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This study describes an effective and eco-friendly approach to the synthesis of zinc oxide nanoparticles (ZnONPs) utilizing papaya fruit peel extract (PPE). The structural evaluation and morphological features of synthesized ZnONPs were examined using various physicochemical analyses. The formulated ZnONPs were spherical to hexagonal in shape with â 170 nm in diameter. ZnONPs exhibited improved antioxidant potential in terms of DPPH radical scavenging activity (IC50 = 98.74 µg/ml) and ferric-reducing potential compared with PPE. The antibacterial activity of ZnONPs was measured against pathogenic strains of Salmonella typhi, Bacillus subtilis, Staphylococcus aureus, and Escherichia coli. The biosynthesized ZnONPs showed potential antibacterial efficacy against all microbes. In addition, ZnONPs exhibited potential photocatalytic activity in rhodamine B degradation in the presence of sunlight. The results indicated that papaya peels, which are these fruit wastes, could be helpful for the green synthesis of ZnONPs with good dose-responsive antioxidant, antibacterial, and photocatalytic activities.
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Carica , Nanopartículas Metálicas , Óxido de Zinco , Antioxidantes/farmacologia , Óxido de Zinco/farmacologia , Óxido de Zinco/química , Nanopartículas Metálicas/química , Antibacterianos/farmacologia , Antibacterianos/química , Escherichia coli , Extratos Vegetais/químicaRESUMO
A considerable amount of fruit waste is being produced every day worldwide. The green synthesis of metal nanoparticles from fruit peel waste can be an innovative, cost-effective, and eco-friendly alternative to traditional methods. Copper nanoparticles (CuNPs) were synthesized by a green method using the pineapple peels extract (PLX) and copper sulfate pentahydrate. The formation of CuNPs was visually identified and detected by UV-Visible spectroscopy. The CuNPs were characterized by Fourier-transform infrared (FTIR) spectroscopy, particle size analyzer, scanning electron microscopy (SEM), and X-ray diffraction (XRD). The antioxidant and reducing power of CuNPs were conducted by %DPPH scavenging and electron transfer-based ferric reducing antioxidant power (FRAP) assay, respectively. The antibacterial properties of CuNPs were determined in gram-positive, and gram-negative bacteria. The results showed that the CuNPs were spherical in shape with mean particle size 290.5 nm. The zeta potential of the nanoparticles was found to be - 12.3 mV indicating the instability in the colloidal state. The FTIR study confirmed the peaks of phytochemicals present in the PLX and the nanoparticles supporting the use of pineapple peels as stabilizing, reducing and capping agents. Both the DPPH and reducing power assay depicted that the synthesized CuNPs had significant antioxidant activity. However, the synthesized CuNPs had strong inhibitory capacity against both gram-positive and gram-negative test organisms. Thus, the CuNPS could be used for its viable antibacterial potential to preserve fruits, flowers, and vegetables from bacterial contamination.
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Ananas , Antibacterianos , Cobre , Química Verde , Nanopartículas Metálicas , Ananas/química , Antibacterianos/farmacologia , Antibacterianos/química , Nanopartículas Metálicas/química , Cobre/química , Antioxidantes/química , Antioxidantes/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier , Extratos Vegetais/química , Testes de Sensibilidade Microbiana , Tamanho da Partícula , Difração de Raios XRESUMO
The current research focused on the green synthesis of silver nanoparticles (AgNPs) using Duabanga grandiflora leaf extract. The green synthesis of AgNPs was confirmed by the surface plasmon resonance band at 453 nm in a UV-Visible analysis. The formulated AgNPs had a diameter of around 99.72 nm with a spherical shape. Fourier transform infrared (FTIR) spectrum revealed the bio-reducing potential of phytochemicals present in D. grandiflora, which fundamentally influenced the synthesis of AgNPs. Zeta potential, dynamic light scattering (DLS), scanning electron microscopic (SEM), energy-dispersive X-ray spectroscopic (EDX), X-ray diffraction (XRD), and transmission electron microscopic (TEM) analyses were executed to reveal the physicochemical attributes of the AgNPs. The AgNPs were further investigated for their antioxidant, antidiabetic, anticancer, and antibacterial potential. The DPPH free radical assay revealed the potential radical scavenging capacity (IC50 = 76.73 µg/ml) of green synthesized AgNPs. α-Amylase inhibitory assay displayed significant inhibitory potential (IC50 = 162.11 µg/ml) of this starch-breaking enzyme by AgNPs, revealing the antidiabetic potential of AgNPs. AgNPs exhibited potential cytotoxic activity (IC50 = 244.57 µg/ml) against malignant human kidney cells. In addition, AgNPs showed outstanding antibacterial activity against both Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureus) bacterial strains. Interestingly, AgNPs showed cytotoxic and antimicrobial activities at much higher concentrations than radical scavenging and α-amylase inhibitory concentrations. Thus, our finding elaborated the scope of green synthesized AgNPs for diverse therapeutic applications (dose-dependent) for further clinical translation.
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Antibacterianos , Nanopartículas Metálicas , Extratos Vegetais , Folhas de Planta , Prata , Nanopartículas Metálicas/química , Prata/química , Prata/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Humanos , Antibacterianos/farmacologia , Antibacterianos/química , Antioxidantes/farmacologia , Antioxidantes/química , Química Verde , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios XRESUMO
A mild and eco-friendly visible-light-induced synthesis of 2-(2-hydrazinyl) thiazole from readily accessible thiosemicarbazide, carbonyl, and phenacyl bromide in the absence of a metal catalyst and/or any extrinsic photosensitizer is reported. This approach only requires a source of visible light and a green solvent at room temperature to produce the medicinally privileged scaffolds of hydrazinyl-thiazole derivatives in good to outstanding yields. Experimental studies support the in situ formation of a visible-light-absorbing, photosensitized colored ternary EDA complex. The next step is to prepare a pair of radicals in an excited state, which makes it easier to prepare thiazole derivatives through a SET and PCET process. DFT calculations additionally supported the mechanistic analysis of the course of the reaction. The antioxidant and antidiabetic properties of some of the compounds in the synthesized library were tested in vitro. All the investigated compounds demonstrated appreciable antioxidant activity, as evidenced by the reducing power experiment and the IC50 values of the DPPH radical scavenging experiment. Furthermore, the IC50 values for 4c, 4d, and 4g also demonstrated a strong α-amylase inhibitory effect.
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Antioxidantes , Tiazóis , Antioxidantes/química , Tiazóis/química , Hipoglicemiantes , Elétrons , OxidantesRESUMO
Silver nanoparticles (Ag NPs) via green synthesis using medicinal plants have been widely used in natural product research due to the economical and eco-friendly properties of NPs. The plant-derived Ag NPs biosynthesis comprises the interaction between silver nitrate (precursor) and bioactive components of plant extract (reducing agents). In this work, Ag NPs were biosynthesized using Osbeckia stellata leaves aqueous extract. Characterization of Ag NPs was done by using ultraviolet-visible absorption (UV-Vis) spectroscopy, dynamic light scattering (DLS), Fourier transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM), and energy-dispersive X-ray analysis (EDX). Further, antioxidant, antidiabetic, cytotoxicity, and antimicrobial activities were evaluated to establish the pharmacological properties of Ag NPs. UV-Vis spectroscopy and FTIR showed an absorption peak of Ag NPs due to the surface plasmonic resonance. In contrast, the particle size in the nanometer range was analyzed by XRD and DLS. The size of the particle was confirmed by the SEM, TEM, and EDX in the nanometer range. This study showed the spherical shape and crystalline nature of NPs. Zeta potential was used to determine the stability of Ag NPs. Biosynthesized Ag NPs showed significantly potent antioxidant, antidiabetic, and cytotoxicity activity. Ag NPs also showed effectiveness against gram-positive (Escherichia coli) and gram-negative (Staphylococcus aureus) bacteria in the antimicrobial activity study. The result concluded that these Ag NPs might be used in biomedical and pharmacological fields.
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Antioxidantes , Nanopartículas Metálicas , Antioxidantes/farmacologia , Antioxidantes/química , Hipoglicemiantes/farmacologia , Nanopartículas Metálicas/química , Testes de Sensibilidade Microbiana , Prata/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Espectroscopia de Infravermelho com Transformada de Fourier , Extratos Vegetais/farmacologia , Extratos Vegetais/químicaRESUMO
Tea is the most popular daily drink consumed globally, with a high concentration of caffeine and polyphenols. In this study, the effects of ultrasonic-assisted extraction and quantification of caffeine and polyphenols from green tea were investigated and optimized using 23 -full factorial design and high-performance thin-layer chromatography. Three parameters were optimized to maximize the concentration of caffeine and polyphenols extracted using ultrasound: crude drug-to-solvent ratio (1:10-1:5), temperature (20-40°C), and ultrasonication time (10-30 min). The optimal conditions achieved from the model for tea extraction were as follows: crude drug-to-solvent ratio, 0.199 g/ml; temperature, 39.9°C; and time, 29.9 min; the extractive value was found to be 16.8%. Images from scanning electron microscopy showed that the matrix underwent a physical alteration and cell wall disintegration, which intensified and accelerated the extraction. This process might be simplified using sonication, which results in a higher extractive yield and a significant concentration of caffeine and polyphenols than the traditional approach, with a smaller quantity of solvent and faster analytical times. The result of high-performance thin-layer chromatography analysis proves a significant positive correlation between extractive value and caffeine and polyphenol concentrations.
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Cafeína , Polifenóis , Cafeína/análise , Polifenóis/análise , Cromatografia em Camada Fina , Chá/química , Extratos Vegetais/química , Solventes/química , Folhas de Planta/química , Cromatografia Líquida de Alta PressãoRESUMO
The green synthesis of metallic nanoparticles has tremendous impacts in various fields as found in recent years due to their low cost, easy and environmentally friendly synthesis. In this article, we report a simple and eco-friendly method for the synthesis of silver nanoparticles (AgNPs) using an aqueous Eupatorium adenophorum (E. adenophorum) leaf extract as a bioreductant. Interestingly, Fourier transform infrared (FTIR) spectroscopy analysis established that the E. adenophorum extract not only served as a bioreductant but also acted as a capping agent to stabilize the nanoparticles by functionalizing the surfaces. Various characterization techniques were adopted, such as X-ray powder diffraction (XRD), FTIR, ultraviolet-visible absorption (UV-Vis) spectroscopy, dynamic light scattering, scanning electron microscopy and energy-dispersive X-ray spectroscopy (EDX) to analyze the biosynthesized AgNPs. Biosynthesized nanoparticles were also explored for antioxidant, antibacterial and photocatalytic activities. The AgNPs showed improved free radical scavenging activity (IC50 48.96 ± 0.84 µg/mL) and bacterial inhibitory effects against both gram-positive (Staphylococcus aureus; 64.5 µg/mL) and gram-negative (Escherichia coli; 82.5 µg/mL) bacteria. Photocatalytic investigation showed AgNPs were effective at degrading rhodamine dye (78.69% in 90 min) when exposed to sunlight. These findings collectively suggest that E. adenophorum AgNPs were successfully prepared without the involvement of any hazardous chemical and it may be an effective antibacterial, antioxidant and promising agent for the removal of hazardous dye from waste water produced by industrial dyeing processes.
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INTRODUCTION: α-Amylase inhibitors from natural sources are of interest for new drug development for the treatment of diabetes mellitus (DM). High-performance thin-layer chromatography (HPTLC) coupled bioassay guided isolation of bioactive compounds has been improved within last few years. OBJECTIVE: A microchemical derivatised HPTLC-coupled attenuated total reflectance-Fourier-transform infrared (ATR-FTIR) and nuclear magnetic resonance (NMR) spectroscopy was employed for profiling α-amylase inhibitor from the aerial part of Asparagus racemosus Willd. METHODOLOGY: Asparagus racemosus Willd. aerial part extracted with different solvents (n-hexane, chloroform, ethyl acetate, and methanol) and assayed to detect free radical scavengers and α-amylase inhibitor by 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay and starch-iodine assay method, respectively. HPTLC-coupled ATR-FTIR and NMR spectroscopy was used to identify the α-amylase inhibitor. RESULTS: Methanolic extract of A. racemosus showed highest antioxidant activity (21.99 µg GAE/µL) where n-hexane extract showed lowest antioxidant activity (5.87 µg GAE/µL). The α-amylase inhibition was recorded as highest and lowest in ethyl acetate extract (13.13 AE/µL) and n-hexane extract (3.92 AE/µL), respectively. The deep blue zone of α-amylase sprayed TLC plate of extracts with hRF = 72 analysed for ATR-FTIR and NMR spectroscopy which revealed the presence of stigmasterol is responsible for α-amylase inhibition. CONCLUSION: The present work establishes the α-amylase inhibiting properties of A. racemosus maintaining its use for the treatment of DM as a traditional medicine. Bioassay guided isolation through HPTLC-coupled ATR-FTIR and NMR spectroscopy offers an effective method for the exploration of bioactive compounds such as α-amylase inhibitor from complex plant extracts.
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Asparagus , Iodo , Acetatos , Antioxidantes/análise , Clorofórmio , Cromatografia em Camada Fina/métodos , Sequestradores de Radicais Livres , Hexanos , Espectroscopia de Ressonância Magnética , Metanol , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Solventes/química , Amido , Estigmasterol , alfa-AmilasesRESUMO
Asparagus racemosus Willd. is widely used to combat various diseases owing to its medicinal properties. In this study, arial parts of A. racemosus were investigated for their total phenolic content, total flavonoid content and antioxidative potential. A high-performance thin-layer chromatography (HPTLC) method combined with effect-directed-analysis was also developed to screen the antioxidant effects of A. racemosus and quantify biologically active compounds on chromatograms from A. racemosus. Total phenolics (154 mg gallic acid equivalent/g), flavonoid contents (497 mg quercetin/g) and IC50 (15.25 µg/ml) were found to be higher in methanolic extract of A. racemosus than in n-hexane, chloroform and ethyl acetate extracts. HPTLC hyphenated with chemical derivatizations (DPPHâ¢, p-anisaldehyde/sulfuric acid, and ferric chloride) was used to evaluate antioxidant activity and the presence of phytosterols, terpenoids and polyphenolic contents. The same compounds at 100*retention factor = 58, 68, 74 and 65 in extracts were responsible for antioxidant activity. Hyphenated HPTLC allowed a rapid characterization of the active compound with a combination of effect-directed-analysis and attenuated total reflectance-Fourier transform infrared spectroscopy. Spectral analysis of the band from attenuated total reflectance identified myricetin, quercetin, p-coumaric acid and caffeic acid as responsible for the antioxidant activity.
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Antioxidantes , Asparagaceae/química , Cromatografia Líquida de Alta Pressão/métodos , Componentes Aéreos da Planta/química , Extratos Vegetais , Antioxidantes/análise , Antioxidantes/química , Cromatografia em Camada Fina/métodos , Flavonoides/análise , Flavonoides/química , Limite de Detecção , Modelos Lineares , Extratos Vegetais/análise , Extratos Vegetais/química , Reprodutibilidade dos Testes , Espectroscopia de Infravermelho com Transformada de Fourier/métodosRESUMO
Spot blotch disease, caused by Bipolaris sorokiniana, is an important threat to wheat, causing an annual loss of ~17%. Under epidemic conditions, these losses may be 100%, yet the molecular responses of wheat to spot blotch remain almost uncharacterized. Moreover, defense-related phytohormone signaling genes have been poorly characterized in wheat. Here, we have identified 18 central components of salicylic acid (SA), jasmonic acid (JA), ethylene (ET), and enhanced disease susceptibility 1 (EDS1) signaling pathways as well as the genes of the phenylpropanoid pathway in wheat. In time-course experiments, we characterized the reprogramming of expression of these pathways in two contrasting genotypes: Yangmai #6 (resistant to spot blotch) and Sonalika (susceptible to spot blotch). We further evaluated the performance of a population of recombinant inbred lines (RILs) by crossing Yangmai#6 and Sonalika (parents) and subsequent selfing to F10 under field conditions in trials at multiple locations. We characterized the reprogramming of defense-related signaling in these RILs as a consequence of spot blotch attack. During resistance to spot blotch attack, wheat strongly elicits SA signaling (SA biogenesis as well as the NPR1-dependent signaling pathway), along with WRKY33 transcription factor, followed by an enhanced expression of phenylpropanoid pathway genes. These may lead to accumulation of phenolics-based defense metabolites that may render resistance against spot blotch. JA signaling may synergistically contribute to the resistance. Failure to elicit SA (and possibly JA) signaling may lead to susceptibility against spot blotch infection in wheat.
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Ascomicetos/fisiologia , Doenças das Plantas/imunologia , Reguladores de Crescimento de Plantas/metabolismo , Imunidade Vegetal , Transdução de Sinais , Triticum/fisiologia , Ascomicetos/citologia , Ciclopentanos/metabolismo , Etilenos/metabolismo , Regulação da Expressão Gênica de Plantas , Endogamia , Anotação de Sequência Molecular , Oxilipinas/metabolismo , Folhas de Planta/genética , Folhas de Planta/imunologia , Folhas de Planta/fisiologia , Ácido Salicílico/metabolismo , Triticum/genética , Triticum/imunologiaRESUMO
BACKGROUND: Abroma augusta L. (Malvaceae) leaf is traditionally used to treat diabetes in India and Southern Asia. Therefore, current study was performed to evaluate the protective effect of defatted methanol extract of A. augusta leaves (AA) against type 2 diabetes mellitus (T2DM) and its associated nephropathy and cardiomyopathy in experimental rats. METHODS: Antidiabetic activity of AA extracts (100 and 200 mg/kg, p.o.) was measured in streptozotocin-nicotinamide induced type 2 diabetic (T2D) rat. Fasting blood glucose level (at specific interval) and serum biochemical markers (after sacrifice) were measured. Redox status, transcription levels of signal proteins (NF-κB and PKCs), mitochondria dependent apoptotic pathway (Bad, Bcl-2, caspase cascade) and histological studies were performed in kidneys and hearts of controls and AA treated diabetic rats. RESULTS: Phytochemical screening of extracts revealed the presence of taraxerol, flavonoids and phenolic compounds in the AA. T2D rats showed significantly (p < 0.01) elevated fasting blood glucose level. Alteration in serum lipid profile and release of membrane bound enzymes like lactate dehydrogenase and creatine kinase, which ensured the participation of hyperlipidemia and cell membrane disintegration in diabetic pathophysiology. T2DM caused alteration in the serum biochemical markers related to diabetic complications. T2DM altered the redox status, decreased the intracellular NAD and ATP concentrations in renal and myocardial tissues of experimental rats. Investigating the molecular mechanism, activation PKC isoforms was observed in the selected tissues. T2D rats also exhibited an up-regulation of NF-κB and increase in the concentrations of pro-inflammatory cytokines (IL-1ß, IL-6 and TNF-α) in the renal and cardiac tissues. The activation of mitochondria dependent apoptotic pathway was observed in renal and myocardial tissues of the T2D rats. However, Oral administration of AA at the doses of 100 and 200 mg/kg body weight per day could reduce hyperglycemia, hyperlipidemia, membrane disintegration, oxidative stress, vascular inflammation and prevented the activation of oxidative stress induced signaling cascades leading to cell death. Histological studies also supported the protective characteristics of AA. CONCLUSIONS: Results suggest that AA could offer prophylactic role against T2DM and its associated reno- and cardio- toxicity.
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Cardiomiopatias/tratamento farmacológico , Nefropatias Diabéticas/tratamento farmacológico , Inflamação/patologia , Malvaceae/química , Estresse Oxidativo , Extratos Vegetais/uso terapêutico , Folhas de Planta/química , Trifosfato de Adenosina/metabolismo , Animais , Biomarcadores/metabolismo , Glicemia/metabolismo , Peso Corporal/efeitos dos fármacos , Cardiomiopatias/sangue , Cardiomiopatias/complicações , Cardiomiopatias/patologia , Fragmentação do DNA/efeitos dos fármacos , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/complicações , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/patologia , Diabetes Mellitus Tipo 2/sangue , Diabetes Mellitus Tipo 2/complicações , Diabetes Mellitus Tipo 2/tratamento farmacológico , Diabetes Mellitus Tipo 2/patologia , Nefropatias Diabéticas/sangue , Nefropatias Diabéticas/complicações , Nefropatias Diabéticas/patologia , Teste de Tolerância a Glucose , Inflamação/complicações , Rim/efeitos dos fármacos , Rim/metabolismo , Rim/patologia , Masculino , Miocárdio/metabolismo , Miocárdio/patologia , NAD/metabolismo , Niacinamida/farmacologia , Niacinamida/uso terapêutico , Tamanho do Órgão/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/farmacologia , Ratos WistarRESUMO
This investigation focuses on the extraction, characterization, and evaluation of taro (Colocasia esculenta) stolon polysaccharide (TSP) as a tablet binding agent, which is obtained from edible taro stolon. TSP was subjected to phytochemical screening and characterized by FTIR, DSC, TGA, DTA, XRD, particle size, polydispersity index, zeta potential, rheological behavior, and SEM. The tablets prepared with varying concentrations of TSP (2.5 %, 5 %, 7.5 %, and 10 % w/w) and diclofenac sodium (DS) were evaluated and compared with the same concentrations of gum acacia and PVP K-30. The presence of carbohydrates was confirmed by Molisch's test. The FTIR spectra established the compatibility of the drug with excipients. The SEM images revealed asymmetric and elongated particles of TSP powder. The hydration kinetics study showed matrix hydration and water penetration velocity within the range of 0.602-0.753 g/g and 0.112-0.189 cm/g.h, respectively. The tablets showed drug release of >75 % at 45 min. The release-exponent value above 0.89 indicated a super case II drug transport combining matrix erosion and diffusion. Optimum tablet hardness and very low friability, even at 2.5 % binder concentration, suggested the potential application of the novel TSP as a tablet binder in the formulation of the tablets.
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AIMS: To elucidate the impact of 10-(6-plastoquinonyl) decyltriphenylphosphonium (SkQ1) as an anti-colitogenic agent for maintenance of colon epithelial tract in ulcerated mice through recovery of mitochondrial dysfunction and mitochondrial stress by virtue of its free radical scavenging properties. MAIN METHODS: DSS induced ulcerated BALB/c mice were treated with SkQ1 for 14 days @ 30 nmol/kg/body wt./day/mice. Post-treatment, isolated colonic mitochondria were utilized for spectrophotometric and spectrofluorometric biochemical analysis of various mitochondrial functional variables including individual mitochondrial respiratory enzyme complexes. Confocal microscopy was utilized for measuring mitochondrial membrane potential in vivo. ELISA technique was adapted for measuring colonic nitrite and 3-nitrotyrosine (3-NT) content. Finally in vitro cell line study was carried out to substantiate in vivo findings and elucidate the involvement of free radicals in UC using antioxidant/free radical scavenging regimen. KEY FINDINGS: Treatment with SkQ1 in vivo reduced histopathological severity of colitis, induced recovery of mitochondrial respiratory complex activities and associated functional variables, improved oxidative stress indices and normalized mitochondrial cardiolipin content. Importantly, SkQ1 lowered nitrite concentration and 3-nitrotyrosine formation in vivo. In vitro SkQ1 restored mitochondrial functions wherein the efficacy of SkQ1 proved equal or better compared to SOD and DMSO indicating predominant involvement of O2- and OH in UC. However, NO and ONOO- also seemed to play a secondary role as MEG and L-NAME provided lesser protection as compared to SOD and DMSO. SIGNIFICANCE: SkQ1 can be considered as a potent anti-colitogenic agent by virtue of its free radical scavenging properties in treating UC.
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Colite Ulcerativa , Colo , Camundongos Endogâmicos BALB C , Mitocôndrias , Estresse Oxidativo , Plastoquinona , Animais , Camundongos , Colite Ulcerativa/tratamento farmacológico , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/metabolismo , Colite Ulcerativa/patologia , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Plastoquinona/análogos & derivados , Plastoquinona/farmacologia , Colo/efeitos dos fármacos , Colo/patologia , Colo/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Masculino , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Tirosina/análogos & derivados , Tirosina/metabolismo , Tirosina/farmacologia , Antioxidantes/farmacologia , Sequestradores de Radicais Livres/farmacologia , Sulfato de DextranaRESUMO
The present investigation was aimed to fabricate and optimize extended-release beads of diclofenac sodium based on an ion-cross-linked matrix of pectin (PTN) and taro (Colocasia esculenta) stolon polysaccharide (TSP) with 23 full factorial design. Total polysaccharide concentration (TPC), polysaccharide ratio (PR), and cross-linker concentration ([CaCl2]) were taken as independent factors with two levels of each. Initially, TSP was extracted, purified, and characterized. Fourier-transform infrared spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) showed drug-polymer compatibility. The study also revealed the significant positive effect of TSP on drug entrapment efficiency (DEE) and sustaining drug release. The response variables (DEE, cumulative % drug-release at 1, 2, 4, 6, and 10 h, release-constant, time for 50 % and 90 % drug release (T50%, T90%), release-similarity factor (f2), and difference factor (f1) were analyzed, and subsequently, independent fabrication variables were numerically optimized by Design-Expert software (Version-13; Stat-Ease Inc., Minneapolis). The optimized batch exhibited appreciable DEE of 88.5 % (± 2.2) and an extended-release profile with significantly higher T50%, T90%, and release-similarity factor (f2) of 4.7 h, 11.4 h, and 71.6, respectively. Therefore, the study exhibited successful incorporation of the novel TSP as a potential alternative adjunct polysaccharide in the pectin-based ion-cross-linked inter-penetrating polymeric network for extended drug release.
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Colocasia , Preparações de Ação Retardada , Diclofenaco , Liberação Controlada de Fármacos , Pectinas , Diclofenaco/química , Pectinas/química , Colocasia/química , Portadores de Fármacos/química , Polissacarídeos/química , Cálcio/química , Microesferas , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
Black rice (Oryza sativa L.) is a rich source of phenolics and anthocyanins. It was aimed to investigate the effect of different extraction methods such as conventional solvent extraction, ultrasound-assisted extraction (UAE), and microwave-assisted extraction (MAE) on antioxidant activity and phenolic profiling of black rice free, esterified, and bound phenolics fractions. Spectrophotometric methods were used to evaluate antioxidant activity and HPTLC was used for phenolics profiling. The highest content of % yield, total anthocyanin (TAC), total phenolic (TPC), and total flavonoid (TFC) contents were detected in MAE. It was also observed that antioxidant activity based on DPPH, ABTS, superoxide radical-scavenging and ferric reducing antioxidant power (FRAP) assays showed highest activity in MAE. Eight phenolic compounds were identified and quantified by a validated HPTLC method. MAE showed most abundant phenolic compounds. A significant positive correlation was established between % yield, total phenolic content, and total flavonoid content (p < 0.05) where a significant negative correlation was established between % yield, TPC, and TFC with IC50 of antioxidant activity (p < 0.05). Diverse phenolic contents and antioxidant activity were studied with different forms of phenolics with the different extraction methods. It designates that the extraction techniques had effects on the bioactive compounds as well biological properties.
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Antioxidantes , Oryza , Antioxidantes/farmacologia , Antioxidantes/química , Oryza/química , Antocianinas , Micro-Ondas , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Fenóis/química , Flavonoides/químicaRESUMO
Different parts of Camellia sinensis (L.) were extracted with solvents according to polarity, and the extracts' phytochemical profiling and biological activities were examined. The total phenolic (TPC) and total flavonoid (TFC) contents increased with the increasing polarity of the solvent which met its maximum in polar solvents. The increasing antioxidant, anti-inflammatory and antidiabetic activities were recorded with increasing polarity of solvents which showed hydroalcoholic as best solvent. The strong and significant correlation was among the TPC, TFC, DPPH, anti-inflammatory and antidiabetic activities for different parts of tea. HPTLC study of individual phenolic acids, epigallocatechin gallate, gallocatechin and theaflavin met their maximum level of content with polar solvents like hydroalcohol, methanol and water mostly in mainly tea leaves. Our finding suggested that the polar solvents and young leaves of tea were beneficial for obtaining extracts. On the other hand, phenolics were found to be potent antioxidant, anti-inflammatory and antidiabetic agent.
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Antioxidantes , Camellia sinensis , Antioxidantes/farmacologia , Antioxidantes/química , Camellia sinensis/química , Solventes , Fenóis/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Chá/química , Anti-Inflamatórios/farmacologiaRESUMO
The present study aimed to evaluate Cassia fistula seed galactomannan (CFSG) as a tablet-binder in the formulation of a monolithic matrix tablet using diclofenac sodium as a model drug. Initially, CFSG was extracted and purified from the seeds of the Cassia fistula tree and then screened for phytochemicals. Native CFSG was characterized with polysaccharide content determination, monosaccharide composition analysis, elemental analysis, FTIR, solid-state 13C NMR, molecular weight, zeta potential, DSC, TGA-DTA, XRD, viscosity, pH and surface tension, rheology, SEM and acute oral toxicity study. Prior to formulation, the drug-CFSG compatibility was checked by FTIR, DSC, and XRD. Diclofenac sodium-loaded granules were prepared by the wet granulation method and evaluated for various granule properties. Finally, granules were compressed into tablets and evaluated for binding and other tablet properties. The granules showed to have optimum micromeritic properties. Tablet hardness and friability were found to be approximately 7 kg/m2 and 0.3 %, respectively, which substantiate the excellent binding capacity of CFSG. Other tablet properties were also found to be within the Pharmacopoeial compliance limit. The tablets with a minimum concentration of CFSG (2.5%w/w) as binder showed appreciable mechanical strength and faster drug release, which ratifies CFSG as an alternative tablet binder.
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Cassia , Diclofenaco , Sementes , Comprimidos/química , SolubilidadeRESUMO
Background: The World Health Organization declared the outbreak of the novel coronavirus (COVID-19) as a global health emergency on January 30, 2020, and as a pandemic disease on March 11, 2020. This review highlights the international situation, risk factors, and related protections to be taken as prerequisite measures and probable treatment options for the COVID-19-infected population in the current scenario. Main text: The SARS-CoV-2 viruses and their variants caused mild-to-severe respiratory tract infection and used airborne pathways as a way of contagion. Human-to-human transmission led to an exponential growth in the rise in the number of cases making it a real burden to immobilize the rapid spread of the virus while asymptomatic patients created ambiguity for confirmation in the community. It was clear from the case studies of patients that most of them were asymptomatic but still vulnerable to the people around, and hence, in a flash, many countries around the globe went into a complete lockdown, influencing the economy and thrashing industrial outputs. On the other hand, numerous researches were made to counteract the spread through studies in antiviral therapy, immune-based therapy, vaccination development, and natural remedies. Conclusion: Although exploration for a specific drug required for the COVID-19 treatment is under extensive research worldwide and some of them are in clinical trial now. Virtual drug library screening is one of the current techniques for repurposing accessible compounds. This review could provide beneficial information about the potential current and future treatment strategies to treat the pandemic COVID-19 infection.
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ETHNOPHARMACOLOGICAL RELEVANCE: With over 950 species, Cyperus is one of the most promising health boosting genera in the Cyperaceae family. Traditional uses of Cyperus sp. have been described for gastrointestinal blood abnormalities, menstrual irregularities, and inflammatory diseases, among others. Cyperus tegetum Roxb belonging to Cyperaceae family, is used in traditional medicine to treat skin cancers. AIM OF THE STUDY: The present study was carried out to explore the potential effect of the extract of the plant Cyperus tegetum against different pharmacological activity namely inflammatory, analgesic activity as well as skin cancer activity in mice. MATERIALS AND METHODS: Cytotoxicity of the extract was measured by MTT and Live/death assay on HeLa cell line. Skin cancer was induced by 7,12-dimethylbenz(a) anthracene (DMBA) and 12-O-tetradecanoylphorbol-13-acetate (TPA) in mice to measure its effects. RESULT: Stigmasterol and some poly phenolic compounds are identified using HPTLC process from the methanol extract of the rhizome of the plant Cyperus tegetum (CT-II). After confirmation of the presence of different polyphenolic compound and triterpenoids in the extract, it was subject to MTT and Live/death assay on HeLa cell line. From the observation it could be concluded that the IC50 of the extract is 300 µg/ml. Thus, the CTII was evaluated further for its in vivo anticancer property. In the tumorigenesis study, the number of tumor growths, the area and weight of the tumor significantly decreases with increment in the dose of CT-II extract and some elevated enzyme release in renal (creatinine, urea) as well as hepatic (AST, ALT, ALP) enzymes are also controlled with the increased dose of the same extract. The elevated enzyme release may be due to cancer induced rupture of the plasma and cellular damage. This CT-II extract also exhibits some other pharmacological activity like anti-inflammatory and analgesic activity. CONCLUSION: As metabolic activation via carcinogens and inflammation response plays important role in development of cancer, antioxidant, anti-inflammatory and analgesic properties can be correlated with anti-cancer properties. Taken all the above studies, it was illustrated that the extract of Cyperus tegetum might be a promising compound to reduce skin cancer risk.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Cyperus/química , Extratos Vegetais/farmacologia , Neoplasias Cutâneas/tratamento farmacológico , Analgésicos/isolamento & purificação , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Feminino , Células HeLa , Humanos , Inflamação/tratamento farmacológico , Inflamação/patologia , Concentração Inibidora 50 , Masculino , Camundongos , Rizoma , Neoplasias Cutâneas/patologiaRESUMO
The matured fruits of Diospyros peregrina are successfully employed by the traditional healers and local people of costal West Bengal, India for the treatment of diabetes. Present investigation was undertaken to evaluate the role of hydroalcoholic extract of D. peregrina (HDP) on type 2 diabetes as well as the augmented oxidative stresses associated with it. Oral administration of HDP at 25, 50 and 100 mg kg(-1) body weight per day to diabetic rats was found to possess significant dose-dependent hypoglycemic and hypolipidemic activity. The diabetic rats showed lower activities of superoxide dismutase (SOD), catalase (CAT) and reduced glutathione (GSH) content in hepatic and renal tissues as compared to normal rats. The activities of SOD, CAT and GSH were found to be increased in extract-treated diabetic rats in selected tissues. The increased level of lipid peroxidation (thiobarbituric acid reactive substances) in diabetic rats was also found to be reverted back to near normal status in extract-treated groups. Thus it may be concluded that the HDP may produce its hypoglycemic effect through antioxidant defense mechanism.