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1.
Chemosphere ; 286(Pt 2): 131784, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34371358

RESUMO

Humus is an important parameter to affect the environmental fate of arsenic (As) in tailing soil. According to the batch and column experiment, the effects of humus (HS) including humic acid (HA), fulvic acid (FA) on the As release and basic properties of soil were studied in the soil from a mining region. In addition, HA was modified by 3-mercaptopropyltrimethoxysilane (3-MPTS) with different sulfur content (S%) to improve the release capacity of As. The results indicated that HS could destroy the binding of As with Fe, Mn, Al and Ca without affecting the basic properties of tailings soil, thus achieving the co-release of As and associated metals. Besides, the As release capacity of FA (25.47 %) was slightly higher than that of HA (21.90 %). The ability of thiol-modified HAs to release As from tailings soil after being modified with different S% of 3-MPTS was significantly improved, of which 2 % had the best treatment. The thiol groups (-SH) reached 45.00 % of total S. With the increase of S%, the surface thoil content, aromatization degree and total reduction capacity (TRC) of HA increased. The study demonstrated that HS and thiol-modified HA could promote the migration of As and could advance the treatment of heavy metal contaminated tailing soil.


Assuntos
Arsênio , Poluentes do Solo , Benzopiranos , Substâncias Húmicas/análise , Solo , Poluentes do Solo/análise , Compostos de Sulfidrila
2.
Food Chem ; 372: 131214, 2022 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-34619523

RESUMO

Currently, the ability to produce several kinds of water-soluble red natural colorants makes the genus Talaromyces particularly important to the dye industry, which can be an alternative to the use of harmful synthetic colorants. In this study, colored compounds produced by Talaromyces amestolkiae were extracted, characterized chemically and the color stability of the fermented broth without any extraction procedure was further evaluated over pH variation. Five azaphilones compounds were detected by Ultrahigh Performance Liquid Chromatography-Mass Spectrometry system, all being complexes of the fatty acid amino-hexanedioic acid and azaphilone Monascus colorants. The color of the fermented broth was stable at a wide range of pH (3-9). Furthermore, T. amestolkiae colorants precipitated through hydrolysis of key chemical groups at extremely acidic (pH 1) and lose red color in extremely basic (pH 13) medium, showing negative halochromism. Nevertheless, these findings enhance the industrial relevance of azaphilone colorants produced by biotechnological process.


Assuntos
Monascus , Talaromyces , Benzopiranos , Pigmentos Biológicos , Talaromyces/genética
3.
Chem Commun (Camb) ; 57(93): 12476-12479, 2021 Nov 23.
Artigo em Inglês | MEDLINE | ID: mdl-34734602

RESUMO

We identified small-molecule enhancers of cellular stress granules by observing molecular crowding of proteins and RNAs in a time-dependent manner. Hit molecules sensitized the IRF3-mediated antiviral mechanism in the presence of poly(I:C) and inhibited the replication of SARS-CoV-2 by inducing stress granule formation. Thus, modulating multimolecular crowding can be a promising strategy against SARS-CoV-2.


Assuntos
Antivirais/farmacologia , Benzopiranos/farmacologia , Grânulos Citoplasmáticos/efeitos dos fármacos , Pirazóis/farmacologia , SARS-CoV-2/efeitos dos fármacos , Replicação Viral/efeitos dos fármacos , Animais , Antivirais/química , Benzopiranos/química , Linhagem Celular Tumoral , Chlorocebus aethiops , Grânulos Citoplasmáticos/metabolismo , Relação Dose-Resposta a Droga , Combinação de Medicamentos , Humanos , Fator Regulador 3 de Interferon/metabolismo , Lopinavir/farmacologia , Testes de Sensibilidade Microbiana , Estrutura Molecular , Poli I-C/farmacologia , Pirazóis/química , Relação Estrutura-Atividade , Células Vero
4.
Anal Chim Acta ; 1183: 338938, 2021 Oct 23.
Artigo em Inglês | MEDLINE | ID: mdl-34627522

RESUMO

The spiropyran (SP) compound is a typical photochromic compound. Its merocyanine configuration (MC) can accept energy and be excited by visible light, while the closed-loop configuration cannot. In this work, the SP was wrapped in ß-cyclodextrin (ß-CD-SP) firstly. When it was competitively replaced by thiamethoxam and dissociated out of ß-CD, it would be converted to MC, which could be excited by visible light around 550 nm to produce red fluorescence. Here, CsPbBr3 was selected as the energy donor based on the principle of fluorescence resonance energy transfer (FRET). In order to connect with ß-CD-SP and improve its stability, CsPbBr3 was wrapped in mesoporous silica, and then the second wrapping was performed to block those mesopores and the amination reaction was carried out (NH2-SiO2@CsPbBr3). Subsequently, NH2-SiO2@CsPbBr3 with green fluorescence (506 nm) was used as the internal standard and excitation light source for MC, and the red fluorescence of MC was used as the response signal to construct a ratiometric fluorescence sensor. When thiamethoxam was added and excited by 365 nm ultraviolet light, the energy would be transferred from NH2-SiO2@CsPbBr3 (506 nm) that emitted green fluorescence to MC, which emitted red fluorescence. So, the fluorescence color changed from green to yellow to red with the addition of the thiamethoxam. This sensor was employed to detect thiamethoxam in soil and yam.


Assuntos
Transferência Ressonante de Energia de Fluorescência , Dióxido de Silício , Benzopiranos , Indóis , Nitrocompostos , Tiametoxam
5.
Environ Monit Assess ; 193(11): 727, 2021 Oct 16.
Artigo em Inglês | MEDLINE | ID: mdl-34655328

RESUMO

Twenty-nine surface sediments from Chaohu Lake in China and from its six main tributaries were sampled to investigate the concentrations of two important polycyclic musks (PCMs), 1,3,4,6,7,8-hexahydro-4,6,6,7,8,8-hexamethylcyclopenta(g)-2-benzopyran (galaxolide, HHCB) and 7-acetyl-1,1,3,4,4,6-hexamethyl-1,2,3,4-tetrahydronaphthalene (tonalide, AHTN), as well as the concentration of 4,6,7,8-hexahydro-4,6,6,7,8,8-hexamethylcyclopenta(g)-2-benzopyran-1-one (galaxolidon, HHCB-lactone), which is the main degradation product of HHCB. Except for the high concentrations of AHTN and HHCB measured in the Nanfei River (879 ng/g dw and 5,513 ng/g dw, respectively), the levels of AHTN and HHCB in the river sediments were 7.08-44.9 ng/g dw and 20.6-268 ng/g dw, respectively, which are slightly lower than those documented in various areas worldwide. The concentrations of AHTN and HHCB in the sediments of Chaohu Lake were one or two orders of magnitude lower than those in the tributary rivers and showed a clear regional distribution. The concentrations of HHCB-lactone were comparable to those of HHCB and presented a significant positive correlation with the concentrations of HHCB, suggesting that the HHCB-lactone originated directly from the degradation of HHCB in wastewater treatment plants (WWTPs) or in the natural environment. The diagnostic ratios of HHCB/AHTN and HHCB-lactone/HHCB and the enantiomeric fractions (EFs) of these PCMs showed that the direct origins of the target PCMs in the study area were municipal and industrial wastewaters discharged from adjacent cities or point sources and that the HHCB-lactone in sediment originated from the natural degradation of HHCB in the rivers and the lake. The results of the risk assessment showed that the PCMs in the watershed sediments were unlikely to pose a threat to aquatic species. However, the effluents of industrial and municipal wastewaters that are discharged into the Nanfei River should be investigated in future research.


Assuntos
Lagos , Poluentes Químicos da Água , Benzopiranos/análise , China , Monitoramento Ambiental , Lactonas , Rios , Poluentes Químicos da Água/análise
6.
Appl Microbiol Biotechnol ; 105(21-22): 8139-8155, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34647136

RESUMO

The accurate taxonomic concept of the fungal Chaetomium species has been a hard work due to morphological similarity. Chemotaxonomy based on secondary metabolites is a powerful tool for taxonomical purposes, which could be used as an auxiliary reference to solve the problems encountered in the classification of Chaetomium. Among secondary metabolites produced by Chaetomium, cytochalasans and azaphilones exhibited a pattern of distribution and frequency of occurrence that establish them as chemotaxonomic markers for the Chaetomium species. This review attempted to elucidate the composition of the Chaetomium species and its relationship with classical taxonomy by summarizing the pattern of cytochalasans and azaphilones distribution and biosynthesis in the Chaetomium species. KEY POINTS: • Secondary metabolites from the genus Chaetomium are summarized. • Cytochalasans and azaphilones could be characteristic metabolites of the Chaetomium species. • Cytochalasans and azaphilones could be used to analyze for taxonomical purposes.


Assuntos
Chaetomium , Benzopiranos , Citocalasinas , Pigmentos Biológicos
7.
J Agric Food Chem ; 69(36): 10709-10721, 2021 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-34476938

RESUMO

Thirty-one new 4H-chromene derivatives were designed and synthesized. Their structures were identified with IR, 1H NMR, 13C NMR, and HRMS. The crystal structure of compound 2a was determined by single-crystal X-ray diffraction. Their antifungal activities were evaluated against Pyricularia oryzae, Erysiphe graminis, Coniella diplodiella, Pseudoperonospora cubensis, and Sclerotinia sclerotiorum. These results demonstrated that most compounds exhibited remarkable inhibitory activities at 20 µg/mL. Compounds 4b and 4c displayed excellent antifungal activity against S. sclerotiorum and possessed better efficacy than fluopyram. At the same time, the inhibitory activity of the bioactive compounds was evaluated against succinate dehydrogenase (SDH). The results showed that these compounds possessed outstanding activity. Compounds 4b and 4c displayed better inhibitory activity than fluopyram. The molecular modeling results revealed that compound 4c had stronger affinity to SDH than fluopyram. It is the first time that the inhibitory activity of 4H-chromene analogs against SDH has been reported.


Assuntos
Benzopiranos , Succinato Desidrogenase , Antifúngicos/farmacologia , Ascomicetos , Benzopiranos/farmacologia , Estrutura Molecular , Relação Estrutura-Atividade , Succinato Desidrogenase/metabolismo
8.
J Hazard Mater ; 416: 126116, 2021 08 15.
Artigo em Inglês | MEDLINE | ID: mdl-34492911

RESUMO

Galaxolide (HHCB), one of the most widely used synthetic musks in personal care products (PCPs), has been recognized as an emerging contaminant with potential human health concerns. To overcome such adverse effects, a systematic molecular design, screening and performance evaluation approach was developed to generate functionally improved and environmentally friendly HHCB derivatives. Among the 90 designed HHCB derivatives, 15 were screened with improved functional properties (i.e., odor stability and intensity) and less environmental impacts (i.e., lower bio-toxicity, bio-accumulation ability, and mobility) using 3D-QSAR models and density functional theory methods. Their human health risks were then assessed by toxicokinetic analysis, which narrowed the candidates to four. Derivative 7, the designed molecule with the least dermal adsorption potential, was evaluated for its interaction with other PCPs additives (i.e., anti-photosensitivity materials and moisturizer) and such impacts on human health risks using molecular docking and molecular dynamic simulation. The environmental fate of Derivative 7 after transformation (i.e., photodegradation, biotransformation, and chlorination) was also discussed. Biotransformation and chlorination were recognized as optimum options for Derivative 7 mitigation. This study provided the theoretical basis for the design of functionally improved and environmentally friendly HHCB alternatives and advanced the understanding of their environmental behaviors and health risks.


Assuntos
Cosméticos , Relação Quantitativa Estrutura-Atividade , Benzopiranos , Biotransformação , Humanos , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular
9.
Environ Toxicol ; 36(12): 2541-2550, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34499403

RESUMO

Bergenin is a C-glucoside of 4-O-methyl gallic acid with a variety of biological activities, such as antioxidant and anti-inflammatory. Herein, we investigated the involvement of bergenin in the protective effect against H2 O2 -induced oxidative stress and apoptosis in human nucleus pulposus cells (HNPCs) and the underlying mechanisms. HNPCs were cotreated with various concentrations of bergenin and 200 µM H2 O2 for 24 h. Cell viability was detected by Cell Counting Kit-8 and lactate dehydrogenase release assays. Reactive oxygen species (ROS) was evaluated utilizing 2',7'-dichlorofluorescein-diacetate. Superoxide dismutase (SOD) and catalase (CAT) activities and glutathione (GSH) levels were measured to assess oxidative stress. Apoptosis was evaluated using terminal deoxynucleotidyl transferase dUTP nick end labeling and caspase-3/7 activity assays. Expression of protein was determined by western blotting. Results indicated that treatment with bergenin significantly alleviated H2 O2 -induced viability reduction and ROS overproduction in HNPCs in a dose-dependent manner. Bergenin alleviated H2 O2 -induced oxidative stress in HNPCs by increased activity of superoxide dismutase and level of glutathione peroxidase. H2 O2 -induced apoptosis and activity of caspase-3/7 were also suppressed by bergenin treatment in HNPCs. Western blotting showed that H2 O2 -induced decrease in expression of peroxisome proliferator-activated receptor γ (PPAR-γ) and increase in nuclear factor κB (NF-κB) were inhibited by bergenin. However, the inhibitory effect of bergenin on H2 O2 -induced viability reduction, oxidative stress and apoptosis were noticeably abrogated in PPAR-γ knockdown HNPCs. In conclusion, our results indicated that bergenin alleviates H2 O2 -induced oxidative stress and apoptosis in HNPCs by activating PPAR-γ and suppressing NF-κB pathway.


Assuntos
NF-kappa B , Núcleo Pulposo , Apoptose , Benzopiranos , NF-kappa B/metabolismo , Núcleo Pulposo/metabolismo , Estresse Oxidativo , PPAR gama/genética , PPAR gama/metabolismo , Espécies Reativas de Oxigênio
10.
Nat Commun ; 12(1): 5321, 2021 09 07.
Artigo em Inglês | MEDLINE | ID: mdl-34493732

RESUMO

CARM1 is often overexpressed in human cancers including in ovarian cancer. However, therapeutic approaches based on CARM1 expression remain to be an unmet need. Cancer cells exploit adaptive responses such as the endoplasmic reticulum (ER) stress response for their survival through activating pathways such as the IRE1α/XBP1s pathway. Here, we report that CARM1-expressing ovarian cancer cells are selectively sensitive to inhibition of the IRE1α/XBP1s pathway. CARM1 regulates XBP1s target gene expression and directly interacts with XBP1s during ER stress response. Inhibition of the IRE1α/XBP1s pathway was effective against ovarian cancer in a CARM1-dependent manner both in vitro and in vivo in orthotopic and patient-derived xenograft models. In addition, IRE1α inhibitor B-I09 synergizes with immune checkpoint blockade anti-PD1 antibody in an immunocompetent CARM1-expressing ovarian cancer model. Our data show that pharmacological inhibition of the IRE1α/XBP1s pathway alone or in combination with immune checkpoint blockade represents a therapeutic strategy for CARM1-expressing cancers.


Assuntos
Carcinoma Epitelial do Ovário/terapia , Endorribonucleases/genética , Neoplasias Ovarianas/terapia , Receptor de Morte Celular Programada 1/genética , Proteína-Arginina N-Metiltransferases/genética , Proteínas Serina-Treonina Quinases/genética , Proteína 1 de Ligação a X-Box/genética , Animais , Anticorpos Monoclonais/farmacologia , Sequência de Bases , Benzopiranos/farmacologia , Carcinoma Epitelial do Ovário/genética , Carcinoma Epitelial do Ovário/imunologia , Carcinoma Epitelial do Ovário/patologia , Linhagem Celular Tumoral , Estresse do Retículo Endoplasmático/efeitos dos fármacos , Endorribonucleases/antagonistas & inibidores , Endorribonucleases/imunologia , Feminino , Regulação Neoplásica da Expressão Gênica , Humanos , Himecromona/análogos & derivados , Himecromona/farmacologia , Inibidores de Checkpoint Imunológico , Camundongos , Terapia de Alvo Molecular , Neoplasias Ovarianas/genética , Neoplasias Ovarianas/imunologia , Neoplasias Ovarianas/patologia , Receptor de Morte Celular Programada 1/antagonistas & inibidores , Receptor de Morte Celular Programada 1/imunologia , Ligação Proteica , Proteína-Arginina N-Metiltransferases/antagonistas & inibidores , Proteína-Arginina N-Metiltransferases/imunologia , Proteínas Serina-Treonina Quinases/antagonistas & inibidores , Proteínas Serina-Treonina Quinases/imunologia , Transdução de Sinais , Proteína 1 de Ligação a X-Box/antagonistas & inibidores , Proteína 1 de Ligação a X-Box/imunologia , Ensaios Antitumorais Modelo de Xenoenxerto
11.
Int J Mol Sci ; 22(18)2021 Sep 17.
Artigo em Inglês | MEDLINE | ID: mdl-34576229

RESUMO

The prevalence of non-alcoholic fatty liver disease (NAFLD) is one of the leading causes of chronic liver diseases worldwide. This study examined the potential protective effects of a naturally occurring polyphenolic compound, methyl brevifolincarboxylate (MBC) on fatty liver injury in vitro. The results showed that MBC at its non-cytotoxic concentrations, reduced lipid droplet accumulation and triglyceride (TG) levels in the oleic acid (OA)-treated human hepatocarcinoma cell line, SK-HEP-1 and murine primary hepatocytes. In OA-treated SK-HEP-1 cells and primary murine hepatocytes, MBC attenuated the mRNA expression levels of the de novo lipogenesis molecules, acetyl-coenzyme A carboxylase (Acc1), fatty acid synthase (Fasn) and sterol regulatory element binding protein 1c (Srebp1c). MBC promoted the lipid oxidation factor peroxisome proliferator activated receptor-α (Pparα), and its target genes, carnitine palmitoyl transferase 1 (Cpt1) and acyl-coenzyme A oxidase 1 (Acox1) in both the SK-HEP-1 cells and primary murine hepatocytes. The mRNA results were further supported by the attenuated protein expression of lipogenesis and lipid oxidation molecules in OA-treated SK-HEP-1 cells. The MBC increased the expression of AMP activated protein kinase (AMPK) phosphorylation. On the other hand, MBC treatment dampened the inflammatory mediator's, tumor necrosis factor (TNF)-α, interleukin-6 (IL-6), IL-8, and IL-1ß secretion, and nuclear factor (NF)-κB expression (mRNA and protein) through reduced reactive oxygen species production in OA-treated SK-HEP-1 cells. Taken together, our results demonstrated that MBC possessed potential protective effects against NAFLD in vitro by amelioration of lipid metabolism and inflammatory markers through the AMPK/NF-κB signaling pathway.


Assuntos
Proteínas Quinases Ativadas por AMP/metabolismo , Benzopiranos/farmacologia , Ácidos Graxos não Esterificados/metabolismo , Hepatócitos/efeitos dos fármacos , Inflamação/tratamento farmacológico , Metabolismo dos Lipídeos , NF-kappa B/metabolismo , Animais , Linhagem Celular Tumoral , Hepatócitos/metabolismo , Humanos , Lipídeos/química , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Ácido Oleico/química , Phyllanthus/efeitos dos fármacos , Espécies Reativas de Oxigênio , Transdução de Sinais , Triglicerídeos/metabolismo
12.
J Org Chem ; 86(19): 13693-13701, 2021 10 01.
Artigo em Inglês | MEDLINE | ID: mdl-34529434

RESUMO

A transition-metal-free postmodification of the Groebke-Blackburn-Bienaymé (GBB) reaction for the synthesis of spiro[chromene-imidazo[1,2-a]pyridin]-3'-imine was discovered. The unusual transformation represents the first example of activation and the reaction of the imidazole carbon atom. In this postcondensational modification, KOt-Bu acts as a base, which, after the isomerization of an alkyne moiety to allene, causes the next unique nucleophilic reaction of the imidazole carbon atom that results in spirocyclic structures. The proposed reaction mechanism was confirmed based on the DFT calculations.


Assuntos
Iminas , Elementos de Transição , Alcinos , Benzopiranos , Ciclização
13.
J Phys Chem Lett ; 12(39): 9470-9474, 2021 Oct 07.
Artigo em Inglês | MEDLINE | ID: mdl-34558899

RESUMO

Mechanophores that are embedded in a polymer backbone respond to the application of mechanical stretching forces by geometric changes such as bond rupture. Typically, these structural changes are irreversible, which limits the applicability of functional materials incorporating mechanophores. Using computational methods, we, here, present a general method of restoring a force-activated mechanophore to its deactivated form by using hydrostatic pressure. We use the spiropyran-merocyanine (SP-MC) interconversion to show that repeated activation of the SP mechanophore and deactivation of MC can be achieved by alternating mechanical stretching and hydrostatic compression, respectively. In the baromechanical cycle, MC acts as a "barophore" that responds to hydrostatic pressure by bond formation. The activation and deactivation of SP/MC are understood in terms of strain and electronic effects. Beneficially, this two-step baromechanical cycle can be observed in real time by using UV/vis spectroscopy. Our calculations pave the way for improving the applicability and reusability of force-responsive materials.


Assuntos
Benzopiranos/química , Indóis/química , Nitrocompostos/química , Pressão Hidrostática , Espectrofotometria Ultravioleta , Termodinâmica
14.
Water Res ; 205: 117652, 2021 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-34583206

RESUMO

Fulvic acids (FAs) are known to regulate the fate of mercury (Hg) in sediments, but the key effects of their properties are still unclear. In this study, field investigations and simulation experiments were conducted in a heavy metal-polluted wetland to identify FA characteristics and their association with the production and bioaccumulation of methylmercury (MeHg). Compared to permanently inundated areas (PIA), seasonally inundated areas (SIAs) had lower total Hg levels in sediments, whereas higher MeHg levels in sediments (0.20 ± 0.09 ng g-1 vs. 0.55 ± 0.31 ng g-1) and benthos (0.25 ± 0.22 ng g-1 vs. 1.62 ± 1.78 ng g-1). Meanwhile, the THg and MeHg concentrations in the same macrophyte species between PIA and SIA also followed a similar rule with benthos. FA-bound Hg in the sediment was significantly correlated with MeHg in the sediment (p < 0.01), as well as THg and MeHg in benthos (p < 0.05), indicating that FAs have the capacity to promote MeHg production and bioaccumulation. Moreover, the FAs in the sediments of the SIA had lower fractions and alkyl C/O-alkyl C ratios, but higher molecular weights and THg/MeHg concentrations than those in the PIA, indicating that FAs in SIA have increased bioavailability and enhanced competition for Hg, favoring significantly elevated FA-bound Hg levels. Biological exposure testing further demonstrated that FAs extracted from SIA had a greater ability to increase the production and bioaccumulation of MeHg than those extracted from PIA. Overall, these results highlight that the molecular composition and sources of FAs, excluding their concentrations, are one of important factors responsible for the obvious spatial heterogeneity of MeHg in sediments and aquatic organisms in the wetland.


Assuntos
Mercúrio , Compostos de Metilmercúrio , Poluentes Químicos da Água , Benzopiranos , Disponibilidade Biológica , Monitoramento Ambiental , Sedimentos Geológicos , Mercúrio/análise , Poluentes Químicos da Água/análise , Áreas Alagadas
15.
J Med Food ; 24(8): 852-859, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34382871

RESUMO

CYJ-27, a synthetic analog of decursin, prevents the generation of proinflammatory cytokines and oxidative stress. In this study, the effects of CYJ-27 on the regulation of inducible nitric oxide synthase (iNOS), heme oxygenase (HO)-1, and cyclooxygenase (COX-)2 were characterized in lipopolysaccharide (LPS)-treated human umbilical vein endothelial cells (HUVECs). In addition, the effects of CYJ-27 on the production of iNOS and representative proinflammatory cytokines, such as tumor necrosis factor (TNF)-α and interleukin (IL)-1ß, were tested in the lung tissues of LPS-treated mice. CYJ-27 promoted the expression of HO-1, suppressed NF-κB-luciferase activity, and reduced COX-2/PGE2 and iNOS/NO, resulting in a diminution in phosphorylated-STAT-1. Furthermore, CYJ-27 promoted the nuclear translocation of Nrf2, enhanced the combination of Nrf2 to antioxidant response elements, and diminished IL-1ß production in LPS-activated HUVECs. CYJ-27-downregulated iNOS/NO expression was rescued after the RNAi suppression of HO-1. In LPS-treated mice, CYJ-27 significantly diminished iNOS production in the lung tissues and TNF-α expression in the bronchoalveolar lavage fluid. These findings indicate that CYJ-27 exerts anti-inflammatory activities by regulating iNOS through downregulation of both NF-κB activation and phosphorylated-STAT-1. Hence, it can act as a template for the development of novel substances to treat inflammatory diseases.


Assuntos
Inflamação , NF-kappa B , Animais , Benzopiranos , Butiratos , Ciclo-Oxigenase 2/metabolismo , Regulação para Baixo , Heme Oxigenase-1/genética , Heme Oxigenase-1/metabolismo , Células Endoteliais da Veia Umbilical Humana/metabolismo , Humanos , Inflamação/tratamento farmacológico , Inflamação/genética , Lipopolissacarídeos , Camundongos , Fator 2 Relacionado a NF-E2/genética , Fator 2 Relacionado a NF-E2/metabolismo , NF-kappa B/genética , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/genética , Óxido Nítrico Sintase Tipo II/metabolismo
16.
J Enzyme Inhib Med Chem ; 36(1): 1798-1809, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34348556

RESUMO

Identifying isoform-specific inhibitors for closely related kinase family members remains a substantial challenge. The necessity for achieving this specificity is exemplified by the RSK family, downstream effectors of ERK1/2, which have divergent physiological effects. The natural product, SL0101, a flavonoid glycoside, binds specifically to RSK1/2 through a binding pocket generated by an extensive conformational rearrangement within the RSK N-terminal kinase domain (NTKD). In modelling experiments a single amino acid that is divergent in RSK3/4 most likely prevents the required conformational rearrangement necessary for SL0101 binding. Kinetic analysis of RSK2 association with SL0101 and its derivatives identified that regions outside of the NTKD contribute to stable inhibitor binding. An analogue with an n-propyl-carbamate at the 4" position on the rhamnose moiety was identified that forms a highly stable inhibitor complex with RSK2 but not with RSK1. These results identify a SL0101 modification that will aid the identification of RSK2 specific inhibitors.


Assuntos
Benzopiranos/síntese química , Monossacarídeos/síntese química , Inibidores de Proteínas Quinases/síntese química , Proteínas Quinases S6 Ribossômicas 90-kDa/antagonistas & inibidores , Sequência de Aminoácidos , Benzopiranos/metabolismo , Carbamatos/química , Humanos , Cinética , Modelos Moleculares , Monossacarídeos/metabolismo , Ligação Proteica , Conformação Proteica , Inibidores de Proteínas Quinases/metabolismo , Ramnose/química , Proteínas Quinases S6 Ribossômicas 90-kDa/genética , Relação Estrutura-Atividade
17.
Biomolecules ; 11(8)2021 07 25.
Artigo em Inglês | MEDLINE | ID: mdl-34439763

RESUMO

As the world develops and population increases, so too does the demand for higher agricultural output with lower resources. Plant biostimulants appear to be one of the more prominent sustainable solutions, given their natural origin and their potential to substitute conventional methods in agriculture. Classified based on their source rather than constitution, biostimulants such as humic substances (HS), protein hydrolysates (PHs), seaweed extracts (SWE) and microorganisms have a proven potential in improving plant growth, increasing crop production and quality, as well as ameliorating stress effects. However, the multi-molecular nature and varying composition of commercially available biostimulants presents challenges when attempting to elucidate their underlying mechanisms. While most research has focused on the broad effects of biostimulants in crops, recent studies at the molecular level have started to unravel the pathways triggered by certain products at the cellular and gene level. Understanding the molecular influences involved could lead to further refinement of these treatments. This review comprises the most recent findings regarding the use of biostimulants in plants, with particular focus on reports of their molecular influence.


Assuntos
Agricultura/métodos , Agricultura/tendências , Produtos Agrícolas , Extratos Vegetais/farmacologia , Reguladores de Crescimento de Plantas/farmacologia , Antioxidantes/metabolismo , Benzopiranos/química , Mudança Climática , Substâncias Húmicas , Fenômenos Fisiológicos Vegetais , Hidrolisados de Proteína/química , Hidrolisados de Proteína/metabolismo , Alga Marinha
18.
Chemistry ; 27(60): 14981-14988, 2021 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-34369018

RESUMO

Composite polymer electrolytes (CPEs) with smart, stimuli-responsive characteristics have gained considerable attention owing to their noninvasive manipulation and applications in future technologies. To address this potential, in this work, we demonstrate photoresponsive composite polymer electrolytes, consisting of gel polymer electrolyte (GPE) and spiropyran-immobilized nanoporous anodic aluminum oxide (SP-AAO) templates. Under UV irradiation, the close SP form isomerizes to the open merocyanine (MC) form, creating extremely polarized AAO surfaces; whereas, under visible light irradiation, the MC form reverts to the SP form, creating neutral surface conditions. The electrostatic interactions between ions and AAO surfaces are investigated by attenuated total reflection Fourier-transform infrared (ATR-FTIR) spectroscopy. Moreover, the behavior of ionic conductivity of the GPE@SP-AAO is found to be consistent with the kinetics of isomerization tracked by UV-Vis spectroscopy. This work provides a promising platform for developing next-generation photoelectronic smart devices.


Assuntos
Nanoporos , Polímeros , Benzopiranos , Eletrólitos , Indóis , Nitrocompostos
19.
J Pharm Sci ; 110(11): 3690-3701, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34391761

RESUMO

The Zaltoprofen/4,4'-Bipyridine system gives rise to two co-crystals of different compositions both endowed - in water and in buffer solution at pH 4.5 - with considerably higher solubility and dissolution rate than the pure drug. The qualitative and quantitative analysis of the DSC measurements, carried out on samples made up of mixtures prepared according to different methodologies, allows us to elaborate and propose an accurate thermodynamic model that fully takes into account the qualitative aspects of the complex experimental framework and which provides quantitative predictions (reaction enthalpies and compositions of the co-crystals) in excellent agreement with the experimental results. Co-crystal formation and cocrystal compositions were confirmed by X-ray diffraction measurements as well as by FT-IR and NMR spectroscopy measurements. The quantitative processing of DSC measurements rationalizes and deepens the scientific aspects underlying the so-called Tammann's triangle and constitutes a model of general validity. The work shows that DSC has enormous potential, which however can be fully exploited only by paying adequate attention to the experimental aspects and the quantitative processing of the measurements.


Assuntos
Preparações Farmacêuticas , Benzopiranos , Varredura Diferencial de Calorimetria , Cristalização , Difração de Pó , Propionatos , Piridinas , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
20.
Phytother Res ; 35(10): 5808-5822, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34375009

RESUMO

Idiopathic pulmonary fibrosis (IPF) is a progressive lung disease characterized by epithelial cell damage, fibroblast activation, and collagen deposition. IPF has high mortality and limited therapies, which urgently needs to develop safe and effective therapeutic drugs. Bergenin, a compound derived from a variety of medicinal plants, has demonstrated multiple pharmacological activities including anti-inflammatory and anti-tumor, also acts as a traditional Chinese medicine to treat chronic bronchitis, but its effect on the pulmonary fibrosis is unknown. In this study, we demonstrated that bergenin could attenuate bleomycin (BLM)-induced pulmonary fibrosis in mice. In vitro studies indicated that bergenin inhibited the transforming growth factor-ß1 (TGF-ß1)-induced fibroblast activation and the extracellular matrix accumulation by inhibiting the TGF-ß1/Smad signaling pathway. Further studies showed that bergenin could induce the autophagy formation of myofibroblasts by suppressing the mammalian target of rapamycin signaling and that bergenin could promote the myofibroblast apoptosis. In vivo experiments revealed that bergenin substantially inhibited the myofibroblast activation and the collagen deposition and promoted the autophagy formation. Overall, our results showed that bergenin attenuated the BLM-induced pulmonary fibrosis in mice by suppressing the myofibroblast activation and promoting the autophagy and the apoptosis of myofibroblasts.


Assuntos
Bleomicina , Fibrose Pulmonar Idiopática , Animais , Benzopiranos , Bleomicina/toxicidade , Fibroblastos , Pulmão , Camundongos , Camundongos Endogâmicos C57BL , Transdução de Sinais , Fator de Crescimento Transformador beta1
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