antibacterial activity

抗菌活性
  • 文章类型: Journal Article
    无乳链球菌(S.无乳),也称为B组链球菌(GBS),是一种高度传染性的病原体。长期使用抗生素会导致抗生素残留和耐药性的重大问题。白屈菜红碱(CHE)是一种天然存在的二苯甲定生物碱,而白屈菜红碱氯化物(CHEC)是其盐酸盐形式,具有多种生物和药理活性。然而,CHEC对GBS的抗菌机制尚不清楚.因此,本研究旨在研究CHEC对GBS的体外抗菌活性,并阐明其作用机制。使用抑制性区评估CHEC对GBS的抗菌作用,最小抑制浓度(MIC),和最小杀菌浓度(MBC)测定,以及通过构建时间杀伤曲线。通过扫描电子显微镜(SEM)和透射电子显微镜(TEM)等技术研究了CHEC的抗菌机理,碱性磷酸酶(AKP)活性的测量,Na+K+的测定,Ca2+Mg2+-三磷酸腺苷(ATP)活性,膜通透性的观察,并分析细胞内活性氧(ROS)和关键毒力基因的mRNA表达水平。结果表明,CHEC对GBS的抑制区直径为14.32mm,12.67mm,和10.76毫米,浓度为2毫克/毫升,1mg/mL,和0.5mg/mL,分别。MIC和MBC值分别确定为256μg/mL和512μg/mL。在时间杀伤曲线中,8×MIC,4×MIC和2×MICCHEC可以在24小时内完全杀死GBS。SEM和TEM分析显示,用CHEC处理的GBS细胞的形态学改变包括收缩,崩溃,和细胞液体的泄漏。此外,CHEC对GBS功效的抗菌机制归因于其细胞壁完整性的破坏以及膜通透性导致细胞内ATP的细胞外释放。AKP,Na+K+,Ca2+Mg2+。此外,CHEC可以增加ROS的产生,从而导致氧化损伤并下调GBS细胞中关键毒力基因的mRNA表达水平。总之,CHEC具有作为抗GBS的抗微生物剂的潜力,需要进一步的研究来阐明其他分子机制。
    Streptococcus agalactiae (S.agalactiae), also known as group B Streptococcus (GBS), is a highly infectious pathogen. Prolonged antibiotic usage leads to significant issues of antibiotic residue and resistance. Chelerythrine (CHE) is a naturally occurring benzophenidine alkaloid and chelerythrine chloride (CHEC) is its hydrochloride form with diverse biological and pharmacological activities. However, the antibacterial mechanism of CHEC against GBS remains unclear. Thus, this study aims to investigate the in vitro antibacterial activity of CHEC on GBS and elucidate its underlying mechanism. The antibacterial effect of CHEC on GBS was assessed using inhibitory zone, minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC) assays, as well as by constructing a time-kill curve. The antibacterial mechanism of CHEC was investigated through techniques such as scanning electron microscopy (SEM) and transmission electron microscopy (TEM), measurement of alkaline phosphatase (AKP) activity, determination of Na+ K+, Ca2+ Mg2+-adenosine triphosphate (ATP) activity, observation of membrane permeability, and analysis of intracellular reactive oxygen species (ROS) and mRNA expression levels of key virulence genes. The results demonstrated that the inhibition zone diameters of CHEC against GBS were 14.32 mm, 12.67 mm, and 10.76 mm at concentrations of 2 mg/mL, 1 mg/mL, and 0.5 mg/mL, respectively. The MIC and MBC values were determined as 256 μg/mL and 512 μg/mL correspondingly. In the time-kill curve, 8 × MIC, 4 × MIC and 2 × MIC CHEC could completely kill GBS within 24 h. SEM and TEM analyses revealed significant morphological alterations in GBS cells treated with CHEC including shrinkage, collapse, and leakage of cellular fluids. Furthermore, the antibacterial mechanism underlying CHEC\'s efficacy against GBS was attributed to its disruption of cell wall integrity as well as membrane permeability resulting in extracellular release of intracellular ATP, AKP, Na+ K+, Ca2+ Mg2+. Additionally CHEC could increase the ROS production leading to oxidative damage and downregulating mRNA expression levels of key virulence genes in GBS cells. In conclusion, CHEC holds potential as an antimicrobial agent against GBS and further investigations are necessary to elucidate additional molecular mechanisms.
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  • 文章类型: Journal Article
    这项研究强调了芝麻种皮(SSC)的潜力,通常在芝麻酱加工过程中丢弃,作为通过提取生物活性化合物进行增值的宝贵资源。它检查了SSC的酚类组成和抗氧化活性,并评估了其对食源性病原体如单核细胞增生李斯特菌的抗菌特性,大肠杆菌O157:H7和鼠伤寒沙门氏菌。此外,SSC进行了纳米乳液涂层,使用动态光散射和扫描电子显微镜进行分析,以增强其作为天然防腐剂的应用。该研究特别关注将SSC纳米乳液掺入牛奶中以确定其作为防腐剂的有效性。SSC表现出相当大的抗氧化活性和酚类含量,儿茶素被确定为主要的多酚。GC-MS分析显示七种主要化合物,以油酸为首。值得注意的是,SSC在100mg/ml时可有效抑制肉汤中的单核细胞增生李斯特菌。SSC及其纳米乳液的应用导致牛奶中细菌形态的改变和细菌数量的显著减少,突出了其作为一种有效的天然抗菌剂的潜力。这项研究的结果强调了SSC作为食品工业中一种有价值的副产品的潜在用途,对食品保存有重大影响。
    The study highlighted the potential of sesame seed coat (SSC), typically discarded during sesame paste processing, as a valuable resource for valorization through extracting bioactive compounds. It examined the phenolic composition and antioxidant activity of SSC, and evaluated its antibacterial properties against foodborne pathogens such as Listeria monocytogenes, Escherichia coli O157:H7, and Salmonella Typhimurium. Additionally, SSC underwent nanoemulsion coating, analyzed using dynamic light scattering and scanning electron microscopy, to enhance its application as a natural preservative. The research specifically focused on incorporating SSC nanoemulsion into milk to determine its effectiveness as a preservative. SSC demonstrated considerable antioxidant activity and phenolic content, with catechin identified as the predominant polyphenol. GC-MS analysis revealed seven major compounds, led by oleic acid. Notably, SSC effectively inhibited L. monocytogenes in broth at 100 mg/ml. The application of SSC and its nanoemulsion resulted in changes to bacterial morphology and a significant reduction in bacterial counts in milk, highlighting its potential as an effective natural antibacterial agent. The findings of this study highlight the potential use of SSC as a valuable by-product in the food industry, with significant implications for food preservation.
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  • 文章类型: Journal Article
    高分子量聚(L-丙交酯)-b-聚(乙二醇)-b-聚(L-丙交酯)(PLLA-PEG-PLLA)是一种柔性且可生物降解的生物塑料,在柔性食品包装中具有广阔的潜力,但没有抗菌能力。因此,在这项工作中,测定了具有抗菌活性的氧化锌纳米颗粒(纳米ZnOs)对PLLA-PEG-PLLA各种性能的影响。纳米ZnOs的加入增强了结晶,拉伸,紫外线屏障,和抗菌性能的PLLA-PEG-PLLA。然而,随着纳米ZnO含量超过2wt%,纳米复合薄膜的结晶和拉伸性能再次下降。当纳米ZnO含量不超过2wt%时,纳米ZnO在PLLA-PEG-PLLA基质中分布良好,当纳米ZnO含量高于2wt%时,表现出一些纳米ZnO团聚体。随着纳米ZnO含量的增加,PLLA-PEG-PLLA基质的热稳定性和吸湿性降低,薄膜的不透明性增加。PLLA-PEG-PLLA/ZnO纳米复合薄膜对大肠杆菌和金黄色葡萄球菌等细菌表现出良好的抗菌活性。可以得出结论,纳米ZnOs可以用作柔性PLLA-PEG-PLLA的多功能填料。因此,添加纳米ZnOs作为成核剂,加强,紫外线屏蔽,柔性PLLA-PEG-PLLA基质中的抗菌剂可以在运输和储存期间为食品和包装提供保护。
    High-molecular-weight poly(L-lactide)-b-poly(ethylene glycol)-b-poly(L-lactide) (PLLA-PEG-PLLA) is a flexible and biodegradable bioplastic that has promising potential in flexible food packaging but it has no antibacterial ability. Thus, in this work, the effect of zinc oxide nanoparticles (nano-ZnOs) which have antimicrobial activity on various properties of PLLA-PEG-PLLA was determined. The addition of nano-ZnOs enhanced the crystallization, tensile, UV-barrier, and antibacterial properties of PLLA-PEG-PLLA. However, the crystallization and tensile properties of nanocomposite films decreased again as the nano-ZnO increased beyond 2 wt%. The nano-ZnO was well distributed in the PLLA-PEG-PLLA matrix when the nano-ZnO content did not exceed 2 wt% and exhibited some nano-ZnO agglomerates when the nano-ZnO content was higher than 2 wt%. The thermal stability and moisture uptake of the PLLA-PEG-PLLA matrix decreased and the film\'s opacity increased as the nano-ZnO content increased. The PLLA-PEG-PLLA/ZnO nanocomposite films showed good antibacterial activity against bacteria such as Escherichia coli and Staphylococcus aureus. It can be concluded that nano-ZnOs can be used as a multi-functional filler of the flexible PLLA-PEG-PLLA. As a result, the addition of nano-ZnOs as a nucleating, reinforcing, UV-screening, and antibacterial agent in the flexible PLLA-PEG-PLLA matrix may provide protection for both the food and the packaging during transportation and storage.
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  • 文章类型: Journal Article
    (1)背景:抗菌素耐药性正以极端的速度增长,已被证明是一个紧迫的话题,研究替代疗法。这种潜在的可能性隐藏在抗菌肽中,因为它们具有低到没有毒性,在低浓度下的有效性,最重要的是它们能够用于多种治疗。这项工作的重点是研究TemporinA的7位修饰对其生物学活性的影响。(2)方法:使用Fmoc/Ot-BuSPPS合成靶向肽。使用肉汤微量稀释法和圆盘扩散法确定类似物的抗菌活性。进行体外测试以确定细胞毒性,光毒性,和肽类似物对一组肿瘤和正常细胞系的抗增殖活性;(3)结果:除DTCit外,所有类似物均显示出良好的抗菌活性,根据圆盘扩散方法,DTDab具有最好的活性。然而,DTCit具有可接受的细胞毒性,结合针对测试MCF-7细胞系的良好选择性;(4)结论:所获得的结果揭示了在TemporinA序列中第7位侧链的碱性和长度对于两种测试活性的重要性。
    (1) Background: Antimicrobial resistance is growing at an extreme pace and has proven to be an urgent topic, for research into alternative treatments. Such a prospective possibility is hidden in antimicrobial peptides because of their low to no toxicity, effectiveness at low concentrations, and most importantly their ability to be used for multiple treatments. This work was focused on the study of the effect of the modification in position 7 of Temporin A on its biological activity; (2) Methods: The targeted peptides were synthesized using Fmoc/Ot-Bu SPPS. The antibacterial activity of the analogs was determined using the broth microdilution method and disk-diffusion method. In vitro tests were performed to determine the cytotoxicity, phototoxicity, and antiproliferative activity of the peptide analogs on a panel of tumor and normal cell lines; (3) Results: All analogs except DTCit showed good antibacterial activity, with DTDab having the best activity according to the disk-diffusion method. However, DTCit had an acceptable cytotoxicity, combined with good selectivity against the test MCF-7 cell line; (4) Conclusions: The obtained results revealed the importance of the basicity and length of the side chain at position 7 in the Temporin A sequence for both tested activities.
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  • 文章类型: Journal Article
    皮肤损伤是一个重要的健康问题,将身体暴露于感染风险。利用含有洋甘菊(ChamomillarecuttaL.)的天然产品有望达到治疗目的。此外,透明质酸(HA),一种以其组织再生能力而闻名的活性成分,可以加速愈合。在这项研究中,我们制备并表征了C.recutta的提取物,并将其整合到用HA稳定的纳米乳液系统中,旨在利用其治愈潜力。我们评估了酒精强度对类黄酮提取的影响,并使用UHPLC/MS对提取物进行化学表征,同时定量其抗氧化和抗菌能力。我们开发了装载有C.recutta提取物的纳米乳液,并评估了HA稳定对pH的影响,液滴大小,多分散指数(PDI),zeta电位,和粘度。结果表明,70%水醇提取产生较高的类黄酮含量。提取物在体外表现出抗氧化能力,皮肤再生的理想特征,并证明了对关键微生物菌株(金黄色葡萄球菌,化脓性链球菌,大肠杆菌,和铜绿假单胞菌)与皮肤定植和感染有关。黄酮类螺旋体苷和芹菜苷是最丰富的生物活性物质。HA的添加导致粘度增加,同时保持适合局部施用的pH。Zeta电位,液滴大小,和PDI符合可接受的标准。此外,将C.recutta提取物掺入纳米乳液中增强了其抗菌作用。因此,负载有C.recutta和HA稳定的纳米乳液系统表现出局部应用的有利特性,显示出帮助愈合过程的希望。
    Skin lesions are an important health concern, exposing the body to infection risks. Utilizing natural products containing chamomile (Chamomilla recutita L.) holds promise for curative purposes. Additionally, hyaluronic acid (HA), an active ingredient known for its tissue regeneration capacity, can expedite healing. In this study, we prepared and characterized an extract of C. recutita and integrated it into a nanoemulsion system stabilized with HA, aiming at harnessing its healing potential. We assessed the impact of alcoholic strength on flavonoid extraction and chemically characterized the extract using UHPLC/MS while quantifying its antioxidant and antimicrobial capacity. We developed a nanoemulsion loaded with C. recutita extract and evaluated the effect of HA stabilization on pH, droplet size, polydispersity index (PDI), zeta potential, and viscosity. Results indicated that 70% hydroalcoholic extraction yielded a higher flavonoid content. The extract exhibited antioxidant capacity in vitro, a desirable trait for skin regeneration, and demonstrated efficacy against key microbial strains (Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli, and Pseudomonas aeruginosa) associated with skin colonization and infections. Flavonoids spireoside and apiin emerged as the most abundant bioactives. The addition of HA led to increased viscosity while maintaining a suitable pH for topical application. Zeta potential, droplet size, and PDI met acceptable criteria. Moreover, incorporating C. recutita extract into the nanoemulsion enhanced its antimicrobial effect. Hence, the nanoemulsion system loaded with C. recutita and HA stabilization exhibits favorable characteristics for topical application, showing promise in aiding the healing processes.
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  • 文章类型: Journal Article
    通过传统浸渍从来自欧洲各个国家的13个杨树蜂胶样品中获得的乙醇提取物进行了总多酚测试,类黄酮含量,和抗氧化活性。此外,用高效液相色谱法测定了18种多酚类化合物(酚酸类和黄酮类化合物)的含量。通过良好扩散法评估了六种具有最高活性的选定提取物对五种菌株的抑制作用(双歧杆菌属。,L.鼠李糖,L.嗜酸菌,大肠杆菌,和拟杆菌属。)使用选择性培养基从肥胖先证者的粪便中自我分离的肠道细菌。发现蜂胶的抗氧化活性因地理来源而异,甚至在同一地区的样品中也有所不同。这表明其他一些因素也会影响蜂胶的质量。不同地理来源的样品主要在单个酚类化合物的份额上有所不同,不可能找到一个特征性的起源标记,仅排除波兰样品中存在的高良姜素。评估蜂胶的抑制活性(在每毫升70mg至10µg的范围内)表明,发现100µg/mL的浓度对于测试的粪便细菌是安全的(双歧杆菌属。,L.鼠李糖,L.嗜酸菌,大肠杆菌,和拟杆菌属。).由于没有发现低剂量蜂胶对肠道菌群的负面影响,可以建议,以推荐剂量使用它只会给身体带来有益的影响。
    Ethanol extracts obtained from 13 poplar propolis samples originating from various European countries by traditional maceration were tested for total polyphenols, flavonoid content, and antioxidant activity. Moreover, the content of 18 polyphenolic compounds (from the group of phenolic acids and flavonoids) was determined using the HPLC method. The inhibitory effect of six selected extracts with the highest activity was assessed by well-diffusion method against five strains (Bifidobacterium spp., L. rhamnosus, L. acidophilus, E. coli, and Bacteroides spp.) of intestinal bacteria self-isolated from the faeces of obese probands with the use of selective media. It was found that the antioxidant activity of propolis varied depending on geographical origin and even among samples from the same region, which indicates that some other factors also influence propolis quality. The samples of different geographical origin varied mainly in the share of individual phenolic compounds, and it was not possible to find a characteristic marker of origin, excluding the galangin present in the Polish samples only. Assessing the inhibitory activity of propolis (in the range of 70 mg to 10 µg per mL) indicated that the concentration of 100 µg/mL was found as being safe for tested fecal bacteria (Bifidobacterium spp., L. rhamnosus, L. acidophilus, E. coli, and Bacteroides spp.). As no negative effect of low doses of propolis on the intestinal microflora was found, it can be suggested that its use in recommended doses brings only beneficial effects to the body.
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  • 文章类型: Journal Article
    蜜蜂收集的花粉(BCP)和蜜蜂面包(BB)是以其有益的生物学特性而闻名的蜜蜂产品。这项研究的主要目的是研究BB微生物群及其对BB发挥的生物活性的贡献。通过不依赖培养的方式研究了在不同成熟阶段收集的BB样品的微生物群(NextGenerationSequencing,NGS)和依赖于文化的方法。微生物群落在BB成熟过程中动态波动,在成熟的BB中结束于稳定的微生物群落结构。测试了蜜蜂面包细菌分离株的表型和与酶的产生和分泌以及抗菌活性有关的基因。在309个细菌分离物中,41个分泌的半纤维素酶,13纤维素酶,39淀粉酶,132蛋白酶,85考马斯亮蓝G或R染料降解酶和72孔雀石绿染料降解酶。此外,在309个细菌分离物中,42对金黄色葡萄球菌具有抗菌活性,34针对铜绿假单胞菌,47对抗肠沙门氏菌。鼠伤寒和43抗肺炎克雷伯菌。与新鲜的BCP相比,人工发酵样品具有更高的抗菌活性,强烈表明BB微生物群有助于BB抗菌活性。我们的发现表明,BB微生物群是新型抗微生物剂和酶的未开发来源,可能导致在医学和食品工业中的新应用。
    Bee-collected pollen (BCP) and bee bread (BB) are honey bee products known for their beneficial biological properties. The main goal of this study was to investigate BB microbiota and its contribution to bioactivity exerted by BB. The microbiota of BB samples collected at different maturation stages was investigated via culture-independent (Next Generation Sequencing, NGS) and culture-dependent methods. Microbial communities dynamically fluctuate during BB maturation, ending in a stable microbial community structure in mature BB. Bee bread bacterial isolates were tested for phenotypes and genes implicated in the production and secretion of enzymes as well as antibacterial activity. Out of 309 bacterial isolates, 41 secreted hemicellulases, 13 cellulases, 39 amylases, 132 proteinases, 85 Coomassie brilliant blue G or R dye-degrading enzymes and 72 Malachite Green dye-degrading enzymes. Furthermore, out of 309 bacterial isolates, 42 exhibited antibacterial activity against Staphylococcus aureus, 34 against Pseudomonas aeruginosa, 47 against Salmonella enterica ser. Typhimurium and 43 against Klebsiella pneumoniae. Artificially fermented samples exerted higher antibacterial activity compared to fresh BCP, strongly indicating that BB microbiota contribute to BB antibacterial activity. Our findings suggest that BB microbiota is an underexplored source of novel antimicrobial agents and enzymes that could lead to new applications in medicine and the food industry.
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  • 文章类型: Journal Article
    这篇综述的目的是介绍樟脑-双环单萜酮在预防皮肤感染中的潜在应用。皮肤病代表一组异质性疾病,其特征在于显著降低生活质量的延长症状。它们影响真皮,表皮,甚至是皮下组织.它们通常具有细菌或真菌背景。皮肤病学皮肤病的治疗是困难和长期的。因此,找到一个化合物很重要,最好是天然来源的,(i)防止这种感染的开始和(ii)支持皮肤的修复过程。根据其记录的抗炎作用,抗菌,抗真菌药,抗痤疮,麻醉剂,加强,和变暖特性,樟脑可用作皮肤传染病的预防措施,也可用作医疗和化妆品的成分。这项工作讨论了樟脑的结构和理化性质,它的发生,以及从天然来源以及通过化学合成获得它的方法。还介绍了樟脑在工业制剂中的用途。此外,在详细查阅文献后,樟脑的新陈代谢,它与其他药用物质的相互作用,讨论了其对皮肤病中涉及的细菌和真菌的抗微生物特性。
    The aim of this review is to present the potential application of camphor-a bicyclic monoterpene ketone-in the prevention of skin infections. Skin diseases represent a heterogeneous group of disorders characterized by prolonged symptoms that significantly diminish the quality of life. They affect the dermis, the epidermis, and even subcutaneous tissue. They very often have a bacterial or fungal background. Therapy for dermatological skin disorders is difficult and long-term. Therefore, it is important to find a compound, preferably of natural origin, that (i) prevents the initiation of this infection and (ii) supports the skin\'s repair process. Based on its documented anti-inflammatory, antibacterial, antifungal, anti-acne, anesthetic, strengthening, and warming properties, camphor can be used as a preventative measure in dermatological infectious diseases and as a component in medical and cosmetic products. This work discusses the structure and physicochemical properties of camphor, its occurrence, and methods of obtaining it from natural sources as well as through chemical synthesis. The use of camphor in industrial preparations is also presented. Additionally, after a detailed review of the literature, the metabolism of camphor, its interactions with other medicinal substances, and its antimicrobial properties against bacteria and fungi involved in skin diseases are discussed with regard to their resistance.
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  • 文章类型: Journal Article
    次级代谢产物,活生物体产生的生物活性化合物,可以揭示自然界中的共生关系。在这项研究中,从含有次生代谢产物的溶剂上清液中提取与共生细菌(Xenorhabdusstockiae和Photorhabdusluminescens)相关的土传昆虫病原线虫,证明了对大肠杆菌的显著抑制作用,金黄色葡萄球菌,B.subtilus,P.奇迹,E.粪便,还有P.Stutzeri.通过傅立叶变换红外光谱对这些次生代谢物的表征揭示了蛋白质的胺基,多酚的羟基和羧基,多糖的羟基,和有机酸的羧基。此外,通过高效液相色谱法分析获得的粗提物,以基本鉴定潜在的生物活性肽。气相色谱-质谱分析来自Xenorhabdusstoriae的乙酸乙酯提取物确定了主要化合物,包括壬酸衍生物,脯氨酸,巴霉素,八癸醛衍生物,三氧杂-5-氮杂-1-硅双环,4-十八进制,甲酯,油酸,和1,2-苯二羧酸。从发光光纹素中进行额外的提取,产生了功能化合物,例如吲哚-3-乙酸,邻苯二甲酸,1-十四醇,奈莫索诺,1-二十烷醇,和不饱和脂肪酸。这些发现支持用于未来病原体抑制的新型天然抗微生物剂的潜在开发。
    Secondary metabolites, bioactive compounds produced by living organisms, can unveil symbiotic relationships in nature. In this study, soilborne entomopathogenic nematodes associated with symbiotic bacteria (Xenorhabdus stockiae and Photorhabdus luminescens) were extracted from solvent supernatant containing secondary metabolites, demonstrating significant inhibitory effects against E. coli, S. aureus, B. subtilus, P. mirabilis, E. faecalis, and P. stutzeri. The characterization of these secondary metabolites by Fourier transforms infrared spectroscopy revealed amine groups of proteins, hydroxyl and carboxyl groups of polyphenols, hydroxyl groups of polysaccharides, and carboxyl groups of organic acids. Furthermore, the obtained crude extracts were analyzed by high-performance liquid chromatography for the basic identification of potential bioactive peptides. Gas chromatography-mass spectrometry analysis of ethyl acetate extracts from Xenorhabdus stockiae identified major compounds including nonanoic acid derivatives, proline, paromycin, octodecanal derivatives, trioxa-5-aza-1-silabicyclo, 4-octadecenal, methyl ester, oleic acid, and 1,2-benzenedicarboxylicacid. Additional extraction from Photorhabdus luminescens yielded functional compounds such as indole-3-acetic acid, phthalic acid, 1-tetradecanol, nemorosonol, 1-eicosanol, and unsaturated fatty acids. These findings support the potential development of novel natural antimicrobial agents for future pathogen suppression.
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  • 文章类型: Journal Article
    这项研究的目的是获得新的卤代内酯,其在环己烷环(在C-3或C-5碳)中具有宝石-二甲基基团,在内酯环中具有甲基基团,然后使用丝状真菌对其进行生物转化。对两种非对映异构体混合物形式的卤代内酯进行生物转化筛选,这表明只有具有位于C-5碳的宝石-二甲基基团的化合物被转化。镰刀菌属菌株进行水解脱卤,而来自Absidia属的菌株对C-7碳进行了羟基化。然后测试底物和生物转化产物对细菌和酵母样真菌的多重耐药菌株的抗微生物活性。化合物5b对杜布立尼和白色念珠菌的抗真菌活性最高,而化合物4a获得了对金黄色葡萄球菌MRSA的抗微生物活性。
    The aim of this study was to obtain new halolactones with a gem-dimethyl group in the cyclohexane ring (at the C-3 or C-5 carbon) and a methyl group in the lactone ring and then subject them to biotransformations using filamentous fungi. Halolactones in the form of mixtures of two diasteroisomers were subjected to screening biotransformations, which showed that only compounds with a gem-dimethyl group located at the C-5 carbon were transformed. Strains from the genus Fusarium carried out hydrolytic dehalogenation, while strains from the genus Absidia carried out hydroxylation of the C-7 carbon. Both substrates and biotransformation products were then tested for antimicrobial activity against multidrug-resistant strains of both bacteria and yeast-like fungi. The highest antifungal activity against C. dubliniensis and C. albicans strains was obtained for compound 5b, while antimicrobial activity against S. aureus MRSA was obtained for compound 4a.
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