RESUMEN
Tuberose flowers (Calcutta Single variety) valued as ornamentals globally, have short shelf-lives of 8 days at 4 ± 1 °C and are therefore discarded post senescence. Previous investigations from our laboratory have established that a combination treatment using GRAS preservatives [(sucrose (4%) and CaCl2 (0.02%)]-cum-gamma-irradiation (0.02 kGy) could extend its shelf-life to 24 days, when stored at 4 ± 1 °C with concomitant enhancement in the content of its bioactive principle, viz. methyl eugenol. Supercritical carbon dioxide (SC-CO2) extract of the tuberose flower wastes post combination treatment therefore had a higher methyl eugenol content (4.11 ± 0.05 µg/g), vis-à-vis its non-treated counterpart (2.03 ± 0.03 µg/g), and thus significantly higher antioxidant and antimicrobial potencies (MIC values of 1.83 ± 0.02 mg/ml and 1.98 ± 0.03 mg/ml against S. aureus ATCC 25923 strain and MDR strain, respectively). The microencapsulated powder of the extract (MEp) obtained by spray drying was applied for healing of epidermal wounds created on New Zealand white rabbits, post skin irritancy test (wherein no clinical sign of toxicity, redness or swelling was observed). When MEp was applied, accelerated healing occurred which commenced on day 2 and was completed by day 6 vis-à-vis that of the control powder set (without extract) which showed no signs of wound healing. Therefore, the sensorially compromised-senesced tuberose flowers, a rich source of methyl eugenol, has been successfully valorized through utilization of the same in developing a novel topical antibiotic powder against potent skin pathogens.
Asunto(s)
Agave , Dióxido de Carbono , Animales , Conejos , Polvos , Staphylococcus aureus , India , Flores , Extractos Vegetales/farmacologíaRESUMEN
Plausible interactions between food contaminants and natural constituents in vivo and protective effect of polyphenols present in I. aquatica against carbofuran toxicity in Charles Foster rats were evaluated. Determinations based on antioxidant enzyme activities showed significant alterations in glutathione, glutathione peroxidase, superoxide dismutase and catalase in tissues (liver and brain) and plasma of pesticide treated group while polyphenolic extracts from I. aquatica (IAE) attenuated their activities when given alongwith carbofuran. IAE decreased enhanced lipid peroxidation levels in plasma and erythrocyte membrane and cholesterol levels in brain and plasma. IAE also minimized histopathological degenerative changes produced by carbofuran. While single cell gel electrophoresis showed that secondary metabolites in leafy vegetables produced a combinatorial effect with pesticide at cellular level, DNA fragmentation level in bone marrow cells showed a decline in the IAE treated rats. Food safety adversely affected by various chemical contaminants can be retained by plant polyphenols and secondary plant constituents that can be found together in bolus. Therefore, the present study gives an insight into the protective role of naturally found polyphenols against pesticide toxicity.
Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Ipomoea/química , Hígado/efectos de los fármacos , Extractos Vegetales/administración & dosificación , Animales , Antioxidantes/administración & dosificación , Antioxidantes/química , Carbofurano/toxicidad , Catalasa/sangre , Enfermedad Hepática Inducida por Sustancias y Drogas/sangre , Enfermedad Hepática Inducida por Sustancias y Drogas/enzimología , Glutatión Peroxidasa/sangre , Peroxidación de Lípido/efectos de los fármacos , Hígado/enzimología , Masculino , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/química , Polifenoles/administración & dosificación , Polifenoles/química , Ratas , Superóxido Dismutasa/sangreRESUMEN
The present treatment for Alzheimer's disease (AD) involves well known synthetic acetylcholine esterase (AChE) inhibitor drugs which besides having short duration of action also have deleterious impact on human health. Therefore, there is a need for natural plant-based biomolecule(s) with potential AChE inhibition activity (ies). The aim of the work is to design a spice-based nano-vehicle as a novel green alternative of synthetic AD drugs by nanoencapsulating a solvent-less supercritical CO2 extract of small cardamom seeds (SCE) having a synergistic consortium of five antioxidant molecules, using polyethylene glycol and emulsifiers, selected based on Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) analyses. Ellman's assay and enzyme inhibition kinetics of the antioxidant molecules as well as the extract and its nanoliposomal formulation (SCE-NL) were performed, followed by rigorous molecular docking and dynamics studies using MM-PBSA and umbrella sampling. The antioxidants exhibited significant AChE inhibition in vitro, individually with 1, 8-cineole having the least IC50 value of 65.53 ± 0.05 µg/mL. . Although SCE-NL had higher IC50 value (575.67 ± 0.5 µg/mL) vis-à-vis that of rivastigmine (67.52 ± 0.02 µg/mL), it is safer for usage being 'green'.The Lineweaver-Burk plots (Vmax â¼1.04 mM/min) revealed competitive mode(s) of inhibition of AChE with each of these antioxidants. Binding energy analyses suggested very good binding free energies and stable docking/binding complexes (between the antioxidants and AChE). This study has delivered a nanoliposomal vehicle of food antioxidants as a putative 'green' alternative of synthetic AChE inhibitor drugs.Communicated by Ramaswamy H. Sarma.
RESUMEN
Protective effect of Moringa oleifera leaf extract (MoLE) against radiation-induced lipid peroxidation has been investigated. Swiss albino mice, selected from an inbred colony, were administered with MoLE (300 mg/kg body wt) for 15 days before exposing to a single dose of 5 Gy 60Co-gamma radiation. After treatments, animals were necropsied at different post irradiation intervals (days 1, 7 and 15) and hepatic lipid peroxidation and reduced glutathione (GSH) contents were estimated to observe the relative changes due to irradiation and its possible amelioration by MoLE. It was observed that, MoLE treatment restored GSH in liver and prevented radiation induced augmentation in hepatic lipid peroxidation. Phytochemical analysis showed that MoLE possess various phytochemicals such as ascorbic acid, phenolics (catechin, epicatechin, ferulic acid, ellagic acid, myricetin) etc., which may play the key role in prevention of hepatic lipid peroxidation by scavenging radiation induced free radicals.
Asunto(s)
Peroxidación de Lípido/efectos de los fármacos , Peroxidación de Lípido/efectos de la radiación , Hígado , Moringa oleifera/química , Extractos Vegetales/farmacología , Radiación Ionizante , Protectores contra Radiación/farmacología , Animales , Depuradores de Radicales Libres/metabolismo , Depuradores de Radicales Libres/farmacología , Humanos , Radical Hidroxilo/metabolismo , Hígado/efectos de los fármacos , Hígado/metabolismo , Hígado/efectos de la radiación , Masculino , Ratones , Extractos Vegetales/metabolismo , Protectores contra Radiación/metabolismo , Sustancias Reactivas al Ácido Tiobarbitúrico/metabolismoRESUMEN
Radioprotective action of gossypetin (GTIN) against gamma (γ)-radiation-induced oxidative stress in liver was explored in the present article. Our main aim was to evaluate the protective efficacy of GTIN against radiation-induced alteration of liver in murine system. To evaluate the effect of GTIN, it was orally administered to mice at a dose of 30 mg/kg body weight for three consecutive days prior to γ-radiation at a dose of 5 Gy. Radioprotective efficacy of GTIN were evaluated at physiological, cellular, and molecular level using biochemical analysis, comet assay, flow cytometry, histopathology, immunofluorescence, and immunoblotting techniques. Ionizing radiation was responsible for augmentation of hepatic oxidative stress in terms of lipid peroxidation and depletion of endogenous antioxidant enzymes. Immunoblotting and immunofluorescence studies showed that irradiation enhanced the nuclear translocation of nuclear factor kappa B (NF-κB) level, which leads to hepatic inflammation. To investigate further, we found that radiation induced the activation of stress-activated protein kinase/c-Jun NH2-terminal kinase (SAPK/JNK)-mediated apoptotic pathway and deactivation of the NF-E2-related factor 2 (Nrf2)-mediated redox signaling pathway, whereas GTIN pretreatment ameliorated these radiation-mediated effects. This is the novel report where GTIN rationally validated the molecular mechanism in terms of the modulation of cellular signaling system' instead of ' This is the novel report where GTIN is rationally validated in molecular terms to establish it as promising radioprotective agents. This might be fruitful especially for nuclear workers and defense personnel assuming the possibility of radiation exposure.
Asunto(s)
Antioxidantes/uso terapéutico , Flavonoides/uso terapéutico , Depuradores de Radicales Libres/uso terapéutico , Rayos gamma/efectos adversos , Hígado/efectos de los fármacos , Protectores contra Radiación/uso terapéutico , Alanina Transaminasa/sangre , Fosfatasa Alcalina/sangre , Animales , Antioxidantes/química , Antioxidantes/farmacología , Aspartato Aminotransferasas/sangre , Disponibilidad Biológica , Catalasa/metabolismo , Roturas del ADN de Doble Cadena , Evaluación Preclínica de Medicamentos , Flavonoides/química , Flavonoides/farmacología , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/farmacología , Glutatión/metabolismo , Hepatocitos/efectos de los fármacos , Hepatocitos/efectos de la radiación , Interleucina-6/sangre , Peroxidación de Lípido/efectos de los fármacos , Peroxidación de Lípido/efectos de la radiación , Hígado/efectos de la radiación , Hígado/ultraestructura , Masculino , Ratones , Estructura Molecular , Factor 2 Relacionado con NF-E2/metabolismo , Oxidación-Reducción , Estrés Oxidativo/efectos de los fármacos , Fosfatidilinositol 3-Quinasas/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Protectores contra Radiación/química , Protectores contra Radiación/farmacología , Transducción de Señal/efectos de los fármacos , Superóxido Dismutasa/metabolismo , Factor de Necrosis Tumoral alfa/sangreRESUMEN
Ionizing radiation is responsible for oxidative stress by generating reactive oxygen species (ROS), which alters the cellular redox potential. This change activates several redox sensitive enzymes which are crucial in activating signaling pathways at molecular level and can lead to oxidative stress induced inflammation. Therefore, the present study was intended to assess the anti-inflammatory role of ferulic acid (FA), a plant flavonoid, against radiation-induced oxidative stress with a novel mechanistic viewpoint. FA was administered (50 mg/kg body wt) to Swiss albino mice for five consecutive days prior to exposing them to a single dose of 10 Gy 60Co γ-irradiation. The dose of FA was optimized from the survival experiment and 50 mg/kg body wt dose showed optimum effect. FA significantly ameliorated the radiation induced inflammatory response such as phosphorylation of IKKα/ß and IκBα and consequent nuclear translocation of nuclear factor kappa B (NF-κB). FA also prevented the increase of cycloxygenase-2 (Cox-2) protein, inducible nitric oxide synthase-2 (iNOS-2) gene expression, lipid peroxidation in liver and the increase of tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) in serum. It was observed that exposure to radiation results in decreased activity of superoxide dismutase (SOD), catalase (CAT) and the pool of reduced glutathione (GSH) content. However, FA treatment prior to irradiation increased the activities of the same endogenous antioxidants. Thus, pretreatment with FA offers protection against gamma radiation induced inflammation.
Asunto(s)
Ácidos Cumáricos/farmacología , Inflamación/tratamiento farmacológico , Inflamación/etiología , Estrés Oxidativo/efectos de los fármacos , Traumatismos Experimentales por Radiación/tratamiento farmacológico , Análisis de Varianza , Animales , Western Blotting , Cromatografía Líquida de Alta Presión , Ácidos Cumáricos/administración & dosificación , Ácidos Cumáricos/uso terapéutico , Ciclooxigenasa 2/metabolismo , Cartilla de ADN/genética , Relación Dosis-Respuesta a Droga , Ensayo de Inmunoadsorción Enzimática , Rayos gamma , Inmunohistoquímica , Interleucina-6/sangre , Peroxidación de Lípido/efectos de los fármacos , Masculino , Ratones , Óxido Nítrico Sintasa de Tipo II/metabolismo , Estrés Oxidativo/efectos de la radiación , Reacción en Cadena de la Polimerasa , Factor de Necrosis Tumoral alfa/sangreRESUMEN
In this study, the extract of a green leafy vegetable Oxalis corniculata (Oxalidaceae) was evaluated for its in vitro antibacterial and in vivo anti colonizing effect against common intestinal pathogenic bacteria. Methanolic extract (80%) of Oxalis corniculata (Oxalidaceae) leaf contained a polyphenol content of 910 mg gallic acid equivalent per gram of dry weight and the yield was 8%. The flavonoid content was 2.353 g quercetin equivalent per 100 g of the extract. In vitro studies indicated that the extract inhibited numerous pathogenic bacteria like Staphylococcus aureus (ATCC 25922), Escherichia coli (ATCC 25923), Shigella dysenteriae 1 (NT4907), Shigella flexneri 2a (2457T), Shigella boydii 4 (BCH612), and Shigella sonnie phase I (IDH00968). The minimum inhibitory concentration (MIC) against E. coli (ATCC 25923) was minimal (0.08 mg/mL), whereas MIC against S. flexneri 2a (2457T) was higher (0.13 mg/mL). A suckling mouse model was developed which involved challenging the mice intragastrically with S. flexneri 2a (2457T) and S. dysenteriae 1 (NT4907) to study the anticolonization activity. It was revealed that the extract was more potent against S. dysenteriae 1 (NT4907) as compared to S. flexneri 2a (2457T). It was also found that simultaneous administration of extract along with bacterial inoculums promoted good anticolonization activity. Significant activity was observed even when treated after 3 h of bacterial inoculation.
Asunto(s)
Antibacterianos/farmacología , Diarrea/tratamiento farmacológico , Magnoliopsida/química , Shigella dysenteriae/efectos de los fármacos , Shigella flexneri/efectos de los fármacos , Animales , Animales Lactantes , Diarrea/microbiología , Humanos , Ratones , Hojas de la Planta/química , Shigella dysenteriae/crecimiento & desarrollo , Shigella flexneri/crecimiento & desarrolloRESUMEN
Polyphenolic extracts (PE) of edible flower of Sesbania grandiflora were tested to evaluate its antimicrobial effect against some common pathogenic bacteria and growth promoting property against probiotic organism Lactobacillus acidophilus. The antimicrobial activity of S. grandiflora flower PE against selected pathogens was evaluated using both in vitro and in situ methods. In vitro studies suggested that PE has inhibitory effect against Staphylococcus aureus, Shigella flexneri 2a, Salmonella Typhi, Escherichia coli and Vibrio cholerae. The gram-positive organism S. aureus was the most sensitive organism to PE and minimum inhibitory concentration (MIC) was found to be 0.013 mg/mL where as the MIC of PE against V. cholerae was the highest (0.25 mg/mL). On the other hand PE showed growth promoting effect on the common probiotic bacterium L. acidophilus. The major finding was that S. grandiflora PE induced a significant biomass increase of L. acidophilus grown in liquid culture media. PE showed reduction of S. aureus growth in food (fish) during storage at 10°C. High performance liquid chromatography analysis showed that rutin, a major flavonoid of the PE diminished in the culture medium MRS broth with the growth of L. acidophilus.
Asunto(s)
Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Péptidos y Proteínas de Señalización Intercelular/farmacología , Polifenoles/farmacología , Sesbania/química , Antibacterianos/aislamiento & purificación , Flores/química , Péptidos y Proteínas de Señalización Intercelular/aislamiento & purificación , Polifenoles/aislamiento & purificaciónRESUMEN
The current study was intended to evaluate the hepatoprotective effect of Epicatechin (EC) against radiation-induced oxidative stress, in terms of inflammation and lipid peroxidation. Swiss albino mice were administered with EC (15 mg/kg body weight) for three consecutive days before exposing them to a single dose of 5-Gy (60)Co gamma (γ) irradiation. Mice were necropsied and livers were taken for immunohistochemistry, western blot analysis and biochemical tests for the detection of markers of hepatic oxidative stress. Nuclear translocation of nuclear factor kappa B (NF-κB) and lipid peroxidation were increased whereas the activities of superoxide dismutase (SOD) and catalase (CAT), reduced glutathione (GSH) content and ferric reducing antioxidant power (FRAP) were diminished upon radiation exposure compared to control. Translocation of NF-κB from cytoplasm to nucleus and lipid peroxidation were found to be inhibited whereas an increase in SOD, CAT, GSH and FRAP was observed in the mice treated with EC prior to irradiation. Thus, pre-treatment with EC offers protection against γ-radiation induced hepatic alterations.
Asunto(s)
Antioxidantes/farmacología , Catequina/farmacología , Hígado/efectos de los fármacos , Estrés Oxidativo/efectos de los fármacos , Traumatismos Experimentales por Radiación/metabolismo , Protectores contra Radiación/farmacología , Animales , Catalasa/metabolismo , Rayos gamma , Glutatión/metabolismo , Inflamación/metabolismo , Inflamación/prevención & control , Peroxidación de Lípido/efectos de los fármacos , Hígado/metabolismo , Hígado/efectos de la radiación , Masculino , Ratones , FN-kappa B/metabolismo , Transporte de Proteínas , Traumatismos Experimentales por Radiación/prevención & control , Especies Reactivas de Oxígeno/antagonistas & inhibidores , Especies Reactivas de Oxígeno/metabolismo , Superóxido Dismutasa/metabolismoRESUMEN
Acephate, an organophosphorus pesticide, has been proved to play an important role in tissue damage by inducing oxidative stress through the release of free radicals. The aim of this study was to evaluate the protective effect of the plant phenolic compounds present in Enydra fluctuans against acephate toxicity based on lipid peroxidation and antioxidant enzymes profile in rats. An oral dose of acephate at 30 mg/kg of body weight has been given against the extracts containing 20mg of polyphenolic compounds (expressed as gallic acid equivalents)/kg body weight for 14 days. The results showed that under the influence of the pesticides, there was significant decrease in the activities of the antioxidant enzymes SOD, Catalase and Glutathione peroxidase (GPx) and an increase in the non-enzymatic Glutathione, with respect to the normal and the plant extract gavaged groups. Also that there was an increase in the plasma and erythrocyte membrane lipid peroxidation levels in the pesticide treated group compared to the normal or the group treated with the plant extract. The present study thus gives an insight into the ill-effects of this organophosphate and the protective role of plant polyphenols in minimizing those effects.
Asunto(s)
Asteraceae/química , Flavonoides/farmacología , Insecticidas/toxicidad , Compuestos Organotiofosforados/toxicidad , Estrés Oxidativo/efectos de los fármacos , Fenoles/farmacología , Animales , Cromatografía Líquida de Alta Presión , Dieta , Membrana Eritrocítica/efectos de los fármacos , Membrana Eritrocítica/metabolismo , Flavonoides/química , Insecticidas/antagonistas & inhibidores , Peroxidación de Lípido/efectos de los fármacos , Hígado/efectos de los fármacos , Hígado/enzimología , Hígado/metabolismo , Masculino , Compuestos Organotiofosforados/antagonistas & inhibidores , Fenoles/química , Fosforamidas , Extractos Vegetales/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Polifenoles , Ratas , Ratas Wistar , Sustancias Reactivas al Ácido Tiobarbitúrico/metabolismoRESUMEN
Three different cultivars of marigold flowers ( Tagetes patula L.) (marigold orange, marigold yellow, and marigold red) were analyzed for the lutein ester contents, and the in vitro antioxidative activities of the flower extracts were compared. The total antioxidant capacity, reducing power, hydroxyl, DPPH, and ABTS(*+) radical scavenging activities, iron chelation capacity, and inhibition of lipid peroxidation in a linoleic acid emulsion system were measured. Iron-mediated Fenton reaction was carried out to evaluate the protective effect of leutin against DNA damage. The marigold orange (MGO) variety contains the maximum amount of lutein. It also had the highest DPPH radical scavenging activity and ABTS radical scavenging activity, with an EC(50) value of 0.344 mg/mL. It was also the most effective against lipid peroxidation and hydroxyl radical scavenging activities. The MGO extract has the maximum reducing power. Hepatic cell damage in iron-mediated Fenton reaction caused by free radicals was reduced by the marigold extracts. Marigold flowers of Indian variety can be effectively utilized to produce lutein ester, which can be used as a food supplement or as an accessible source of natural antioxidants.