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A one-pot Synthesis of Some New Heterocyclic Compounds Derived from Chalcones and Study of their Antitumor and Antimicrobial Activities 查尔酮类杂环化合物的一锅合成及其抗肿瘤和抗菌活性研究
Pub Date : 2022-12-01 DOI: 10.21608/jsrs.2022.275779
Hadeer M. Hassan, Eman A. Mohamed, B. Awad, Eman M. Mohamed
The aim of the present work is to efficiently synthesize promising novel antitumor and antimicrobial active heterocyclic compounds from chalcones 1a and 1b as a precursor which contain naphthalene moiety and indole or piperonal moiety, respectively, using conventional, ultrasonic and microwave irradiation techniques. The best yields and purity were afforded with the microwave irradiation technique. Reaction of 1a and 1b with the appropriate reagent gave the corresponding pyrazolines 2a, 2b, pyrimidine-2-thioneses 3a, 3b, oxazepines 4a, 4b, diazepines 5a, 5b, triazolo-pyrimidines 6a, 6b, and pyrimidine-2-thiols 7a, 7b derivatives. Compounds 7a, 7b were used to produce 8a, 8b. Moreover, pyrimidine-2-thione 3a was used to synthesize pyrimidin2-ylthioacetic acid 9a, and 2-hydrazinylpyrido[2,3-d]pyrimidine derivative 10a which has been used as a functionalizing agent to produce compounds 11a-14a. The structural formulas of the synthesized compounds were confirmed by their spectral data; FT-IR, H NMR, C NMR and MS. Compounds 3a, 5a, 7a, 13a showed a very high activity as antitumor, whereas compounds 4a, 6a, and 13a showed high activity as antibacterial and antifungal agents.
以查尔酮1a和查尔酮1b为前体,分别含有萘段和吲哚或胡椒基段,利用常规、超声和微波辐照技术,高效合成具有抗肿瘤和抗菌活性的新型杂环化合物。采用微波辐照技术获得了最佳的收率和纯度。1a和1b与相应的试剂反应得到相应的吡唑啉2a、2b、嘧啶-2-硫醚3a、3b、恶氮卓类4a、4b、二氮卓类5a、5b、三唑嘧啶6a、6b和嘧啶-2-硫醚7a、7b衍生物。化合物7a、7b分别用于制备8a、8b。利用嘧啶-2-硫酮3a合成了嘧啶-2-基硫乙酸9a,并以2-肼基吡啶[2,3-d]嘧啶衍生物10a作为功能化剂制备了化合物11a-14a。合成的化合物的结构式通过光谱数据得到了证实;其中化合物3a、5a、7a、13a具有较高的抗肿瘤活性,化合物4a、6a、13a具有较高的抗菌和抗真菌活性。
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引用次数: 0
Impacts of Genetically Modified Food on Insulin Hormone, Glucose, and Lipid Profile of Male and Female Wister Albino Rats 转基因食品对雄性和雌性白化大鼠胰岛素、激素、葡萄糖和脂质谱的影响
Pub Date : 2022-12-01 DOI: 10.21608/jsrs.2022.275795
Manal A. Salama, Ola S. Serag El Din, Nehal A. Abd El Wahed
In recent years, genetically modified (GM) crops aim to produce food and feed which has become part of the usual agriculture in many areas of the world. Whether GM food and feed have positive or negative impacts on humans or animals is still unclear. Therefore, an investigation of the effects of different diets containing genetically modified food (GMF) on insulin hormone, glucose, and lipid profile were carried out in the present study. Male and female Wister Albino rats70-80 g range body weight was used in the present study. Each sex was divided into 4 groups (n = 10 per group). Control group fed on the basal diet American Institute of Nutrition for Growth (AIN93 G) and three treated groups were given GM (corn, wheat, and rice) and water adlibitum for three months. The reason for choosing these foods is because they are the most basic foods consumed in our daily life (bread and rice). At the end of the experimental period results compared to the control group GM (corn, wheat, and rice) for both sexes showed a significant decrease in serum insulin and the significant increase in serum glucose. Also, significant increase in total cholesterol (TC) , triglycerides (TG), low density lipoprotein-cholesterol (LDL-C), very low density lipoproteins (VLDL), Risk ratio I and Risk ratio II. Yet, serum high density lipoproteins cholesterol (HDL-C) levels showed significant decrease in all groups. Body weight showed a significant increase in all groups of males and female rats.
近年来,转基因作物旨在生产粮食和饲料,这已成为世界许多地区常规农业的一部分。转基因食品和饲料对人类或动物的影响是正面的还是负面的,目前还不清楚。因此,本研究旨在研究含转基因食品(GMF)的不同饮食对胰岛素、激素、葡萄糖和血脂的影响。本研究选用70 ~ 80 g体重范围的雄性和雌性Wister Albino大鼠。每个性别分为4组,每组n = 10。对照组饲喂美国生长营养研究所(AIN93 G)基础日粮,3个试验组饲喂转基因玉米、小麦和水稻,连续3个月饮水。选择这些食物的原因是因为它们是我们日常生活中最基本的食物(面包和米饭)。在试验期结束时,与对照组相比,转基因(玉米、小麦和水稻)组的男女血清胰岛素显著降低,血清葡萄糖显著升高。此外,总胆固醇(TC)、甘油三酯(TG)、低密度脂蛋白-胆固醇(LDL-C)、极低密度脂蛋白(VLDL)、风险比I和风险比II显著增加。然而,血清高密度脂蛋白胆固醇(HDL-C)水平在所有组中均显著降低。所有雄性和雌性大鼠的体重都明显增加。
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引用次数: 0
Cell progression of biofilm formation in Candida albicans and estimation of aspartic proteinase activity 白色念珠菌生物膜形成的细胞进程和天冬氨酸蛋白酶活性的估计
Pub Date : 2022-12-01 DOI: 10.21608/jsrs.2022.275792
Rowida Elshazly, Shaimaa Selmi Sobieh, Sanaa Sobhy Zaki, Sahar Abdel Fattah Abdel Tawab
Yeast cells are commonly used as powerful model system to study morphological phenotype and their processes. The study of morphogenesis of different modes of growth in yeast during biofilm development is an important issue. Cell progression is important tool to understand morphological transition and virulence in C. albicans. Biofilm formation and aspartic proteinase activity are two major important virulence factors associated with the pathogenicity of C. albicans. This study aimed to highlight the formation of biofilm, monitor the development of biofilm progression and estimate the activity of aspartic proteinase. Biofilm formation was assessed by Eliza plate and monitored at different pH values, different incubation time and different media. Biofilm development was visualized microscopically. Cell division and mitotic phases in yeast cells were studied and photographed. The production of aspartic proteinase was assessed by bovine serum albumin agar plates and evaluated at different pH values and different incubation time intervals. Results revealed that C. albicans was positive for biofilm formation and aspartic proteinase production. pH and different media had marked significant effect on biofilm formation. Additionally, the transition from simple yeast budding form to a complex filament structure was time dependent. Moreover, pH showed significant effect on aspartic proteinase activity.
酵母细胞通常被用作研究形态表型及其过程的有力模型系统。研究酵母在生物膜发育过程中不同生长方式的形态发生是一个重要的课题。细胞进展是了解白色念珠菌形态转变和毒力的重要工具。生物膜形成和天冬氨酸蛋白酶活性是与白色念珠菌致病性相关的两个重要毒力因子。本研究旨在揭示生物膜的形成,监测生物膜的进展,并估计天冬氨酸蛋白酶的活性。在不同的pH值、不同的培养时间和不同的培养基下,采用elisa平板检测生物膜的形成情况。显微镜下观察生物膜的发育。对酵母细胞的分裂和有丝分裂期进行了研究和拍照。用牛血清白蛋白琼脂平板测定天冬氨酸蛋白酶的产量,并在不同的pH值和不同的孵育时间间隔下进行测定。结果显示,白色念珠菌对生物膜的形成和天冬氨酸蛋白酶的产生呈阳性。pH和不同培养基对生物膜的形成有显著影响。此外,从简单的酵母出芽形式到复杂的细丝结构的转变与时间有关。pH对天冬氨酸蛋白酶活性有显著影响。
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引用次数: 0
Molecular Identification of Ladybird Beetles (Coccinella: Coccinellidae) Using DNA Barcodes 基于DNA条形码的瓢虫分子鉴定(瓢虫科
Pub Date : 2022-12-01 DOI: 10.21608/jsrs.2022.275796
Hanan Abdalla, Yosur Gamal Fiteha, Mohamed Abdel-Salam Rashed, Ramadan Mohamed Ali, Aya Mohamed Abdel-Salam Hammad, Ahmed Saber Mohamed Bream, Mahmoud Magdy
DNA barcoding is a molecular genetics technique commonly applied for species identification based on the cytochrome c oxidase subunit I (COI) gene located on the mitochondrial DNA genome. Based on our analysis, the DNA barcodes were generated from 16 specimen of Coccinella (family Coccinellidae). All the samples were collected from diverse sites in Egypt and Libya. Morphological traits based on the number of dorsal spots, DNA extraction, PCR amplification of COI, sequencing, nucleotide BLAST, and phylogenetics analyses were used to classify the specimens. A phylogenetic tree was constructed using the maximum likelihood method, including 46 COI sequences (the study and NCBI sequences). Three Coccinella clusters were defined and classified as Coccinella septempunctata, Coccinella novemnotata, and Coccinella undecimpunctata each species clustered into a unique branch. DNA barcodes discriminated clearly against the analyzed species. This study validated the COI efficiency as a marker for DNA barcoding of insects (Coccinella, family Coccinellidae).
DNA条形码是一种常用的分子遗传学技术,基于线粒体DNA基因组上的细胞色素c氧化酶亚基I (COI)基因进行物种鉴定。基于我们的分析,生成了16份球菌属(Coccinella)标本的DNA条形码。所有的样本都是从埃及和利比亚的不同地点收集的。根据背斑数量、DNA提取、COI PCR扩增、测序、核苷酸BLAST和系统发育分析等形态学特征对标本进行分类。采用最大似然法构建系统发育树,包括46条COI序列(本研究序列和NCBI序列)。定义了3个瓢虫群,分别为七星瓢虫、新星瓢虫和非影响瓢虫,每一种都聚集在一个独特的分支中。DNA条形码对所分析的物种有明显的区别。本研究验证了COI作为昆虫(Coccinella, coccinellae科)DNA条形码标记的有效性。
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引用次数: 0
Trends in the assessment of multidrug efficiency against identified bacterial strains isolated from wounds at El-Demerdash Hospital, Egypt 对埃及El-Demerdash医院伤口分离出的已确定菌株的多药疗效评估趋势
Pub Date : 2022-12-01 DOI: 10.21608/jsrs.2022.275789
Howida R. Mohammed, Zeinab M.H. Kheiralla, Maha A. Hewedy, Ayman F. Ahmed, Elham E. Moustafa, Salah Abdelbary
Multidrug-resistant (MDR) bacteria is a severe problem for universal public health which increases morbidity and mortality rate. These resistant bacteria lead to ineffective treatment of drugs resulting in the spreading and persistence of infections. So, the major target of this study is to estimate the competence of multidrug antibacterial agents against bacterial strains isolated from wound samples and then identify the most potent Multidrug-resistant (MDR) bacteria. Fifty wound swab specimens were gathered from various wounds and several patients from the Central Microbiology Laboratory of El-Demerdash Hospital, Cairo, Egypt. Eightynine bacterial isolates were isolated from fifty wound samples then cultured on different media and tested for their susceptibility to different thirty antibiotic discs using the agar disc diffusion method. After recording the results of the susceptibility test, the post potent resistant bacterial isolates recorded 3 bacterial isolates which resistant to 30 different antibiotic types. These resistant bacterial isolates were identified using morphological, biochemical, and molecular techniques. The results recorded that the post potent resistant bacterial isolates identified as Klebsiella oxytoca, Pseudomonas aeruginosa, and Escherichia coli. This study concluded that with the increase in the random use of antibiotic drugs resulted in the presence of multi-antibacterial resistant strains. There are bacterial strains that were isolated from wounds in patients at El-Demerdash Hospital, Egypt, and identified. They can resist about thirty different antibiotic discs. Abbreviation: Multiple antibiotic resistance (MAR).
耐多药细菌(MDR)是一个严重的公共卫生问题,它增加了发病率和死亡率。这些耐药细菌导致药物治疗无效,导致感染的传播和持续存在。因此,本研究的主要目标是评估多药抗菌剂对伤口样品中分离的细菌的能力,从而确定最有效的多药耐药(MDR)细菌。从埃及开罗El-Demerdash医院中央微生物实验室的各种伤口和几名患者收集了50个伤口拭子标本。从50份创面样品中分离出89株细菌,分别在不同培养基上培养,采用琼脂盘扩散法检测其对30种不同抗生素片的敏感性。记录药敏试验结果后,有效耐药后分离菌株记录了3株对30种不同抗生素耐药的菌株。利用形态学、生化和分子技术鉴定了这些耐药菌株。结果表明,后强效耐药菌株为氧化克雷伯菌、铜绿假单胞菌和大肠杆菌。本研究认为,随着随机使用抗生素药物的增加,导致多重耐药菌株的出现。在埃及El-Demerdash医院,从病人的伤口中分离并鉴定出了一些细菌菌株。它们可以抵抗大约30种不同的抗生素盘。简称:多重抗生素耐药性(Multiple antibiotic resistance, MAR)。
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引用次数: 0
Antibiotic resistant and mecA gene characterization of Staphylococcus epidermidis isolated from five hospitals in Gaza strip 从加沙地带五家医院分离的表皮葡萄球菌的抗生素耐药性和mecA基因特征
Pub Date : 2022-02-28 DOI: 10.21608/jsrs.2020.41139.1026
M. Alnajar, S. Abdelsalam, N. E. El Aila, B. Ayesh, M. Fahd
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引用次数: 0
Reproductive Toxicity Induced by Low Dose Bisphenol A (BPA) in Male Rats 低剂量双酚A (BPA)对雄性大鼠生殖毒性的影响
Pub Date : 2022-02-28 DOI: 10.21608/jsrs.2020.40944.1029
sara elshafiey, M. El-Gendy, Mohamed Rashed, Ramadan Mohamed Ali, A. Kamel
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引用次数: 0
Efficiency of transgenic Chlamydomonas reinhardtii for removing of toxicity of cyanide compound 转基因莱茵衣藻对氰化物的脱毒效果
Pub Date : 2021-12-26 DOI: 10.21608/jsrs.2021.85161.1061
Rasha Elgammal, Y. El-Ayouty, S. Sobieh, wafaa abouelkheir, A. EL-Sheimy, A. Soror
In this study, we used the Agrobacterium tumefaciens–mediated transformation approach to transfer the activity of the cyanobacterial cyanase enzyme into the microalga, Chlamydomonas reinhardtii. In transgenic C. reinhardtii strains, the recombinant cyanase enzyme was proven to be active. In comparison to wild-type control, transgenic type demonstrated higher rates of ammonia release, reduced loss of pigmentation, and a lower percentage of growth retardation when varied amounts of cyanide (up to 200 ppm) were applied to the growth medium. Moreover, cyanase activity increases as concentration of cyanide increase especially in case of transgenic. The maximum activity was indicated in presence of 100 mg/l cyanide it reached eight folds more than wild activity at the same cyanide concentration. Results of this study provide an effective eco-friendly phytoremediation system for detoxification of cyanide using micro-alga compared to previously reported conventional system for removal of cyanide compounds, Also, some factors are taken in consideration like different pH, contact time and the transgenic type has been the priority for removal cyanide at wide range of pH with two folds more than wild type.
在这项研究中,我们使用农杆菌介导的转化方法将蓝藻的氰化酶活性转移到微藻莱茵衣藻中。在转基因莱茵梭菌中,重组氰化酶被证明是有活性的。与野生型对照相比,当在生长培养基中施用不同量的氰化物(高达200 ppm)时,转基因型表现出更高的氨释放率、更少的色素沉着损失和更低的生长迟缓百分比。此外,氰化酶活性随氰化物浓度的增加而增加,特别是在转基因情况下。当氰化物浓度为100 mg/l时,其活性达到野生活性的8倍。本研究结果为微藻解毒提供了一种有效的生态友好型植物修复系统,与以往报道的传统氰化物脱毒系统相比,考虑了不同pH、接触时间等因素,转基因微藻在大pH范围内的脱毒能力是野生型的2倍以上。
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引用次数: 2
Effect of Pb+2 ion on physico chemical properties of fly ash -slag geopolymer pastes Pb+2离子对粉煤灰-矿渣地聚合物膏体理化性能的影响
Pub Date : 2021-12-26 DOI: 10.21608/jsrs.2021.62415.1051
S. Abdallah, doaa abdelmonium, Sheren M. Ragai
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引用次数: 2
 Morphological and Quantitative traits of phylogenetic relationships of some barley (Hordeum vulgare L.) accessions in Egypt 埃及部分大麦(Hordeum vulgare L.)种质的形态和数量性状的系统发育关系
Pub Date : 2021-12-26 DOI: 10.21608/jsrs.2021.54324.1041
sarah shata, Wafaa Morsy, fatthy abdel-tawab, Lamyaa Kamal
arley (Hordeum vulgare L.) is one of the founder crops of Old-World agriculture, it was one of the first domesticated cereals. It is also a model experimental system because of its short life cycle and morphological, physiological, and genetic characteristics. Barley is used for, in order of importance, animal feed, brewing malts and human food. Barley is found in widely varying environments globally. It has wide adaptation ability to different climatic conditions and various environments comprising drought and irrigated environments (Nevo, 1992; Gomez-Macpherson, 2001).
大麦(Hordeum vulgare L.)是旧大陆农业的创始作物之一,它是最早被驯化的谷物之一。由于其生命周期短,具有形态、生理、遗传等方面的特点,也是一种典型的实验系统。大麦被用于,按重要性排序,动物饲料,酿造麦芽和人类食品。大麦在全球各种不同的环境中都有发现。它对不同的气候条件和包括干旱和灌溉环境在内的各种环境具有广泛的适应能力(Nevo, 1992;Gomez-Macpherson, 2001)。
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引用次数: 0
期刊
Journal of Scientific Research in Science
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