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Schisandra chinensis (Schisandraceae) is a medicinal plant widely used in traditional Chinese medicine. Under the name Wu Wei Zi, it is used to treat many diseases, especially as a stimulant, adaptogen, and hepatoprotective. Dibenzocyclooctadiene lignans are the main compounds responsible for the effect of S. chinensis. As a part of ongoing studies to identify and evaluate anti-inflammatory natural compounds, we isolated a series of dibenzocyclooctadiene lignans and evaluated their biological activity. Furthermore, we isolated new sesquiterpene 7,7-dimethyl-11-methylidenespiro[5.5]undec-2-ene-3-carboxylic acid. Selected dibenzocyclooctadiene lignans were tested to assess their anti-inflammatory potential in LPS-stimulated monocytes by monitoring their anti-NF-κB activity, antioxidant activity in CAA assay, and their effect on gap junction intercellular communication in WB-ras cells. Some S. chinensis lignans showed antioxidant activity in CAA mode and affected the gap junction intercellular communication. The anti-inflammatory activity was proven for (-)-gomisin N, (+)-γ-schisandrin, rubrisandrin A, and (-)-gomisin J.
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Lignanas , Compostos Policíclicos , Schisandra , Lignanas/farmacologia , Ciclo-Octanos/farmacologia , Anti-Inflamatórios/farmacologiaRESUMO
Background: Oxidative stress is a key factor in the pathophysiology of many diseases. This study aimed to verify the antioxidant activity of selected plant phenolics in cell-based assays and determine their direct or indirect effects. Methods: The cellular antioxidant assay (CAA) assay was employed for direct scavenging assays. In the indirect approach, the influence of each test substance on the gene and protein expression and activity of selected antioxidant enzymes was observed. One assay also dealt with activation of the Nrf2-ARE pathway. The overall effect of each compound was measured using a glucose oxidative stress protection assay. Results: Among the test compounds, acteoside showed the highest direct scavenging activity and no effect on the expression of antioxidant enzymes. It increased only the activity of catalase. Diplacone was less active in direct antioxidant assays but positively affected enzyme expression and catalase activity. Morusin showed no antioxidant activity in the CAA assay. Similarly, pomiferin had only mild antioxidant activity and proved rather cytotoxic. Conclusions: Of the four selected phenolics, only acteoside and diplacone demonstrated antioxidant effects in cell-based assays.
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Antioxidantes/farmacologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Elementos de Resposta Antioxidante , Antioxidantes/química , Biomarcadores , Expressão Gênica , Glucose , Humanos , Estrutura Molecular , Fator 2 Relacionado a NF-E2/genética , Fator 2 Relacionado a NF-E2/metabolismo , Estresse Oxidativo , Fenóis/química , Extratos Vegetais/química , Superóxido Dismutase-1/genética , Superóxido Dismutase-1/metabolismoRESUMO
Extensive phytochemical analysis of the CHCl3-soluble part of an ethanolic extract of branches and twigs of Broussonetia papyrifera led to the isolation of fourteen compounds, including a novel 5,11-dioxabenzo[b]fluoren-10-one derivative named broussofluorenone C (12). The isolated compounds 1-14 were characterized based on their NMR and HRMS data, and examined for their anti-inflammatory activities in LPS-stimulated THP-1 cells as well as for their cellular antioxidant effects. Compounds 7-10 and 12 showed inhibitory effects on NF-κB/AP-1 activation and compounds 7-9 were subsequently confirmed to suppress the secretion of both IL-1ß and TNF-α in LPS-stimulated THP-1 cells more significantly than the prednisone used as a positive control. In the CAA assay, compound 10 exhibited the greatest antioxidant effect, greater than that of the quercetin used as a positive control. The results show possible beneficial effects and utilization of B. papyrifera wood in the treatment of inflammatory diseases as well as oxidative stress.
Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Broussonetia/química , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Relação Dose-Resposta a Droga , Humanos , Interleucina-1beta/antagonistas & inibidores , Interleucina-1beta/biossíntese , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Estrutura Molecular , NF-kappa B/análise , NF-kappa B/antagonistas & inibidores , NF-kappa B/biossíntese , Estresse Oxidativo/efeitos dos fármacos , Relação Estrutura-Atividade , Células THP-1 , Fator de Transcrição AP-1/análise , Fator de Transcrição AP-1/antagonistas & inibidores , Fator de Transcrição AP-1/biossíntese , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Fator de Necrose Tumoral alfa/biossínteseRESUMO
A set of 25 novel, silicon-based carbamate derivatives as potential acetyl- and butyrylcholinesterase (AChE/BChE) inhibitors was synthesized and characterized by their in vitro inhibition profiles and the selectivity indexes (SIs). The prepared compounds were also tested for their inhibition potential on photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. In fact, some of the newly prepared molecules revealed comparable or even better inhibitory activities compared to the marketed drugs (rivastigmine or galanthamine) and commercially applied pesticide Diuron®, respectively. Generally, most compounds exhibited better inhibition potency towards AChE; however, a wider activity span was observed for BChE. Notably, benzyl N-[(1S)-2-[(tert-butyldimethylsilyl)oxy]-1-[(2-hydroxyphenyl)carbamoyl]ethyl]-carbamate (2) and benzyl N-[(1S)-2-[(tert-butyldimethylsilyl)oxy]-1-[(3-hydroxyphenyl)carbamoyl]ethyl]-carbamate (3) were characterized by fairly high selective indexes. Specifically, compound 2 was prescribed with the lowest IC50 value that corresponds quite well with galanthamine inhibition activity, while the inhibitory profiles of molecules 3 and benzyl-N-[(1S)-2-[(tert-butyldimethylsilyl)oxy]-1-[(4-hydroxyphenyl)carbamoyl]ethyl]carbamate (4) are in line with rivastigmine activity. Moreover, a structure-activity relationship (SAR)-driven similarity evaluation of the physicochemical properties for the carbamates examined appeared to have foreseen the activity cliffs using a similarity-activity landscape index for BChE inhibitory response values. The 'indirect' ligand-based and 'direct' protein-mediated in silico approaches were applied to specify electronic/steric/lipophilic factors that are potentially valid for quantitative (Q)SAR modeling of the carbamate analogues. The stochastic model validation was used to generate an 'average' 3D-QSAR pharmacophore pattern. Finally, the target-oriented molecular docking was employed to (re)arrange the spatial distribution of the ligand property space for BChE and photosystem II (PSII).
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Carbamatos/química , Carbamatos/farmacologia , Inibidores da Colinesterase/química , Silício/química , Sítios de Ligação , Butirilcolinesterase , Sobrevivência Celular/efeitos dos fármacos , Cloroplastos , Inibidores da Colinesterase/farmacologia , Transporte de Elétrons/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Ligantes , Simulação de Acoplamento Molecular , Complexo de Proteína do Fotossistema II , Spinacia oleracea , Relação Estrutura-Atividade , Células THP-1/efeitos dos fármacosRESUMO
Maytenus macrocarpa (Celastraceae) is a tree native to Amazonia. Its roots, leaves, bark, and combinations of these are used in traditional medicine mainly to treat rheumatism and, to a lesser extent, to heal wounds and to combat bronchitis and diarrhea. To date, mainly triterpenes and dihydro-ß-agarofuran sesquiterpenes were isolated from M. macrocarpa. Extracts and selected pure compounds isolated from the leaves, roots, and stem bark showed antibacterial, antiviral, antiparasitic, anti-inflammatory, and cytotoxic activities in vitro. The aim of this review is to summarize the available ethnobotanical, phytochemical, and pharmacological information about this traditional Amazonian medicinal tree, as well as to attract the attention of phytochemists and pharmacognosists to this potentially interesting source of ethnopharmaceuticals.
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Maytenus/química , Doenças Reumáticas/tratamento farmacológico , Cicatrização/efeitos dos fármacos , Antibacterianos/química , Antibacterianos/uso terapêutico , Antivirais/química , Antivirais/uso terapêutico , Humanos , Casca de Planta/química , Folhas de Planta/química , Raízes de Plantas/química , Doenças Reumáticas/patologiaRESUMO
Oxidative stress is a fundamental principle in the pathophysiology of many diseases. It occurs when the production of reactive oxygen species exceeds the capacity of the cell defense system. The hydroxyl radical is a reactive oxygen species that is commonly formed in vivo and can cause serious damage to biomolecules, such as lipids, proteins, and nucleic acids. It plays a role in inflammation-related diseases, like chronic inflammation, neurodegeneration, and cancer. To overcome excessive oxidative stress and thus to prevent or stop the progression of diseases connected to it, scientists try to combat oxidative stress and to find antioxidant molecules, including those that scavenge hydroxyl radical or diminish its production in inflamed tissues. This article reviews various methods of hydroxyl radical production and scavenging. Further, flavonoids, as natural plant antioxidants and essential component of the human diet, are reviewed as compounds interacting with the production of hydroxyl radicals. The relationship between hydroxyl radical scavenging and the structure of the flavonoids is discussed. The structural elements of the flavonoid molecule most important for hydroxyl radical scavenging are hydroxylation of ring B and a C2-C3 double bond connected with a C-3 hydroxyl group and a C-4 carbonyl group. Hydroxylation of ring A also enhances the activity, as does the presence of gallate and galactouronate moieties as substituents on the flavonoid skeleton.
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Reactive oxygen species (ROS) are highly considered in the ethiopathogenesis of different pathological conditions because they may cause significant damage to cells and tissues. In this paper, we focused on potential antioxidant properties of two medical plants such as the Agrimonia eupatoria L. and Cynara cardunculus L. Both plants have previously been studied for their pharmacological activities, especially as hepatoprotective and hypoglycemic activities. It has been suggested, that their effects are related to the antioxidant properties of polyphenols, which are dominant compounds of the plants' extracts. In the present study HPLC-MS analysis of water infusion was performed allowing the identification of several phenolic constituents. Furthermore, antioxidant effects of the two extracts were compared showing higher effects for agrimony extract compared to artichoke. Thus, agrimony was selected for the in vivo study using the skin flap viability model. In conclusion, our results provide evidence that the A. eupatoria extract may be a valuable source of polyphenols to be studied for the future development of supplements useful in the prevention of diseases linked to oxidative stress.
Assuntos
Agrimonia/química , Antioxidantes/química , Cynara/química , Fenóis/química , Extratos Vegetais/química , Animais , Antioxidantes/farmacologia , Catalase/metabolismo , Linhagem Celular/efeitos dos fármacos , Linhagem Celular/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Dano ao DNA/efeitos dos fármacos , Humanos , Estresse Oxidativo/efeitos dos fármacos , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Ratos , Espécies Reativas de Oxigênio/metabolismo , Superóxido Dismutase/metabolismoRESUMO
Along with the known kaempferol-3-O-α-l-rhamnopyranosyl-(1 â 2)-[6-O-(3-hydroxy-3-methylglutaryl)]-ß-d-galactopyranoside (1), five new flavonoids, containing the rarely isolated aglycon tamarixetin, were isolated from a methanolic extract of the endemic Balkan species Astragalus thracicus Griseb. Three of the new compounds are substituted with 3-hydroxy-3-methylglutaryl residue (HMG), untypical for the genus Astragalus. The compounds were identified as tamarixetin-3-O-α-l-rhamnopyranosyl-(1 â 2)-[6-O-(3-hydroxy-3-methylglutaryl)]-ß-d-galactopyranoside (2), tamarixetin-3-O-(2,6-di-O-α-l-rhamnopyranosyl)-ß-d-galactopyranoside (3), tamarixetin 3-O-ß-d-apiofuranosyl-(1 â 2)-ß-d-galactopyranoside (4), tamarixetin-3-O-ß-d-apiofuranosyl-(1 â 2)-[6-O-(3-hydroxy-3-methylglutaryl)]-ß-d-galactopyranoside (5), and tamarixetin-3-O-ß-d-apiofuranosyl-(1 â 2)-[α-l-rhamnopyranosyl-(1 â 6)]-ß-d-galactopyranoside (6). Selected compounds from A. thracicus were tested to evaluate their anticollagenase activity. The greatest effect was observed for quercetin-3-O-ß-d-apiofuranosyl-(1 â 2)-ß-d-galactopyranoside, possibly due to the presence of an ortho-dihydroxy arrangement of flavonoid ring B. The effect on collagenase and elastase was further evaluated also by in silico study, and the test compounds showed some level of in silico interaction.
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ETHNOPHARMACOLOGICAL RELEVANCE: Paulownia tomentosa Steud. (P. tomentosa) is a medium-sized tree traditionally used in Chinese folk medicine for the treatment of infectious diseases. It is a rich source of prenylated phenolic compounds that have been extensively studied for their promising biological activities. AIM OF THE STUDY: Due to the increasing development of antibiotic resistance, our study investigated plant-derived natural products from the fruits of P. tomentosa that could control Staphylococcus aureus infections with novel targets/modes of action and reduce antimicrobial resistance. MATERIALS AND METHODS: The ethanolic extract was fractionated and detected by liquid chromatography. The antistaphylococcal effects of the plant formulations were studied in detail in vitro by various biological methods, including microdilution methods for minimum inhibitory concentration (MIC), the checkerboard titration technique for synergy assay, fluorescence measurements for membrane disruption experiments, autoinducer-2-mediated bioassay for quorum sensing inhibition, and counting of colony-forming units for relative adhesion. Morphology was examined by transmission electron microscopy. RESULTS: Total ethanolic extract and chloroform fraction showed MICs of 128 and 32 µg/mL, respectively. Diplacol, diplacone, and 3'-O-methyl-5'-hydroxydiplacone inhibited S. aureus growth in the range of 8-16 µg/mL. Synergistic potential was shown in combination with mupirocin and fusidic acid. The ethanolic extract and the chloroform fraction destroyed the cell membranes by 91.61% and 79.46%, respectively, while the pure compounds were less active. The ethanolic extract and the pure compounds reduced the number of adhered cells to 47.33-10.26% compared to the untreated control. All tested plant formulations, except diplacone, inhibited quorum sensing of S. aureus. Transmission electron microscopy showed deformation of S. aureus cells. CONCLUSIONS: The products from the fruit of P. tomentosa showed antimicrobial properties against S. aureus alone and in combination with antibiotics. By affecting intracellular targets, geranylated flavonoids proposed novel approaches in the control of staphylococcal infections.
Assuntos
Anti-Infecciosos , Lamiales , Infecções Estafilocócicas , Staphylococcus aureus , Frutas/química , Extratos Vegetais/química , Clorofórmio , Anti-Infecciosos/farmacologia , Antibacterianos/química , Testes de Sensibilidade Microbiana , Etanol/farmacologiaRESUMO
This study investigates the effects of incorporating ZnO, TiO2, and colloidal Ag nanoparticles on the antioxidant, antimicrobial, and physical properties of biodegradable chitosan films. The research focuses on addressing the growing demand for sustainable packaging solutions that offer efficient food preservation while mitigating environmental concerns. In this investigation, the physical properties including thickness, water content, solubility, swelling degree, tensile strength, and elasticity of the chitosan films were examined. Additionally, the samples were analyzed for total polyphenol content, antimicrobial activity, and antioxidant capacity. Notably, the incorporation of ZnO nanoparticles led to the lowest water content and highest strength values among the tested films. Conversely, the addition of colloidal Ag nanoparticles resulted in films with the highest antioxidant capacities (DPPH: 32.202 ± 1.631 %). Remarkably, antimicrobial tests revealed enhanced activity with the inclusion of colloidal silver nanoparticles, yet the most potent antimicrobial properties were observed in films containing ZnO (E.coli: 2.0 ± 0.0 mm; MRSA: 2.0 ± 0.5 mm). The findings of this study hold significant implications for the advancement of edible biodegradable films, offering potential for more efficient food packaging solutions that address environmental sustainability concerns. By elucidating the effects of nanoparticle incorporation on film properties, this research contributes to the ongoing discourse surrounding sustainable packaging solutions in the food industry.
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Antimicrobial resistance is a public health threat and the increasing number of multidrug-resistant bacteria is a major concern worldwide. Common antibiotics are becoming ineffective for skin infections and wounds, making the search for new therapeutic options increasingly urgent. The present study aimed to investigate the antibacterial potential of prenylated phenolics in wound healing. Phenolic compounds isolated from the root bark of Morus alba L. were investigated for their antistaphylococcal potential both alone and in combination with commonly used antibiotics. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined by microdilution and agar method. Synergy was investigated using the checkerboard titration technique. Membrane-disrupting activity and efflux pump inhibition were evaluated to describe the potentiating effect. Prenylated phenolics inhibited bacterial growth of methicillin-resistant Staphylococcus aureus (MRSA) at lower concentrations (MIC 2-8 µg/ml) than commonly used antibiotics. The combination of active phenolics with kanamycin, oxacillin, and ciprofloxacin resulted in a decrease in the MIC of the antimicrobial agent. Kuwanon C, E, T, morusin, and albafuran C showed synergy (FICi 0.375-0.5) with oxacillin and/or kanamycin. Prenylated phenolics disrupted membrane permeability statistically significantly (from 28 ± 16.48% up to 73 ± 2.83%), and membrane disruption contributes to the complex antibacterial activity against MRSA. In addition, kuwanon C could be considered an efflux pump inhibitor. Despite the antibacterial effect on MRSA and the multiple biological activities, the prenylated phenolics at microbially significant concentrations have a minor effect on human keratinocyte (HaCaT) viability. In conclusion, prenylated phenolics in combination with commonly used antibiotics are promising candidates for the treatment of MRSA infections and wound healing, although further studies are needed.
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ETHNOPHARMACOLOGICAL RELEVANCE: Paulownia tomentosa Steud., a traditional Chinese medicinal plant, was used for many centuries in Chinese herbal medicine as a component of remedies for many illnesses, including inflammatory diseases. It is a rich source of phenolic compounds, mainly geranylated flavonoids, which are currently studied for their promising biological activities. AIM OF THE STUDY: The study aimed to isolate minor geranylated flavanones and flavones from P. tomentosa fruit and evaluate their cytotoxicity and possible anti-inflammatory effects in a cell-based model of inflammation. MATERIALS AND METHODS: Chromatographic separation of chloroform portion of the ethanolic extract of P. tomentosa fruit led to the isolation of twenty-seven flavonoids (1-27), twenty-six of them geranylated with different modifications and one non-geranylated flavanone, and two phenolic compounds. Compounds were identified using UV, IR, HRMS, NMR, and CD spectroscopy. Ten of these compounds (7-10, 12, 21, 22, 24, 25, and 27) were determined to be new flavonoid derivatives obtained from a natural source for the first time. Selected compounds were analyzed for cytotoxicity and anti-inflammatory potential to affect the activation of nuclear factor κB/activator protein 1 (NF-κB/AP-1) after lipopolysaccharide (LPS) stimulation. RESULTS: All the test compounds (1-21 and 23-26) reduced the activation of NF-κB/AP-1 24 h after the addition of LPS. Eight compounds (5, 14-18, 21, and 26) were more active than prednisone, a widely used anti-inflammatory drug. However, this effect was not seen significantly on the level of TNF-α and IL-1ß, which can be explained by the plurality of possible outcomes of activation of the NF-κB pathway in cells. CONCLUSIONS: Results of the presented study confirmed that constituents from traditional Chinese medicinal plant P. tomentosa Steud. have promising anti-inflammatory activities and can serve as a potential source of inspiration for new anti-inflammatory medications.
Assuntos
Lamiales , Plantas Medicinais , Anti-Inflamatórios/química , Flavonoides/análise , Frutas/química , Lipopolissacarídeos/farmacologia , NF-kappa B/metabolismo , Extratos Vegetais/análise , Extratos Vegetais/farmacologia , Plantas Medicinais/metabolismo , Fator de Transcrição AP-1/metabolismoRESUMO
Within the group of higher fungi, edible medicinal mushrooms have a long history of being used as food and in folk medicine. These species contain biologically active substances with many potential beneficial effects on human health. The Pleurotus genus is representative of medicinal mushrooms because Pleurotus ostreatus is one of the most commonly cultivated culinary mushrooms. In our study, we focused on lesser-known species in the genus Pleurotus and measured their antioxidant and anti-inflammatory activity. We prepared extracts of the mushrooms and analyzed them using HPLC-HRMS, GC-MS, and 1H-NMR. Significant differences in biological activities were found among the Pleurotus spp. extracts. A MeOH extract of P. flabellatus was the most active as a radical scavenger with the highest ORAC, while a chloroform extract had significant anti-inflammatory COX-2 activity. The 80% MeOH extract of P. flabellatus contained the highest amounts of ergosterol, ergothioneine, and mannitol. The 80% MeOH extract of P. ostreatus Florida was the most active in the NF-κB inhibition assay and had the highest content of ß-glucans (43.3% by dry weight). Given the antioxidant and anti-inflammatory properties of P. flabellatus, the potential therapeutic usefulness of this species is worth evaluating through in-depth investigations and confirmation by clinical trials.
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Glucan particles (GPs) from Saccharomyces cerevisiae consist mainly of ß-1,3-d-glucan. Curcumin is a phenolic compound of plant origin. A 24 h incubation with a mixture of GPs and curcumin increased the expression of the Nrf2 protein and increased the activation of the Nrf2-ARE system significantly.
Assuntos
Antioxidantes , Curcumina , Glucanos/química , Estresse Oxidativo/efeitos dos fármacos , Saccharomyces cerevisiae/química , Antioxidantes/química , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Curcumina/química , Curcumina/farmacologia , Composição de Medicamentos , Células Hep G2 , Humanos , Fator 2 Relacionado a NF-E2/metabolismo , Células THP-1RESUMO
Yeast glucan particles (GPs) are promising agents for the delivery of biologically active compounds as drugs. GPs possess their own biological activities and can act synergistically with their cargo. This study aimed to determine how incorporating artemisinin, ellagic acid, (-)-epigallocatechin gallate, morusin, or trans-resveratrol into GPs affects their anti-inflammatory and antioxidant potential in vitro. Two different methods - slurry evaporation and spray drying - were used to prepare composites (GPs + bioactive compound) and the anti-inflammatory and antioxidative properties of the resultant products were compared. Several of the natural compounds showed the beneficial effects of being combined with GPs. The materials prepared by spray drying showed greater activity than those made using a rotary evaporator. Natural compounds incorporated into yeast GPs showed greater anti-inflammatory potential in vitro than simple suspensions of these compounds as demonstrated by their inhibition of the activity of transcription factors NF-κB/AP-1 and the secretion of the pro-inflammatory cytokine TNF-α.
Assuntos
Glucanos/química , Glucanos/farmacologia , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Artemisininas/farmacologia , Catequina/análogos & derivados , Catequina/química , Catequina/farmacologia , Citocinas , Ácido Elágico/química , Ácido Elágico/farmacologia , Flavonoides/química , Flavonoides/farmacologia , Monócitos/efeitos dos fármacos , NF-kappa B , Resveratrol/química , Resveratrol/farmacologia , Saccharomyces cerevisiae , Proteínas de Saccharomyces cerevisiaeRESUMO
The aim of the research was to produce edible packaging based on chitosan with the addition of various concentrations of extracts of blueberry, red grape and parsley marcs. Packaging was made from extrudate extracts, which were subsequently analyzed by physicochemical methods: zeta-potential, gas barrier properties, thickness, water content, solubility, swelling degree, textural properties, total polyphenol content (TPC), polyphenols by high pressure liquid chromatography (HPLC), antioxidant activity, attenuated total reflectance Fourier-Transform spectroscopy (FTIR), antimicrobial activity and determination of migration of bioactive substances. The results indicate that a higher content of plant extracts have a statistically significant (p < 0.05) influence on properties of experimentally produced edible films. Edible films produced with the highest concentrations of red grapes marc extracts showed the most advantageous properties since antimicrobial activity against E. coli were the highest in this kind of produced film. The physical properties of edible films were also improved by the addition of extracts; gas permeability toward oxygen can be defined as advantageous, as can swelling degree, which decreased with higher concentrations of extracts. The research emphasized the possibility to use plant foodstuffs by-products in the production of edible/biodegradable films, helping in the overall sustainability and eco-friendliness of food/package production.
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Antiradical and cytoprotective activities of several flavanones isolated from Paulownia tomentosa (Thunb.) Steud. (Scrophulariaceae) have been evaluated using different in vitro and in vivo methods. The capacity of flavanones to scavenge radicals was measured in vitro by means of DPPH and ABTS assays, the inhibition of hydroxyl radicals produced in Fenton reactions, FRAP, scavenging superoxide radicals using enzymatic and nonenzymatic assays and the inhibition of peroxynitrite-induced nitration of tyrosine. The in vivo testing involved measuring the cytoprotective effect of chosen flavanones against alloxan-induced diabetes in mice. The activity of tested compounds was expressed either as a Trolox® equivalent or was compared with rutin or morine as known antioxidant compounds. The highest activity in most tests was observed for diplacone and 3´-O-methyl-5´-hydroxydiplacone, and the structure vs. the antioxidant activity relationship of geranyl or prenyl-substituted flavonoids with different substitutions at the B and C ring was discussed.
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Citoproteção/efeitos dos fármacos , Flavanonas/farmacologia , Sequestradores de Radicais Livres/farmacologia , Scrophulariaceae/química , Animais , Diabetes Mellitus Experimental/tratamento farmacológico , Flavanonas/isolamento & purificação , Sequestradores de Radicais Livres/isolamento & purificação , Frutas/química , Camundongos , Relação Estrutura-AtividadeRESUMO
Sulfate is present in foods, beverages, and drinking water. Its reduction and concentration in the gut depend on the intestinal microbiome activity, especially sulfate-reducing bacteria (SRB), which can be involved in inflammatory bowel disease (IBD). Assimilatory sulfate reduction (ASR) is present in all living organisms. In this process, sulfate is reduced to hydrogen sulfide and then included in cysteine and methionine biosynthesis. In contrast to assimilatory sulfate reduction, the dissimilatory process is typical for SRB. A terminal product of this metabolism pathway is hydrogen sulfide, which can be involved in gut inflammation and also causes problems in industries (due to corrosion effects). The aim of the review was to compare assimilatory and dissimilatory sulfate reduction (DSR). These processes occur in some species of intestinal bacteria (e.g., Escherichia and Desulfovibrio genera). The main attention was focused on the description of genes and their location in selected strains. Their coding expression of the enzymes is associated with anabolic processes in various intestinal bacteria. These analyzed recent advances can be important factors for proposing possibilities of metabolic pathway extension from hydrogen sulfide to cysteine in intestinal SRB. The switch from the DSR metabolic pathway to the ASR metabolic pathway is important since toxic sulfide is not produced as a final product.
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Bactérias/patogenicidade , Microbioma Gastrointestinal/imunologia , Sulfatos/metabolismo , Humanos , Redes e Vias MetabólicasRESUMO
(4-Oxo-2-thioxothiazolidin-3-yl)acetic acids exhibit a wide range of pharmacological activities. Among them, the only derivative used in clinical practice is the aldose reductase inhibitor epalrestat. Structurally related compounds, [(5Z)-(5-arylalkylidene-4-oxo-2-thioxo-1,3-thiazolidin-3-yl)]acetic acid derivatives were prepared previously as potential antifungal agents. This study was aimed at the determination of aldose reductase inhibitory action of the compounds in comparison with epalrestat and evaluation of structure-activity relationships (SAR). The aldose reductase (ALR2) enzyme was isolated from the rat eye lenses, while aldehyde reductase (ALR1) was obtained from the kidneys. The compounds studied were found to be potent inhibitors of ALR2 with submicromolar IC50 values. (Z)-2-(5-(1-(5-butylpyrazin-2-yl)ethylidene)-4-oxo-2-thioxothiazolidin-3-yl)acetic acid (3) was identified as the most efficacious inhibitor (over five times more potent than epalrestat) with mixed-type inhibition. All the compounds also exhibited low antiproliferative (cytotoxic) activity to the HepG2 cell line. Molecular docking simulations of 3 into the binding site of the aldose reductase enzyme identified His110, Trp111, Tyr48, and Leu300 as the crucial interaction counterparts responsible for the high-affinity binding. The selectivity factor for 3 in relation to the structurally related ALR1 was comparable to that for epalrestat. SAR conclusions suggest possible modifications to improve further inhibition efficacy, selectivity, and biological availability in the group of rhodanine carboxylic acids.
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Ácido Acético/farmacologia , Aldeído Redutase/antagonistas & inibidores , Inibidores Enzimáticos/farmacologia , Ácido Acético/síntese química , Ácido Acético/química , Aldeído Redutase/metabolismo , Animais , Sítios de Ligação , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Células Hep G2 , Humanos , Cristalino/efeitos dos fármacos , Cristalino/enzimologia , Ligantes , Masculino , Ratos Wistar , Rodanina/análogos & derivados , Rodanina/química , Rodanina/farmacologia , Tiazolidinas/química , Tiazolidinas/farmacologiaRESUMO
Recently, the problem of viral infection, particularly the infection with herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2), has dramatically increased and caused a significant challenge to public health due to the rising problem of drug resistance. The antiherpetic drug resistance crisis has been attributed to the overuse of these medications, as well as the lack of new drug development by the pharmaceutical industry due to reduced economic inducements and challenging regulatory requirements. Therefore, the development of novel antiviral drugs against HSV infections would be a step forward in improving global combat against these infections. The incorporation of biologically active natural products into anti-HSV drug development at the clinical level has gained limited attention to date. Thus, the search for new drugs from natural products that could enter clinical practice with lessened resistance, less undesirable effects, and various mechanisms of action is greatly needed to break the barriers to novel antiherpetic drug development, which, in turn, will pave the road towards the efficient and safe treatment of HSV infections. In this review, we aim to provide an up-to-date overview of the recent advances in natural antiherpetic agents. Additionally, this paper covers a large scale of phenolic compounds, alkaloids, terpenoids, polysaccharides, peptides, and other miscellaneous compounds derived from various sources of natural origin (plants, marine organisms, microbial sources, lichen species, insects, and mushrooms) with promising activities against HSV infections; these are in vitro and in vivo studies. This work also highlights bioactive natural products that could be used as templates for the further development of anti-HSV drugs at both animal and clinical levels, along with the potential mechanisms by which these compounds induce anti-HSV properties. Future insights into the development of these molecules as safe and effective natural anti-HSV drugs are also debated.