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Role of CNK1, Ephrin B1, GPR19 and SMURF1 in breast cancer early diagnosis, metastasis and drug resistance CNK1、Ephrin B1、GPR19和SMURF1在乳腺癌早期诊断、转移和耐药中的作用
Pub Date : 2021-06-06 DOI: 10.21608/EJCHEM.2021.77940.3833
Afnan N. Abdrabou, Sara M. Radwan, Reham El shimy, H. E. Mesallamy
Background: The extracellular signal-regulated kinase (ERK) pathway is a key signaling pathway involved in the regulation of normal cell proliferation, survival and differentiation. However, aberrant regulations of the ERK pathway contribute to cancer and other human diseases. Objective: This study was designed to investigate the role of some ERK pathway effectors such as the connector enhancer of kinase suppressor of Ras1 (CNK1), Ephrin B1, G protein-coupled receptor 19 (GPR19) and SMAD ubiquitination regulatory factor 1 (SMURF1) in breast cancer (BC) diagnosis and metastasis risk prediction. Methods: The study involved 50 (ERPRHer2=6, ERPRHer2=11, ERPRHER2=8, ERPRHer2=25) newly diagnosed BC patients, 15 chemotherapy resistant BC patients, 15 benign breast tumor patients and 10 controls. All total 65 BC patients (including the chemotherapy resistant group) were subdivided into two groups: metastatic BC (17 patients), and nonmetastatic BC group (48 patients). CNK1, Ephrin B1, GPR19 and SMURF1 serum levels were analyzed using ELISA. Results: The study revealed significantly higher serum levels of CNK1, Ephrin B1, GPR19 and SMURF1 in all malignant groups (ERPRHer2, ERPRHer2, ERPRHER2, ERPRHer2), as well as a significant elevation in the chemotherapy resistant BC group as compared to non-resistant group (P < 0.001). They also revealed excellent value for de novo BC diagnosis and metastasis prediction. Conclusion: CNK1, Ephrin B1, GPR19 and SMURF1 may be considered as novel biomarkers for BC diagnosis and prediction of metastasis risk.
背景:细胞外信号调节激酶(extracellular signal-regulated kinase, ERK)通路是参与调节正常细胞增殖、存活和分化的关键信号通路。然而,ERK通路的异常调控导致癌症和其他人类疾病。目的:探讨Ras1激酶抑制因子连接增强子(CNK1)、Ephrin B1、G蛋白偶联受体19 (GPR19)、SMAD泛素化调节因子1 (SMURF1)等ERK通路效应物在乳腺癌(BC)诊断和转移风险预测中的作用。方法:新诊断BC患者50例(ERPRHer2=6, ERPRHer2=11, ERPRHer2= 8, ERPRHer2=25),化疗耐药BC患者15例,乳腺良性肿瘤患者15例,对照组10例。所有65例BC患者(包括化疗耐药组)被细分为两组:转移性BC(17例)和非转移性BC组(48例)。ELISA法检测各组血清CNK1、Ephrin B1、GPR19、SMURF1水平。结果:研究显示,在所有恶性组(ERPRHer2、ERPRHer2、ERPRHer2、ERPRHer2)中,血清CNK1、Ephrin B1、GPR19和SMURF1水平均显著升高,且化疗耐药的BC组与非耐药组相比显著升高(P < 0.001)。它们还显示了对新发BC的诊断和转移预测的良好价值。结论:CNK1、Ephrin B1、GPR19和SMURF1可作为诊断和预测BC转移风险的新型生物标志物。
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引用次数: 0
Synthesis, Characterization and Biological Activity Study of Cobalt(II), Nickel(II) and Copper(II) Complexes Derived from Mixed Bi dentate Ligands of Oxime and Phenanthroline11 肟和邻菲罗啉混合双齿配体衍生钴(II)、镍(II)和铜(II)配合物的合成、表征及生物活性研究11
Pub Date : 2021-06-05 DOI: 10.21608/EJCHEM.2021.78216.3827
M. Abid, Fathil R. Hafith, Taghreed M. Musa, B. F. Abbas
The present work involves the synthesis and characterization of cobalt (II), nickel (II) and copper (II) complexes derived from (1:1:1) mole ratios of coumarine-oxime:1,10-phenanthroline:metal ions with respect to the continuous variation method of Job via spectroscopic studies. The isolated metal complexes were characterized with their ligands of 3-acetoxime-coumarine by elemental analyses, FT-IR, EI-MS and NMR spectra. The flame atomic absorption spectroscopy, molar conductivity in DMF and magnetic moment measurements were also employed to determine the supposed molecular weights and their geometry. Furthermore the gravimetric thermal analysis (TG-DTA) was estimated for copper(II) and nickel(II) complexes and the observed data form weight loss percents confirmed the suggested chemical formulas and structures of complexes. The results observed from UV-Visible spectra and elemental analyses together with mass spectra confirmed the octahedral geometry around the cobalt(II) and copper(II) ions whereas the diamagnetic complex of nickel(II) was square-planner in [Ni(Phen)(L)]Cl2 formula. As well as the biological activities of complexes solutions were tested against two types of bacteria and the inhibition zones data proved that all solutions were active compared with standard drugs of 10 ppm concentrations.
目前的工作涉及合成和表征钴(II),镍(II)和铜(II)络合物衍生(1:1:1)摩尔比香豆素-肟:1,10-菲罗啉:金属离子通过光谱研究的连续变化方法。通过元素分析、红外光谱(FT-IR)、质谱(EI-MS)和核磁共振谱(NMR)对金属配合物进行了表征。火焰原子吸收光谱、DMF的摩尔电导率和磁矩测量也被用来确定假设的分子量和它们的几何形状。此外,还对铜(II)和镍(II)配合物进行了重热分析(TG-DTA),并从失重率的数据中证实了所建议的配合物的化学式和结构。紫外-可见光谱、元素分析和质谱结果证实了钴(II)和铜(II)离子周围的八面体几何结构,而镍(II)的抗磁性配合物在[Ni(Phen)(L)]Cl2分子式中呈方形规划。并对配合物溶液对两种细菌的生物活性进行了测试,抑菌区数据证明,与浓度为10ppm的标准药物相比,所有溶液都具有活性。
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引用次数: 0
Synthesis and Characterization of Novel Pyrazole Derivatives from 4-Florophenylhydrazine and Study Their Cytotoxicity as Anti-Cancer Agent 11 新型4-Florophenylhydrazine吡唑衍生物的合成、表征及抗癌细胞毒性研究
Pub Date : 2021-06-05 DOI: 10.21608/EJCHEM.2021.78214.3825
Sumaya M. Salih, Hameed M. Alkubaisi, F. L. Faraj
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引用次数: 0
Synthesis and Structural Studies of Transition Metals Complexes with Poly dentate Azo dye ligand Derived from Coumarine11 香豆素偶氮染料配体过渡金属配合物的合成与结构研究
Pub Date : 2021-06-05 DOI: 10.21608/EJCHEM.2021.78215.3826
A. Jabbar, M. Al-Jibouri, A. H. Ismail
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引用次数: 0
Synthesis, characterization, and anticoagulant activity of new functionalized biscoumarins 新型功能化双香豆素的合成、表征和抗凝血活性
Pub Date : 2021-06-05 DOI: 10.21608/EJCHEM.2021.73699.3641
Yasser Fakri Mustafa, E. Mohammed, R. Khalil
Despite their rarity and structural complexity, natural and synthetic biscoumarins have polarized much attention from investigators particularly due to their characteristic activity as anticoagulant agents. In this work, a panel of twelve functionalized biscoumarins was synthesized in two schematic steps; the first one started by condensing various phenol-based derivatives with malonic acid via a Pechmann-type reaction yielding alkyl-substituted 4-hydroxycoumarins herein symbolized as (E1-E12). The latter compounds were undergone a self-coupling under the influence of methylene iodide to afford the target functionalized biscoumarins, which were symbolized as (EY1-EY12). The potential of the synthesized biscoumarins as anticoagulant applicants was investigated in vivo using rabbit as an animal model. The employed assay was the prothrombin time that was monitored after three and five days of the last oral treatment. The results gathered from this test revealed that the synthesized biscoumarins have a promising anticoagulant activity compared with warfarin as a standard anticoagulant drug, with privileged influence contributed to those substituted at position 7 of the coumarin framework. The authors concluded that the substitution of an alkyl group at that position of the coumarin monomer may intensify the anticoagulant activity of the prepared biscoumarins. Also, this intensity was directly proportionated to the increase in the molecular weight of this alkyl group. Accordingly, the synthesized biscoumarins possessing this property would provide an efficient base for synthesizing new compounds, which have a promising anticoagulant effect.
尽管天然双香豆素和合成双香豆素罕见且结构复杂,但由于其作为抗凝血剂的特性,研究人员对它们的关注已经分化。在这项工作中,通过两个示意图步骤合成了12个功能化双香豆素;第一种是通过pechmann型反应将各种酚基衍生物与丙二酸缩合,生成烷基取代的4-羟基香豆素,符号为(E1-E12)。后一种化合物在碘化亚甲基的作用下发生自偶联,得到目标功能化双香豆素,符号为(EY1-EY12)。以兔为动物模型,研究了合成的双香豆素作为抗凝剂的潜力。所采用的测定方法是在最后一次口服治疗3天和5天后监测凝血酶原时间。实验结果表明,与华法林相比,合成的双香豆素具有很好的抗凝活性,在香豆素框架的第7位取代的那些具有特殊的影响。作者认为,在香豆素单体的该位置取代烷基可能会增强所制备的双香豆素的抗凝血活性。而且,这种强度与烷基分子量的增加成正比。因此,所合成的双香豆素具有这一特性,将为合成具有良好抗凝作用的新化合物提供有效的基础。
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引用次数: 15
Preparation and Characterization of some new Benzothiazole-Heterocyclic Derivatives 新型苯并噻唑杂环衍生物的制备与表征
Pub Date : 2021-06-01 DOI: 10.21608/EJCHEM.2021.73818.3650
R. Aldujaili, A. Alhasan
In this work new different hetero cyclic derivatives were synthesized that which including β-Lactam, teterazole and also thiazole rings.The starting material is 2-amino-6-methoxy-Benzothiazole. All these reactions follow by (TLC) and Measurement melting points for some of these derivatives. The compounds identified by FT-IR and some of them by 1H-NMR and 13C-NMR spectra., The prepared benzothiazole derivatives in this study gave good results through appearance of new bands and disapearance of other bands in formatted compounds that gave first data to formation benzothiazole derivative , while second technique represented by resonance spectra that gave also good results for formatted benzothiazole derivative.m in addition to flowing of all reactions by paper chromatography.
本文合成了新的杂环衍生物,包括β-内酰胺、四唑和噻唑环。原料为2-氨基-6-甲氧基苯并噻唑。所有这些反应都遵循(TLC)和测量这些衍生物的熔点。化合物经FT-IR鉴定,部分经1H-NMR和13C-NMR鉴定。本研究制备的苯并噻唑衍生物通过在格式化的化合物中出现新的带和其他带的消失得到了很好的结果,这为苯并噻唑衍生物的形成提供了第一个数据,而以共振光谱为代表的第二种技术也为格式化的苯并噻唑衍生物提供了很好的结果。M除流动外,所有的反应都用纸色谱法。
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引用次数: 2
Prediction of Thermal Isomerization Temperatures of Substituted Benzocyclobutenes to o- Quinodimethanes Using Hardness, Polarizability and energies of σ, σ* and π* orbitals. 利用σ、σ*和π*轨道的硬度、极化率和能预测取代苯并环丁烯到o-喹二甲烷的热异构化温度。
Pub Date : 2021-06-01 DOI: 10.21608/EJCHEM.2021.50081.3057
A. Al-Sabawi, Hyffaa Y. Hussien, Abdulkhalik S. Alkazzaz
The prediction of Thermal Isomerization temperatures (IT) of benzocyclobutenes is useful for their applications in synthesis and polymerization. In this study, ITs were predicted by equations formulated from the hardness, of the products transition states or the difference between the hardness of product and transition state. Also, ITs predicted from the orbital energies of the σ, σ*, π and π* orbitals of the benzocyclobutenes.
预测苯并环丁烯的热异构化温度对其在合成和聚合中的应用具有重要意义。在本研究中,ITs是由硬度,产品的过渡态或产品的硬度与过渡态之差的公式来预测的。同时,利用苯并环丁烯的σ、σ*、π和π*轨道的轨道能量进行了预测。
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引用次数: 0
Bioactive Phytoconstituents of Morus Plants exhibiting Numerous Therapeutic Activities 桑属植物具有多种治疗活性的生物活性成分
Pub Date : 2021-06-01 DOI: 10.21608/EJCHEM.2021.76688.3788
Alaadin E. El-Haddad, E. Deeb, A. Amer, Amr M. Saadeldeen, Fakher M. Ahmed, M. Salem, H. Taha
Morus is a plant genus of the family Moraceae, most of which is used as a decoction in traditional medicines for the treatment of cough, bronchitis, pulmonary diseases and reduces the plasma sugar level. Many studies in Morus phytochemistry have contributed to the discovery of Diels-Alder-type adducts, arylbenzofurans, and flavonoids with antioxidant, antihyperglycemic, antihypertensive, antihyperlipidemic, and anti-inflammatory activities. The purpose of this article was to offers an account of the updated knowledge on the phytochemicals and pharmacological activities of these compounds. This review will help to fully understanding the efficacy and pave the way for further explore the comprehensive use of Morus. We conclude that Morus needs further reports in the identification of bioactive constituents and strengthen the claim of folk medicines.
桑葚是桑科的一种植物属,在传统医药中多作为汤剂用于治疗咳嗽、支气管炎、肺部疾病和降低血糖水平。在桑树植物化学的许多研究中,发现了具有抗氧化、降糖、降压、降血脂和抗炎活性的双桤木型加合物、芳基苯并呋喃和类黄酮。本文的目的是对这些化合物的植物化学成分和药理活性的最新知识进行介绍。本文综述有助于充分认识桑属植物的药效,为进一步探索桑属植物的综合利用铺平道路。我们认为桑属植物在生物活性成分鉴定方面需要进一步的报道,并加强民间药物的主张。
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引用次数: 1
Rate Theory and Relaxation Map Analysis of Iodine-Doped Poly(Ethyl Methacrylate) composite films using Thermally Stimulated Depolarization Current-Thermal Sampling (TSDC-TS) Technique 利用热激退极化电流-热采样(TSDC-TS)技术分析掺碘聚甲基丙烯酸乙酯复合膜的速率理论和弛豫图
Pub Date : 2021-05-31 DOI: 10.21608/EJCHEM.2021.69217.3516
Wafaa B. Elsharkawy
Abstract. Iodine-doped Poly (Ethyl Methacrylate) composites have been prepared using casting method. Global TSDC of the composite samples has been investigated using TSDC-TS technique. It is found that, global TSDC spectra of pure PEMA are characterized by two relaxations. The first relaxation which is observed as a shoulder in the temperature range 324-333 K is attributed to the motion of side group and named -relaxation. Whereas, the second relaxation is observed in the glass temperature range of PEMA at Tm= 347 K and named as dipolar relaxation, i.e., -relaxation. On doping with iodine, a new relaxation peak has been obtained at high temperatures ~ 397-409 K, and named as space charge relaxation, i.e., -relaxation. Complex TSDC spectra of PEMA-Iodine composites have been resolved into its elementary peaks using TS technique. These elementary peaks have been used to construct relaxation map (RM) of all samples using Eyring transformation. The existence of compensation phenomenon for all samples is also verified and the coordinates of each compensation point have been estimated. These coordinates are used to calculate the density of disorder (DOD) and thermal expansion coefficient of the samples. The thermodynamic parameters of the samples, such as, enthalpy, entropy and Gibbs free energy have been calculated at different poling temperatures.
摘要采用铸造法制备了掺杂碘的聚甲基丙烯酸乙酯复合材料。采用TSDC- ts技术对复合材料样品的整体TSDC进行了研究。发现纯PEMA的全局TSDC谱具有两个弛豫特征。在324 ~ 333k温度范围内观察到的第一个松弛为肩状松弛,归因于侧基的运动,命名为-松弛。而在PEMA的玻璃温度范围内(Tm= 347 K)出现了第二次弛豫,称为偶极弛豫,即-弛豫。碘掺杂后,在~ 397 ~ 409 K的高温下出现了一个新的弛豫峰,命名为空间电荷弛豫,即-弛豫。利用TS技术对pma -碘复合材料的TSDC光谱进行了解析。这些基本峰被用来用Eyring变换构造所有样本的松弛图(RM)。验证了所有样本都存在补偿现象,并估计了每个补偿点的坐标。这些坐标用于计算样品的无序密度(DOD)和热膨胀系数。计算了样品在不同极化温度下的焓、熵和吉布斯自由能等热力学参数。
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引用次数: 1
Beneficial Bioapplications of Silver Nanoparticles Synthesized by a Marine Crustacean (Erugosquilla massavensis) 海洋甲壳类合成银纳米粒子的有益生物应用
Pub Date : 2021-05-30 DOI: 10.21608/EJCHEM.2021.70308.3549
D. Beltagy, N. Abdo, N. Samak, Gihan M. El-khodary, K. Abdel-Aziz, M. Mona
Silver nanoparticles (AgNPs) have wide applications. Production of AgNPs can be occurred through different method chemical, physical, and green methods. The most popular methods are chemical approaches. Marine organisms exhibit a wide range of bioactivity. The present study was designed to establish the biosynthesis of silver nanoparticles from marine crustacean extract of the hard and soft parts of male and female E. massavensis. The microstructure, morphology and optical absorption properties of the nanoparticles were characterized by X-ray diffraction (XRD), scanning electron microscopy (SEM) and UV-visible spectroscopy. The formation of silver nanoparticles was confirmed by Uv-Vis absorption and the spectra were observed plasmon bands between 441.79–462.74 nm. XRD results show that the nanoparticles are crystalline in nature. SEM images detected the quasi-spherical AgNPs morphological shape. Silver nanoparticles from marine crustacean extract of the hard part of male E. massavensis (HM4) showed the best results in morphology and particle size. Evaluation of the cytotoxicity of AgNPs (HM4) on different cancer cell lines antiviral, anti-microbial, anti-diabetic, anti-arthritic, anti-aging and anti-inflammatory properties were assessed. AgNPs characterization may be introduced a promising applications in medical aspects.
纳米银具有广泛的应用前景。AgNPs的生产可以通过不同的方法发生,化学,物理和绿色方法。最常用的方法是化学方法。海洋生物表现出广泛的生物活性。本研究旨在建立海洋甲壳类动物提取液的生物合成纳米银的方法。采用x射线衍射(XRD)、扫描电镜(SEM)和紫外可见光谱(UV-visible spectroscopy)对纳米颗粒的微观结构、形貌和光学吸收性能进行了表征。紫外可见吸收证实了银纳米粒子的形成,光谱在441.79 ~ 462.74 nm之间。XRD结果表明,所制备的纳米颗粒具有结晶性质。SEM图像检测到AgNPs的准球形形态。以马尾松雄鱼硬部海洋甲壳类提取液(HM4)制备的银纳米粒子在形态和粒径上效果最好。评价AgNPs (HM4)对不同肿瘤细胞系的抗病毒、抗微生物、抗糖尿病、抗关节炎、抗衰老和抗炎作用。AgNPs的表征在医学方面具有广阔的应用前景。
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引用次数: 0
期刊
The Egyptian Journal of Chemistry
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