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1.
Int J Biol Macromol ; 267(Pt 2): 131586, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38615861

RESUMO

While hydrogels have potential for food packaging, limited research on hydrogels with excellent mechanical performance and antibacterial activity for preserving chicken breasts. Herein, we created antibacterial hydrogels by embedding methyl-ß-cyclodextrin/thyme oil inclusion complexes (MCD/TO-ICs) into a polyvinyl alcohol matrix containing dendrobium polysaccharides and guar gum in varying ratios using freeze-thaw cycling method. The resulting hydrogels exhibited a more compact structure than those without MCD/TO-ICs, enhancing thermal stability and increasing glass transition temperature due to additional intermolecular interactions between polymer chains that inhibited chain movement. XRD analysis showed no significant changes in crystalline phase, enabling formation of a 3D network through abundant hydrogen bonding. Moreover, the hydrogel demonstrated exceptional durability, with a toughness of 350 ± 25 kJ/m3 and adequate tearing resistance of 340 ± 30 J/m2, capable of lifting 3 kg weight, 1200 times greater than the hydrogel itself. Additionally, the hydrogels displayed excellent antimicrobial activity and antioxidant properties. Importantly, the hydrogels effectively maintained TVB-N levels and microbial counts within acceptable ranges, preserving sensory properties and extending the shelf life of chilled chicken breasts by four days. This study highlights the potential of MCD/TO-IC-incorporated polysaccharide hydrogels as safe and effective active packaging solutions for preserving chilled chicken in food industry.


Assuntos
Galinhas , Hidrogéis , Polissacarídeos , Animais , Hidrogéis/química , Hidrogéis/farmacologia , Polissacarídeos/química , Polissacarídeos/farmacologia , Conservação de Alimentos/métodos , beta-Ciclodextrinas/química , Embalagem de Alimentos/métodos , Galactanos/química , Galactanos/farmacologia , Anti-Infecciosos/farmacologia , Anti-Infecciosos/química , Antibacterianos/farmacologia , Antibacterianos/química , Antioxidantes/farmacologia , Antioxidantes/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Mananas , Gomas Vegetais
2.
Innovation (Camb) ; 5(2): 100591, 2024 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-38414519

RESUMO

Electricity is the lifeblood of modern society. However, the predominant source of electricity generation still relies on non-renewable fossil fuels, whose combustion releases greenhouse gases contributing to global warming. The increasing demand for energy and escalating environmental concerns necessitate proactive measures to develop innovative green energy technologies capable of both cooling the Earth and generating electricity. Here, we look forward to an interdisciplinary power system integrating solar absorbers, radiative coolers, and thermoelectric generators. This system can simultaneously harvest thermal energy from the sun and from cold space, thereby transforming the challenges posed by global warming into opportunities for the production of clean electricity. We underscore recent advancements in this field and address key challenges while also exploring forward-looking opportunities in the foreseeable future. The proposed integrated energy technology achieves uninterrupted power supply through the unrestricted capture of thermal energy, offering a robust alternative pathway for next-generation sustainable energy technologies.

3.
Luminescence ; 39(1): e4674, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38286602

RESUMO

Recently, long persistent phosphors (LPPs) have attracted significant attention as promising candidates for biomedical applications. However, the serious decrease in luminescence intensity in tissue still remains a major challenge. Therefore, exploring more competitive LPPs and achieving reproducible tissue imaging is crucial. In this study, a new series of near-infrared (NIR) phosphors La3 Ga5 Sn1-x O14 :xCr3+ (x = 0.005-0.05) were synthesized using a high-temperature solid-state method. The as-synthesized samples were characterized using X-ray diffraction, diffuse/photoluminescence spectroscopy, fluorescence decay curves, and thermoluminescence spectroscopy. Upon excitation with ultraviolet light, strong emission bands were observed in the range 600-1200 nm with an optimal doping concentration of x = 0.02 mol. Moreover, La3 Ga5 SnO14 :Cr3+ exhibits persistent luminescence due to the presence of suitable energy traps, which prompted the phosphor to emit NIR light even after the removal of the excitation source.


Assuntos
Luminescência , Raios Ultravioleta , Difração de Raios X
4.
Front Bioeng Biotechnol ; 11: 1322514, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38155924

RESUMO

Liver disease has emerged as a significant worldwide health challenge due to its diverse causative factors and therapeutic complexities. The majority of liver diseases ultimately progress to end-stage liver disease and liver transplantation remains the only effective therapy with the limitations of donor organ shortage, lifelong immunosuppressants and expensive treatment costs. Numerous pre-clinical studies have revealed that extracellular vesicles released by mesenchymal stem cells (MSC-EV) exhibited considerable potential in treating liver diseases. Although natural MSC-EV has many potential advantages, some characteristics of MSC-EV, such as heterogeneity, uneven therapeutic effect, and rapid clearance in vivo constrain its clinical translation. In recent years, researchers have explored plenty of ways to improve the therapeutic efficacy and rotation rate of MSC-EV in the treatment of liver disease. In this review, we summarized current strategies to enhance the therapeutic potency of MSC-EV, mainly including optimization culture conditions in MSC or modifications of MSC-EV, aiming to facilitate the development and clinical application of MSC-EV in treating liver disease.

5.
Molecules ; 28(17)2023 Aug 27.
Artigo em Inglês | MEDLINE | ID: mdl-37687096

RESUMO

A rigid polyurethane foam (RPUF) composite was prepared by compounding phytic acid (PA)-functionalized Graphite oxide (PA-GO) with flame-retardant poly (Ammonium phosphate) (APP) and expandable graphite (EG). The effects of PA-GO on the thermal, flame-retardant, and mechanical properties of RPUF were studied using a thermogravimetric analyzer, a limiting oxygen index (LOI) tester, a UL-94 vertical combustion tester, a cone calorimeter, scanning electron microscopy, and a universal tensile testing machine. The results indicated that there was a significant synergistic flame-retardant effect between PA-GO and the intumescent flame retardants (IFR) in the RPUF matrix. Compared with RPUF-1, the addition of 0.3 wt% PA-GO could increase LOI from 25.7% to 26.5%, increase UL-94 rating from V-2 to V-0, and reduce the peak heat release rate (PHRR) and total heat release rate (THR) by 28.5% and 22.2%, respectively. Moreover, the amount of residual char increased from 22.2 wt% to 24.6 wt%, and the char layer was continuous and dense, with almost no holes. Meanwhile, the loss of mechanical properties was apparently lightened.

6.
ACS Macro Lett ; 12(10): 1311-1316, 2023 Oct 17.
Artigo em Inglês | MEDLINE | ID: mdl-37708566

RESUMO

A polymer nanoparticle network using single-chain nanoparticles (SCNPs) as cross-links is designed. The experimental and theoretical study shows that incorporating SCNPs in polymer networks leads to smaller mesh size, faster terminal relaxation time, and reduced fluctuation among cross-links, resulting in a significant increase in shear storage modulus, and enhancement in tensile stress. Notably, the reversible single-chain collapse of SCNPs under thermal stimulation enables the polymer network to undergo coherent changes between two topological states, thereby exhibiting reversible transformations between soft and stiff states. This approach and finding can effectively tailor the mechanical properties of polymer networks, potentially leading to the development of intelligent, responsive materials.

7.
Angew Chem Int Ed Engl ; 62(38): e202309601, 2023 Sep 18.
Artigo em Inglês | MEDLINE | ID: mdl-37548132

RESUMO

High-voltage aqueous rechargeable energy storage devices with safety and high specific energy are hopeful candidates for the future energy storage system. However, the electrochemical stability window of aqueous electrolytes is a great challenge. Herein, inspired by density functional theory (DFT), polyethylene glycol (PEG) can interact strongly with water molecules, effectively reconstructing the hydrogen bond network. In addition, N, N-dimethylformamide (DMF) can coordinate with Zn2+ , assisting in the rapid desolvation of Zn2+ and stable plating/stripping process. Remarkably, by introducing PEG400 and DMF as co-solvents into the electrolyte, a wide electrochemical window of 4.27 V can be achieved. The shift in spectra indicate the transformation in the number and strength of hydrogen bonds, verifying the reconstruction of hydrogen bond network, which can largely inhibit the activity of water molecule, according well with the molecular dynamics simulations (MD) and online electrochemical mass spectroscopy (OEMS). Based on this electrolyte, symmetric Zn cells survived up to 5000 h at 1 mA cm-2 , and high voltage aqueous zinc ion supercapacitors assembled with Zn anode and activated carbon cathode achieved 800 cycles at 0.1 A g-1 . This work provides a feasible approach for constructing high-voltage alkali metal ion supercapacitors through reconstruction strategy of hydrogen bond network.

8.
Nat Prod Res ; : 1-7, 2023 May 03.
Artigo em Inglês | MEDLINE | ID: mdl-37132421

RESUMO

Three new compounds, apocimycin A-C, were identified from a saltern-derived Micromonospora sp. strain FXY415, isolated from Dongshi saltern, Fujian, China. Their planar structures and relative configuration were confirmed mainly by analysis of 1D- and 2D- NMR spectra. Three compounds belong to 4,6,8-trimythyl nona-2,7-dienoic acid derivatives, apocimycin A also has a phenoxazine nucleus. Apocimycin A-C exhibited weak cytotoxic and antimicrobial activities. Our research showed again that microbial communities in extreme environments are a potential resource in looking for new and bioactive led compounds.

9.
Bioorg Chem ; 136: 106547, 2023 07.
Artigo em Inglês | MEDLINE | ID: mdl-37105000

RESUMO

There is an urgent need to discover new antibacterial drugs and provide new treatment options for clinical antimicrobial resistance (AMR) pathogen infections. Inspired by the structural insights from analyzing the co-crystal structure of lefamulin with the ribosomes of S. aureus, a series of novel pleuromutilin derivatives of phenylene sulfide incorporated with urea moiety were designed and synthesized. The structure-activity relationship (SAR) study revealed that derivatives with urea in the meta position of phenylene sulfide had optimal antibacterial activities in vitro. Among them, 21h was the most potent one against Methicillin-resistant Staphylococcus aureus (MRSA) and clinical AMR Gram-positive bacteria with minimum inhibitory concentrations (MICs) in the range of 0.00195-0.250 µg/mL. And it possessed low resistance frequency, prolonged Post-Antibiotic Effect and the capability to overcome lefamulin-induced resistance. Furthermore, 21h exhibited potent antibacterial activity in vivo in both the thigh infection model and trauma infection model, representing a promising lead for the development of new antibiotics against Gram-positive pathogens, especially for AMR bacteria.


Assuntos
Antibacterianos , Staphylococcus aureus Resistente à Meticilina , Antibacterianos/farmacologia , Antibacterianos/química , Staphylococcus aureus , Relação Estrutura-Atividade , Testes de Sensibilidade Microbiana , Sulfetos/farmacologia , Pleuromutilinas
10.
Sci Adv ; 8(33): eabo7500, 2022 Aug 19.
Artigo em Inglês | MEDLINE | ID: mdl-35977027

RESUMO

Color is the mapping of electromagnetic waves of different wavelengths in human vision. The electronic color recognition system currently in use is mainly based on the photoelectric effect. Here, we demonstrate a color materials' recognition system based on photothermoelectric effects. The system uses a microfabricated thermoelectric generator (TEG) as a platform, which is covered with dye-colored fabric pieces or structure-colored laser-patterned metal sheets. Under light irradiation, the fabrics/metals selectively absorb light and convert it into heat, which flows through the underlying TEG arrays and then converted into electrical signal output to realize the distinction of color and materials. This previously unidentified high-sensitivity TEG detection method provides a potential approach for precise color materials' detection over wide areas and may help understand the mechanism of bionic color recognition.

11.
Front Cell Infect Microbiol ; 12: 1055929, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36605124

RESUMO

Multidrug-resistant (MDR) bacteria pose a significant clinical threat to human health, but the development of antibiotics cannot meet the urgent need for effective agents, especially those that can kill persisters and biofilms. Here, we reported that nigericin showed potent bactericidal activity against various clinical MDR Gram-positive bacteria, persisters and biofilms, with low frequencies of resistance development. Moreover, nigericin exhibited favorable in vivo efficacy in deep-seated mouse biofilm, murine skin and bloodstream infection models. With Staphylococcus aureus, nigericin disrupted ATP production and electron transport chain; cell death was associated with altered membrane structure and permeability. Obtaining nigericin-resistant/tolerant mutants required multiple rounds of challenge, and, cross-resistance to members of several antimicrobial classes was absent, probably due to distinct nigericin action with the GraSR two-component regulatory system. Thus, our work reveals that nigericin is a promising antibiotic candidate for the treatment of chronic or recurrent infections caused by Gram-positive bacteria.


Assuntos
Staphylococcus aureus Resistente à Meticilina , Infecções Estafilocócicas , Humanos , Animais , Camundongos , Nigericina/farmacologia , Nigericina/uso terapêutico , Testes de Sensibilidade Microbiana , Antibacterianos/uso terapêutico , Infecções Estafilocócicas/tratamento farmacológico , Biofilmes
12.
Molecules ; 26(21)2021 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-34770914

RESUMO

Eight new cytochalasins 1-8 and ten known analogs 9-18 were isolated from the endophytic fungus Phomopsis sp. xz-18. The planar structures of the cytochalasins were determined by HR-ESI-MS and NMR analysis. Compounds 1, 2, 9 and 10 were 5/6/6/7/5-fused pentacyclic cytochalasins; compounds 3 and 4 had conjugated diene structures in the macrocycle; and compound 6 had a ß,γ-unsaturated ketone. The absolute configuration of 6 was confirmed for the first time by the octant rule. The acid-free purification process proved that the pentacyclic system was a natural biosynthetic product and not an acid-mediated intramolecular cyclized artifact. The new compounds did not exhibit activities against human cancer cell lines in cytotoxicity bioassays or antipathogenic fungal activity, but compounds 1, 3 and 4 showed moderate antibacterial activity in disk diffusion assays.


Assuntos
Antifúngicos/farmacologia , Citocalasinas/farmacologia , Endófitos/efeitos dos fármacos , Phomopsis/efeitos dos fármacos , Antifúngicos/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Citocalasinas/química , Endófitos/metabolismo , Metabolismo Energético/efeitos dos fármacos , Humanos , Espectroscopia de Ressonância Magnética , Redes e Vias Metabólicas , Testes de Sensibilidade Microbiana , Estrutura Molecular , Phomopsis/metabolismo
13.
Micromachines (Basel) ; 12(5)2021 Apr 22.
Artigo em Inglês | MEDLINE | ID: mdl-33922193

RESUMO

The interface affects the transmission behavior of electrons and phonons, which in turn determines the performance of thermoelectric materials. In this paper, metals (Cu, Ag, Au)/Al2O3/Bi2Te3 heterostructures have been fabricated from bottom to up to optimize the thermoelectric power factor. The introducing metals can be alloyed with Bi2Te3 or form interstitials or dopants to adjust the carrier concentration and mobility. In addition, the metal-semiconductor interface as well as the metal-insulator-semiconductor interface constructed by the introduced metal and Al2O3 would further participate in the regulation of the carrier transport process. By adjusting the metal and oxide layer, it is possible to realize the simultaneous optimization of electric conductivity and Seebeck coefficient. This work will enable the optimal and novel design of heterostructures for thermoelectric materials with further improved performance.

14.
Org Biomol Chem ; 19(7): 1616-1619, 2021 02 25.
Artigo em Inglês | MEDLINE | ID: mdl-33533370

RESUMO

A novel and straightforward intramolecular cyclization of glycine derivatives to 2-substituted benzoxazoles through copper-catalyzed oxidative C-H/O-H cross-coupling was described. A variety of glycine derivatives involving short peptides underwent cross-dehydrogenative-coupling readily to afford diverse 2-substituted benzoxazoles. The synthetic method has the advantages of simple operation, broad substrate scope and mild reaction conditions, thus providing an alternative effective approach for benzoxazole construction.

15.
Org Biomol Chem ; 18(44): 9095-9099, 2020 11 28.
Artigo em Inglês | MEDLINE | ID: mdl-33146660

RESUMO

The amide group has one of the most significant functionalities found in many natural products. Herein, low-nucleophilic amides are used in a Mannich-type reaction to synthesize N-acyl-protected amine derivatives. A highly efficient synthetic method utilizing simple aldehydes, N-substituted anilines, and amides as substrates was established through a one-pot amide pathway activated by hydrogen bonding between the ZnCl2 and amide under solvent-free conditions. This strategy can be broadly applied to medicinal chemistry. More importantly, compared with the previous Lewis acid catalyzed reaction, we proposed a new application of zinc chloride.

16.
Eur J Med Chem ; 207: 112755, 2020 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-32882611

RESUMO

The receptor tyrosine kinase rearranged during transfection (RET) plays pivotal roles in several cancers, including thyroid carcinoma and non-small cell lung cancer (NSCLC). Currently, there are several FDA-approved RET inhibitors, but their indication is limited to thyroid cancer, and none can overcome their gatekeeper mutants (V804L and V804M). Here, we report the discovery of 9x representing a new chemotype of potent and selective RET inhibitors, using a rational design strategy of type II kinase inhibitors. 9x exhibited both superior antiproliferative activities against NSCLC-related carcinogenic fusions KIF5B-RET and CCDC6-RET and gatekeeper mutant-transformed Ba/F3 cells, with the lowest GI50 of 9 nM, and substantial inhibitory activities against wild-type RET and RET mutant proteins, with the best IC50 of 4 nM. More importantly, 9x also showed nanomole potency against RET-positive NSCLC cells LC-2/ad, but not against a panel of RET-negative cancer cells, such as A549, H3122, A375 or parental Ba/F3 cells, demonstrating its selective 'on-target' effect. In mouse xenograft models, 9x repressed tumor growth driven by both wild type KIF5B-RET-Ba/F3 and gatekeeper mutant KIF5B-RET(V804M)-Ba/F3 cells in a dose-dependent manner. Together, these data establish that 9x provides a good starting point for the development of targeted therapeutics against RET-positive cancers, especially NSCLC.


Assuntos
Desenho de Fármacos , Mutação , Inibidores de Proteínas Quinases/química , Inibidores de Proteínas Quinases/farmacologia , Proteínas Proto-Oncogênicas c-ret/antagonistas & inibidores , Pirazóis/química , Pirazóis/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Humanos , Proteínas Proto-Oncogênicas c-ret/genética
17.
Int J Syst Evol Microbiol ; 70(9): 5026-5031, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32790600

RESUMO

A novel actinomycete, designated WYY166T, was isolated from the rhizosphere of Suaeda australis Moq. collected in Dongfang, PR China. The taxonomic position of this strain was investigated using a polyphasic approach. Phylogenetic analysis based on its 16S rRNA gene referred strain WYY166T to the genus Nonomuraea, and it was most closely related to the type strains Nonomuraea candida HMC10T, Nonomuraea turkmeniaca DSM 43926T, Nonomuraea maritima NBRC 106687T and Nonomuraea polychroma DSM 43925T (98.35, 97.60, 97.36 and 97.30% sequence similarity, respectively). Genome sequencing revealed a genome size of 11.27 Mbp and a G+C content of 71.10 mol%. The genome average nucleotide identity (ANI) values and the digital DNA - DNA hybridization (dDDH) values between strain WYY166T and the other species of the genus were found to be low (ANI 81.63~85.23 %, dDDH 23.6~31.6 %), suggesting that it represented a new species. The physiological evaluation showed that it had remarkable nitrate reduction activity. The whole-cell hydrolysates contained meso-diaminopimelic acid and madurose. The N-acyl type of muramic acid was acetyl. The major menaquinones were MK-9 (H4) (86.9 %) and MK-9 (H2) (13.1 %). The predominant fatty acids were iso-C16 : 0 (53.2 %), 10-methyl C17 : 0 (10.7 %), C17 : 1 ω6c (8.3 %) and iso-C16 : 1 h (7.3 %). These physiological, biochemical and chemotaxonomic data suggested that strain WYY166T should be classified as representing a novel species of the genus Nonomuraea, for which the name Nonomuraea nitratireducens sp. nov. is proposed. The type strain is WYY166T (=MCCC 1K03779T=KCTC 49343T).


Assuntos
Actinobacteria/classificação , Chenopodiaceae/microbiologia , Filogenia , Rizosfera , Microbiologia do Solo , Actinobacteria/isolamento & purificação , Técnicas de Tipagem Bacteriana , Composição de Bases , China , DNA Bacteriano/genética , Ácido Diaminopimélico/química , Ácidos Graxos/química , Hibridização de Ácido Nucleico , RNA Ribossômico 16S/genética , Análise de Sequência de DNA , Vitamina K 2/análogos & derivados , Vitamina K 2/química
18.
Cell Chem Biol ; 27(11): 1359-1370.e8, 2020 11 19.
Artigo em Inglês | MEDLINE | ID: mdl-32649904

RESUMO

Multidrug resistance (MDR) in cancer remains a major challenge for the success of chemotherapy. Natural products have been a rich source for the discovery of drugs against MDR cancers. Here, we applied high-throughput cytotoxicity screening of an in-house natural product library against MDR SGC7901/VCR cells and identified that the cyclodepsipeptide verucopeptin demonstrated notable antitumor potency. Cytological profiling combined with click chemistry-based proteomics revealed that ATP6V1G directly interacted with verucopeptin. ATP6V1G, a subunit of the vacuolar H+-ATPase (v-ATPase) that has not been previously targeted, was essential for SGC7901/VCR cell growth. Verucopeptin exhibited strong inhibition of both v-ATPase activity and mTORC1 signaling, leading to substantial pharmacological efficacy against SGC7901/VCR cell proliferation and tumor growth in vivo. Our results demonstrate that targeting v-ATPase via its V1G subunit constitutes a unique approach for modulating v-ATPase and mTORC1 signaling with great potential for the development of therapeutics against MDR cancers.


Assuntos
Antineoplásicos/farmacologia , Produtos Biológicos/farmacologia , Depsipeptídeos/farmacologia , Resistência a Múltiplos Medicamentos/efeitos dos fármacos , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , ATPases Vacuolares Próton-Translocadoras/antagonistas & inibidores , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Produtos Biológicos/síntese química , Produtos Biológicos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Depsipeptídeos/síntese química , Depsipeptídeos/química , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Humanos , Masculino , Alvo Mecanístico do Complexo 1 de Rapamicina/antagonistas & inibidores , Alvo Mecanístico do Complexo 1 de Rapamicina/metabolismo , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Neoplasias Experimentais/tratamento farmacológico , Neoplasias Experimentais/metabolismo , Neoplasias Experimentais/patologia , Subunidades Proteicas/efeitos dos fármacos , Proteômica , ATPases Vacuolares Próton-Translocadoras/metabolismo
19.
Bioorg Chem ; 101: 103949, 2020 08.
Artigo em Inglês | MEDLINE | ID: mdl-32531507

RESUMO

A one-pot efficient biocatalytic strategy for the synthesis of 3,4-dihydropyrimidin-2-(1H)-ones was developed in a circulating microwave reactor selecting α-chymotrypsin as the promiscuous biocatalyst. In the circulating reaction system, the combination of microwave heating and external cooling could avoid the denaturation and inactivation of enzyme, and greatly improved the radiation power of microwave, thus improving the specific effects of microwave. During the reaction process, the microwave radiation power was automatically adjusted by adjusting the speed of the reaction mixture circulation. When the microwave power was maintained at 110 W, the best results could be obtained with the highest yield of 96% at 55 °C in 50 min, and the reaction had a wide range of substrates. But no obvious product was detected in a tank microwave reactor at 55 °C for 100 min, under this condition, the microwave power was maintained at about 3 W. As a contrast, the reaction only obtained 63% yield in 55 °C oil bath for 96 h.


Assuntos
Reatores Biológicos , Micro-Ondas , Animais , Biocatálise , Bovinos , Quimotripsina/metabolismo
20.
Org Lett ; 22(11): 4366-4371, 2020 06 05.
Artigo em Inglês | MEDLINE | ID: mdl-32459492

RESUMO

A synthesis program for structurally complex macrocycles is very challenging. Herein, we propose a biosynthesis pathway of the pyranylated cyclodepsipeptide verucopeptin to make enough supply and to diversify verucopeptin by genetic manipulation and one-step semisynthesis. The synthesis relies on the intrinsic reactivity of the interchangeable hemiketal pyrane and opened keto along with adjacent alkene. Biological evaluation of verucopeptin-oriented analogs delivers a potent AMP-activated protein kinase (AMPK) agonist, antibacterial agent, and selective NFκB modulator.


Assuntos
Proteínas Quinases Ativadas por AMP/metabolismo , Antibacterianos/farmacologia , Depsipeptídeos/farmacologia , NF-kappa B/antagonistas & inibidores , Inibidores de Proteínas Quinases/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Actinomadura/química , Antibacterianos/biossíntese , Antibacterianos/química , Depsipeptídeos/biossíntese , Depsipeptídeos/química , Células HEK293 , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , NF-kappa B/metabolismo , Inibidores de Proteínas Quinases/química , Inibidores de Proteínas Quinases/metabolismo , Transdução de Sinais/efeitos dos fármacos
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