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1.
Sensors (Basel) ; 23(21)2023 Oct 27.
Artigo em Inglês | MEDLINE | ID: mdl-37960451

RESUMO

Aiming at the problem of asynchronous multi-target tracking, this paper studies the AA fusion optimization problem of multi-sensor networks. Firstly, each sensor node runs a PHD filter, and the measurement information obtained from different sensor nodes in the fusion interval is flood communicated into composite measurement information. The Gaussian component representing the same target is associated with a subset by distance correlation. Then, the Bayesian Cramér-Rao Lower Bound of the asynchronous multi-target-tracking error, including radar node selection, is derived by combining the composite measurement information representing the same target. On this basis, a multi-sensor-network-optimization model for asynchronous multi-target tracking is established. That is, to minimize the asynchronous multi-target-tracking error as the optimization objective, the adaptive optimization design of the selection method of the sensor nodes in the sensor network is carried out, and the sequential quadratic programming (SQP) algorithm is used to select the most suitable sensor nodes for the AA fusion of the Gaussian components representing the same target. The simulation results show that compared with the existing algorithms, the proposed algorithm can effectively improve the asynchronous multi-target-tracking accuracy of multi-sensor networks.

2.
Food Chem X ; 19: 100826, 2023 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-37780250

RESUMO

This study aims to analysis the structures of polysaccharides isolated from Pteridium revolutum and their antioxidant and antiglycated activities. Three novel water-soluble heteropolysaccharides, named PRP0, PRP1, and PRP2, were isolated from P. revolutum. The average molecular weight was determined by high performance gel permeation chromatography analysis as 1.04 × 106, 8.39 × 105, and 7.37 × 105 Da, respectively. Their structures were characterized using physicochemical and spectroscopic methods. The antioxidant and antiglycated activities were assayed in vitro. PRP0, PRP1, and PRP2 consist of l-Ara, l-Rha, d-Man, d-Xyl, d-Fuc, d-Gal, and d-Glc in different proportions. PRP1 mainly has a backbone of (1 â†’ 3,6)-linked d-Man and (1 â†’ 3)-linked d-Gal on main chain. PRP2 is mainly composed of (1 â†’ 2,4)-linked d-Man and (1 â†’ 3)-linked d-Gal on main chain. All polysaccharides have strong scavenging power on 2,2-difenil-1-picril-hidrazil and hydroxyl radicals and significantly antiglycated activity in Bovine serum albumin-Glucose model, which showing that the polysaccharides have potential application value on the functional food.

3.
Environ Sci Pollut Res Int ; 30(26): 68373-68386, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-37120503

RESUMO

The mussel Mytilus coruscus is an important and very popular seafood in China and widespread along the eastern coast of China. In this study, we investigated the molecular response of mussel gonads to cadmium accumulation at two concentrations (80 and 200 µg/L) for 30 days using ionomics and proteomics techniques. The shrinkage of the cells and moderate hemocytic infiltration were observed in the Cd-treated groups. The strontium, selenium (Se), and zinc contents were significantly altered, and the relationships between iron, copper, Se, manganese, calcium, sodium, and magnesium were also significantly altered. Label-free quantitative proteomics analysis revealed a total of 227 differentially expressed proteins. These proteins were associated with multiple biological processes, including the tricarboxylic acid cycle, structural reorganization of cells, biosynthesis of amino acids, inflammatory response of cells, and tumorigenesis. Nonetheless, our ionomics and proteomics analysis revealed that mussels could partly alleviate the adverse effects of Cd by altering the metal contents and correlations between minerals, thereby enhancing the biosynthesis of some amino acids and activity of antioxidant enzymes. Overall, this study provides an insight into the mechanism underlying Cd toxicity in mussel gonads from a metal and protein perspective.


Assuntos
Mytilus , Poluentes Químicos da Água , Animais , Mytilus/metabolismo , Cádmio/farmacologia , Proteômica , Proteínas , Alimentos Marinhos , Aminoácidos , Gônadas/metabolismo , Poluentes Químicos da Água/metabolismo
4.
Foods ; 11(13)2022 Jun 22.
Artigo em Inglês | MEDLINE | ID: mdl-35804650

RESUMO

Pteridium aquilinum (L.) Kuhn (Pteridaceae family) has been widely used as a food and medicine in China and Korea. Previous studies indicate that P. aquilinum contains a variety of bioactive chemical components such as flavonoids, phenols, terpenoids, saponins, polysaccharides, and so on. In the present study, a novel polysaccharide (named as PAP-3) with average molecular weight of 2.14 × 105 Da was obtained from P. aquilinum. The structure was studied through physicochemical and spectroscopic analysis. The results indicated that PAP-3 consists of arabinose, rhamnose, fucose, galactose, mannose, and xylose in a molar ratio of 1.58:1.00:3.26:4.57:4.81:3.33. The polysaccharide is mainly composed of (1→2)-linked xylose and (1→3,6)-linked mannose on the main chain, with (1→2)-linked xylose, (1→6)-linked mannose, and (1→6)- and (1→3,6)-linked galactose as side chains. Galactose, fucose, and xylose are located at the end of the side chains. The in vitro immunomodulatory and antioxidant activities were assayed. PAP-3 has strong free-radical scavenging activity on DPPH and ABTS radicals and significant immunomodulatory activity on RAW264.7 cells. These data provide useful information for further study on the polysaccharides of P. aquilinum and their applications in the food and medical industries.

5.
Biol Trace Elem Res ; 200(12): 5242-5250, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34997533

RESUMO

Metal accumulation in the marine environment can increase the metal content of fish living in it. For this reason, it is essential to evaluate the nutrition from fish consumption and assess metal toxicity risk. Ten species of demersal fish, which are part of the daily diet of coastal residents, were sampled using trammel net in the East China Sea. Levels of the microelements, the constant elements, and the toxic elements of muscle tissue were analyzed. Spiny red gurnard had the highest concentrations of calcium, copper, and iron, whereas pufferfish and threadfin porgy were good sources of zinc and magnesium. The levels of lead, cadmium, and inorganic arsenic in all samples were below the limit values according to Chinese national standards. Although some concerns were raised about the concentration of mercury (Hg) in threadfin porgy, silver croaker, and fivespot flounder, molar ratios (selenium, Se:Hg) and the Se health benefit values (HBVSe) indicated that they were safe for human consumption. Additionally, the estimated weekly intake and % weekly contribution of 10 fish species with different elements were provided, giving a reference for the people's healthy consumption.


Assuntos
Arsênio , Mercúrio , Perciformes , Selênio , Poluentes Químicos da Água , Animais , Arsênio/análise , Cádmio/análise , Cálcio , Cobre/análise , Peixes , Humanos , Ferro , Magnésio , Mercúrio/análise , Medição de Risco , Poluentes Químicos da Água/análise , Zinco/análise
6.
Biomed Pharmacother ; 144: 112336, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34678719

RESUMO

Natural products exist in various natural foods such as plants, herbs, fruits, and vegetables. Furthermore, marine life offers potential natural products with significant biological activity. The biochemical reaction is known as advanced glycation end products (AGEs) occurs in the human body. On the other hand, foods are capable of a wide range of processing conditions resulting in the generation of exogenous AGEs adducts. Protein glycation and the formation of advanced glycation end products both contribute to the pathogenesis of hyperglycemic complications. AGEs also play a pivotal role in microvascular and macrovascular complications progression by receptors for advanced glycation end products (RAGE). RAGE activate by AGEs leads to up-regulation of transcriptional factor NF-kB and inflammatory genes. Around the globe, researchers are working in various approaches for therapeutical implications on controlling AGEs mediated disease complications. In this regard, one of the potential promising agents observed with a wide range of AGEs inhibition by food-derived natural products. Current biotechnological tools have been turned to natural products or phytochemicals to manufacture the molecules without compromising their functionality. Metabolic engineering and bioinformatics perspectives have recently enabled the generation of a few potent metabolites with anti-diabetic activity. As the primary focus, this review article will also discuss multidisciplinary approaches that emphasize current advances in anti-diabetic therapeutic action and future perspectives of natural products.


Assuntos
Produtos Biológicos/uso terapêutico , Glicemia/efeitos dos fármacos , Diabetes Mellitus/tratamento farmacológico , Produtos Finais de Glicação Avançada/antagonistas & inibidores , Hipoglicemiantes/uso terapêutico , Compostos Fitoquímicos/uso terapêutico , Fitoterapia , Preparações de Plantas/uso terapêutico , Animais , Produtos Biológicos/isolamento & purificação , Biomarcadores/sangue , Glicemia/metabolismo , Diabetes Mellitus/sangue , Produtos Finais de Glicação Avançada/metabolismo , Humanos , Hipoglicemiantes/isolamento & purificação , Resistência à Insulina , Compostos Fitoquímicos/isolamento & purificação , Preparações de Plantas/isolamento & purificação
7.
J Food Biochem ; 45(6): e13756, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-33993503

RESUMO

Zn-binding protein was obtained after purification from scallops (Mizuhopecten yessoensis) using gel permeation and ion-exchange chromatography. Amino acid determination showed that the cysteine of the zinc-binding protein accounted for one-third of the total amino acids, which is a typical feature of metallothionein (MT). The spectra of Fourier Transform Infrared Spectroscopy (FTIR) and Circular Dichroism (CD) were analyzed to predict the secondary structure information of zinc-binding protein: the α-helix was 46.55%, the ß-sheets was 27.07%, the random coil was 16.48%, and the ß-turns was 9.89%. Using a commercial kit to measure its antioxidant activity in vitro, the result showed that it had good scavenging ability to 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydroxyl radical (·OH), and reducing the ability to ferrous iron ions. With the process provided by this study, zinc-binding protein can be prepared in large quantities, which is the basis for its future commercialization. PRACTICAL APPLICATIONS: According to the extraction and purification process established in this study, a large amount of zinc-bound MT from the viscera of scallops can be obtained. And the zinc-bound MT had good antioxidant activity. In addition, the yield of each purification step has been calculated. The zinc-bound MTs from scallop' viscera can be prepared in large quantities by directly using the process in this manuscript or by equal magnification of this process. In the future, large-scale production can be considered to increase the economic value of scallops' viscera.


Assuntos
Pectinidae , Zinco , Animais , Proteínas de Transporte , Pectinidae/metabolismo , Estrutura Secundária de Proteína
8.
Food Res Int ; 140: 110011, 2021 02.
Artigo em Inglês | MEDLINE | ID: mdl-33648243

RESUMO

The ovalbumin (OVA)-pectin (PEC)-sodium alginate (SA)-Vitamin D3 (VD3) complex nanoparticles were fabricated by antisolvent precipitation method, and the excellent encapsulation efficiency and loading capacity of VD3 were obtained by 96.6% and 2.8%, respectively. Compared with ternary OVA-PEC-VD3 complexes, the addition of SA with strong negative charge effectively regulated the OVA-PEC complexes and significantly improved the stability of OVA-PEC-SA-VD3 complex nanoparticles with preferable size as small as 126 nm. The storage stability was also investigated after low temperature storage for 31 d, and the particle size of quaternary complexes was increased only 40 nm. In vitro digestion results elucidated that the complex nanoparticles had good stability in the simulated gastric fluid, and almost completely released in the simulated intestinal fluid confirmed by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) experiments and scanning electron microscope (SEM) images. The release kinetics study clarified that it was close to Fick release. Fluorescence and Fourier transform infrared spectroscopy (FTIR) experiments showed that quaternary complex nanoparticles were mainly combined by electrostatic, hydrophobic and hydrogen bonding interactions. The novel quaternary protein-polysaccharide complexes have excellent stability and great sustained-release performance for VD3, which may be helpful for the digestion and absorption of vitamin by human body, thus have potential applications in the food and drug industry.


Assuntos
Alginatos , Nanopartículas , Digestão , Humanos , Ovalbumina , Pectinas
9.
Food Chem ; 354: 129516, 2021 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-33744663

RESUMO

In this work, the ß-lactoglobulin/gum arabic (ß-Lg-GA) complexes were prepared to encapsulate epigallocatechin gallate (EGCG), forming ß-Lg-GA-EGCG complex nanoparticles with an average particle size of 133 nm. The ß-Lg-GA complexes exhibited excellent encapsulation efficiency (84.5%), and the antioxidant performance of EGCG in vitro was improved after encapsulation. It was recorded that 86% of EGCG could be released in simulated intestinal fluid after 3 h of digestion, much faster than that in simulated gastric fluid, indicating that the ß-Lg-GA complexes were effective in enhancing EGCG stability, which was confirmed using SDS-PAGE and SEM. Further spectrum results demonstrated that various intramolecular interactions including electrostatic, hydrophobic and hydrogen bonding interactions contribute to the formation of ß-Lg-GA-EGCG complex nanoparticles. Also, XRDexperiments indicated that EGCG was successfully encapsulated by ß-Lg-GA complexes. Therefore, the ß-Lg-GA complexes hold great potentials in the protective delivery of sensitive bioactives.


Assuntos
Catequina/análogos & derivados , Goma Arábica/química , Lactoglobulinas/química , Nanopartículas/química , Catequina/química , Preparações de Ação Retardada , Digestão , Tamanho da Partícula , Eletricidade Estática
10.
Protein Expr Purif ; 182: 105838, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-33561519

RESUMO

Zinc-binding proteins named MT-M-I and MT-M-II were obtained after purification from metal-exposed hairy clams (Arca subcrenata) using gel permeation and ion-exchange chromatography. MT-M-I and MT-M-II were resolved by ion-exchange chromatography, and they were found to have similar molecular weights. MT-M-I and MT-M-II can bind 6 and 7 equivalents of Zn2+ in vitro, and they showed unusual migration behaviors in Tricine sodium dodecyl sulfate polyacrylamide gel electrophoresis (Tricine-SDS-PAGE). Such migration behaviors may be due to themetal thiolate clusters in these proteins. In terms of amino acid composition, the proportion of cysteine in MT-M-I and MT-M-II was approximately 30%, and glycine accounted for approximately 15%, where as aromatic amino acids were absent. Considering the performance in Tricine-SDS-PAGE and the amino acid compositions, MT-M-I and MT-M-II conform to the molecular characteristics of the metallothionein proteins. The structures were explored using circular dichroism (CD) and Fourier-transform infrared spectroscopy (FTIR). Also determined the antioxidant activities in terms of DPPH radical scavenging ability, hydroxyl radical (·OH) scavenging ability, and ferric-reducing/antioxidant power. The antioxidant activities of MT-M-I were found to be stronger than those of MT-M-II.


Assuntos
Bivalves/química , Proteínas de Transporte , Sequestradores de Radicais Livres , Metalotioneína , Animais , Proteínas de Transporte/química , Proteínas de Transporte/isolamento & purificação , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/isolamento & purificação , Metalotioneína/química , Metalotioneína/isolamento & purificação , Estrutura Secundária de Proteína
11.
Nat Prod Res ; 35(6): 945-950, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31135215

RESUMO

Premna fulva Craib, locally known as "Zhangu" in China, is a kind of traditional medicinal plant. A phytochemical investigation on this plant led to the isolation of a novel flavonoid glycoside along with three known analogues. The chemical structure of the new compound was determined by spectral and chemical analysis as apigenin 8-C-ß-D-xylopyranoside (1). Compound 1 showed weak inhibitory activities in vitro against to four tumor cell lines (HL-60, Bcap37, SMMC7721, and P388) with IC50 values of 12.58, 19.31, 31.02, and 48.19 µg/mL, respectively. The result might be helpful to explain the application of P. fulva in Traditional Chinese Medicine.[Figure: see text].


Assuntos
Flavonoides/farmacologia , Glicosídeos/farmacologia , Lamiaceae/química , Antineoplásicos Fitogênicos/farmacologia , Apigenina/farmacologia , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Morte Celular/efeitos dos fármacos , Linhagem Celular Tumoral , China , Flavonoides/química , Glicosídeos/química , Humanos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Plantas Medicinais/química , Proibitinas , Espectroscopia de Prótons por Ressonância Magnética
12.
Sensors (Basel) ; 22(1)2021 Dec 23.
Artigo em Inglês | MEDLINE | ID: mdl-35009616

RESUMO

Gaussian mixture probability hypothesis density (GM-PHD) filtering based on random finite set (RFS) is an effective method to deal with multi-target tracking (MTT). However, the traditional GM-PHD filter cannot form a continuous track in the tracking process, and it is easy to produce a large number of redundant invalid likelihood functions in a dense clutter environment, which reduces the computational efficiency and affects the update result of target probability hypothesis density, resulting in excessive tracking error. Therefore, based on the GM-PHD filter framework, the target state space is extended to a higher dimension. By adding a label set, each Gaussian component is assigned a label, and the label is merged in the pruning and merging step to increase the merging threshold to reduce the Gaussian component generated by dense clutter update, which reduces the computation in the next prediction and update. After pruning and merging, the Gaussian components are further clustered and optimized by threshold separation clustering, thus as to improve the tracking performance of the filter and finally realizing the accurate formation of multi-target tracks in a dense clutter environment. Simulation results show that the proposed algorithm can form a continuous and reliable track in dense clutter environment and has good tracking performance and computational efficiency.


Assuntos
Algoritmos , Análise por Conglomerados , Simulação por Computador , Funções Verossimilhança , Distribuição Normal
13.
Mini Rev Med Chem ; 20(12): 1101-1117, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-29189150

RESUMO

Withanolides are a group of highly oxygenated steroids derived from a C28 ergostane skeleton, and have attracted significant scientific interest due to their complex structural features and multiple bioactivities. More than 170 new natural withanolides were isolated and identified in the last 5 years. This review provides a comprehensive summary of the structural, biological and pharmacological activities of these new compounds.


Assuntos
Anti-Infecciosos/química , Vitanolídeos/química , Animais , Antozoários/química , Antozoários/metabolismo , Anti-Infecciosos/farmacologia , Citocinas/metabolismo , Datura/química , Datura/metabolismo , Ergosterol/análogos & derivados , Ergosterol/química , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Conformação Molecular , Withania/química , Withania/metabolismo
14.
Org Lett ; 21(16): 6539-6542, 2019 08 16.
Artigo em Inglês | MEDLINE | ID: mdl-31364857

RESUMO

Talaromyolides A-D (1-4) and talaromytin (5) were isolated from a marine fungus Talaromyces sp. CX11. Their structures were unambiguously determined by nuclear magnetic resonance (NMR), mass spectrometry, X-ray crystallography experiments, and time-dependent density functional theory electronic circular dichroism calculations. Talaromyolides A and D represent two novel carbon skeletons. Talaromytin exhibits two slowly interconverting conformers in DMSO-d6 and CH3OH-d4 that were studied by temperature-dependent NMR experiments. Talaromyolide D exhibits potent antiviral activity against pseudorabies virus (PRV) with a CC50 value of 3.35 µM.


Assuntos
Antivirais/farmacologia , Talaromyces/química , Terpenos/química , Antineoplásicos/química , Antineoplásicos/farmacologia , Antivirais/química , Linhagem Celular Tumoral , Dicroísmo Circular , Cristalografia por Raios X , Teoria da Densidade Funcional , Avaliação Pré-Clínica de Medicamentos , Herpesvirus Suídeo 1/efeitos dos fármacos , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Talaromyces/metabolismo , Terpenos/farmacologia
15.
Int J Biol Macromol ; 133: 564-574, 2019 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-31004640

RESUMO

Dendrobium devonianum has been used as herbal medicines and nutraceutical products since ancient time in China. However, its chemical composition and pharmacological mechanisms are not fully known. In present studies, by chemical purification and characteristic identification, we discovered a novel polysaccharide from D. devonianum, which was designated as DvP-1 with molecular weights of 9.52 × 104 Da. DvP-1 is a homogeneous heteropolysaccharide consisting of D-mannose and d-glucose in the molar ration of 10.11: 1. The main glycosidic linkages were ß-1, 4-Manp, which were substituted with acetyl groups at the O-2, O-3 and/or O-6 positions. DvP-1 was found to directly stimulate the activation of macrophages in vitro, as evidenced by inducing morphologic change, thereby promoting the production of cytokines TNF-α, IL-6 and NO, and enhancing the pinocytic activity of macrophages. By establishing a zebrafish model, we also found that DvP-1 could alleviate vinorelbine-induced decrease of macrophages in vivo. Further findings indicated that DvP-1 activated macrophages through several toll-like receptors (TLRs), but mainly through TLR4. DvP-1 served as a TLR4 agonist and induced ERK, JNK, p38, and IκB-α phosphorylation, suggesting the activation of MAPK and NFκB signaling pathways downstream of TLR4. These findings could help us further understand the immunomodulating effects of D. devonianum in Chinese medicines or health foods for immunocompromised persons. They also show the medicinal value of DvP-1 for the treatment of cancer and infectious diseases caused by TLR4 dysfunction.


Assuntos
Dendrobium/química , Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Polissacarídeos/farmacologia , Receptor 4 Toll-Like/agonistas , Animais , Proliferação de Células/efeitos dos fármacos , Citocinas/biossíntese , Macrófagos/citologia , Camundongos , Monossacarídeos/análise , Polissacarídeos/química , Células RAW 264.7 , Baço/imunologia , Vinorelbina/farmacologia , Peixe-Zebra
16.
Environ Microbiol ; 21(1): 496-510, 2019 01.
Artigo em Inglês | MEDLINE | ID: mdl-30452116

RESUMO

Co-occurring microorganisms have been proved to influence the performance of each other by metabolic means in nature. Here we generated a synthetic fungal-bacterial community comprising Penicillium citrinum and Pseudomonas aeruginosa employing the previously described membrane-separated co-culture device. By applying a newly designed molecular networking routine, new citrinin-related metabolites induced by the fungal-bacterial cross-talk were unveiled in trace amounts. A mechanically cycled co-culture setup with external pumping forces accelerating the chemically interspecies communication was then developed to boost the production of cross-talk-induced metabolites. Multivariate data analysis combined with molecular networking revealed the accumulation of a pair of co-culture-induced molecules whose productions were positively correlated to the exchange rate in the new co-cultures, facilitating the discovery of the previously undescribed antibiotic citrinolide with a novel skeleton. This highly oxidized citrinin adduct showed significantly enhanced antibiotic property against the partner strain P. aeruginosa than its precursor citrinin, suggesting a role in the microbial competition. Thus, we propose competitive-advantage-oriented structural modification driven by microbial defence response mechanism in the interspecies cross-talk might be a promising approach in the search for novel antibiotics. Besides, this study highlights the utility of MS-based metabolomics as an effective tool in the direct biochemical analysis of the community metabolism.


Assuntos
Antibacterianos/metabolismo , Citrinina/análogos & derivados , Citrinina/metabolismo , Penicillium/metabolismo , Pseudomonas aeruginosa/metabolismo , Metabolômica , Metabolismo Secundário/fisiologia
17.
Mar Drugs ; 16(9)2018 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-30213076

RESUMO

Natural products from marine actinomycetes remain an important resource for drug discovery, many of which are produced by the genus, Streptomyces. However, in standard laboratory conditions, specific gene clusters in microbes have long been considered silent or covert. Thus, various stress techniques activated latent gene clusters leading to isolation of potential metabolites. This study focused on the analysis of two new angucycline antibiotics isolated from the culture filtrate of a marine Streptomyces pratensis strain NA-ZhouS1, named, stremycin A (1) and B (2) which were further determined based on spectroscopic techniques such as high resolution time of flight mass spectrometry (HR-TOF-MS), 1D, and 2D nuclear magnetic resonance (NMR) experiments. In addition, four other known compounds, namely, 2-[2-(3,5-dimethyl-2-oxo-cyclohexyl)-6-oxo-tetrahydro-pyran-4yl]-acetamide (3), cyclo[l-(4-hydroxyprolinyl)-l-leucine] (4), 2-methyl-3H-quinazoline-4-one (5), and menthane derivative, 3-(hydroxymethyl)-6-isopropyl-10,12-dioxatricyclo[7.2.1.0]dodec-4-en-8-one (6) were obtained and elucidated by means of 1D NMR spectrometry. Herein, we describe the "Metal Stress Technique" applied in the discovery of angucyclines, a distinctive class of antibiotics that are commonly encoded in microbiomes but have never been reported in "Metal Stress" based discovery efforts. Novel antibiotics 1 and 2 exhibited antimicrobial activities against Pseudomonas aeruginosa, methicillin resistant Staphylococcus aureus (MRSA), Klebsiella pneumonia, and Escherichia coli with equal minimum inhibitory concentration (MIC) values of 16 µg/mL, while these antibiotics showed inhibition against Bacillus subtilis at MIC value of approximately 8⁻16 µg/mL, respectively. As a result, the outcome of this investigation revealed that metal stress is an effective technique in unlocking the biosynthetic potential and resulting production of novel antibiotics.


Assuntos
Antibacterianos/biossíntese , Organismos Aquáticos/fisiologia , Fatores Biológicos/biossíntese , Descoberta de Drogas/métodos , Streptomyces/fisiologia , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Fatores Biológicos/isolamento & purificação , Fatores Biológicos/farmacologia , Vias Biossintéticas/genética , Espectrometria de Massas , Metais Pesados/toxicidade , Testes de Sensibilidade Microbiana , Família Multigênica , Estresse Fisiológico
18.
Phytochemistry ; 154: 73-76, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30006090

RESUMO

Three undescribed aporphine alkaloids laurodionine B (1), illigerine A (2), and N-formyl-laurolitsine (3) were isolated from the methanolic extracts of the Chinese medicinal plant, Illigera aromatica, together with three known analogues (4-6). The chemical structures of 1-6 were identified by spectroscopic methods including 1D and 2D NMR (1H, 13C, COSY, HSQC, and HMBC) and high resolution mass spectrometry (HRESIMS). Compounds 1-3 showed moderate inhibitory activities in vitro against two cultured tumor cell lines, Hela and SMMC7721, with IC50 values of 32.42-62.90 µM. Only compound 1 had in vitro cytotoxic activity against Bcap37 cells, with the IC50 value of 90.61 µM.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Aporfinas/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Hernandiaceae/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Aporfinas/química , Aporfinas/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , China , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Humanos , Medicina Tradicional Chinesa , Estrutura Molecular , Relação Estrutura-Atividade , Células Tumorais Cultivadas
19.
Mini Rev Med Chem ; 18(19): 1590-1602, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29692245

RESUMO

Aporphine alkaloids, characterized by a heterocyclic aromatic basic skeleton, are known from different organisms and exhibit various biological activities: anti-tumor, anti-viral, anti-microbial, anti-inflammatory etc. The review gives information which provides an overview of the latest progress in the structural diversity and the biological activity of the aporphine alkaloids with their derivatives isolated from natural resource in recent years. Additionally, the synthetic approaches of aporphine alkaloids have also been reviewed.


Assuntos
Alcaloides/farmacologia , Aporfinas/farmacologia , Alcaloides/síntese química , Alcaloides/química , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Aporfinas/síntese química , Aporfinas/química , Isomerismo , Estrutura Molecular
20.
Mini Rev Med Chem ; 18(13): 1072-1094, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29512458

RESUMO

Recently, the marine-derived Aspergillus present as producers of a large number of structurally novel secondary metabolites. Some of these metabolites have shown antitumor, antimicrobial, anti-inflammatory, antioxidant and enzymatic activities, and may be promising resources for new therapeutic drugs. This review sums up 232 new bioactive metabolites from the marine-derived Aspergillus with classification through their biological activities and chemical structures in 2006-2016. Besides, structure-activity relationships of some compounds are explored.


Assuntos
Anti-Infecciosos/química , Antioxidantes/química , Aspergillus/química , Terpenos/química , Acetilcolinesterase/química , Acetilcolinesterase/metabolismo , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Antioxidantes/isolamento & purificação , Aspergillus/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Humanos , Água do Mar/microbiologia , Terpenos/isolamento & purificação
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