海洋缩酚酸肽类药物的研究进展

缩酚酸肽(depsipeptide)是存在于海洋生物中数量较多的一类天然生物活性物质,是包含酯键的一类多肽,具有抗肿瘤、抗菌、抗病毒、抗炎、抗血栓和抗动脉粥样硬化等活性。本文综述缩酚酸肽的来源、结构、生物活性等基础信息和国内外缩酚酸肽类药物的研究进展,并展望缩酚酸肽类药物研究开发的前景。     

含APD环缩酚酸肽类天然产物的研究进展

含有4-氨基-2,4-戊二烯酸的环缩酚酸肽类天然产物是一类包含酯键的环状多肽次级代谢产物,通常具有抗肿瘤、抗病原体等生物活性。此文根据国内外最新研究现状,介绍了这类物质的来源、结构、制备现状、生物活性以及开发前景。     

生物活性肽的抗肿瘤作用及其机理研究进展

生物活性肽是一类天然存在于动、植物和微生物等生物体内,或动、植物蛋白质经蛋白酶酶解以及人工化学合成或生物工程方法而得,且具有特殊生理活性的生物物质,具有较显著的抗肿瘤作用。此文介绍了生物活性肽的分类与特性、抗肿瘤作用,并简述了生物活性肽增强机体特异性和非特异性免疫功能、抗自由基与辐射损伤、诱导肿瘤细胞凋亡和直接作用于肿瘤细胞等多种作用机理,并简述了生物活性肽实现抗癌以及临床抗肿瘤药用等内容。     

海洋生物活性肽及其药物应用研究进展

海洋生物活性肽是海洋生物免疫系统长期进化而来的一类蛋白类分子,在宿主防御系统中起重要作用。大部分海洋生物活性肽可与细胞膜结合,起到抑制或杀死细菌、真菌、肿瘤细胞和病毒的作用。因其具有功能多样、来源广泛、特异性强、毒副作用小等优势,成为当今医药界的研究热点。本文主要综述了近年来有关海洋生物活性肽的发现、分类、提取及其抑菌机制的研究进展,为海洋生物活性肽类药物的进一步研究奠定基础。     

微生物来源的缩肽类化合物enopeptin A的研究(I)：菌种选育及发酵工艺研究

Enopeptin A是一种缩酚酸肽类化合物,具有抗菌、抗病毒等生物活性。以本实验室保藏的链霉菌SIIA-H7264为出发菌,通过紫外(UV)照射、甲基磺酸乙酯(EMS)诱变、亚硝基胍(NTG)诱变以及常压室温等离子体(ARTP)诱变,获得1株高产突变株A-21,其发酵产物Enopeptin A的产量较出发菌株提高了3倍。对发酵条件、发酵培养基组分进行单因素及响应面优化试验,最终Enopeptin A的产量达到1750μg/mL,较初始工艺提高了2.98倍。     

cryptophycin52在人肿瘤细胞系的体外药理

大量的天然产物被用于抗肿瘤细胞的有丝分裂和干扰微管的正常功能。这一类天然产物或其衍生物如长春花碱、紫杉醇等已被用于临床治疗肿瘤。但是多药耐药性限制了这类药物的应用,而ｃｒｙｐｔｏｐｈｙｃｉｎ家族中的新抗肿瘤制剂对Ｐ糖蛋白（Ｐｇｐ）介导的多药耐药性机制敏感性低。ｃｒｙｐｔｏｐｈｙｃｉｎ是一种缩酚酸肽类抗肿瘤制剂。这一类药物的先导化合物ｃｒｙｐｔｏｐｈｙｃｉｎ１是从念珠蓝细菌属（Ｎｏｓｔｏｃｓｐ．）中分离出来的,最初作为抗真菌药物,随后发现它具有对抗肿瘤细胞的细胞毒性,ｃｒｙｐｔｏｐｈｙｃｉｎ５２是…     

大豆抗氧化肽对H2O2诱导的红细胞过氧化的影响

近年来,人们越来越重视生物活性肽的研究和开发。大豆肽是大豆经分离纯化得到的低分子量的肽类混合物[1,2]。大豆肽具抗氧化活性的肽片段———抗氧化肽(简称SBP)。抗氧化肽作为一类重要的自由基清除剂在清除体内过多的自由基,保护机体免受自由基损伤,增强机体的免疫力等方面有     

RGD序列肽偶联物的研究进展

目的 综述并介绍RGD序列肽与多酸、抗癌药、CM—Chitin、PEG、PEU、EAA、CEMA等偶联物的合成方法。其合成一般采用缩合剂将肽和其他组分连接起来，偶联物的生物活性较其非偶联物强，是很有前途的多肽类药物，值得继续研究。     

抑菌剂N~4—对甲苯基苯甲醛缩氨硫脲的合成

<正> 缩氨基硫脲是一类具有广泛性生物活性的化合物,它具有抗细菌、抗真菌、抗肿瘤、抗病毒等活性。为了寻找高效、低毒的杀菌药物,我们合成了N~4—对甲苯基苯甲酸缩氨基硫脲,通过元素分析,红外光谱对其结构进行了确证,并对其抑菌活性进行初步     

急性脑外伤病人脑脊液血浆内皮素含量的变化及其临床意义

内皮素是1988年日本学者Yanag sawa发现的一类由内皮细咆合成的生物活性肽。随后有人证实神经胶质细咆也产生内皮素(ET),并以旁分泌的方式对神经胶质细胞和神经元发挥作用。这说明ET可能是一种潜在的神经调节因子,内皮素以其强大的缩血管作用而引起人们广泛关注,近几年来有关内皮素与腑血管病的研究已有较多报道。但对脑外伤后脑脊液及血浆ET含量的     

Ellagitannins as active constituents of medicinal plants

Isolation and structure determination, accompanied by measurement of various biological activities of each isolated tannin, particularly of ellagitannins, have brought about a marked change in the concept of tannins as active constituents of medicinal plants. Their biological activities should now be discussed on the basis of the structural differences among each tannin, in a way similar to that of the other types of natural organic compounds. The anti-tumor activity exclusively exhibited by several oligomeric ellagitannins, and their anti-HIV activities are examples of such biological activities. The inhibitory activity against lipid peroxidation, which is different in the strength among tannins of various structures, is exhibited in general more strongly by ellagitannins than by the other types of tannins of similar structures. The radical-scavenging activities of tannins as the mechanism of their inhibition, which is regarded to participate in several biological activities of tannins, have been supported by the ESR spectral measurements. Other biological activities, i.e., inhibition of mutagenicity of carcinogens, inhibition of tumor promotion, etc., have been found for tannins including ellagitannins.     

含有黄嘌呤衍生物的N-杂环卡宾金属配合物的生物活性研究进展

N-杂环卡宾(NHC)是一类多功能的配体,能够与过渡金属形成稳定的配位化合物,在催化、药学和材料科学等领域有着广泛的应用。黄嘌呤衍生物具有抗肿瘤转移和抗血管生成等生物活性,且结构易于修饰。将黄嘌呤衍生的NHC配体与过渡金属相结合有望得到具有全新生物活性的金属配合物。综述黄嘌呤衍生物的生物活性,以及黄嘌呤衍生的NHC金属配合物的结构特点和生物活性,并对黄嘌呤NHC金属配合物的研究进行了总结和展望,以期为进一步的研究提供参考。     

Pharmacological activities of a new glycosaminoglycan,acharan sulfate isolated from the giant African snail Achatina fulica

Acharan sulfate (AS) is a glycosaminoglycan (GAG) prepared from the giant African snail, Achatina fulica. In this study, some biological activities of AS were evaluated on the basis of structural similarities to heparin/heparan sulfate and the biological functions of GAGs. We demonstrated that it exhibited strong immunostimulating activities as measured by carbon clearance test in mice and in vivo phagocytosis. It also exhibited a significant hypoglycemic activity in epinephrine (EP)-induced hyperglycemia as well as antifatigue effects by weight-loaded forced swimming test. And it showed hypolipidemic activities in cholesterol-rich mixture induced hyperlipidemia in rats. The above results indicate that AS has diverse biological activities and suggest therapeutically important target molecules.     

Molecular connectivity. 6. Examination of the parabolic relationship between molecular connectivity and biological activity.

The topologically derived, nonempirical molecular connectivity index, chi, for several classes of compounds is shown to be parabolically related to the biological activities of these compounds. Similar nonlinear relationships were previously shown between the octanol-water partition coefficients, expressed as log P, of the compounds and their biological activities. These and previous studies indicate that many physiochemical properties presently used in structure-activity studies may be intermediaries between the nonempirical molecular structure encoded in chi and measured biological activities.     

褐藻胶寡糖生物活性研究进展

褐藻胶寡糖(Alginate Oligosaccharide, AOS)是褐藻胶降解而产生的一种功能性寡糖,大小在2~25个糖单元不等,其水溶性强,稳定性高,而且具有免疫调节、抗肿瘤、抑菌、降血压、肠道菌群调节等多种生物学活性,在药物研发、保健食品功能开发和农业应用等领域具有广泛的应用前景。本文主要综述了褐藻胶寡糖在医药、保健食品等领域的生物活性和应用。     

Flavonoid-membrane interactions： possible consequences for biological effects of some polyphenolic compounds

Flavonoids are found ubiquitously in higher plants and constitute an important component of the majority of people daily diets. The biological activities of flavonoids cover a very broad spectrum, from anticancer and antibacterial activities through to inhibition of bone resorption. In the present paper, the interactions between flavonoids and lipid bilayers as well as biological membranes and their components are reviewed, with special emphasis on the structure-activity relationships and mechanisms underlying the biological activity of flavonoids.     

Phenylpropanoid sucrose esters: plant-derived natural products as potential leads for new therapeutics

Natural products are regarded as vital key source of lead compounds for drug discovery due to their structural diversity and broad array of biological activities. Phenylpropanoid sucrose esters are naturally occurring compounds isolated from various plants and are structurally characterized by a sucrose core connected to one or more Ph-CH=CH-CO- moieties through an ester linkage. These compounds were extensively used in folk medicine and are found to possess many biological activities such as antitumor, antibacterial, antioxidant, antiviral, anti-inflammatory, neuro-protective and glycosidase inhibitory activities. This extensive review, which is the first of its kind on phenylpropanoid sucrose esters, aims to provide an up-to-date account of naturally occurring known phenylpropanoid sucrose esters with special focus on their sources, structures, biological and pharmacological activities.     

吴茱萸碱类衍生物的生物活性研究进展

吴茱萸碱是一类从传统中药吴茱萸中分离得到的咔啉喹唑啉酮类生物碱,具有抗肿瘤、抗炎、抗肥胖、抗阿尔茨海默病、抗菌、杀虫等作用.近年来,吴茱萸碱因其较低的细胞毒性、广泛的生物活性及优良的理化性质而成为药物研发领域的热点,尤其在抗肿瘤先导化合物的寻找研究中取得了较大的进展.本文将从生物活性、作用机制及抗肿瘤活性相关的衍生物设计合成等方面对吴茱萸碱的研究进展作一综述.     

2,4-Disubstituted thiazoles as multitargated bioactive molecules

Thiazoles are important heterocyclics exhibiting boundaryless biological activities, such as antibacterial, antifungal, anti-inflammatory, antitumor, antitubercular, antidiabetic, antiviral, and antioxidant. Substituents on a particular position of the thiazole ring affect the biological outcomes to a great extent. Therefore, researchers have synthesized compounds containing the thiazole ring with variable substituents as target structures, and evaluated their biological activities. The present review describes the biological importance of recently developed 2,4-disubstituted thiazole derivatives. Moreover, we have thrown light on various targets of 2,4-disubstituted thiazoles through which they induce biological effects, which will be helpful to those who are working on the design and structure–activity relationship of bioactive molecules.