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1.
J Agric Food Chem ; 72(14): 7684-7693, 2024 Apr 10.
Artigo em Inglês | MEDLINE | ID: mdl-38532701

RESUMO

Fosmidomycin (FOS) is a natural product inhibiting the DXR enzyme in the MEP pathway and has stimulated interest for finding more suitable FOS analogues. Herein, two series of FOS analogue hydroxamate-containing bisphosphonates as proherbicides were designed, with bisphosphonate replacing the phosphonic unit in FOS while retaining the hydroxamate (BPF series) or replacing it with retro-hydroxamate (BPRF series). The BPF series were synthesized through a three-step reaction sequence including Michael addition of vinylidenebisphosphonate, N-acylation, and deprotection, and the BPRF series were synthesized with a retro-Claisen condensation incorporated into the reaction sequence. Evaluation on model plants demonstrated several compounds having considerable herbicidal activities, and in particular, compound 8m exhibited multifold activity enhancement as compared to the control FOS. The proherbicide properties were comparatively validated. Furthermore, DXR enzyme assay, dimethylallyl pyrophosphate rescue, and molecular docking verified 8m to be a promising proherbicide candidate targeting the DXR enzyme. In addition, 8m also displayed good antimalarial activities.


Assuntos
Aldose-Cetose Isomerases , Antimaláricos , Fosfomicina , Fosfomicina/análogos & derivados , Difosfonatos , Simulação de Acoplamento Molecular , Fosfomicina/farmacologia , Aldose-Cetose Isomerases/metabolismo
2.
Pest Manag Sci ; 80(2): 846-856, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-37794283

RESUMO

BACKGROUND: The enzymes involved in the 2-C-methyl-d-erythritol 4-phosphate (MEP) pathway are attractive targets of a new mode of action for developing anti-infective drugs and herbicides, and inhibitors against 1-deoxy-d-xylulose 5-phosphate reductoisomerase (IspC), the second key enzyme in the pathway, have been intensively investigated; however, few works are reported regarding IspC inhibitors designed for new herbicide discovery. RESULTS: A series of fosmidomycin (FOS) analogs were designed with nitrogen-containing linkers replacing the trimethylene linker between the two active substructures of FOS, phosphonic acid and hydroxamic acid. Synthesis followed a facile three-step route of sequential aza-Michael addition of α-amino acids to dibenzyl vinylphosphonate, amidation of the amino acid carboxyl with O-benzyl hydroxylamine, and simultaneous removal of the benzyl protective groups. Biological activity evaluation of IspC and model plants revealed that some compounds had moderate enzyme and model plant growth inhibition effects. In particular, compound 10g, which has a N-(4-fluorophenylethyl) nitrogen-containing linker, exhibited the best plant inhibition activities, superior to the control FOS against the model plants Arabidopsis thaliana, Brassica napus L., Amaranthus retroflexus and Echinochloa crus-galli. A dimethylallyl pyrophosphate rescue assay on A. thaliana confirmed that both 10g and FOS exert their herbicidal activity by blocking the MEP pathway. This result consistent with molecular docking, which confirmed 10g and FOS binding to the IspC active site in a similar way. CONCLUSION: Compound 10g has excellent herbicidal activity and represents the first herbicide lead structure of a new mode of action that targets IspC enzyme in the MEP pathway. © 2023 Society of Chemical Industry.


Assuntos
Eritritol/análogos & derivados , Fosfomicina , Herbicidas , Fosfatos Açúcares , Simulação de Acoplamento Molecular , Fosfomicina/farmacologia , Herbicidas/química , Nitrogênio
3.
IEEE Trans Image Process ; 33: 366-381, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38117622

RESUMO

To enhance the viewer experience of standard dynamic range (SDR) video content on high dynamic range (HDR) displays, inverse tone mapping (ITM) is employed. Objective visual quality assessment (VQA) models are needed for effective evaluation of ITM algorithms. However, there is a lack of specialized VQA models for assessing the visual quality of inversely tone-mapped HDR videos (ITM-HDR-Videos). This paper addresses both an algorithmic and a dataset gap by introducing a novel SDR referenced HDR (SD-R-HD) VQA model tailored for ITM-HDR-Videos, along with the first public dataset specifically constructed for this purpose. The innovations of the SD-R-HD VQA model include 1) utilizing available SDR video as a reference signal, 2) extracting features that characterize standard ITM operations such as global mapping and local compensation, and 3) directly modeling interframe inconsistencies introduced by ITM operations. The newly created ITM-HDR-VQA dataset comprises 200 ITM-HDR-Videos annotated with mean opinion scores, gathered over 320 man-hours of psychovisual experiments. Experimental results demonstrate that the SD-R-HD VQA model significantly outperforms existing state-of-the-art VQA models.

4.
Molecules ; 28(22)2023 Nov 09.
Artigo em Inglês | MEDLINE | ID: mdl-38005231

RESUMO

Fosmidomycin (FOS) is a naturally occurring compound active against the 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR) enzyme in the 2-C-methyl-D-erythritol 4-phosphate (MEP) pathway, and using it as a template for lead structure design is an effective strategy to develop new active compounds. In this work, by replacing the hydroxamate unit of FOS with pyrazole, isoxazole and the related heterocycles that also have metal ion binding affinity, while retaining the monophosphonic acid in FOS or replacing it with a bisphosphonic acid group, heterocycle-containing mono- and bisphosphonic acid compounds as FOS analogs were designed. The key steps involved in the facile synthesis of these FOS analogs included the Michael addition of diethyl vinylphosphonate or tetraethyl vinylidenebisphosphonate to ß-dicarbonyl compounds and the subsequent cyclic condensation with hydrazine or hydroxylamine. Two additional isoxazolinone-bearing FOS analogs were synthesized via the Michaelis-Becker reaction with diethyl phosphite as a key step. The bioactivity evaluation on model plants demonstrated that several compounds have better herbicidal activities compared to FOS, with the most active compound showing a 3.7-fold inhibitory activity on Arabidopsis thaliana, while on the roots and stalks of Brassica napus L. and Echinochloa crus-galli in a pre-emergence inhibitory activity test, the activities of this compound were found to be 3.2- and 14.3-fold and 5.4- and 9.4-fold, respectively, and in a post-emergency activity test on Amaranthus retroflexus and Echinochloa crus-galli, 2.2- and 2.0-fold inhibition activities were displayed. Despite the significant herbicidal activity, this compound exhibited a DXR inhibitory activity lower than that of FOS but comparable to that of other non-hydroxamate DXR inhibitors, and the dimethylallyl pyrophosphate rescue assay gave no statistical significance, suggesting that a different target might be involved in the inhibiting process. This work demonstrates that using bioisosteric replacement can be considered as a valuable strategy to discover new FOS analogs that may have high herbicidal activities.


Assuntos
Aldose-Cetose Isomerases , Arabidopsis , Fosfomicina , Herbicidas , Fosfomicina/farmacologia , Arabidopsis/metabolismo
5.
Fitoterapia ; 166: 105472, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-36914013

RESUMO

Three new monomeric (1-3) and two newdimeric guaianolides (4 and 5), along with three known analogues (6-8) were isolated from the aerial part of Achillea alpina L. Compounds 1-3 were three novel 1,10-seco-guaianolides, while 4 and 5 were two novel 1,10-seco-guaianolides involved heterodimeric [4 + 2] adducts. The new structures were elucidated by analysis of spectroscopic data and quantum chemical calculations. All isolates were evaluated for their hypoglycemic activity with a glucose consumption model in palmitic acid (PA)-induced HepG2-insulin resistance (IR) cells, and compound 1 showed the most promising activity. A mechanistic study revealed that compound 1 appeared to mediate hypoglycemic activity via inhibition of the ROS/TXNIP/NLRP3/caspase-1 pathway.


Assuntos
Achillea , Sesquiterpenos , Achillea/química , Estrutura Molecular , Hipoglicemiantes/farmacologia , Extratos Vegetais/química , Sesquiterpenos/farmacologia , Sesquiterpenos/química
6.
J Enzyme Inhib Med Chem ; 38(1): 2166035, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36651035

RESUMO

High aldehyde dehydrogenase (ALDH) activity is a metabolic feature of adult stem cells and various cancer stem cells (CSCs). The ALDEFLUOR system is currently the most commonly used method for evaluating ALDH enzyme activity in viable cells. This system is applied extensively in the isolation of normal stem cells and CSCs from heterogeneous cell populations. For many years, ALDH1A1 has been considered the most important subtype among the 19 ALDH family members in determining ALDEFLUOR activity. However, in recent years, studies of many types of normal and tumour tissues have demonstrated that other ALDH subtypes can also significantly influence ALDEFLUOR activity. In this article, we briefly review the relationships between various members of the ALDH family and ALDEFLUOR activity. The clinical significance of these ALDH isoforms in different cancers and possible directions for future studies are also summarised.


Assuntos
Aldeído Desidrogenase , Neoplasias , Adulto , Humanos , Aldeído Desidrogenase/metabolismo , Relevância Clínica , Neoplasias/metabolismo , Isoformas de Proteínas/metabolismo , Células-Tronco Neoplásicas/metabolismo , Células-Tronco Neoplásicas/patologia , Linhagem Celular Tumoral
7.
IEEE Trans Pattern Anal Mach Intell ; 45(6): 7781-7798, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-36445991

RESUMO

Anomaly detection has wide applications in machine intelligence but is still a difficult unsolved problem. Major challenges include the rarity of labeled anomalies and it is a class highly imbalanced problem. Traditional unsupervised anomaly detectors are suboptimal while supervised models can easily make biased predictions towards normal data. In this paper, we present a new supervised anomaly detector through introducing the novel Ensemble Active Learning Generative Adversarial Network (EAL-GAN). EAL-GAN is a conditional GAN having a unique one generator versus multiple discriminators architecture where anomaly detection is implemented by an auxiliary classifier of the discriminator. In addition to using the conditional GAN to generate class balanced supplementary training data, an innovative ensemble learning loss function ensuring each discriminator makes up for the deficiencies of the others is designed to overcome the class imbalanced problem, and an active learning algorithm is introduced to significantly reduce the cost of labeling real-world data. We present extensive experimental results to demonstrate that the new anomaly detector consistently outperforms a variety of SOTA methods by significant margins.

8.
J Asian Nat Prod Res ; 25(4): 316-323, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35771726

RESUMO

Two new guaianolide-type sesquiterpenoids chrysanthemulides K and L (1 and 2), together with six known analogues (3-8), were isolated from an CH2Cl2 extract of the aerial parts of Chrysanthemum indicum. The structures of new compounds 1 and 2 were established by extensive spectroscopic analysis, including UV, IR, MS, NMR and computational electronic circular dichroism (ECD) methods. Inhibitory effects of all compounds on nitric oxide production were investigated in lipopolysaccharide (LPS)-induced RAW 264.7 cells. Results showed that compounds 1-8 displayed NO production inhibitory activity with IC50 values ranged from 3.5 to 34.3 µM.


Assuntos
Chrysanthemum , Sesquiterpenos , Animais , Camundongos , Chrysanthemum/química , Células RAW 264.7 , Sesquiterpenos/química , Extratos Vegetais/farmacologia , Espectroscopia de Ressonância Magnética , Óxido Nítrico , Estrutura Molecular , Lipopolissacarídeos/farmacologia
9.
RSC Adv ; 12(49): 31663-31670, 2022 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-36380931

RESUMO

In this work a carboxylated MWCNTs-chitosan composite sol-gel material was developed via one-step electrodeposition on a glassy carbon electrode as the cytosensing interface of a novel impedance cytosensor. SEM verified the formation of a three-dimensional hierarchical and porous microstructure favorable for the adhesion and spreading of osteoblastic MC3T3-E1 cells. By correlating impedance measurements with fluorescence microscopic characterization results, the cytosensor was demonstrated to have the ability to determine the MC3T3-E1 cell concentration ranging from 5 × 103 to 5 × 108 cell per mL with a detection limit of 1.8 × 103 cell per mL. The impedance cytosensor also enabled monitoring of the cell behavior regarding the processes of cell attachment, spreading, and proliferation in a label-free and quantitative manner. By taking advantage of this cytosensing method, investigating the effect of the C-terminal pentapeptide of osteogenic growth peptide (OGP(10-14)) on MC3T3-E1 cells was accomplished, demonstrating the potential for the application of OGP(10-14) in bone repair and regeneration. Therefore, this work afforded a convenient impedimetric strategy for osteoblastic cell counting and response monitoring that would be useful in evaluating the interactions between osteoblastic cells and specified drugs.

10.
Phytochemistry ; 202: 113297, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-35803306

RESUMO

Chemical investigation on the aerial part of Achillea alpina L. led to the isolation of twenty sesquiterpenoids. The structures of the undescribed achigermalides A-H were determined by extensive spectroscopic analysis, including NMR, HRESIMS, UV and IR, and their absolute configurations were established by computational electronic circular dichroism (ECD) method. The X-ray crystal structure for 8α-angeloxy-1ß,2ß:4ß,5ß-diepoxy-10ß-hydroxy-6ßH,7αH,11ßH-12,6α-guaianolide was reported for the first time. Glucose consumption was analyzed to investigate the effect of all compounds on palmitic acid (PA)-mediated insulin resistance (IR) in HepG2 cells, and achigermalides D-F, desacetylherbohde A, and 4E,10E-3-(2-methylbutyroyloxy)-germacra-4,10(1)-diene-12,6α-olide appreciably enhanced the glucose consumption at low concentrations of 1.56-6.25 µM. Moreover, achigermalide D decreased the expression of IL-1ß and the generation of reactive oxygen species (ROS), and also down-regulated the protein levels of TXNIP, NLRP3, caspase-1 and NF-κB in the Western blot analysis, suggesting achigermalide D mediated IR via the suppression of NLRP3 inflammasome pathway.


Assuntos
Achillea , Resistência à Insulina , Sesquiterpenos , Achillea/metabolismo , Glucose , Células Hep G2 , Humanos , Inflamassomos/metabolismo , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Ácido Palmítico/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Sesquiterpenos/química , Sesquiterpenos/farmacologia , Sesquiterpenos de Germacrano
11.
J Interv Card Electrophysiol ; 65(3): 643-649, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-35804256

RESUMO

BACKGROUND: Although fluoroless transseptal puncture (TSP) guided by intracardiac echocardiography (ICE) has been used for many years, there are no reports of an accurate site-specific method for TSP in detail, especially about the safety and efficiency of the method. This study aimed to compare the efficacy and safety of TSP guided by three-dimensional ICE using a fluoroless site-specific method with that of the conventional fluoroless method in patients with atrial fibrillation (AF). METHODS: This prospective study included 60 patients with AF scheduled for radiofrequency ablation who were assigned to undergo modified fluoroless site-specific TSP (SS-ICE group, n = 30) or conventional fluoroless TSP (C-ICE group, n = 30). TSP was guided by three-dimensional ICE in both study groups. RESULTS: All fluoroless TSP were performed successfully in both groups. There were no significant differences in patient characteristics, Pre-TSP time (11.3 ± 1.7 min vs. 11.1 ± 1.6 min, P = 0.822) and TSP time (3.4 ± 0.9 min vs. 3.5 ± 1.1 min, P = 0.772) between the SS-ICE group and the C-ICE group. The distance between the actual traversing point and the presetting point in the fossa ovalis was less than 5 mm in 87% of patients (26/30, 3.1 ± 1.2 mm) in the SS-ICE group. There were no TSP-related complications in either group. CONCLUSION: SS-ICE method is a simple, safe, and effective approach for fluoroless site-specific TSP.


Assuntos
Ecocardiografia , Humanos , Estudos Prospectivos
12.
Cancer Lett ; 536: 215662, 2022 06 28.
Artigo em Inglês | MEDLINE | ID: mdl-35331786

RESUMO

Metastasis is the leading cause of death for patients with colorectal cancer (CRC). The development of therapeutic regimens that selectively inhibit the biological processes involved in CRC cell dissemination is important. We used multiple Affymetrix DNA microarray hybridization datasets to identify genes related to metastasis and have significant prognostic value for patients with CRC. Quantitative real-time PCR, immunofluorescent and immunohistochemical staining were used to evaluate mRNA and protein expression. The function of aldehyde dehydrogenase 1A3 (ALDH1A3) in invasion was assessed by performing transwell assays and animal experiments. Real-time PCR, luciferase reporter assays, and western blotting were used to identify the genes regulated by ALDH1A3. Molecular docking, MTS assays, cellular thermal shift assays, isothermal titration calorimetry, microscale thermophoresis, and enzymatic activity assays were used to screen and verify the efficacy of the ALDH1A3-specific inhibitor YD1701 (dibenzo-30-crown10-ether). Finally, subcutaneous or orthotopic xenograft models were established to investigate the therapeutic potential of YD1701. Human ALDH1A3 was identified to correlate with a metastatic phenotype in CRC cells and a poor patient prognosis. Moreover, ALDH1A3 upregulated the expression of ZEB1 and SNAI2 by inhibiting miR-200 family members. The ALDH1A3-specific inhibitor YD1701 was screened, attenuated the invasion of CRC cells in vitro, and prolonged the survival of mice bearing subcutaneous or orthotopic xenografts. Our results show that ALDH1A3 promotes invasion and metastasis via the miR-200-ZEB1/SANI2 axis and is thus a plausible marker for predicting CRC progression. Inhibiting ALDH1A3 with the identified compound YD1701 might represent an effective therapeutic approach to prevent the metastasis of CRC.


Assuntos
Neoplasias Colorretais , MicroRNAs , Aldeído Desidrogenase/metabolismo , Animais , Linhagem Celular Tumoral , Movimento Celular/genética , Proliferação de Células , Neoplasias Colorretais/tratamento farmacológico , Neoplasias Colorretais/genética , Neoplasias Colorretais/metabolismo , Transição Epitelial-Mesenquimal/genética , Regulação Neoplásica da Expressão Gênica , Humanos , Camundongos , MicroRNAs/genética , Simulação de Acoplamento Molecular , Metástase Neoplásica
13.
IEEE Trans Image Process ; 31: 1475-1489, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35044915

RESUMO

Facial attributes in StyleGAN generated images are entangled in the latent space which makes it very difficult to independently control a specific attribute without affecting the others. Supervised attribute editing requires annotated training data which is difficult to obtain and limits the editable attributes to those with labels. Therefore, unsupervised attribute editing in an disentangled latent space is key to performing neat and versatile semantic face editing. In this paper, we present a new technique termed Structure-Texture Independent Architecture with Weight Decomposition and Orthogonal Regularization (STIA-WO) to disentangle the latent space for unsupervised semantic face editing. By applying STIA-WO to GAN, we have developed a StyleGAN termed STGAN-WO which performs weight decomposition through utilizing the style vector to construct a fully controllable weight matrix to regulate image synthesis, and employs orthogonal regularization to ensure each entry of the style vector only controls one independent feature matrix. To further disentangle the facial attributes, STGAN-WO introduces a structure-texture independent architecture which utilizes two independently and identically distributed (i.i.d.) latent vectors to control the synthesis of the texture and structure components in a disentangled way. Unsupervised semantic editing is achieved by moving the latent code in the coarse layers along its orthogonal directions to change texture related attributes or changing the latent code in the fine layers to manipulate structure related ones. We present experimental results which show that our new STGAN-WO can achieve better attribute editing than state of the art methods.


Assuntos
Semântica
14.
IEEE Trans Neural Netw Learn Syst ; 33(10): 5626-5640, 2022 10.
Artigo em Inglês | MEDLINE | ID: mdl-33900923

RESUMO

Class imbalance is a prevalent phenomenon in various real-world applications and it presents significant challenges to model learning, including deep learning. In this work, we embed ensemble learning into the deep convolutional neural networks (CNNs) to tackle the class-imbalanced learning problem. An ensemble of auxiliary classifiers branching out from various hidden layers of a CNN is trained together with the CNN in an end-to-end manner. To that end, we designed a new loss function that can rectify the bias toward the majority classes by forcing the CNN's hidden layers and its associated auxiliary classifiers to focus on the samples that have been misclassified by previous layers, thus enabling subsequent layers to develop diverse behavior and fix the errors of previous layers in a batch-wise manner. A unique feature of the new method is that the ensemble of auxiliary classifiers can work together with the main CNN to form a more powerful combined classifier, or can be removed after finished training the CNN and thus only acting the role of assisting class imbalance learning of the CNN to enhance the neural network's capability in dealing with class-imbalanced data. Comprehensive experiments are conducted on four benchmark data sets of increasing complexity (CIFAR-10, CIFAR-100, iNaturalist, and CelebA) and the results demonstrate significant performance improvements over the state-of-the-art deep imbalance learning methods.


Assuntos
Aprendizado Profundo , Redes Neurais de Computação
15.
Clin Transl Immunology ; 10(10): e1342, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34646556

RESUMO

OBJECTIVES: Immunoglobulin A vasculitis (IgAV), previously known as Henoch-Schönlein purpura, is the most common vasculitis that has a classical skin manifestation of palpable purpuric rash. Factors pertinent to IgAV remain inadequately understood. Here, we aimed to examine the gut microbiome shifts associated with IgAV and its recovery. METHODS: Stool samples were collected from 10 children with IgAV (6-14 years old) before and after a multi-drug therapy, along with 9 age-matched healthy children. The samples were subjected to metagenomic analyses to investigate the taxonomic and functional shifts of the gut microbiome. RESULTS: The analyses revealed that compared with healthy controls, treatment-naïve patients exhibited substantial taxonomic and functional alterations of gut microbiota, including 104 IgAV-depleted species and 7 IgAV-elevated species (FDR < 0.05). After treatment, the IgAV patients displayed a partial restoration of the microbiota shifts, as the relative abundances of some biomarkers (e.g. 9 genera and 22 species) became comparable (FDR > 0.1) between the patients and healthy controls. The treatment-responsive features included Weissella, Faecalibacterium prausnitzii and Bifidobacterium pseudocatenulatum and three components of a putative glutamine transport system. Importantly, gram-positive bacteria accounted for over 85% of the numbers and total relative abundance of the species that were associated with IgAV and responsive to the treatment. In addition, of the 122 IgAV-depleted bacterial genes, 82 were mainly contributed by gram-positive bacteria and 12 by gram-negative bacteria. CONCLUSIONS: Gram-positive bacteria are the main drivers underlying the gut microbiome shifts of IgAV, which may assist rational management of the disease.

16.
World J Clin Cases ; 9(24): 7146-7153, 2021 Aug 26.
Artigo em Inglês | MEDLINE | ID: mdl-34540971

RESUMO

BACKGROUND: Neuroendocrine carcinoma of the breast (NECB) is a rare type of malignant tumor. Due to the rarity of NECB, the relevant literature mostly comprises case reports. Available data on treatment options for NECB are very limited. CASE SUMMARY: A 62-year-old woman presented to our hospital in October 2016 for intermittent vomiting and diarrhea and masses in the liver found on abdominal computed tomography (CT) imaging. She was diagnosed in July 2012 with neuroendocrine carcinoma of the right breast in local hospital. The patient initially presented with a painful lesion of the right breast. She then undergone surgical resection and adjuvant chemotherapy with pirarubicin and paclitaxel for four cycles as well as endocrine therapy. She was regularly followed every 3 mo after surgery. Enhanced abdominal CT imaging at our hospital revealed multiple suspicious masses in the liver with the largest lesion measuring 8.4 cm × 6.3 cm. Chest CT revealed masses in the anterior chest wall and lung. Core needle biopsy of the lesion revealed liver metastases of NECB. A bone scan showed right second anterior rib metastases. Upper endoscopy and colonoscopy did not provide any evidence of another possible primary tumor. She stopped receiving endocrine therapy and then received etoposide and cisplatin (EP) chemotherapy as a first-line treatment regimen for six cycles at our hospital after liver, bone, and lung metastases. On October 2017, the chemotherapy regimen was changed to S-1 (40 mg twice daily, days 1-14) combined with temozolomide (200 mg once daily, days 10-14) (STEM) every 21 d as a second-line treatment regimen due to disease progression. Progression-free survival (PFS) and adverse effects after treatment were analyzed, and the efficacy of the STEM regimen was assessed using RECIST version 1.1. This patient achieved a partial response after using the STEM regimen, with a PFS of 23 mo. Adverse effects included only grade 1 digestive tract reactions with no need for a reduction in chemotherapy. CONCLUSION: This case report suggests that the STEM regimen may be effective and well tolerated as the second-line treatment for advanced NECB. STEM is still highly effective in patients who show disease progression with the EP regimen. More evidence is needed to prove the validity of STEM.

17.
RSC Adv ; 11(28): 16955-16961, 2021 May 06.
Artigo em Inglês | MEDLINE | ID: mdl-35479714

RESUMO

4-Substituted catechols with different C[double bond, length as m-dash]C bonds as urushiol analogues were synthesized through the a three-step route including reductive amination reaction of 3,4-dihydroxybenzaldehyde with N-Boc-piperazine, Boc deprotection, and amidation with various fatty acids. Electrochemical polymerization of these analogues on a copper surface afforded robust coatings with desirable adhesive force, hydrophobicity and thermal stability. Cyclic voltammetry and infrared spectroscopic characterizations revealed that the coating formation of urushiol analogues resulted from the electrooxidation-induced radical coupling of phenoxyl radicals with a phenyl ring and the side chain C[double bond, length as m-dash]C bond. The coating of the urushiol analogue bearing only one side chain C[double bond, length as m-dash]C bond exhibited the best performance in copper corrosion inhibition, with an inhibition efficiency of 99.99% and long-term effect (99.9% after 4 weeks of immersion in 3.5 wt% NaCl). The desired performance of these urushiol analogues suggests that they could be of practical applications as an alternative to the resource-limited natural urushiol.

18.
IEEE Trans Med Imaging ; 40(1): 116-128, 2021 01.
Artigo em Inglês | MEDLINE | ID: mdl-32915729

RESUMO

Accurately locating the fovea is a prerequisite for developing computer aided diagnosis (CAD) of retinal diseases. In colour fundus images of the retina, the fovea is a fuzzy region lacking prominent visual features and this makes it difficult to directly locate the fovea. While traditional methods rely on explicitly extracting image features from the surrounding structures such as the optic disc and various vessels to infer the position of the fovea, deep learning based regression technique can implicitly model the relation between the fovea and other nearby anatomical structures to determine the location of the fovea in an end-to-end fashion. Although promising, using deep learning for fovea localisation also has many unsolved challenges. In this paper, we present a new end-to-end fovea localisation method based on a hierarchical coarse-to-fine deep regression neural network. The innovative features of the new method include a multi-scale feature fusion technique and a self-attention technique to exploit location, semantic, and contextual information in an integrated framework, a multi-field-of-view (multi-FOV) feature fusion technique for context-aware feature learning and a Gaussian-shift-cropping method for augmenting effective training data. We present extensive experimental results on two public databases and show that our new method achieved state-of-the-art performances. We also present a comprehensive ablation study and analysis to demonstrate the technical soundness and effectiveness of the overall framework and its various constituent components.


Assuntos
Fóvea Central , Disco Óptico , Cor , Fóvea Central/diagnóstico por imagem , Fundo de Olho , Disco Óptico/diagnóstico por imagem , Retina
19.
IEEE Trans Image Process ; 30: 176-190, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33119509

RESUMO

Fog removal from an image is an active research topic in computer vision. However, current literature is weak in the following two areas which in many ways are hindering progress for developing defogging algorithms. First, there is no true real-world and naturally occurring foggy image datasets suitable for developing defogging models. Second, there is no suitable mathematically simple and easy to use image quality assessment (IQA) methods for evaluating the visual quality of defogged images. We address these two aspects in this paper. We first introduce a new foggy image dataset called multiple real-world foggy image dataset (MRFID). MRFID contains foggy and clear images of 200 outdoor scenes. For each scene, one clear image and 4 foggy images of different densities defined as slightly foggy, moderately foggy, highly foggy, and extremely foggy, are manually selected from images taken from these scenes over the course of one calendar year. We then process the foggy images of MRFID using 16 defogging methods to obtain 12,800 defogged images (DFIs) and perform a comprehensive subjective evaluation of the visual quality of the DFIs. Through collecting the mean opinion score (MOS) of 120 subjects and evaluating a variety of fog-relevant image features, we have developed a new Fog-relevant Feature based SIMilarity index (FRFSIM) for assessing the visual quality of DFIs. We present extensive experimental results to show that our new visual quality assessment measure, the FRFSIM, is more consistent with the MOS than other IQA methods and is therefore more suitable for evaluating defogged images than other state-of-the-art IQA methods. Our dataset and relevant code are available at http://www.vistalab.ac.cn/MRFID-for-defogging/.

20.
J Biophotonics ; 14(3): e202000415, 2021 03.
Artigo em Inglês | MEDLINE | ID: mdl-33231354

RESUMO

Cold atmospheric plasma (CAP) applications can potentially lead to effective therapy for numerous skin diseases. Our aim is to systematically review the available data and map the use of CAP in dermatology. PubMed, Embase and Web of science were explored before 2020 for studies regarding the use of CAP in dermatology. A total of 166 studies were finally included. 74.1% of these studies used indirect CAP sources. Most studies used plasma jet (67.5%). Argon was the mostly used working gas (48.2%). Plasma application itself could be direct (89.2%) and indirect (16.3%). The proportion of studies with in vivo results remained 57.2%, of which most concerned direct plasma treatment (97.9%). Analyses performed indicate that CAP has been beneficial in many skin disorders. While, most CAP applications were focused on wound healing and melanoma treatment. This study provides a brief overview of CAP sources and relative medical applications in dermatology.


Assuntos
Dermatologia , Gases em Plasma , Dermatopatias , Humanos , Plasma , Gases em Plasma/uso terapêutico , Dermatopatias/terapia , Cicatrização
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