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Papain, bromelain, and ficin are commonly used plant proteases used for meat tenderization. Other plant proteases explored for meat tenderization are actinidin, zingibain, and cucumin. The application of plant crude extracts or powders containing higher levels of compounds exerting tenderizing effects is also gaining popularity due to lower cost, improved sensory attributes of meat, and the presence of bioactive compounds exerting additional benefits in addition to tenderization, such as antioxidants and antimicrobial effects. The uncontrolled plant protease action could cause excessive tenderization (mushy texture) and poor quality due to an indiscriminate breakdown of proteins. The higher cost of separation and the purification of enzymes, unstable structure, and poor stability of these enzymes due to autolysis are some major challenges faced by the food industry. The meat industry is targeting the recycling of enzymes and improving their stability and shelf-life by immobilization, encapsulation, protein engineering, medium engineering, and stabilization during tenderization. The present review critically analyzed recent trends and the prospects of the application of plant proteases in meat tenderization.
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The Wnt signaling pathway is intricately connected with bone mass regulation in humans and rodent models. We designed an antibody-based platform that generates potent and selective Wnt mimetics. Using this platform, we engineer bi-specific Wnt mimetics that target Frizzled and low-density lipoprotein receptor-related proteins and evaluate their effects on bone accrual in murine models. These synthetic Wnt agonists induce rapid and robust bone building effects, and correct bone mass deficiency and bone defects in various disease models, including osteoporosis, aging, and long bone fracture. Furthermore, when these Wnt agonists are combined with antiresorptive bisphosphonates or anti-sclerostin antibody therapies, additional bone accrual/maintenance effects are observed compared to monotherapy, which could benefit individuals with severe and/or acute bone-building deficiencies. Our data support the continued development of Wnt mimetics for the treatment of diseases of low bone mineral density, including osteoporosis.
Assuntos
Conservadores da Densidade Óssea/farmacologia , Reabsorção Óssea/tratamento farmacológico , Fraturas do Fêmur/tratamento farmacológico , Osteoporose Pós-Menopausa/tratamento farmacológico , Proteínas Wnt/agonistas , Idoso , Envelhecimento/fisiologia , Animais , Densidade Óssea/efeitos dos fármacos , Densidade Óssea/fisiologia , Conservadores da Densidade Óssea/uso terapêutico , Reabsorção Óssea/fisiopatologia , Difosfonatos/farmacologia , Difosfonatos/uso terapêutico , Modelos Animais de Doenças , Avaliação Pré-Clínica de Medicamentos , Sinergismo Farmacológico , Quimioterapia Combinada/métodos , Feminino , Fraturas do Fêmur/patologia , Fêmur/efeitos dos fármacos , Fêmur/lesões , Fêmur/patologia , Humanos , Camundongos , Osteoporose Pós-Menopausa/fisiopatologia , Via de Sinalização Wnt/efeitos dos fármacos , Adulto JovemRESUMO
Chestnut inner shell (CIS) is rich in phenols and flavonoids such as gallic acid and ellagic acid, which are known to exhibit effective antioxidant and anti-obesity properties. Fermentation using lactic acid bacteria can enhance the physiological activity by increasing the contents of such functional ingredients. In this study, we evaluated the anti-obesity effects of a CIS extract subjected to a fermentation process (fermented CIS [FCIS]). Treatment with CIS and FCIS extracts (125, 250, and 500 µg/mL) increased cell viability and did not induce apoptosis, indicating no toxicity. The extract suppressed the gene expression of adipogenic factors, peroxisome proliferation-activated receptor gamma, CCAAT/enhancer binding protein (C/EBP) alpha, and C/EBP beta (by 7.75% and 67.59%, 21.41% and 66.27% in 500 µg/mL, respectively), and consequently suppressed the expression of downstream lipogenic factors such as fatty acid synthase, stearoyl CoA desaturase-1, citrate synthase, and ATP citrate lyase. The expression of factors involved in fat catabolism and ß-oxidation increased in a dose-dependent manner, thereby preventing fat accumulation. This observation was consistent with the significant decrease in the staining intensity for lipid droplets, which indicated that lipid accumulation was decreased by 15.46% and 29.44% in 3T3L-1 and 27.01% and 46.68% in C3H10T1/2. Together, these results demonstrate the higher anti-obesity effects of FCIS extract than that of CIS extract, indicating the potential applicability of FCIS as an effective natural raw material to curb obesity.
Assuntos
Adipócitos , Fármacos Antiobesidade , Células 3T3-L1 , Adipócitos/metabolismo , Adipogenia , Animais , Fármacos Antiobesidade/farmacologia , Diferenciação Celular , Fermentação , Camundongos , Obesidade/tratamento farmacológico , PPAR gama/metabolismo , Extratos Vegetais/farmacologiaRESUMO
We demonstrated the effect of a mixture containing fermented Achyranthes japonica Nakai (FS) in the context of a monosodium iodoacetate (MIA)-induced osteoarthritis animal model. The mineralization, anabolic and catabolic factors, and the amount of cytokines within the articular cartilage of rats were measured after administration of MIA. We found that dietary supplementation with methylsulfonylmethane (positive control) and FS (FS 100 mg/kg body weight [b.w.] and FS 300 mg/kg b.w.) effectively suppressed pathological changes in the knee joint and inhibited changes in the architectural and mineralization parameters. In addition, prostaglandin E2 (PGE2) and proinflammatory cytokines in the serum and catabolic factors, including matrix metalloproteinase (MMP)-3 and MMP-7 in articular cartilage, were decreased by dietary supplementation with FS in MIA-induced osteoarthritis. Based on these findings, we suggest that FS can be used for the development of potential therapies for osteoarthritis.
Assuntos
Achyranthes/química , Cartilagem Articular , Suplementos Nutricionais , Alimentos Fermentados , Osteoartrite do Joelho/dietoterapia , Animais , Citocinas , Modelos Animais de Doenças , Ácido Iodoacético , Articulação do Joelho , Osteoartrite do Joelho/induzido quimicamente , RatosRESUMO
Licorice (Glycyrrhiza uralensis) contains several compounds that have been reported to alleviate menopausal symptoms via interacting with estrogen receptors (ERs). The compounds exist mainly in the form of glycosides, which exhibit low bioavailability and function. To bioconvert liquiritin and isoliquiritin, the major estrogenic compounds, to the corresponding deglycosylated liquiritigenin and isoliquiritigenin, respectively, licorice was fermented with Monascus, which has been demonstrated to deglycosylate other substances. The contents of liquiritigenin and isoliquiritigenin in Monascus-fermented licorice increased by 10.46-fold (from 38.03 µM to 379.75 µM) and 12.50-fold (from 5.53 µM to 69.14 µM), respectively, compared with their contents in non-fermented licorice. Monascus-fermented licorice exhibited 82.5% of the ERß binding activity of that observed in the positive control (17 ß-estradiol), whereas the non-fermented licorice exhibited 54.1% of the binding activity in an in vivo ER binding assay. The increase in the ERß binding activity was associated with increases in liquiritigenin and isoliquiritigenin contents. Liquiritigenin acts as a selective ligand for ERß, which alleviates menopausal symptoms with fewer side effects, such as heart disease and hypertension, compared with a ligand for ERα. In addition, Monascus-fermented licorice contained 731 mg/kg of monacolin K, one of the metabolites produced by Monascus that reduces serum cholesterol. Therefore, Monascus-fermented licorice is a promising material for the prevention and treatment of menopausal syndrome with fewer side effects.
Assuntos
Biotransformação , Glycyrrhiza uralensis/química , Glycyrrhiza/química , Menopausa/efeitos dos fármacos , Monascus/metabolismo , Extratos Vegetais/farmacologia , Chalconas/química , Chalconas/farmacologia , Cromatografia Líquida de Alta Pressão , Avaliação Pré-Clínica de Medicamentos , Receptor beta de Estrogênio/metabolismo , Fermentação , Flavanonas/química , Flavanonas/farmacologia , Flavanonas/uso terapêutico , Glucosídeos/química , Glucosídeos/farmacologia , Fogachos/tratamento farmacológico , Fogachos/metabolismo , Lovastatina/química , Lovastatina/farmacologia , Menopausa/metabolismo , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Ligação ProteicaRESUMO
The anti-obesity effects of fermented Castanea crenata inner shell extract (FCCE) were investigated using high-fat diet (HFD)-induced obese mice. In the FCCE intake groups, body weight gain and adipocyte area were significantly reduced, especially body weight gain in the 250 mg/kg FCCE group (G4) decreased by 37%, respectively, compared with negative control group (G2, HFD group). After oral administration of the FCCE, the increase of serum low-density lipoprotein (LDL)-cholesterol induced by HFD was suppressed significantly, as well as the level of aspartate aminotransferase, and alanine aminotransferase, which are markers of hepatitis induced by obesity. Serum leptin in G4 group was significantly decreased to less than that of G2 group. Also, in G4 and 500 mg/kg FCCE group (G5), enzymes-related lipogenesis, citrate synthase, and ATP citrate lyase were decreased, whereas the level of enoyl-CoA hydratase used for ß-oxidation was significantly increased in comparison with normal diet group. Furthermore, the FCCE stimulated the expression of lipolytic regulators, especially AMP-activated protein kinase. In conclusion, we suggest that the FCCE may ameliorate in diet-induced obesity by regulating lipid metabolism.
Assuntos
Fármacos Antiobesidade/administração & dosagem , Fagaceae/metabolismo , Obesidade/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Proteínas Quinases Ativadas por AMP/metabolismo , ATP Citrato (pro-S)-Liase/metabolismo , Animais , Fármacos Antiobesidade/metabolismo , LDL-Colesterol/metabolismo , Dieta Hiperlipídica/efeitos adversos , Fagaceae/química , Fagaceae/microbiologia , Humanos , Leptina/sangue , Lipogênese/efeitos dos fármacos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Obesos , Obesidade/metabolismo , Obesidade/fisiopatologia , Extratos Vegetais/metabolismo , Saccharomyces cerevisiae/metabolismo , Triglicerídeos/metabolismoRESUMO
Phytoestrogens possess beneficial effects in the management of menopausal symptoms with few side effects. Soybeans are major natural sources of isoflavones, with high estrogen receptor (ER)-ß selectivity. The objective of this study therefore was to develop a solvent-mediated extraction method for soybean germinated embryos (SGEs) and to investigate the biological activities of the extract. Ethanolic extraction yielded the SGE extract (SGEE), which had a unique composition of biologically active aglycones and soyasaponins. SGEE showed a proliferative effect in MCF7 cells and ERß-selective transcriptional activities in human embryonic kidney cells. In addition, oral administration of SGEE to ovariectomized rats resulted in the induction of ERß and estrogen-responsive genes in the uterus and a decrease in tail skin temperature and uterus weight. Our data suggest that germination and ethanolic extraction are effective measures for producing isoflavone-rich food supplements, which may be useful as alternative menopausal hormone therapy.
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Receptor beta de Estrogênio/metabolismo , Glycine max/química , Extratos Vegetais/farmacologia , Saponinas/farmacologia , Moduladores Seletivos de Receptor Estrogênico/farmacologia , Pele/efeitos dos fármacos , Útero/efeitos dos fármacos , Animais , Temperatura Corporal , Feminino , Germinação , Humanos , Células MCF-7 , Menopausa , Tamanho do Órgão/efeitos dos fármacos , Ovariectomia , Fitoestrógenos/farmacologia , Fitoterapia , Ratos Sprague-Dawley , Sementes , Cauda , Útero/metabolismoRESUMO
The objective of this experiment was to evaluate the antioxidant potential of Allium hookeri (AH) root in two forms, powdered AH root and fermented powdered AH root, to demonstrate its value as an antibiotic alternative feed additive for broiler chickens. A total of 125 male Ross-708 broiler chickens were randomly assigned to five groups (nâ¯=â¯25 birds/group) and fed standard diets supplemented with root or fermented root of AH at two different levels (1% or 5%). Control birds were provided with non-supplemented basal diets. Body weights was measured at days 14 and 21 of age. To monitor antioxidant activities, heme oxygenase (HMOX), aflatoxin B1 aldehyde reductase (AFAR), superoxide dismutase 1 (SOD1), and catalase (CAT) enzyme levels were quantified by real-time PCR in the jejunums 21-day-old birds. Also, serum levels of SOD, CAT, and malondialdehyde (MDA) were measured using commercial kits. The results showed greater body weight gains at day 14 in chickens fed diets supplemented with 1% AH root, as compared to the control group (pâ¯<â¯0.05). Up-regulated transcript levels of AFAR, HMOX1, and CAT were observed in the jejunum of chickens fed diets supplemented with AH. The serum levels SOD and CAT were significantly increased (pâ¯<â¯0.05) in groups treated with AH, whereas MDA levels were decreased in groups fed diets supplemented with AH, as compared to the control group. These results indicated that an optimum level of dietary AH supplementation to young broiler chickens influences growth and improves antioxidant activities.
Assuntos
Allium/química , Fenômenos Fisiológicos da Nutrição Animal , Galinhas/crescimento & desenvolvimento , Galinhas/metabolismo , Ração Animal , Animais , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Dieta , Suplementos Nutricionais , MasculinoRESUMO
Curcumin is a natural polyphenol and essential curcuminoid derived from the rhizome of the medicinal plant Curcuma longa (L.) is universally acknowledged as "Wonder drug of life". It is a vital consumable and restorative herb, commonly keened for several ailments such as cancer, arthritis, pain, bruises, gastrointestinal quandaries, swelling and much more. Despite its enormous curative potential, the poor aqueous solubility and consequently, minimal systemic bioavailability with rapid degradation are some of the major factors which restrict the utilization of curcumin at medical perspective. However, to improve its clinically relevant parameters, nanoformulation of curcumin is emerging as a novel substitute for their superior therapeutic modality. It enhances its aqueous solubility and targeted delivery to the tissue of interest that prompts to enhance the bioavailability, better drug conveyance, and more expeditious treatment. Subsequent investigations are endeavored to enhance the bio-distribution of native curcumin by modifying with felicitous nano-carriers for encapsulation. In this review, we specifically focus on the recent nanotechnology based implementations applied for overcoming the innate constraints of native curcumin and additionally the associated challenges which restrict its potential therapeutic applications both in vivo and in-vitro studies, as well as their detailed mechanism of action, have additionally been discussed.
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Tartary buckwheat (Fagopyrum tataricum) has been established globally as a nutritionally important food item, particularly owing to high levels of bioactive compounds such as rutin. This study investigated the effect of tartary buckwheat extracts (TBEs) on adipogenesis and inflammatory response in 3T3-L1 cells. TBEs inhibited lipid accumulation, triglyceride content, and glycerol-3-phosphate dehydrogenase (GPDH) activity during adipocyte differentiation of 3T3 L1 cells. The mRNA levels of genes involved in fatty acid synthesis, such as peroxisome proliferator-activated receptor-γ (PPAR-γ), CCAAT/enhancer binding protein-α (CEBP-α), adipocyte protein 2 (aP2), acetyl-CoA carboxylase (ACC), fatty acid synthase (FAS), and stearoylcoenzyme A desaturase-1 (SCD-1), were suppressed by TBEs. They also reduced the mRNA levels of inflammatory mediators such as tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), monocyte chemoattractant protein 1 (MCP-1), and inducible nitric oxide synthase (iNOS). In addition, TBEs were decreased nitric oxide (NO) production. These results suggest that TBEs may inhibit adipogenesis and inflammatory response; therefore, they seem to be beneficial as a food ingredient to prevent obesity-associated inflammation.
Assuntos
Adipócitos/efeitos dos fármacos , Adipogenia/efeitos dos fármacos , Fagopyrum/química , Obesidade/tratamento farmacológico , Extratos Vegetais/farmacologia , Rutina , Células 3T3-L1 , Acetil-CoA Carboxilase/metabolismo , Adipócitos/citologia , Adipócitos/metabolismo , Animais , Proteína alfa Estimuladora de Ligação a CCAAT/metabolismo , Diferenciação Celular , Ácido Graxo Sintases/metabolismo , Glicerolfosfato Desidrogenase/metabolismo , Inflamação/metabolismo , Interleucina-6/metabolismo , Metabolismo dos Lipídeos/efeitos dos fármacos , Camundongos , Óxido Nítrico/biossíntese , Obesidade/complicações , Obesidade/metabolismo , PPAR gama/metabolismo , Rutina/administração & dosagem , Rutina/química , Rutina/farmacologia , Rutina/uso terapêutico , Triglicerídeos/metabolismo , Fator de Necrose Tumoral alfa/metabolismoRESUMO
The aim of this study was to evaluate the wrinkle improving effect of hyaluronic acid intakes. Wrinkles were induced by exposing the skin of hairless mice to ultraviolet B (UVB) irradiation for 14 weeks. Hyaluronic acid was administered to the mice for 14 weeks including 4 weeks before experiments. Skin tissue was assayed by enzyme-linked immunosorbent assay to determine protein expression of wrinkle-related markers. The group supplemented with high concentrations of hyaluronic acid appeared significantly better than control group for collagen, matrix metalloproteinase 1, interleukin (IL)-1ß, and IL-6 assay. Transforming growth factor-ß1 (TGF-ß1) and hyaluronic acid synthase 2 (HAS-2) were not shown to be significantly different. In conclusion, hyaluronic acid administration regulated expression levels of proteins associated with skin integrity, and improved the wrinkle level in skin subjected to UVB irradiation.
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Ácido Hialurônico/uso terapêutico , Envelhecimento da Pele/efeitos dos fármacos , Pele/efeitos dos fármacos , Pele/efeitos da radiação , Administração Oral , Animais , Colágeno/metabolismo , Ensaio de Imunoadsorção Enzimática , Feminino , Interleucina-6/metabolismo , Metaloproteinase 13 da Matriz/metabolismo , Camundongos , Camundongos Pelados , Proteoma , Fator de Crescimento Transformador beta1/metabolismo , Raios UltravioletaRESUMO
We undertook a study to assess the effects of Allium hookeri (AH) root and fermented root on inflammation and intestinal integrity of lipopolysaccharide (LPS)-challenged broiler chickens. Birds were assigned to six groups (n = 25 birds/treatment) and fed with basal diets (CON) or basal diets supplemented with AH root or fermented root at two concentrations (1 or 5%). At 7 d of age, five groups (n= 125) in each dietary treatment were injected with LPS (1 mg/kg body weight), and the remaining 25 birds were injected with sterile phosphate-buffered saline (PBS) as a negative control. LPS challenge significantly reduced average body weight gain at 24 h post-injection compared with PBS control. Fermented root supplementation increased average body weight gain by 1% compared with the LPS-challenged control. Serum α- 1-AGP levels, interleukin (IL)-1ß, IL-8, tumor necrosis factor superfamily member 15 (TNFSF15), and LPS-induced tumor necrosis factor-α factor (LITAF) transcript levels were significantly higher in the small intestine in LPS-injected chickens. However α-1-AGP levels were reduced by AH root or fermented root (1 and 5%) supplementation and IL-1ß, IL-8, and LITAF were also down-regulated by root and fermented root (1 and 5%) supplementation. The reduced expression of tight junction proteins (junctional adhesion molecule 2 (JAM2) and occludin) and intestinal mucin 2 (MUC2) by LPS challenge was reversed by root or fermented root (1 and 5%) supplementation. These findings demonstrate that dietary AH root and fermented root influence antiinflammatory activity and tight junction protein expression in LPS-induced chickens.
Assuntos
Allium/química , Galinhas , Expressão Gênica , Inflamação/veterinária , Proteínas de Junções Íntimas/genética , Ração Animal/análise , Animais , Dieta/veterinária , Suplementos Nutricionais/análise , Relação Dose-Resposta a Droga , Inflamação/tratamento farmacológico , Inflamação/imunologia , Intestinos/imunologia , Lipopolissacarídeos/farmacologia , Masculino , Raízes de Plantas/química , Doenças das Aves Domésticas/tratamento farmacológico , Doenças das Aves Domésticas/imunologia , Proteínas de Junções Íntimas/metabolismoRESUMO
Obesity is viewed as a serious public health problem. This study aimed to investigate the antiobesity effects of fermented garlic extract by lactic acid bacteria (LAFGE) on obesity. Male C57BL/6J mice were fed with high-fat diet (HFD) to induce obesity. The HFD-induced obese mice were orally administrated with 250 or 500 mg/kg LAFGE for 8 weeks. Feeding HFD-fed mice with 250 or 500 mg/kg LAFGE reduced body weight by 14% and 18%, respectively, compared to HFD. HFD-fed mice with 500 mg/kg LAFGE administration had lower epididymal, retroperitoneal, and mesenteric adipose tissue mass by 36%, 44%, and 63%, respectively, compared to HFD. The concentration of plasma triacylglyceride and total cholesterol was significantly lower in the HFD-fed mice with LAFGE administration. Moreover, LAFGE supplementation suppressed adipogenesis by downregulation in mRNA and protein expression of PPARγ, C/EBPα, and lipogenic proteins, including SREBP-1c, FAS, and SCD-1. Based on these findings, LAFGE may ameliorate diet-induced obesity by inhibiting adipose tissue hypertrophy by suppressing adipogenesis.
Assuntos
Adipogenia/efeitos dos fármacos , Fármacos Antiobesidade/farmacologia , Fermentação , Alho , Lactobacillus plantarum/metabolismo , Obesidade/metabolismo , Extratos Vegetais/farmacologia , Tecido Adiposo/metabolismo , Animais , Fármacos Antiobesidade/uso terapêutico , Peso Corporal/efeitos dos fármacos , Proteína alfa Estimuladora de Ligação a CCAAT/sangue , Colesterol/sangue , Dieta Hiperlipídica , Regulação para Baixo , Metabolismo dos Lipídeos/efeitos dos fármacos , Camundongos Endogâmicos C57BL , Camundongos Obesos , Obesidade/tratamento farmacológico , PPAR gama/sangue , Fitoterapia , Extratos Vegetais/uso terapêutico , RNA Mensageiro/metabolismo , Estearoil-CoA Dessaturase/sangue , Proteína de Ligação a Elemento Regulador de Esterol 1/sangue , Triglicerídeos/sangueRESUMO
Solanum tuberosum L. cv Jayoung (JY) is a potato with dark purple flesh and contains substantial amounts of polyphenols. In this study, we evaluated the therapeutic effects of S. tuberosum L. cv JY in a mouse model of Dermatophagoides farinae body (Dfb)-induced atopic dermatitis (AD). The ethanol extract of the peel of JY (EPJ) ameliorated Dfb-induced dermatitis severity, serum levels of immunoglobulin E (IgE) and thymus and activation-regulated chemokine. Histological analysis of the skin also revealed that EPJ treatment significantly decreased mast cell infiltration. The suppression of dermatitis by EPJ treatment was accompanied by a decrease in the skin levels of type 2 helper T-cell cytokines such as interleukin (IL)-4, IL-5, and IL-13. The induction of thymic stromal lymphopoietin, which leads to a systemic Th2 response, was also decreased in the skin by EPJ. Nuclear translocation of nuclear factor-κB p65 was decreased by EPJ in Dfb-induced NC/Nga mice. The protein expression of filaggrin in the AD-like skin lesions was restored by EPJ treatment. These results suggested that EPJ may be a potential therapeutic tool for the treatment of AD.
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Dermatite Atópica/tratamento farmacológico , Ácaros , Fitoterapia , Extratos Vegetais/uso terapêutico , Pele/efeitos dos fármacos , Solanum tuberosum/química , Equilíbrio Th1-Th2/efeitos dos fármacos , Animais , Antígenos , Citocinas/sangue , Dermatite Atópica/etiologia , Dermatite Atópica/imunologia , Dermatite Atópica/metabolismo , Proteínas Filagrinas , Proteínas de Filamentos Intermediários/metabolismo , Masculino , Camundongos , Epiderme Vegetal , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Polifenóis/uso terapêutico , Pele/metabolismo , Pele/patologia , Linfócitos T Auxiliares-Indutores/metabolismo , Células Th1/metabolismo , Células Th2/metabolismoRESUMO
Baicalin is a flavonoid derived from the dried root of Scutellaria baicalensis. In this study, oxygen-induced retinopathy was used to characterize the anti-angiogenic properties of baicalin in mice. Pups were exposed to a hyperbaric oxygen environment to induce retinal angiogenesis and were subjected to intraperitoneal injection of baicalin. Avascular area, neovascular tufts, and neovascular lumens were quantified from digital images. Compared to the vehicle, baicalin clearly reduced the central avascular zone and the number of neovascular tufts and lumens. High-dose baicalin (10 mg/kg) significantly reduced the expression of matrix metalloproteinase-2 (MMP-2), MMP-9, angiotensin II, and vascular endothelial growth factor (VEGF). These results show that baicalin is a powerful antiangiogenic compound that attenuates new vessel formation in the retina after systemic administration, and is a candidate substance for therapeutic inhibition of retinal angiogenesis.
Assuntos
Modelos Animais de Doenças , Flavonoides/uso terapêutico , Retinopatia da Prematuridade/tratamento farmacológico , Angiotensina II/metabolismo , Animais , Regulação para Baixo/efeitos dos fármacos , Metaloproteinase 2 da Matriz/metabolismo , Metaloproteinase 9 da Matriz/metabolismo , Camundongos , Fator A de Crescimento do Endotélio Vascular/metabolismoRESUMO
This study evaluated the chemical composition, antioxidant, anti-inflammatory and anticancer activities of a Euphorbia hirta L. extract. The antioxidant activities of whole E. hirta ethanol extract were determined by electron spin resonance spectrophotometric analysis of 1,1-diphenyl-2-picryl-hydrazyl (DPPH), hydroxyl, and alkyl radical levels and by using an online high-performance liquid chromatography (HPLC)-2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) assay. The E. hirta ethanol extract (0.5 mg/mL) exhibited DPPH-scavenging activity of 61.19% ± 0.22%, while the positive control (0.5 mg/mL ascorbic acid) had 100% ± 0.22% activity. The concentration of the extract required to trap 50% of DPPH (IC50) was 0.205 mg/mL. Online HPLC analysis of the extract also showed strong antioxidant activity. The anti-inflammatory activity of the E. hirta extract was assessed in lipopolysaccharide-induced RAW 264.7 macrophages. The anti-inflammatory activity was highest in the presence of 200 µg/mL E. hirta extract, and nitric oxide production was decreased significantly (p < 0.05). The extract also showed selective anticancer activity at a concentration of 100 µg/mL (p < 0.05). These results indicated that E. hirta may warrant further investigation for the development of antioxidant, anti-inflammatory, and anticancer herbal medications.
Assuntos
Anti-Inflamatórios/administração & dosagem , Antioxidantes/administração & dosagem , Macrófagos/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Animais , Anti-Inflamatórios/química , Antioxidantes/química , Cromatografia Líquida de Alta Pressão , Euphorbia/química , Radicais Livres/química , Humanos , Camundongos , Óxido Nítrico/metabolismo , Extratos Vegetais/químicaRESUMO
An optical coherence tomography (OCT) system employing a microelectromechanical system (MEMS) mirror was used to measure the refractive index (RI) of anatomically different regions in acute brain tissue slices, in which viability was maintained. RI was measured in white-matter and grey-matter regions, including the cerebral cortex, putamen, hippocampus, thalamus and corpus callosum. The RI in the corpus callosum was found to be ~4% higher than the RIs in other regions. Changes in RI with tissue deformation were also measured in the cerebral cortex and corpus callosum under uniform compression (20-80% strain). For 80% strain, measured RIs increased nonlinearly by up to 70% and 90% in the cerebral cortex and corpus callosum respectively. Knowledge of RI in heterogeneous tissues can be used to correct distorted optical images caused by RI variations between different regions. Also deformation-dependent changes in RI can be applied to OCT elastography or to mechanical tests based on optical imaging such as indentation tests.
Assuntos
Encéfalo/citologia , Refratometria/instrumentação , Refratometria/métodos , Tomografia de Coerência Óptica/instrumentação , Tomografia de Coerência Óptica/métodos , Animais , Sobrevivência Celular , Córtex Cerebral/citologia , Corpo Caloso/citologia , Desenho de Equipamento , Hipocampo/citologia , Masculino , Modelos Teóricos , Técnicas de Cultura de Órgãos , Putamen/citologia , Ratos , Ratos Sprague-Dawley , Tálamo/citologiaRESUMO
Three known 2-arylbenzofurans, moracin P (1), moracin O (2) and mulberrofuran Q (3) were isolated from the MeOH extract of the Mori Cortex Radicis. These compounds 1-3 enhanced cell viability in dose-dependent manner against oxygen-glucose deprivation (OGD)-induced cell death in neuroblastoma SH-SY5Y cells, which was measured by MTT reduction assay. (EC(50) values of 10.4, 12.6, and 15.9 µM, respectively). In addition, the compounds 1-3 were examined for their inhibitory effect on OGD-induced ROS production by FACS analysis. We observed these compounds reduced ROS production in OGD-induced cell death (IC(50) values of 1.9, 0.3 and 12.1 µM, respectively). Consequently, reactive oxygen species (ROS) were overexpressed in OGD-induced cells and all three compounds reduced ROS induced by OGD in dosedependent manner. Taken together, compounds 1-3 might protect neuronal cell death against the oxidative stress induced by OGD, though further studies in vitro and in vivo models are necessary.
Assuntos
Benzofuranos/farmacologia , Morte Celular , Glucose/metabolismo , Moraceae , Fármacos Neuroprotetores/farmacologia , Oxigênio/metabolismo , Extratos Vegetais/farmacologia , Benzofuranos/isolamento & purificação , Linhagem Celular Tumoral , Sobrevivência Celular/fisiologia , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Formazans/metabolismo , Humanos , Concentração Inibidora 50 , Neurônios/citologia , Neurônios/metabolismo , Fármacos Neuroprotetores/isolamento & purificação , Estresse Oxidativo , Espécies Reativas de Oxigênio/metabolismo , Sais de Tetrazólio/metabolismoRESUMO
This study investigated the inhibitory effects of costunolide isolated from the leaves of Laurus nobilis L. (Lauraceae) on basophil-mediated allergic reactions and interleukin (IL)-5-mediated B cell growth. The effects of costunolide on ß-hexosaminidase (a key parameter of degranulation) release and IL-4 expression in rat basophilic leukemia (RBL-2H3) cells were determined by measuring ß-hexosaminidase activity and by semi-quantitative RT-PCR, respectively. The effects of costunolide on Y16 pro-B cell viability and growth were determined by 3-(4,5-dimethylthiazol-2-yl)2,5-diphenyltetrazolium bromide (MTT) assay. Costunolide was found significantly to inhibit ß-hexosaminidase activity (p < 0.01) and IL-4 transcription in RBL-2H3 cells in a dose-dependent manner. Its 50% inhibitory concentration (IC50 ) was 34 µM, while that of the positive control, ketotifen, was 24 µM (IL-4 mRNA transcription). Moreover, costunolide dose-dependently suppressed pro-B cell growth in IL-5-stimulated Y16 cells. These results provide evidence that costunolide stabilizes mast cells by inhibiting IgE-mediated degranulation and inhibits IL-5-stimulated B cell growth.
Assuntos
Degranulação Celular/efeitos dos fármacos , Laurus/química , Mastócitos/efeitos dos fármacos , Células Precursoras de Linfócitos B/efeitos dos fármacos , Sesquiterpenos/farmacologia , Animais , Linhagem Celular Tumoral , Relação Dose-Resposta a Droga , Imunoglobulina E , Concentração Inibidora 50 , Interleucina-4/metabolismo , Interleucina-5 , Mastócitos/fisiologia , Ratos , beta-N-Acetil-Hexosaminidases/metabolismoRESUMO
Dopamine (DA), as a neurotoxin, can elicit severe Parkinson's disease-like syndrome by elevating intracellular reactive oxygen species (ROS) levels and apoptotic activity. We examined the inhibitory effects of 3α-acetoxyeudesma-1,4(15),11(13)-trien-12,6α-olide (AETO), purified from the leaves of Laurus nobilis L., on DA-induced apoptosis and α-synuclein (α-syn) formation in dopaminergic SH-SY5Y cells. AETO decreased the active form of caspase-3 and the levels of p53, which were accompanied by increased levels of Bcl-2 in a dose-dependent manner. Flow cytometric and Western blot analysis showed that AETO significantly inhibited DA-induced apoptosis along with suppression of intracellular tyrosinase activity, ROS generation, quinoprotein, and α-syn formation (P < 0.01). These results indicate that AETO inhibited DA-induced apoptosis, which is closely related to the suppression of intracellular tyrosinase activity and the formation of α-syn, ROS, and quinoprotein in SH-SY5Y cells.