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1.
Carbohydr Polym ; 250: 116800, 2020 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-33049807

RESUMO

Chitosan, as a biodegradable and biocompatible polymer, is characterized by anti-microbial and anti-cancer properties. It lately has received a widespread interest for use as the pulmonary particulate backbone materials of drug carrier for the treatment of infectious disease and cancer. The success of chitosan as pulmonary particulate drug carrier is a critical interplay of their mucoadhesive, permeation enhancement and site/cell-specific attributes. In the case of nanocarriers, various microencapsulation and micro-nano blending systems have been devised to equip them with an appropriate aerodynamic character to enable efficient pulmonary aerosolization and inhalation. The late COVID-19 infection is met with acute respiratory distress syndrome and cancer. Chitosan and its derivatives are found useful in combating HCoV and cancer as a function of their molecular weight, substituent type and its degree of substitution. The interest in chitosan is expected to rise in the next decade from the perspectives of drug delivery in combination with its therapeutic performance.


Assuntos
Anti-Infecciosos/química , Antineoplásicos/química , Quitosana/análogos & derivados , Portadores de Fármacos/química , Anti-Infecciosos/farmacologia , Anti-Infecciosos/uso terapêutico , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Betacoronavirus/isolamento & purificação , Materiais Biocompatíveis/química , Sobrevivência Celular/efeitos dos fármacos , Infecções por Coronavirus/tratamento farmacológico , Infecções por Coronavirus/patologia , Infecções por Coronavirus/virologia , Humanos , Neoplasias Pulmonares/patologia , Pandemias , Pneumonia Viral/tratamento farmacológico , Pneumonia Viral/patologia , Pneumonia Viral/virologia
2.
PLoS One ; 15(8): e0237567, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32797097

RESUMO

Distinct morphological MgO nanoparticles (MgONPs) were synthesized using biomasses of Saussurea costus roots. The biomass of two varieties of Saussurea costus (Qustal hindi and Qustal bahri) were used in the green synthesis of MgONPs. The physical and chemical features of nanoparticles were confirmed by spectroscopic and microscopic techniques. The surface morphology of the obtained nanoparticles was detected at different magnifications by SEM and TEM microscopy and the size of nanoparticles were found to be 30 and 34 nm for Qustal hindi and Qustal bahri, respectively. The antimicrobial activity of the prepared MgONPs was screened against six pathogenic strains. The synthesized nanoparticles by Qustal bahri biomass exerted significant inhibition zones 15, 16, 18, 17, 14, and 10 mm against E. coli, P. aeruginosa, C. tropicalis and C. glabrata, S. aureus and B. subtilis as compared to those from Qustal hindi 12, 8 and 17 mm against B. subtilis, E. coli and C. tropicalis, respectively. MgONPs showed a potential cytotoxicity effect against MCF-7 breast cancer cell lines. Cellular investigations of MgONPs revealed that the prepared nanoparticles by Qustal bahri exhibited high cytotoxicity against MCF-7 cancer cell lines. IC50 values in MCF-7 cells were found to be 67.3% and 52.1% for MgONPs of Saussurea costus biomasses, respectively. Also, the photocatalytic activity of MgONPs of each Saussurea costus variety was comparatively studied. They exhibited an enhanced photocatalytic degradation of methylene blue after UV irradiation for 1 h as 92% and 59% for those prepared by Qustal bahri and Qustal hindi, respectively. Outcome of results revealed that the biosynthesized MgONPs showed promising biomedical potentials.


Assuntos
Anti-Infecciosos/farmacologia , Antineoplásicos/farmacologia , Neoplasias da Mama/tratamento farmacológico , Óxido de Magnésio/farmacologia , Azul de Metileno/química , Saussurea/química , Anti-Infecciosos/química , Antineoplásicos/química , Bactérias/efeitos dos fármacos , Biomassa , Catálise , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Feminino , Fungos/efeitos dos fármacos , Química Verde , Humanos , Células MCF-7 , Óxido de Magnésio/química , Nanopartículas Metálicas/química , Testes de Sensibilidade Microbiana , Processos Fotoquímicos , Extratos Vegetais/química , Raízes de Plantas/química
3.
PLoS One ; 15(7): e0236319, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32726328

RESUMO

Jacaranda mimosifolia trees are grown in frost-free regions globally. The aim of this study was to evaluate the methanol crude extract and various fractions of increasing polarity of J. mimosifolia leaves for bioactive metabolites, as well as antimicrobial, antioxidant and anticancer activities. The anti-inflammatory potential of the various fractions of J. mimosifolia leaf extract was studied via the lipoxygenase (LOX) inhibitory assay. Methanol crude extract (ME), derived fractions extracted with chloroform (CF) and ethyl acetate (EAF), and residual aqueous extract (AE) of dried J. mimosifolia leaves were assayed for polyphenolic compounds, their antioxidant, antimicrobial and lipoxygenase (LOX) inhibitory activities, and anticancer properties. Polyphenolic compounds were determined via HPLC while phytochemicals (total phenolics, flavonoids, tannins and ortho-diphenol contents), antioxidant activities (DPPH, hydrogen peroxideperoxide, hydroxyl and superoxide radical anions) and LOX were measured via spectrophotometry. Methanol extracts and various fractions were evaluated for antibacterial activities against Bacillus subtilis, Klebsiella pneumonia, Pseudomonas aeruginosa and Staphylococcus aureus. Antifungal potential of the fractions was tested against three species: Aspergillus flavus, Aspergillus fumigatus and Fusarium oxysporum. The highest values for total phenolic content (TPC), total flavonoid content (TFC), flavonols, tannins and ortho-diphenols were in the ME, followed by CF > EAF > AE. ME also had the highest antioxidant activity with EC50 values 48±1.3, 45±2.4, 42±1.3 and 46±1.3 µg/mL based on the DPPH, hydrogen peroxide, hydroxyl radical and superoxide radical assays, respectively. TPC and TFC showed a significant, strong and positive correlation with the values for each of these antioxidant activities. ME exhibited anti-inflammatory potential based on its LOX inhibitory activity (IC50 = 1.3 µg/mL). ME also had the maximum antibacterial and antifungal potential, followed by EAF > CF > AE. Furthermore, ME showed the strongest cytotoxic effect (EC50 = 10.7 and 17.3 µg/mL) against human hormone-dependent prostate carcinoma (LnCaP) and human lung carcinoma (LU-1) cell lines, respectively. Bioactive compounds present in leaf methanol extracts of J. mimosifolia were identified using gas chromatography-mass spectrometry (GC-MS). Fifteen compounds were identified including phenolic and alcoholic compounds, as well as fatty acids. Our results suggest that J. mimosifolia leaves are a good source of natural products with antioxidant, anti-inflammatory and anti-cancer properties for potential therapeutic, nutraceutical and functional food applications.


Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Bignoniaceae/química , Extratos Vegetais/farmacologia , Anti-Infecciosos/química , Antioxidantes/química , Aspergillus/efeitos dos fármacos , Aspergillus/patogenicidade , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Citotoxinas/química , Citotoxinas/farmacologia , Humanos , Inibidores de Lipoxigenase/química , Inibidores de Lipoxigenase/farmacologia , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Extratos Vegetais/química , Folhas de Planta/química , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/patogenicidade
4.
Plast Reconstr Surg ; 146(1): 91-103, 2020 07.
Artigo em Inglês | MEDLINE | ID: mdl-32590651

RESUMO

BACKGROUND: Host defense peptides are a family of endogenous short peptides that are found in all living beings and play a critical role in innate immunity against infection. METHODS: A nonsystematic review of host defense peptides was conducted with specific interest in properties and applications relevant to plastic and reconstructive surgery. RESULTS: In addition to their direct antimicrobial actions against pathogens, including multidrug-resistant bacteria, they also demonstrate important functions in immunomodulation, tumor cell lysis, and tissue regeneration. These properties have made them a topic of clinical interest for plastic surgeons because of their potential applications as novel antibiotics, wound healing medications, and cancer therapies. The rising clinical interest has led to a robust body of literature describing host defense peptides in great depth and breadth. Numerous mechanisms have been observed to explain their diverse functions, which rely on specific structural characteristics. However, these peptides remain mostly experimental, with limited translation to clinical practice because of numerous failures to achieve acceptable results in human trials. CONCLUSIONS: Despite the broad ranging potential of these peptides for use in the field of plastic and reconstructive surgery, they are rarely discussed in the literature or at scientific meetings. In this review, the authors provide a summary of the background, structure, function, bacterial resistance, and clinical applications of host defense peptides with the goal of stimulating host defense peptide-based innovation within the field of plastic and reconstructive surgery.


Assuntos
Peptídeos Catiônicos Antimicrobianos , Imunidade Inata/fisiologia , Procedimentos Cirúrgicos Reconstrutivos/métodos , Cirurgia Plástica/métodos , Anti-Infecciosos/química , Peptídeos Catiônicos Antimicrobianos/fisiologia , Peptídeos Catiônicos Antimicrobianos/uso terapêutico , Farmacorresistência Bacteriana/fisiologia , Humanos , Cicatrização/fisiologia
5.
Exp Parasitol ; 216: 107935, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32569599

RESUMO

Toxoplasma gondii is an important pathogen that causes serious public health problems. Currently, therapeutic drugs for toxoplasmosis cause serious side effects, and more effective and novel substances with relatively low toxicity are urgently needed. Ursolic acid (UA) has many properties that can be beneficial to healthcare. In this study, we synthesized eight series of UA derivatives bearing a tetrazole moiety and evaluated their anti-T. gondii activity in vitro using spiramycin as a positive control. Most of the synthesized derivatives exhibited better anti-T. gondii activity in vitro than UA, among which compound 12a exhibited the most potent anti-T. gondii activity. Furthermore, the results of biochemical parameter determination indicated that 12a effectively restored the normal body weight of mice infected with T. gondii, reduced hepatotoxicity, and exerted significant anti-oxidative effects compared with the findings for spiramycin. Additionally, our molecular docking study indicated that the synthesized compounds could act as potential inhibitors of T. gondii calcium-dependent protein kinase 1 (TgCDPK1), with 12a possessing strong affinity for TgCDPK1 via binding to the key amino acids GLU129 and TYR131.


Assuntos
Anti-Infecciosos/farmacologia , Toxoplasma/efeitos dos fármacos , Toxoplasmose Animal/tratamento farmacológico , Toxoplasmose/tratamento farmacológico , Triterpenos/farmacologia , Alanina Transaminase/sangue , Animais , Anti-Infecciosos/química , Anti-Infecciosos/uso terapêutico , Aspartato Aminotransferases/sangue , Coccidiostáticos/química , Coccidiostáticos/farmacologia , Modelos Animais de Doenças , Feminino , Glutationa/metabolismo , Fígado/efeitos dos fármacos , Fígado/enzimologia , Fígado/patologia , Malondialdeído/metabolismo , Camundongos , Simulação de Acoplamento Molecular , Tamanho do Órgão/efeitos dos fármacos , Inibidores de Proteínas Quinases/farmacologia , Proteínas Quinases , Distribuição Aleatória , Espiramicina/farmacologia , Baço/efeitos dos fármacos , Baço/patologia , Triterpenos/química , Triterpenos/uso terapêutico
6.
PLoS One ; 15(6): e0235193, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32584882

RESUMO

Antimicrobial resistance is becoming a growing health problem, which has become a challenge for the physicians to control infection and also an economic burden on the healthcare. This increase in resistance to the present antimicrobial agents led the researchers to find some alternative and more efficient drugs which can fight with the resistant microorganisms more effectively. Hence, in silico approach is used to design some novel drugs against various targets of microorganisms. For effective virtual screening of the drugs, there is a need to know about the chemical structure and properties of the antimicrobial agents. Therefore, we have prepared a comprehensive database as a platform for the researcher to search for possible lead molecules. Antimicrobial chemotherapeutics database (ACD) is comprised of ~4100 synthetic antimicrobial compounds as well as ~1030 active antimicrobial peptides. The Antimicrobial peptides are mainly from biological sources but some of them are synthetic in nature. Only those compounds, which are found to be active against either bacteria (both Gram-positive and negative) or fungus, are selected for this database.The ACD database is freely available at URL: http://amdr.amu.ac.in/acd, and it is compatible with desktops, smartphones, and tablets.


Assuntos
Anti-Infecciosos , Simulação por Computador , Bases de Dados de Produtos Farmacêuticos , Infecções por Bactérias Gram-Negativas/tratamento farmacológico , Infecções por Bactérias Gram-Positivas/tratamento farmacológico , Micoses/tratamento farmacológico , Animais , Anti-Infecciosos/química , Anti-Infecciosos/uso terapêutico , Avaliação Pré-Clínica de Medicamentos , Fungos , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Humanos
7.
Arch Microbiol ; 202(7): 1985-1996, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32476047

RESUMO

A soft coral-derived fungus Penicillium sp. among other isolates e high antibacterial, anti-yeast and cytotoxic activities. The fungus, Penicillium sp. MMA, isolated from Sarcphyton glaucoma, afforded nine diverse compounds (1-9). Their structures were identified by 1D and 2 D NMR and ESI-MS spectroscopic data as two alkaloids: veridicatol (1), aurantiomide C (2); one sesquiterpene, aspterric acid (3); two carboxylic acids, 3,4-dihydroxy-benzoic acid; (4) and linoleic acid (5); three steroids, ergosterol (6), ß-Sitosterol (7), ß-Sitosterol glucoside (8) along with the sphingolipid, cerebroside A (9). Biologically, the antimicrobial, antioxidant, in vitro cytotoxicity and antibiofilm activities were studied in comparison with the fungal extract. The in silico computational studies were implemented to predict drug and lead likeness properties for 1-4. The fungus was taxonomically characterized by morphological and molecular biology (18srRNA) approaches.


Assuntos
Anti-Infecciosos , Antineoplásicos , Bactérias/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Fungos/efeitos dos fármacos , Penicillium/química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Oceano Índico , Estrutura Molecular , Penicillium/classificação , Penicillium/genética , Penicillium/metabolismo , RNA Ribossômico 18S/genética
8.
Acta Crystallogr C Struct Chem ; 76(Pt 4): 359-366, 2020 04 01.
Artigo em Inglês | MEDLINE | ID: mdl-32229717

RESUMO

Derivatives of pyrimidine-2(1H)-selenone are a group of compounds with very strong antimicrobial activity. In order to study the effect of the position of the methoxy substituent on biological activity, molecular geometry and intermolecular interactions in the crystal, three derivatives were prepared and evaluated with respect to their antimicrobial activities, and their crystal structures were determined by X-ray diffraction. The investigated compounds, namely, 1-(X-methoxyphenyl)-4-methyl-6-phenylpyrimidine-2(1H)-selenones (X = 2, 3 and 4 for 1, 2 and 3, respectively), C18H16N2OSe, showed very strong activity against selected strains of Gram-positive bacteria and fungi. Two compounds, 1 and 2, crystallize in the monoclinic space group P21/c, while 3 crystallizes in the space group P21/n; 1 has two molecules in the asymmetric unit and the other two (2 and 3) have one molecule. The geometries of the investigated compounds differ slightly in the mutual orientations of the aromatic and pyrimidineselenone rings. The O atom in 1 stabilizes the conformation of the molecules via intramolecular C-H...O hydrogen bonding. The packing of molecules is determined by weak C-H...N and C-H...Se intermolecular interactions and additionally in 1 and 2 by C-H...O intermolecular interactions. The introduction of the methoxy substituent results in greater selectivity of the investigated compounds.


Assuntos
Anti-Infecciosos/química , Pirimidinas/química , Anti-Infecciosos/farmacologia , Cristalografia por Raios X , Fungos , Ligação de Hidrogênio , Estrutura Molecular
9.
Nucleic Acids Res ; 48(9): 4946-4959, 2020 05 21.
Artigo em Inglês | MEDLINE | ID: mdl-32232361

RESUMO

Human cytosolic leucyl-tRNA synthetase (hcLRS) is an essential and multifunctional enzyme. Its canonical function is to catalyze the covalent ligation of leucine to tRNALeu, and it may also hydrolyze mischarged tRNAs through an editing mechanism. Together with eight other aminoacyl-tRNA synthetases (AaRSs) and three auxiliary proteins, it forms a large multi-synthetase complex (MSC). Beyond its role in translation, hcLRS has an important moonlight function as a leucine sensor in the rapamycin complex 1 (mTORC1) pathway. Since this pathway is active in cancer development, hcLRS is a potential target for anti-tumor drug development. Moreover, LRS from pathogenic microbes are proven drug targets for developing antibiotics, which however should not inhibit hcLRS. Here we present the crystal structure of hcLRS at a 2.5 Å resolution, the first complete structure of a eukaryotic LRS, and analyze the binding of various compounds that target different sites of hcLRS. We also deduce the assembly mechanism of hcLRS into the MSC through reconstitution of the entire mega complex in vitro. Overall, our study provides the molecular basis for understanding both the multifaceted functions of hcLRS and for drug development targeting these functions.


Assuntos
Leucina-tRNA Ligase/química , Anti-Infecciosos/química , Biocatálise , Domínio Catalítico , Desenho de Fármacos , Humanos , Leucina-tRNA Ligase/efeitos dos fármacos , Leucina-tRNA Ligase/metabolismo , Modelos Moleculares , Proteínas Monoméricas de Ligação ao GTP/metabolismo , Domínios Proteicos , RNA de Transferência de Leucina/metabolismo , Aminoacilação de RNA de Transferência
10.
Poult Sci ; 99(4): 1875-1887, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32241467

RESUMO

The present study was undertaken to investigate the effect of aqueous Withania somnifera root (WSR) extract in broiler chicks experimentally infected with Escherichia coli O78 @ 107 CFU/0.5 ml intraperitoneally. Clinical signs and mortality due to colibacillosis observed in infected chicks were mild and lasted for short duration in WSR extract supplemented group as compared with the nonsupplemented group. A significant increase in serum alanine transaminase, aspartate transaminase, lactate dehydrogenase, and creatine phosphokinase activities and a decrease in total protein and albumin concentrations were observed in the infected groups, though these changes were of lower magnitude in WSR extract supplemented group. A significantly higher activity of oxidative blood parameters such as superoxide dismutase, catalase, glutathione reductase, and glutathione-S-transferase enzymes were noticed in WSR extract supplemented group. The WSR extract supplemented group revealed significantly higher E. coli-specific antibody titer and enhanced lymphocyte proliferation response as compared with the nonsupplemented group. The gross and histopathological lesions of colibacillosis were mild in the WSR extract-supplemented infected group as compared with the nonsupplemented infected group. Withania somnifera root extract supplementation produced 31.48 and 34.38% protection in the gross and histopathological lesions in E. coli infected chicks, respectively. It is concluded that supplementation of 20% WSR extract @ 20 ml/L of water caused a reduction in the severity, mortality, and recovery period of E. coli infection and enhanced the humoral and cellular immune responses suggesting its protective effect on limiting the pathology of E. coli infection in broiler chickens.


Assuntos
Anti-Infecciosos/metabolismo , Galinhas , Infecções por Escherichia coli/veterinária , Escherichia coli/fisiologia , Extratos Vegetais/metabolismo , Doenças das Aves Domésticas/tratamento farmacológico , Withania/química , Ração Animal/análise , Animais , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/química , Dieta/veterinária , Suplementos Nutricionais/análise , Relação Dose-Resposta a Droga , Infecções por Escherichia coli/tratamento farmacológico , Infecções por Escherichia coli/microbiologia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Raízes de Plantas/química , Doenças das Aves Domésticas/microbiologia , Distribuição Aleatória
11.
Chemistry ; 26(38): 8452-8457, 2020 Jul 08.
Artigo em Inglês | MEDLINE | ID: mdl-32294272

RESUMO

This Full Paper reports the formation of silver (Ag) NPs within spatially resolved two-component hydrogel beads, which combine a low-molecular-weight gelator (LMWG) DBS-CONHNH2 and a polymer gelator (PG) calcium alginate. The AgNPs are formed through in situ reduction of AgI , with the resulting nanoparticle-loaded gels being characterised in detail. The antibacterial activity of the nanocomposite gel beads was tested against two drug-resistant bacterial strains, often associated with hospital-acquired infections: vancomycin-resistant Enterococcus faecium (VRE) and Pseudomonas aeruginosa (PA14), and the AgNP-loaded gels showed good antimicrobial properties against both types of bacteria. It is suggested that the gel bead format of these AgNP-loaded hybrid hydrogels makes them promising versatile materials for potential applications in orthopaedics or wound healing.


Assuntos
Alginatos/química , Antibacterianos/química , Anti-Infecciosos/química , Hidrogéis/química , Nanopartículas Metálicas/química , Prata/química , Testes de Sensibilidade Microbiana , Polímeros/química , Pseudomonas aeruginosa , Cicatrização
12.
Food Chem ; 319: 126553, 2020 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-32197214

RESUMO

The development of natural additives is considered an important research topic. In this work, the use of Cymbopogon citratus (CC) extract as a natural additive for chicken sausage refrigerated was investigated. The CC extract was characterized by electrospray ionization with high-resolution time-of-flight mass spectrometry (ESI-ToF-MS) and the identified compounds were directly related to the antioxidant activity demonstrated by CC in the fresh sausage. In total, 31 phytochemical compounds were identified, and 27 of these still were not described in the literature for CC. The antimicrobial activity showed that CC extract is a potential antibacterial agent. Besides, the results showed that CC extract reduced lipid oxidation compared to synthetic additive. The sensorial characteristics were maintained, demonstrating good acceptability by the consumer. The results confirmed that CC can keep the quality of chicken sausage refrigerated for up to 42 days of storage.


Assuntos
Anti-Infecciosos/química , Antioxidantes/química , Cymbopogon/química , Produtos da Carne/análise , Compostos Fitoquímicos/química , Oxirredução , Extratos Vegetais/química , Espectrometria de Massas por Ionização por Electrospray
13.
BMC Complement Med Ther ; 20(1): 89, 2020 Mar 17.
Artigo em Inglês | MEDLINE | ID: mdl-32183792

RESUMO

BACKGROUND: Hydrolates, complex mixtures containing traces of essential oils (EOs), are inexpensive, easy to make and less toxic than their corresponding EOs. The antibacterial and antifungal activity of the hydrolate of Coridothymus capitatus (L.) Reichenb. fil. (Lamiaceae) alone and in combination with antimicrobial drugs, such as tetracycline and itraconazole, were evaluated. METHODS: The chemical composition was analysed by gas-chromatography-mass spectrometry (GC-MS). Standard methods were performed to evaluate the susceptibility of some Gram-positive and Gram-negative bacteria, and Candida spp. to the hydrolate, in comparison with its EO. The hydrolate mechanism of action was assayed by propidium iodide and MitoTracker staining. Checkerboard tests were carried out for combinations studies. RESULTS: GC-MS identified 0.14% (v/v) of total EO content into hydrolate and carvacrol as a dominant component. The hydrolate showed a good antimicrobial activity against bacteria and yeasts. It exhibited a synergistic effect with itraconazole against Candida krusei, and an additive effect with tetracycline against methicillin-resistant Staphylococcus aureus strains. Hydrolate changed the membranes permeability of bacteria and yeasts and altered mitochondrial function of yeasts. CONCLUSIONS: Our study extends the knowledge by exploiting non-conventional antimicrobial agents to fight the emergence of antibiotic resistance.


Assuntos
Anti-Infecciosos/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Lamiaceae/química , Óleos Voláteis/farmacologia , Leveduras/efeitos dos fármacos , Antibacterianos/uso terapêutico , Anti-Infecciosos/química , Antifúngicos/uso terapêutico , Cromatografia Gasosa , Quimioterapia Combinada , Itraconazol/uso terapêutico , Espectrometria de Massas , Óleos Voláteis/química , Tetraciclina/uso terapêutico
14.
Phytother Res ; 34(9): 2140-2158, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32159263

RESUMO

The family Arecaceae includes 181 genera and 2,600 species with a high diversity in physical characteristics. Areca plants, commonly palms, which are able to grow in nearly every type of habitat, prefer tropical and subtropical climates. The most studied species Areca catechu L. contains phytochemicals as phenolics and alkaloids with biological properties. The phenolics are mainly distributed in roots followed by fresh unripe fruits, leaves, spikes, and veins, while the contents of alkaloids are in the order of roots, fresh unripe fruits, spikes, leaves, and veins. This species has been reputed to provide health effects on the cardiovascular, respiratory, nervous, metabolic, gastrointestinal, and reproductive systems. However, in many developing countries, quid from this species has been associated with side effects, which include the destruction of the teeth, impairment of oral hygiene, bronchial asthma, or oral cancer. Despite these side effects, which are also mentioned in this work, the present review collects the main results of biological properties of the phytochemicals in A. catechu. This study emphasizes the in vitro and in vivo antioxidant, antimicrobial, anticancer, and clinical effectiveness in humans. In this sense, A. catechu have demonstrated effectiveness in several reports through in vitro and in vivo experiments on disorders such as antimicrobial, antioxidant, or anticancer. Moreover, our findings demonstrate that this species presents clinical effectiveness on neurological disorders. Hence, A. catechu extracts could be used as a bioactive ingredient for functional food, nutraceuticals, or cosmeceuticals. However, further studies, especially extensive and comprehensive clinical trials, are recommended for the use of Areca in the treatment of diseases.


Assuntos
Agricultura , Areca/fisiologia , Pesquisa Biomédica , Alimentos , Fitoterapia , Agricultura/tendências , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Areca/química , Pesquisa Biomédica/métodos , Pesquisa Biomédica/tendências , Fazendas , Humanos , Fenóis/química , Fenóis/farmacologia , Compostos Fitoquímicos/efeitos adversos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Fitoterapia/métodos , Fitoterapia/tendências , Folhas de Planta/química
15.
Biochim Biophys Acta Biomembr ; 1862(7): 183236, 2020 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-32126226

RESUMO

Piscidins are host-defense peptides (HDPs) from fish that exhibit antimicrobial, antiviral, anti-cancer, anti-inflammatory, and wound-healing properties. They are distinctively rich in histidine and contain an amino terminal copper and nickel (ATCUN) binding motif due to the presence of a conserved histidine at position 3. Metallation lowers their total charge and provides a redox center for the formation of radicals that can convert unsaturated fatty acids (UFAs) into membrane-destabilizing oxidized phospholipids (OxPLs). Here, we focus on P1, a particularly membrane-active isoform, and investigate how metallating it and making OxPL available influence its membrane activity. First, we quantify through dye leakage experiments the permeabilization of the apo- and holo-forms of P1 on model membranes containing a fixed ratio of anionic phosphatidylglycerol (PG) and zwitterionic phosphatidylcholine (PC) but varying amounts of Aldo-PC, an OxPL derived from the degradation of several UFAs. Remarkably, metallating P1 increases membranolysis by a factor of five in each lipid system. Conversely, making Aldo-PC available improves permeabilization by a factor of two for each peptide form. Second, we demonstrate through CD-monitored titrations that the strength of the peptide-membrane interactions is similar in PC/PG and PC/PG/Aldo-PC. Thus, peptide-induced membrane activity is boosted by properties intrinsic to the peptide (e.g., charge and structural changes associated with metallation) and bilayer (e.g., reversal of sn-2 chain due to oxidation). Third, we show using oriented-sample 15N solid-state NMR that the helical portion of P1 lies parallel to the bilayer surface in both lipid systems. 31P NMR experiments show that both the apo- and holo-states interact more readily with PC in PC/PG. However, the presence of Aldo-PC renders the holo-, but not the apo-state, more specific to PG. Hence, the membrane disruptive effects of P1 and its specificity for the anionic lipids found on pathogenic cell membrane surfaces are simultaneously optimized when it is metallated and the OxPL is present. Overall, this study deepens our insights into how OxPLs affect peptide-lipid interactions and how host defense metallopeptides could help integrate the effects of antimicrobial agents.


Assuntos
Peptídeos Catiônicos Antimicrobianos/química , Ácidos Graxos Insaturados/química , Proteínas de Peixes/genética , Metais/química , Animais , Anti-Infecciosos/química , Peptídeos Catiônicos Antimicrobianos/genética , Sítios de Ligação , Membrana Celular , Cobre/química , Ácidos Graxos Insaturados/genética , Proteínas de Peixes/química , Histidina/química , Histidina/genética , Humanos , Bicamadas Lipídicas/química , Lipídeos de Membrana/química , Lipídeos de Membrana/genética , Níquel/química , Fosfolipídeos/química , Fosfolipídeos/genética
16.
J Photochem Photobiol B ; 204: 111806, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-32044619

RESUMO

The cotton fabrics are a cosmopolitan in usage due to their extraordinary features. The clothes are a very good medium for the growth of pathogenic microorganisms. The nanoparticles have diverse benefits in the biomedical field like drug carrier and as antimicrobials. The current investigation was aimed to synthesize the metallic silver nanoparticles (AgNPs) from the aqueous extract of Curcuma longa leaf and evaluating their antimicrobial and wound healing potential of AgNPs coated cotton fabric. The synthesized AgNPs were characterized by HR-TEM and FT-IR examinations. The formulated AgNPs were coated with cotton fabrics to test their efficiency against the pathogenic microorganisms. The existence of AgNPs in the cotton fabrics was confirmed via the SEM along with EDX analysis. The antimicrobial potential of fabricated AgNPs and its coated cotton fabrics was inspected against the human pathogenic strains. The wound healing efficacy was examined in the L929 cells. The HR-TEM analysis proved the existence of spherical shaped AgNPs. In the antimicrobial activity, the CL-AgNPs loaded cotton fabric was exhibited an appreciable decrease in the growth of pathogenic microorganisms. The crude extract, as well as formulated AgNPs, also exhibited the noticeable antimicrobial potency against the S.aureus, P.aeruginosa, S.pyogenes, and C.albicans. The AgNPs loaded cotton fabrics was displayed the potent wound healing activity in the fibroblast (L929) cells. Consequently, it was concluded that the formulated AgNPs from C.longa coated cotton fabrics may be utilized for the variety of applications in hospital patients and even medical workers to prevent the microbial infection.


Assuntos
Anti-Infecciosos/química , Fibra de Algodão/análise , Curcuma/química , Nanopartículas Metálicas/química , Prata/química , Animais , Anti-Infecciosos/farmacologia , Candida albicans/efeitos dos fármacos , Linhagem Celular , Movimento Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Curcuma/metabolismo , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Química Verde , Nanopartículas Metálicas/toxicidade , Camundongos , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Folhas de Planta/química , Folhas de Planta/metabolismo
17.
Lett Appl Microbiol ; 70(5): 380-387, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32048328

RESUMO

Chitosan with higher molecular weight exhibited higher antimicrobial efficacy against foodborne pathogens. However, the poor water solubility of higher or medium molecular weight chitosan limits its applications. To overcome the challenge, our research team searched for simple preparation procedure for fast-dissolving medium molecular weight chitosan in water. Throughout the process, we were able to obtain a higher concentration of medium molecular weight water-soluble (MMWWS) chitosan (400 kDa). The MMWWS chitosan showed physicochemical properties that are suitable for edible coating. Antibacterial activities of 400-kDa chitosan coating prepared in acetic acid (1% v/v) or aspartic acid (1% or 3% w/v) were examined. The surface of catfish cubes was inoculated with six foodborne pathogens and then coated with chitosan solutions. The survival of each pathogen was evaluated during shelf life storage. Compared with the control, 3% w/v chitosan coating in aspartic acid solution exhibited the most effective antibacterial activities among other coating treatments, completely inhibiting Vibrio parahaemolyticus on the surface of catfish. The study suggested that chitosan dissolved in aspartic acid has the potential for use as an alternative antimicrobial coating for catfish fillet.


Assuntos
Anti-Infecciosos/farmacologia , Quitosana/farmacologia , Conservação de Alimentos/métodos , Ictaluridae/microbiologia , Animais , Anti-Infecciosos/química , Ácido Aspártico/química , Quitosana/química , Filmes Comestíveis , Microbiologia de Alimentos , Peso Molecular , Alimentos Marinhos/microbiologia
18.
World J Microbiol Biotechnol ; 36(2): 30, 2020 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-32025825

RESUMO

The objective of this study was to determine whether seeds of Brassica oleracea var. italica (i.e. broccoli, an edible plant) produce defensins that inhibit phytopathogenic fungi and pathogenic bacteria of clinical significance. Crude extracts obtained from broccoli seeds were fractioned by molecular exclusion techniques and analyzed by liquid chromatography-high-resolution mass spectrometry. Two peptides were identified, BraDef1 (10.68 kDa) and BraDef2 (9.9 kDa), which were categorized as Class I defensins based on (a) their primary structure, (b) the presence of four putative cysteine disulfide bridges, and (c) molecular modeling predictions. BraDef1 and BraDef2 show identities of, respectively, 98 and 71%, and 67 and 85%, with defensins from Brassica napus and Arabidopsis thaliana. BraDef (BraDef1 + BraDef2) disrupted membranes of Colletotrichum gloeosporioides and Alternaria alternata and also reduced hyphal growth of C. gloeosporioides by ~ 56% after 120 h of incubation. Pathogenic bacteria (Bacillus cereus 183, Listeria monocytogenes, Salmonella typhimurium, Pseudomonas aeruginosa, and Vibrio parahaemolitycus) were susceptible to BraDef, but probiotic bacteria such as Bifidobacterium animalis, Lactobacillus acidophilus, and Lactobacillus casei were not inhibited. To our knowledge, this is the first report of defensins present in seeds of B. oleracea var. italica (i.e. edible broccoli). Our findings suggest an applied value for BraDef1/BraDef2 in controlling phytopathogenic fungi and pathogenic bacteria of clinical significance.


Assuntos
Anti-Infecciosos/farmacologia , Brassica/química , Defensinas/farmacologia , Sequência de Aminoácidos , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Bactérias/efeitos dos fármacos , Cromatografia Líquida , Defensinas/química , Defensinas/isolamento & purificação , Fungos/efeitos dos fármacos , Espectrometria de Massas , Testes de Sensibilidade Microbiana , Modelos Moleculares , Extratos Vegetais/química , Sementes/química
19.
World J Microbiol Biotechnol ; 36(2): 31, 2020 Feb 11.
Artigo em Inglês | MEDLINE | ID: mdl-32048066

RESUMO

Biogenic production of nanoparticles is eco-friendly, less expensive method with various medical and biological applications. Nanotechnology along with photodynamic therapy is gaining tremendous importance with enhanced efficacy. The present work was aimed to evaluate methanolic extracts and nanoparticles of two selected plants (Datura suavolens and Verbina tenuisecta) for cytotoxic photodynamic, antioxidant and antimicrobial study. Both extract and silver (5 mM) nanoparticles of Datura plant showed significant activities against bacterial strains. Maximum ZOI of 27.3 ± 1.6 mm was observed with nanoparticles of Datura branches with minimum inhibitory (MIC) value of 32 µg/ml. In case of antifungal and antioxidant assay samples were moderately active. Silver nanoparticles and extracts were effective against rhabdomyosarcoma cell line with lowest IC50 value of 42.5 ± 0.6 µg/ml and percent viability of 25.6 ± 1.3 of Verbena tenuisecta. However, nanoparticles of Datura leaves and branches were more potent with IC50 value of 2.4 ± 0.9 µg/ml and 7.8 ± 1.1 µg/ml respectively. The result of photodynamic study showed that efficacy of photosensitizer was enhanced and percent viability reduced when nanoparticles used as an adjunct. The color change and UV spectra (415‒425 nm) indicated the production of nanoparticles. Fourier transform infrared spectroscopy (FTIR) spectra showed presence of different functional groups e.g., hydroxyl, carbonyl and amino. Nanoparticles are sphenoid in morphology and size ranges between 20-150 nm. Current study showed these silver nanoparticles can be used as cytotoxic agent in photodynamic therapy and can play a critical role to establish medicinal potential of selected plants.


Assuntos
Datura/química , Metanol/farmacologia , Prata/farmacologia , Verbena/química , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Nanopartículas Metálicas , Metanol/química , Metanol/isolamento & purificação , Testes de Sensibilidade Microbiana , Fármacos Fotossensibilizantes/química , Fármacos Fotossensibilizantes/isolamento & purificação , Fármacos Fotossensibilizantes/farmacologia , Extratos Vegetais/química , Folhas de Planta/química , Prata/química , Prata/isolamento & purificação
20.
Food Chem ; 317: 126389, 2020 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-32097822

RESUMO

Glyceollins are a class of antimicrobial prenylated pterocarpans produced in soybean seedlings upon fungus elicitation. Priming with reactive oxygen species (ROS) prior to elicitation with Rhizopus oligosporus/oryzae (R) was investigated for its potential to enhance glyceollin production. ROS-priming prior to R-elicitation (ROS + R) increased glyceollin production (8.6 ± 0.9 µmol/g dry weight (DW)) more than 4-fold compared to elicitation without priming (1.9 ± 0.4 µmol/g DW). Furthermore, ROS-priming was superior to two physical primers which were used as benchmark primers, namely slicing (5.0 ± 0.6 µmol glyceollins/g DW) and sonication (4.8 ± 1.0 µmol glyceollins/g DW). Subsequently, the robustness of ROS + R was assessed by applying it to another soybean cultivar, where it also resulted in a significantly higher glyceollin content than R-elicitation without priming. ROS-priming prior to elicitation provides opportunities for improving the yield in large-scale production of natural antimicrobials due to the ease of application and the robustness of the effect across cultivars.


Assuntos
Anti-Infecciosos/metabolismo , Doenças das Plantas/imunologia , Pterocarpanos/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Rhizopus/fisiologia , Soja/metabolismo , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Doenças das Plantas/microbiologia , Pterocarpanos/química , Pterocarpanos/farmacologia , Plântula/química , Plântula/metabolismo , Plântula/microbiologia , Soja/química , Soja/microbiologia
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