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Frontmatter
Pub Date : 2018-09-01 DOI: 10.1515/znc-2018-frontmatter9-10
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引用次数: 0
Frontmatter
Pub Date : 2018-07-01 DOI: 10.1515/znc-2018-frontmatter7-8
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引用次数: 0
Synthesis and biological evaluation of newer 1,3,4-oxadiazoles incorporated with benzothiazepine and benzodiazepine moieties 含苯并噻唑和苯二氮卓的1,3,4-恶二唑的合成及生物学评价
Pub Date : 2017-02-09 DOI: 10.1515/znc-2016-0129
P. Navin, Patel Sarvil, P. Amit, P. Divyesh, Rajani Dhansukh, R. Moo-Puc, G. Rivera
Abstract A series of thiazepines and diazepines having 1,3,4-oxadiazole moiety were synthesized, and they were analyzed for their in vitro antimicrobial activity against several bacteria (Staphylococcus aureus, Staphylococcus pyogenes, Escherichia coli, and Pseudomonas aeruginosa) and fungi (Candida albicans, Aspergillus niger, and Aspergillus Clavatus) and protozoa (Entamoeba histolytica, Giardia lamblia, Trypanosoma cruzi and Leishmania mexicana). Few of the selected compounds were tested for their antitubercular activity. However, it was noticed that the potency of final analogs against each strain placed reliance on the type of substituent present on aryl ring of oxadiazole as well as presence of thiophene, pyridine, and furan at benzothiazepines and benzodiazepines. The biological screening identified that some of the compounds were found to possess good antimicrobial and antitubercular (62.5–100 μg/mL of MIC) activity.
摘要合成了一系列含有1,3,4-恶二唑片段的噻唑类药物和二氮类药物,分析了它们对几种细菌(金黄色葡萄球菌、化脓性葡萄球菌、大肠杆菌、铜绿假单胞菌)、真菌(白色念珠菌、黑曲霉、克拉曲霉)和原虫(溶组织内阿米巴、兰贾第鞭毛虫、克氏锥虫和墨西哥利什曼原虫)的体外抑菌活性。所选化合物中很少有抗结核活性。然而,人们注意到,最终类似物对每种菌株的效力取决于恶二唑芳基环上取代基的类型,以及苯并噻唑类和苯二氮卓类药物中噻吩、吡啶和呋喃的存在。生物学筛选发现部分化合物具有良好的抗菌和抗结核活性(MIC值为62.5 ~ 100 μg/mL)。
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引用次数: 8
Bioenergetic strategy of microalgae for the biodegradation of tyrosol and hydroxytyrosol 微藻生物降解酪醇和羟基酪醇的生物能策略
Pub Date : 2017-02-07 DOI: 10.1515/znc-2016-0214
Aikaterini Papazi, A. Ioannou, Myrto Symeonidi, A. Doulis, K. Kotzabasis
Abstract Olive mill wastewater has significant polluting properties due to its high phenolic content [mainly tyrosol (trs) and hydroxytyrosol (htrs)]. Growth kinetics and a series of fluorescence induction measurements for Scenedesmus obliquus cultures showed that microalgae can be tolerant of these phenolic compounds. Changes in the cellular energy reserves and concentration of the phenolic compounds adjust the “toxicity” of these compounds to the microalgae and are, therefore, the main parameters that affect biodegradation. Autotrophic growth conditions of microalgae and high concentrations of trs or htrs induce higher biodegradation compared with mixotrophic conditions and lower phenolic concentrations. When microalgae face trs and htrs simultaneously, biodegradation begins from htrs, the more energetically demanding compound. All these lead to the conviction that microalgae have a “rational” management of cellular energy balance. Low toxicity levels lead to higher growth and lower biodegradation, whereas higher toxicity levels lead to lower growth and higher biodegradation. The selection of appropriate conditions (compatible to the bioenergetic strategies of microalgae) seems to be the key for a successful biodegradation of a series of toxic compounds, thus paving the way for future biotechnological applications for solving complicated pollution problems, like the detoxification of olive mill wastewater.
橄榄厂废水中酚类物质(主要是酪醇(trs)和羟基酪醇(htrs))含量高,具有显著的污染特性。生长动力学和一系列的荧光诱导测量表明,微藻可以耐受这些酚类化合物。细胞能量储备和酚类化合物浓度的变化调节了这些化合物对微藻的“毒性”,因此是影响生物降解的主要参数。与混合营养条件和低酚浓度相比,微藻自养生长条件和高浓度trs或htrs诱导的生物降解率更高。当微藻同时面对trs和htrs时,生物降解从htrs开始,htrs是一种更需要能量的化合物。所有这些都使我们相信微藻对细胞能量平衡有着“理性”的管理。低毒性水平导致较高的生长和较低的生物降解,而高毒性水平导致较低的生长和较高的生物降解。选择合适的条件(与微藻的生物能策略相容)似乎是成功生物降解一系列有毒化合物的关键,从而为未来生物技术应用于解决复杂的污染问题铺平了道路,如橄榄厂废水的解毒。
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引用次数: 11
Effects of Hypericum perforatum extract on oxaliplatin-induced neurotoxicity: in vitro evaluations 贯叶连翘提取物对奥沙利铂诱导的神经毒性的影响:体外评价
Pub Date : 2017-02-04 DOI: 10.1515/znc-2016-0194
L. Cinci, L. di Cesare Mannelli, A. Maidecchi, L. Mattoli, C. Ghelardini
Abstract Hypericum perforatum L. has been used for centuries as a natural remedy for the treatment of many disorders. Neuropathic pain is a common side effect of oxaliplatin-based chemotherapy and often the cause of therapy discontinuation. Thanks to its anti-inflammatory and analgesic effects, the use of H. perforatum may be a novel therapeutic strategy for neuropathy. The aim of this paper was to evaluate the effect of H. perforatum hydrophilic extract on an in vitro model of oxaliplatin-induced neurotoxicity. The antioxidant potential of extract was first evaluated in cell-free models by the thiobarbituric acid-reactive substances assay and nitro blue tetrazolium oxidation test; the ability of H. perforatum extract to reduce oxaliplatin-induced caspase-3 activity in rat astrocytes and its potential interference with the cytotoxic effects of oxaliplatin in a colorectal cancer in vitro model (HT-29 cells) were also evaluated. The extract showed a significant antioxidant effect and was able to reduce caspase-3 activity in rat astrocytes. Of note, the extract alone exerted a cytotoxic effect in HT-29 cells and did not reduce the cytotoxicity of oxaliplatin in HT-29 cells. These data suggest that H. perforatum could be used as a novel therapeutic strategy for counteracting chemotherapy-induced neuropathy.
几个世纪以来,贯叶连翘(Hypericum perforatum L.)一直被用作治疗许多疾病的天然药物。神经性疼痛是基于奥沙利铂的化疗的常见副作用,经常导致治疗中断。由于其抗炎和镇痛作用,使用贯叶连翘可能是一种新的治疗神经病变的策略。本研究旨在评价贯叶连翘亲水性提取物对奥沙利铂诱导的神经毒性体外模型的影响。通过硫代巴比妥酸活性物质测定和硝基蓝四氮唑氧化试验,首先在无细胞模型中评价提取物的抗氧化潜力;在结直肠癌体外模型(HT-29细胞)中,还评估了贯叶连翘提取物降低奥沙利铂诱导的大鼠星形胶质细胞caspase-3活性的能力及其对奥沙利铂细胞毒性作用的潜在干扰。该提取物具有明显的抗氧化作用,可降低大鼠星形胶质细胞中caspase-3的活性。值得注意的是,提取物单独对HT-29细胞产生细胞毒性作用,并没有降低奥沙利铂对HT-29细胞的细胞毒性。这些数据表明,贯叶连翘可以作为一种新的治疗策略来对抗化疗引起的神经病变。
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引用次数: 12
Bioenergetics of lactate vs. acetate outside TCA enhanced the hydrogen evolution levels in two newly isolated strains of the photosynthetic bacterium Rhodopseudomonas 两株新分离的光合细菌红假单胞菌(Rhodopseudomonas)中,TCA外乳酸与乙酸的生物能量学提高了析氢水平
Pub Date : 2017-01-25 DOI: 10.1515/znc-2016-0070
A. Danial, A. M. Abdel Wahab, Houssam H Arafat, R. Abdel-Basset
Abstract Two local hydrogen-evolving strains of purple nonsulfur bacteria have been isolated, characterized, and identified as Rhodopseudomonas sp. TUT (strains Rh1 and Rh2). Lactate followed by succinate and malate supported the highest amounts of H2 production, growth (O.D.660nm, proteins and bacteriochlorphyll contents), nitrogenase activity, and uptake hydrogenase; the least of which was acetate. Alginate-immobilized cells evolved higher hydrogen amounts than free cell counterparts. Rh1 was more productive than Rh2 at all circumstances. Lactate-dependent hydrogen evolution was more than twice that of acetate, due to ATP productivity (2/–1, respectively), which is limiting to the nitrogenase activity. The preference of lactate over other acids indicates the feasibility of using these two strains in hydrogen production from dairy wastewater.
摘要分离并鉴定了两株本地紫色非硫细菌,鉴定为Rhodopseudomonas sp. TUT(菌株Rh1和Rh2)。乳酸、琥珀酸和苹果酸对H2产量、生长(od值为660nm,蛋白质和细菌叶绿素含量)、氮酶活性和摄取氢化酶的影响最大;其中最少的是醋酸盐。海藻酸固定的细胞进化出比自由细胞更高的氢含量。Rh1在任何情况下都比Rh2生产效率高。由于ATP产量(分别为2/ -1),乳酸依赖的析氢量是醋酸盐的两倍多,这限制了氮酶的活性。乳酸对其他酸的偏好表明这两种菌株在乳品废水制氢中的可行性。
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引用次数: 3
Influence of structure of lactones with the methylcyclohexene and dimethylcyclohexene ring on their biotransformation and antimicrobial activity 含甲基环己烯和二甲基环己烯的内酯结构对其生物转化和抗菌活性的影响
Pub Date : 2017-01-20 DOI: 10.1515/znc-2016-0188
Katarzyna Wińska, M. Grabarczyk, Wanda Mączka, B. Żarowska, G. Maciejewska, M. Anioł
Abstract The aim of this article is influence of the structure of lactones with the methylcyclohexene and dimethylcyclohexene ring on their biotransformation and antimicrobial activity. This work was based on the general remark that even the smallest change in the structure of a compound can affect its biological properties. The results of the biotransformation of four bicyclic unsaturated lactones with one or two methyl groups in the cyclohexene ring was tested using fifteen fungal strains (Fusarium species, Penicillium species, Absidia species, Cunninghamella japonica, and Pleurotus ostreatus) and five yeast strains (Yarrowia lipolytica, Rhodorula marina, Rhodorula rubra, Candida viswanathii, and Saccharomyces cerevisiae). During these transformations, new epoxylactone and hydroxylactone were obtained. The relationship between the substrate structure and the ability of the microorganisms to transform them were analysed. Only compounds with C–O bond of lactone ring in the equatorial position were transformed by fungus. All presented here lactones were examined also for their antimicrobial activity. It turned out that these compounds exhibited growth inhibition of bacteria and fungi, mainly Bacillus subtilis, Candida albicans, Aspergillus niger, and Penicillium expansum.
摘要本文研究了含甲基环己烯和二甲基环己烯的内酯结构对其生物转化和抗菌活性的影响。这项工作是基于一个普遍的观点,即即使是化合物结构上最小的变化也会影响它的生物学特性。利用15株真菌(镰刀菌属、青霉属、Absidia属、Cunninghamella japonica、Pleurotus ostreatus)和5株酵母菌(Yarrowia lipolytica、Rhodorula marina、Rhodorula rubra、Candida viswanathii、Saccharomyces cerevisiae)对4种环己烯环上含有1个或2个甲基的双环不饱和内酯进行了生物转化试验。在这些转化过程中,得到了新的环氧内酯和羟内酯。分析了底物结构与微生物转化底物能力的关系。真菌只转化了内酯环C-O键位于赤道位置的化合物。所有在这里提出的内酯也检查了他们的抗菌活性。结果表明,这些化合物对细菌和真菌的生长具有抑制作用,主要是枯草芽孢杆菌、白色念珠菌、黑曲霉和扩张青霉。
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引用次数: 5
Antinociceptive effect of Aristolochia trilobata stem essential oil and 6-methyl-5-hepten-2yl acetate, its main compound, in rodents 三叶马兜铃精油及其主要化合物6-甲基-5-庚烯-2乙酸酯对啮齿动物的抗伤感受作用
Pub Date : 2017-01-20 DOI: 10.1515/znc-2016-0053
J. Quintans, R. S. Alves, D. A. Santos, M. Serafini, P. Alves, E. Costa, G. Zengin, L. Quintans-Júnior, A. Guimarães
Abstract Aristolochia trilobata L. is an aromatic plant, popularly known as “mil-homens”, and its essential oil (EO) is generally used to treat colic, diarrhea and dysentery disorders. We evaluated the antinociceptive effect of A. trilobata stem EO and of its major compound, the (R)-(-)-6-methyl-5-hepten-2-yl acetate (sulcatyl acetate: SA), using acetic acid (0.85%)-induced writhing response and formalin-induced (20 μL of 1%) nociceptive behavior in mice. We also evaluated the EO and SA effect on motor coordination, using the rota-rod apparatus. EO (25, 50 and 100 mg/kg) or SA (25 and 50 mg/kg) reduced nociceptive behavior in the writhing test (p<0.001). EO (100 mg/kg) and SA (25 and 50 mg/kg) decreased the nociception on the first phase of the formalin test (p<0.05). On the second phase, EO (25: p<0.01; 50: p<0.05 and 100 mg/kg: p<0.001) and SA (25 and 50 mg/kg; p<0.001) reduced the nociceptive response induced by formalin. EO and SA were not able to cause changes in the motor coordination of animals. Together, our results suggest that EO has an analgesic profile and SA seems to be one of the active compounds in this effect.
摘要:三叶马兜铃(Aristolochia trilobata L.)是一种芳香植物,俗称“马兜铃”,其精油(EO)一般用于治疗绞痛、腹泻和痢疾等疾病。采用乙酸(0.85%)诱导小鼠扭体反应和福尔马林(20 μL 1%)诱导小鼠伤害性行为的方法,研究了三叶草提取物及其主要化合物(R)-(-)-6-甲基-5-庚烯-2-乙酸磺酰乙酸酯(SA)的抗伤害性作用。我们还使用旋转杆装置评估了EO和SA对运动协调的影响。EO(25、50和100 mg/kg)或SA(25和50 mg/kg)在扭体试验中降低了伤害性行为(p<0.001)。EO (100 mg/kg)和SA(25和50 mg/kg)降低了福尔马林第一阶段试验的伤害感受(p<0.05)。在第二阶段,EO (25: p<0.01;50: p<0.05和100 mg/kg: p<0.001)和SA(25和50 mg/kg;P <0.001)降低了福尔马林诱导的伤害性反应。EO和SA不能引起动物运动协调性的改变。综上所述,我们的研究结果表明,EO具有镇痛作用,而SA似乎是这种作用中的活性化合物之一。
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引用次数: 3
PEGylation potentiates hepatoma cell targeted liposome-mediated in vitro gene delivery via the asialoglycoprotein receptor 聚乙二醇化增强肝癌细胞靶向脂质体介导的体外基因传递通过asialalglyprotein受体
Pub Date : 2017-01-07 DOI: 10.1515/znc-2016-0172
N. K. Mkhwanazi, C. D. de Koning, W. V. van Otterlo, M. Ariatti, Moganavelli Singh
Abstract Hepatocellular carcinoma is a burgeoning health issue in sub-Saharan Africa and East Asia where it is most prevalent. The search for gene medicine treatment modalities for this condition represents a novel departure from current treatment options and is gaining momentum. Here we report on nonPEGylated and on sterically stabilized PEGylated cationic liposomes decorated with D-galacto moieties linked to 24.1 Å spacers for asialoglycoprotein receptor (ASGP-R)-targeted vehiculation of pCMV-luc plasmid DNA. Cargo DNA is fully liposome associated at N/P ratio=3:1 and is partially protected from the effects of serum nucleases. Moreover, at this ratio, lipoplex dimensions (89–97 nm) are compatible with the requirements for extravasation in vivo. Ethidium displacement assays show that the reporter DNA is in a less condensed state when bound to PEGylated liposomes than with nonPEGylated liposomes. PEGylated lipoplexes were well tolerated by both HEK293 (ASGP-R-negative) and HepG2 (ASGP-R-positive) cell lines and delivered DNA to the human hepatoma cell line HepG2 by ASGP-R mediation at levels three-fold greater than nonPEGylated lipoplexes. PEGylated ASGP-R-targeted liposomes reported in this study possess the required characteristics for hepatotropic gene delivery and may be considered for further application in vivo.
肝细胞癌是撒哈拉以南非洲和东亚地区一个新兴的健康问题,在那里它是最普遍的。对这种疾病的基因药物治疗方式的研究代表了对当前治疗方案的一种新颖的背离,并且正在获得动力。在这里,我们报道了非聚乙二醇化和空间稳定的聚乙二醇化阳离子脂质体,这些脂质体由连接24.1 Å间隔物的d -半乳糖修饰,用于asialglycoprotein receptor (ASGP-R)靶向pCMV-luc质粒DNA的载体化。货物DNA是完全脂质体,N/P比=3:1,部分保护不受血清核酸酶的影响。此外,在这个比例下,脂质体尺寸(89-97 nm)符合体内外渗的要求。乙啶置换试验表明,报告DNA在与聚乙二醇化脂质体结合时比与非聚乙二醇化脂质体结合时处于更少的凝聚状态。聚乙二醇化脂质体对HEK293 (ASGP-R阴性)和HepG2 (ASGP-R阳性)细胞系均具有良好的耐受性,并通过ASGP-R介导向人肝癌细胞系HepG2传递DNA,其水平比非聚乙二醇化脂质体高3倍。本研究报道的聚乙二醇化asgp - r靶向脂质体具有致肝基因传递所需的特性,可以考虑进一步在体内应用。
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引用次数: 3
Termiglaucescin, a new polyhydroxy triterpene glucoside from Terminalia glaucescens with antioxidant and anti-inflammatory potential 冬青素是一种新的多羟基三萜葡萄糖苷,具有抗氧化和抗炎作用
Pub Date : 2016-12-20 DOI: 10.1515/znc-2016-0178
A. Dawé, B. Talom, G. W. Kapche, Kauser Siddiqui, Fawai Yakai, E. Talla, M. A. Shaiq, Iqbal Lubna, B. T. Ngadjui
Abstract Termiglaucescin (1), a new triterpene glucoside, has been isolated from the ethyl acetate extract of the root bark of Terminalia glaucescens Planch. ex Benth, together with 11 known compounds, β-D-glucopyranosyl 2α,3β,6β-trihydroxy-23-galloylolean-12-en-28-oate (2), arjunglucoside I (3), sericoside (4), arjungenin (5), sericic acid (6), arjunetin (7), chebuloside II (8), 3,3′,4-tri-O-methylelagic acid (9), 3,3′-di-O-methylelagic acid (10), β-sitosterol (11) and stigmasterol (12). Compounds 2, 3, 7, 8 and 9 are reported from the plant for the first time. The structures of the isolated compounds were characterized by spectroscopic data interpretations, especially 1D and 2D NMR. The triterpenic isolates showed potent antioxidant and anti-inflammatory activities.
摘要:从毛茛根皮的乙酸乙酯萃取物中分离得到一种新的三萜葡萄糖苷Termiglaucescin(1)。ex Benth,连同11个已知化合物,β- d -葡萄糖吡喃基2α,3β,6β-三羟基-23-没食子甘油三酯-12-烯-28-燕麦酸酯(2),arjungen苷I(3),丝胶苷(4),arjungenin(5),丝胶酸(6),arjunetin (7), chebulo苷II(8), 3,3 ',4-三-o -甲基鞣花酸(9),3,3 ' -二-o -甲基鞣花酸(10),β-谷甾醇(11)和豆甾醇(12)。化合物2、3、7、8和9为首次从该植物中分离得到。分离得到的化合物的结构通过波谱数据,特别是一维和二维核磁共振进行了表征。三萜分离物具有较强的抗氧化和抗炎活性。
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引用次数: 4
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