Anti-obesity role of adzuki bean extract containing polyphenols: in vivo and in vitro effects

BACKGROUND: The aim of this work was to evaluate the effects of polyphenol‐rich adzuki bean extract on lipid metabolism, triglyceride accumulation and proinflammatory cytokine secretion in vivo and in vitro. RESULTS: For the in vivo study, rats were divided into four groups: group C was fed a control diet, group A was fed the control diet with 1% adzuki bean extract, group CF was fed a high fat diet, and group AF was fed a high fat diet with 1% adzuki bean extract. For the in vitro study, the ability of adzuki bean extract to suppress triglyceride incorporation, glycerol phosphate dehydrogenase activity and inflammatory response was investigated in cultured human adipocytes. Data from the animal study showed that adzuki bean extract improved lipid metabolism in both the normal and high‐fat diet groups. Adzuki bean extract treatment in the high‐fat group resulted in significant reductions in total hepatic lipid accumulation and lipid secretion into the feces. Incubation of adipocytes with adzuki bean extract significantly decreased triglyceride accumulation, glycerol phosphate dehydrogenase activity and inflammatory responses without affecting cell viability. CONCLUSION: The results of this study demonstrate that adzuki bean extract has high potential to serve as a natural anti‐obesity agent. Copyright © 2012 Society of Chemical Industry     

In vitro antioxidant activity and in vivo photoprotective effect of a red orange extract

Ultraviolet radiation causes damage to the skin, which may result in both precancerous and cancerous skinlesions and acceleration of skin ageing. Topical administration of enzymatic and non-enzymatic antioxidants is an effective strategy for protecting the skin against UV-mediated oxidative damage. Hence, a systematic study to evaluate the in vitro antioxidant activity and in vivo photoprotective effect of a standardized red orange extract (ROE) has been undertaken, where the main active ingredients are anthocyanins, hydroxycinnamic acids, flavanones and ascorbic acid. For the in vitro experiments, the ROE was tested in three models: (1) bleaching of the stable 1,1-diphenyl-2-picrylhydrazyl radical (DPPH test); (2) peroxidation, induced by the water-soluble radical initiator 2,2'-azobis(2-amidinopropane) hydrochloride, of mixed dipalmitoylphosphatidylcholine/linoleic acid unilamellar vesicles (LUVs) (LP-LUV test); and (3) UV-induced peroxidation of phospatidylcholine multilamellar vesicles (UV-IP test). The in vivo antioxidant/radical scavenger activity was assessed by determining the ability of topically applied ROE to reduce UVB-induced skin erythema in healthy human volunteers. The results obtained in the DPPH, LP-LUV and UV-IP tests demonstrated the strong antioxidant properties of ROE, with a clear relationship between ROE scavenger efficiency and its content in antioxidant compounds. In particular, the findings obtained in the UV-IP test provide a strong rationale for using this extract as a photoprotective agent. During in vivo experiments, ROE provided to efficiently protect against photooxidative skin damage when topically applied immediately after skin exposure to UVB radiations. Interestingly, the protective effect of ROE appears higher than that elicited by another natural antioxidant (tocopherol) commonly employed in cosmetic formulations. In conclusion, the present findings demonstrate that ROE affords excellent skin photoprotection, which is very likely a result of the antioxidant/radical scavenger activity of its active ingredients. Thus, ROE might have interesting applications in both anti-photoageing and after-sun cosmetic products.     

Selective androgen receptor modulators: in vitro and in vivo metabolism and analysis

For future targeted screening in National Residue Control Programmes, the metabolism of seven SARMs, from the arylpropionamide and the quinolinone classes, was studied in vitro using S9 bovine liver enzymes. Metabolites were detected and identified with ultra-performance liquid chromatography (UPLC) coupled to time-of-flight mass spectrometry (ToF-MS) and triple quadrupole mass spectrometry (QqQ-MS). Several metabolites were identified and results were compared with literature data on metabolism using a human cell line. Monohydroxylation, nitro-reduction, dephenylation and demethylation were the main S9 in vitro metabolic routes established. Next, an in vivo study was performed by oral administration of the arylpropionamide ostarine to a male calf and urine samples were analysed with UPLC-QToF-MS. Apart from two metabolites resulting from hydroxylation and dephenylation that were also observed in the in vitro study, the bovine in vivo metabolites of ostarine resulted in glucuronidation, sulfation and carboxylation, combined with either a hydroxylation or a dephenylation step. As the intact mother compounds of all SARMs tested are the main compounds present after in vitro incubations, and ostarine is still clearly present in the urine after the in vivo metabolism study in veal calves, the intact mother molecules were selected as the indicator to reveal treatment. The analytical UPLC-QqQ-MS/MS procedure was validated for three commercially available arylpropionamides according to European Union criteria (Commission Decision 2002/657/EC), and resulted in decision limits ranging from 0.025 to 0.05 µg l^–1 and a detection capability of 0.025 µg l^–1 in all cases. Adequate precision and intra-laboratory reproducibility (relative standard deviation below 20%) were obtained for all SARMs and the linearity was 0.999 for all compounds. This newly developed method is sensitive and robust, and therefore useful for confirmation and quantification of SARMs in bovine urine samples for residue control programmes and research purposes.     

淡竹叶多酚的提取纯化工艺优化、组分分析及体外抗氧化活性研究

目的 确定淡竹叶多酚提取纯化工艺,分析主要成分及体外抗氧化活性。方法 采用超声辅助提取淡竹叶多酚,通过响应面实验确定最佳提取条件。选取适合淡竹叶多酚纯化的大孔树脂,对纯化工艺参数进行优化。通过高效液相色谱-质谱法(high performance liquid chromatography-mass spectrometry, HPLC-MS)鉴定淡竹叶多酚的主要成分,并评价其体外抗氧化活性。结果 淡竹叶多酚的最佳提取工艺参数为:乙醇体积分数60%、超声功率500 W、料液比1:25 (g/mL)、超声时间24 min及超声温度59℃,该条件下淡竹叶多酚提取量为8.01 mg/g。淡竹叶多酚纯化工艺参数为:上样质量浓度6 mg/mL、pH 4、流速2 mL/min、解吸液为70%乙醇、解吸体积90 mL,纯化后的淡竹叶多酚纯度由12.86%提高到76.18%。通过HPLC-MS鉴定出16种酚类成分,且纯化后多酚有较高的抗氧化活性。结论 本研究得到了淡竹叶多酚提取纯化工艺,得到的多酚纯化物有明显的抗氧化活性。     

Effects of in vivo phlorizin treatment and in vitro addition of carnitine,propionate, acetate,and 5-tetradecyloxy-2-furoic acid on palmitate metabolism in ovine hepatocytes

Modulatory effects of l-carnitine, acetate, propionate, and 5-tetradecyloxy-2-furoic acid (TOFA; an inhibitor of acetyl-CoA carboxylase) on oxidation and esterification of [1-¹⁴C]-palmitate were studied in hepatocytes isolated from phlorizin-treated and control wethers. Our hypotheses were that (1) palmitate oxidation would be greater in hepatocytes from sheep injected with phlorizin; (2) l-carnitine would increase palmitate oxidation more in hepatocytes from sheep injected with phlorizin; and (3) acetate and propionate would decrease oxidation in sheep hepatocytes partly through action of acetyl-CoA carboxylase. Palmitate metabolism did not differ between cells from control and those from phlorizin-treated wethers. Carnitine increased oxidation of palmitate to CO₂ and acid-soluble products (ASP; mainly ketone bodies) and decreased esterification of palmitate in isolated hepatocytes from both groups of wethers, but the increase in oxidation to ASP was greater in cells from phlorizin-treated wethers. Propionate increased palmitate oxidation to CO₂ in phlorizin-treated wethers. Propionate increased oxidation of palmitate to ASP in control wethers but decreased oxidation to ASP in phlorizin-treated wethers. Propionate increased esterification of palmitate to total esterified products and triglyceride, and the effect was larger in phlorizin-treated wethers. Acetate decreased palmitate esterification to total esterified products in control wethers, but the effect was blunted in phlorizin-treated wethers. Acetate did not affect palmitate oxidation. Addition of TOFA increased production of triglyceride from palmitate in the presence of propionate. The lack of interaction between TOFA and propionate indicates that propionate does not inhibit carnitine palmitoyltransferase I via cytosolic generation of methylmalonyl-CoA by acetyl-CoA carboxylase. In conclusion, although in vivo phlorizin treatment did not affect in vitro metabolism of palmitate by isolated ovine hepatocytes, phlorizin increased the stimulatory effect of carnitine on oxidation of palmitate to ASP and the inhibitory effect of propionate on oxidation of palmitate to ASP. Metabolism of acetate and propionate by acetyl-CoA carboxylase did not affect palmitate oxidation or esterification. Results provide additional insight into control of fatty acid metabolism in hepatocytes.     

The in vitro and in vivo metabolism of dimethoate by stored wheat and sorghum grains

In vivo and in vitro investigations showed that wheat and sorghum rapidly degrade diniethoate to nontoxic anionic derivatives. Slight oxidation to a toxic analogue occurs but this is similarly degraded.     

Silver/chitosan-based Janus particles: Synthesis,characterization, and assessment of antimicrobial activity in vivo and vitro

Janus particles containing chitosan and silver were synthesized in an eco-friendly manner and were confirmed using transmission electron microscopy. Based on the data of the antimicrobial activity assessment, this material exhibited a higher antimicrobial activity than virgin chitosan with long–lasting antibacterial effectiveness against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Salmonella choleraesuis bacteria, as well as Botrytis cinerea fungi. The results showed that the Janus polymer could completely suppress the growth and germination of B. cinerea at a concentration of 0.02 mg/mL in vitro and in vivo. This Janus polymer is an advanced functional material that combines the suitable properties of both components and could be an alternative new antimicrobial agent due to its unique chemical properties and pronounced antimicrobial activity. This material is a potential candidate for use in the food industry to prevent microbial contamination and to inhibit the growth of microorganisms, enhancing product quality and, extend shelf-life of fresh and processed agri-food products.     

Zingiber officinale extract exhibits antidiabetic potential via modulating glucose uptake, protein glycation and inhibiting adipocyte differentiation: an in vitro study

BACKGROUND: Ginger, the rhizome of Zingiber officinale Roscoe (Zingiberaceae), a perennial herbaceous plant is native to Southern Asia. Study was aimed to evaluate antioxidant and antidiabetic potential of ginger extract and its characterization. Possible mode of action to elicit antidiabetic activity was also evaluated. METHODS AND RESULTS: Ethyl acetate extract of ginger (EAG) was evaluated for its antioxidant activity in terms of DPPH radical scavenging potential with an IC₅₀ value of 4.59 µg/ml. Antidiabetic activity of EAG was evaluated by estimating antiglycation potential (IC₅₀ 290.84 µg/ml). HPLC profiling of EAG revealed the presence of phenolic components, gingerol and shoagol as major constituents. After determining sub‐toxic concentration of EAG (50 µg/ml), efficacy of extract to enhance glucose uptake in cell lines were checked in L6 mouse myoblast and myotubes. EAG was effective at 5 µg/ml concentration in both cases. Antibody based studies in treated cells revealed the effect of EAG in expressing Glut 4 in cell surface membrane compared to control. CONCLUSION: The antidiabetic effect of ginger was experimentally proved in the study and has concluded that the activity is initiated by antioxidant, antiglycation and potential to express or transport Glut4 receptors from internal vesicles. Copyright © 2012 Society of Chemical Industry     

In vitro and in vivo antihyperglycemic effect of 2 amadori rearrangement compounds, arginyl-fructose and arginyl-fructosyl-glucose

During the heat processing of raw ginseng to produce red ginseng, amino acid derivatives such as arginyl-fructose (AF) and arginyl-fructosyl-glucose (AFG) are formed at high levels, through amadori rearrangement, the early step of Maillard reaction, from arginine and glucose or maltose, respectively. However, very limited information is available about the effect of the structural difference between AF and AFG on various biological activities. This is the first report of the mode of action and effect of AF and AFG on the type 2 diabetes management related inhibition of postprandial hyperglycemia in vitro and in animal model. In our previous study, standards AF and AFG were chemically synthesized and in this study their inhibitory activities against rat intestinal α-glucosidases and porcine pancreatic α-amylase were investigated in vitro. The IC(50) value of the in vitro inhibitory activity of AF and AFG on rat intestinal sucrase was high and in similar levels (6.40 and 6.20 mM, respectively). Additionally, a mild pancreatic α-amylase inhibitory activity was observed, with IC(50) values 36.30 and 37.60 mM for AF and AFG, respectively. The effect of AF and AFG on the postprandial blood glucose increase after meal was investigated in Sprague Dawley rats fed on starch or sucrose meals. Both amadori compounds significantly reduced the postprandial blood glucose levels after starch or sucrose loading. These results indicate that AF and AFG, Maillard reaction products, may have antidiabetic effect by suppressing carbohydrate absorption in the gastrointestinal level, and thereby reducing the postprandial increase of blood glucose.     

Effects of cooking methods on polyphenols,pigments and antioxidant activity in potato tubers

Potato tubers, which are one of the richest sources of antioxidants, are always cooked before human consumption. The objective of this study was to understand the effects of various domestic cooking methods, i.e., boiling, microwaving and baking on total phenolics, flavonoids, flavonols, lutein, anthocyanins and antioxidant activities in 5 cultivars and 9 advanced selections with different skin and flesh colors after 6 months of storage. The three cooking methods reduced the levels of these compounds and the percentage of DPPH (2,2-Diphenyl-1-pikryl-hydrazyl) radical scavenging activity in all the cultivars and selections. Boiling minimized these losses. Red fleshed tubers contained more flavonoids, whereas purple tubers contained more flavonols. Despite severe loss of these compounds due to cooking, both the flesh types retained larger amounts of all these compounds due to higher initial levels. Decline in the radical scavenging activity is directly related to loss of these compounds due to cooking treatments in all white and colored flesh tubers. Red and purple fleshed tubers exhibited greater radical scavenging activity than yellow and white fleshed tubers after each of the cooking treatments. Correction procedures were introduced to exclude interfering compounds (ascorbic acid, other oxidizing agents and reducing sugars) in Folin-Ciocalteu Reagent (FCR) assay of estimating total phenolics in potato.     

Protective effect of Perilla frutescens cv. Chookyoupjaso mutant water extract against oxidative injury in vitro and in vivo

The aim of this study was to elucidate the protective ability of the Perilla frutescens cv. Chookyoupjaso mutant water extract (PFWE) against oxidative injury in vitro and in vivo. In in vitro experiments, our results showed that PFWE indicated the intracellular reactive oxygen species (ROS) scavenging activity as well as cytoprotective effect in SIN-1-treated HepG2 cells. The intracellular ROS scavenging activity of PFWE was 44% at 50 μg/mL, 50% at 100 μg/mL, and 56% at 200 μg/mL. Furthermore, in vivo results showed that treatment with PFWE attenuated the activity of serum alkaline phosphatase (ALP) and lipid peroxidation increased by carbon tetrachloride (CCl₄) and also markedly recovered the activity of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), and glutathione reductase (GR) decreased by CCl₄ in BALB/c mice. GPx activity was elevated almost 3-fold compared to control group at 50 mg/kg of PFWE. The present study suggests that PFWE possesses significant protective effects against oxidative injury.     

产CLA乳酸菌体内、体外抑菌活性的研究

采用体内和体外抑菌法研究产CLA乳酸菌对大肠杆菌、金黄色葡萄球菌和沙门氏菌的抑菌作用。体外抑菌实验表明,乳酸菌发酵上清液对大肠杆菌的抑制作用最强,对沙门氏菌和金黄色葡萄球菌的抑制作用相对较弱。体外研究还发现,乳酸菌发酵液在pH<5.0时,抑菌效果较好,并且具一定的热稳定性,对过氧化氢酶和蛋白酶的抗性较高。体内抑菌实验表明,该乳酸菌能够有效降低以上三种致病菌引起的小鼠死亡率,且体内抑菌效果随剂量的增加而增强。结论:产CLA乳酸菌在体内和体外均有较好的抑菌效果。      

Effects of glucose, propionic acid, and nonessential amino acids on glucose metabolism and milk yield in Holstein dairy cows

Whole-body glucose rate of appearance (Ra) responses and milk lactose secretion were compared in dairy cows receiving duodenal infusions of glucose (Glc), a mixture of 5 nonessential amino acids (NEAAm), or ruminal infusions of propionic acid (C3). Four mid-lactation Holstein cows, fitted with both duodenum and rumen cannulas, were used in a 4 × 4 Latin square design with 14-d periods. Cows were fed a grass silage-based diet (Ctrl) that provided 88% of net energy of lactation and 122% of protein requirements. Concentrate was formulated with wheat (21.5%) and barley (20%) containing some starch. Isoenergetic infusions (5.15 Mcal/d of digestible energy) of Glc into the duodenum (7.7 mol/d), C3 into the rumen (14.1 mol/d), or NEAAm into the duodenum (in mol/d; Ala: 1.60; Asp: 0.60; Glu: 5.94; Gly: 1.22; Ser: 2.45) were given as a supplement to the Ctrl diet. During each period on d 13, [6,6-²H₂]glucose was infused into one jugular vein and blood samples were taken from the other jugular vein to measure glucose enrichment and determine Ra. Dry matter intake decreased slightly with the infusions (6%), but did not differ among them. Whole body glucose Ra averaged 502, 745, 600, and 576 mmol/h for Ctrl, Glc, C3, and NEAAm, respectively. It increased with the increase in energy supply (Ctrl vs. infusions) and differed according to the nutrients infused. The Ra response was higher with Glc and C3 than with NEAAm and higher with Glc than with C3. Plasma concentrations of insulin were not affected, but insulin-like growth factor 1 increased with infusions. Plasma glucagon increased with NEAAm, which could favor the increased Ra. Overall, milk lactose yield (137, 141, 142, and 130 mmol/h for Ctrl, Glc, C3, and NEAAm, respectively) was not modified by the infusions, but was lower with NEAAm compared with Glc and C3. Changes in lactose yield did not parallel the increase in Ra, and therefore the ratio of lactose yield to Ra decreased with the infusions and was lower in Glc compared with C3, suggesting a shift of glucose utilization away from lactose synthesis toward other pathways, including mammary metabolism. Intestinal Glc was the most efficient nutrient in terms of increasing glucose Ra; however, there was no direct link between the increases in whole body glucose Ra observed with the 3 types of nutrients and milk lactose yield.     

Effects of bacterial cellulose on glucose metabolism in an in vitro chyme model and its rheological evaluation

Hyperglycaemia affects the health of people worldwide. The study investigated the effects of bacterial cellulose (BC) on glucose metabolism using an in vitro chyme model, including glucose adsorption, glucose diffusion, kinetics model of glucose and rheological properties of BC. The results indicated that BC exhibited significant inhibition of α-amylase in a dose-dependent manner (IC₅₀ = 7.86 mg mL⁻¹) and could significantly adsorb glucose by binding to the glucose molecules (4.11 ± 0.18 mmol g⁻¹) (P < 0.05). The BC chyme system was a non-Newtonian fluid showing shear thinning and has the characteristics of elastic solid. The diffusion behaviour of glucose in the BC chyme system conformed to first-order release kinetics model, indicating its inhibition of glucose diffusion by changing the rheological properties of chyme. This study provides a theoretical basis for dietary intervention and nutritional support for patients with hyperglycaemia.