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1.
Braz J Biol ; 83: e244551, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34378661

RESUMO

Origanum vulgare has been of great interest in academia and pharma industry due to its antioxidant, antifungal and antitumor properties. The present study aimed to find the anti-MRSA potential and in vivo toxicity assessments of O. vulgare. O. vulgare extract was used to monitor anti-MRSA activity in mice. Following MRSA established infection in mice (Mus musculus), treatment with O. vulgare was continued for 7 days. Autopsies were performed and re-isolation, gross lesion scoring and bacterial load in various organs were measured. Additionally, blood sample was analysed for hematological assays. Toxicity assessment of O. vulgare potential as medicine was done at 200 mg/kg and 400 mg/kg by evaluating liver and kidney functions. Bacterial load and gross lesion in lungs and heart were significantly low compared to positive control following O. vulgare treatment. Likewise, O. vulgare treated groups had hematological, neutrophil and TLC values similar to control groups. Increased AST, ALP and total bilirubin alongwith marked hepatocellular degeneration and distortion around the central vein, inflammatory cell infiltration, and cytoplasmic vacuolization of hepatic cells was observed at higher dose. It is concluded that crude extract of O. vulgare may contain beneficial secondary metabolites and in future may be explored for curing infectious diseases.


Assuntos
Anti-Infecciosos , Óleos Voláteis , Origanum , Animais , Anti-Infecciosos/toxicidade , Antioxidantes , Fígado , Camundongos , Extratos Vegetais/toxicidade
2.
Molecules ; 26(16)2021 Aug 23.
Artigo em Inglês | MEDLINE | ID: mdl-34443693

RESUMO

The multi-step synthesis, physico-chemical characterization, and biological activity of novel valine-derived compounds, i.e., N-acyl-α-amino acids, 1,3-oxazol-5(4H)-ones, N-acyl-α-amino ketones, and 1,3-oxazoles derivatives, bearing a 4-[(4-chlorophenyl)sulfonyl]phenyl moiety are reported here. The structures of the newly synthesized compounds were confirmed by spectral (UV-Vis, FT-IR, MS, 1H- and 13C-NMR) data and elemental analysis results, and their purity was determined by RP-HPLC. The new compounds were assessed for their antimicrobial activity and toxicity to aquatic crustacean Daphnia magna. Also, in silico studies regarding their potential mechanism of action and toxicity were performed. The antimicrobial evaluation revealed that the 2-{4-[(4-chlorophenyl)sulfonyl]benzamido}-3-methylbutanoic acid and the corresponding 1,3-oxazol-5(4H)-one exhibited antimicrobial activity against Gram-positive bacterial strains and the new 1,3-oxazole containing a phenyl group at 5-position against the C. albicans strain.


Assuntos
Anti-Infecciosos/síntese química , Anti-Infecciosos/toxicidade , Ácido Benzoico/síntese química , Ácido Benzoico/toxicidade , Simulação por Computador , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Ácido Benzoico/química , Ácido Benzoico/farmacologia , Biofilmes/efeitos dos fármacos , Daphnia/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Testes de Sensibilidade Microbiana , Espectroscopia de Prótons por Ressonância Magnética , Testes de Toxicidade
3.
Molecules ; 26(13)2021 Jul 02.
Artigo em Inglês | MEDLINE | ID: mdl-34279398

RESUMO

The aim of this study was to compare the influence of the extraction method, chemical composition, antimicrobial effects, antioxidant activity, and cytotoxicity on human cells of the non-polar extracts of grape (Vitis labrusca) and blackberry (Rubus fruticosus) seeds. The Soxhlet (Sox), Bligh-Dyer (BD), and ultrasound (US) methods were used for extractions. For blackberry non-polar seed extract, extraction via the BD method showed the highest mean values of total phenolic content (TPC), expressed in milligrams of gallic acid equivalent per 100 mL of non-polar seed extracts (102.37 mg GAE/100 mL), and higher antioxidant activity in relation to the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical, expressed in milligrams of gallic acid equivalent per 100 mL of non-polar seed extracts (11.50 mg AAE/100 mL), if compared with the Sox and US extractions. Similar results were obtained for the non-polar grape seed extracts, where BD extraction obtained the highest values for TPC (28.61 mg GAE/100 mL) and DPPH (35.36 mg AAE/100 mL). The type of extraction method had an impact on the composition of fatty acids. Only the non-polar blackberry and grape seed extracts obtained via the Sox method showed some in vitro inhibitory effect against Escherichia coli (IAL 2064) and Staphylococcus aureus (ATCC 13565). Regardless of the extraction method used, the non-polar blackberry and grape seed extracts did not decrease the cell viability (IC50 >1000 µg/mL) of cancer and normal cell lines, thus indicating the relative safety of the extracts. All the seed extracts decreased the generation of reactive oxygen species in the cell lines. Blackberry and grape seed lipid fractions can be utilized as antioxidants, and the extraction methods used cause significant changes in relation to their bioactivity and chemical composition.


Assuntos
Anti-Infecciosos/química , Antioxidantes/química , Extrato de Sementes de Uva/química , Rubus/química , Anti-Infecciosos/farmacologia , Anti-Infecciosos/toxicidade , Antioxidantes/farmacologia , Antioxidantes/toxicidade , Escherichia coli/efeitos dos fármacos , Ácidos Graxos/análise , Flavonoides/análise , Extrato de Sementes de Uva/farmacologia , Staphylococcus aureus/efeitos dos fármacos
4.
Environ Toxicol Pharmacol ; 87: 103718, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34329803

RESUMO

Exposure to the antimicrobial agent Triclosan (TCS) induces oxidative stress in diverse organisms, including birds. However, whether TCS-induced oxidative stress effectively translates into detrimental effects is still unclear. The present study examined whether prenatal TCS exposure induces oxidative stress and telomere shortening in the brain and the liver of near-term embryos of the yellow-legged gull (Larus michahellis). Prenatal TCS exposure caused a significant overproduction of reactive oxygen species (ROS) in the brain, but no oxidative damage occurred. Telomeres of TCS-exposed embryos had brain telomeres 30 % shorter compared to controls, probably because the relatively modest antioxidant defenses of this organ during prenatal development cannot counteract the impact of the TCS-induced ROS. No telomere shortening was observed in the liver. Our results demonstrated that prenatal exposure to TCS in wild bird species can modulate the oxidative status and induce telomere shortening in the brain of the yellow-legged gull embryos.


Assuntos
Anti-Infecciosos/toxicidade , Encéfalo/efeitos dos fármacos , Charadriiformes/embriologia , Charadriiformes/genética , Encurtamento do Telômero/efeitos dos fármacos , Triclosan/toxicidade , Animais , Encéfalo/embriologia , Encéfalo/metabolismo , Dano ao DNA , Embrião não Mamífero/efeitos dos fármacos , Embrião não Mamífero/metabolismo , Feminino , Masculino , Estresse Oxidativo/efeitos dos fármacos
5.
Ecotoxicol Environ Saf ; 220: 112398, 2021 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-34116333

RESUMO

Presently, toxicological assessment of multiple veterinary antimicrobials has not been performed on mammals. In this study, we assessed the short-term toxicity of enrofloxacin (E) combined with colistin (C) and quinocetone (Q). Young male rats were orally dosed drug mixtures and single drugs in 14 consecutive days, each at the dose of 20, 80, and 400 mg/(kg·BW) for environmental toxicologic study. The results showed that at the high dose treatment, the combination of E + C+Q significantly decreased body intake, lymphocytes count on rats; significantly increased the values of Alanine aminotransferase (ALT), Glutamic oxaloacetic transaminase (AST) and, cholinesterase (CHE); it also got the severest histopathological changes, where sinusoidal congestion and a large number of black particles in sinusoids were observed. This means E + C+Q in the high dose groups was able to cause significant damage to the liver. Other combinations or doses did not induce significant liver damage. Transcriptome analysis was then performed on rats in high dose group for further research. For E + C and E + Q, an amount of 375 and 480 differently expressed genes were filtered out, revealing their possible underlying effect on genomes. For E + C+Q, a weighted gene co-expression network analysis was performed and 96 hub genes were identified to reveal the specific effect induced by this combination. This study indicates that joint toxicity should be taken into consideration when involving the risk assessment of these antimicrobials.


Assuntos
Anti-Infecciosos/toxicidade , Colistina/toxicidade , Enrofloxacina/toxicidade , Expressão Gênica/efeitos dos fármacos , Fígado/efeitos dos fármacos , Quinoxalinas/toxicidade , Drogas Veterinárias/toxicidade , Alanina Transaminase/metabolismo , Animais , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/farmacologia , Aspartato Aminotransferases/metabolismo , Colistina/administração & dosagem , Combinação de Medicamentos , Resíduos de Drogas , Enrofloxacina/administração & dosagem , Exposição Ambiental , Perfilação da Expressão Gênica , Humanos , Fígado/enzimologia , Fígado/patologia , Masculino , Quinoxalinas/administração & dosagem , Ratos Sprague-Dawley , Fatores de Tempo , Drogas Veterinárias/administração & dosagem
6.
Ecotoxicol Environ Saf ; 220: 112389, 2021 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-34082246

RESUMO

Triclosan (TCS) is an endocrine-disrupting chemical (EDC), which is used ubiquitously as an antimicrobial ingredient in healthcare products and causes contamination in the environment such as air, water, and biosolid-amended soil. Exposure to TCS may increase the risk of reproduction diseases and health issues. Several groups, including ours, have proved that TCS increased the biosynthesis of steroid hormones in different types of steroidogenic cells. However, the precise mechanism of toxic action of TCS on increased steroidogenesis at a molecular level remains to be elucidated. In this study, we try to address the mode of action that TCS affects energy metabolism with increased steroidogenesis. We evaluated the adverse effects of TCS on energy metabolism and steroidogenesis in human ovarian granulosa cells. The goal is to elucidate how increased steroidogenesis can occur with a shortage of adenosine triphosphate (ATP) whereas mitochondria-based energy metabolism is impaired. Our results demonstrated TCS increased estradiol and progesterone levels with upregulated steroidogenesis gene expression at concentrations ranging from 0 to 10 µM. Besides, glucose consumption, lactate level, and pyruvate kinase transcription were increased. Interestingly, the lactate level was attenuated with increased steroidogenesis, suggesting that pyruvate fate was shifted away from the formation of lactate towards steroidogenesis. Our study is gathering evidence suggesting a mode of action that TCS changes energy metabolism by predominating glucose flow towards the biosynthesis of steroid hormones. To the best of our knowledge, this is the first report that TCS presents such toxic action in disrupting hormone homeostasis.


Assuntos
Anti-Infecciosos/toxicidade , Disruptores Endócrinos/toxicidade , Células da Granulosa/efeitos dos fármacos , Triclosan/toxicidade , Anaerobiose , Animais , Estradiol/metabolismo , Feminino , Regulação da Expressão Gênica/efeitos dos fármacos , Células da Granulosa/metabolismo , Humanos , Progesterona/metabolismo
7.
Artigo em Inglês | MEDLINE | ID: mdl-33979267

RESUMO

The popularity of nanotechnology results from the possibility of obtaining materials that have better chemical, electrical, thermal, mechanical, or optical properties. Nano-sized materials are characterized by an increased surface area, which improves their chemical reactivity and mobility. Due to their enhanced reactivity and appropriately small size, some nanoparticles are used as antimicrobial and antifungal agents. Nanoparticles exhibit antimicrobial potential through multifaceted mechanisms. The adhesion of nanoparticles to microbial cells, and reactive oxygen species, and their penetration inside the cells, have been recognized as the most prominent modes of antimicrobial action. This review presents the mechanism of action of nanometals and oxide nanoparticles used as antimicrobials and the mechanisms of bacterial resistance to the toxic effects of nanoparticles. The article presents methods of forming microorganism resistance to the toxic effects of nanoparticles and the negative impact of nanoparticles on human health.


Assuntos
Anti-Infecciosos/farmacologia , Nanopartículas/química , Nanopartículas/toxicidade , Anti-Infecciosos/química , Anti-Infecciosos/toxicidade , Humanos , Óxidos/química
8.
Food Chem Toxicol ; 153: 112284, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34044082

RESUMO

Aqueous extracts from blackcurrant press cake (BC), Norway spruce bark (NS), Scots pine bark (SP), and sea buckthorn leaves (SB) were obtained using maceration and pressurized hot water and tested for their bioactivities. Maceration provided the extraction of higher dry matter contents, including total phenolics (TPC), anthocyanins, and condensed tannins, which also impacted higher antioxidant activity. NS and SB extracts presented the highest mean values of TPC and antioxidant activity. Individually, NS extract presented high contents of proanthocyanidins, resveratrol, and some phenolic acids. In contrast, SB contained a high concentration of ellagitannins, ellagic acid, and quercetin, explaining the antioxidant activity and antibacterial effects. SP and BC extracts had the lowest TPC and antioxidant activity. However, BC had strong antiviral efficacy, whereas SP can be considered a potential ingredient to inhibit α-amylase. Except for BC, the other extracts decreased reactive oxygen species (ROS) generation in HCT8 and A549 cells. Extracts did not inhibit the production of TNF-alpha in lipopolysaccharide-stimulated THP-1 macrophages but inhibited the ROS generation during the THP-1 cell respiratory burst. The recovery of antioxidant compounds from these by-products is incentivized for high value-added applications.


Assuntos
Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Extratos Vegetais/farmacologia , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/toxicidade , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/toxicidade , Antioxidantes/isolamento & purificação , Antioxidantes/toxicidade , Bactérias/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Linhagem Celular Tumoral , Enterovirus Humano B/efeitos dos fármacos , Química Verde , Hippophae/química , Humanos , Testes de Sensibilidade Microbiana , Picea/química , Pinus sylvestris/química , Casca de Planta/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Folhas de Planta/química , Ribes/química
9.
Ecotoxicol Environ Saf ; 220: 112325, 2021 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-34052755

RESUMO

Triclosan (TCS), a ubiquitous antimicrobial agent, has been frequently detected in wild fish, leading to concerns regarding TCS safety in the aquatic environment. The present work aims to investigate the TCS-mediated effects on various tissues (the liver, gills, brain, and testes) of wild-sourced adult mosquitofish based on histological analysis and transcriptome. Severe morphological injuries were only found in the liver and gills. The histopathological alterations in the liver were characterized by cytoplasmic vacuolation and degeneration, eosinophilic cytoplasmic inclusions, and nuclear polymorphism. The gill lesions contained epithelial lifting, intraepithelial edema, fusion and shortening of the secondary lamellae. Consistently, the numbers of differently expressed genes (DEGs) identified by transcriptome were in the order of liver (1627) > gills (182) > brain (9) > testes (4). Trend-aligned histopathological and transcriptomic changes in the 4 tissues, suggesting the tissue-specific response manner of mosquitofish to TCS, and the liver and gills were the target organs. TCS interrupted many biological pathways associated with lipogenesis and lipid metabolism, transmembrane transporters, protein synthesis, and carbohydrate metabolism in the liver, and it induced nonspecific immune response in the gills. TCS-triggered hepatotoxicity and gills damnification may lead to inflammation, apoptosis, diseases, and even death in mosquitofish. TCS showed moderate acute toxicity and bioaccumulative property on mosquitofish, suggesting that prolonged or massive use of TCS may pose an ecological risk.


Assuntos
Anti-Infecciosos/toxicidade , Ciprinodontiformes/fisiologia , Brânquias/efeitos dos fármacos , Fígado/efeitos dos fármacos , Transcriptoma/efeitos dos fármacos , Triclosan/toxicidade , Animais , Relação Dose-Resposta a Droga , Masculino , Especificidade de Órgãos , Distribuição Aleatória
10.
Biochem Biophys Res Commun ; 550: 107-112, 2021 04 23.
Artigo em Inglês | MEDLINE | ID: mdl-33689880

RESUMO

Lipopolysaccharide (LPS) is a major pathogenic factor in endotoxin shock or sepsis. Most antibiotics have little clinical anti-endotoxin activity, but some antimicrobial peptides (AMPs) have been shown to be effective in blocking LPS. We identified a novel peptide from the skin secretions of Bombina maxima (B. _maxima) by challenging the skin of frogs with an LPS solution. Peptide 2 has an amino acid sequence of LVGKLLKGAVGDVCGLLPIC. Peptide 2 possesses low hemolytic activity, low cytotoxicity against RAW 264.7 cells, and strong anti-inflammatory activity. Moreover, peptide 2 plays an anti-inflammatory role by inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6). A biolayer interferometry (BLI) assay indicated that peptide 2 binds to LPS with strong affinity and that this interaction has an affinity constant (KD) value of 1.05 × 10-9 M. A survival study showed that peptide 2 possesses potent LPS-neutralizing activity to protect LPS-treated mice from death. In conclusion, we have identified a potent peptide with LPS neutralizing activity, which lays a foundation for future research and development.


Assuntos
Anuros/metabolismo , Lipopolissacarídeos/antagonistas & inibidores , Peptídeos/isolamento & purificação , Peptídeos/farmacologia , Sepse/tratamento farmacológico , Pele/química , Pele/metabolismo , Animais , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Anti-Infecciosos/toxicidade , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/toxicidade , Citocinas/biossíntese , Citocinas/genética , Citocinas/imunologia , Avaliação Pré-Clínica de Medicamentos , Hemólise/efeitos dos fármacos , Humanos , Lipopolissacarídeos/imunologia , Masculino , Camundongos , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Peptídeos/toxicidade , Ligação Proteica , Células RAW 264.7 , RNA Mensageiro/genética , Taxa de Sobrevida
11.
Chemosphere ; 271: 129818, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-33736217

RESUMO

The use of carbohydrates, as a part of surface-active compounds, has been studied due to their biodegradability and nontoxic profile. A series of alkyl glycosides containing d-lyxose and l-rhamnose with alkyl chains of 8-12 carbon atoms were investigated. The effects of structural variations on their physico-chemical and biological properties have been evaluated for a detailed understanding of their properties. Alkyl glycosides were tested on their toxicity against bacterial cells of the genus Pseudomonas (MTT assay), microbiological adhesion to hydrocarbons (MATH assay), cell surface hydrophobicity (Congo red assay), cell membrane permeability (crystal violet assay), and bacterial biofilm formation. Furthermore, their antifungal activity against two pathogenic microorganisms Candida albicans and Aspergillus niger was investigated using the disc diffusion method. Toxicological studies revealed that compounds could reduce the metabolic activity of bacterial cells only moderately but they increased the hydrophobicity of cell surface in Pseudomonas strains. In addition, alkyl glycosides changed the permeability of the cell membranes to the level of 30-40% for this strain. The compounds with an even number of carbon atoms in their alkyl chain promoted stronger bacterial biofilm formation on the glass surface. All studied derivatives demonstrated very strong antifungal activity against fungus A. niger but very small effect against C. albicans. Overall, the results showed that long-chain alkyl glycosides could be considered as inexpensive, biocompatible, nontoxic agents, and serve for the surface design to avoid bacterial adhesion as an alternative solution to antibiotic treatment.


Assuntos
Anti-Infecciosos , Tensoativos , Antibacterianos/toxicidade , Anti-Infecciosos/toxicidade , Antifúngicos/toxicidade , Candida albicans , Testes de Sensibilidade Microbiana , Tensoativos/toxicidade
12.
PLoS One ; 16(2): e0247531, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33630913

RESUMO

Silver nanoparticle (Ag-NP) is well known for its high antibacterial efficacy. However, its toxicity toward mammalian cells is still a concern in clinical applications. The aim of our study was to evaluate the composition effects of Ag-NP supported by silicate nanoplatelet (NSP) with respect to the cytotoxicity and genotoxicity, and was in reference to the poly (styrene-co-maleic anhydride)-supported Ag-NP (Ag-NP/SMA). The NSP at the geometric dimension of averaged 80 x 80 x 1 nm3 was prepared from the exfoliation of natural clays and used to support different weight ratio of Ag-NP. The supporting limitation of NSP on Ag-NP was below the weight ratio of 15/85 (Ag-NP to NSP), and the detached Ag-NP from the Ag-NP/NSP (30/70) and Ag-NP/SMA hybrids were observed by TEM. Ames test was performed to assess the mutagenic potential of different compositions of Ag-NP/NSP, only Ag-NP/NSP (30/70) and Ag-NP/SMA hybrids exhibited mutagenicity when the concentration was 1.09 ppm or higher. In viewing of cytotoxicity using MTT tests toward HaCaT cells, the IC30 of Ag-NP/NSP (1/99, 7/93 and 15/85) were 1416.7, 243.6, and 148.9 ppm respectively, while Ag-NP/SMA was 64.8 ppm. The IC30 of Ag-NP/NSP (1/99, 7/93 and 15/85) were at least 833, 78 and 7 folds higher than their corresponding minimum inhibitory concentrations (MIC) respectively, and whereas Ag-NP/SMA was 6.4 folds. The Ag-NP/NSP and Ag-NP/SMA hybrids had been further investigated for genotoxicity by chromosomal aberrations and in vivo micronucleus assay within the concentration at IC10 and IC30, only Ag-NP/SMA showed a higher frequency of chromosomal aberrations. Our findings indicated that the viability of utilizing the NSP to maintain Ag-NP for antimicrobial activity, and the high-surface area of NSP served as an excellent support for associating Ag-NP and consequently rendering the mitigation of the inherent toxicity of Ag-NP in clinical uses.


Assuntos
Anti-Infecciosos/toxicidade , Argila/química , Nanopartículas Metálicas/toxicidade , Silicatos/química , Prata/toxicidade , Sobrevivência Celular/efeitos dos fármacos , Células HaCaT , Humanos
13.
J Ethnopharmacol ; 270: 113873, 2021 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-33485970

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Usnic acid (UA) is one of the well-known lichen metabolites that induces liver injury. It is mainly extracted from Usnea longissima and U. diffracta in China or from other lichens in other countries. U. longissima has been used as traditional Chinese medicine for treatment of cough, pain, indigestion, wound healing and infection. More than 20 incidences with hepatitis and liver failure have been reported by the US Food and Drug Administration since 2000. UA is an uncoupler of oxidative phosphorylation causing glutathione and ATP depletion. Previous histological studies observed extensive cell and organelle swellings accompanied with hydrotropic vacuolization of hepatocytes. AIM OF THE STUDY: This study was to investigate the mechanism of UA-induced liver toxicity in normal human L02 liver cells and ICR mice using various techniques, such as immunoblotting and siRNA transfection. MATERIALS AND METHODS: Assays were performed to evaluate the oxidative stress and levels of GSH, MDA and SOD. Double flouresencence staining was used for the detection of apoptotic cell death. The protein expressions, such as glutathione S transferase, glutathione reductase, glutathione peroxidase 4, catalase, c-Jun N-terminal protein kinase, caspases, gastamin-D and porimin were detected by Western blotting. Comparisons between transfected and non-transfected cells were applied for the elucidation of the role of porimin in UA-induced hepatotoxicity. Histopathological examination of mice liver tissue, serum total bilirubin and hepatic enzymes of alanine aminotransferase and aspatate aminotransferase were also studied. RESULTS: The protein expressions of glutathione reductase, glutathione S transferase and glutathione peroxidase-4 were increased significantly in normal human L02 liver cells. Catalase expression was diminished in dose-dependent manner. Moreover, (+)-UA did not induce the activation of caspase-3, caspase-1 or gasdermin-D. No evidence showed the occurrence of pyroptosis. However, the porimin expressions were increased significantly. In addition, (+)-UA caused no cytotoxicity in the porimin silencing L02 cells. CONCLUSIONS: In conclusion, (+)-UA induces oncotic L02 cell death via increasing protein porimin and the formation of irreversible membrane pores. This may be the potential research area for future investigation in different aspects especially bioactivity and toxicology.


Assuntos
Anti-Infecciosos/toxicidade , Benzofuranos/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Hepatócitos/efeitos dos fármacos , Hepatócitos/metabolismo , Peptídeos e Proteínas de Sinalização Intracelular/metabolismo , Isquemia/metabolismo , Receptores de Superfície Celular/metabolismo , Animais , Inibidores de Caspase/farmacologia , Caspases/metabolismo , Morte Celular/efeitos dos fármacos , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Doença Hepática Induzida por Substâncias e Drogas/patologia , Técnicas de Silenciamento de Genes , Glutationa/metabolismo , Glutationa/farmacologia , Humanos , Peptídeos e Proteínas de Sinalização Intracelular/efeitos dos fármacos , Peptídeos e Proteínas de Sinalização Intracelular/genética , Isquemia/induzido quimicamente , Proteínas Quinases JNK Ativadas por Mitógeno/metabolismo , Fígado/efeitos dos fármacos , Fígado/patologia , Camundongos Endogâmicos ICR , Necrose/induzido quimicamente , Estresse Oxidativo/efeitos dos fármacos , Proteínas de Ligação a Fosfato/metabolismo , Receptores de Superfície Celular/efeitos dos fármacos , Receptores de Superfície Celular/genética
14.
Environ Monit Assess ; 193(2): 77, 2021 Jan 20.
Artigo em Inglês | MEDLINE | ID: mdl-33474619

RESUMO

The presence of antimicrobials in wastewater (WW), surface water (SW), groundwater (GW), and even in potable water from treatment plants has been reported from many countries. Their presence in the water sources is causing the rise and spread of antimicrobial resistance (AMR), thereby threatening our public health, global economy, and development. This necessitates the constant monitoring of these compounds along with the evaluation of their associated risk to aquatic organisms. In this study, GW, WW, and SW samples from different parts of West Bengal (India) were analyzed using the SPE-HPLC-DAD method for detecting two frequently used fluoroquinolones (ciprofloxacin, CIP and ofloxacin, OFL). The highest concentration of CIP and OFL was 5.75 µg/L (GW) and 17.84 µg/L (WW), respectively. The antimicrobial activity was determined against Escherichia coli and Staphylococcus aureus isolates from WW against CIP, which showed that Escherichia coli and Staphylococcus aureus had developed ~ 69 and ~ 12 times resistance compared to their respective pure strains. The risk assessment showed that CIP poses an insignificant threat to fish and Daphnia (RQ < 1) but a significant threat to green algae and Microcystis aeruginosa (RQ> > 1). OFL concentration also poses a great threat to all the organisms for which the assessment was made (RQ> > 1). Moreover, risk assessment in terms of AMR showed that the present level of these antimicrobials in different water sources could cause the development of resistance among the microbial community (RQ > 1). These results emphasize the need for constant monitoring of pharmaceutical compounds, especially antimicrobials, to be kept under check.


Assuntos
Anti-Infecciosos , Monitoramento Ambiental , Animais , Antibacterianos/análise , Antibacterianos/toxicidade , Anti-Infecciosos/toxicidade , Ciprofloxacina , Índia , Testes de Sensibilidade Microbiana
15.
Prep Biochem Biotechnol ; 51(1): 54-68, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32701049

RESUMO

Silver nanoparticles (AgNPs) have unique properties and a large range of applications. Biosynthesis of stable AgNPs using the extracellular filtrate of Bacillus subtilis was proved by the characteristic surface plasmon resonance at about 420-430 nm. They were polycrystalline with spherical, hexagonal, and irregular shapes and they were negatively charged (-40 mV) with an average diameter of 20 nm. FTIR spectrum confirmed the presence of protein molecules coating AgNPs. The optimum conditions for the synthesis of tested AgNPs were 1:6 filtrate dilution, 1 mM AgNO3, pH 7, 30 °C , 48 h contact time under static and illuminating conditions. The synthesized AgNPs showed antibacterial activities against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus cereus, and Salmonella typhi, antifungal activity against Candida albicans and antiviral activity against rotavirus. Also, they showed potent cytotoxic effects on lung and hepatic carcinoma human cell lines. Meanwhile, the acute toxicity study against mice showed no significant changes in hematological, biochemical, and histological parameters of AgNPs treated mice. They also showed mild hepatoprotective effect in thioacetamide (TAA) - induced hepatic fibrosis in rats. AgNPs treated textiles fabrics showed high antimicrobial activities against different pathogenic microorganisms as well as UV protection adequacy.


Assuntos
Anti-Infecciosos/farmacologia , Antineoplásicos/farmacologia , Bacillus subtilis/química , Nanopartículas Metálicas/química , Prata/química , Têxteis , Células A549 , Animais , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/toxicidade , Antineoplásicos/administração & dosagem , Antineoplásicos/toxicidade , Candida albicans/efeitos dos fármacos , Chlorocebus aethiops , Escherichia coli/efeitos dos fármacos , Feminino , Células Hep G2 , Humanos , Masculino , Nanopartículas Metálicas/administração & dosagem , Nanopartículas Metálicas/toxicidade , Camundongos , Testes de Sensibilidade Microbiana , Pseudomonas aeruginosa/efeitos dos fármacos , Ratos , Ratos Wistar , Rotavirus/efeitos dos fármacos , Salmonella typhi/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos
16.
Eur J Pharmacol ; 890: 173649, 2021 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-33049300

RESUMO

Cathelicidins are a class of gene-encoded multifunctional factors in host defence systems. They have recently attracted a great deal of attention as promising drug candidates. Cathelicidins are well studied in vertebrates, yet no studies have been reported concerning gecko cathelicidin. Recently, we identified a novel cathelicidin from Gekko japonicus, Gj-CATH3. Unlike most cathelicidins, Gj-CATH3 exhibits potent antioxidant activity in vitro. Unfortunately, slight toxicity and high synthesis cost restrict its application. Thus, we designed a series of Gj-CATH3 analogues for development of short peptides with improved cell selectivity. Functional analysis showed that two truncated peptides, Gj-CATH3-(38-42)-peptide and Gj-CATH3-(33-42)-peptide, exhibited excellent antioxidant activity against ABTS and DPPH free radicals. Further, cytotoxicity and hemolytic activities were observably lower compared to Gj-CATH3. Interestingly, both peptides also demonstrate significant wound healing properties in a mouse model with full-thickness skin wounds. The peptides induce HaCaT cell proliferation and prevent decreases in SOD activity and increases of MDA concentration in injured-skin tissue. This report is the first to address cathelicidin from reptilia that exhibit potent wound healing activity. Our research will enrich understanding of cathelicidin biological functions, and provide a theoretical basis for its clinical application.


Assuntos
Anti-Infecciosos/química , Antioxidantes/química , Antioxidantes/farmacologia , Catelicidinas/química , Catelicidinas/farmacologia , Peptídeos/química , Peptídeos/farmacologia , Cicatrização/efeitos dos fármacos , Animais , Anti-Infecciosos/farmacologia , Anti-Infecciosos/toxicidade , Antioxidantes/toxicidade , Catelicidinas/genética , Catelicidinas/toxicidade , Linhagem Celular , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Modelos Animais de Doenças , Hemólise/efeitos dos fármacos , Humanos , Lagartos , Malondialdeído/metabolismo , Camundongos Endogâmicos ICR , Peptídeos/toxicidade , Pele/efeitos dos fármacos , Pele/lesões , Pele/patologia , Superóxido Dismutase/metabolismo
17.
ACS Appl Mater Interfaces ; 13(1): 1333-1344, 2021 Jan 13.
Artigo em Inglês | MEDLINE | ID: mdl-33351598

RESUMO

Dimethyl disulfide (DMDS), a promising alternative fumigant, has been highly desirable for excellent management of soil pests and diseases. However, high volatility and moderate toxicity of this sulfide limit its application. To address these issues, a novel controlled release formulation of DMDS was proposed employing multiple emulsions and polyurea microcapsules (DMDS@MEs-MCs). The successful combination of the two technologies was revealed by confocal laser scanning microscopy, scanning electron microscopy, thermogravimetric analysis, and Fourier transform infrared. According to the multiple encapsulation structure, the encapsulation efficiency decreased by only 3.13% after thermal storage, compared with a 15.21% decrease of microcapsules made with only a monolayer film. DMDS@MEs-MCs could effectively control the release of active ingredient, which increased applicator and environmental safety during application. Moreover, it could be facilely used by spraying and drip irrigation instead of a special fumigation device. The innovative formulation exhibited better control efficacy on soil pathogens (Fusarium spp. and Phytophthora spp.) and root-knot nematodes (Meloidogyne spp.) than DMDS technical concentration (DMDS TC). In addition, it did not inhibit seed germination after 10 days when the plastic film was removed from the fumigated soil. This method appears to be of broad interest for the development of safe and handy fumigant application.


Assuntos
Anti-Infecciosos/toxicidade , Cápsulas/química , Dissulfetos/toxicidade , Portadores de Fármacos/química , Emulsões/química , Polímeros/química , Animais , Cápsulas/toxicidade , Cucumis sativus/efeitos dos fármacos , Preparações de Ação Retardada/química , Preparações de Ação Retardada/toxicidade , Portadores de Fármacos/toxicidade , Liberação Controlada de Fármacos , Emulsões/toxicidade , Fusarium/efeitos dos fármacos , Phytophthora/efeitos dos fármacos , Polímeros/toxicidade , Microbiologia do Solo , Tylenchoidea/efeitos dos fármacos
18.
J Ethnopharmacol ; 264: 113291, 2021 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-32841700

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Plumeria rubra L. (Apocynaceae) is a deciduous, commonly ornamental, tropical plant grown in home premises, parks, gardens, graveyards, because of its beautiful and attractive flowers of various colours and size. The different parts of the plant are used traditionally to treat various diseases and conditions like leprosy, inflammation, diabetic mellitus, ulcers, wounds, itching, acne, toothache, earache, tongue cleaning, pain, asthma, constipation and antifertility. AIM OF THE REVIEW: The main aim of this review is to provide an overview and critically analyze the reported ethnomedical uses, phytochemistry, pharmacological activities and toxicological studies of P. rubra and to identify the remaining gaps and thus supply a basis for further investigations. The review also focuses towards drawing attention of people and researchers about the wide spread pharmaceutical properties of the plant for its better utilization in the coming future. MATERIAL AND METHODS: All the relevant data and information on P. rubra was gathered using various databases such as PubMed, Springer, Taylor and Francis imprints, NCBI (National Center for Biotechnology Information), Science direct, Google scholar, Chemspider, SciFinder, research and review articles from peer-reviewed journals and unpublished data such as Phd thesis, etc. Some other 'grey literature' sources such as webpages, ethnobotanical books, chapters, wikipedia were also studied. RESULTS: More than 110 chemical constituents have been isolated from P. rubra including iridoids, terpenoids, flavonoids and flavonoid glycosides, alkaloids, glycosides, fatty acid esters, carbohydrates, animo acids, lignan, coumarin, volatile oils, etc. The important chemical constituents responsible for pharmacological activities of the plant are fulvoplumierin, plumieride, rubrinol, lupeol, oleanolic acid, stigmasterol, taraxasteryl acetate, plumieride-p-E-coumarate, rubranonoside, rubrajalellol, plumericin, isoplumericin, etc. The plant possess a wide range of pharmacological activities present namely antibacterial, antiviral, anti-inflammatory, antipyretic, antidiabetic, hepatoprotective, anticancer, anthelmintic, antifertility and many other activities. CONCLUSION: P. rubra is a valuable medicinal source and further study in this topic can validate the traditional and ethnobotanical use of the plant. However, many aspects of the plant have not been studied yet. The pharmacological activity of active chemical constituent isolated from the plant is proven only for a couple of activities hence, lack of bio-guided isolation strategies is observed. Further studies on bioavailability, pharmacokinetics, mechanism of action and structural activity relationship studies of isolated pure compounds will contribute more in understanding their pharmacological effects. Higher doses of plant extracts are administered to experimental animals, therefore their toxicity and side effects in humans are needed to be thoroughly studied, although no side effect or toxicity is seen or observed in experimental animals. Studies are also essential to investigate the long term in vivo toxicity and clinical efficacy of the plant.


Assuntos
Apocynaceae , Etnofarmacologia/métodos , Compostos Fitoquímicos/toxicidade , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/toxicidade , Extratos Vegetais/uso terapêutico , Analgésicos/isolamento & purificação , Analgésicos/uso terapêutico , Analgésicos/toxicidade , Animais , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/uso terapêutico , Anti-Infecciosos/toxicidade , Etnofarmacologia/tendências , Humanos , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/uso terapêutico , Hipoglicemiantes/toxicidade , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/isolamento & purificação
19.
Biomed Pharmacother ; 133: 111052, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33378958

RESUMO

The irrational use of medications has increased the incidence of microbial infections, which are a major threat to public health. Moreover, conventional therapeutic strategies are starting to become ineffective to treat these infections. Hence, there is a need to develop and characterize novel antimicrobial compounds. Phytochemicals are emerging as a safe and accessible alternative to conventional therapeutics for treating infectious diseases. Curcumin is extracted from the dried rhizome of the spice turmeric (Curcuma longa (Zingiberaceae)). However, the bioavailability of curcumin is low owing to its lipophilic property and thus has a low therapeutic efficacy in the host. A previous study synthesized structural variants of curcumin, which are called monocurcuminoids (CNs). CNs are synthesized based on the chemical structure of curcumin with only one methyl bridge. The biological activities of four previously synthesized CNs (CN59, CN63, CN67, and CN77), curcumin, and turmeric powder were examined in this study. Gas chromatography-tandem mass spectrometry analysis of curcumin and turmeric powder revealed similar peaks, which indicated the presence of curcumin in turmeric powder. The antioxidant activity of the test compounds was evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) assays. The ABTS radical scavenging activities of the test compounds were similar to those of vitamin C. The minimum inhibitory concentration (MIC) values of the test compounds against seven microbial strains were in the range of 4.06-150 µg/mL. The MIC value was equal to minimum bactericidal concentration value for CN63 (150 µg/mL) and CN67 (120 µg/mL) against Staphylococcus aureus. The treatment combination of CN77 (8.75 or 4.37 µg/mL) and turmeric powder (9.37 or 4.68 µg/mL) exerted synergistic growth-inhibiting effects on Aeromonas hydrophila, Candida albicans, and Pseudomonas aeruginosa. Photodynamic therapy using 2X MIC of CN59 decreased the growth of Enterococcus faecalis by 4.18-fold compared to the control group and completely inhibited the growth of Escherichia coli. The results of the hemolytic assay revealed that the test compounds were not cytotoxic with half-maximal inhibitory concentration values ranging from 49.65-130.9 µM. The anticoagulant activity of most compounds was comparable to that of warfarin but higher than that of heparin. This indicated that these compounds target the intrinsic coagulation pathway. These results demonstrated that these CNs are a safe and promising alternative for curcumin.


Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Bactérias/efeitos dos fármacos , Bioprospecção , Candida albicans/efeitos dos fármacos , Diarileptanoides/farmacologia , Fotoquimioterapia , Fármacos Fotossensibilizantes/farmacologia , Animais , Anti-Infecciosos/síntese química , Anti-Infecciosos/toxicidade , Antioxidantes/síntese química , Antioxidantes/toxicidade , Bactérias/crescimento & desenvolvimento , Benzotiazóis/química , Compostos de Bifenilo/química , Coagulação Sanguínea/efeitos dos fármacos , Candida albicans/crescimento & desenvolvimento , Diarileptanoides/síntese química , Diarileptanoides/toxicidade , Resistência Microbiana a Medicamentos , Hemólise/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Fármacos Fotossensibilizantes/síntese química , Fármacos Fotossensibilizantes/toxicidade , Picratos/química , Carneiro Doméstico , Ácidos Sulfônicos/química
20.
Ecotoxicol Environ Saf ; 207: 111178, 2021 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-32905931

RESUMO

Acibenzolar-S-methyl (ASM) is one of the most effective plant resistance activators and protects against a broad spectrum of fungal, bacterial and viral pathogens. A rapid, efficient and high-throughput analysis method for ASM and its metabolite acibenzolar acid in fruits and vegetables was developed using potato, garlic, cabbage, grape and tomato as representative commodities by modified QuEChERS and UPLC-MS/MS. The modified procedure showed satisfying recoveries (70-108%) fortified in the range of 0.01-1 mg/kg with relative standard deviations (RSDs) lower than 17.7%. With the established analytical method, the dietary risk of ASM in fruits and vegetables from Chinese markets were further monitored using risk quotient (RQ) method. The RQ value based on ASM residue in China are far less than 1, elucidating that the potential health risk induced by ASM ingestion for Chinese population is not significant. Comparing the residue and risk assessment results of ASM in agricultural products in China to those in Codex, the maximum residue limits (MRLs) for ASM on garlic, cabbage and tomato established by CAC (Codex Alimentarius Commission) can be safely adopted in China, whereas the MRLs on potato and grape in China should be proposed as 0.01 mg/kg.


Assuntos
Anti-Infecciosos/toxicidade , Tiadiazóis/toxicidade , Brassica , China , Cromatografia Líquida/métodos , Exposição Dietética , Frutas/química , Alho , Lycopersicon esculentum , Medição de Risco , Solanum tuberosum , Espectrometria de Massas em Tandem/métodos , Verduras/química , Vitis
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