植物乳杆菌DY6主要抑菌代谢物的分析和鉴定

【背景】被广泛应用于食品和饲料等多个行业的乳酸菌已成为制作生物防腐剂的研究热点。【目的】探究抑菌性能良好的植物乳杆菌DY6的抑菌物质,为其进一步应用提供参考依据。【方法】对植物乳杆菌发酵液中抑菌物质的理化特性进行研究,采用GC-MS分析发酵上清液代谢物,通过多元统计学分析方法推测主要抑菌物质,抑菌物质通过半制备进行初步分离后用GC-MS鉴定。【结果】植物乳杆菌DY6对金黄色葡萄球菌、大肠杆菌、沙门氏菌都有较强的抑制作用。采用不同发酵时间的发酵液作为研究对象,测定发酵上清液的抑菌能力,发酵0-4 h上清液无抑菌能力,发酵至8 h抑菌能力逐步上升,发酵24-48 h发酵上清液抑菌能力趋于稳定,在48 h时抑菌能力最佳,抑菌直径为15.28mm。通过多元统计学分析乳酸菌发酵液差异标志物,发现主要差异物为有机酸(如乳酸、乙酸、丙酸等)和脂肪酸(如辛酸、癸酸等)。经过半制备液相分离发酵上清液得到的抑菌组分,主要有有机酸(如乳酸、乙酸、3-苯基乳酸、苯丙酸等)和脂肪酸(如癸酸、辛酸、壬酸等),另外还有少量的醛类和醇类物质。【结论】确定了植物乳杆菌DY6的抑菌物质主要为有机酸和脂肪酸,为其进一步防腐应用提供了理论基础。     

刺五加内生真菌分离鉴定及抗菌活性研究

为开发利用刺五加内生真菌资源,寻找新型抗菌物质,从刺五加根茎叶中分离纯化得到内生真菌71株,经菌落形态和显微形态去重后进行ITS序列分子鉴定为18个种,来自于4目、8科、11属,其中链格孢属与镰孢霉属为优势属。根、茎、叶中内生真菌多样性指数分别为1. 112 31、1. 523 658、0. 264 1。18种刺五加内生真菌中,16种内生真菌至少对一种指示菌有抗菌活性。CWJ-5(镰孢霉属Fusarium oxysporum)对金黄色葡萄球菌抑菌效果显著,抑菌直径27. 17±0. 07 mm; CWJ-6(链格孢属Alternaria alternata)对大肠埃希菌抑菌效果显著,抑菌直径18. 07±0. 01 mm。结果表明刺五加内生真菌资源丰富,有很大的开发利用空间,部分菌种抑菌活性显著,值得进一步研究。     

Isolation and characterization of novel glycoproteins from fish epidermal mucus: correlation between their pore-forming properties and their antibacterial activities

In fish, a layer of mucus covers the external body surface contributing therefore, among other important biological functions, to the defense system of fish. The prevention of colonization by aquatic parasites, bacteria and fungi is mediated both by immune system compounds (IgM, lysozyme, etc.) and by antibacterial peptides and polypeptides. We have recently shown that only the hydrophobic components of crude epidermal mucus of fresh water and sea water fish exhibit strong pore-forming properties, which were well correlated with antibacterial activity [N. Ebran, S. Julien, N. Orange, P. Saglio, C. Lemaitre, G. Molle, Comp. Biochem. Physiol. 122 (1999)]. Here, we have isolated novel glycosylated proteins from the hydrophobic supernatant of tench (Tinca tinca), eel (Anguilla anguilla) and rainbow trout (Oncorhynchus mykiss) mucus. The study of their secondary structure was performed by circular dichroism and revealed structures in random coil and alpha-helix in the same proportions. When reconstituted in planar lipid bilayer, they induced the formation of ion channels. This pore-forming activity was well correlated with a strong antibacterial activity (minimal inhibitory concentration < 1 microM for the three proteins) against both gram-negative and gram-positive bacteria. Our results suggest that fish secrete antibacterial glycoproteins able to kill bacteria by forming large pores (several hundreds to thousands of pS) in the target membrane.     

毒根斑鸠菊中的一个新倍半萜的分离与鉴定

为了更好的研究毒根斑鸠菊(Vernonia cumingiana Benth)叶茎的化学成分与活性测定,利用硅胶柱层析、Sephadex LH-20等柱色谱技术对毒根斑鸠菊叶茎提取物进行了分离,并采用现代波谱学技术(1 H NMR、13C NMR、HMBC、HMQC等)及X-射线单晶衍射技术并根据其理化性质鉴定了七个化...     

Structure-activity relationships in a series of semisynthetic polycyclic glycopeptide antibiotics

The main achievements in the development of methods for the design of semisynthetic antibiotics of a new generation belonging to the group of polycyclic glycopeptides directed against infections caused by multidrug-resistant bacteria and dangerous human and animal viruses are reviewed. The review is focused on the results obtained at the Gauze Institute in the area of chemical modification of natural antibiotics (eremomycin, vancomycin, teicoplanin, etc.) directed toward modification of their antibacterial and/or antiviral activity. A special emphasis is placed on the study of the mechanisms of action of these antibiotics, which could be the basis of a rational approach to their chemical modification involving the transformation of the inner binding pocket and the peripheral regions of the molecules that participate in the formation of their complexes with targets. The study of the recently discovered antiviral activity of modified glycopeptide antibiotics is also discussed. A possibility of obtaining new highly active anti-HIV-1 and anti-HIV-2 preparations on the basis of hydrophobic derivatives of the aglycones of glycopeptide antibiotics was demonstrated. New semisynthetic derivatives of antibiotics that exhibit a high antibacterial activity in vivo, have good pharmacological characteristics, and are promising for practical use are described.     

Structure-activity relationships in a series of semisynthetic polycyclic glycopeptide antibiotics

The main achievements in the development of methods for the design of semisynthetic antibiotics of a new generation belonging to the group of polycyclic glycopeptides directed against infections caused by multidrug-resistant bacteria and dangerous human and animal viruses are reviewed. The review is focused on the results obtained at the Gauze Institute in the area of chemical modification of natural antibiotics (eremomycin, vancomycin, teicoplanin, etc.) directed toward modification of their antibacterial and/or antiviral activity. A special emphasis is placed on the study of the mechanisms of action of these antibiotics, which could be the basis of a rational approach to their chemical modification involving the transformation of the inner binding pocket and the peripheral regions of the molecules that participate in the formation of their complexes with targets. The recently discovered antiviral activity of modified glycopeptides antibiotics is also discussed. A possibility of obtaining new highly active anti-HIV-1 and anti-HIV-2 preparations on the basis of hydrophobic derivatives of the aglycones of glycopeptide antibiotics was demonstrated. New semisynthetic derivatives of antibiotics that exhibit a high antibacterial activity in vivo, have good pharmacological characteristics, and are promising for practical use are described.     

Factors affecting antibacterial activity of hop compounds and their derivatives.

The antibacterial effect of weak acids derived from the hop plant (Humulus lupulus L.) increased with decreasing pH. Analysis of the minimum inhibitory concentration of such compounds against Lactobacillus brevis IFO 3960 over pH 4-7 suggests that undissociated molecules were mainly responsible for inhibition of bacterial growth. The antibacterial activity of trans-isohumulone was ca 20 times greater than that of humulone, 11 times greater than that of colupulone and nine times greater than that of trans-humulinic acid when the degree of ionization was taken into account. Monovalent cations (K+, Na+, NH4+, Rb+, Li+) stimulated antibacterial activity of trans-isohumulone but the effect was smaller than that observed with H+. The response to divalent cations varied: Ca2+ had little effect on antibacterial activity, whereas Mg2+ reduced activity. Lipid materials and beta-cyclodextrin also antagonized the antibacterial action of trans-isohumulone.     

家蝇抗菌物质的诱导

针刺损伤诱导的家蝇三龄幼虫免疫血淋巴对动、植物病原菌有广谱的抗菌活性,同时,未经诱导的家蝇幼虫也具有抗菌活性。ＳＤＳ－ＰＡＧＥ电泳分析表明：外源诱导能增强原有抗菌物质的表达量,并能激活新的蛋白产生。家蝇免疫血淋巴中的抗菌物质具热稳定性和耐冷冻贮藏的特性     

Antibacterial activity of plastics coated with silver-doped organic-inorganic hybrid coatings prepared by sol-gel processes

Silver-doped organic-inorganic hybrid coatings were prepared starting from tetraethoxysilane- and triethoxysilane-terminated poly(ethylene glycol)-block-polyethylene by the sol-gel process. They were applied as a thin layer (0.6-1.1 microm) to polyethylene (PE) and poly(vinyl chloride) (PVC) films and the antibacterial activity of the coated films was tested against Gram-negative (Escherichia coli ATCC 25922) and Gram-positive (Staphylococcus aureus ATCC 6538) bacteria. The effect of several factors (such as organic-inorganic ratio, type of catalyst, time of post-curing, silver ion concentration, etc.) was investigated. Measurements at different contact times showed a rapid decrease of the viable count for both tested strains. The highest antibacterial activity [more than 6 log reduction within 6 h starting from 106 colony-forming units (cfu) mL-1] was obtained for samples with an organic-inorganic weight ratio of 80:20 and 5 wt % silver salt with respect to the coating. For the coatings prepared by an acid-catalyzed process, a high level of permanence of the antibacterial activity of the coated films was demonstrated by repeatedly washing the samples in warm water or by immersion in physiological saline solution at 37 degrees C for 3 days. The release of silver ions per square meter of coating is very similar to that previously observed for polyamides filled with metallic silver nanoparticles; however, when compared on the basis of Ag content, the concentration of silver ions released from the coating is much higher than that released from 1 mm thick specimens of polyamide (PA) filled with silver nanoparticles. Transparency and good adhesion of the coating to PE and PVC plastic substrates without any previous surface treatment are further interesting features.     

Identification of difurocumenonol, a new antimicrobial compound from mango ginger (Curcuma amada Roxb.) rhizome

AIM: The aim of the present work was to purify and characterize potential natural antibacterial compound from mango ginger (Curcuma amada Roxb.) rhizome. METHODS AND RESULTS: The mango ginger rhizome powder was sequentially extracted and screened for antibacterial activity by agar well diffusion method and broth dilution method. Nonpolar extracts of mango ginger showed high antibacterial activity against gram-positive bacteria with low minimum inhibitory concentration (60-180 ppm). Among five extracts of mango ginger, the chloroform extract demonstrated highest antibacterial activity. Antibacterial activity-guided fractionation of the chloroform extract by repeated silica gel column chromatography yielded pure compound. The purified antibacterial compound was analysed by UV, IR, LC-MS and 2D-HMQCT NMR spectra and was identified as a difurocumenonol, a novel compound not reported previously. CONCLUSIONS: Mango ginger extracts and isolated difurocumenonol demonstrated high antibacterial activity against gram-negative and gram-positive bacteria. SIGNIFICANCE AND IMPACT OF THE STUDY: A novel and natural antibacterial compound as well as mango ginger extracts can be used as food preservative to control the growth of food-borne pathogens and as a source of mango flavour.     

Factors affecting antibacterial activity of hop compounds and their derivatives

W.J. SIMPSON AND A.R.W. SMITH. 1992. The antibacterial effect of weak acids derived from the hop plant ( Humulus lupulus L.) increased with decreasing pH. Analysis of the minimum inhibitory concentration of such compounds against Lactobacillus brevis IFO 3960 over pH4–7 suggests that undissociated molecules were mainly responsible for inhibition of bacterial growth. The antibacterial activity of trans -isohumulone was ca 20 times greater than that of humulone, 11 times greater than that of colupulone and nine times greater than that of trans -humulinic acid when the degree of ionization was taken into account. Monovalent cations (K+, Na+, NH₄+, Rb+, Li+) stimulated antibacterial activity of trans -isohumulone but the effect was smaller than that observed with H+. The response to divalent cations varied: Ca2+ had little effect on antibacterial activity, whereas Mg2+ reduced activit. Lipid materials and β-cyclodextrin also antagonized the antibacterial action of trans -isohumulone.     

Molecular docking elucidates the plausible mechanisms underlying the anticancer properties of acetyldigitoxigenin from Adenium obesum

Adenium obesum (Forssk.) Roem. & Schult. is a promising medicinal plant belonging to the Apocynaceae family. It is a rich source of various phytochemicals such as cardiac glycosides, flavonoids, terpeniods, pregnanes etc. which have different pharmacological properties such as anticancer, antibacterial, acaricidal etc. While previous reports showed the anticancer activity of the aerial parts of the plant extract of A. obesum, the mechanisms of action of its chemical constituents are not known. The present study is aimed at elucidation of plausible mechanisms of anticancer activity of the plant by evaluating the binding interaction of its nine major selected compounds with macromolecular receptors implicated in the initiation and progression of cancer using various in silico approaches. Molecular docking results showed that the compound Δ¹⁶-3-Acetyldigitoxigenin (16-anhydro-3-acetylgitoxigenin) scored the best binding energy scores with the majority of the target proteins. The molecular binding of the compound was stabilized through hydrogen bonds as well as hydrophobic interactions, and also possesses favorable drug-like properties without significant toxicities.     

石榴果皮提取物抑菌活性研究

以12种常见的食品污染菌为供试菌,采用平板打孔法对10个品种石榴果皮的9种溶剂提取物进行抑菌效果研究,并对甲醇提取物的化学成分进行了初步分析。结果表明,甲醇提取物抑菌活性最强;石榴果皮提取物对供试菌种中的细菌的抑制效果最强,对革兰氏阳性菌的抑制效果强于对革兰氏阴性细菌的抑制效果,对酵母菌的抑制效果较弱,对霉菌几乎没有抑制作用。在供试的10个石榴品种中,‘峄城软籽’石榴果皮甲醇提取物的抑菌活性最高。化学成分系统预试结果表明,石榴果皮甲醇提取物中含有黄酮及其苷类物质、生物碱、酚类、鞣质类等成分。     

Purification and identification of antimicrobial sesquiterpene lactones from yacon (Smallanthus sonchifolius) leaves

The extraction of yacon [Smallanthus sonchifolius (Poepp. and Endl.) H. Robinson; Asteraceae] leaves and chromatographic separation yielded two new antibacterial melampolide-type sesquiterpene lactones, 8beta-tigloyloxymelampolid-14-oic acid methyl ester and 8beta-methacryloyloxymelampolid-14-oic acid methyl ester, as well as the four known melampolides, sonchifolin, uvedalin, enhydrin and fluctuanin. The newly identified compound, 8beta-methacryloyloxymelampolid-14-oic acid methyl ester, exhibited potent antimicrobial activity against Bacillus subtilis and Pyricularia oryzae, while 8beta-tigloyloxymelampolid-14-oic acid methyl ester showed lower activity. Fluctuanin exhibited the strongest antibacterial activity against B. subtilis among these six sesquiterpene lactones.     

凝结芽孢杆菌活菌片预防小儿肺炎继发性腹泻疗效观察

目的观察和评价凝结芽孢杆菌活菌片（商品名：爽舒宝）与抗菌药联用预防小儿肺炎继发性腹泻的临床疗效。方法将164例肺炎患儿随机分为预防组和对照组,预防组84例,对照组80例,两组均给予抗菌药及对症支持治疗。其中预防组在治疗的同时序贯（间隔2～3h）应用凝结芽孢杆菌活菌片,出现腹泻继续服用;对照组单用抗菌药,出现腹泻用凝结芽孢杆菌活菌片治疗。对两组继发性腹泻的发生率、腹泻持续天数、肺炎治疗的总疗程、腹痛和肠鸣音异常等症状和体征进行统计分析。结果预防组继发腹泻10例,发生率11．9％,对照组继发腹泻41例,发生率51．3％,两组相比差异具有统计学意义（P〈0．01）;预防组腹泻持续时间和治疗疗程显著短于对照组（P〈0．05）;预防组患儿腹痛、肠鸣音异常和脱水等症状和体征发生率均少于对照组（P〈0．05）。结论凝结芽孢杆菌活菌片与抗菌药序贯应用治疗肺炎,能显著降低继发性腹泻的发生率,缩短疗程,值得临床推广。     

QS-type bacterial signal molecules of nonpeptide origin

This review classifies and analyzes the literature data on bacterial autoinducers (AI), the signal molecules produced and secreted by bacterial cells and responsible for intercellular communication (quorum sensing, QS). The most important families of nonpeptide AI are discussed, including N-acyl homoserine lactones, derivatives of 2-methyl-2,3,4,5-tetrahydroxy tetrahydrofuran, indole and quinoline derivatives, and adrenalinerelated compounds. The data is provided on the intracellular and membrane receptors specifically binding to AI, as well as on the effector systems that are activated by AI and mediate their regulatory effects. The possible role of some vertebrate hormones (adrenergic agonists, serotonin, etc.) as AI and their effect on bacterial activity are discussed. The data are presented suggesting a high efficiency of AI-based antibacterial preparations, which selectively disrupt the bacterial information network and thus suppress bacterial infections.     

Antimicrobial, antioxidant, cytotoxicity and platelet aggregation inhibitory activity of a novel molecule isolated and characterized from mango ginger (Curcuma amada Roxb.) rhizome

Mango ginger (Curcuma amada Roxb.) rhizome is used in the manufacture of pickles and other food preparations due to its unique raw mango flavour. The chloroform extract of mango ginger rhizome was subjected to antibacterial activity-guided purification by repeated silica gel column chromatography to obtain a pure compound. The structure of the isolated compound was deduced by analysing UV, IR, LC-MS and 2D-HMQCT NMR spectral data, and named it as amadaldehyde, a novel compound. It exhibited a wide range of antibacterial activity with potential bactericidal activity against several bacteria. The purified compound also exhibited antioxidant activity, cytotoxicity and platelet aggregation inhibitory activities.     

Antibacterial activity of aspen bark extracts against some pneumotropic microorganisms

Extractive substances obtained from the bark of aspen (Populus tremula L.) with the use of petroleum ether (lipids I) and diethyl ether (lipids II) have exhibited high antibacterial activity with respect to Streptococcus pneumoniae and Haemophilus influenzae, causing 100% cell destruction. The minimum inhibiting concentration for S. pneumoniae has been found to be 0.5 - 50 mg/ml for lipids I and 0.0005 - 0.5 mg/ ml for lipids II, depending on the strain of bacteria. The antibacterial activity of rhytidome extracts is somewhat higher than that of phloem extracts. To suppress the growth of H. influenzae, more concentrated solutions of these extracts from 30 to 50 mg/ml are needed. Staphylococcus aureus was resistent in lipids. The action of temperature, mineral acids and alkali on lipids, as well as prolonged storage of strains in a refrigerator decreases the antibacterial activity of extracts under study.     

影响多粘类芽胞杆菌发酵液抑菌活性因素的研究

目的以点青霉菌作为指示菌,研究影响植物内生多粘芽胞杆菌发酵液抑菌活性的部分因素,为鉴定发酵液的抑菌物质提供基础研究。方法通过对多粘类芽胞杆菌发酵液进行不同处理（改变pH、加热、乙醇处理和蛋白酶酶解）,采用牛津杯法观察处理后发酵液对点青霉菌抑菌活性的变化。结果多粘类芽胞杆菌发酵液的抑菌效果在酸性条件下稳定,抑菌效果明显;而在中性和碱性范围内不稳定,抑菌效果不明显;多粘类芽胞杆菌发酵液中的有些抑菌物质具备良好的热稳定性;80％乙醇处理的发酵上清液有抑菌作用;经蛋白酶酶解后发酵液的抑菌活性变化不大。结论多粘类芽胞杆菌产生的乙醇沉淀物具有抑菌作用;发酵液中可能含有类细菌素的抑菌物质。