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1.
PLoS One ; 15(8): e0237844, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32834013

RESUMO

The feasibility of the production of germinated rice extracts using indigenous rice from Southern Thailand, including Khemtong (KHT) and Khai Mod Rin (KMR) from a single location at the Pak Phanang River Basin in Nakhon Si Thammarat, was investigated. The nutritional composition and bioactivity of the germinated rice extracts from both cultivars were evaluated. Optimum germination time for both rices was 96 h, leading to the highest GABA, thiamine, free amino acid, total sugar, and α-amylase activity (p<0.05). Germinated KHT had a higher α-amylase activity than germinated KMR at all germination times. Mashing at 60°C/pH 5.5 rendered the extract with the highest GABA content (p<0.05) and desirable contents of other nutrients. In comparison with germinated Sungyod (local colored rice) and Jasmine (commercial Thai rice) extracts, KHT and KMR showed a higher scavenging activity against DPPH•, OH•, and H2O2 (p<0.05) with a comparable ABTS•+ inhibition. For metal chelation, reducing power and ACE inhibitory activity, the germinated Sungyod extract was greater than KHT/KMR. The results demonstrated the potential use of germinated local Thai rice for the production of functional beverages.


Assuntos
Germinação , Fenômenos Fisiológicos da Nutrição , Oryza/química , Oryza/crescimento & desenvolvimento , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Aminoácidos/análise , Inibidores da Enzima Conversora de Angiotensina/farmacologia , Antioxidantes/farmacologia , Compostos de Bifenilo/química , Estudos de Viabilidade , Flavonoides/análise , Depuradores de Radicais Livres/química , Minerais/análise , Fenóis/análise , Ácido Fítico/análise , Picratos/química , Açúcares/análise , Tiamina/análise , Fatores de Tempo , alfa-Amilases/metabolismo , Ácido gama-Aminobutírico/análise
2.
J Nat Med ; 74(4): 741-749, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32601830

RESUMO

Cancer cachexia is a complex and multifactorial syndrome that influences about 50-80% of cancer patients and may lead to 20% of cancer deaths and muscle atrophy is the key characteristic of the syndrome. Recent researches have shown that myostatin is a negative regulator in the growth and differentiation of skeletal muscle. Herein, C2C12 cancer cachexia model was established with C26 conditioned culture medium (CCM), then treated with magnolol to evaluate the pharmacological activity of magnolol in myotube atrophy. Our results demonstrated that magnolol inhibited the activity of myostatin promotor and the myostatin signaling pathway. In C2C12 cancer cachexia model, magnolol decreased myostatin expression, inhibited the phosphorylation of SMAD2/3 activated by C26 conditioned culture medium (CCM), and elevated the phosphorylation of FOXO3a lowered by CCM. Myosin heavy chain (MyHC), myogenin (MyoG), and myogenic differentiation (MyoD), as three common myotube markers in C2C12 myotube, were decreased by CCM, which could be effectively reversed by magnolol via activation of AKT/mTOR-regulated protein synthesis and inhibition of ubiquitin-mediated proteolysis. This study reveals that magnolol inhibits myotube atrophy induced by CCM by increasing protein synthesis and decreasing ubiquitin-mediated proteolysis, so that magnolol is a promising leading compound in treating muscle atrophy induced by cancer cachexia.


Assuntos
Anti-Inflamatórios não Esteroides/química , Produtos Biológicos/química , Compostos de Bifenilo/química , Caquexia/tratamento farmacológico , Lignanas/química , Fibras Musculares Esqueléticas/efeitos dos fármacos , Atrofia Muscular/tratamento farmacológico , Miostatina/metabolismo , Neoplasias/complicações , Animais , Linhagem Celular Tumoral , Humanos , Camundongos , Transfecção
3.
Int J Nanomedicine ; 15: 4021-4047, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32606662

RESUMO

Purpose: Periodontitis is a chronic inflammatory disease associated with microbial accumulation. The purpose of this study was to reuse the agricultural waste to produce cellulose nanofibers (CNF) and further modification of the CNF with κ-carrageenan oligosaccharides (CO) for drug delivery. In addition, this study is focused on the antimicrobial activity of surfactin-loaded CO-CNF towards periodontal pathogens. Materials and Methods: A chemo-mechanical method was used to extract the CNF and the modification was done by using CO. The studies were further proceeded by adding different quantities of surfactin [50 mg (50 SNPs), 100 mg (100 SNPs), 200 mg (200 SNPs)] into the carrier (CO-CNF). The obtained materials were characterized, and the antimicrobial activity of surfactin-loaded CO-CNF was evaluated. Results: The obtained average size of CNF and CO-CNF after ultrasonication was 263 nm and 330 nm, respectively. Microscopic studies suggested that the CNF has a short diameter with long length and CO became cross-linked to form as beads within the CNF network. The addition of CO improved the degradation temperature, crystallinity, and swelling property of CNF. The material has a controlled drug release, and the entrapment efficiency and loading capacity of the drug were 53.15 ± 2.36% and 36.72 ± 1.24%, respectively. It has antioxidant activity and inhibited the growth of periodontal pathogens such as Streptococcus mutans and Porphyromonas gingivalis by preventing the biofilm formation, reducing the metabolic activity, and promoting the oxidative stress. Conclusion: The study showed the successful extraction of CNF and modification with CO improved the physical parameters of the CNF. In addition, surfactin-loaded CO-CNF has potential antimicrobial activity against periodontal pathogens. The obtained biomaterial is economically valuable and has great potential for biomedical applications.


Assuntos
Carragenina/química , Celulose/química , Lipopeptídeos/química , Nanofibras/química , Peptídeos Cíclicos/química , Periodonto/microbiologia , Animais , Bactérias/metabolismo , Compostos de Bifenilo/química , Sobrevivência Celular , Difusão Dinâmica da Luz , Depuradores de Radicais Livres/química , Malondialdeído/metabolismo , Camundongos , Testes de Sensibilidade Microbiana , Nanofibras/ultraestrutura , Oligossacarídeos/química , Picratos/química , Células RAW 264.7 , Soja/química , Espectroscopia de Infravermelho com Transformada de Fourier
4.
J Chromatogr A ; 1623: 461150, 2020 Jul 19.
Artigo em Inglês | MEDLINE | ID: mdl-32505270

RESUMO

Antioxidants play an essential role in human health, as they have been found to be capable of lowering the incidence of many diseases, such as cancer and angiocardiopathy. Currently, more attention is paid to natural antioxidants because of the possible insecurity of synthetic antioxidants. Thus, the development of efficient techniques or methods to separate antioxidants from natural sources is requested urgently. High-speed counter current chromatography (HSCCC) is a unique support-free liquid-liquid chromatographic technique and has been widely applied in the field of separation of natural products. In this review, we summarize and analyze the related researches on the application of HSCCC in the separation of various natural antioxidants so far. The purpose of the article is to provide a certain theoretical support for the separation of natural antioxidants by HSCCC, and to make full use of advantages of HSCCC in the separation of bioactive components. In particular, some key problems associated with the separation strategies, the structural categories of natural antioxidants, solvent system choices, and the application of different elution modes in HSCCC separation, are summarized and commented. We expect that the content reviewed can offer more evidence for the development of the field of natural antioxidants separation, so as to achieve large-scale preparation of natural antioxidants.


Assuntos
Antioxidantes/isolamento & purificação , Distribuição Contracorrente/métodos , Compostos de Bifenilo/química , Cromatografia Líquida de Alta Pressão , Humanos , Concentração de Íons de Hidrogênio , Picratos/química , Solventes/química
5.
Chem Biol Interact ; 326: 109137, 2020 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-32442417

RESUMO

In the present study eighteen inhibitors of the hydrolytic enzymes of the endocannabinoid system were investigated for antioxidant activity using lipid peroxidation (LP) method. Among the assayed compounds ten belong to carbamates with phenyl [1,1'-biphenyl]-3-ylcarbamate (6), reported for the first time, and eight are retro-amide derivatives of palmitamine. Interestingly, results indicated that most of the tested compounds have good antioxidant properties. In particular, 1,3-di([1,1'-biphenyl]-3-yl)urea (3) shows IC50 = 26 ± 6 µM comparable to ones obtained for standard antioxidants trolox and quercetin (IC50 = 22 ± 6 µM and 23 ± 6 µM, respectively). Compound 3 was investigated further by means of DFT calculations, to clarify a possible mechanism of the antioxidant action. In order to estimate the capability of 3 to act as radical scavenger the structure was optimized at B3LYP/6-311++G** level and the respective bond dissociation enthalpies were calculated. The calculations in non-polar medium predicted as favorable mechanism a donation of a hydrogen atom to the free radical and formation of N-centered radical, while in polar solvents the mechanism of free radical scavenging by SPLET dominates over HAT H-abstraction. The possible radical scavenging mechanisms of another compound with potent antioxidant properties (IC50 = 53 ± 12 µM), the retro-amide derivative of palmitamine (compound 18), was estimated computationally based on the reaction enthalpies of a model compound (structural analogue to 18). The computations indicated that the most favorable mechanisms are hydrogen atom transfer from the hydroxyl group in meta-position of the benzamide fragment in nonpolar medium, and proton transfer from the hydroxyl group in ortho-position of the benzamide fragment in polar medium.


Assuntos
Compostos de Bifenilo/química , Peroxidação de Lipídeos/efeitos dos fármacos , Ureia/química , Anilidas/química , Antioxidantes/química , Benzamidas/química , Ácidos Graxos/química , Depuradores de Radicais Livres/química , Radicais Livres/química , Hidrogênio/química , Ácidos Palmíticos/química , Solventes/química
6.
Chemosphere ; 253: 126728, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32298913

RESUMO

Nile perch wastewater was biodegraded using two Bacillus species to recover bioactive substances to enhance its reutilization value. The two Bacillus species successfully produced low-molecular-weight substances with a 47.8% degree of hydrolysis. The antioxidant activities of the Nile perch wastewater increased as the biodegradation proceeded, and the culture supernatant exhibited the highest DPPH (80.1%), ABTS (93.1%) and Fe2+ chelating (88.5%) antioxidant activities at 60 h. The antioxidant potential of the biodegraded Nile perch wastewater was found to be higher than those of other fish hydrolysates. Moreover, the biodegraded Nile perch wastewater exhibited effective antimicrobial activity against Vibrio vulnificus, exhibiting a minimal inhibitory concentration of 585 µg mL-1. Two-dimensional thin layer chromatography analysis revealed the specific amino acids responsible for the antioxidant activity, and molecular-weight cut-off ultrafiltration revealed that the <2-kDa fraction exhibited the highest antioxidant activity with the lowest IC50 values (0.43 and 0.22 mg mL-1 for DPPH and ABTS antioxidant activities, respectively). This is the first report of the reutilization of Nile perch wastewater as a natural antioxidant and antimicrobial ingredient for nutraceuticals.


Assuntos
Antibacterianos/isolamento & purificação , Antioxidantes/isolamento & purificação , Bacillus/metabolismo , Peptídeos/isolamento & purificação , Percas , Águas Residuárias/química , Aminoácidos/isolamento & purificação , Aminoácidos/farmacologia , Animais , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Biodegradação Ambiental , Compostos de Bifenilo/química , Quelantes/isolamento & purificação , Quelantes/farmacologia , Pesqueiros , Hidrólise , Peso Molecular , Peptídeos/farmacologia , Percas/crescimento & desenvolvimento , Picratos/química , Ultrafiltração , Vibrio vulnificus/efeitos dos fármacos
7.
Carbohydr Polym ; 235: 115935, 2020 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-32122478

RESUMO

A facile method for the activation of γ-cyclodextrin metal-organic framework (CD-MOF) without channel blockage and framework collapse was first developed using supercritical carbon dioxide (scCO2), which enabled higher surface area and larger pore volume. The scCO2-assisted impregnation method was also applied to introduce the insoluble drug, honokiol (HNK), into the pores of CD-MOF with higher cargo loading compared to the conventional liquid phase incorporation in ethanol. Notably, the resulting HNK-loaded CD-MOF (HNK@CD-MOF) had improved apparent solubility and enhanced dissolution rate. The intestinal cellular uptake and transport experiments demonstrated that CD-MOF could enhance cellular uptake and increase drug transport across the intestinal epithelial cells compared to the cyclodextrin inclusion complex. Moreover, the in vivo pharmacokinetic studies further confirmed that CD-MOF could significantly improve the oral absorption and bioavailability of HNK. Overall, the scCO2 activation and scCO2-assisted impregnation approaches were demonstrated as promising strategies to maximize the potential capability of CD-MOF.


Assuntos
Compostos de Bifenilo/farmacocinética , Dióxido de Carbono/química , Sistemas de Liberação de Medicamentos , Lignanas/farmacocinética , Estruturas Metalorgânicas/química , gama-Ciclodextrinas/química , Animais , Disponibilidade Biológica , Compostos de Bifenilo/química , Células CACO-2 , Corantes Fluorescentes/química , Humanos , Concentração de Íons de Hidrogênio , Lignanas/química , Masculino , Estrutura Molecular , Imagem Óptica , Tamanho da Partícula , Ratos , Ratos Sprague-Dawley , Solubilidade , Propriedades de Superfície , Células Tumorais Cultivadas
8.
Carbohydr Polym ; 235: 115981, 2020 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-32122511

RESUMO

In an effort to enhance antitumor and anti-metastasis of breast cancer, honokiol (HNK) was encapsulated into hyaluronic acid (HA) modified cationic liposomes (Lip). The prepared HA-Lip-HNK had a spherical shape with a narrow size distribution. The enhanced antitumor efficacy of HA-Lip-HNK was investigated in 4T1 cells in vitro, wherein flow cytometry and confocal microscopy analysis revealed its HA/CD44-mediated greater cellular internalization. As anticipate, the significant cytotoxicity of the HA-Lip-HNK was also observed in 4T1 tumor spheroids. Furthermore, the superior prevention of tumor metastasis by HA-Lip-HNK was verified by in vitro anti-invasion, wound healing and anti-migration assessments, and in vivo bioluminescence imaging in pulmonary metastasis model. Finally, compared with unmodified liposomes, the HA-Lip-HNK exhibited higher tumor accumulation, and achieved a tumor growth inhibition rate of 59.5 %. As a result, the HA-Lip-HNK may serve as a promising tumor-targeted drug delivery strategy for the efficient therapy of metastatic breast cancer.


Assuntos
Antineoplásicos/farmacologia , Compostos de Bifenilo/farmacologia , Neoplasias da Mama/tratamento farmacológico , Ácido Hialurônico/farmacologia , Lignanas/farmacologia , Neoplasias Pulmonares/tratamento farmacológico , Neoplasias Pulmonares/secundário , Nanopartículas/química , Animais , Antineoplásicos/administração & dosagem , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Compostos de Bifenilo/administração & dosagem , Compostos de Bifenilo/química , Neoplasias da Mama/patologia , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Modelos Animais de Doenças , Portadores de Fármacos/administração & dosagem , Portadores de Fármacos/química , Portadores de Fármacos/farmacologia , Sistemas de Liberação de Medicamentos , Ensaios de Seleção de Medicamentos Antitumorais , Ácido Hialurônico/administração & dosagem , Ácido Hialurônico/química , Injeções Intravenosas , Lignanas/administração & dosagem , Lignanas/química , Neoplasias Pulmonares/patologia , Camundongos , Nanopartículas/administração & dosagem , Tamanho da Partícula , Propriedades de Superfície
9.
J Chromatogr A ; 1620: 460988, 2020 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-32115233

RESUMO

Traditional Chinese medicine (TCM), especially herbal medicine compound preparation, faces great challenges in its quality control due to a myriad of components involved. How to perform quality control of TCM more effectively has been a research topic. In this study, we used Tianmeng oral liquid (TOL) as a case study and developed a comprehensive strategy based on non-targeted, targeted and bioactive analyses for quality evaluation of TOL from different batches. Firstly, a non-targeted fingerprinting analysis was performed by HPLC-DAD and UHPLC-MS/MS. Twenty-five batches of TOL were clearly discriminated by similarity analysis and hierarchical cluster analysis and components were tentatively identified. Secondly, the targeted quantitative methods based on HPLC-DAD and HPLC-MS were applied to simultaneous quantitative determination of five and eight marker compounds, especially toxic component strychnine, respectively. The quantitative data were processed with principal component analysis for differentiating different batches of samples. Finally, we explored the feasibility of establishing a total antioxidant capacity (TAC) model. How to use the peak area instead of the corresponding concentration to determine the antioxidant activity-related compounds was theoretically explained for the first time, which was of great significance for the study of the fingerprint-efficacy relationship. The orthogonal signal correction-partial least squares model was employed to predict the TAC of TOL from their chromatographic fingerprints and identify three potential antioxidant markers. These results demonstrated that the comprehensive strategy from fingerprinting, chemical composition, multiple-component quantification, and antioxidant activity could be applied to quality evaluation of TOL and discrimination of the expired and unexpired samples.


Assuntos
Medicamentos de Ervas Chinesas/química , Medicina Tradicional Chinesa , Administração Oral , Compostos de Bifenilo/química , Calibragem , Cromatografia Líquida de Alta Pressão/métodos , Depuradores de Radicais Livres/química , Análise dos Mínimos Quadrados , Limite de Detecção , Modelos Teóricos , Picratos/química , Análise de Componente Principal , Padrões de Referência , Reprodutibilidade dos Testes , Soluções
10.
J Med Chem ; 63(8): 4090-4106, 2020 04 23.
Artigo em Inglês | MEDLINE | ID: mdl-32202425

RESUMO

Fatty-acid binding protein 4 (FABP4) is a promising therapeutic target for immunometabolic diseases, while its potential for systemic inflammatory response syndrome treatment has not been explored. Here, a series of 2-(phenylamino)benzoic acids as novel and potent FABP4 inhibitors are rationally designed based on an interesting fragment that adopts multiple binding poses within FABP4. A fusion of these binding poses leads to the design of compound 3 with an ∼460-fold improvement in binding affinity compared to the initial fragment. A subsequent structure-aided optimization upon 3 results in a promising lead (17) with the highest binding affinity among all the inhibitors, exerting a significant anti-inflammatory effect in cells and effectively attenuating a systemic inflammatory damage in mice. Our work therefore presents a good example of lead compound discovery derived from the multiple binding poses of a fragment and provides a candidate for development of drugs against inflammation-related diseases.


Assuntos
Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/metabolismo , Descoberta de Drogas/métodos , Proteínas de Ligação a Ácido Graxo/antagonistas & inibidores , Proteínas de Ligação a Ácido Graxo/metabolismo , Células 3T3 , Administração Oral , Animais , Anti-Inflamatórios/química , Compostos de Bifenilo/administração & dosagem , Compostos de Bifenilo/química , Compostos de Bifenilo/metabolismo , Células CACO-2 , Relação Dose-Resposta a Droga , Humanos , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Endogâmicos ICR , Ligação Proteica/efeitos dos fármacos , Ligação Proteica/fisiologia , Estrutura Secundária de Proteína , Estrutura Terciária de Proteína , Pirazóis/administração & dosagem , Pirazóis/química , Pirazóis/metabolismo , Resultado do Tratamento
11.
Curr Pharm Biotechnol ; 21(11): 1070-1078, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32101118

RESUMO

INTRODUCTION: The plant, Astilboides tabularis (Hemsl.) Engler, is used in Chinese and Korean medicine to regulate blood sugar levels; however, little is known about its precise effects. MATERIALS AND METHODS: In this study, we aimed to measure the composition as well as the antioxidant, and anti-proliferative capacities of A. tabularis. Various extracts were generated using different organic solvents, and in vitro antioxidant activities were evaluated using DPPH free radical-scavenging and reducing power assays. The extracts were also evaluated based on their ability to inhibit lipopolysaccharide (LPS)-induced Nitric Oxide (NO) production in RAW 264.7 cells. RESULTS: Research shows that the A. tabularis ethyl acetate (EtOAc) extract showed significant antioxidant activity. Additionally, this extract could inhibit the LPS-induced expression of inflammatory mediators and pro-inflammatory cytokines in RAW 264.7 cells, including inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and interleukin-1 beta (IL-1ß). Notably, the A. tabularis EtOAc extract also displayed potent cytotoxic effects against MCF-7 and HeLa cancer cell lines, as determined by MTT assays. Lastly, total phenol and flavonoid content was measured for all extracts, and four flavonoid compounds-catechin, kaempferol, quercitrin, and isoquercetin were isolated from the EtOAc extract. Their structures were confirmed using mass spectrometry and nuclear magnetic resonance, and these isolated compounds were found to display potent DPPH free radical-scavenging activity. CONCLUSION: Thus, our data suggest that phenolic compounds in A. tabularis extracts promote antioxidant activity, and furthermore, these extracts show numerous features that indicate potential for therapeutic development.


Assuntos
Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Proliferação de Células/efeitos dos fármacos , Óxido Nítrico/antagonistas & inibidores , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Saxifragaceae/química , Animais , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/química , Sobrevivência Celular/efeitos dos fármacos , Radicais Livres/química , Células HeLa , Humanos , Lipopolissacarídeos/farmacologia , Células MCF-7 , Camundongos , Óxido Nítrico/biossíntese , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Picratos/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Polifenóis/química , Polifenóis/isolamento & purificação , Células RAW 264.7
12.
Curr Pharm Biotechnol ; 21(10): 927-938, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32065101

RESUMO

BACKGROUND: The essential oil of methyl eugenol rich Cymbopogon khasianus Hack. was evaluated and its bioactivities were compared with pure methyl eugenol. So far, methyl eugenol rich essential oil of lemongrass was not studied for any biological activities; hence, the present study was conducted. OBJECTIVE: This study examined the chemical composition of essential oil of methyl eugenol rich Cymbopogon khasianus Hack., and evaluated its antioxidant, anti-inflammatory, antimicrobial, and herbicidal properties and genotoxicity, which were compared with pure compound, methyl eugenol. MATERIAL AND METHODS: Methyl eugenol rich variety of Cymbopogon khasianus Hack., with registration no. INGR18037 (c.v. Jor Lab L-9) was collected from experimental farm CSIR-NEIST, Jorhat, Assam (26.7378°N, 94.1570°E). The essential oil wasobtained by hydro-distillation using a Clevenger apparatus. The chemical composition of the essential oil was evaluated using GC/MS analysis and its antioxidant (DPPH assay, reducing power assay), anti-inflammatory (Egg albumin denaturation assay), and antimicrobial (Disc diffusion assay, MIC) properties, seed germination effect and genotoxicity (Allium cepa assay) were studied and compared with pure Methyl Eugenol compound (ME). RESULTS: Major components detected in the Essential Oil (EO) through Gas chromatography/mass spectroscopy analysis were methyl eugenol (73.17%) and ß-myrcene (8.58%). A total of 35components were detected with a total identified area percentage of 98.34%. DPPH assay revealed considerable antioxidant activity of methyl eugenol rich lemongrass essential oil (IC50= 2.263 µg/mL), which is lower than standard ascorbic acid (IC50 2.58 µg/mL), and higher than standard Methyl Eugenol (ME) (IC50 2.253 µg/mL). Methyl eugenol rich lemongrass EO showed IC50 38.00 µg/mL, ME 36.44 µg/mL, and sodium diclofenac 22.76 µg/mL, in in-vitro anti-inflammatory test. Moderate antimicrobial activity towards the 8 tested microbes was shown by methyl eugenol rich lemongrass essential oil whose effectiveness against the microbes was less as compared to pure ME standard. Seed germination assay further revealed the herbicidal properties of methyl eugenol rich essential oil. Moreover, Allium cepa assay revealed moderate genotoxicity of the essential oil. CONCLUSION: This paper compared the antioxidant, anti-inflammatory, antimicrobial, genotoxicity and herbicidal activities of methyl eugenol rich lemongrass with pure methyl eugenol. This methyl eugenol rich lemongrass variety can be used as an alternative of methyl eugenol pure compound. Hence, the essential oil of this variety has the potential of developing cost-effective, easily available antioxidative/ antimicrobial drugs but its use should be under the safety range of methyl eugenol and needs further clinical trials.


Assuntos
Cymbopogon/química , Eugenol/análogos & derivados , Óleos Voláteis/farmacologia , Folhas de Planta/química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Compostos de Bifenilo/química , Aberrações Cromossômicas/efeitos dos fármacos , Cymbopogon/genética , Eugenol/isolamento & purificação , Eugenol/farmacologia , Eugenol/toxicidade , Fungos/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Bactérias Gram-Positivas/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Óleos Voláteis/isolamento & purificação , Óleos Voláteis/toxicidade , Ovalbumina/imunologia , Picratos/química , Extratos Vegetais/química
13.
Chemosphere ; 246: 125849, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32092814

RESUMO

The sodium pyrophosphate (SP)-enhanced Fenton reaction has been proven to have promising potential in remediation of polychlorinated biphenyls in soils by keeping iron ions soluble at high pH and minimizing the useless decomposition of H2O2. However, little information can be obtained about the effect of environmental factors on its remediation performance. Thus, the effect of environmental factors on the degradation of 2,2',5-trichlorodiphenyl (PCB18), one of the main PCB congeners in Chinese sites, was investigated in this study. PCB18 degradation was sensitive to pH, which ranged from 39.8% to 99.5% as increased pH from 3.0 to 9.0. ·OH was responsible for PCB18 degradation at pH 5.0, while both ·OH and O2- resulted in PCB 18 degradation at pH 7.0 with the calculated reaction activation energy of 73.5 kJ mol-1. Bivalent cations and transition metal ions decreased PCB18 degradation markedly as their concentrations increased. The addition of humic acid had an inhibitory on PCB18 degradation, but no obvious inhibition of PCB18 removal was observed when the same concentration of fulvic acid was added. The addition of 1 and 10 µM model humic constituents (MHCs) promoted PCB18 degradation, but the addition of 100 µM MHCs decreased PCB18 removal. Biphenyl, two dichlorobiphenyl, and two hydroxy trichlorobiphenyl derivatives were identified as the major degradation products of PCB18 in the Fe2+/SP/H2O2 system at pH 7.0. Thus, an oxidative pathway contributed by OH and a reductive pathway induced by O2- were proposed as the main mechanisms for PCB18 degradation in the SP-enhanced Fenton reaction.


Assuntos
Compostos de Bifenilo/química , Poluentes Ambientais/química , Modelos Químicos , Quelantes , Substâncias Húmicas , Peróxido de Hidrogênio/química , Ferro/química , Oxirredução , Bifenilos Policlorados/química , Solo
14.
Chemosphere ; 247: 125844, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32069708

RESUMO

Biphenyl 2,3-dioxygenase (BphA), a Rieske-type and first enzyme in the aerobic degradation process, plays a key role in the metabolizing process of biphenyl/polychlorinated biphenyl aromatic pollutants in the environment. To understand the catalytic mechanism of biphenyl 2,3-dioxygenase, the conversions leading to the cis-diols are investigated by means of quantum mechanics/molecular mechanics (QM/MM) method. A hydroperoxo-iron (III) species is involved in the enzyme-catalyzed reaction. Herein, we explored the direct reaction mechanism of hydroperoxo-iron (III) species with biphenyl and 4-4'-dichlorobiphenyl. The reaction process involves an epoxide intermediate, it could develop into a carbocation intermediate, and ultimately evolve into a cis-diol product. The important roles of several residues during the dioxygenation process were highlighted. This study may provide theoretical support for further directed mutations and enzymatic engineering of BphA, as well as promote the development of degrading environmentally persistent biphenyl/polychlorinated biphenyl aromatic contaminants.


Assuntos
Compostos de Bifenilo/química , Dioxigenases/metabolismo , Poluentes Ambientais/química , Bifenilos Policlorados/química , Catálise , Dioxigenases/genética , Hidroxilaminas , Hidroxilação , Oxigenases/metabolismo , Bifenilos Policlorados/metabolismo
15.
Pak J Biol Sci ; 23(2): 190-205, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31944079

RESUMO

BACKGROUND AND OBJECTIVE: Quarantine treatment enables export of mango fruits to parts of the world that enforce quarantine against fruit fly. Chilling injuries (CI) are prevalent in the mango fruits stored at temperatures lower than 12°C during cold-quarantine. So, this research examined the potentially enable of cold-shock treatment and integrated of edible coating with packing in (EPE) foam net to enhance the resistance of Naomi mango fruits during cold export. MATERIALS AND METHODS: The effect of cold quarantine was studied on fruit quality of 'Naomi' mango for 2016 and 2017 seasons. In this respect, mango fruits were coated with sodium alginate at 3%, semperfreshTM at 1% and packed in (EPE) foam net to reduce CI during cold quarantine. The treated fruits were stored for 4 h at 0°C, then transferred to 20°C for 20 h (cold-shock treatment) prior to store at 2±1°C and 90-95% RH for 15 days (quarantine treatment). While, the control fruit were directly stored at 2±1°C and 90-95% RH for 15 days. Thereafter, all fruits were stored at 20±2°C for and 70-75% RH for 7 days as shelf life period to simulate a marketing period. RESULTS: All applied treatments significantly reduced fruits weight loss (%), respiration rate, retard the loss of soluble solid (%) titratable acidity (%), have a good potential in maintaining firmness (lb inch-2), skin color h°, vitamin C, total phenol, flavonoids content, membrane stability index (MSI %), high rate of antioxidant capacity and retard the loss of shelf-life of fruits than the control. CONCLUSION: It was concluded that edible coatings used semperfreshTM at 1% with (EPE) foam net packing have a good potential in controlling postharvest chilling injury and maintaining the fruit quality being the most effective treatment on all parameters tested. It could potentially enable the export mango fruits to all quarantine-enforcing countries.


Assuntos
Conservação de Alimentos/métodos , Armazenamento de Alimentos/métodos , Mangifera , Antioxidantes/química , Ácido Ascórbico/química , Compostos de Bifenilo/química , Temperatura Baixa , Resposta ao Choque Frio , Flavonoides/química , Depuradores de Radicais Livres/química , Frutas/química , Gases , Metanol/química , Fenóis/química , Picratos/química , Extratos Vegetais/química , Superóxido Dismutase/metabolismo , Temperatura
16.
Acta Pharm ; 70(2): 215-226, 2020 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-31955145

RESUMO

Heliangolide is a naturally occurring sesquiterpene lactone and its derivatives are biologically active compounds present in most medicinal plants. This study evaluated the antioxidant and antidiabetic properties of a heliangolide sesquiterpene lactone isolated from Helianthus annuus L. leaves. The heliangolide sesquiterpene lactone was isolated through a combination of solvent-solvent partitioning, column chromatography, thin layer chromatography and high-performance liquid chromatography techniques. The antioxidant activity of the compound was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide radical scavenging assays while the antidiabetic effects were investigated in alloxan-induced diabetic rats. The heliangolide derivative at the concentration of 954.2 µmol L-1 showed 23.7 % DPPH and 26 % nitric oxide radical inhibitions compared with 96.6 and 50.9 %, resp., displayed by the controls (2,271.2 µmol L-1). It also reduced the fasting blood glucose (FBG) levels in a time-dependent manner. The highest activity was recorded within 6 h post-treatment at 0.2 mmol kg-1 bm. The heliangolide derivative exhibited significant (p < 0.05) antioxidant and antidiabetic properties and provides a basis for further development of constituents of Helianthus annuus leaves for the management of such diseases.


Assuntos
Antioxidantes/farmacologia , Diabetes Mellitus Experimental/tratamento farmacológico , Helianthus/química , Hipoglicemiantes/farmacologia , Lactonas/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Sesquiterpenos/farmacologia , Animais , Compostos de Bifenilo/química , Modelos Animais de Doenças , Flavonoides/farmacologia , Masculino , Picratos/química , Plantas Medicinais/química , Ratos , Ratos Wistar
17.
J Trace Elem Med Biol ; 58: 126448, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31901726

RESUMO

BACKGROUND: Increasing resistance to available drugs and their associated side-effects have drawn wide attention towards designing alternative therapeutic strategies for control of hyperglycemia and oxidative stress. The roles of the sizes and shapes of the nanomaterials used in the treatment and management of Type 2 Diabetes Mellitus (T2DM) in preventing chronic hyperglycaemia and oxidative stress are investigated. We report specifically on the effects of doping silver (Ag) into the ZnO nanorods (ZnO:Ag NR's) as a rational drug designing strategy. METHODS: Inhibition of porcine pancreatic α-amylase, murine pancreatic amylase, α-glucosidase, murine intestinal glucosidase and amyloglucosidase are checked for evaluation of antidiabetic potential. In addition, the radical scavenging activities of ZnO:Ag NR's against nitric oxide, DDPH and superoxide radicals are evaluated. RESULTS: Quantitative radical scavenging and metabolic enzyme inhibition activities of ZnO:Ag NR's at a concentration of 100 µg/mL were found to depend on the amount of Ag doped in up to a threshold level (3-4 %). Circular dichroism analysis revealed that the interaction of the NR's with the enzymes altered their secondary conformation. This alteration is the underlying mechanism for the potent enzyme inhibition. CONCLUSIONS: Enhanced inhibition of enzymes and scavenging of free radicals primarily responsible for reactive oxygen species (ROS) mediated damage, provide a strong scientific rationale for considering ZnO:Ag NR's as a candidate nanomedicine for controlling postprandial hyperglycaemia and the associated oxidative stress.


Assuntos
Antioxidantes/farmacologia , Hipoglicemiantes/farmacologia , Nanotubos/química , Prata/farmacologia , Óxido de Zinco/farmacologia , Amilases/antagonistas & inibidores , Amilases/metabolismo , Animais , Compostos de Bifenilo/química , Inibidores Enzimáticos/farmacologia , Depuradores de Radicais Livres/metabolismo , Inibidores de Glicosídeo Hidrolases/farmacologia , Intestinos/enzimologia , Camundongos , Nanotubos/ultraestrutura , Óxido Nítrico/metabolismo , Pâncreas/enzimologia , Picratos/química , Superóxidos/metabolismo , Suínos , alfa-Glucosidases/metabolismo
18.
J Biomol NMR ; 74(1): 1-7, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31912345

RESUMO

When planning a fluorine labeling strategy for 19F solid state NMR (ssNMR) studies of the structure and/or mobility of fluorine labeled compounds in situ in an oriented biological system, it is important to characterize the NMR properties of the label. This manuscript focuses on the characterization of a selection of aromatic fluorine compounds in dimyristoylphosphatidylcholine bilayers using 19F ssNMR from the standpoint of determining the optimum arrangement of fluorine nuclei on a pendant aromatic ring before incorporation into more complex biological systems.


Assuntos
Flúor/química , Marcação por Isótopo , Ressonância Magnética Nuclear Biomolecular , Compostos de Bifenilo/química , Dimiristoilfosfatidilcolina/química , Bicamadas Lipídicas/química
19.
J Enzyme Inhib Med Chem ; 35(1): 424-431, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31899985

RESUMO

A series of 16 novel benzenesulfonamides incorporating 1,3,5-triazine moieties substituted with aromatic amines, dimethylamine, morpholine and piperidine were investigated. These compounds were assayed for antioxidant properties by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay, 2,2`-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical decolarisation assay and metal chelating methods. They were also investigated as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and tyrosinase, which are associated with several diseases such as Alzheimer, Parkinson and pigmentation disorders. These benzenesulfonamides showed moderate DPPH radical scavenging and metal chelating activity, and low ABTS cation radical scavenging activity. Compounds 2 b, 3d and 3 h showed inhibitory potency against AChE with % inhibition values of >90. BChE was also effectively inhibited by most of the synthesised compounds with >90% inhibition potency. Tyrosinase was less inhibited by these compounds.


Assuntos
Acetilcolinesterase/efeitos dos fármacos , Antioxidantes/farmacologia , Butirilcolinesterase/efeitos dos fármacos , Inibidores da Colinesterase/farmacologia , Inibidores Enzimáticos/farmacologia , Monofenol Mono-Oxigenase/antagonistas & inibidores , Sulfonamidas/química , Sulfonamidas/farmacologia , Triazinas/química , Benzotiazóis/química , Compostos de Bifenilo/química , Picratos/química , Ácidos Sulfônicos/química
20.
Curr Pharm Biotechnol ; 21(3): 244-255, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31924154

RESUMO

OBJECTIVES: This project aims to develop a bio-natural nano-product with Cosmeceutical and pharmaceutical applications. METHODS: E. sativa oil was evaluated for its anti-oxidant, sun protection factor and elastase inhibition. Then, nanoemulgel formulations were prepared for E. sativa oil through the combination of nanoemulsion with hydrogel. E. sativa nanoemulsion formulations were prepared by the help of a selfemulsification technique. After this, the optimum formulation was mixed with Carbopol to produce the nanoemulgel. Anti-bacterial and anti-fungal activities were evaluated. RESULTS: Nanoemulsion occurred when the size of the droplets was 195.29 nm with the lowest polydispersibility index 0.207. The results of antioxidant, anti-elastase and SPF activities for E. sativa oil were 2.10 µg/ml, 25.1 µg/ml and an SPF value of 5.57, respectively. In addition, in the anti-bacterial test for Staphylococcus aureus, it was found that nanoemulgel has an inhibition zone of 2.1 cm in diameter. According to the MRSA, the inhibition zone was 1.5 cm. CONCLUSION: E. Sativa oil could be a promising candidate in cosmeceutical and pharmaceutical preparations.


Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Brassicaceae/química , Nanoestruturas/química , Elastase Pancreática/antagonistas & inibidores , Óleos Vegetais/isolamento & purificação , Fator de Proteção Solar , Animais , Anti-Infecciosos/isolamento & purificação , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/química , Candida/efeitos dos fármacos , Composição de Medicamentos , Emulsões , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Hidrogéis/química , Picratos/química , Sementes/química , Pele/efeitos dos fármacos , Pele/enzimologia , Suínos
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