核桃肽生物活性的研究进展

综述了核桃肽的提取工艺及其抗氧化、抗疲劳、降血糖、免疫调节等生物活性。     

生物活性肽的生理功能及研究进展

随着人们生活水平的提高,伴随现代文明而来的各种富裕病如高血压、高血脂、肥胖病、糖尿病和癌症等越来越引起人们的关注,人们的消费观念已从单纯的吃饱吃好向防病治病方向转变。生物活性肽具有涉及神经、激素和免疫调节、抗血栓、抗高血压、抗胆固醇、抗细菌病毒、抗癌、抗氧化、清除自由基、改善氮素吸收关系和矿质运输、促生长、调节食品风味、口味、硬度等多种生理功能,被誉为21世纪人类健康的新宠儿。简述了生物活性肽的特点、生理功能及其研究进展。     

乳清蛋白生物活性肽研究进展

以乳清蛋白为原料,经过酶解或发酵等方法可以获得独特理化性质的生物活性肽。乳清蛋白生物活性肽来源广、活性强、分子量小,在食品和医药行业有很高的应用研究价值,已经成为研究热点。随着制备、分离纯化以及鉴定技术的不断发展和成熟,越来越多的乳清蛋白生物活性肽被发现。本研究主要综述了乳清蛋白生物活性肽的制备、分离纯化、鉴定方法以及生物功能,并展望了乳清蛋白生物活性肽应用前景,以期为功能性乳清蛋白生物活性肽产品的开发与应用提供参考。     

3个六肽的胰岛素受体结合和体内生物活性

为了研究胰岛素受体结合部位的结构和功能,设计并用固相方法合成了３个六肽．在浓度大于１×１０３ｎｍｏｌ／Ｌ时,ｃｙｃｌｏ（Ｐｈｅ－Ｐｈｅ－Ｖａｌ－Ｌｅｕ－Ｔｙｒ－Ｇｌｙ）具有明显的胰岛素受体结合活力;Ｈ－Ｐｈｅ－Ｐｈｅ－Ｖａｌ－Ｌｅｕ－Ｔｙｒ－Ｇｌｙ－ＯＨ的这一活力则不明显;而Ｈ－Ｇｌｙ－Ｇｌｕ－Ａｒｇ－Ｇｌｙ－Ｐｈｅ－Ｐｈｅ－ＯＨ则增强胰岛素和其受体的亲和性．然而,它们都没有体内生物活性．这表明：环六肽部分模拟了胰岛素受体结合部位的空间构象;胰岛素受体结合部位的疏水性和其中的Ｂ２３Ｇｌｙ－Ｂ２４Ｐｈｅ－Ｂ２５Ｐｈｅ对胰岛素和其受体的结合起重要作用．     

生物活性肽的辐射防护作用研究进展

对多种生物活性肽的辐射防护作用的研究进展进行了综述,为天然辐射防护剂的研发及临床应用提供科学依据。     

乳酪蛋白源生物活性肽的研究进展

酪蛋白是生物活性肽的重要来源,可以通过体内的胃肠消化和食品加工过程中的酶解将其释放出来。乳酪蛋白源的生物活性肽的生物学意义、对人类健康的影响和其在新型功能性食品加工中的作用具有重要的研究价值。     

生物活性低聚肽生理功能的研究进展

相比多肽,低聚肽具有优异的吸收机制与生物活性,本文主要从生物活性低聚肽生理功能的角度综述生物活性低聚肽的研究进展,并对生物活性低聚肽的研究前景进行了展望。     

生物活性肽抗氧化作用的研究进展

生物活性肽因其显著的抗氧化特性,在维护人体健康和抵御疾病方面展现出了巨大的应用潜力。文章针对近年来生物活性肽来源、抗氧化作用及相关机制、活性评价手段等方面的研究进行了简单的概括,旨在加深学界对生物活性肽抗氧化作用的理解,并为生物活性肽抗氧化作用的进一步研究和应用提供理论依据。     

长效多肽药物研究进展

重组蛋白药物在体内存留时间的长短,极大地影响到药物的使用剂量和治疗效果。防止多肽在体内迅速降解、延长半衰期成为蛋白质工程药物改造的重要课题之一。经过许多学者多年来的不懈研究,不少长效多肽药物已经上市,还有一些正在进行临床研究。综述了几种多肽药物常用的长效改造方法如化学修饰、基因融合、点突变以及药物制剂释放系统的改造。     

Conformational Analysis of the Thrombin Receptor Agonist Peptides SFLLR and SFLLR-NH2 by NMR: Evidence for a Cyclic Bioactive Conformation

The conformational properties of the pentapeptide Ser-Phe-Leu-Leu-Arg (P5), a human thrombin receptor-derived sequence forming part of a tethered ligand which activates the thrombin receptor, and its more active amide derivative Ser-Phe-Leu-Leu-Arg-NH₂ (P5-NH₂), have been studied by proton NMR spectroscopy in dimethylsulfoxide. Measurements of nuclear Overhauser effects, performed using two-dimensional rotating frame nuclear Overhauser (ROESY) and one-dimensional nuclear Overhauser enhancement (NOE) spectroscopy, revealed that P5 exists mainly in an extended conformation. However, proton–proton 1D-NOEs between Phe CH and Ser CH, Leu³ CH and Leu³ NH, and Leu⁴ CH and Leu⁴ NH, as well as between the Ser and Arg sidechains, also implicated a minor conformer for P5 having a curved backbone and a near-cyclic structure. In contrast to P5, measurements of NOEs and ROEs for P5-NH₂ revealed a more stabilized cyclic structure which may account for its higher biological potency. Thus strong interresidue sequential NH (i)–NH (i + 1) interactions, as well as C-terminal carboxamide to N-terminal side-chain interactions, i.e., Arg CONH₂ to Phe ring and Arg CONH₂ to Ser , observed at lower levels of the ROESY spectrum, supported a curved backbone structure for SFLLR-NH₂. Since the higher potaency P5-NH₂ analogue adopts predominantly a cyclic structure, a cyclic bioactive conformation for thrombin receptor agonist peptides is suggested.     

From short peptides to nanofibers to macromolecular assemblies in biomedicine

In the last few years, a variety of self-assembling short peptides that consist exclusively of simple amino acids have been designed and modified. These peptides exhibit self-assembling dynamic behaviors. At the molecular structural level, they form α-helical, β-sheet and β-hairpins structures in water. These structures further undergo spontaneous assembly to form nanofibers which aggregate into supramolecular scaffolds that entrap large volumes of water. Furthermore, nanostructures and supramolecular structures that self-organized from these short peptides also have a broad spectrum of biotechnological applications. They are useful as biological materials for 2D and 3D tissue cell cultures, regenerative and reparative medicine, tissue engineering as well as injectable drug delivery matrices that gel in situ. We have endeavored to do a comprehensive review of short peptides that form nanofibrous hydrogels. In particular, we have focused on recent advances in peptide assembly motifs and applications.     

植物内生真菌在医药开发上的应用研究及展望

本文主要概述了植物内生真菌及其生理活性物质研究的最新进展,而今,它们在医药领域的应用越来越受到人们的关注,植物内生真菌是新的天然药物的重要源泉,在新药开发上具有广阔的发展前景。     

Identification of a Peptide Mimic of Bioactive Gibberellins with Affinity to GA 2-Oxidase

Previously we reported the first example of peptide mimics of a small hydrophobic molecule, a phytohormone gibberellin. The second peptide mimic of gibberellin has been identified from random peptide libraries by its affinity to a type of catalyzing enzyme of gibberellins, which specifically recognizes bioactive gibberellins. These results suggest that even hydrophobic compounds can be mimicked by peptides.     

产高活性抗癌物质的粘细菌的定向筛选

粘细菌是一类复杂的具有多细胞行为的原核生物,属于革兰氏阴性菌。粘细菌能够产生丰富的活性物质,并且具有菌株特异性,为人类不断发现新的活性物质提供了广阔的前景。本文以3株肿瘤细胞系为筛选模型,采用MTT法,对370多株分离的粘细菌及其代谢产物进行定向筛选,获得六株产高活性物质的粘细菌,并根据《伯杰氏细菌鉴定手册》(第八版),初步把这六株菌株归属到属。     

内毒素结合肽模拟肽P11的体外活性研究

目的对从噬菌体展示随机肽库筛选获得的内毒素结合肽模拟肽进行体外拈抗内毒素活性鉴定。方法采用FMOC固相合成法化学合成内毒素结合肽模拟肽P11,并进行拮抗内毒素活性和细胞毒性测定。结果亲和ELISA检测显示P11与LPS有较高的亲和力,通过生长曲线和流式细胞学分析细胞周期显示P11对人U937细胞生长无明显影响。流式细胞检测显示P11呈剂量依赖性抑制FITC—LPS与人外周血单核细胞（PBMC）结合。细胞因子生成抑制实验显示10μg/mlP11可显著抑制LPS诱导PBMC和U937细胞TNF—αmRNA转录和蛋白表达。结论体外活性鉴定结果表明化学合成的模拟肽P11可抑制LPS诱导的炎性反应。     

Cell-penetrating peptides: Application in vaccine delivery

Recent years have seen a surge in interest in cell-penetrating peptides (CPP) as an efficient means for delivering therapeutic targets into cellular compartments. The cell membrane is impermeable to hydrophilic substances yet linking to CPP can facilitate delivery into cells. Thus the unique translocatory property of CPP ensures they remain an attractive carrier, with the capacity to deliver cargoes in an efficient manner having applications in drug delivery, gene transfer and DNA vaccination. Fundamental for an effective vaccine is the delivery of antigen epitopes to antigen-presenting cells, ensuing processing and presentation and induction of an immune response. Vaccination with proteins or synthetic peptides incorporating CTL epitopes have proven limited due to the failure for exogenous antigens to be presented efficiently to T cells. Linking of antigens to CPP overcomes such obstacles by facilitating cellular uptake, processing and presentation of exogenous antigen for the induction of potent immune responses. This review will encompass the various strategies for the delivery of whole proteins, T cell epitopes and preclinical studies utilizing CPP for cancer vaccines.     

Differential binding of ICln in platelets to integrin-derived activating and inhibitory peptides

The capacity of platelets to form a thrombus is mediated by integrin α_IIbβ₃. The cytoplasmic tail of α_IIb contains a highly conserved motif, ⁹⁸⁹KVGFFKR⁹⁹⁵, which plays a critical role in regulating integrin activation and acts as a recognition site for various intracellular proteins, e.g. CIB1, PP1, ICln and RN181. Previously, we demonstrated that a cell-permeable integrin-derived activating (IDA) peptide, KVGFFKR, induces platelet activation, whereas an integrin-derived inhibitory (IDI) peptide, KVGAAKR, is antithrombotic. To elucidate the molecular mechanism underlying these opposite effects we investigate the affinity of known integrin α_IIb binding proteins for the two immobilized peptides in dependence on the activation state of platelets by means of peptide-affinity chromatography, blotting techniques and protein:peptide docking studies.Our results provide a model for the inhibition of ICln interaction with the integrin in activated platelets by the IDI-peptide. Thus, ICln:IDI-peptide interaction profiles can have a pivotal purpose in the search for consensus pharmacophores specifically inhibiting ICln function in platelets potentially leading to the development of integrin-derived antithrombotic drugs.     

The specific T-cell response to antigenic peptides is influenced by bystander peptides

T lymphocytes recognize antigens in the form of peptides presented by major histocompatibility complex (MHC) molecules on the cell surface. Only a small proportion of MHC class I and class II molecules are loaded with foreign antigenic peptides; the vast majority are loaded with thousands of different self peptides. It was suggested that MHC molecules presenting self peptides may serve either to decrease (antagonistic effect) or increase (synergistic effect) the T cell response to a specific antigen. Here, we present our finding that transfected mouse fibroblasts presenting a single antigenic peptide covalently bound to a class II MHC molecule stimulated specific mouse T cell hybridoma cells to an interleukin-2 response less efficiently than fibroblasts presenting a similar amount of antigenic peptide in the presence of class II molecules loaded with heterogenous bystander peptides.