais de Cálcio Tipo L/metabolismo , Neurotoxinas , Domínios Proteicos , Microscopia Crioeletrônica
2.
Cell ; 185(25): 4801-4810.e13, 2022 Dec 08.
Artigo em Inglês | MEDLINE | ID: mdl-36417914

RESUMO

Drug-drug interaction of the antiviral sofosbuvir and the antiarrhythmics amiodarone has been reported to cause fatal heartbeat slowing. Sofosbuvir and its analog, MNI-1, were reported to potentiate the inhibition of cardiomyocyte calcium handling by amiodarone, which functions as a multi-channel antagonist, and implicate its inhibitory effect on L-type Cav channels, but the molecular mechanism has remained unclear. Here we present systematic cryo-EM structural analysis of Cav1.1 and Cav1.3 treated with amiodarone or sofosbuvir alone, or sofosbuvir/MNI-1 combined with amiodarone. Whereas amiodarone alone occupies the dihydropyridine binding site, sofosbuvir is not found in the channel when applied on its own. In the presence of amiodarone, sofosbuvir/MNI-1 is anchored in the central cavity of the pore domain through specific interaction with amiodarone and directly obstructs the ion permeation path. Our study reveals the molecular basis for the physical, pharmacodynamic interaction of two drugs on the scaffold of Cav channels.


Assuntos
Amiodarona , Sofosbuvir , Sofosbuvir/efeitos adversos , Amiodarona/farmacologia , Antivirais/farmacologia , Miócitos Cardíacos/metabolismo , Sítios de Ligação , Canais de Cálcio Tipo L/metabolismo , Cálcio/metabolismo
3.
Cell ; 182(1): 98-111.e18, 2020 07 09.
Artigo em Inglês | MEDLINE | ID: mdl-32544384

RESUMO

Lysosomal cholesterol egress requires two proteins, NPC1 and NPC2, whose defects are responsible for Niemann-Pick disease type C (NPC). Here, we present systematic structural characterizations that reveal the molecular basis for low-pH-dependent cholesterol delivery from NPC2 to the transmembrane (TM) domain of NPC1. At pH 8.0, similar structures of NPC1 were obtained in nanodiscs and in detergent at resolutions of 3.6 Å and 3.0 Å, respectively. A tunnel connecting the N-terminal domain (NTD) and the transmembrane sterol-sensing domain (SSD) was unveiled. At pH 5.5, the NTD exhibits two conformations, suggesting the motion for cholesterol delivery to the tunnel. A putative cholesterol molecule is found at the membrane boundary of the tunnel, and TM2 moves toward formation of a surface pocket on the SSD. Finally, the structure of the NPC1-NPC2 complex at 4.0 Å resolution was obtained at pH 5.5, elucidating the molecular basis for cholesterol handoff from NPC2 to NPC1(NTD).


Assuntos
Colesterol/metabolismo , Peptídeos e Proteínas de Sinalização Intracelular/química , Peptídeos e Proteínas de Sinalização Intracelular/metabolismo , Lisossomos/metabolismo , Proteínas de Transporte Vesicular/química , Proteínas de Transporte Vesicular/metabolismo , Sequência de Aminoácidos , Animais , Linhagem Celular , Proteínas de Fluorescência Verde/metabolismo , Humanos , Concentração de Íons de Hidrogênio , Modelos Moleculares , Nanopartículas/química , Nanopartículas/ultraestrutura , Proteína C1 de Niemann-Pick , Domínios Proteicos , Homologia Estrutural de Proteína , Relação Estrutura-Atividade
4.
Nature ; 596(7870): 143-147, 2021 08.
Artigo em Inglês | MEDLINE | ID: mdl-34234349

RESUMO

The neuronal-type (N-type) voltage-gated calcium (Cav) channels, which are designated Cav2.2, have an important role in the release of neurotransmitters1-3. Ziconotide is a Cav2.2-specific peptide pore blocker that has been clinically used for treating intractable pain4-6. Here we present cryo-electron microscopy structures of human Cav2.2 (comprising the core α1 and the ancillary α2δ-1 and ß3 subunits) in the presence or absence of ziconotide. Ziconotide is thoroughly coordinated by helices P1 and P2, which support the selectivity filter, and the extracellular loops (ECLs) in repeats II, III and IV of α1. To accommodate ziconotide, the ECL of repeat III and α2δ-1 have to tilt upward concertedly. Three of the voltage-sensing domains (VSDs) are in a depolarized state, whereas the VSD of repeat II exhibits a down conformation that is stabilized by Cav2-unique intracellular segments and a phosphatidylinositol 4,5-bisphosphate molecule. Our studies reveal the molecular basis for Cav2.2-specific pore blocking by ziconotide and establish the framework for investigating electromechanical coupling in Cav channels.


Assuntos
Analgésicos não Narcóticos/farmacologia , Bloqueadores dos Canais de Cálcio/farmacologia , Canais de Cálcio Tipo N/química , Canais de Cálcio Tipo N/metabolismo , Microscopia Crioeletrônica , ômega-Conotoxinas/farmacologia , Canais de Cálcio Tipo N/ultraestrutura , Humanos , Modelos Moleculares , Fosfatidilinositol 4,5-Difosfato/metabolismo , Fosfatidilinositol 4,5-Difosfato/farmacologia , Conformação Proteica/efeitos dos fármacos , Estabilidade Proteica/efeitos dos fármacos
5.
Nature ; 581(7808): 333-338, 2020 05.
Artigo em Inglês | MEDLINE | ID: mdl-32433614

RESUMO

As members of the membrane-bound O-acyltransferase (MBOAT) enzyme family, acyl-coenzyme A:cholesterol acyltransferases (ACATs) catalyse the transfer of an acyl group from acyl-coenzyme A to cholesterol to generate cholesteryl ester, the primary form in which cholesterol is stored in cells and transported in plasma1. ACATs have gained attention as potential drug targets for the treatment of diseases such as atherosclerosis, Alzheimer's disease and cancer2-7. Here we present the cryo-electron microscopy structure of human ACAT1 as a dimer of dimers. Each protomer consists of nine transmembrane segments, which enclose a cytosolic tunnel and a transmembrane tunnel that converge at the predicted catalytic site. Evidence from structure-guided mutational analyses suggests that acyl-coenzyme A enters the active site through the cytosolic tunnel, whereas cholesterol may enter from the side through the transmembrane tunnel. This structural and biochemical characterization helps to rationalize the preference of ACAT1 for unsaturated acyl chains, and provides insight into the catalytic mechanism of enzymes within the MBOAT family8.


Assuntos
Biocatálise , Microscopia Crioeletrônica , Esterol O-Aciltransferase/química , Esterol O-Aciltransferase/metabolismo , Domínio Catalítico , Humanos , Modelos Moleculares , Multimerização Proteica , Esterol O-Aciltransferase/ultraestrutura , Especificidade por Substrato
6.
Mol Psychiatry ; 2023 Mar 13.
Artigo em Inglês | MEDLINE | ID: mdl-36914810

RESUMO

Recent studies based on animal models of various neurological disorders have indicated that mitophagy, a selective autophagy that eliminates damaged and superfluous mitochondria through autophagic degradation, may be involved in various neurological diseases. As an important mechanism of cellular stress response, much less is known about the role of mitophagy in stress-related mood disorders. Here, we found that tumor necrosis factor-α (TNF-α), an inflammation cytokine that plays a particular role in stress responses, impaired the mitophagy in the medial prefrontal cortex (mPFC) via triggering degradation of an outer mitochondrial membrane protein, NIP3-like protein X (NIX). The deficits in the NIX-mediated mitophagy by TNF-α led to the accumulation of damaged mitochondria, which triggered synaptic defects and behavioral abnormalities. Genetic ablation of NIX in the excitatory neurons of mPFC caused passive coping behaviors to stress, and overexpression of NIX in the mPFC improved TNF-α-induced synaptic and behavioral abnormalities. Notably, ketamine, a rapid on-set and long-lasting antidepressant, reversed the TNF-α-induced behavioral abnormalities through activation of NIX-mediated mitophagy. Furthermore, the downregulation of NIX level was also observed in the blood of major depressive disorder patients and the mPFC tissue of animal models. Infliximab, a clinically used TNF-α antagonist, alleviated both chronic stress- and inflammation-induced behavioral abnormalities via restoring NIX level. Taken together, these results suggest that NIX-mediated mitophagy links inflammation signaling to passive coping behaviors to stress, which underlies the pathophysiology of stress-related emotional disorders.

7.
Can J Microbiol ; 70(3): 102-108, 2024 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-38096506

RESUMO

Arsenic (As) is a metal with potentially toxic effects on different organisms. Hydrogen sulfide (H2S) plays a vital role in mitigating heavy metal toxicity by reducing oxidative stress in plants and animals. However, the role of H2S in alleviating arsenic toxicity in yeast cells remains unclear. In this study, the role of NaHS (exogenous physiological H2S) in alleviating As-induced yeast cell death was investigated. Yeast cells in the logarithmic phase were pretreated with 0.05 mmol/L NaHS for 6 h, and then incubated in the YPD medium with or without 1 mmol/L As. After 12 h of treatment, relative survival rate, H2S content, oxidative stress biomarkers, and antioxidant machinery were measured. Our results showed that sodium arsenite-induced yeast cell death and pretreatment with 0.05 mmol/L NaHS significantly alleviated sodium arsenite-induced cell death. Under sodium arsenite conditions, the levels of intracellular reactive oxygen species (ROS) and malondialdehyde (MDA) increased, accompanied by the inhibition of the catalase (CAT) activity and the downregulation of CTT1 expression. However, the activities of the superoxide dismutase (SOD) and glutathion peroxidase (GPX) increased, and the expression of SOD1 and GPX2 was markedly upregulated in the group treated with sodium arsenite. When yeast cells were pretreated with NaHS, the intracellular ROS and MDA levels decreased significantly, and the activities of SOD, CAT, and GPX increased significantly. This was associated with a significant increase in relative survival rate and H2S content compared to the arsenic treatment alone. Our findings indicate that NaHS alleviates sodium arsenite-induced yeast cell death, mainly by enhancing the antioxidant defense system.


Assuntos
Arsênio , Arsenitos , Sulfeto de Hidrogênio , Compostos de Sódio , Sulfetos , Animais , Sulfeto de Hidrogênio/farmacologia , Sulfeto de Hidrogênio/metabolismo , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Saccharomyces cerevisiae/metabolismo , Arsênio/toxicidade , Espécies Reativas de Oxigênio/metabolismo , Superóxido Dismutase/metabolismo , Morte Celular
8.
Molecules ; 29(3)2024 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-38338343

RESUMO

Respiratory syncytial virus (RSV) is a significant viral pathogen that causes respiratory infections in infants, the elderly, and immunocompromised individuals. RSV-related illnesses impose a substantial economic burden worldwide annually. The molecular structure, function, and in vivo interaction mechanisms of RSV have received more comprehensive attention in recent times, and significant progress has been made in developing inhibitors targeting various stages of the RSV replication cycle. These include fusion inhibitors, RSV polymerase inhibitors, and nucleoprotein inhibitors, as well as FDA-approved RSV prophylactic drugs palivizumab and nirsevimab. The research community is hopeful that these developments might provide easier access to knowledge and might spark new ideas for research programs.


Assuntos
Infecções por Vírus Respiratório Sincicial , Vírus Sincicial Respiratório Humano , Humanos , Lactente , Idoso , Antivirais/farmacologia , Antivirais/uso terapêutico , Palivizumab/farmacologia , Palivizumab/uso terapêutico , Infecções por Vírus Respiratório Sincicial/tratamento farmacológico , Infecções por Vírus Respiratório Sincicial/prevenção & controle , Antirretrovirais/uso terapêutico
9.
Brain Behav Immun ; 108: 204-220, 2023 02.
Artigo em Inglês | MEDLINE | ID: mdl-36496170

RESUMO

Increasing evidence supports the pathogenic role of neuroinflammation in psychiatric diseases, including major depressive disorder (MDD) and neuropsychiatric symptoms of Coronavirus disease 2019 (COVID-19); however, the precise mechanism and therapeutic strategy are poorly understood. Here, we report that myeloid differentiation factor 88 (MyD88), a pivotal adaptor that bridges toll-like receptors to their downstream signaling by recruiting the signaling complex called 'myddosome', was up-regulated in the medial prefrontal cortex (mPFC) after exposure to chronic social defeat stress (CSDS) or severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) spike protein. The inducible expression of MyD88 in the mPFC primed neuroinflammation and conferred stress susceptibility via amplifying immune danger signals, such as high-mobility group box 1 and SARS-CoV-2 spike protein. Overexpression of MyD88 aggravated, whereas knockout or pharmacological inhibition of MyD88 ameliorated CSDS-induced depressive-like behavior. Notably, TJ-M2010-5, a novel synthesized targeting inhibitor of MyD88 dimerization, alleviated both CSDS- and SARS-CoV-2 spike protein-induced depressive-like behavior. Taken together, our findings indicate that inhibiting MyD88 signaling represents a promising therapeutic strategy for stress-related mental disorders, such as MDD and COVID-19-related neuropsychiatric symptoms.


Assuntos
COVID-19 , Transtorno Depressivo Maior , Fator 88 de Diferenciação Mieloide , Humanos , Proteínas Adaptadoras de Transdução de Sinal/metabolismo , COVID-19/metabolismo , COVID-19/psicologia , Fator 88 de Diferenciação Mieloide/metabolismo , Doenças Neuroinflamatórias , SARS-CoV-2/metabolismo
10.
Br J Clin Pharmacol ; 89(3): 1139-1151, 2023 03.
Artigo em Inglês | MEDLINE | ID: mdl-36217805

RESUMO

AIMS: The aim of this study was to develop a population pharmacokinetic (PK) model to simultaneously describe both total and unbound concentrations of ciprofol and its major glucuronide metabolite, M4, and to link it to the population pharmacodynamics (PD) model in subjects with various renal functions. METHODS: A total of 401 and 459 pairs of total and unbound plasma concentrations of ciprofol and M4, respectively, as well as 2190 bispectral index (BIS) data from 24 Chinese subjects with various renal functions were available. Covariates that may potentially contribute to the PK and PD variability of ciprofol were screened using a stepwise procedure. The optimal ciprofol induction dosing regimen was determined by model-based simulations. RESULTS: The PK of unbound ciprofol could best be described by a three-compartment model, while a two-compartment model could adequately describe unbound M4 PK. The concentrations of total and unbound ciprofol and M4 were linked using a linear protein binding model. The relationship between plasma concentrations of ciprofol and BIS data was best described by an inhibitory sigmoidal Emax model with a two-compartment biophase distribution compartment. Hemoglobin was the identified covariate determining the central compartment clearance of ciprofol; uric acid was a covariate affecting the central compartment clearance of M4 and protein binding rate, kB . The included covariates had no effect on the PD of ciprofol. Simulation results indicated that the label-recommended dose regimen was adequate for anaesthesia induction. CONCLUSIONS: The developed model fully characterized the population PK and PD profiles of ciprofol. No dose adjustment is required in patients with mild and moderate renal impairment.


Assuntos
Rim , Modelos Biológicos , Humanos , Relação Dose-Resposta a Droga , Rim/fisiologia
11.
J Org Chem ; 88(19): 14193-14199, 2023 Oct 06.
Artigo em Inglês | MEDLINE | ID: mdl-37696811

RESUMO

A [4 + 1] cyclization and C-C bond cleavage process mediated reaction for constructing 3-carbonyl imidazo[1,5-a] pyridines from 1,3-dicarbonyl compounds and pyridin-2-ylmethanamines has been developed. Various 1,3-dicarbonyl compounds are applicable, and selectivity could be achieved. Importantly, this strategy could be extended to an atom economy method by employing a cyclic 1,3-dicarbonyl compound, and it provided a new view for C-C bond cleavage reactions.

12.
Proc Natl Acad Sci U S A ; 117(31): 18497-18503, 2020 08 04.
Artigo em Inglês | MEDLINE | ID: mdl-32680969

RESUMO

Membrane proteins (MPs) used to be the most difficult targets for structural biology when X-ray crystallography was the mainstream approach. With the resolution revolution of single-particle electron cryo-microscopy (cryo-EM), rapid progress has been made for structural elucidation of isolated MPs. The next challenge is to preserve the electrochemical gradients and membrane curvature for a comprehensive structural elucidation of MPs that rely on these chemical and physical properties for their biological functions. Toward this goal, here we present a convenient workflow for cryo-EM structural analysis of MPs embedded in liposomes, using the well-characterized AcrB as a prototype. Combining optimized proteoliposome isolation, cryo-sample preparation on graphene grids, and an efficient particle selection strategy, the three-dimensional (3D) reconstruction of AcrB embedded in liposomes was obtained at 3.9 Å resolution. The conformation of the homotrimeric AcrB remains the same when the surrounding membranes display different curvatures. Our approach, which can be widely applied to cryo-EM analysis of MPs with distinctive soluble domains, lays out the foundation for cryo-EM analysis of integral or peripheral MPs whose functions are affected by transmembrane electrochemical gradients or/and membrane curvatures.


Assuntos
Proteínas de Escherichia coli/metabolismo , Escherichia coli/metabolismo , Lipossomos/ultraestrutura , Proteínas de Membrana/metabolismo , Proteínas Associadas à Resistência a Múltiplos Medicamentos/metabolismo , Membrana Celular/metabolismo , Membrana Celular/ultraestrutura , Microscopia Crioeletrônica , Escherichia coli/ultraestrutura , Proteínas de Escherichia coli/ultraestrutura , Lipossomos/metabolismo , Proteínas de Membrana/ultraestrutura , Modelos Moleculares , Proteínas Associadas à Resistência a Múltiplos Medicamentos/ultraestrutura , Conformação Proteica
13.
Molecules ; 27(4)2022 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-35209244

RESUMO

Most Polygonatum species are widely used in China as a source of medicine and food. In this study, a UPLC-QTOF-MS/MS system was used to conduct an untargeted metabolomics analysis and compare the classes and relative contents of metabolites in the seeds of four Polygonatum species: P. sibiricum (Ps), P. cyrtonema (Pc), P. kingianum (Pk), and P. macropodium (Pm). The objectives of this study were to clarify the metabolic profiles of these seeds and to verify their medicinal and nutritional value via comparative analyses. A total of 873 metabolites were identified, including 185 flavonoids, 127 lipids, 105 phenolic acids, and 36 steroids. The comparative analysis of metabolites among Polygonatum seed samples indicated that flavonoids, steroids, and terpenoids were the main differentially abundant compounds. The results of principal component analysis and hierarchical clustering were consistent indicating that the metabolites in Ps and Pm are similar, but differ greatly from Pc and Pk. The data generated in this study provide additional evidence of the utility of Polygonatum seeds for producing food and medicine.


Assuntos
Metaboloma , Metabolômica , Polygonatum/química , Sementes/química , Cromatografia Líquida de Alta Pressão , Biologia Computacional/métodos , Metabolômica/métodos , Polygonatum/classificação , Espectrometria de Massas por Ionização e Dessorção a Laser Assistida por Matriz , Espectrometria de Massas em Tandem
14.
J Nurs Manag ; 30(2): 511-520, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34890482

RESUMO

AIM: The aim of this work is to investigate nurses' perceptions of barriers constraining the implementation of the Internet Plus Nursing Service program. BACKGROUND: The Internet Plus Nursing Service programme helps meet the demands of an ageing population, people with chronic diseases, the disabled, and home convalescents, and affirms the value of nurses. However, this programme has failed to elicit nurses' active participation, and there is limited knowledge regarding nurses' perceptions of the barriers to the programme's implementation. METHODS: A qualitative study was conducted. Thematic analysis of the data was performed. RESULTS: The analysis yielded three main themes: a sense of insecurity, role conflict, and a lack of support. CONCLUSION: This study explores nurses' perspectives on the factors impeding the implementation of the programme, which are identified as being insufficient protection and support on nurses at personal, sociocultural, infrastructural, and organizationallevels. IMPLICATIONS FOR NURSING MANAGEMENT: The study results will guide the department of nursing management to foster supportive work and social environment for nurses, which will decrease their feeling of insecurity and role conflicts and provides them enough infrastructural and organizational supports through proposing emergency code system and improving training system and team collaboration.


Assuntos
Enfermeiras e Enfermeiros , Serviços de Enfermagem , Humanos , Internet , Pesquisa Qualitativa
15.
Exp Cell Res ; 386(1): 111700, 2020 01 01.
Artigo em Inglês | MEDLINE | ID: mdl-31678213

RESUMO

The immune system is felt to play an essential role in pulmonary fibrosis (PF). CD4+CD25+ regulatory T cells (Tregs) are crucial in maintaining immune tolerance and immune homeostasis, but their role in the pathogenesis of PF is controversial and still unclear. We here explored the relationship between peripheral blood CD4+CD25+ Tregs and the course of bleomycin-induced PF in mice. Mouse PF models were established by intratracheal instillation of bleomycin. Lung histology, hydroxyproline, Th1/Th2 balanc, CD4+CD25+ Tregse were analyzed at the 3rd,7th,14th,21st and 28th days after instillation. CD4+CD25+ Tregs were also transferred into mice with or without PF by tail vein injection. The trend of CD4+CD25+ Tregs changes was increased firstly, decreased, increased again from 7th to 28th days after bleomycin instillation, which had great relevance with alveolitis and fibrosis scores. There also were high Th1 polarization index from 3rd to 14th days and high Th2 polarization index at 21st and 28th days after bleomycin treatment. CD4+CD25+ Tregs could promote the secretion of Th2 cytokines and inhibit the secretion of Th1 cytokines, allow the Th1/Th2 balance to Th2 direction in PF. Moreover, preventive adoptive transfer of CD4+CD25+ Tregs may ameliorate the process of PF, while acute adoptive transfer of CD4+CD25+ Tregs may aggravate the process of PF. These findings suggested that the dynamic changes of CD4+CD25+ Tregs as dependent factor might designate a different course of PF induced by bleomycin in mice, and might be a selected drug use indicator for therapy of PF.


Assuntos
Fibrose Pulmonar/imunologia , Linfócitos T Reguladores/imunologia , Animais , Bleomicina/toxicidade , Células Cultivadas , Citocinas/genética , Citocinas/metabolismo , Subunidade alfa de Receptor de Interleucina-2/genética , Subunidade alfa de Receptor de Interleucina-2/metabolismo , Masculino , Camundongos , Fibrose Pulmonar/sangue , Fibrose Pulmonar/etiologia , Linfócitos T Reguladores/citologia
16.
Sensors (Basel) ; 21(2)2021 Jan 17.
Artigo em Inglês | MEDLINE | ID: mdl-33477350

RESUMO

Nitrogen is an important indicator for monitoring wheat growth. The rapid development and wide application of non-destructive detection provide many approaches for estimating leaf nitrogen content (LNC) in wheat. Previous studies have shown that better results have been obtained in the estimation of LNC in wheat based on spectral features. However, the lack of automatically extracted features leads to poor universality of the estimation model. Therefore, a feature fusion method for estimating LNC in wheat by combining spectral features with deep features (spatial features) was proposed. The deep features were automatically obtained with a convolutional neural network model based on the PyTorch framework. The spectral features were obtained using spectral information including position features (PFs) and vegetation indices (VIs). Different models based on feature combination for evaluating LNC in wheat were constructed: partial least squares regression (PLS), gradient boosting decision tree (GBDT), and support vector regression (SVR). The results indicate that the model based on the fusion feature from near-ground hyperspectral imagery has good estimation effect. In particular, the estimation accuracy of the GBDT model is the best (R2 = 0.975 for calibration set, R2 = 0.861 for validation set). These findings demonstrate that the approach proposed in this study improved the estimation performance of LNC in wheat, which could provide technical support in wheat growth monitoring.


Assuntos
Triticum , Análise dos Mínimos Quadrados , Nitrogênio , Folhas de Planta , Análise Espectral
17.
Sichuan Da Xue Xue Bao Yi Xue Ban ; 52(4): 649-654, 2021 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-34323045

RESUMO

OBJECTIVE: To establish a nicotine intravenous self-administration rat model, and to examine, with this model, the effects of two flavoring additives, menthol and cineole, on nicotine dependence. METHODS: Thirty male Sprague-Dawley (SD) rats were included in the study. After jugular venous catheterization was performed, fixed concentration of nicotine was administered in order to train the rats and establish the rat model of intravenous self-administration groups, receiving intraperitoneal injection of menthol, cineole, and dimethyl sulfoxide (DMSO), the vehicle that was used for the control group. The rats were tested with different fixed-ratio (FR) schedules, including FR1 schedule, in which the rat received one nicotine infusion for every active nose poke, FR2 schedule, in which the rat received one nicotine infusion for every two active nose pokes, and FR5 schedule, in which the rat received one nicotine infusion for every five active nose pokes. The number of active and inactive poke responses and the number of nicotine infusion were documented accordingly. RESULTS: After 10 days of training in nicotine self-administration, the 30 rats demonstrated significant increase in the number of active poke responses and the number of nicotine infusion, which were maintained at a stable and relatively high level. The number of active poke responses was significantly higher that of inactive poke responses ( P< 0.001). The rat model of intravenous nicotine self-administration was successfully established. In the testing phase, under the FR2 schedule, the menthol group showed a reduced number of active poke responses ( P=0.020). Under the FR5 schedule, the groups showed obvious interaction between time and the number of active poke responses ( P<0.011), with the menthol group showing reduced number of active poke responses on day three ( P=0.011) and the cineole group showing rising number of active poke responses on day three ( P=0.003). The DMSO control group did not show any significant change. CONCLUSIONS: Menthol and cineole are shown to have an effect on nicotine dependence. When there is relative difficulty involved in obtaining nicotine, menthol suppresses nicotine dependence, whereas cineole enhances nicotine dependence.


Assuntos
Mentol , Tabagismo , Animais , Condicionamento Operante , Eucaliptol , Masculino , Ratos , Ratos Sprague-Dawley , Reforço Psicológico , Nicotiana
18.
Zhongguo Zhong Yao Za Zhi ; 46(3): 745-756, 2021 Feb.
Artigo em Chinês | MEDLINE | ID: mdl-33645043

RESUMO

Standards for seeds and seedlings of Chinese materia medica are very important to the production, quality control and management of seeds and seedlings of Chinese materia medica. In this paper, the current standards including international standards, national standards, industry standards, local standards and group standards before 2020, involving relevant standards for seeds and seedlings of Chinese materia medica, were comprehensively and systematically summarized. Relevant standards for seeds and seedlings of Chinese materia medica were analyzed based on the standard issue year, the source and types of Chinese materia medica, and whether they are included in the Pharmacopoeia of the People's Republic of China 2015. It is suggested that the standards for seed and seedling of Chinese materia medica shall be systematic, professional and feasible, so as to ensure the sould and sustainable development of the seed and seedling industry of Chinese materia medica.


Assuntos
Medicamentos de Ervas Chinesas , Materia Medica , China , Humanos , Medicina Tradicional Chinesa , Padrões de Referência , Plântula , Sementes
19.
Sensors (Basel) ; 19(20)2019 Oct 12.
Artigo em Inglês | MEDLINE | ID: mdl-31614815

RESUMO

Nitrogen (N) content is an important basis for the precise management of wheat fields. The application of unmanned aerial vehicles (UAVs) in agriculture provides an easier and faster way to monitor nitrogen content. Previous studies have shown that the features acquired from UAVs yield favorable results in monitoring wheat growth. However, since most of them are based on different vegetation indices, it is difficult to meet the requirements of accurate image interpretation. Moreover, resampling also easily ignores the structural features of the image information itself. Therefore, a spectral-spatial feature is proposed combining vegetation indices (VIs) and wavelet features (WFs), especially the acquisition of wavelet features from the UAV image, which was transformed from the spatial domain to the frequency domain with a wavelet transformation. In this way, the complete spatial information of different scales can be obtained to realize good frequency localization, scale transformation, and directional change. The different models based on different features were compared, including partial least squares regression (PLSR), support vector regression (SVR), and particle swarm optimization-SVR (PSO-SVR). The results showed that the accuracy of the model based on the spectral-spatial feature by combining VIs and WFs was higher than that of VIs or WF indices alone. The performance of PSO-SVR was the best (R2 = 0.9025, root mean square error (RMSE) = 0.3287) among the three regression algorithms regardless of the use of all the original features or the combination features. Our results implied that our proposed method could improve the estimation accuracy of aboveground nitrogen content of winter wheat from UAVs with consumer digital cameras, which have greater application potential in predicting other growth parameters.

20.
Sensors (Basel) ; 19(3)2019 Feb 12.
Artigo em Inglês | MEDLINE | ID: mdl-30759869

RESUMO

Unmanned aerial vehicle (UAV)-based multispectral sensors have great potential in crop monitoring due to their high flexibility, high spatial resolution, and ease of operation. Image preprocessing, however, is a prerequisite to make full use of the acquired high-quality data in practical applications. Most crop monitoring studies have focused on specific procedures or applications, and there has been little attempt to examine the accuracy of the data preprocessing steps. This study focuses on the preprocessing process of a six-band multispectral camera (Mini-MCA6) mounted on UAVs. First, we have quantified and analyzed the components of sensor error, including noise, vignetting, and lens distortion. Next, different methods of spectral band registration and radiometric correction were evaluated. Then, an appropriate image preprocessing process was proposed. Finally, the applicability and potential for crop monitoring were assessed in terms of accuracy by measurement of the leaf area index (LAI) and the leaf biomass inversion under variable growth conditions during five critical growth stages of winter wheat. The results show that noise and vignetting could be effectively removed via use of correction coefficients in image processing. The widely used Brown model was suitable for lens distortion correction of a Mini-MCA6. Band registration based on ground control points (GCPs) (Root-Mean-Square Error, RMSE = 1.02 pixels) was superior to that using PixelWrench2 (PW2) software (RMSE = 1.82 pixels). For radiometric correction, the accuracy of the empirical linear correction (ELC) method was significantly higher than that of light intensity sensor correction (ILSC) method. The multispectral images that were processed using optimal correction methods were demonstrated to be reliable for estimating LAI and leaf biomass. This study provides a feasible and semi-automatic image preprocessing process for a UAV-based Mini-MCA6, which also serves as a reference for other array-type multispectral sensors. Moreover, the high-quality data generated in this study may stimulate increased interest in remote high-efficiency monitoring of crop growth status.

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