The beta-defensin-fold family of polypeptides.

Polypeptides adopting a fold very similar to that of beta-defensins are found in diverse organisms, including sea anemones, snakes, platypus and humans. These molecules of approximately 35-50 amino acid residues possess disparate activities, such as anti-microbial, myonecrotic, analgesic, and ion-channel inhibiting. The family of beta-defensin-fold structures generally consists of a short helix or turn followed by a small twisted anti-parallel beta-sheet. The six cysteine residues which are paired in a 1-5, 2-4, 3-6 fashion are crucial for determining and maintaining the compact core configuration of the structures. The primary structural similarity between members of the family suggests that the global fold is robust and that the nature of the side-chains determine the functional specificity. The distinct compact fold shared by these polypeptides may be useful in the design of molecules with desired pharmacological activity.     

96例药品不良反应/事件报告分析

目的通过对96例药品不良反应/事件报告进行统计分析,为临床合理用药提供参考。方法采用回顾性研究方法,对2012年我院上报的96例药品不良反应/事件报告,分别从药物种类、抗菌药物类别、临床表现、给药途径及患者年龄等方面进行系统分析。结果 96例药品不良反应/事件报告中,涉及药品45种,其中抗菌药物有关的药品不良反应/事件最多(50例,占52.08%);静脉滴注给药发生引起的最多(88例,占91.67%)。60岁以上老人发生率高于其他年龄段43例(占44.79%),严重药品不良反应/事件4例(占4.17%)。药品不良反应/事件临床表现最为常见的是皮肤及其附件损害(77例,占80.21%),其次是心血管系统损害等。结论应重视药品不良反应/事件,合理使用抗菌药物,以减少和避免药品不良反应/事件的发生。     

两栖类皮肤抗菌肽的分离纯化与抗菌活性检测技术

两栖类皮肤抗菌肽由于具有广谱、高效的抗菌活性,且不引起微生物耐药性等特点,已成为目前开发新型抗菌药物的理想材料。文章概述了两栖类抗菌肽的主要特点及其分离纯化和抗菌活性检测的主要方法,并对这些技术的原理、方法及其近年来在抗菌肽研究中的进展进行了介绍。同时本文还比较了各种方法的优缺点,对当前研究中所存在的一些问题进行了初步的探讨,以期为两栖类抗菌肽的应用提供理论依据。     

Chemical composition,in vitro anti-microbial,antifungal and antioxidant activities of the essential oil and methanolic extract of Hymenocrater longiflorus Benth., of Iran

In this study we identified the chemical composition, anti-microbial and antioxidant effects of essential oil and methanolic extract of Hymenocrater longiflorus Benth. Totally 87 volatile compounds from the essential oil in H. longiflorus, were identified by gas chromatography–mass spectrometry (GC–MS). These compounds are mainly monoterpene hydrocarbons, sesquiterpene hydrocarbons, oxygenated monoterpenes and oxygenated sesquiterpenoids compounds. The anti-microbial and antifungal activity of plants extracts against several pathogenic microorganisms was studied by disc diffusion and minimum inhibitory concentration procedures. The results revealed that the essential oil and polar sub-fraction are effective mostly against Staphylococcus aureus, Aspergillus niger and Candida albicans. The antioxidant activity was also determined by 1,1′-diphenyl-2-picryl-hydrazyl (DPPH) free radical scavenging, β-carotene linoleic acid assay and reducing power. In addition the total phenol of essential oil (54.6 ± 1.2), polar sub-fraction (50.0 ± 1.4) and non-polar sub-fraction (64.7 ± 2.0) were determined.     

Synthesis of new 2-thiouracil-5-sulfonamide derivatives with biological activity

2-Thiouracil-5-sulfonylchloride 1 reacted with a series of aromatic and heterocyclic amines to give 2a-j. The same compound 1 was reacted with a series of sulphonamides giving different sulphonamides of type 3a-e. On the other hand compound 1 was allowed to react with p-aminoacetophenone givining compound 4 which in turn was allowed to react with derivatives of alkyl thiosemicarbazides to give thiosemicarbazones of type 5a-e, also compound 4 was monobrominated to give compound 6 which in turn was reacted thiosemicarbazones of some aldehydes to give the corresponding thiazole derivatives 7a-f. In the same time compound 4 was reacted with a series of aromatic and heterocyclic aldehydes givining chalcones 8a-g (Claisen-Schemidt reaction). Also compound 4 was allowed to react with a series of aromatic and heterocyclic aldehydes, ethyl cyano acetate and/or malononitrile, and ammonium acetate giving pyridine derivatives 9a-d and 10a-e respectively. The biological effects of some of the new synthesized compounds was also investigated.     

Synthesis and anti-microbial activities of choline-like quaternary ammonium chlorides

New choline-like quaternary ammonium chlorides were obtained. The work-up procedure of synthesis was quick and efficient. The obtained chlorides showed anti-microbial activities. Quaternary ammonium chlorides derivatives of deanol esters exhibited strong activity and wide anti-bacterial spectra, similar to the activity of benzalkonium chloride. The relationship between chemical structure and anti-microbial activity was analyzed by the QSAR method.     

白花蛇舌草提取物的抑菌作用研究

目的：观察白花舌草提取物的抗菌实验效果。方法：采用试管连续稀释法进行体外抗菌研究。结果：白花蛇舌草对金黄色葡萄球菌、大肠杆菌、绿脓杆菌、白色念球菌均有抑杀作用。结论：白花蛇舌草具有较强的抗菌作用。     

Synergistic Antimicrobial Activities of Phytoestrogens in Crude Extracts of Two Sesame Species Against Some Common Pathogenic Microorganisms

Intensive studies on extracts and biologically active compounds isolated from medicinal plants have doubled in the last decade worldwide. However, as a result of paucity of knowledge and folkloric claim on the effectiveness of sesame leaves in infectious disease treatments, we aimed to determine the synergistic antimicrobial activity of essential oils and lignans present in the crude leaves extracts of Sesame radiatum and Sesame indicum. Ethanolic, methanolic and aqueous extracts of both leaves were studied for their in-vitro synergistic antimicrobial activity against both Gram positive and Gram negative micro-organisms, and Yeast using Agar diffusion method. The GC-MS phytochemical screening of methanolic extract showed that the major compounds in essential oils are of carboxylic acids and phenolic groups especially, the most potent antioxidants known to man like sesamol, sesamolin and sesamin among others. Methanolic and ethanolic extracts have broad spectrum antimicrobial effect against all the tested pathogenic micro-organisms except Streptococcus pneumoniae and Staphylococcus aureus respectively, while the aqueous extract exhibited inhibitory activity on Staphylococcus aureus, Streptococcus pneumoniae and Candida albicans. The result confirmed the folkloric claims of the antimicrobial effectiveness of locally consumed sesame leaves extracts especially against bacterial and common skin infection in many areas of Nigeria.     

海南三亚红树林放线菌多样性及抗菌活性

目的 研究海南三亚红树林底泥样品中放线菌的多样性及抗菌活性,以期发现可以产生新颖活性物质的药用放线菌资源。方法 采用11种分离培养基以稀释涂布法对样品中的放线菌进行选择性分离;对分离菌株的16S rRNA基因序列进行扩增、比对,开展多样性分析;放线菌发酵液经乙酸乙酯萃取,采用纸片法对粗提物进行抗菌活性筛选;同时对放线菌的生物合成基因NRPS、PKS I和PKS II进行筛选。结果 共分离到149株放线菌,它们分布于6个目12个科16个属,其中小单孢菌属为优势菌属;菌株MG16072的16S rRNA基因序列与最近有效菌株Actinomadura hallensis H647-1T的相似率为97.94%,为潜在Actinomadura属新种;抗菌活性检测结果显示,有20株放线菌至少对1株检定菌具有抗菌活性;NRPS、PKS I、PKS II基因筛选结果显示,有82株放线菌至少含有1种生物合成基因。结论 海南三亚红树林含有丰富的药用放线菌资源,具有从中发现新颖活性物质的潜力。