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抗菌肽是生物体内产生的一种具有生物活性的小分子多肽,具有广谱抗细菌、抗病毒、抗真菌甚至抗癌作用。SMAP-29是来源于绵羊骨髓细胞,包含29个氨基酸的Cathelicidin类α-螺旋结构抗菌肽。SMAP-29具有多种生物活性,包括抗革兰氏阳/阴性菌、抗真菌、抗病毒、抗寄生虫、抗螺旋体、抗衣原体和中和内毒素活性,并且具有作用机制独特、快速杀灭细菌的特点。以下综述了SMAP-29抗菌肽家族的基因和蛋白结构、结构与活性关系、作用机制、生物功能、基因重组表达,重点阐述了SMAP-29结构、分子设计的必要性和基于 相似文献
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食用菌因药食两用的特点被广泛研究,具有提升机体免疫,阻止和防御疾病的功能作用。不同食用菌中所含的生物活性组分不同,主要有:多糖类、蛋白类、萜类、生物碱类等,这些组分具有抗氧化、抗肿瘤、免疫调节、抗炎症反应、抗心血管疾病、抗细菌、抗辐射及抗糖尿病等功效,其中抗肿瘤作用研究居多,研究发现其分子作用机制主要通过调控细胞信号通路中相关因子表达水平抑制肿瘤细胞增殖,诱导细胞凋亡的,这为开发天然无毒性肿瘤药物制剂奠定了理论基础。针对食用菌不同生物活性组分抗肿瘤分子机制的最新研究进展展开简要综述。 相似文献
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具有生物活性的天然三萜化合物的研究进展 总被引:1,自引:0,他引:1
三萜类化合物是广泛存在于自然界的一类有机化合物,其中很多具有一定的生物活性。该文着重综述了近五年来具有抗炎、抗菌、抗肿瘤生物活性的天然游离三萜化合物的研究进展。 相似文献
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灵菌红素是由微生物产生的一种红色次级代谢产物,因其具有抗菌、抗癌和抗疟疾等功效,受到了生物医药领域的广泛关注。微生物发酵是当前产灵菌红素的主要方法,分离筛选高产灵菌红素的微生物、优化发酵条件是提高灵菌红素产率的重要途径。本研究从深圳湾筛选出一株含有红色色素的菌株,并基于16S rRNA基因序列对该菌株进行了系统发育分析和物种鉴定。紫外可见光全波长扫描和HPLC-MS图谱分析证明,该菌株所产红色色素为灵菌红素。进一步通过单因素试验和正交优化法优化了该菌产灵菌红素的发酵条件和发酵培养基组分。系统发育分析表明,该菌株为一株海洋粘质沙雷氏菌(Serratia marcescens),并将其命名为S. marcescens SOCE 001。产灵菌红素的最佳发酵条件为:温度28 ℃、振荡培养转速220 r/min、培养基pH 7。发酵培养基最佳组合为:果糖添加量2 g/L、蛋白胨添加量10 g/L,MgSO4添加量2 g/L。优化发酵条件后,经24 h培养, 灵菌红素产量可达2.468 g/L。 相似文献
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没药的化学成分及其生物活性 总被引:4,自引:0,他引:4
没药属(Commiphora)植物分泌的胶状树脂作为没药(myrrh)为世界多个国家常用植物药,其所含成分包括萜类、甾体、黄酮、木脂素等次生代谢产物.现代药理研究表明没药提取物和所含的化学成分具有细胞毒、抗细菌、抗真菌、镇痛、抗氧化、抗炎等生物活性.本文综述了国内外没药化学成分和生物活性的研究概况. 相似文献
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微生物源抗菌肽研究概况 总被引:1,自引:0,他引:1
抗菌肽是广泛存在于生物体内的一种小分子多肽,具有分子量小、高效、稳定、作用机制独特和不易产生耐药性等特点,对细菌、真菌、寄生虫、病毒以及肿瘤细胞均有抑制作用。介绍了微生物来源,尤其是细菌源抗菌肽的结构特点、生物活性、作用机制及其在感染性疾病中的应用情况。 相似文献
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Nada Stankovic Lidija Senerovic Tatjana Ilic-Tomic Branka Vasiljevic Jasmina Nikodinovic-Runic 《Applied microbiology and biotechnology》2014,98(9):3841-3858
The growing demand to fulfill the needs of present-day medicine in terms of novel effective molecules has lead to reexamining some of the old and known bacterial secondary metabolites. Bacterial prodigiosins (prodiginines) have a long history of being re markable multipurpose compounds, best examined for their anticancer and antimalarial activities. Production of prodigiosin in the most common producer strain Serratia marcescens has been described in great detail. However, few reports have discussed the ecophysiological roles of these molecules in the producing strains, as well as their antibiotic and UV-protective properties. This review describes recent advances in the production process, biosynthesis, properties, and applications of bacterial prodigiosins. Special emphasis is put on undecylprodigiosin which has generally been a less studied member of the prodigiosin family. In addition, it has been suggested that proteins involved in undecylprodigiosin synthesis, RedG and RedH, could be a useful addition to the biocatalytic toolbox being able to mediate regio- and stereoselective oxidative cyclization. Judging by the number of recent references (216 for the 2007–2013 period), it has become clear that undecylprodigiosin and other bacterial prodigiosins still hold surprises in terms of valuable properties and applicative potential to medical and other industrial fields and that they still deserve continuing research curiosity. 相似文献
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In our previous papers [e.g. Sato et al., J. Biol. Chem. 273 (1998) 21455-21462], we have shown that prodigiosins can uncouple various H(+)-ATPases through their H(+)/Cl(-) symport activity. BE-18591 is an enamine of 4-methoxy-2,2'-bipyrrole-5-carboxyaldehyde (tambjamine group antibiotics) which resembles the prodigiosins. We found that BE-18591 was a new group of antibiotics that uncouples various H(+)-ATPases: it inhibited proton pump activities with IC(50)s of about 1-2 nM (about 20 pmol/mg protein) for submitochondrial particles as well as gastric vesicles and of 230 nM (about 230 pmol/mg protein) for lysosomes, but it had little effect on their ATP hydrolyses (up to 10 microM), a property of H(+)/Cl(-) symport activity. At low concentrations (<1 microM), BE-18591 inhibited immunoproliferation, the IC(50) of lipopolysaccharide-stimulated mouse splenocytes was 38 nM, that of Concanavalin A-stimulated cells was 230 nM. Gastritis of rabbits was also inhibited. At higher concentrations (>1 microM), BE-18591 induced neurite outgrowth (15% induction in 48 h at 4 microM), inhibited bone resorption (approximately 35% in 48 h at 10 microM) and caused cell death (approximately 30% in 48 h at 4 microM) but with little apoptosis. 相似文献
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《Journal of enzyme inhibition and medicinal chemistry》2013,28(4):870-875
A series of some 4-(aza substituted) methylene substituted dihydroxy coumarines were evaluated for their antioxidant and antielastase activities. Different in vitro methodologies such as total reducing power, 1,1-diphenyl-2-picryl-hydrazil (DPPH·) free radical scavenging, ABTS radical scavenging activity were used as antioxidant activity. All the tested compounds exhibited potent free radical scavenging ability and antielastase activites. 相似文献
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Accumulated evidence shows that leisure activities have a positive impact on cognitive function and dementia. This review aimed to systematically summarize the current evidence on this topic taking into account the limitations of the studies and biological plausibility for the underlying mechanisms linking cognition, dementia and leisure activities, with special attention on mental, physical and social activities. We included only longitudinal studies, with a follow-up time of at least 2 years, published in English from 1991 to March 2011 on leisure activities and cognition (n = 29) or dementia (n = 23) and provided some evidence from intervention studies on the topic. A protective effect of mental activity on cognitive function has been consistently reported in both observational and interventional studies. The association of mental activity with the risk of dementia was robust in observational studies but inconsistent in clinical trials. The protective effect of physical activity on the risk of cognitive decline and dementia has been reported in most observational studies, but has been less evident in interventional studies. Current evidence concerning the beneficial effect of other types of leisure activities on the risk of dementia is still limited and results are inconsistent. For future studies it is imperative that the assessment of leisure activities is standardized, for example, the frequency, intensity, duration and the type of activity; and also that the cognitive test batteries and the definition of cognitive decline are harmonized/standardized. Further, well designed studies with long follow-up times are necessary. This article is part of a Special Issue entitled: Imaging Brain Aging and Neurodegenerative disease. 相似文献
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Ahmed Kamal M. Naseer A. Khan K. Srinivasa Reddy Y. V. V. Srikanth S. Kaleem Ahmed K. Pranay Kumar 《Journal of enzyme inhibition and medicinal chemistry》2013,28(2):559-565
A versatile and efficient method has been developed for the synthesis of bis(indolyl)methanes by using aluminium triflate (0.5 mol%) as a novel catalyst. Further, some of the synthesized compounds were evaluated for their efficacy as antibacterial and antifungal activities. Most of the compounds have shown moderate to good inhibitory activity. 相似文献
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Xiaowen Wang Mingbo Su You Li Tongchao Liu Yujie Wang Yabing Chen Le Tang Yu-Peng He Xiaoguang Ding Fang Yu Jingkang Shen Jia Li Yubo Zhou Yue-Lei Chen Bing Xiong 《Bioorganic & medicinal chemistry letters》2019,29(6):844-847
Tranylcypromine moiety extracted from LSD1 inhibitors and 6-trifluoroethyl thienopyrimidine moiety from menin-MLL1 PPI inhibitors were merged to give new chemotypes for medicinal chemistry study. Among 15 new compounds prepared in this work, some exhibited nanomolar LSD1 activity and good selectivity over MAO-A/B, low micromolar menin-MLL1 PPI inhibitory activity, as well as submicromolar MV4-11 antiprofilative activities. Intracellular LSD1 engagement of compounds with higher enzymatic and antiproliferative activities was confirmed by CD86 mRNA up-regulation experiments. 相似文献
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Molecular design, synthesis and bioactivity of glycosyl hydrazine and hydrazone derivatives: notable effects of the sugar moiety 总被引:1,自引:0,他引:1
Cui Z Yang X Shi Y Uzawa H Cui J Dohi H Nishida Y 《Bioorganic & medicinal chemistry letters》2011,21(23):7193-7196
Assuming that the water solubility of our previous hydrazone derivatives would improve after modification with sugars while keeping or modulating their notable biological activities, we designed and synthesized some glycosyl hydrazine and hydrazone derivatives. Bioassay results indicated that the antitumor activity of our previously prepared hydrazones reduced or disappeared after modification with sugars. On the contrary, some glycosyl derivatives displayed much better antifungal activity against selected fungi. Obviously, a small sugar can change the biological activity of hydrazones significantly. 相似文献
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Fang-li Gang Feng Zhu Xiao-ting Li Jie-lu Wei Wen-jun Wu Ji-wen Zhang 《Bioorganic & medicinal chemistry》2018,26(16):4644-4649
A series of l-pyroglutamic acid analogues from natural product lead were designed and synthesized, as well as their antifungal activities against Phytophthora infestans, neuritogenic activities, antibacterial activities and anti-inflammatory activities are described. The bioassays and SAR study showed that the majority of l-pyroglutamic acid esters have a significant antifungal activity against P. infestans, especially 2d and 2j demonstrated the best activities with EC50 values of 1.44 and 1.21?μg?mL?1, which were about seven times that of commercial azoxystrobin (7.85?μg?mL?1). Moreover, compounds 2e, 2g and 4d displayed anti-inflammatory activity against LPS-induced NO production in BV-2 microglial cells; neuritogenic activity in NGF-induced PC-12 cells is the same activity. This study demonstrates that compounds 2d and 2j are potential drugs to control P. infestans. 相似文献
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Production of leucinostatins and nematicidal activity of Australian isolates of Paecilomyces lilacinus (Thom) Samson 总被引:5,自引:0,他引:5
Park JO Hargreaves JR McConville EJ Stirling GR Ghisalberti EL Sivasithamparam K 《Letters in applied microbiology》2004,38(4):271-276
AIMS: To evaluate the relationship between leucinostatin production by Paecilomyces lilacinus isolates and their biological activities. METHODS AND RESULTS: The nematicidal, parasitic and enzymatic activity of Australian P. lilacinus isolates were investigated. Nematicidal activities of culture filtrates were measured by mortality and inhibition of reproduction of Caenorhabditis elegans, whereas egg-parasitic activity was measured by colonization on Meloidogyne javanica. Enzymatic activities (protease and chitinase) were assayed on solid media. The results suggest that leucinostatins in P. lilacinus are indicators of nematicidal activity, whereas chitinase activity might be related to parasitism. CONCLUSIONS: Nematicidal activity of culture filtrates of Paecilomyces lilacinus strains related to their ability to produce leucinostatins. SIGNIFICANCE AND IMPACT OF THE STUDY: This is the first study describing the leucinostatins as nematicides. 相似文献