食源性生物活性肽对2型糖尿病的干预作用及其机制研究进展

2型糖尿病属于非胰岛素依赖性糖尿病,全世界每年有数百万人患2型糖尿病或成为潜在患者。食源性活性肽不仅具有基本的营养优势,而且更易被机体吸收,有研究证实生物活性肽可以抑制与2型糖尿病相关的代谢酶活力,促进肠促胰岛素分泌,改善胰岛素抵抗,因此可以作为有效管理该疾病的功能性食品或药物。本文综述了食源性生物活性肽的特性和来源,以及目前其关于调节血糖作用机制的研究进展,归纳了食源性代谢酶调节剂的相关研究,以期为食源性生物活性肽的进一步研究提供参考。     

Bitter melon (Momordica charantia): a natural healthy vegetable

Bitter melon provides health benefits against various ailments for improving the quality of life. It is nutrient dense plant-based food containing versatility of bioactive compounds such as alkaloids, polypeptide, vitamins, and minerals. Owing to presence of bioactive compounds, it has the ability to fight against various lifestyle related disorders, e.g. cancer insurgence, diabetes mellitus, abdominal pain, kidney (stone), fever, and scabies. Amongst bioactive moieties, p-insulin is similar to insulin whose subcutaneous injection significantly lower blood glucose levels in diabetic patients. It also contains steroidal saponins called charantin, act alike peptides and certain alkaloids that effectively control sugar level in blood. The therapeutic perspectives have been also highlighted as they are helpful in regulating blood cholesterol thus protecting the body from cardiovascular disorders like atherosclerosis. Whole fruit, seeds and leaves of bitter melon regulates impaired antioxidant status and suppress fat accumulation. Moreover, curative potential of its bioactive components and their utilization in value added food products are also the limelight of article.     

禽蛋源生物活性肽的研究进展

禽蛋蛋白质具有多种功能和生物活性,是制备生物活性肽的潜在前体物质。众多研究已证实禽蛋源多肽是一类很有前景的保健食品和功能性食品成分,除含传统的营养价值之外,还因其众多的生物活性而广受青睐,如抗氧化、降血压、抗菌、抗病毒、抗癌、抗糖尿病、抗炎、金属离子结合与转运、免疫调节、改善骨骼健康等。本文综述了禽蛋源生物活性肽的制备、鉴定、功能活性及胃肠道消化吸收与转运方面的研究进展,并对后续的研究趋势和实际应用过程中所面临的问题进行了展望,以期为禽蛋源生物活性肽后续的深入研究与应用开发提供一定的参考。     

Peptides Derived from Foods as Supportive Diet Components in the Prevention of Metabolic Syndrome

Metabolic syndrome (MSyn) includes physiological, biochemical, clinical, and metabolic abnormalities, leading to an increase in health problems like obesity, dyslipidemia, cardiovascular diseases, and diabetes, which contribute to an increase in mortality rate. One of the main factors having a key impact on our health is the food we consume. Thus, scientists work towards the discovery of novel bioactive compounds with therapeutic potential to address MSyn. According to scientific reports, peptides derived from food proteins exhibit bioactivities important for the prevention of MSyn diseases; that is, they regulate blood pressure and glycemia; reduce cholesterol level and body mass; and scavenge free radicals. The aim of this review is to study the potential role of peptides in the prevention of MSyn. Particularly peptides which exhibit the following activities: antihypertensive [angiotensin‐converting enzyme (ACE) inhibition (EC 3.4.15.1)], antidiabetic [dipeptidyl peptidase IV (DPP‐IV) (EC 3.4.14.5)/α‐glucosidase (EC 3.2.1.20)/α‐amylase (EC 3.2.1.1) inhibition)], cholesterol level reduction, antioxidative, and obesity prevention, were studied. If possible, special attention is paid in the review to the bioactivities of peptides that were measured in vivo. Some examples of peptides showing dual or multiple action against MSyn targets are presented. Moreover, using the database of bioactive peptide sequences (BIOPEP) we made a list of peptides serving simultaneous functions in counteracting MSyn dysfunctions. Such an approach may simplify the discovery of MSyn preventive peptides, as well as highlight some of them as potent bioactive ingredients that may be incorporated into foods. Moreover, the research strategy involving the in silico and in vitro/in vivo methodologies may be useful in the production of food protein hydrolysates supporting the treatment of MSyn dysfunctions.     

植物源生物活性肽的研究进展

生物活性肽是一类对生物机体有益且易被机体吸收的小分子聚合物,是由2～20个氨基酸组成的蛋白质片段,其功能性质由氨基酸组成和排列顺序决定。植物是生物活性肽的天然宝库,植物源生物活性肽种类丰富、结构新颖,是近年来的研究热点。生物活性肽被视为营养保健品和功能食品成分,除了含有丰富的营养价值之外,还具有抗氧化、降血压、抑菌、降血脂和维持血糖水平平衡等功能,可利用其功能治疗、控制和预防慢性疾病,对食品、医药和美容等领域的发展具有重要意义。本文综述了近5年从植物中获取生物活性肽的最新进展,系统地总结了抗氧化肽、降压肽、抗菌肽、降血糖肽和降血脂肽的作用机制,与目前最常见的健康问题进行对应说明。对生物活性肽的制备方法、分离纯化和鉴定技术进行总结比较,并对生物活性肽的未来发展趋势以及在实际应用中遇到的问题进行展望,为未来植物源生物活性肽的进一步研究开发与应用提供参考。     

Recently isolated antidiabetic hydrolysates and peptides from multiple food sources: a review

Abstract

Diabetes, a metabolic syndrome of global importance has been on a progressive rise in recent years. Several pharmacological approaches have been made, which have proved effective, but with underlying side effects. Bioactive hydrolysates (BHs) and peptides (BPs) from food sources, however, have shown the relative advantage of imparting less adverse effects. Furthermore, BHs and BPs from food have been discovered to impart their antidiabetic potentials through one or more mechanisms such as inhibition of digestive enzymes, inhibition of the antigenic enzyme – Dipeptyl peptidase IV (DPP-IV), decrease in blood glucose levels and increase in insulin uptake. Several plants and animal sources have been used as protein sources for the isolation of antidiabetic hydrolysates and peptides through different mechanisms and analytical techniques. This review integrates recent research information about several popular and unconventional food sources of BHs and BPs, their isolation techniques, antidiabetic effects and protein profiles. In addition, the fractionation technique(s) employed in each study and inhibition potentials of BHs and BPs are reviewed. This article is intended to supplement accessible scholarly literature and intellectual awareness on the subject of food-oriented approach for the management of diabetes.     

浙江七叶和汕美2号南瓜降血糖作用研究

研究并比较浙江七叶和汕美2号南瓜栽培品种对四氧嘧啶糖尿病小鼠降血糖作用。采用尾静脉注射四氧嘧啶建立小鼠糖尿病模型,灌胃南瓜提取物治疗7 d后测定小鼠空腹血糖和餐后血糖值、肝糖原、胰岛素、TG、TC、MDA含量和SOD活力水平。两种南瓜均对糖尿病小鼠有一定治疗效果,各提取部位均能显著降低糖尿病小鼠空腹血糖值和MDA含量,同时显著升高肝糖元、胰岛素含量及SOD活力水平,但对餐后血糖值影响不显著。且对各指标的影响,浙江七叶南瓜和汕美2号南瓜各部位提取物表现不同,浙江七叶南瓜提取物对糖尿病小鼠空腹血糖、肝糖原、SOD、MDA等指标的改善作用强于汕美2号南瓜提取物,而对TG与胰岛素含量的影响作用则相反。结果表明,南瓜治疗糖尿病的作用机制很可能是通过修复受损的胰岛β细胞使其恢复正常的分泌功能或是促进肝糖元合成及糖类转化有关,且与调节小鼠体内氧化应激作用有紧密的联系。      

In vitro antidiabetic and antihypercholesterolemic activities of camel milk protein hydrolysates derived upon simulated gastrointestinal digestion of milk from different camel breeds

Milk protein hydrolysates derived from 4 camel breeds (Pakistani, Saheli, Hozami, and Omani) were evaluated for in vitro inhibition of antidiabetic enzymatic markers (dipeptidyl peptidase IV and α-amylase) and antihypercholesterolemic enzymatic markers (pancreatic lipase and cholesterol esterase). Milk samples were subjected to in vitro simulated gastric (SGD) and gastrointestinal digestion (SGID) conditions. In comparison with intact milk proteins, the SGD-derived milk protein hydrolysates showed enhanced inhibition of α-amylase, dipeptidyl peptidase IV, pancreatic lipase, and cholesterol esterase as reflected by lower half-maximal inhibitory concentration values. Overall, milk protein hydrolysates derived from the milk of Hozami and Omani camel breeds displayed higher inhibition of different enzymatic markers compared with milk protein hydrolysates from Pakistani and Saheli breeds. In vitro SGD and SGID processes significantly increased the bioactive properties of milk from all camel breeds. Milk protein hydrolysates from different camel breeds showed significant variations for inhibition of antidiabetic and antihypercholesterolemic enzymatic markers, suggesting the importance of breed selection for production of bioactive peptides. However, further studies on identifying the peptides generated upon SGD and SGID of milk from different camel breeds are needed.     

n-3多不饱和脂肪酸对不同饲料喂养大鼠血糖及血脂的影响

目的:考察n-3多不饱和脂肪酸对不同饲料喂养大鼠血糖、胰岛素及血脂的影响。方法:将SD大鼠随机分成14个组,分别为:空白对照组（普通饲料喂养）,高糖高脂对照组（高糖高脂饲料喂养）,普通饲料喂养的α-亚麻酸和深海鱼油高、中、低剂量组,高糖高脂饲料喂养的α-亚麻酸和深海鱼油高、中、低剂量组。α-亚麻酸和深海鱼油高、中、低剂量组分别灌胃150、300、600mg/kg的α-亚麻酸和深海鱼油。连续灌胃8周后,分别对各组大鼠的血糖、胰岛素和血脂四项进行测定。结果:α-亚麻酸对不同饲料喂养大鼠的血糖、胰岛素以及血脂都没有影响。与空白对照组相比,深海鱼油能使大鼠空腹血糖浓度明显升高（p<0.05）,空腹胰岛素浓度明显降低（p<0.05）。深海鱼油对TG和HDL-C无影响;但是深海鱼油能使高糖高脂饲料喂养大鼠的TC和LDL-C呈下降趋势,其中TC的水平下降具有显著性差异（与高糖高脂对照组相比,p<0.05）。结论:在150⁶00mg/kg的灌胃剂量下,α-亚麻酸对大鼠的血糖、胰岛素以及血脂都没有影响;深海鱼油对不同饲料喂养大鼠都有抑制胰岛素分泌和升高血糖的作用,同时对高糖高脂饲料喂养导致的大鼠TC水平升高有降低作用。      

Bioactive peptides from nuts: A review

Oxidative stress occurs because of an imbalance in the production of reactive oxygen species. Nuts are rich in bioactive compounds, including phenolic compounds, tannins, and phytosterols. Although nuts are widely consumed because of their beneficial effects on nutrition and health, there is limited information about bioactive peptides from nuts. Pine nut and walnut-derived peptides are the most studied because these nuts contain a higher amount of protein. Different biological activities have been demonstrated for nut peptides; many of them exhibit antioxidant, anticancer, antihypertensive, antidiabetic, immunomodulatory, antiseizure, or neuroprotective activity. Recent studies have focused on increasing the bioactivity of identified bioactive peptides by applying new technologies and chemosynthetic strategies. Research tendency points to the generation of peptides with specific sequences for application in specific diseases. Nut bioactive peptides can become key functional ingredients for food, pharmaceuticals, or cosmetics.     

Xylitol Improves Pancreatic Islets Morphology to Ameliorate Type 2 Diabetes in Rats: A Dose Response Study

Xylitol has been reported as a potential antidiabetic sweetener in a number of recent studies; however, the most effective dietary dose and organ‐specific effects are still unclear. Six‐week‐old male Sprague‐Dawley rats were randomly divided into 5 groups: normal control (NC), diabetic control (DBC), diabetic xylitol 2.5% (DXL2.5), diabetic xylitol 5.0% (DXL5), and diabetic xylitol 10.0% (DXL10). Diabetes was induced only in the animals in DBC and DXL groups and considered diabetic when their nonfasting blood glucose level was >300 mg/dL. The DXL groups were fed with 2.5%, 5.0%, and 10% xylitol solution, whereas the NC and DBC groups were supplied with normal drinking water. After 4‐wk intervention, body weight, food and fluid intake, blood glucose, serum fructosamine, liver glycogen, serum alanine transaminase, aspartate transaminase, lactate dehydrogenase, creatine kinase, uric acid, creatinine, and most serum lipids were significantly decreased, and serum insulin concentration, glucose tolerance ability, and pancreatic islets morphology were significantly improved in the DXL10 group compared to the DBC group. The data of this study suggest that 10% xylitol has the better antidiabetic effects compared to 2.5% and 5.0% and it can be used as an excellent antidiabetic sweetener and food supplement in antidiabetic foods.     

Bioactive Peptides Derived from Seaweed Protein and Their Health Benefits: Antihypertensive,Antioxidant, and Antidiabetic Properties

Cardiovascular diseases and diabetes are the biggest causes of death globally. Therefore, prevention of these diseases is a focus of pharmaceuticals and functional food manufacturers. This review summarizes recent research trends and scientific knowledge in seaweed protein‐derived peptides with particular emphasis on production, isolation and potential health impacts in prevention of hypertension, diabetes and oxidative stress. The current status and future prospects of bioactive peptides are also discussed. Bioactive peptides have strong potential for use in therapeutic drug and functional food formulation in health management strategy, especially cardiovascular disease and diabetes. Seaweeds can be used as sustainable protein sources in the production of these peptide‐based drugs and functional foods for preventing such diseases. Many studies have reported that peptides showing angiotensin converting enzyme inhibition, antihypertensive, antioxidative and antidiabetics activities, have been successfully isolated from seaweed. However, further research is needed in large‐scale production of these peptides, efficient isolation methods, interactions with functional foods and other pharmaceuticals, and their ease to digestion in in vivo studies and safety to validate the health benefits of these peptides.     

Bioactive Natural Constituents from Food Sources—Potential Use in Hypertension Prevention and Treatment

Prevention and management of hypertension are the major public health challenges worldwide. Uncontrolled high blood pressure may lead to a shortened life expectancy and a higher morbidity due to a high risk of cardiovascular complications such as coronary heart disease (which leads to heart attack) and stroke, congestive heart failure, heart rhythm irregularities, and kidney failure etc. In recent years, it has been recognized that many dietary constituents may contribute to human cardiovascular health. There has been an increased focus on identifying these natural components of foods, describing their physiological activities and mechanisms of actions. Grain, vegetables, fruits, milk, cheese, meat, chicken, egg, fish, soybean, tea, wine, mushrooms, and lactic acid bacteria are various food sources with potential antihypertensive effects. Their main bioactive constituents include angiotensin I-converting enzyme (ACE) inhibitory peptides, vitamins C and E, flavonoids, flavanols, cathecins, anthocyanins, phenolic acids, polyphenols, tannins, resveratrol, polysaccharides, fiber, saponin, sterols, as well as K, Ca, and P. They may reduce blood pressure by different mechanisms, such as ACE inhibition effect, antioxidant, vasodilatory, opiate-like, Ca²⁺ channel blocking, and chymase inhibitory activities. These functional foods may provide new therapeutic applications for hypertension prevention and treatment, and contribute to a healthy cardiovascular population. The present review summarizes the antihypertensive food sources and their bioactive constituents, as well as physiological mechanisms of dietary products, especially focusing on ACE inhibitory activity.     

Antihypertensive peptides of animal origin: A review

Many bioactive peptides trigger certain useful antihypertensive activities in the living body system and there is a mounting worldwide interest in the therapeutic potential of these bioactive peptides for exploitation in vivo against the hypertension. Studies suggest the antihypertensive properties for many bioactive peptides of animal origin with underlying mechanisms ranging from inhibition of angiotensin-converting enzyme to additional mechanisms to lower blood pressure such as opioid-like activities and mineral-binding and antithrombotic properties. Antihypertensive peptides are the most extensively studied of all the bioactivities induced by food protein hydrolysates, highlighting their importance in human health and disease prevention and treatment. There exist enormous opportunities for the production of novel peptide-based products in biopharmaceutical manufacturing industries for the treatment, prevention, and mitigation of hypertension. Numerous products have already struck on the global market and many more are in process. This article focuses on antihypertensive peptides identified in the meat, fish, blood, milk, dairy products, and egg and their probable application as novel ingredients in the development of functional food products as dietary treatment of hypertension.     

Pumpkin oil cake protein as a new carrier for encapsulation incorporated in food matrix: Effect of processing,storage and in vitro digestion on bioactivity

In this paper, valorisation of pumpkin oil cake as source of new protein carrier material for encapsulation was examined in order to enrich real food products. Cookies were used as a model system for addition of encapsulates at three different levels: 10%, 15% and 20%. The physicochemical and sensory properties were investigated, as well as conditions of stability after storage, in terms of total phenolic and betalain content. Furthermore, antioxidant, α-glucosidase and ACE inhibitory potential of cookies was evaluated after simulated gastrointestinal digestion. The cookies showed good technological quality as well as acceptable sensorial properties. The addition of encapsulate increases the total phenolic and betalain contents and shoved significant stability during storage time. Novel peptides were produced after gastrointestinal digestion, which enhanced bioactive properties of enriched products through synergistic action with active compounds from beetroot juice. Obtained digest shoved significant antioxidant, antidiabetic and antihypertension activities, hence ensuring a potential healing effect that could be reached by consuming these cookies.     

Plant proteases for bioactive peptides release: A review

ABSTRACT

Proteins are a potential source of health-promoting biomolecules with medical, nutraceutical, and food applications. Nowadays, bioactive peptides production, its isolation, characterization, and strategies for its delivery to target sites are a matter of intensive research. In vitro and in vivo studies regarding the bioactivity of peptides has generated strong evidence of their health benefits. Dairy proteins are considered the richest source of bioactive peptides, however proteins from animal and vegetable origin also have been shown to be important sources. Enzymatic hydrolysis has been the process most commonly used for bioactive peptide production. Most commercial enzymatic preparations frequently used are from animal (e.g., trypsin and pepsin) and microbial (e.g., Alcalase® and Neutrase®) sources. Although the use of plant proteases is still relatively limited to papain and bromelain from papaya and pineapple, respectively, the application of new plant proteases is increasing. This review presents the latest knowledge in the use and diversity of plant proteases for bioactive peptides release from food proteins including both available commercial plant proteases as well as new potential plant sources. Furthermore, the properties of peptides released by plant proteases and health benefits associated in the control of disorders such as hypertension, diabetes, obesity, and cancer are reviewed.     

Bioactive peptide production by hydrolysis of porcine blood proteins in a continuous enzymatic membrane reactor

BACKGROUND: During slaughter a hog produces approximately 3 L of blood. However, only a small proportion of porcine blood is currently used in food, feed or fertiliser, most of it being treated as waste and discarded. In this study the possibility of hydrolysing porcine blood proteins by enzyme in a membrane reactor for the production of bioactive peptides was investigated. Red blood corpuscles, blood plasma and defibrinated blood plasma were hydrolysed by various proteases, and the hydrolysates were evaluated for bioactive properties. RESULTS: The hydrolysate produced by hydrolysing red blood corpuscles with a mixture of trypsin, chymotrypsin and thermolysin had the highest angiotensin I‐converting enzyme (ACE)‐inhibitory activity (IC₅₀ = 0.58 mg mL^?1) and scavenging effect on α,α‐diphenyl‐β‐picrylhydrazyl (DPPH) (65%) after 6 and 10 h of hydrolysis respectively. When the hydrolysis was carried out in an enzymatic membrane reactor with an enzyme/substrate ratio of 1:5 and a residence time of 100 min, the process reached steady state in 2 h. The ACE‐inhibitory activity of the product during the steady state process was 86% and its scavenging effect on DPPH was 54%. The membrane process also decolourised the enzyme‐hydrolysed product, thus improving the appearance of the product. CONCLUSION: This study demonstrated that hydrolysates of porcine blood possess antihypertensive and antioxidant activities. Using red blood corpuscles as the substrate, the hydrolysis could be carried out in a membrane reactor with a mixture of proteases to produce bioactive peptides continuously. Therefore processing of porcine blood in an enzymatic membrane reactor is a potential method for producing a health‐promoting product. Copyright © 2008 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.     

Management of diabetic complications through fruit flavonoids as a natural remedy

Diabetes mellitus is a global disorder, and a major issue for health care systems. The current review outlooks the use of fruit flavonoids as natural remedy in the prevention of diabetes mellitus. The onset of diabetes mainly depends upon genetics and lifestyle issues. Currently used therapeutic options for the control of diabetes, like dietary amendments, oral hypoglycemic drugs, and insulin, have their own limitations. Fruit flavonoids possess various antidiabetic, anti-inflammatory, and antioxidant potentials and act on various cellular signaling pathways in pancreas, white adipose tissue, skeletal muscle, and liver function, which in result induces antidiabetic effects. Recently, antidiabetic effect of fruit flavonoids has been studied using various animal models and clinical trials. Research studies revealed a statistically significant potential of fruit flavonoids in managing the altered glucose and oxidative metabolisms in diabetes. Unlike synthetic antidiabetic agents, fruit flavonoids manage diabetes without compromising cellular homeostasis thereby posing no side effects. Further studies are required in purification and characterization of different fruit flavonoids with respect to their beneficial effect for diabetic patients.     

Whey as a source of peptides with remarkable biological activities

The dairy industry generates increased amounts of whey from both cheese and casein production facilities. Whey presents an elevated content of lactose and proteins, which are associated with its high biological oxygen demand and decomposing potential. Despite its potential as pollutant, whey has been considered as a dairy by-product due to its nutritional, functional and bioactive properties. The use of enzyme technology may be an interesting strategy to convert whey into added-value products. The hydrolysis of whey proteins can generate bioactive peptides, which are described to perform physiological effects in vivo, such as antioxidant, antimicrobial, antihypertensive and antidiabetic activities. Bioactive peptides derived from whey proteins have been also associated with immunomodulatory, anticancer, opioid and hypocholesterolemic activities. This review presents a discussion on the main biological activities of peptides derived from whey proteins.