生物活性肽及其研究进展

生物活性肽来源广泛,目前已成为世界范围内的研究热点。生物活性肽具有显著的生理功能,如神经调节、激素作用、免疫调节、抗血栓、抗高血压、降胆固醇、抑菌、抗病毒、抗癌、抗氧化作用等,被誉为21世纪人类健康的新宠儿。本文综述了生物活性肽的种类、生理功能、吸收、制备、分离及研究进展,以期为生物活性肽的进一步研究和应用提供参考。     

海洋生物活性肽及其生物活性研究进展

概述存在于海绵、海鞘等海洋低等生物和海洋鱼贝类中的生物活性肽，以及这些活性肽的抗肿瘤、抗菌、抗高血压及抗氧化等生物活性的研究进展。     

甜杏仁的药理作用研究进展

甜杏仁广泛应用于食品工业、医药和保健领域,具有多样的生物活性和药理作用.其多种活性成分如多元酚酸类、黄酮类、天然维生素E和不饱和脂肪酸类物质已被现代研究证实是甜杏仁中重要的药理活性成分.甜杏仁及其提取物具有抗氧化、抗肿瘤、抗真菌、肝脏保护、抗糖尿病和抗高血脂等药理作用.综述了近年来国内外关于甜杏仁及其不同提取物药理作用...     

鸡源性活性肽的研究进展

随着我国鸡养殖和加工能力的提高,人们不仅追求鸡肉来源的营养成分,同时更需要提高其保健价值,其中鸡源性活性肽的生物活性及产业化应用备受人们关注.鸡源性活性肽不仅具有不同于蛋白质及氨基酸的消化吸收特性,还具有抗氧化、抗炎、免疫调节等诸多生物活性.此外,鸡肉加工副产物鸡骨、鸡皮、鸡血及鸡内脏等也是制备活性肽的主要原料,因而极...     

肌肽在医药领域的应用及其研究概况

肽是一种由氨基酸组成的生物大分子。近年来,随着分子生物学的发展,大大促进了生物学与医学、药学等各学科之间的相互渗透,肽也因此而成为非常重要的生化药物,越来越多地应用于临床,且已显示出了良好效果。其中人们对激素类活性肽如下丘脑、垂体、胃肠道等分泌的一些肽类物质研究的较早且成果较多,相应的药物也已临床应用到了高血压、糖尿病、癌症、胃肠道病、精神病等疾病的预防及诊疗。     

海绵的生物活性研究新进展

海洋物种是生物多样性的来源,能够产生结构多样、生物活性多样的次生代谢物。海绵是其中最丰富的天然产物来源,其药理活性丰富,具有极高的临床应用价值,被认为是药物宝库。目前人们已经发现其具有抗肿瘤、抗病毒、抗菌、抗氧化、抗炎、免疫调节等生物活性。多年来,对海绵的化学成分研究较多,但对其丰富的生物活性研究相对较少。对海绵次生代谢物的生物活性研究现状进行综述,以期发现活性较好的化合物,为新药开发提供依据。此外,还从药物开发领域对进入临床实验的海绵衍生化合物成药性、成本效益等进行讨论。     

褐藻多糖生物活性的研究进展

海藻类的生物活性引起了人们的广泛关注,尤其是对褐藻多糖的研究。海藻多糖是海洋中最重要的药理活性物质之一,而且资源丰富,容易获取。对褐藻多糖以及生物活性的研究,已有较多的报道,并取得较大的进展。褐藻多糖虽在组成和化学结构上存在差异,但在生物活性方面有很多的相似性,如大多具有抗肿瘤、抗氧化、抗菌、调节免疫和抗炎活性、保湿等作用。     

棕矢车菊素的药理作用及其作用机制的研究进展

棕矢车菊素是主要存在于艾叶、野马追中的具有药理活性的黄酮类化合物,是一种多靶点的药物,具有抗氧化、抗癌、抗菌、抗炎、抗过敏等多种生物活性。对棕矢车菊素的抗肿瘤、抗炎、抗菌、降血糖、免疫抑制等多种药理活性及其作用机制进行综述,以期为其开发应用提供理论依据。     

海带多糖药理作用研究进展

海带多糖是海带中主要的生物活性成分,具有多方面的药理活性,如抗血栓、调血脂、降血糖、改善血流变及循环、抗肿瘤、抗辐射、免疫调节、抗氧化、抗突变、抗疲劳、抗炎及保护肝脏等作用,综述了近年来对海带多糖的药理作用研究进展.     

荔枝和荔枝核的化学成分、生物活性及药理作用研究

主要综述了近年荔枝及荔枝核的化学成分、生物活性及药理作用研究进展.目前,已从荔枝和荔枝核中分离出多糖、总皂苷和黄酮类化合物等活性成分.研究证明,荔枝和荔枝核及其活性成分除具有阻断亚硝胺合成及清除亚硝酸根离子、抗氧化和清除自由基以及抑制HBsAg,HBeAg和HBV-DNA等的生物活性外,还有抗炎、止痛、退热和抑制小鼠移植性肿瘤、对抗免疫性和急性肝损伤、降血糖、调血脂、抗氧化和增强胰岛素抵抗模型大鼠胰岛素敏感性等药理作用.提出应加强对其主要活性成分、有效部位的确定;继续深入开展有效成分对代谢综合征和胰岛素抵抗-炎症作用的药理研究;采用＂血清药理学＂方法,观察药物对转染乙肝病毒2.2.15细胞株病毒表达作用以及动物体内实验等研究.     

Novel pharmacological targets from Indian cone snails

The oceans are a source of combinatorial library of unique natural products, 'not found in the terrestrial environment'. Marine invertebrates such as sponges, molluscs, bryozoans, tunicates (Urochordata) and their associated microorganisms are the major representatives of promising bioactive compounds. Among these, the predatory molluscan cone snails have evolved with highly structured small and complex array of peptides (more than 50,000) linked to their prey capture and defence. These peptides have become a valuable source of neuro pharmacological targets as many of them selectively modulate ion channels and transporters. A group of scientists from United States, Europe, Australia, Israel and China have been characterized drugs for neuropathic pain and pharmacological targets from the peptides of a few cone snail species. Several are now in Clinical and preclinical development. Less than 1% of the cono peptides are pharmacologically characterized. India has a diversity of 20-30% of total cone snail species distributed worldwide. A group of Indian Scientists have made promising drug discovery programs from Conus peptides. This review will focus on the Conus peptides from Indian cone snails species, their neuro pharmacological targets and future directions.     

Advancements in the anti-diabetes chemotherapeutics based on amino acids, peptides, and peptidomimetics

Diabetes Mellitus (DM) is a highly prevalent chronic disease. Recent years have witnessed development of many new oral drugs; novel insulin analogs and their delivery systems for the treatment of patients with either type-1 or type-2 DM. The impetus for developing new antidiabetic drugs comes from the unmet need of pharmacological tools that allow diabetic patients to achieve recommended glucose control targets by precise, safe and effective ways. The number of people afflicted with DM worldwide has increased considerably in recent years and is projected to increase dramatically over the next decades. In the recent times, design and synthesis of bioactive peptides and peptidomimetics has undergone a paradigm shift. Non-proteinogenic amino acids, peptides and peptidomimetics are emerging as novel drug candidates for the treatment of various diseases and/or disorders. This review mainly discusses the advancements in the usage of unnatural amino acids, peptides and peptidomimetics as potential therapeutic agents for the treatment of DM.     

Short peptide modules for enhancing intestinal barrier function

The intestinal epithelial barrier is indispensable to our immune system. Defects in this barrier function have been observed in intestinal disorders such as inflammatory bowel diseases, food allergies, and celiac diseases. Therefore, the modulation of the barrier function is currently viewed as a potentially positive pharmacological outcome. This review describes a unique peptide, Asn-Pro-Trp- Asp-Gln (NPWDQ), which can finely adjust the intestinal barrier. It is obtained by the hydrolysis of casein, a major milk protein, and considerably inhibits the permeation of ovalbumin, one of the food allergens, in Caco-2, a human intestinal cell line. Using DNA microarray, we observed that NPWDQ only up-regulated expression of the occludin gene, whereas the levels of other genes, such as those of the claudin and zonula occludens families, remained unchanged. Increased protein expression of occludin was also observed. The fact that milk-derived peptide(s) can enhance intestinal barrier function gives a new significance to lactation because it plays an important role in promoting the maturation of the intestinal barrier. In this context, it is highly probable and worthy of considerable attention that various bioactive peptides with this type of activity are yet to be observed in the bovine and/or human casein sequence. Moreover, milkderived peptides could be considered as potential candidates for the prevention of certain intestinal disorders.     

Preparation of peptide and protein powders for inhalation

Innovations in biotechnology and recombinant techniques have led to a large increase in the number of macromolecule drugs developed over the last several years. These molecules are enabling new therapies for many previously untreated or poorly treated diseases. Due to poor oral absorption, most biopharmaceuticals are delivered by injection. Medical science, health care providers and consumers have been searching for alternative methods of delivering macromolecule drugs. Animal and human clinical studies have demonstrated that pharmacological doses of bioactive peptides and proteins pass, by a natural biological process, from the lungs into the bloodstream or local tissue. New macromolecule drugs are also being developed for treatment of respiratory diseases such as cystic fibrosis, adult and infant respiratory distress syndromes, asthma and emphysema. This paper reviews formulations for delivering therapeutic aerosols to the lungs. Particular emphasis will be placed on preparing fine powders containing macromolecule drugs.     

红景天苷及其类似物合成研究进展

红景天苷为景天科植物红景天的主要活性成分。研究发现,红景天苷具有抗缺氧、抗疲劳、抗微波辐射、兴奋中枢神经和调节内分泌等药理活性,由于其结构简单,毒性小,广泛的药理活性而倍受人们的关注。笔者从化学合成和生物合成两个方面对红景天苷及其类似物的合成进行了综述。     

延长溶栓药物半衰期的策略研究

血栓性疾病是近年来人类健康的头号杀手,其临床治疗一直备受关注。以溶栓药物为基础的溶栓疗法虽可以有效治疗血栓性疾病,但存在药物半衰期短和给药频繁等问题。延长药物半衰期对将来溶栓药物的发展尤为重要。本文系统分析现有溶栓药物半衰期的影响因素和相应的解决策略,为将来的药物改造提供一定的理论指导。     

呋咱氮氧化物类一氧化氮供体型药物的研究进展

一氧化氮作为生物信使或效应分子在体内发挥重要的生理作用,且其体内水平异常与多种疾病的发生和发展密切相关。因此,一氧化氮供体型药物的研究备受关注。呋咱氮氧化合物即是一类重要的一氧化氮供体,其与某些药物分子偶联而合成的一氧化氮供体型药物可提高药物的药理活性。综述具不同药理作用的呋咱氮氧化物类一氧化氮供体型药物的研究进展。     

Lyotropic liquid crystal systems in drug delivery

Lyotropic liquid crystal systems, such as reversed bicontinuous cubic and hexagonal mesophases, are attracting more and more attention because of their unique microstructures and physicochemical properties. Various bioactive molecules such as chemical drugs, peptides and proteins can be solubilized in either aqueous or oil phase and be protected from hydrolysis or oxidation. Furthermore, several studies have demonstrated sustained release of bioactive molecules from reversed cubic and hexagonal mesophases. This article gives an overview of recent advances and current status of reversed cubic and hexagonal mesophases, especially with respect to their preparation methods and applications in the field of drug delivery. In addition, potential problems and possible future research directions are highlighted.     

抗菌肽药物的局限性及应对策略

随着多重耐药的病原体数量持续增加,寻找合适的抗生素替代药物的需求日趋迫切。抗菌肽作为微生物自身的防御武器,尽管还存在毒性高、稳定性低和生产成本高等限制其开发成药物的问题需要解决,但由于其具有广泛的抗菌谱、特殊的抗菌机制以及不容易产生耐药性还是受到广泛的关注。近年来,通过计算机辅助药物设计、化学合成等方式来规避劣势,开发抗菌肽药物,有望成为新一类用于临床的新型抗生素,并取代传统的抗生素成为新的抗感染治疗药物。     

海藻多糖的化学结构及生物活性研究新进展

多糖是海藻中一类重要的生物活性物质,近年来已引起国内外学者的广泛重视。大量研究表明,海藻多糖化学结构新颖、复杂,具有免疫调节、抗肿瘤、抗氧化、抗病毒和防治心血管疾病等多种药理活性。本文主要从海藻多糖的化学结构和生物活性2个方面对海藻多糖的研究进展进行综述,为后期对海藻多糖的深入研究和开发功能性食品或药品提供一定的理论指导。