抗菌防腐剂（Ⅱ）新型合成抗菌防腐剂（待续）

介绍了阳离子杀菌剂,羧酸（酯）类,酰胺类,植物抗病诱导剂,异噻唑啉酮类,恶唑类,咪唑类,苯（苄）胺基嘧啶类,吡咯类,嘌呤类,卤代类,无机金属类等新型合成抗菌防腐剂的化学结构,作用机理及应用等。     

抗菌防腐剂(Ⅱ)新型合成抗菌防腐剂(续完)

概括介绍了阳离子杀菌剂、羧酸（酯）类、酰胺类，植物抗病诱导剂，异噻唑酮类、恶唑类、咪唑类、苯（苄）胺基嘧啶粉、吡咯为、嘌呤类，卤代类、无机金属类等新型合成抗菌防腐剂的化学结构、作用机理及应用等。     

抗菌防腐剂(Ⅲ) 天然抗菌防腐剂

从植物源、动物源及微生物源3个方面介绍了天然抗菌防腐剂如植物提取物、壳聚糖、抗菌肽、溶菌酶及抗生素等的发展状况.     

抗菌防剂（Ⅲ）天然抗菌防腐剂

从植物源、动物源及微生物源3个方面好天然抗菌防腐剂如植物提取物，壳聚糖，抗菌肽，溶菌酶及抗生素等的发展状况。     

抗菌陶瓷材料的应用及其开发前景

随着人民生活水平的提高和保健意识的增强,人们对工作和家庭环境的卫生也日益重视,从而促进了具有抗菌功能材料的研究与开发,各种抗菌制品应运而生,并获得了迅速的发展。目前,日本已研制开发成功一系列抗菌陶瓷制品投放市场,我国也正在进行抗菌陶瓷材料的研究和开发。 抗菌性陶瓷材料的特点及其功能 抗菌性陶瓷材料也称无机抗菌剂,它是在特殊的无机材料中加入含有抗菌作用的金属离子而构成的抗菌剂。抗菌剂根据材料的不同,将基础抗菌剂分为有机抗菌剂和无机抗菌剂两种类型。有机抗菌剂为传统抗菌剂,在医疗及工业领域得到广泛应用。无机抗菌剂在使用安全性、持久性、抗菌性和耐热性等方面都优于有机抗菌剂,因此,无机抗菌剂的应用更为广泛。     

稀土β-成核剂改性无规共聚聚丙烯抗菌塑料的性能表征

讨论了无机金属离子/纳米二氧化钛抗菌剂和有机季铵盐抗菌剂对加入WBGⅡ的无规共聚聚丙烯(PPR)复合材料抗菌性能、力学性能和结晶性能的影响。结果表明:抗菌剂的加入明显地提高了PPR的抗菌能力,且无机抗菌剂的作用效果要优于所选取的有机季铵盐抗菌剂,但其对于基体力学性能的影响也较大。无机抗菌剂用量在6～10份时,对大肠杆菌、金黄色葡萄球菌的抗菌率分别达到93.8%～99.2%、91.7%～98.2%;有机季铵盐抗菌剂用量在2.5份时,对大肠杆菌、金黄色葡萄球菌的抗菌率分别达到91.0%、91.4%。     

抗菌聚氨酯研究进展

介绍抗菌聚氨酯的研究状况,涉及无机抗菌剂、有机抗菌剂、天然抗菌剂的性质和抗菌机理,探讨了抗菌聚氨酯的应用和发展趋势。     

抗菌水性聚氨酯研究进展

介绍了近年来国内外学者在抗菌水性聚氨酯材料方面的研究情况,以及利用物理和化学手段等工艺在水性聚氨酯中引入抗菌剂从而制备新型抗菌水性聚氨酯的方法,同时综述了无机、有机和天然抗菌剂等各类抗菌剂在水性聚氨酯抗菌改性方面的应用,并进一步对抗菌水性聚氨酯材料的未来研究方向和关注热点提出了展望。     

抗菌聚氨酯的研究进展

本文介绍了抗菌聚氨酯的研究状况,各种无机抗菌剂、有机抗菌剂、天然抗菌剂的性质和抗菌机理,探讨了抗菌聚氨酯的应用和发展趋势。     

抗菌剂与抗菌纤维的研究进展

介绍了无机抗菌剂、有机抗菌剂、天然抗菌剂和高分子抗菌剂的抗菌机理,主要有金属离子接触反应机理、催化激活机理、阳离子固定机理和损坏机理。阐述了抗菌纤维的功能及国内外的抗菌纤维最新的研究。指出抗菌纤维正朝着抗菌范围更广、抗菌耐久性更好、功能更齐全的方向发展。     

Protease Inhibitors from Plants with Antimicrobial Activity

Antimicrobial proteins (peptides) are known to play important roles in the innate host defense mechanisms of most living organisms, including plants, insects, amphibians and mammals. They are also known to possess potent antibiotic activity against bacteria, fungi, and even certain viruses. Recently, the rapid emergence of microbial pathogens that are resistant to currently available antibiotics has triggered considerable interest in the isolation and investigation of the mode of action of antimicrobial proteins (peptides). Plants produce a variety of proteins (peptides) that are involved in the defense against pathogens and invading organisms, including ribosome-inactivating proteins, lectins, protease inhibitors and antifungal peptides (proteins). Specially, the protease inhibitors can inhibit aspartic, serine and cysteine proteinases. Increased levels of trypsin and chymotrypsin inhibitors correlated with the plants resistance to the pathogen. Usually, the purification of antimicrobial proteins (peptides) with protease inhibitor activity was accomplished by salt-extraction, ultrafiltration and C₁₈ reverse phase chromatography, successfully. We discuss the relation between antimicrobial and anti-protease activity in this review. Protease inhibitors from plants potently inhibited the growth of a variety of pathogenic bacterial and fungal strains and are therefore excellent candidates for use as the lead compounds for the development of novel antimicrobial agents.     

Fluorescein analogues inhibit SecA ATPase: the first sub-micromolar inhibitor of bacterial protein translocation

SecA is a central component of the general secretion system that is essential for bacterial growth and thus an ideal target for antimicrobial agents. A series of fluorescein analogues were first screened against the ATPase activity using the truncated unregulated SecA catalytic domain. Rose bengal (RB) and erythrosin B (EB) were found to be potent inhibitors SecA with IC(50) values of 0.5 μM and 2 μM, respectively. RB and EB inhibit the catalytic SecA ATPase more effectively than the F(1) F(0) -proton ATPase. We used three assays to test the effect of these compounds on full-length SecA ATPase: in solution (intrinsic ATPase), in membrane preparation, and translocation ATPase. RB and EB show the following trend in terms of IC(50) values: translocation ATPase相似文献   

Receptor‐Based Virtual Screening and Biological Characterization of Human Apurinic/Apyrimidinic Endonuclease (Ape1) Inhibitors

The endonucleolytic activity of human apurinic/apyrimidinic endonuclease (AP endo, Ape1) is a major factor in maintaining the integrity of the genome. Conversely, as an undesired effect, Ape1 overexpression has been linked to resistance to radio‐ and chemotherapeutic treatments in several human tumors. Inhibition of Ape1 using siRNA or the expression of a dominant negative form of the protein has been shown to sensitize cells to DNA‐damaging agents, including various chemotherapeutic agents. Therefore, inhibition of the enzymatic activity of Ape1 might result in a potent antitumor therapy. A number of small molecules have been described as Ape1 inhibitors; however, those compounds are in the early stages of development. Herein we report the identification of new compounds as potential Ape1 inhibitors through a docking‐based virtual screening technique. Some of the compounds identified have in vitro activities in the low‐to‐medium micromolar range. Interaction of these compounds with the Ape1 protein was observed by mass spectrometry. These molecules also potentiate the cytotoxicity of the chemotherapeutic agent methyl methanesulfonate in fibrosarcoma cells. This study demonstrates the power of docking and virtual screening techniques as initial steps in the design of new drugs, and opens the door to the development of a new generation of Ape1 inhibitors.     

耐火浇注料用分散剂进展

简要介绍了分散剂在耐火浇注料中的作用及作用机理,以及无机分散剂与有机分散剂的不同分散作用机理。着重介绍了有机分散剂的进展及各分散剂的化学结构式、性质与使用效果,并提出耐火浇注料用分散剂的发展方向。     

Synthesis of 2-mercaptobenzothiazole and 2-mercaptobenzimidazole derivatives condensed with carbohydrates as a potential antimicrobial agents

The thiazole and imidazole nucleus, as well as carbohydrates are important classes of compounds found in many natural and synthetic products with a wide range of biological activities. Due to the importance of these classes of compounds as antimicrobial agents, the present article reports the synthesis of a new series of nine compounds based on the coupling of 2-mercaptobenzothiazole and 2-mercaptobenzimidazole with different carbohydrates.     

Amino Acid Based Antimicrobial Agents – Synthesis and Properties

Structures of several dozen of known antibacterial, antifungal or antiprotozoal agents are based on the amino acid scaffold. In most of them, the amino acid skeleton is of a crucial importance for their antimicrobial activity, since very often they are structural analogs of amino acid intermediates of different microbial biosynthetic pathways. Particularly, some aminophosphonate or aminoboronate analogs of protein amino acids are effective enzyme inhibitors, as structural mimics of tetrahedral transition state intermediates. Synthesis of amino acid antimicrobials is a particular challenge, especially in terms of the need for enantioselective methods, including the asymmetric synthesis. All these issues are addressed in this review, summing up the current state-of-the-art and presenting perspectives fur further progress.     

纸张增干强剂研究与应用进展

纸张增干强剂的发展经历了从最初的传统植物胶类干强剂,到淀粉类干强剂,再到有机高分子类干强剂;从简单的天然有机高分子类干强剂,到合成的有机高分子类干强剂,再到基于生态安全性的天然改性有机高分子干强剂的发展过程。为了促进纸张干强剂的迅速发展和实际应用,本文综述了纸张干强剂在国内的研究进展与应用现状,重点对淀粉和聚丙烯酰胺两大类增干强剂分别阐述了其特点以及在纸张增强过程中的应用情况,并对其发展方向进行了分析和评价,尤其是针对目前我国增干强剂研究与开发应用中的不足,对今后的研究工作提出了一些建议和设想。     

纳米抗菌塑料

介绍了纳米抗菌剂和纳米抗菌塑料的制备工艺以及纳米抗菌塑料性能的评价方法,并展望了纳米抗菌塑料的发展前景。     

Discovery of Benzimidazole–Quinolone Hybrids as New Cleaving Agents toward Drug‐Resistant Pseudomonas aeruginosa DNA

A series of benzimidazole–quinolone hybrids as new potential antimicrobial agents were designed and synthesized. Bioactive assays indicated that some of the prepared compounds exhibited potent antibacterial and antifungal activities. Notably, 2‐fluorobenzyl derivative 5 b (ethyl 7‐chloro‐6‐fluoro‐1‐[[1‐[(2‐fluorophenyl)methyl]benzimidazol‐2‐yl]methyl]‐4‐oxo‐quinoline‐3‐carboxylate) showed remarkable antimicrobial activity against resistant Pseudomonas aeruginosa and Candida tropicalis isolated from infected patients. Active molecule 5 b could not only rapidly kill the tested strains, but also exhibit low toxicity toward Hep‐2 cells. It was more difficult to trigger the development of bacterial resistance of P. aeruginosa against 5 b than that against norfloxacin. Molecular docking demonstrated that 5 b could effectively bind with topoisomerase IV–DNA complexes, and quantum chemical studies theoretically elucidated the good antimicrobial activity of compound 5 b . Preliminary experimental reaction mechanism exploration suggested that derivative 5 b could not intercalate into DNA isolated from drug‐resistant P. aeruginosa, but was able to cleave DNA effectively, which might further block DNA replication to exert powerful bioactivities. In addition, compound 5 b is a promising antibacterial agent with membrane disruption abilities.