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To explore the combined effects of exercise and melatonin supplement against the challenges of isoproterenol-induced cardiac oxidative stress and injury in rats., the expression of peroxisome proliferator-activated receptor gamma co-activator-1α (PGC-1α), mitochondrial biogenesis, and adenosine triphosphate (ATP) was up-regulated in cardiac muscle in normal rats and in a melatonin and exercise regimented group. Cardiac injury was induced by two subcutaneous injections of isoproterenol in the rats. The combination of exercise and melatonin supplement successfully counteracted the isoproterenol-induced cardiac injury, which is reflected by the improved hemodynamic parameters, reduction in oxidative stress markers, and cardiac injury serum markers (cardiac troponin-I and creatine kinase-MB). The cardiac tissue level of ATP, expression of PGC-1α and mitochondrial biogenesis-related genes, mitochondrial membrane potential, and the activities of typical antioxidants (glutathione, superoxide dismutase) were preserved, whereas the levels of reactive oxygen species, lipid peroxidation, and inflammatory cytokines were suppressed in the melatonin and exercise regimented (MEI) group compared to the group treated with isoproterenol alone. Furthermore, the expression of endoplasmic reticular stress- and apoptosis-related proteins (Bax, Bcl2, and caspase-3) was also effectively suppressed in the MEI group. Therefore, the present study suggests that melatonin supplement in combination with exercise prevents cardiac injury, possibly through the preservation of mitochondrial function and inhibition of oxidative stress in rats.
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Fourteen flavones (1-14) including twelve polymethoxylated flavones, two A-type proanthocyanidins (oligomeric flavonoids) (15, 16), one benzoyl glucoside (17), one triterpenoid (18), and one phenylpropanoid (19) were isolated from the leaves of the South Asian medicinal plant Ceriscoides campanulata (Roxb.) Tirveng (Rubiaceae). The structures of the compounds were identified based on their spectroscopic and spectrometric data and in comparison with literature data. Isolated compounds were tested in vitro against inflammatory enzymes (COX-2, iNOS), pro-inflammatory cytokines (IL-1ß, IL-6, TNF-α), esophageal squamous carcinoma cell line (TE13), and carbohydrate digestion enzymes (α-amylase, α-glucosidase). Proanthocyanidins 15 and 16 significantly attenuated the LPS-induced inflammatory response of COX-2, iNOS, IL-1ß, IL-6, TNF-α in RAW 264.7 cells. Proanthocyanidins also satisfactorily inhibited the regrowth (64%), migration (51%), and formation of tumor-spheres (48%) in ESCC cell line TE13 at 50% toxic concentration. Compounds 15 and 16 showed the most potent effect against mammalian α-amylase (IC50 8.4 ± 0.3 µM and 3.5 ± 0.0 µM, respectively) compared to reference standard acarbose (IC50 5.9 ± 0.1 µM). As yeast α-glucosidase inhibitors, compounds 15 and 16 also displayed significant activities (IC50 6.2 ± 0.3 and 4.7 ± 0.1 µM, respectively), while compounds 1-6 displayed weaker α-glucosidase inhibitory activities, ranging from 49 to 142 µM, compared to acarbose (IC50 665 ± 42 µM). In an anticholinesterase assay, compounds 1, 2, 6 (IC50 51 ± 2, 53 ± 7, 64 ± 5 µM, respectively), and 4 (IC50 44 ± 1 µM) showed moderate inhibitory activities against acetylcholinesterase and butyrylcholinesterase, respectively. Furthermore, molecular docking and molecular dynamic simulation analyses of compounds 15 and 16 were performed against human pancreatic α-amylase and human lysosomal acid α-glucosidase to elucidate the interactions of these compounds in the respective enzymes' active sites.
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Carcinoma de Células Escamosas , Diabetes Mellitus , Neoplasias Esofágicas , Proantocianidinas , Rubiaceae , Acetilcolinesterase/metabolismo , Animais , Butirilcolinesterase/análise , Butirilcolinesterase/metabolismo , Simulação por Computador , Células Epiteliais/metabolismo , Neoplasias Esofágicas/tratamento farmacológico , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Humanos , Inflamação , Mamíferos/metabolismo , Simulação de Acoplamento Molecular , Estrutura Molecular , Folhas de Planta/química , Proantocianidinas/análise , Proantocianidinas/farmacologia , alfa-Amilases , alfa-Glucosidases/metabolismoRESUMO
Many Bangladeshi medicinal plants have been used to treat Alzheimer's disease and other neurodegenerative diseases. In the present study, the anticholinesterase effects of eight selected Bangladeshi medicinal plant species were investigated. Species were selected based on the traditional uses against CNS-related diseases. Extracts were prepared using a gentle cold extraction method. In vitro cholinesterase inhibitory effects were measured by Ellman's method in 96-well microplates. Blumea lacera (Compositae) and Cyclea barbata (Menispermaceae) were found to have the highest acetylcholinesterase inhibitory (IC50, 150 ± 11 and 176 ± 14 µg/mL, respectively) and butyrylcholinesterase inhibitory effect (IC50, 297 ± 13 and 124 ± 2 µg/mL, respectively). Cyclea barbata demonstrated competitive inhibition, where Blumea lacera showed an uncompetitive inhibition mode for acetylcholinesterase. Smilax guianensis (Smilacaceae) and Byttneria pilosa (Malvaceae) were also found to show moderate AChE inhibition (IC50, 205 ± 31 and 221 ± 2 µg/mL, respectively), although no significant BChE inhibitory effect was observed for extracts from these plant species. Among others, Thunbergia grandiflora (Acanthaceae) and Mikania micrantha (Compositae) were found to display noticeable AChE (IC50, 252 ± 22 µg/mL) and BChE (IC50, 314 ± 15 µg/mL) inhibitory effects, respectively. Molecular docking experiment suggested that compounds 5-hydroxy-3,6,7,3',4'-pentamethoxyflavone (BL4) and kaempferol-3-O-α-L-rhamnopyranosyl-(1â¶6)-ß-D-glucopyranoside (BL5) from Blumea lacera bound stably to the binding groove of the AChE and BChE by hydrogen-bond interactions, respectively. Therefore, these compounds could be candidates for cholinesterase inhibitors. The present findings demonstrated that Blumea lacera and Cyclea barbata are interesting objects for further studies aiming at future therapeutics for Alzheimer's disease.
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Mounting evidence support the potential benefits of functional foods or nutraceuticals for human health and diseases. Black cumin (Nigella sativa L.), a highly valued nutraceutical herb with a wide array of health benefits, has attracted growing interest from health-conscious individuals, the scientific community, and pharmaceutical industries. The pleiotropic pharmacological effects of black cumin, and its main bioactive component thymoquinone (TQ), have been manifested by their ability to attenuate oxidative stress and inflammation, and to promote immunity, cell survival, and energy metabolism, which underlie diverse health benefits, including protection against metabolic, cardiovascular, digestive, hepatic, renal, respiratory, reproductive, and neurological disorders, cancer, and so on. Furthermore, black cumin acts as an antidote, mitigating various toxicities and drug-induced side effects. Despite significant advances in pharmacological benefits, this miracle herb and its active components are still far from their clinical application. This review begins with highlighting the research trends in black cumin and revisiting phytochemical profiles. Subsequently, pharmacological attributes and health benefits of black cumin and TQ are critically reviewed. We overview molecular pharmacology to gain insight into the underlying mechanism of health benefits. Issues related to pharmacokinetic herb-drug interactions, drug delivery, and safety are also addressed. Identifying knowledge gaps, our current effort will direct future research to advance potential applications of black cumin and TQ in health and diseases.
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Nigella sativa/química , Preparações de Plantas/química , Preparações de Plantas/farmacologia , Anti-Inflamatórios/farmacocinética , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacocinética , Antioxidantes/farmacologia , Benzoquinonas/análise , Disponibilidade Biológica , Sobrevivência Celular/efeitos dos fármacos , Suplementos Nutricionais , Sistemas de Liberação de Medicamentos , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos , Metabolismo Energético , Alimento Funcional , Humanos , Imunomodulação/efeitos dos fármacos , Inflamação/terapia , Estresse Oxidativo/efeitos dos fármacos , Fitoterapia/métodos , Preparações de Plantas/farmacocinéticaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Tabebuia pallida (Lindl.) Miers (T. pallida) is a well-known native Caribbean medicinal plant. The leaves and barks of T. pallida are used as traditional medicine in the form of herbal or medicinal tea to manage cancer, fever, and pain. Moreover, extracts from the leaves of T. pallida showed anticancer activity. However, the chemical profile and mechanism of anticancer activity of T. pallida leaves (TPL), stem bark (TPSB), root bark (TPRB) and flowers (TPF) remain unexplored. AIM OF THE STUDY: The present study was designed to explore the regulation of apoptosis by T. pallida using Ehrlich Ascites Carcinoma (EAC) cultured cells and an EAC mouse model. LC-ESI-MS/MS was used for compositional analysis of T. pallida extracts. MATERIALS AND METHODS: Dried and powdered TPL, TPSB, TPRB and TPF were extracted with 80% methanol. Using cultured EAC cells and EAC-bearing mice with and without these extracts, anticancer activities were studied by assessing cytotoxicity and tumor cell growth inhibition, changes in life span of mice, and hematological and biochemical parameters. Apoptosis was analyzed by microscopy and expression of selected apoptosis-related genes (Bcl-2, Bcl-xL, NFκ-B, PARP-1, p53, Bax, caspase-3 and -8) using RT-PCR. LC-ESI-MS analysis was performed to identify the major compounds from active extracts. Computer aided analyses was undertaken to sort out the best-fit phytoconstituent of total ten isolated compounds of this plant for antioxidant and anticancer activity. RESULTS: In EAC mice compared with untreated controls, the TPL extract exhibited the highest cancer cell toxicity with significant tumor cell growth inhibition (p < 0.001), reduced ascites by body weight (p < 0.01), increased the life span (p < 0.001), normalized blood parameters (RBC/WBC counts), and increased the levels of superoxide dismutase and catalase. TPL-treated EAC cells showed increased apoptotic characteristics of membrane blebbing, chromatin condensation and nuclear fragmentation, and caspase-3 activation, compared with untreated EAC cells. Moreover, annexin V-FITC and propidium iodide signals were greatly enhanced in response to TPL treatment, indicating apoptosis induction. Pro- and anti-apoptotic signaling after TPL treatment demonstrated up-regulated p53, Bax and PARP-1, and down-regulated NFκ-B, Bcl-2 and Bcl-xL expression, suggesting that TPL shifts the balance of pro- and anti-apoptotic genes towards cell death. LC-ESI-MS data of TPL showed a mixture of glycosides, lapachol, and quercetin antioxidant and its derivatives that were significantly linked to cancer cell targets. The compound, pelargonidin-3-O-glucoside was found to be most effective in computer aided models. CONCLUSIONS: In conclusion, the TPL extract of T. pallida possesses significant anticancer activity. The tumor suppressive mechanism is due to apoptosis induced by activation of antioxidant enzymes and caspases and mediated by a change in the balance of pro- and anti-apoptotic genes that promotes cell death.
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Antineoplásicos/uso terapêutico , Apoptose/efeitos dos fármacos , Carcinoma/tratamento farmacológico , Fitoterapia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Animais , Antineoplásicos/administração & dosagem , Antineoplásicos/efeitos adversos , Antineoplásicos/química , Caspase 3/genética , Caspase 3/metabolismo , Caspase 8/genética , Caspase 8/metabolismo , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Humanos , Masculino , Camundongos , Neoplasias Experimentais , Extratos Vegetais/administração & dosagem , Extratos Vegetais/efeitos adversos , Extratos Vegetais/químicaRESUMO
BACKGROUND AND AIMS: Inflammation and calcification are major factors responsible for degeneration of bioprosthetic valve and other substitute heart valve implantations. The objective of this study was to evaluate the anti-inflammatory and anti-calcification effects of Entelon150® (consisting of grape-seed extract) in a beagle dog model of intravascular bovine pericardium implantation. METHODS: In total, 8 healthy male beagle dogs were implanted with a bovine pericardium bilaterally in the external jugular veins and divided into two groups. Animals in the Entelon150® group (n = 4) were treated with 150 mg of Entelon150® twice daily for six weeks after surgery. The negative control (NC) group (n = 4) was treated with 5 ml of saline using the same method. After six weeks, we measured the calcium content, performed histological examination, and performed molecular analysis. RESULTS: The calcium content of implanted tissue in the Entelon150® group (0.56±0.14 mg/g) was significantly lower than that in the NC group (1.48±0.57 mg/g) (p < 0.05). Histopathological examination showed that infiltration of chronic inflammatory cells, such as fibroblasts and macrophages, occurred around the graft in all groups; however, the inflammation level of the implanted tissue in the Entelon150® group was s lower than that in the NC group. Both immunohistochemical and western blot analyses revealed that bone morphogenetic protein 2 expression was significantly attenuated in the Entelon150® group. CONCLUSIONS: Our results indicate that Entelon150® significantly attenuates post-implantation inflammation and degenerative calcification of the bovine pericardium in dogs. Therefore, Entelon150® may increase the longevity of the bovine pericardium after intravascular implantation.
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Anti-Inflamatórios/uso terapêutico , Calcinose/tratamento farmacológico , Extrato de Sementes de Uva/uso terapêutico , Complicações Pós-Operatórias/tratamento farmacológico , Substituição da Valva Aórtica Transcateter/métodos , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/farmacologia , Bioprótese , Calcinose/etiologia , Bovinos , Cães , Fibroblastos/efeitos dos fármacos , Extrato de Sementes de Uva/administração & dosagem , Extrato de Sementes de Uva/farmacologia , Próteses Valvulares Cardíacas , Macrófagos/efeitos dos fármacos , Masculino , Pericárdio/transplante , Substituição da Valva Aórtica Transcateter/efeitos adversosRESUMO
Honey and its compounds are drawing attention as an effective natural therapy because of its ability to attenuate acute inflammation through enhancing immune response. Several studies have proved its potential healing capability against numerous chronic diseases/conditions, including pulmonary disorders, cardiac disorders, diabetes, hypertension, autophagy dysfunction, bacterial, and fungal infections. More importantly, honey has proved its virucidal effect on several enveloped viruses such as HIV, influenza virus, herpes simplex, and varicella-zoster virus. Honey may be beneficial for patients with COVID-19 which is caused by an enveloped virus SARS-CoV-2 by boosting the host immune system, improving comorbid conditions, and antiviral activities. Moreover, a clinical trial of honey on COVID-19 patients is currently undergoing. In this review, we have tried to summarize the potential benefits of honey and its ingredients in the context of antimicrobial activities, some chronic diseases, and the host immune system. Thus, we have attempted to establish a relationship with honey for the treatment of COVID-19. This review will be helpful to reconsider the insights into the possible potential therapeutic effects of honey in the context of the COVID-19 pandemic. However, the effects of honey on SARS-CoV-2 replication and/or host immune system need to be further investigated by in vitro and in vivo studies.
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OBJECTIVE: The purpose of this study was to evaluate the clinical outcome of surgical decompression and rehabilitation therapy in dogs with thoracolumbar intervertebral disk herniation (IVDH). MATERIALS AND METHODS: After surgery, physiotherapeutic rehabilitation was performed by a combination of electrotherapy, infrared therapy, training for standing, deep tendon reflex, and aquatic treadmill exercise. A total of 186 dogs were selected from the hospital records and included in two groups: the rehabilitated group (RG, n = 96) and non-rehabilitated group (NRG, n = 90). Dogs in each group were subdivided into three groups based on a pre-operative clinical severity grading system and those in grades 2-4 were included in this study. Post-operative neurologic functions, unassisted standing, walking, and the success rate of both groups were evaluated and compared. RESULTS: Overall, 86.46% (83/96) of dogs had a successful neurologic outcome in the RG group, which was significantly (p < 0.01) higher than the NRG group 52.22% (47/90). Interestingly, the success rate differed when the preoperative grading system was considered. The success rates of grades 2, 3, and 4 were 97.14% (34/35), 97.33% (42/45), and 43.75% (7/16), respectively, in the rehabilitated groups, whereas in the non-rehabilitated groups, success rates were 82.35% (28/34), 51.85% (14/27), and 17.24% (5/29), respectively. The differences in success rates among the groups according to grading were 14.79%, 41.48%, and 26.51%, respectively, indicating that the proposed rehabilitation therapy is remarkably advantageous for increasing the success rate. CONCLUSION: Rehabilitation therapy after surgical decompression of thoracolumbar IVDH improves neurologic functions and increases the success rate, especially when the preoperative pathological condition is severe.
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The world is hungry for energy. Plant oils in the form of triacylglycerol (TAG) are one of the most reduced storage forms of carbon found in nature and hence represent an excellent source of energy. The myriad of applications for plant oils range across foods, feeds, biofuels, and chemical feedstocks as a unique substitute for petroleum derivatives. Traditionally, plant oils are sourced either from oilseeds or tissues surrounding the seed (mesocarp). Most vegetative tissues, such as leaves and stems, however, accumulate relatively low levels of TAG. Since non-seed tissues constitute the majority of the plant biomass, metabolic engineering to improve their low-intrinsic TAG-biosynthetic capacity has recently attracted significant attention as a novel, sustainable and potentially high-yielding oil production platform. While initial attempts predominantly targeted single genes, recent combinatorial metabolic engineering strategies have focused on the simultaneous optimization of oil synthesis, packaging and degradation pathways (i.e., 'push, pull, package and protect'). This holistic approach has resulted in dramatic, seed-like TAG levels in vegetative tissues. With the first proof of concept hurdle addressed, new challenges and opportunities emerge, including engineering fatty acid profile, translation into agronomic crops, extraction, and downstream processing to deliver accessible and sustainable bioenergy.
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Biomassa , Engenharia Metabólica , Óleos de Plantas/metabolismo , Triglicerídeos/metabolismoRESUMO
BACKGROUND: Opuntia ficus-indica var. saboten (OFIS) is used widely in Korea to treat constipation due to its diuretic effects and its enhancement of bowel function and appetite. However, its safety has not yet been established. The aim of this study was to evaluate the repeated oral toxicity and genotoxicity of OFIS extract (OE). METHODS: White female and male Sprague Dawley rats (n = 6) were divided into 4 groups, and OE was administered to them orally (0, 500, 1000, and 2000 mg/kg/day, respectively) for one week. The Ames test, the chromosomal aberration assay, and the mammalian micronucleus test were performed to determine the OE genotoxicity. The Ames test was conducted using Salmonella typhimurium (S. typhimurium) strains TA100, TA1535, TA98, and TA153 and Escherichia coli (E. coli) WP2 urvA, and Chinese hamster lung (CHL) cells were used for the chromosomal aberration assay. The mammalian micronucleus test was performed using mouse bone marrow cells. RESULTS: This study revealed that OE administration did not alter the normal rat behavior, body weight gain, and food and water consumption with respect to the normal controls. In addition, there were no toxic effects observed during the ophthalmological test. The biochemical hematological and serum values as well as urinalysis parameters and organ weights were all similar to those of the normal control group. In addition, no mutagenicity effects from the OE were found in S. typhimurium or E. coli with or without S9 activation according to the Ames test. The OE did not significantly alter the number of structural aberrations in the CHL cells in the presence or absence of S9 activation. The oral administration of OE also caused no significant increase in the number of micronucleated polychromatic erythrocytes or in the mean ratio of polychromatic to total erythrocytes. CONCLUSIONS: In conclusion, OE could be considered as a reliable and safe herbal medicine or functional food since no toxicity was found under the conditions of this study.
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Mutagênicos/toxicidade , Opuntia , Extratos Vegetais/toxicidade , Administração Oral , Animais , Células da Medula Óssea/efeitos dos fármacos , Células Cultivadas , Aberrações Cromossômicas/induzido quimicamente , Ingestão de Alimentos/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Feminino , Masculino , Camundongos , Testes para Micronúcleos , Testes de Mutagenicidade , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Caules de Planta/química , Ratos , Ratos Sprague-Dawley , Salmonella typhimurium/efeitos dos fármacosRESUMO
The aim of this study was to investigate the chondroprotective effect of a standardized extract (KBH-JP-040) of the Korean traditional herbs Kalopanax pictus Castor-Aralia, Hericium erinaceus (Bull.) Persoon, and Astragalus membranaceus Schischkin on in vivo and in vitro osteoarthritis (OA) models. Cultured rat chondrocytes were pre-treated with KBH-JP-040 (50, 100 and 200 µg/mL) for 1 h, then recombinant human IL-1α (rhIL-1α) for 24 h. For the in vivo model, rabbits (n = 60) were equally divided into experimental groups: normal control (NC), a collagenase-induced OA group, and OA groups treated with KBH-JP-040 (75, 100, and 150 mg/kg body weight) and celecoxib (Cx, 100 mg/kg) orally for 28 days. Treatment with KBH-JP-040 significantly attenuated inflammatory cytokines and matrix metalloproteinases (MMPs), suppressed the expression of IκBα, NF-κB, and JNK/p38 mitogen-activated protein (MAP) kinase, and upregulated aggrecan and collagen type-II expression in rhIL-1α-stimulated chondrocytes. Furthermore, the serum and synovial levels of inflammatory cytokines of rabbits also decreased in the treatment groups when compared with the OA group. Improved magnetic resonance imaging and histopathological findings further confirmed the therapeutic efficacy of KBH-JP-040 against OA. In conclusion, these results indicate that KBH-JP-040 possesses chondroprotective effects, suppressing inflammation and MMPs, and downregulating IκBα, NF-κB, and JNK/p38 MAP kinase-signaling pathways. This might be a potential therapeutic candidate for OA treatment.
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Anti-Inflamatórios/farmacologia , Artrite Experimental/prevenção & controle , Astragalus propinquus , Basidiomycota , Condrócitos/efeitos dos fármacos , Articulações/efeitos dos fármacos , Kalopanax , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Artrite Experimental/induzido quimicamente , Artrite Experimental/diagnóstico por imagem , Artrite Experimental/metabolismo , Astragalus propinquus/química , Basidiomycota/química , Celecoxib/farmacologia , Células Cultivadas , Condrócitos/metabolismo , Colágeno/metabolismo , Colagenases , Citocinas/metabolismo , Relação Dose-Resposta a Droga , Mediadores da Inflamação/metabolismo , Interleucina-1beta/farmacologia , Articulações/diagnóstico por imagem , Articulações/metabolismo , Kalopanax/química , Imageamento por Ressonância Magnética , Masculino , Metaloproteinases da Matriz/metabolismo , Fitoterapia , Extratos Vegetais/isolamento & purificação , Plantas Medicinais , Coelhos , Ratos , Ratos Sprague-Dawley , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais/efeitos dos fármacosRESUMO
CONTEXT: Salicornia europaea (Amaranthaceae) (SE) has been shown to reduce obesity, but it remains a problem as a food supplement because of its high salt content (25-35% NaCl). OBJECTIVES: This study investigated the anti-obesity effects and mechanism of action of desalted SE powder (DSP). MATERIALS AND METHODS: Sprague-Dawley rats (n = 50) were divided into a normal control group (NC), a high-fat diet (HFD)-induced obesity control group (HFD), and HFD groups co-administered DSP (250 and 500 mg/kg) or Garcinia cambogia (Clusiaceae) extract (GE, 200 mg/kg, standard control) orally each day for 12 weeks. RESULTS: The body weight was significantly reduced by co-administration of DSP (596.51 ± 19.84 kg, 4.60% and 562.08 ± 9.74 kg, 10.10%, respectively) and GE (576.00 ± 11.29 kg, 7.88%) relative to the HFD group (625.25 ± 14.02 kg) and was accompanied by reduced abdominal fat mass, and serum lipid levels, with no effects on feed intake. To find the underlying mechanism of the anti-obesity effects, trans-ferulic acid (TFA) was identified as the main ingredient and investigated with regard to whether it attenuated adipogenesity in 3T3L-1 cells. DSP-derived TFA suppressed adipocyte differentiation and accumulation of intracellular lipids. TFA also down-regulated the adipogenesis-related gene expression of sterol regulatory element-binding protein 1, peroxisome proliferator-activated receptor γ, CCAAT/enhancer binding protein-α and fatty acid synthase. CONCLUSIONS: These findings suggest that DSP may be considered for use as a food supplement intent of controlling obesity through its antiobesity and antiadipogenic properties.
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Adipogenia/efeitos dos fármacos , Fármacos Antiobesidade/uso terapêutico , Chenopodiaceae , Ácidos Cumáricos/uso terapêutico , Obesidade/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Células 3T3-L1 , Adipogenia/fisiologia , Animais , Fármacos Antiobesidade/isolamento & purificação , Fármacos Antiobesidade/farmacologia , Peso Corporal/efeitos dos fármacos , Peso Corporal/fisiologia , Ácidos Cumáricos/isolamento & purificação , Ácidos Cumáricos/farmacologia , Relação Dose-Resposta a Droga , Masculino , Camundongos , Obesidade/metabolismo , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Ratos , Ratos Sprague-DawleyRESUMO
The opportunistic fish pathogen, Enterococcus faecalis has been reported to cause mass mortality in several fish species in different countries. The objectives of this study were to (i) identify E. faecalis from the diseased fishes through molecular techniques; (ii) assess the antibiotic susceptibility profile of E. faecalis isolates; and (iii) control disease in tilapia fish by treatment with medicinal plant extracts. A total of 48 isolates were phenotypically identified as Enterococcus species from tilapia, stinging catfish and walking catfish cultivated in several fish farms in Gazipur. Ten randomly selected isolates were identified as E. faecalis by 16S rRNA gene sequencing. Artificial infection revealed that most of the isolates caused moderate to high mortality in fishes with characteristic disease symptoms. These isolates exhibited resistance to multiple antibiotics in vitro. Bioassay revealed that organic extracts of Tamarindus indica and Emblica officinalis leaves, Allium sativum bulb, and Syzygium aromaticum bud inhibited the growth of E. faecalis. Methanol extracts of A. sativum and methanol and acetone extracts of S. aromaticum significantly reduced the mortality of fish artificially infected with E. faecalis as both preventive and therapeutic agents. This is the first report on molecular identification, and herbal control of fish pathogenic E. faecalis in Bangladesh.
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Peixes-Gato/microbiologia , Farmacorresistência Bacteriana Múltipla/genética , Enterococcus faecalis , Doenças dos Peixes , Infecções por Bactérias Gram-Positivas , Extratos Vegetais/farmacologia , Tilápia/microbiologia , Animais , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Enterococcus faecalis/genética , Enterococcus faecalis/isolamento & purificação , Enterococcus faecalis/metabolismo , Doenças dos Peixes/tratamento farmacológico , Doenças dos Peixes/genética , Doenças dos Peixes/microbiologia , Infecções por Bactérias Gram-Positivas/tratamento farmacológico , Infecções por Bactérias Gram-Positivas/genética , Infecções por Bactérias Gram-Positivas/microbiologia , Infecções por Bactérias Gram-Positivas/veterinária , Extratos Vegetais/químicaRESUMO
INTRODUCTION: The objective was to investigate the effects of melatonin and exercise on insulin resistance (IR), hypertension and fatigue syndrome in a rat model of type 2 diabetes mellitus (T2DM). MATERIALS AND METHODS: Rats were divided into 5 groups namely normal control (NC), T2DM control group (DC), diabetes plus exercise (DE), diabetes plus oral melatonin supplement (DM) and diabetes plus melatonin and exercise (DME) groups. Melatonin was administered orally 5mg/kg twice daily and 40min swimming/day 5days/week were regimented after diabetes induction. RESULTS: Blood pressure, fasting blood glucose, insulin, IR, serum leptin, lipid profiles, inflammatory cytokines, lipid peroxidation increased significantly (P<0.01) while serum adiponectin, antioxidant activities (superoxide dismutase, glutathione), exercise performance significantly decreased (P<0.001) in the DC group compared with the control group. Combined effects of exercise and melatonin ameliorated markedly hypertension, IR, biochemical alteration induced by diabetes and significantly increased exercise performance (P<0.01). The expression glucose transporter type 4 (GLUT4) mitochondrial biogenesis related proteins such as peroxisome proliferator-activated receptor gamma coactivator 1α (PGC-1 α), nuclear respiratory factor (NRFs) and mitochondrial transcription factor-A were up-regulated skeletal and cardiac muscle in the DME group. CONCLUSION: Melatonin supplementation in combination with exercise behavior may ameliorate IR, hypertension and exercise performance or fatigue possibly by improving antioxidative activities, hyperlipidemia, inflammatory cytokines via up-regulation of GLUT4, PGC-1 α and mitochondrial biogenesis in T2DM rats.
Assuntos
Diabetes Mellitus Tipo 2/terapia , Fadiga/terapia , Hipertensão/terapia , Resistência à Insulina/fisiologia , Melatonina/administração & dosagem , Condicionamento Físico Animal/fisiologia , Animais , Diabetes Mellitus Tipo 2/sangue , Diabetes Mellitus Tipo 2/complicações , Dieta Hiperlipídica/efeitos adversos , Modelos Animais de Doenças , Fadiga/sangue , Fadiga/complicações , Hipertensão/sangue , Hipertensão/complicações , Masculino , Condicionamento Físico Animal/métodos , Ratos , Ratos Sprague-DawleyRESUMO
BACKGROUND: In humans, many diseases are associated with the accumulation of free radicals. Antioxidants can scavenge free radicals and minimize their impact. Therefore, the search for naturally occurring antioxidants of plant origin is imperative. Here, we aimed to investigate the antioxidant and free radical scavenging properties of methanolic extracts from Tabebuia pallida (T. pallida) stem bark (TPSB), root bark (TPRB), leaves (TPL), and flowers (TPF). METHODS: The antioxidant and free radical scavenging activity were determined by several standard methods using spectrophotomer. Total phenolic and flavonoid contents were estimated using Folin-Ciocalteu reagent and aluminum chloride colorimetric assay methods, respectively. RESULTS: Among the extracts, TPL showed the highest total antioxidant capacity followed by TPRB, TPF, and TPSB. Based on DPPH and hydroxyl radical scavenging activity, TPL showed strong scavenging activity (91.05 ± 1.10 and 62.00 ± 0.57) with IC50 of 9.20 ± 0.28 and 46.00 ± 2.84 µg/mL, respectively when compared with standard BHT (IC50 of 7.00 ± 0.25 µg/mL) and CA (75.00 ± 0.14 µg/mL). These results suggest that TPL had the highest radical scavenging activity among the extractives that closely resembled the standard's. In lipid peroxidation inhibition assay, TPL exhibited the most potent inhibitory activity (83.18 ± 2.12 %) with IC50 of 12.00 ± 2.12 µg/mL, which closely resembled standard CA (IC50 of 10.50 ± 0.28 µg/mL). Also, the reducing capacity on ferrous ion was in the following order: TPL > TPRB > TF > TPSB. The phenolic and flavonoid contents of TPL were higher than other extractives. A positive correlation (p value <0.001) was observed between phenolic content and free radical (DPPH(·) and (·)OH) scavenging efficiencies and lipid peroxidation inhibition activity. CONCLUSION: Methanolic extract of T. pallida leaf is a potential source of natural antioxidants and serves as an effective free radical scavenger and/or inhibitor. Hence, T. pallida might be a good plant-based pharmaceutical product for several diseases caused by free radicals.
Assuntos
Antioxidantes/farmacologia , Sequestradores de Radicais Livres/farmacologia , Componentes Aéreos da Planta , Extratos Vegetais/farmacologia , Raízes de Plantas , Plantas Medicinais , Bangladesh , TabebuiaRESUMO
The objective of this study was to investigate the therapeutic efficacies of crude yam (Dioscorea batatas) powder (PY), water extract of yam (EY), and allantoin (the active constituent of yam) in streptozotocin (STZ)-induced diabetic rats with respect to glucose, insulin, glucagon-like peptide-1 (GLP-1), C-peptide, glycated hemoglobin (HbAlc), lipid metabolism, and oxidative stress. For this purpose, 50 rats were divided into five groups: normal control (NC), diabetic control (STZ), and STZ plus treatment groups (STZ + PY, STZ + EY, and STZ + allantoin). After treatment for one-month, there was a decrease in blood glucose: 385 ± 7 in STZ, 231 ± 3 in STZ + PY, 214 ± 11 in STZ + EY, and 243 ± 6 mg/dL in STZ + allantoin, respectively. There were significant statistical differences (p < 0.001) compared to STZ (100%): 60% in STZ + PY, 55% in STZ + EY, and 63% in STZ + allantoin. With groups in the same order, there were significant decreases (p < 0.001) in HbAlc (100% as 24.4 ± 0.6 ng/mL, 78%, 75%, and 77%), total cholesterol (100% as 122 ± 3 mg/dL, 70%, 67%, and 69%), and low-density lipoprotein (100% as 29 ± 1 mg/dL, 45%, 48%, and 38%). There were also significant increases (p < 0.001) in insulin (100% as 0.22 ± 0.00 ng/mL, 173%, 209%, and 177%), GLP-1 (100% as 18.4 ± 0.7 pmol/mL, 160%, 166%, and 162%), and C-peptide (100% as 2.56 ± 0.10 ng/mL, 129%, 132%, and 130%). The treatment effectively ameliorated antioxidant stress as shown by a significant decrease (p < 0.001) in malondialdehyde (100% as 7.25 ± 0.11 nmol/mL, 87%, 86%, and 85%) together with increases (p < 0.01) in superoxide dismutase (100% as 167 ± 6 IU/mL, 147%, 159%, and 145%) and reduced glutathione (100% as 167 ± 6 nmol/mL, 123%, 141%, and 140%). The results indicate that yam and allantoin have antidiabetic effects by modulating antioxidant activities, lipid profiles and by promoting the release of GLP-1, thereby improving the function of ß-cells maintaining normal insulin and glucose levels.
Assuntos
Alantoína/uso terapêutico , Glicemia/metabolismo , Diabetes Mellitus Experimental/tratamento farmacológico , Dioscorea/química , Insulina/sangue , Fitoterapia , Extratos Vegetais/uso terapêutico , Alantoína/farmacologia , Animais , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Peptídeo C/metabolismo , Diabetes Mellitus Experimental/sangue , Peptídeo 1 Semelhante ao Glucagon/sangue , Hemoglobinas Glicadas/metabolismo , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Lipoproteínas LDL/sangue , Masculino , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Ratos Sprague-Dawley , Superóxido Dismutase/metabolismoRESUMO
BACKGROUND: Ucche (Momordica charantia L. var. muricata (Willd.) Chakravarty) has been reported to possess many benefits and medicinal properties. However, the protective effect of ucche against carbon tetrachloride (CCl4) induced hepatotoxicity have not been clarified fully yet. The aim of the present study was to investigate the effects of ucche on oxidative stress and inflammation in liver of CCl4 treated rats. METHODS: Female Long Evans rats were administered with CCl4 orally (1 ml/kg) twice a week for 2 weeks and were supplemented with freshly prepared crashed ucche (10% wt/wt of diet) with powdered chaw food. Both plasma and liver tissues were analyzed for AST, ALT and ALP activities. Oxidative stress parameters were measure by determining malondialdehyde (MDA), nitric oxide (NO), advanced protein oxidation product (APOP), and reduced glutathione (GSH) concentrations and catalase activities in plasma and liver tissues. Moreover, inflammation and tissue fibrosis were confirmed by histological staining of liver tissue sections. RESULTS: Our data suggest that ucche significantly prevented CCl4-induced hepatotoxicity, indicated by both diagnostic indicators of liver damage (serum transferases activities) and histopathological analysis. Moreover, CCl4 administration induced profound elevation of reactive oxygen species (ROS) production and oxidative stress, as evidenced by increasing lipid peroxidation level and depletion of antioxidant enzymes in liver. Fresh ucche supplementation prevented the oxidative stresses and improved antioxidant enzyme function. Furthermore, fresh ucche supplementation reduced hepatic inflammatory cell infiltration, iron deposition and fibrosis in liver of CCl4 treated rats. CONCLUSION: In conclusion, these results suggested that the inhibition of CCl4-induced inflammation by ucche is due at least in part to its anti-oxidant activity and its ability to modulate the inflammation and fibrosis in liver.
Assuntos
Antioxidantes/uso terapêutico , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Suplementos Nutricionais , Cirrose Hepática/prevenção & controle , Momordica charantia , Estresse Oxidativo/efeitos dos fármacos , Fitoterapia , Animais , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Antioxidantes/farmacologia , Tetracloreto de Carbono , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/patologia , Feminino , Glutationa/metabolismo , Inflamação/metabolismo , Inflamação/prevenção & controle , Ferro/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Cirrose Hepática/metabolismo , Cirrose Hepática/patologia , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos , Ratos Long-Evans , Espécies Reativas de Oxigênio/metabolismoRESUMO
Diabetes, obesity, and metabolic syndrome are becoming epidemic both in developed and developing countries in recent years. Complementary and alternative medicines have been used since ancient era for the treatment of diabetes and cardiovascular diseases. Bitter melon is widely used as vegetables in daily food in Bangladesh and several other countries in Asia. The fruits extract of bitter melon showed strong antioxidant and hypoglycemic activities in experimental condition both in vivo and in vitro. Recent scientific evaluation of this plant extracts also showed potential therapeutic benefit in diabetes and obesity related metabolic dysfunction in experimental animals and clinical studies. These beneficial effects are mediated probably by inducing lipid and fat metabolizing gene expression and increasing the function of AMPK and PPARs, and so forth. This review will thus focus on the recent findings on beneficial effect of Momordica charantia extracts on metabolic syndrome and discuss its potential mechanism of actions.