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1.
J Nat Prod ; 2024 Apr 18.
Artigo em Inglês | MEDLINE | ID: mdl-38634860

RESUMO

An unprecedented di-seco-indole diterpenoid, peniditerpenoid A (1), and a rare N-oxide-containing indole diterpenoid derivative, peniditerpenoid B (2), together with three known ones (3-5), were obtained from the mangrove-sediment-derived fungus Penicillium sp. SCSIO 41411. Their structures were determined by the analysis of spectroscopic data, quantum chemical calculations, and X-ray diffraction analyses. Peniditerpenoid A (1) inhibited lipopolysaccharide-induced NF-κB with an IC50 value of 11 µM and further effectively prevented RANKL-induced osteoclast differentiation in bone marrow macrophages. In vitro studies demonstrated that 1 exerted significant inhibition of NF-κB activation in the classical pathway by preventing TAK1 activation, IκBα phosphorylation, and p65 translocation. Furthermore, 1 effectively reduced the level of NFATc1 activation, resulting in the attenuation of osteoclast differentiation. Our findings suggest that 1 holds promise as an inhibitor with significant potential for the treatment of diseases related to osteoporosis.

2.
J Nat Prod ; 87(2): 322-331, 2024 02 23.
Artigo em Inglês | MEDLINE | ID: mdl-38334086

RESUMO

A strategy integrating in silico molecular docking with LXRα and phenotypic assays was adopted to discover anti-hypercholesterolemia agents in a small library containing 205 marine microorganism-derived natural products, collected by our group in recent years. Two fumitremorgin derivatives, 12R,13S-dihydroxyfumitremorgin C (1) and tryprostatin A (3), were identified as potential LXRα agonists, by real-time qPCR and Western blot (WB) analysis, together with a surface plasmon resonance (SPR) assay. The anti-hypercholesterolemic effects of 1 and 3, together with their mechanisms, were investigated in depth using different cell and mouse models, among which the study of LXRα is of crucial importance. Compound 1 or 3 exhibited the capacity to effectively reverse excessive lipid accumulation in a hepatic steatosis cell model and significantly reduce liver damage and blood cholesterol levels in high cholesterol diet (HCD)-fed wild-type mice, whereas those beneficial effects were completely nullified in HCD-fed LXRα-knockout mice. Furthermore, 1 and 3 outperformed common LXRα agonists by suppressing the expression of sterol regulatory element-binding protein 1 (SREBP1) in HCD-fed mice, mitigating lipotoxicity. Thus, this study highlights the discovery of two marine microorganism-derived anti-hypercholesterolemia agents targeting LXRα.


Assuntos
Hipercolesterolemia , Receptores Nucleares Órfãos , Animais , Camundongos , Colesterol/metabolismo , Hipercolesterolemia/tratamento farmacológico , Fígado , Receptores X do Fígado/metabolismo , Camundongos Knockout , Simulação de Acoplamento Molecular , Receptores Nucleares Órfãos/metabolismo , Receptores Nucleares Órfãos/farmacologia
3.
BMC Plant Biol ; 24(1): 157, 2024 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-38424498

RESUMO

BACKGROUND: D-type cyclins (CYCD) regulate the cell cycle G1/S transition and are thus closely involved in cell cycle progression. However, little is known about their functions in rice. RESULTS: We identified 14 CYCD genes in the rice genome and confirmed the presence of characteristic cyclin domains in each. The expression of the OsCYCD genes in different tissues was investigated. Most OsCYCD genes were expressed at least in one of the analyzed tissues, with varying degrees of expression. Ten OsCYCD proteins could interact with both retinoblastoma-related protein (RBR) and A-type cyclin-dependent kinases (CDKA) forming holistic complexes, while OsCYCD3;1, OsCYCD6;1, and OsCYCD7;1 bound only one component, and OsCYCD4;2 bound to neither protein. Interestingly, all OsCYCD genes except OsCYCD7;1, were able to induce tobacco pavement cells to re-enter mitosis with different efficiencies. Transgenic rice plants overexpressing OsCYCD2;2, OsCYCD6;1, and OsCYCD7;1 (which induced cell division in tobacco with high-, low-, and zero-efficiency, respectively) were created. Higher levels of cell division were observed in both the stomatal lineage and epidermal cells of the OsCYCD2;2- and OsCYCD6;1-overexpressing plants, with lower levels seen in OsCYCD7;1-overexpressing plants. CONCLUSIONS: The distinct expression patterns and varying effects on the cell cycle suggest different functions for the various OsCYCD proteins. Our findings will enhance understanding of the CYCD family in rice and provide a preliminary foundation for the future functional verification of these genes.


Assuntos
Ciclinas , Oryza , Ciclinas/genética , Ciclinas/metabolismo , Oryza/genética , Oryza/metabolismo , Fosforilação , Quinases Ciclina-Dependentes/genética , Quinases Ciclina-Dependentes/metabolismo , Ciclo Celular/genética , Proteína do Retinoblastoma/genética , Proteína do Retinoblastoma/metabolismo , Mitose
4.
IEEE Trans Image Process ; 33: 1403-1418, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38358873

RESUMO

Bimodal objects, such as the checkerboard pattern used in camera calibration, markers for object tracking, and text on road signs, to name a few, are prevalent in our daily lives and serve as a visual form to embed information that can be easily recognized by vision systems. While binarization from intensity images is crucial for extracting the embedded information in the bimodal objects, few previous works consider the task of binarization of blurry images due to the relative motion between the vision sensor and the environment. The blurry images can result in a loss in the binarization quality and thus degrade the downstream applications where the vision system is in motion. Recently, neuromorphic cameras offer new capabilities for alleviating motion blur, but it is non-trivial to first deblur and then binarize the images in a real-time manner. In this work, we propose an event-based binary reconstruction method that leverages the prior knowledge of the bimodal target's properties to perform inference independently in both event space and image space and merge the results from both domains to generate a sharp binary image. We also develop an efficient integration method to propagate this binary image to high frame rate binary video. Finally, we develop a novel method to naturally fuse events and images for unsupervised threshold identification. The proposed method is evaluated in publicly available and our collected data sequence, and shows the proposed method can outperform the SOTA methods to generate high frame rate binary video in real-time on CPU-only devices.

5.
J Med Chem ; 67(4): 2602-2618, 2024 Feb 22.
Artigo em Inglês | MEDLINE | ID: mdl-38301128

RESUMO

To discover novel osteoclast-targeting antiosteoporosis leads from natural products, we identified 40 tanzawaic acid derivatives, including 22 new ones (1-8, 14-19, 27-32, 37, and 38), from the South China Sea mangrove-derived fungus Penicillium steckii SCSIO 41025. Penicisteck acid F (2), one of the new derivatives showing the most potent NF-κB inhibitory activity, remarkably inhibited osteoclast generation in vitro. Mechanistically, 2 reduced RANKL-induced IκBα degradation, NF-κB p65 nuclear translocation, the activation and nuclear translocation of NFATc1, and the relevant mRNA expression. NF-κB p65 could be a potential molecular target for 2, which has been further determined by the cellular thermal shift assay, surface plasmon resonance, and the gene knock-down assay. Moreover, 2 could also alleviate osteoporosis in ovariectomized mice by reducing the quantities of osteoclasts. Our finding offered a novel potential inhibitor of osteoclastogenesis and osteoporosis for further development of potent antiosteoporosis agents.


Assuntos
Reabsorção Óssea , Osteoporose , Animais , Camundongos , NF-kappa B/metabolismo , Osteogênese , Regulação para Baixo , Reabsorção Óssea/tratamento farmacológico , Osteoclastos/metabolismo , Osteoporose/tratamento farmacológico , Ligante RANK/metabolismo , Diferenciação Celular , Fatores de Transcrição NFATC/metabolismo
6.
J Fungi (Basel) ; 10(1)2024 Jan 03.
Artigo em Inglês | MEDLINE | ID: mdl-38248947

RESUMO

Acremonium fungi is one of the greatest and most complex genera in Hyphomycetes, comprising 130 species of marine and terrestrial sources. The past decades have witnessed substantial chemical and biological investigations on the diverse secondary metabolites from the Acremonium species. To date, over 600 compounds with abundant chemical types as well as a wide range of bioactivities have been obtained from this genus, attracting considerable attention from chemists and pharmacologists. This review mainly summarizes the sources, chemical structures, and biological activities of 115 recently reported new compounds from the genus Acremonium from December 2016 to September 2023. They are structurally classified into terpenoids (42%), peptides (29%), polyketides (20%), and others (9%), among which marine sources are predominant (68%). Notably, these compounds were primarily screened with cytotoxic, antibacterial, and anti-inflammatory activities. This paper provides insights into the exploration and utilization of bioactive compounds in this genus, both within the scientific field and pharmaceutical industry.

7.
Phytomedicine ; 123: 155219, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38056150

RESUMO

BACKGROUND: Lung cancer is one of the deadliest cancers world-wide and immunotherapy has been considered as a promising therapeutic strategy. Previously, our study found that tannins in Phyllanthus emblica L. (PTF) could inhibit the growth of tumor by activating the immune response in liver cancer, and also exhibited a cytotoxicity on human lung cancer cells A549, H460, H1703 in vitro. OBJECTIVE: To explore whether PTF inhibited the growth of lung cancer through its immune-regulating function and to clarify underlying mechanisms. METHODS: The induction of immunogenic cell death (ICD) were characterized by calreticulin exposure, extracellular ATP secretion, and High Mobility Group Box 1(HMGB1) release both in vivo using LLC-derived xenograft tumor model and in vitro using both mouse LLC and human A549 cancer cells. RESULTS: PTF inhibited lung cancer cells growth and tumorigenesis in vivo/vitro and promoted anti-tumor immune responses. We further found that PTF could induce ICD, which then activated Type I interferon responses and CXCL9/10-mediated chemotaxis. Mechanistically, PTF induced the formation of intracellular protein aggregates and following activation of PERK/ATF4/CHOP-dependent endoplasmic reticulum stress-related ICD. Moreover, PTF improved the antitumor efficacy of cisplatin by inducing ICD both in vitro and in vivo. Finally, we screened out 5 components from PTF, including gallocatechin, gallic acid, methyl gallate, ethyl gallate and ellagic acid, which could induce ICD in vitro and might be considered as the potential antitumor pharmacodynamic substances. CONCLUSION: In conclusion, PTF inhibits the growth of lung cancer by triggering ICD and remodeling the tumor microenvironment, suggesting that PTF may have promising prospects as an adjacent immunotherapy for cancers.


Assuntos
Neoplasias Pulmonares , Phyllanthus emblica , Humanos , Animais , Camundongos , Neoplasias Pulmonares/tratamento farmacológico , Neoplasias Pulmonares/patologia , Cisplatino/uso terapêutico , Taninos/farmacologia , Morte Celular Imunogênica , Estresse do Retículo Endoplasmático , Linhagem Celular Tumoral , Microambiente Tumoral
8.
Comput Struct Biotechnol J ; 21: 5839-5850, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38074472

RESUMO

Generative adversarial networks (GANs) have successfully generated functional protein sequences. However, traditional GANs often suffer from inherent randomness, resulting in a lower probability of obtaining desirable sequences. Due to the high cost of wet-lab experiments, the main goal of computer-aided antibody optimization is to identify high-quality candidate antibodies from a large range of possibilities, yet improving the ability of GANs to generate these desired antibodies is a challenge. In this study, we propose and evaluate a new GAN called the Language Model Guided Antibody Generative Adversarial Network (AbGAN-LMG). This GAN uses a language model as an input, harnessing such models' powerful representational capabilities to improve the GAN's generation of high-quality antibodies. We conducted a comprehensive evaluation of the antibody libraries and sequences generated by AbGAN-LMG for COVID-19 (SARS-CoV-2) and Middle East Respiratory Syndrome (MERS-CoV). Results indicate that AbGAN-LMG has learned the fundamental characteristics of antibodies and that it improved the diversity of the generated libraries. Additionally, when generating sequences using AZD-8895 as the target antibody for optimization, over 50% of the generated sequences exhibited better developability than AZD-8895 itself. Through molecular docking, we identified 70 antibodies that demonstrated higher affinity for the wild-type receptor-binding domain (RBD) of SARS-CoV-2 compared to AZD-8895. In conclusion, AbGAN-LMG demonstrates that language models used in conjunction with GANs can enable the generation of higher-quality libraries and candidate sequences, thereby improving the efficiency of antibody optimization. AbGAN-LMG is available at http://39.102.71.224:88/.

9.
BMC Bioinformatics ; 24(1): 486, 2023 Dec 19.
Artigo em Inglês | MEDLINE | ID: mdl-38114906

RESUMO

BACKGROUND: Automatic and accurate extraction of diverse biomedical relations from literature is a crucial component of bio-medical text mining. Currently, stacking various classification networks on pre-trained language models to perform fine-tuning is a common framework to end-to-end solve the biomedical relation extraction (BioRE) problem. However, the sequence-based pre-trained language models underutilize the graphical topology of language to some extent. In addition, sequence-oriented deep neural networks have limitations in processing graphical features. RESULTS: In this paper, we propose a novel method for sentence-level BioRE task, BioEGRE (BioELECTRA and Graph pointer neural net-work for Relation Extraction), aimed at leveraging the linguistic topological features. First, the biomedical literature is preprocessed to retain sentences involving pre-defined entity pairs. Secondly, SciSpaCy is employed to conduct dependency parsing; sentences are modeled as graphs based on the parsing results; BioELECTRA is utilized to generate token-level representations, which are modeled as attributes of nodes in the sentence graphs; a graph pointer neural network layer is employed to select the most relevant multi-hop neighbors to optimize representations; a fully-connected neural network layer is employed to generate the sentence-level representation. Finally, the Softmax function is employed to calculate the probabilities. Our proposed method is evaluated on three BioRE tasks: a multi-class (CHEMPROT) and two binary tasks (GAD and EU-ADR). The results show that our method achieves F1-scores of 79.97% (CHEMPROT), 83.31% (GAD), and 83.51% (EU-ADR), surpassing the performance of existing state-of-the-art models. CONCLUSION: The experimental results on 3 biomedical benchmark datasets demonstrate the effectiveness and generalization of BioEGRE, which indicates that linguistic topology and a graph pointer neural network layer explicitly improve performance for BioRE tasks.


Assuntos
Idioma , Redes Neurais de Computação , Mineração de Dados , Linguística , Processamento de Linguagem Natural
10.
Mar Drugs ; 21(12)2023 Nov 28.
Artigo em Inglês | MEDLINE | ID: mdl-38132937

RESUMO

The Mycobacterium tuberculosis (MTB) infection causes tuberculosis (TB) and has been a long-standing public-health threat. It is urgent that we discover novel antitubercular agents to manage the increased incidence of multidrug-resistant (MDR) or extensively drug-resistant (XDR) strains of MTB and tackle the adverse effects of the first- and second-line antitubercular drugs. We previously found that gliotoxin (1), 12, 13-dihydroxy-fumitremorgin C (2), and helvolic acid (3) from the cultures of a deep-sea-derived fungus, Aspergillus sp. SCSIO Ind09F01, showed direct anti-TB effects. As macrophages represent the first line of the host defense system against a mycobacteria infection, here we showed that the gliotoxin exerted potent anti-tuberculosis effects in human THP-1-derived macrophages and mouse-macrophage-leukemia cell line RAW 264.7, using CFU assay and laser confocal scanning microscope analysis. Mechanistically, gliotoxin apparently increased the ratio of LC3-II/LC3-I and Atg5 expression, but did not influence macrophage polarization, IL-1ß, TNF-a, IL-10 production upon MTB infection, or ROS generation. Further study revealed that 3-MA could suppress gliotoxin-promoted autophagy and restore gliotoxin-inhibited MTB infection, indicating that gliotoxin-inhibited MTB infection can be treated through autophagy in macrophages. Therefore, we propose that marine fungi-derived gliotoxin holds the promise for the development of novel drugs for TB therapy.


Assuntos
Gliotoxina , Mycobacterium tuberculosis , Tuberculose , Animais , Camundongos , Humanos , Gliotoxina/farmacologia , Tuberculose/tratamento farmacológico , Antituberculosos/farmacologia , Antituberculosos/uso terapêutico , Macrófagos , Fungos , Autofagia
11.
MAbs ; 15(1): 2285904, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38010801

RESUMO

Prior research has generated a vast amount of antibody sequences, which has allowed the pre-training of language models on amino acid sequences to improve the efficiency of antibody screening and optimization. However, compared to those for proteins, there are fewer pre-trained language models available for antibody sequences. Additionally, existing pre-trained models solely rely on embedding representations using amino acids or k-mers, which do not explicitly take into account the role of secondary structure features. Here, we present a new pre-trained model called BERT2DAb. This model incorporates secondary structure information based on self-attention to learn representations of antibody sequences. Our model achieves state-of-the-art performance on three downstream tasks, including two antigen-antibody binding classification tasks (precision: 85.15%/94.86%; recall:87.41%/86.15%) and one antigen-antibody complex mutation binding free energy prediction task (Pearson correlation coefficient: 0.77). Moreover, we propose a novel method to analyze the relationship between attention weights and contact states of pairs of subsequences in tertiary structures. This enhances the interpretability of BERT2DAb. Overall, our model demonstrates strong potential for improving antibody screening and design through downstream applications.


Assuntos
Aminoácidos , Proteínas , Sequência de Aminoácidos , Proteínas/química , Aminoácidos/química , Estrutura Secundária de Proteína , Anticorpos
12.
Waste Manag ; 171: 207-217, 2023 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-37666146

RESUMO

The acceptance of battery electric vehicles (BEVs) is continuously increasing to mitigate CO2 emissions, resulting in an increase in the future material demand for LIBs. Therefore, the proper handling of End-of-life (EOL) BEV batteries requires careful attention to mitigate the supply chain issues for future LIBs materials, especially in Asia. A system dynamics model assessment was performed to evaluate the EOL of LIBs by considering the dynamic lifespan, recovery rate, and economic value under three growth rate scenarios in Asia from 2022 to 2030, depending on the battery chemistry over time. We find that comparing three different scenarios to materials demand, the result showed that materials demand for LIBs is greater in higher scenarios as compared with lower and reference scenarios. Moreover, in the low scenario, the nickel demand and recovery from end-of-life LIBs BEVs will achieve 244.0 and 43.28 kt in 2030. Based on the dynamic economic evaluation, an overall, higher potential economic value of all materials would achieve around 1471 million USD in 2030 in the low scenario. This study manifested that recycling LIBs materials has enormous economic potential and would be a step towards economic sustainability, especially in Asia in the near future.

13.
Food Funct ; 14(18): 8661-8662, 2023 Sep 19.
Artigo em Inglês | MEDLINE | ID: mdl-37655684

RESUMO

Correction for 'Moringa oleifera leaf polysaccharides exert anti-lung cancer effects upon targeting TLR4 to reverse the tumor-associated macrophage phenotype and promote T-cell infiltration' by Shukai Wang et al., Food Funct., 2023, 14, 4607-4620, https://doi.org/10.1039/D2FO03685A.

14.
Chem Biodivers ; 20(9): e202300851, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37584103

RESUMO

In our search for peroxisome proliferator-activated receptor (PPAR) agonists, five undescribed compounds, namely two acyclic diterpenes (1 and 2; cladopsol A and cladopsol B), two sesquiterpenes (3 and 4; cladopsol C and cladopsol D), and one C21-ecdysteroid (5; cladopsol E), and 15 known compounds were isolated from the jellyfish-derived fungus - Cladosporium oxysporum. The structures of the undescribed compounds were defined using UV, NMR, HR-ESI-MS, and electronic circular dichroism (ECD) spectroscopy and a modified Mosher's method. Luciferase reporter assay and docking analysis suggested that cladopsol B may function as a PPAR-γ partial agonist with a potential antidiabetic lead which may evade the side effects of full agonists. Moreover, cladopsol B stimulated glucose uptake in HepG2 cells with an efficacy comparable to that of rosiglitazone, but with less side effect induced by lipid accumulation in 3T3-L1 cells. Therefore, cladopsol B could serve as a molecular skeleton in a study of advanced antidiabetic lead with less side effect.


Assuntos
Agonistas PPAR-gama , Receptores Ativados por Proliferador de Peroxissomo , Hipoglicemiantes/farmacologia , Cladosporium , PPAR gama/agonistas
15.
Sheng Wu Gong Cheng Xue Bao ; 39(7): 2818-2838, 2023 Jul 25.
Artigo em Chinês | MEDLINE | ID: mdl-37584134

RESUMO

Phenylalanine ammonia-lyase (PAL) is the key entry enzyme of plant phenylpropanoid pathway. It plays an important role in the biosynthesis of podophyllotoxin, an anti-tumor lignan that is currently produced from its main natural source Sinopodophyllum hexandrum (Royle) Ying. In this study, we cloned the gene ShPAL encoding phenylalanine ammonia-lyase by RT-PCR from the root of S. hexandrum ecotype inhabited in the Aba' district, Sichuan, based on its public SRA transcriptome data-package. Bioinformatics analyses showed that the ShPAL-encoded protein is composed of 711 amino acids, contains the conserved domains of PAL, and has the signature motif within the active center of aromatic ammonia-lyases. Moreover, ShPAL protein was predicted to have a secondary structure mainly composed of α-helix and random coil, a typical 'seahorse' shape monomer tertiary structure, and a homologous tetramer three-dimensional structure by Swiss-Modelling. The phylogenetic lineage analysis indicated ShPAL was of the highest sequence identity and the shortest evolutionary distance with the PAL of Epimedium sagittatum from the same Berberidaceae family. Subcellular localization experiments showed that ShPAL protein was mainly distributed in the cytoplasm, despite of a minority on the endoplasmic reticulum membrane. Furthermore, ShPAL protein was recombinantly expressed in Escherichia coli and purified by histidine-tag affinity chromatography. Its enzymatic activity was determined up to 20.91 U/mg, with the optimum temperature of 41 ℃ and pH of 9.0. In contrast, the enzyme activity of its F130H mutant decreased by about 23.6%, yet with the same trends of change with temperature and pH, confirming that phenylalanine at this position does affect the substrate specificity of PAL. Both the wild type and the mutant have relatively poor thermostability, but good pH-stability. These results may help to further investigate the regulatory role of PAL in the process of podophyllotoxin biosynthesis and advance the heterologous synthesis of podophyllotoxin to protect the germplasm resource of S. hexandrum. They also demonstrate that ShPAL has a potential application in biochemical industry and biomedicine.


Assuntos
Fenilalanina Amônia-Liase , Podofilotoxina , Fenilalanina Amônia-Liase/genética , Fenilalanina Amônia-Liase/química , Fenilalanina Amônia-Liase/metabolismo , Filogenia , Clonagem Molecular
16.
Food Funct ; 14(10): 4607-4620, 2023 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-37158366

RESUMO

Tumor-associated macrophages (TAMs) participate in tumorigenesis, growth, invasion as well as metastasis by facilitating an immunosuppressive tumor microenvironment. Reversing the pro-tumoral M2 phenotype of TAMs has become a hot spot in advancing cancer immunotherapy. In the current study, the content of Moringa oleifera leaf polysaccharides (MOLP) was determined and characterized, along with the anti-cancer mechanism of MOLP studied in a Lewis lung cancer (LLC) tumor-bearing mouse model and bone marrow-derived macrophages. The monosaccharide composition and gel permeation chromatography analyses show that MOLP are mainly composed of galactose, glucose, and arabinose, with approximately 17.35 kDa average molecular weight (Mw). In vivo studies demonstrate that MOLP convert TAMs from the immunosuppressive M2 phenotype to the antitumor M1 phenotype, thus inducing CXCL9 and CXCL10 expression and increasing T-cell infiltration in the tumor. Furthermore, macrophage depletion and T cell suppression demonstrated that the tumor suppressive effect of MOLP was reliant on reprogramming macrophage polarization and T cell infiltration. In vitro studies revealed that MOLP could induce the phenotypic switch from M2 macrophages to M1 by targeting TLR4. The current study highlights that MOLP are promising anticancer plant-derived polysaccharides with potential in modulating the immune microenvironment and have a bright application prospect in the immunotherapy of lung cancer.


Assuntos
Neoplasias Pulmonares , Moringa oleifera , Animais , Camundongos , Macrófagos Associados a Tumor/metabolismo , Receptor 4 Toll-Like/genética , Receptor 4 Toll-Like/metabolismo , Moringa oleifera/metabolismo , Linfócitos T , Neoplasias Pulmonares/tratamento farmacológico , Fenótipo , Polissacarídeos/farmacologia , Folhas de Planta/metabolismo , Microambiente Tumoral
17.
Artigo em Inglês | MEDLINE | ID: mdl-37030848

RESUMO

Present endoscopic ultrasound (EUS) imaging methods for circular array (CA) suffer from the nonuniform spatial resolution in the imaging of a dual-layered media, such as the tubes' immersion EUS inspection. The problem is mainly attributed to the restricted focus and beam de-focusing at the interface. In this article, a circular total focusing method (CTFM) is proposed, which leverages the concept of the conventional total focusing method (TFM) and makes three vital improvements to overcome the challenges. First, to obtain the accurate time-of-flight (TOF) in the dual-layered media, a fourth-order equation of Snell's law is built and solved in polar coordinate system. Second, a fast geometric approximation method is derived to correct the TOF distortion caused by the transducer's eccentricity. Third, the intensity compensation is applied to flatten the imaging intensity at different positions by considering the directivity of element, transmission at interface, and divergence in media. The CTFM is validated on a tube's immersion EUS using a 10 MHz CA with 128 elements. Experimental results demonstrate that the proposed CTFM outperforms existing imaging methods. The lateral and axial resolutions are 0.71 and 0.30 mm, which are 27.5% and 33.3% higher than those of the classic delay-and-sum (DAS) method. The CTFM image shows high and uniform signal-to-noise ratio (SNR) which is 33.6% higher than that of DAS images. The CTFM provides a novel EUS imaging modality which can be applied in both medical and nondestructive testing domains.

18.
Eur J Med Chem ; 252: 115330, 2023 Apr 05.
Artigo em Inglês | MEDLINE | ID: mdl-37011553

RESUMO

The emergence of drug-resistant Vibrio poses a serious threat to aquaculture and human health, thus there is an urgent need for the discovery of new related antibiotics. Given that marine microorganisms (MMs) are evidenced as important sources of antibacterial natural products (NPs), great attention has been gained to the exploration of potential anti-Vibrio agents from MMs. This review summarizes the occurrence, structural diversity, and biological activities of 214 anti-Vibrio NPs isolated from MMs (from 1999 to July 2022), including 108 new compounds. They were predominantly originated from marine fungi (63%) and bacteria (30%) with great structural diversity, including polyketides, nitrogenous compounds, terpenoids, and steroids, among which polyketides account for nearly half (51%) of them. This review will shed light on the development of MMs derived NPs as potential anti-Vibrio lead compounds with promising applications in agriculture and human health.


Assuntos
Produtos Biológicos , Policetídeos , Humanos , Produtos Biológicos/farmacologia , Produtos Biológicos/química , Fungos/química , Antibacterianos/farmacologia , Antibacterianos/química , Bactérias/química , Organismos Aquáticos/química
19.
J Nat Prod ; 86(4): 994-1002, 2023 04 28.
Artigo em Inglês | MEDLINE | ID: mdl-36947873

RESUMO

Seven new 18-residue peptaibols, trichorzins A-G (1-7), were isolated from the sponge-derived fungus Trichoderma sp. GXIMD 01001. Their structures and configurations were characterized by a comprehensive interpretation of the NMR spectroscopic data, MS/MS fragmentation, Marfey's method, and ECD analysis. The general sequences of trichorzins A-G are as follows: Ac-Aib1-Ala/Ser2-Ala3-Aib/Iva4-Iva5-Gln6-Aib/Iva7-Val/allo-Ile8-Aib9-Gly10-Leu11-Aib12-Pro13-Leu14-Aib15-Aib16-Gln17-Trpol/Pheol18. The obtained compounds were assessed for their potential antiproliferative and antimicrobial activities. All obtained compounds did not show potent antibacterial activity but exhibited significant cytotoxicity, with the lowest IC50 values at 0.46-4.7 µM against four human carcinoma cell lines.


Assuntos
Peptaibols , Trichoderma , Humanos , Peptaibols/química , Trichoderma/química , Espectrometria de Massas em Tandem , Antibacterianos/química
20.
J Zhejiang Univ Sci B ; 24(3): 275-280, 2023 Mar 15.
Artigo em Inglês, Chinês | MEDLINE | ID: mdl-36916003

RESUMO

Marine microorganisms, especially marine fungi, have historically proven their value as a prolific source for structurally novel and pharmacologically active secondary metabolites (Deshmukh et al., 2018; Carroll et al., 2022). The corals constitute a dominant part of reefs with the highest biodiversity, and harbor highly diverse and abundant microbial symbionts in their tissue, skeleton, and mucus layer, with species-specific core members that are spatially partitioned across coral microhabitats (Wang WQ et al., 2022). The coral-associated fungi were very recently found to be vital producers of structurally diverse compounds, terpenes, alkaloids, peptides, aromatics, lactones, and steroids. They demonstrate a wide range of bioactivity such as anticancer, antimicrobial, and antifouling activity (Chen et al., 2022). The genetically powerful genus Emericella (Ascomycota), which has marine and terrestrial sources, includes over 30 species and is distributed worldwide. It is considered a rich source of diverse secondary metabolites with antimicrobial activity or cytotoxicity (Alburae et al., 2020). Notably, Emericella nidulans, the sexual state of a classic biosynthetic strain Aspergillus nidulans, was recently reported as an important source of highly methylated polyketides (Li et al., 2019) and isoindolone-containing meroterpenoids (Zhou et al., 2016) with unusual skeletons.


Assuntos
Alcaloides , Antozoários , Anti-Infecciosos , Aspergillus nidulans , Policetídeos , Animais , Policetídeos/farmacologia , Policetídeos/química , Antozoários/microbiologia , Anti-Infecciosos/farmacologia
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