RESUMEN
Various conventional treatments including endocrine therapy, radiotherapy, surgery, and chemotherapy have been used for several decades to treat breast cancer; however, these therapies exhibit various life-threatening and debilitating adverse effects in patients. Additionally, combination therapies are required for prompt action as well as to prevent drug resistance toward standard breast cancer medications. Ferrite nanoparticles (NPs) are increasingly gaining momentum for their application in the diagnosis and treatment of breast cancer. Spinel ferrites are particularly used against breast cancer and have shown in vitro and in vivo better efficacy as compared to conventional cancer therapies. Magnetic resonance imaging contrast agents, magnetic particle imaging tracers, cell separation, and immune assays are some aspects related to the diagnosis of breast cancer against which different ferrite NPs have been successfully evaluated. Moreover, citrate-coated nickel ferrite, Mg/Zn ferrites, poly amidoamine dendrimers, cobalt ferrites, graphene oxide cobalt ferrites, doxorubicin functionalized cobalt ferrites, chitosan-coated zinc ferrites, PEG-coated cobalt ferrite, and copper ferrite NPs have demonstrated antiproliferative action against different breast cancer cells. Oxaliplatin-loaded polydopamine/BSA-copper ferrites, functionalized cobalt and zinc ferrites of curcumin, oxaliplatin-copper ferrite NPs, tamoxifen/diosgenin encapsulated ZnO/Mn ferrites, and fabricated core-shell fibers of doxorubicin have been developed to increase the bioavailability and anti-proliferative effect and decrease the toxicity of anticancer drugs. These ferrite NPs showed an anticancer effect at different doses in the presence or absence of an external magnetic field. The present review covers the in-depth investigations of ferrite NPs for the diagnosis and management of breast cancer.
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Neoplasias de la Mama , Humanos , Femenino , Neoplasias de la Mama/diagnóstico , Neoplasias de la Mama/tratamiento farmacológico , Cobre , Oxaliplatino , Doxorrubicina , Cobalto , ZincRESUMEN
An experiment was carried out to explore the impact of petroleum hydrocarbons (PHs)-degrading microbial consortium (MC) on phytoremediation ability and growth of water hyacinth (WH) plants in water contaminated with lead (Pb) and PHs. Buckets (12-L capacity) were filled with water and WH plants, PHs (2,400 mg L-1) and Pb (10 mg L-1) in respective buckets. Plants were harvested after 30 days of transplanting and results showed that PHs and Pb substantially reduced the agronomic (up to 62%) and physiological (up to 49%) attributes of WH plants. However, the application of MC resulted in a substantial increase in growth (38%) and physiology (22%) of WH plants over uninoculated contaminated control. The WH + MC were able to accumulate 93% Pb and degrade/accumulate 72% of PHs as compared to initial concentration. Furthermore, combined use of WH plants and MC in co-contamination of PHs and Pb, reduced Pb and PHs contents in water by 74% and 68%, respectively, than that of initially applied concentration. Our findings suggest that the WH in combination with PHs-degrading MC could be a suitable nature-based water remediation technology for organic and inorganic contaminants and in future it can be used for decontamination of mix pollutants from water bodies.
Phytoremediation by aquatic macrophytes is a promising technique for the cleanup of environmental toxins from wastewater. To our knowledge, this is the first study reporting the integrated use of water hyacinth (WH) plants and a newly developed multi-trait microbial consortium for the simultaneous remediation of organic (i.e., petroleum hydrocarbons) and inorganic (i.e., lead) pollutants from the contaminated water. Findings of this study provide the basic but important information on the combined use of WH and microbes for remediation of mix pollution from water bodies.
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Eichhornia , Petróleo , Contaminantes del Suelo , Biodegradación Ambiental , Plomo , Hidrocarburos , Plantas , Contaminantes del Suelo/análisis , SueloRESUMEN
Transfersomes (TFS) are the promising carriers for transdermal delivery of various low and high molecular weight drugs, owing to their self-regulating and self-optimizing nature. Herein, we report synthesis and characterization of TFS loaded with meloxicam (MLX), an NSAID, and dexamethasone (DEX), a steroid, for simultaneous transdermal delivery. The different formulations of TFS containing varying amounts of lecithin, Span 80, and Tween 80 (TFS-1 to TFS-6) were successfully prepared by thin-film hydration method. The size of ranged between 248 and 273 nm, zeta potential values covering from -62.6 to -69.5 mV, polydispersity index (PDI) values in between 0.329 and 0.526, and entrapment efficiency of MLX and DEX ranged between 63-96% and 48-81%, respectively. Release experiments at pH 7.4 demonstrated higher cumulative drug release attained with Tween 80 compared to Span 80-based TFS. The scanning electron microscopy (SEM) of selected formulations -1 and TFS-3 revealed spherical shape of vesicles. Furthermore, three optimized transfersomal formulations (based on entrapment efficiency, TFS-1, TFS-3, and TFS-5) were incorporated into carbopol-940 gels coded as TF-G1, TF-G3, and TF-G5. These transfersomal gels were subjected to pH, spreadability, viscosity, homogeneity, skin irritation, in vitro drug release, and ex vivo skin permeation studies, and the results were compared with plain (nontransfersomal) gel having MLX and DEX. TFS released 71.72% to 81.87% MLX in 12 h; whereas, DEX release was quantified as 74.72% to 83.72% in same time. Nevertheless, TF-based gels showed slower drug release; 51.54% to 59.60% for MLX and 48.98% to 61.23% for DEX. The TF-G systems showed 85.87% permeation of MLX (TF-G1), 68.15% (TF-G3), and 68.94% (TF-G5); whereas, 78.59%, 70.54%, and 75.97% of DEX was permeated by TF-G1, TF-G3, and TF-G5, respectively. Kinetic modeling of release and permeation data indicated to follow Korsmeyer-Peppas model showing diffusion diffusion-based drug moment. Conversely, plain gel influx was found mere 26.18% and 22.94% for MLX and DEX, respectively. These results suggest that TF-G loaded with MLX and DEX can be proposed as an alternate drug carriers for improved transdermal flux that will certainly increase therapeutic outcomes.
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Dexametasona , Lecitinas , MeloxicamRESUMEN
Saponins are natural compounds found in plants and have a diverse range of applications. However, the therapeutic potential of saponins in regulating cytotoxicity, angiogenesis, and inflammation in mammalian cells is yet to be explored. Here, we investigated the therapeutic effects of saponins from green tea by exploring the cytotoxic effects of saponins by inducing apoptosis in the human cancer cell lines hepatocellular carcinoma (HEPG2) and colorectal adenocarcinoma (HT29). The anti-angiogenesis effect of saponins was also investigated in human umbilical vein endothelial cells (HUVEC). We explored the ability of saponins to attenuate inflammation in a dose-dependent manner in normal human cells. It was found that saponins exhibit cytotoxic effects in cancer cells and not in normal cells at the same concentration. Cytotoxicity was measured by inducing apoptosis by enhancing caspase-3 (cas-3) activation and B-cell lymphoma-2 (Bcl-2)-associated X protein (BAX) gene expression and suppressing the antiapoptotic protein, Bcl-2. The inhibition of HUVEC proliferation was due to the suppression of the phosphoinositide 3-kinase (PI3K), protein kinase B (AKT), vascular endothelial growth factor receptor-2 (VEGFR-2), and nuclear factor kappa B (NF-κB). We also observed the antioxidant potential of green tea-derived saponins against free radicals in reactive oxygen species (ROS)-induced cells. Here we observed that the saponins exhibited free radical scavenging activities and activated nuclear factorerythroid 2-related factor 2 (NRF-2) leading to the upregulation of antioxidant-related genes in human embryonic kidney 293 (HEK293) cells. Furthermore, we demonstrated that the anti-inflammatory effects were due to the suppression of pro-inflammatory cytokines interleukin (IL)-1ß, IL-6, tumor necrosis factor-alpha (TNF-α), and inducible nitric oxide synthase (iNOS) in HEK293 cells. The significance of the work is we are the first to report on the anti-cancer effects of saponins based on the anti-inflammatory, antioxidant, anti-angiogenesis, and apoptosis induction properties. In conclusion, green tea-derived saponins could be effective therapeutics for the treatment of cancer.
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Proteínas Proto-Oncogénicas c-akt , Saponinas , Inhibidores de la Angiogénesis/farmacología , Inhibidores de la Angiogénesis/uso terapéutico , Animales , Antiinflamatorios/farmacología , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Caspasa 3/metabolismo , Células Endoteliales/metabolismo , Células HEK293 , Humanos , Inflamación/tratamiento farmacológico , Interleucina-6/metabolismo , Mamíferos/metabolismo , FN-kappa B/metabolismo , Óxido Nítrico Sintasa de Tipo II/metabolismo , Fosfatidilinositol 3-Quinasa/metabolismo , Fosfatidilinositol 3-Quinasas/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Especies Reactivas de Oxígeno/metabolismo , Saponinas/farmacología , Saponinas/uso terapéutico , Té , Factor de Necrosis Tumoral alfa/metabolismo , Factor A de Crecimiento Endotelial Vascular/metabolismo , Receptor 2 de Factores de Crecimiento Endotelial Vascular/metabolismo , Proteína X Asociada a bcl-2/metabolismoRESUMEN
Pterostilbene is a stilbene flavonoid that occurs naturally in various plants as well as produced by genetic engineering. It exhibits anti-inflammatory, analgesic, anti-oxidant and neuroprotective activities. This research was aimed to determine the potential of pterostilbene against arthritis and peripheral neuropathy in Complete Freund's Adjuvant (CFA) induced arthritis. Rat hind paw was injected with 0.1 ml CFA to induce arthritis. Standard control animals received oral methotrexate (3 mg/kg/week). Pterostilbene at 12.5, 25 and 50 mg/kg was given orally to different groups of arthritic rats from day 7-28 for 21 days. Pterostilbene significantly reduced paw diameter and retarded the decrease in body weight of arthritic rats. It profoundly (p < 0.05-0.0001) reduced lipid peroxidation and nitrites, while increased superoxide dismutase (SOD) in the liver tissue. Pterostilbene treatment significantly (p < 0.0001) reduced TNF-α and IL-6 levels. Pterostilbene markedly improved (p < 0.05-0.001) motor activity and showed analgesic effect in arthritic rats at 25 and 50 mg/kg as compared to disease control rats. Furthermore, it notably (p < 0.05-0.0001) increased SOD activity, nitrites, noradrenaline and serotonin levels in the sciatic nerve of arthritic rats. Treatment with pterostilbene also ameliorated the CFA-induced pannus formation, cartilage damage and synovial hyperplasia in the arthritic rat paws. It is determined from the current study that pterostilbene was effective in reducing CFA-induced arthritis in rats through amelioration of oxidative stress and inflammatory mediators. It was also effective to treat peripheral neuropathy through modulation of oxidative stress and neurotransmitters in sciatic nerves.
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Artritis Experimental , Enfermedades del Sistema Nervioso Periférico , Estilbenos , Animales , Ratas , Analgésicos/farmacología , Artritis Experimental/tratamiento farmacológico , Artritis Experimental/inducido químicamente , Citocinas , Adyuvante de Freund , Neurotransmisores/farmacología , Nitritos , Estrés Oxidativo , Ratas Wistar , Estilbenos/farmacología , Superóxido DismutasaRESUMEN
Tauopathy is one of the major causes of neurodegenerative disorders and diseases such as Alzheimer's disease (AD). Hyperphosphorylation of tau proteins by various kinases leads to the formation of PHF and NFT and eventually results in tauopathy and AD; similarly, neuroinflammation also exaggerates and accelerates neuropathy and neurodegeneration. Natural products with anti-tauopathy and anti-neuroinflammatory effects are highly recommended as safe and feasible ways of preventing and /or treating neurodegenerative diseases, including AD. In the present study, we isolated theasaponin E1 from ethanol extract of green tea seed and evaluated its therapeutic inhibitory effects on tau hyper-phosphorylation and neuroinflammation in neuroblastoma (SHY-5Y) and glioblastoma (HTB2) cells, respectively, to elucidate the mechanism of the inhibitory effects. The expression of tau-generating and phosphorylation-promoting genes under the effects of theasaponin E1 were determined and assessed by RT- PCR, ELISA, and western blotting. It was found that theasaponin E1 reduced hyperphosphorylation of tau and Aß concentrations significantly, and dose-dependently, by suppressing the expression of GSK3 ß, CDK5, CAMII, MAPK, EPOE4(E4), and PICALM, and enhanced the expression of PP1, PP2A, and TREM2. According to the ELISA and western blotting results, the levels of APP, Aß, and p-tau were reduced by treatment with theasaponin E1. Moreover, theasaponin E1 reduced inflammation by suppressing the Nf-kB pathway and dose-dependently reducing the levels of inflammatory cytokines such as IL-1beta, IL-6, and TNF-alpha etc.
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Enfermedad de Alzheimer , Fármacos Neuroprotectores , Saponinas , Enfermedad de Alzheimer/tratamiento farmacológico , Enfermedad de Alzheimer/metabolismo , Glucógeno Sintasa Quinasa 3/metabolismo , Humanos , Enfermedades Neuroinflamatorias , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/uso terapéutico , Fosforilación , Saponinas/farmacología , Saponinas/uso terapéutico , Semillas/metabolismo , Té , Proteínas tau/metabolismoRESUMEN
In this article, formulation studies for terbinafine hydrochloride nanoemulsions, prepared by high-energy ultrasonication technique, are described. Pseudo-ternary phase diagram was constructed in order to find out the optimal ratios of oil and surfactant/co-solvent mixture for nanoemulsion production. Clove and olive oils were selected as oil phase. Based on the droplet size evaluation, maximum nanoemulsion region were determined for formulation development. Further characterization included polydispersity index (PDI), zeta potential, Fourier transform infrared (FT-IR) spectroscopy, morphology, pH, viscosity, refractive index, ex vivo skin permeation, skin irritation, and histopathological examination. Droplet sizes of optimized formulations were in colloidal range. PDI values below 0.35 indicated considerably homogeneous nanoemulsions. Zeta potential values were from 13.2 to 18.1 mV indicating good stability, which was also confirmed by dispersion stability studies. Ex vivo permeation studies revealed almost total skin permeation of terbinafine hydrochloride from the nanoemulsions (96-98%) in 6 hours whereas commercial product reached only 57% permeation at the same time. Maximum drug amounts were seen in epidermis and dermis layers. Skin irritation and histopathological examination demonstrated dermatologically safe formulations. In conclusion, olive oil and clove oil-based nanoemulsion systems have potential to serve as promising carriers for topical terbinafine hydrochloride delivery.
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Antifúngicos/farmacología , Aceite de Clavo/química , Nanopartículas/química , Aceite de Oliva/química , Terbinafina/farmacología , Administración Tópica , Animales , Antifúngicos/administración & dosificación , Antifúngicos/efectos adversos , Antifúngicos/farmacocinética , Química Farmacéutica , Portadores de Fármacos , Emulsiones/química , Concentración de Iones de Hidrógeno , Ratones , Tamaño de la Partícula , Absorción Cutánea/efectos de los fármacos , Solubilidad , Propiedades de Superficie , Terbinafina/administración & dosificación , Terbinafina/efectos adversos , Terbinafina/farmacocinética , ViscosidadRESUMEN
Obesity is a public health problem characterized by increased body weight due to abnormal adipose tissue expansion. Bioactive compound consumption from the diet or intake of dietary supplements is one of the possible ways to control obesity. Natural products with adipogenesis-regulating potential act as obesity treatments. We evaluated the synergistic antiangiogenesis, antiadipogenic and antilipogenic efficacy of standardized rebaudioside A, sativoside, and theasaponin E1 formulations (RASE1) in vitro in human umbilical vein endothelial cells (HUVECs), 3T3-L1 preadipocytes respectively, and in vivo using a high-fat and carbohydrate diet-induced obesity mouse model. Orlistat was used as a positive control, while untreated cells and animals were normal controls (NCs). Adipose tissue, liver, and blood were analyzed after dissection. Extracted stevia compounds and green tea seed saponin E1 exhibited pronounced antiobesity effects when combined. RASE1 inhibited HUVEC proliferation and tube formation by suppressing VEGFR2, NF-κB, PIK3, and-catenin beta-1 expression levels. RASE1 inhibited 3T3-L1 adipocyte differentiation and lipid accumulation by downregulating adipogenesis- and lipogenesis-promoting genes. RASE1 oral administration reduced mouse body and body fat pad weight and blood cholesterol, TG, ALT, AST, glucose, insulin, and adipokine levels. RASE1 suppressed adipogenic and lipid metabolism gene expression in mouse adipose and liver tissues and enhanced AMP-activated protein kinase levels in liver and adipose tissues and in serum adiponectin. RASE1 suppressed the NF-κB pathway and proinflammatory cytokines IL-10, IL-6, and TNF-α levels in mice which involve inflammation and progression of obesity. The overall results indicate RASE1 is a potential therapeutic formulation and functional food for treating or preventing obesity and inflammation.
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Productos Biológicos/uso terapéutico , Inflamación/tratamiento farmacológico , Obesidad/tratamiento farmacológico , Células 3T3-L1 , Adipocitos/efectos de los fármacos , Adipocitos/metabolismo , Adipogénesis/efectos de los fármacos , Adipogénesis/genética , Inhibidores de la Angiogénesis/uso terapéutico , Animales , Productos Biológicos/administración & dosificación , Productos Biológicos/toxicidad , Modelos Animales de Enfermedad , Diterpenos de Tipo Kaurano/administración & dosificación , Composición de Medicamentos , Sinergismo Farmacológico , Femenino , Glucósidos/administración & dosificación , Células Endoteliales de la Vena Umbilical Humana , Humanos , Inflamación/metabolismo , Metabolismo de los Lípidos/efectos de los fármacos , Lipogénesis/efectos de los fármacos , Lipogénesis/genética , Lipólisis/efectos de los fármacos , Ratones , Ratones Endogámicos ICR , Obesidad/genética , Obesidad/metabolismo , Ácido Oleanólico/administración & dosificación , Ácido Oleanólico/análogos & derivados , Fitoterapia , ARN Mensajero/genética , ARN Mensajero/metabolismo , Saponinas/administración & dosificación , Transducción de Señal/efectos de los fármacos , Stevia/química , Té/químicaRESUMEN
Extraction and exploration of petroleum hydrocarbons (PHs) to satisfy the rising world population's fossil fuel demand is playing havoc with human beings and other life forms by contaminating the ecosystem, particularly the soil. In the current review, we highlighted the sources of PHs contamination, factors affecting the PHs accumulation in soil, mechanisms of uptake, translocation and potential toxic effects of PHs on plants. In plants, PHs reduce the seed germination andnutrients translocation, and induce oxidative stress, disturb the plant metabolic activity and inhibit the plant physiology and morphology that ultimately reduce plant yield. Moreover, the defense strategy in plants to mitigate the PHs toxicity and other potential remediation techniques, including the use of organic manure, compost, plant hormones, and biochar, and application of microbe-assisted remediation, and phytoremediation are also discussed in the current review. These remediation strategies not only help to remediate PHs pollutionin the soil rhizosphere but also enhance the morphological and physiological attributes of plant and results to improve crop yield under PHs contaminated soils. This review aims to provide significant information on ecological importance of PHs stress in various interdisciplinary investigations and critical remediation techniques to mitigate the contamination of PHs in agricultural soils.
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Petróleo , Contaminantes del Suelo , Biodegradación Ambiental , Ecosistema , Humanos , Hidrocarburos/toxicidad , Petróleo/toxicidad , Suelo , Microbiología del Suelo , Contaminantes del Suelo/análisis , Contaminantes del Suelo/toxicidadRESUMEN
Lead (Pb) is considered an important environmental contaminant due to its considerable toxicity to living organisms. It can enter and accumulate in plant tissues and become part of the food chain. In the present study, individual and combined effects of Bacillus sp. MN-54 and phosphorus (P) on maize growth and physiology were evaluated in Pb-contaminated soil. A pristine soil was artificially contaminated with two levels of Pb (i.e., 250 and 500 mg kg-1 dry soil) and was transferred to plastic pots. Bacillus sp. MN-54 treated and untreated maize (DK-6714) seeds were planted in pots. Recommended doses of nutrients (N and K) were applied in each pot while P was applied in selective pots. Results showed that Pb stress hampered the maize growth and physiological attributes in a concentration-dependent manner, and significant reductions in seedling emergence, shoot and root lengths, fresh and dry biomasses, leaf area, chlorophyll content, rate of photosynthesis, and stomatal conductance were recorded compared with control. Application of Bacillus sp. MN-54 or P particularly in combination significantly reduced the toxic effects of Pb on maize. At higher Pb level (500 mg kg-1), the combined application effectively reduced Pb uptake up to 42.4% and 50% by shoots, 30.8% and 33.9% by roots, and 18.4% and 26.2% in available Pb content in soil after 45 days and 90 days, respectively compared with that of control. Moreover, the use of Bacillus sp. MN-54 significantly improved the P uptake by maize plants by 44.4% as compared with that of control. Our findings suggest that the combined use of Bacillus sp. MN-54 and P could be effective and helpful in improving plant growth and Pb immobilization in Pb-contaminated soil.
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Bacillus , Contaminantes del Suelo , Biodegradación Ambiental , Plomo , Manganeso , Fósforo , Raíces de Plantas/química , Radioisótopos , Suelo , Contaminantes del Suelo/análisis , Zea maysRESUMEN
Alzheimer's disease (AD) is the most frequent type of dementia affecting memory, thinking and behaviour. The major hallmark of the disease is pathological neurodegeneration due to abnormal aggregation of Amyloid beta (Aß) peptides generated by ß- and γ-secretases via amyloidogenic pathway. Purpose of the current study was to evaluate the effects of theasaponin E1 on the inhibition of Aß producing ß-, γ-secretases (BACE1, PS1 and NCT) and acetylcholinesterase and activation of the non-amyloidogenic APP processing α-secretase (ADAM10). Additionally, theasaponin E1 effects on Aß degrading and clearing proteins neprilysin and insulin degrading enzyme (IDE). The effect of theasaponin E1 on these crucial enzymes was investigated by RT-PCR, ELISA, western blotting and fluorometric assays using mouse neuroblastoma cells (SweAPP N2a). theasaponin E1 was extracted and purified from green tea seed extract via HPLC, and N2a cells were treated with different concentrations for 24 h. Gene and protein expression in the cells were measured to determine the effects of activation and/or inhibition of theasaponin E1 on ß- and γ-secretases, neprilysin and IDE. Results demonstrated that theasaponin E1 significantly reduced Aß concentration by activation of the α-secretase and neprilysin. The activities of ß- and γ-secretase were reduced in a dose-dependent manner due to downregulation of BACE1, presenilin, and nicastrin. Similarly, theasaponin E1 significantly reduced the activity of acetylcholinesterase. Overall, from the results it is concluded that green tea seed extracted saponin E1 possess therapeutic significance as a neuroprotective natural product recommended for the treatment of Alzheimer's disease.
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Camellia sinensis/química , Regulación de la Expresión Génica/efectos de los fármacos , Neuronas/efectos de los fármacos , Fármacos Neuroprotectores/farmacología , Ácido Oleanólico/análogos & derivados , Saponinas/farmacología , Proteína ADAM10/genética , Proteína ADAM10/metabolismo , Acetilcolinesterasa/genética , Acetilcolinesterasa/metabolismo , Secretasas de la Proteína Precursora del Amiloide/antagonistas & inhibidores , Secretasas de la Proteína Precursora del Amiloide/genética , Secretasas de la Proteína Precursora del Amiloide/metabolismo , Péptidos beta-Amiloides/antagonistas & inhibidores , Péptidos beta-Amiloides/genética , Péptidos beta-Amiloides/metabolismo , Animales , Ácido Aspártico Endopeptidasas/antagonistas & inhibidores , Ácido Aspártico Endopeptidasas/genética , Ácido Aspártico Endopeptidasas/metabolismo , Línea Celular Tumoral , Relación Dosis-Respuesta a Droga , Insulisina/antagonistas & inhibidores , Insulisina/genética , Insulisina/metabolismo , Glicoproteínas de Membrana/antagonistas & inhibidores , Glicoproteínas de Membrana/genética , Glicoproteínas de Membrana/metabolismo , Proteínas de la Membrana/agonistas , Proteínas de la Membrana/genética , Proteínas de la Membrana/metabolismo , Ratones , Neprilisina/antagonistas & inhibidores , Neprilisina/genética , Neprilisina/metabolismo , Neuronas/metabolismo , Neuronas/patología , Fármacos Neuroprotectores/aislamiento & purificación , Ácido Oleanólico/aislamiento & purificación , Ácido Oleanólico/farmacología , Extractos Vegetales/química , Presenilinas/antagonistas & inhibidores , Presenilinas/genética , Presenilinas/metabolismo , Saponinas/aislamiento & purificación , Semillas/química , Té/químicaRESUMEN
BACKGROUND: Obesity is a risk factor for many diseases including diabetes, cancer, arthritis, and cardiovascular diseases. Angiogenesis nourishes adipose tissues and contributes to obesity; it can be prevented by suppressing the expression of associated signaling molecules. Natural products have garnered attention owing to their safety and efficacy in treating several diseases, including obesity. METHODS: Crude Microcystins were extracted from the blooming Microcystis aeruginosa under stress conditions, by ultrasonication following by solvent extraction. The microcystin extract was evaluated for its potential of inhibiting angiogenesis and adipogenesis. The antiangiogenic activity of the microcystins extract was investigated using human umbilical vein endothelial cells (HUVECs), and its anti-obesity activity was determined in vitro by quantification of the accumulated lipids in mouse 3 T3-L1 cells via Oil Red O staining method. RESULTS: The microcystin extract suppressed HUVECs proliferation and tubes formation in Matrigel in a dose-dependent manner. RT-PCR analysis revealed the downregulation of the mRNA expression of angiogenesis-related signaling molecules, such as PI3K, ß-catenin, vascular endothelial growth factor receptor-2 (VEGFR-2), vascular endothelial-cadherin, Akt1, and NF-κB. Additionally, it inhibited the differentiation of premature 3 T3 cells and lipid accumulation in a dose-dependent manner. It suppressed adipogenesis and lipogenesis by reducing the expression level of peroxisome proliferator-activated receptor γ, CCAAT/enhancer binding protein α, and sterol regulatory element-binding protein. CONCLUSIONS: Crude microcystin exerts anti-angiogenic and anti-obesity effects due to the inhibitory effects on the genes expression of associated signaling molecules and transcriptional factors.
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Adipogénesis/efectos de los fármacos , Inhibidores de la Angiogénesis/farmacología , Fármacos Antiobesidad/farmacología , Microcistinas/farmacología , Microcystis/química , Células 3T3-L1 , Adipocitos/efectos de los fármacos , Adipocitos/metabolismo , Animales , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Células Endoteliales de la Vena Umbilical Humana , Humanos , Lipogénesis/efectos de los fármacos , Lipogénesis/genética , Ratones , Neovascularización Patológica/metabolismoRESUMEN
Cornus kousa the Korean dogwood has been traditionally used in East Asia as therapeutic traditional medicine however biological activities of Cornus kousa have not been investigated previously. The aim of the present study was to evaluate anti-obesity activities coupled with anti-angiogenic activities of anthocyanins rich fraction of ethanolic leaf extract of Cornus kousa (ELECk) in HUVECs and 3T3- L1 cells. Dried plants leaves were extracted with 70% ethanol and anthocyanin fraction (AnT Fr) was obtained by eluting the ethanolic extract through non-polar macroporous resin and further purification by HPLC. Antiangiogenic activities were determined by antiproliferative effect of AnT Fr on HUVECs. In the presence of various concentrations of AnT Fr, 3T3-L1 preadipocytes were induced to differentiate. Lipid accumulation in differentiated adipocytes were quantified by Oil-Red O staining. AnT Fr significantly suppressed angiogenesis by inhibiting proliferation and tube formation of HUVECs via downregulating VEGRF 2, PI3K, ß-catenin, NF-kB, and Akt1 in a dose dependent manner. AnT Fr inhibited lipid accumulation by down-regulating adipogenesis and lipogenesis promoting signaling proteins, PPARγ, CCAAT, C/EBPα, aP2, FAS, and LPL, however enhanced AMPK activation to p-AMPK in 3T3 cells quantified and expressed by western blotting. AnT Fr inhibit lipid accumulation by regulating adipogenesis and lipogenesis related genes and signaling proteins. The anti-obesity activities exerted by Cornus kousa are associated with antiangiogenic activities of anthocyanins rich fraction of Cornus kousa. Hence the presence of bioactive anthocyanins, Cornus kosa, is a good candidate for nutraceutical and pharmaceutical formulation for treating or controlling obesity.
Asunto(s)
Adipogénesis/efectos de los fármacos , Antocianinas/farmacología , Cornus/química , Lipogénesis/efectos de los fármacos , Obesidad/tratamiento farmacológico , Extractos Vegetales/farmacología , Animales , Antocianinas/aislamiento & purificación , Regulación hacia Abajo/efectos de los fármacos , Células Endoteliales de la Vena Umbilical Humana , Humanos , Ratones , Células 3T3 NIH , Extractos Vegetales/aislamiento & purificaciónRESUMEN
Bacteria are one of the major causes of severe infections and diseases of plants and animals. Salmonella are crucially important due to infection in poultry leading to huge economical loses. Due to high cost and microbial resistance to the currently available chemical antibiotics, demand of screening natural products with antibiotics effects is increased. Plants are rich sources of natural bioactive compounds with antibiotic effects. Saponins are natural compounds of plant sources having a diverse range of applications. In present study we investigated the in vitro and in vivo antibacterial activities of green tea seed extracted saponins. Green tea seeds crude extract was prepared in 70% ethanol by continuous reflux in heating mantel for 5 hours. Crude saponins were extracted from the crude ethanolic extract of green tea seed by column chromatography using macroporous resin (D101). Saponin mixture in fraction 1 (Fr1) was obtained from crude saponins extract via column chromatography. Fr2 and Fr3 were isolated from saponins mixture by preparative HPLC. Antibacterial activities of the isolated saponins fractions were investigated against Escherichia coli (ATCC 25922), Streptococcus aureus (ATCC 12600), and six serovars of Salmonella. In vitro antibacterial activities were determined by disc-diffusion method and growth inhibition in liquid culture using 96-well plate. Results showed that the green tea isolated saponins fractions possess antibacterial effects in the following order Fr1>Fr2>Fr3. Antibacterial mechanism of saponins was elucidated by cell wall and membrane damaging potential of saponins determined by measuring AKP and soluble proteins levels. Fr1 was further used for in vivo antibacterial activities. Five-week grown chickens were selected for in vivo work, divided into three groups as control, infected, and treatment groups. Infected and treatment groups chickens were infected with bacteria and only treatment group chickens were treated with saponins. The qRT- PCR analysis of the blood and feces samples of the different groups' animals shows the presence of bacteria only in infected group while reduced expression levels of the bacterial pathogens were found in the samples of treatment group. Our results demonstrated that the green tea seed saponins used in this study possess strong antibacterial activities.
RESUMEN
Improper decisions concerning animal carcass disposal sites pose grave threats to environmental biosecurity. However, only a few studies have focused on the effects of different land-use types on the composition of carcass-derived pollutants and microbial responses to the disturbances. This study was conducted using soil microcosms with minced pork built from arable land and forest soils for 5 weeks. To compare the risk induced from different land-use types by carcass burial, the soil properties, the microbial community, and multiple-antibiotic-resistant bacteria were evaluated for microcosm containing 0, 1.5 and 7.5 g of minced pork. The abiotic properties, including pH, organic carbon, nitrogen and phosphorus compounds, significantly increased, regardless of the land-use types and applied load masses. The microbial diversity indices of the forest soil were reduced, whereas those of the arable land remained relatively stable. The disturbances produced from carcass-derived pollutants altered the bacterial community structures differently for the different land-use types. The treatment increased multiple-antibiotic-resistant bacteria in the both soil samples, although the increase in the forest soil was significantly less compared to the arable land soils.
Asunto(s)
Bosques , Contaminantes del Suelo/análisis , Suelo/química , Porcinos , Animales , Carbono/análisis , Recuento de Colonia Microbiana , Concentración de Iones de Hidrógeno , Nitrógeno/análisis , Fósforo/análisis , Carne Roja , Medición de Riesgo , Microbiología del SueloRESUMEN
The current study aimed to develop novel pH independent microparticles loaded with ropinirole (ROP) for sustained drug release. Eudragit RS 100 was used as release retardant and microparticles were fabricated by oil-in-oil emulsion solvent evaporation method. A three-factor three-level Box-Behnken design using Design-Expert software was employed to optimize formulation variables. Ropinirole loaded microparticles were evaluated with respect to morphology, particle size, encapsulation efficiency, and in vitro release profile. Optical microscopy and SEM micrographs indicated spherical shape with smooth surface and well-defined boundary. The particle size was in the range of 98.86 to 236.29 µm, being significantly increased with increasing polymer concentration. Higher polymer load also increased the thickness of internal polymer network, which led to reduced drug loss and higher entrapment efficiency (89%). The cumulative in vitro release was found to be in the range of 54.96 to 99.36% during the release studies (12 h) following zero order release kinetics and non-Fickian diffusion pattern. The developed microparticles have the potential to sustain the release of ropinirole, which may lead to a reduction in its adverse effects and improved management of Parkinson's disease.