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Desmarestia anceps Montagne (Phaeophyceae) against Colorectal Cancer Cells: Cytotoxic Activity and Proapoptotic Effects 对大肠癌细胞的细胞毒活性及促凋亡作用
Pub Date : 2022-01-01 DOI: 10.4236/abc.2022.126019
R. Frassini, D. Steffens, S. Moura, C. Aguzzoli, A. P. Martins, P. Colepicolo, M. Fujii, N. Yokoya, C.M.P. Pereira, Ana Cláudia Phillipus, M. Falkenberg, J. P. Henriques, M. Roesch-Ely
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引用次数: 0
Phytochemical Analysis and Bioactivity Screening of Primary and Secondary Metabolic Products of Medicinal Plants in the Valleys of Medina Region Saudi Arabia 沙特阿拉伯麦地那地区山谷药用植物初级和次级代谢产物的植物化学分析及生物活性筛选
Pub Date : 2022-01-01 DOI: 10.4236/abc.2022.124009
Safa Alsaedi, G. Aljeddani
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引用次数: 4
Syntheses, Characterization and Biological Activity of Novel Thiazoylazo Dye and Its Coordination Compounds 新型噻唑偶氮染料及其配位化合物的合成、表征及生物活性研究
Pub Date : 2021-09-26 DOI: 10.4236/abc.2021.115013
T. Aiyelabola
The present work describes the synthesis of a novel heterocyclic azo dye by general diazonization of 2-amino-4,5-dimethylthiazole followed by the diazo- coupling of the resulting diazonium ion with 5-methyl-2-(propan-2-yl)phenol to obtain ligand L. This was characterized using Fourier-transformed infrared and electronic spectrophotometry. Ligand L was further coordinated with five metal ions, M:L, 1:2 [M = Cu(II), Mn(II), Zn(II), Ni(II) and Co(II)]. The coordination compounds obtained were characterized by electronic, IR spectrophotometry, magnetic susceptibility and percentage metal analyses. The results obtained suggested that a thiazoylazo dye was obtained as ligand L. It was proposed that two molecules of the solvent coordinated to the metal ion in addition with the ligands to give an octahedral geometry for copper(II), manganese(II) and nickel(II) complexes. On the other hand, square planar geometry was suggested for zinc(II) and cobalt(II) complexes. The anti-infla- mmatory activity of the ligand and coordination compounds was evaluated using four in vitro-based assays viz: xanthine oxidase and lipoxygenase inhibition assay, membrane stability and protein denaturation assay. The synthesized compounds generally exhibited good anti-inflammatory activity in all the assays carried out. However, the reference standards, in this instance, were more effective in the case of xanthine oxidase, lipoxygenase and protein denaturation inhibitory assays. For the membrane stability study, the coordination compounds and ligand L elicited more potent anti-inflammatory activity than the standard drug.
本文介绍了一种新型杂环偶氮染料的合成方法,该方法是将2-氨基-4,5-二甲基噻唑进行重氮化,然后将重氮离子与5-甲基-2-(丙二基)苯酚进行重氮偶联,得到配体l。配体L进一步与5种金属离子M:L, 1:2配位[M = Cu(II), Mn(II), Zn(II), Ni(II)和Co(II)]。通过电子、红外光谱、磁化率和金属百分比分析对所制得的配合物进行了表征。结果表明,得到了一种噻唑偶氮染料作为配体l,并提出溶剂的两个分子与金属离子配位,使铜(II)、锰(II)和镍(II)配合物具有八面体的几何结构。另一方面,锌(II)和钴(II)配合物建议采用方形平面几何结构。通过黄嘌呤氧化酶和脂氧合酶抑制实验、膜稳定性和蛋白质变性实验等四种体外实验,对配体和配合物的抗炎活性进行了评价。在所进行的所有实验中,所合成的化合物普遍表现出良好的抗炎活性。然而,在这种情况下,参考标准品在黄嘌呤氧化酶、脂氧合酶和蛋白质变性抑制试验中更有效。在膜稳定性研究中,配位化合物和配体L比标准药物具有更强的抗炎活性。
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引用次数: 2
Application of TIRFM in Biomolecule Research and Clinical Medicine TIRFM在生物分子研究和临床医学中的应用
Pub Date : 2021-09-26 DOI: 10.4236/abc.2021.115014
Ye-Qin Zhang
With the increasing demand for imaging quality, many scientists constantly explore new imaging instruments to meet the requirements. The total internal reflection fluorescence microscopy has some incomparable superiorities, so it has become one of the research hotspots in recent years. It can show great performance in single-molecule imaging because it has unique imaging principles. This apparatus is used mainly in two fields, biomolecule research and clinical medicine. To know this instrument’s function, the summary of applications in these two parts was given in this article. Now, scientists who have been focusing on this apparatus try to make this microscope combined with other late-model precise instruments that probe some unknown interaction mechanism of action. The TIRFM will show extraordinary talents in many aspects, and it will become a powerful tool for people to explore the mysteries of life.
随着对成像质量要求的不断提高,许多科学家不断探索新的成像仪器来满足要求。全内反射荧光显微镜具有无与伦比的优势,成为近年来的研究热点之一。它具有独特的成像原理,可以在单分子成像中显示出良好的性能。该仪器主要应用于生物分子研究和临床医学两个领域。为了了解该仪器的功能,本文对这两部分的应用进行了总结。现在,一直专注于这种仪器的科学家们试图将这种显微镜与其他晚期精密仪器相结合,以探测一些未知的相互作用机制。TIRFM将在许多方面展现非凡的才能,它将成为人们探索生命奥秘的有力工具。
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引用次数: 1
Triterpenoids and Semisynthetic Derivatives with Antimicrobial Activities from the Leaves of Caloncoba glauca (Flacourtiaceae) 海苔叶中的三萜类化合物及具有抗菌活性的半合成衍生物
Pub Date : 2021-07-22 DOI: 10.4236/abc.2021.114011
J. Mpetga, A. R. N. Donfack, J. Tamokou, Iréne Chinda Kengne, P. Tane, Xiao-jiang Hao, Mathieu Tene
Chemical investigation of the MeOH extract from the leaves of C. glauca yielded nine known triterpenoids (1-9) belonging to the cycloartane and friedelane series. Two of these compounds namely glaucartanoic acid A (1) and 3β,21β-dihydroxy-30-nor-(D:A)-friedoolean-20(29)-en-27-oic acid (5) were subjected to chemical derivatizations and afforded five new derivatives: diacetylglaucartanoic acid A (1a), 24-acetylglaucartanoic acid A (1b), glaucartanoic acid A methyl ester (1c), 24-methoxyglaucartanoic acid A methyl ester (1d), and 3β,21β-diacetoxy-30-nor-(D:A)-friedoolean-20(29)-en-27-oic acid (5a). Their structures were assigned based on their NMR and MS data and by comparison with literature values. The MeOH extract, isolated compounds and some new semi-synthetic derivatives were subjected to in vitro antimicrobial assays against a panel of pathogenic microorganisms, including Gram-positive and Gram-negative bacteria, and fungi using broth microdilution method. The MeOH extract displayed activity towards all the tested pathogenic bacterial and fungal strains with good activity (MIC against Staphylococcus aureus ATCC25923 and Shigella flexneri SDINT. Compounds 3 and 5 showed the most potent antimicrobial effect.
对C.glauca叶中MeOH提取物的化学研究产生了九种已知的三萜类化合物(1-9),属于环artane和friedelane系列。其中两个化合物,即海蓝酸A(1)和3β,21β-二羟基-30-或-(D:A)-Freedoolean-20(29)-en-27-酸(5,21β-二乙酰氧基-30-或-(D:A)-friedolean-20(29)-烯-27-酸(5a)。基于它们的NMR和MS数据并通过与文献值的比较来确定它们的结构。使用肉汤微量稀释法对甲醇提取物、分离的化合物和一些新的半合成衍生物进行了体外抗菌试验,以对抗一组病原微生物,包括革兰氏阳性菌和革兰氏阴性菌,以及真菌。MeOH提取物对所有测试的具有良好活性的致病细菌和真菌菌株都显示出活性(对金黄色葡萄球菌ATCC25923和福氏志贺菌SDINT的MIC)。化合物3和5显示出最有效的抗菌作用。
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引用次数: 2
Design, Synthesis and in Vitro Antibacterial Activity of 2-thiomethyl-benzimidazole Derivatives 2-硫代甲基苯并咪唑衍生物的设计、合成及体外抗菌活性
Pub Date : 2021-07-22 DOI: 10.4236/abc.2021.114012
Ablo Evrard, Coulibali Sioménan, Camara Tchambaga Etienne, Touré Daouda, C. Souleymane, Sissouma Drissa, A. Ané
A series of novel substituted benzimidazole (7a - n) derivatives were synthesized and characterized by 1H, 13C Nuclear Magnetic Resonance (NMR) spectra and High Resolution Mass Spectrometry (HRMS). The substitution was done in position -1 and -2 by appropriate groups. These compounds are obtained by N-alkylation reaction with thiomethyl-1H-benzimidazole intermediates (5a - g). Design of intermediates (5a - g) was made by condensation reaction between 2-methylbenzimidazole thiourunium salt (3) and functionalized halides (4) in the presence of sodium hydroxide (NaOH). Among the twenty-one compounds synthesized, ten were evaluated for their antimicrobial activity on three bacterial strains namely: Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923 and Pseudomonas aeruginosa ATCC 27853. Only E. coli ATTC 25922 was susceptible to the synthesized derivatives 5g, 7f and 7h with a significant antibacterial activity (CMI is between 250 and 500 μg/mL).
合成了一系列新的取代苯并咪唑(7a-n)衍生物,并用核磁共振(NMR)和高分辨质谱(HRMS)对其进行了表征。由适当的组在位置-1和位置-2进行置换。这些化合物是通过与硫代甲基-1H-苯并咪唑中间体(5a-g)的N-烷基化反应获得的。中间体(5a-g)的设计是通过2-甲基苯并咪唑硫鎓盐(3)和官能化卤化物(4)在氢氧化钠(NaOH)存在下的缩合反应进行的。在合成的21种化合物中,有10种化合物对3种细菌菌株进行了抗菌活性评价,即:大肠杆菌ATCC 25922、金黄色葡萄球菌ATCC 25923和铜绿假单胞菌ATCC 27853。只有大肠杆菌ATTC 25922对合成的衍生物5g、7f和7h敏感,具有显著的抗菌活性(CMI在250至500μg/mL之间)。
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引用次数: 2
Syntheses, Characterization, Antimicrobial Activity and Extraction Studies of Tetraaza Macrocyclic/Linear Schiff Bases Derived from Benzene-1,4-Dicarboxaldehyde and Their Coordination Compounds 苯-1,4-二甲酸四氮杂大环/线性席夫碱及其配位化合物的合成、表征、抗菌活性及提取研究
Pub Date : 2021-05-11 DOI: 10.4236/ABC.2021.113007
T. Aiyelabola, J. Jordaan, D. Otto, E. Akinkunmi
Non-template [2 + 2] condensation of benzene-1,4-dicarboxaldehyde with two diamines: ethane-1,2-diamine and propane-1,2-diamine was carried out to give Ligands 1 and 2. Additionally, template [1 + 2] condensation of benzene-1,4-dicarboxaldehyde with ethane-1,2-diamine and propane-1,2-diamine were also carried out to give Ligands 3 and 4. These were characterized using 1H and 13C NMR, UV-Vis and infra-red spectroscopy and mass spectrometry. Coordination compounds of each ligand were further synthesized using Ni(II) and Cu(II) ions. They were characterized by Uv-vis, infrared spectroscopy, mass spectrometry, magnetic susceptibility and energy dispersion X-ray spectroscopy EDX. The ligands and complexes were further analyzed for their antimicrobial activities and extraction efficiency. The results obtained suggested that tetraaza macrocyclic and linear compounds were obtained for [2 + 2] and [1 + 2] condensation reactions respectively. Coordination compounds of the macrocyclic ligand yielded octahedral geometry for Ni(II) and Cu(II) complexes of Ligand 1 and square planar geometry for Ni(II) and Cu(II) complexes of Ligand 2. On the other hand square planar geometry was proposed for coordination compounds of Ligand 3 and 4 exception for the Ni(II) complex of Ligand 3. All ligands coordinated to the metal ion in a tetradentate fashion. In some cases chelation enhanced the antimicrobial activity of some of the ligands. The results further showed that Ligands 1-4 effectively extracted cadmium(II). zinc(II) and lead(II) ions in solution.
苯-1,4-二甲醛与两种二胺:乙烷-1,2-二胺和丙烷-1,2-二胺进行非模板[2+2]缩合,得到配体1和2。此外,还进行了苯-1,4-二甲醛与乙烷-1,2-二胺和丙烷-1,2-二胺的模板[1+2]缩合,得到配体3和4。使用1H和13C NMR、UV-Vis和红外光谱以及质谱对其进行表征。使用Ni(II)和Cu(II)离子进一步合成了每个配体的配位化合物。通过紫外可见光谱、红外光谱、质谱、磁化率和能量色散X射线光谱EDX对它们进行了表征。进一步分析了配体和配合物的抗菌活性和提取效率。结果表明,四氮杂大环化合物和线性化合物分别用于[2+2]和[1+2]缩合反应。大环配体的配位化合物产生配体1的Ni(II)和Cu(II)配合物的八面体几何结构和配体2的Ni(Ⅱ)和铜(II)复合物的正方形平面几何结构。另一方面,对于配体3和配体4的配位化合物,除了配体3的Ni(II)络合物之外,提出了正方形平面几何结构。所有配体都以四齿的方式与金属离子配位。在某些情况下,螯合作用增强了一些配体的抗微生物活性。结果进一步表明,配体1-4有效地提取了镉(II)。锌(II)和铅(II)离子。
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引用次数: 4
Syntheses, Characterization and Biological Activity of Coordination Compounds of 3-Hydroxy-2-methyl-4 H -pyran-4-one and Its Mixed Ligand Complexes with 1,2-Diaminocyclohexane 3-羟基-2-甲基-4H-吡喃-4-酮及其与1,2-二氨基环己烷混合配体配合物的合成、表征及生物活性
Pub Date : 2021-05-11 DOI: 10.4236/ABC.2021.113008
T. Aiyelabola
Coordination compounds of 3-hydroxy-2-methyl-4H-pyran-4-one with iron(III), cobat(III) and chromium(III) were synthesized with M:L (1:2). Mixed ligand coordination compounds of 3-hydroxy-2-methyl-4H-pyran-4-one and 1,2-diaminocyclohexane using the same metal ions were also synthesized M:L1:L2 (1:1:1) where L1 is 3-hydroxy-2-methyl-4H-pyran-4-one and L2 is 1,2-diaminocyclohexane. The coordination compounds obtained were characterized using electronic and infrared spectral analyses, magnetic susceptibility and percentage metal analysis. They were also evaluated for their cytotoxic and antioxidant activities. The result obtained suggested that octahedral geometry was obtained for all the compounds, as a result of additional two molecules of the solvent coordinated to the metal ions. Both the primary and secondary ligands coordinated in a bidentate fashion. The synthesized compounds exhibited moderate cytotoxicity, although none was as active as the standard. The cobalt(III) mixed ligand complex elicited the highest activity. The synthesized compounds all exhibited good to moderate antioxidant activity.
用M∶L(1∶2)合成了3-羟基-2-甲基-4H-吡喃-4-酮与铁(III)、钴(III)和铬(III)的配位化合物。使用相同的金属离子合成了3-羟基-2-甲基-4H-吡喃-4-酮和1,2-二氨基环己烷的混合配体配位化合物M:L1:L2(1:1:1),其中L1是3-羟基-2-甲酯-4H-吡烷-4-酮,L2是1,2-二胺环己烷。利用电子和红外光谱分析、磁化率和金属百分比分析对所获得的配位化合物进行了表征。还评估了它们的细胞毒性和抗氧化活性。所获得的结果表明,由于另外两个溶剂分子与金属离子配位,所有化合物都获得了八面体几何结构。初级和次级配体都以双齿方式配位。合成的化合物表现出中等的细胞毒性,尽管没有一种化合物像标准化合物那样具有活性。钴(III)混合配体复合物引发了最高的活性。合成的化合物均表现出良好至中等的抗氧化活性。
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引用次数: 1
Ethnobotany, Pharmacology and Phytochemical Investigations of the Seeds of Pentaclethra macrophylla Benth (Mimosaceae) 大叶五草种子的民族植物学、药理学和植物化学研究(含笑科)
Pub Date : 2021-05-11 DOI: 10.4236/ABC.2021.113009
P. Sinda, B. Ponou, B. Tsafack, J. Kühlborn, R. Tchuenguem, R. Teponno, J. Dzoyem, T. Opatz, L. Tapondjou
Phytochemical investigation of the seeds of Pentaclethra macrophylla led to the isolation of a mixture of two new aromatic monoterpene glycosides, pentamacrophylloside A (1a) and pentamacrophylloside B (1b), together with six known secondary metabolites: Comososide (2), secopentaclethroside (3), caffeoylputrescine (4), β-sitosterol-3-O-β-D-glucopyranoside (5), 2-hydroxymethyl-5-(2-hydroxypropan-2-yl)phenol (6), and sucrose (7). Their structures were elucidated mainly by extensive spectroscopic analysis (1D and 2D NMR), high-resolution mass spectrometry and by comparison of their spectral data with those of related compounds. The extracts and compounds 3 and 4 were screened for their antimicrobial activity. The n-BuOH fraction showed a weak effect against three microbial strains: Candida albicans (MIC: 256 μg/mL), Enterococcus faecalis (MIC: 512 μg/mL), and Proteus mirabilis (MIC: 512 μg/mL) while no significant inhibition was observed for pure compounds when compared to ketoconazole and ciprofloxacin used as references. Furthermore, the ethnobotany and pharmacology of this plant are reviewed, and the chemophenetic significance of the isolation of the above secondary metabolites is discussed. This is the first report on the isolation of aromatic monoterpenoids from a plant of the genus Pentaclethra.
对大叶五肢草(Pentaclethra macrophylla)种子进行植物化学研究,分离出两种新的芳香单萜苷,五肢草苷a (1a)和五肢草苷B (1b),以及六种已知的次生代谢物:Comososide(2)、secopentaclethroside(3)、caffeoylpurescine(4)、β-谷甾醇-3- o -β- d -glucopyranoside(5)、2-hydroxymethyl-5-(2-hydroxypropan-2-yl)phenol(6)和蔗糖(7)。它们的结构主要通过广泛的光谱分析(1D和2D NMR)、高分辨率质谱分析以及与相关化合物的光谱数据比较来确定。对提取物及化合物3、4进行抑菌活性筛选。正丁醇提取物对白色念珠菌(MIC: 256 μg/mL)、粪肠球菌(MIC: 512 μg/mL)和奇异变形杆菌(MIC: 512 μg/mL)的抑菌效果较弱,对纯化合物的抑菌效果与酮康唑和环丙沙星对照无明显差异。综述了该植物的民族植物学和药理学研究进展,并对分离上述次生代谢物的化学意义进行了讨论。本文首次从五草属植物中分离得到芳香单萜类化合物。
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引用次数: 3
Association between Uric Acid and Metabolic Syndrome in Homozygous Sickle Cell Patients 纯合子镰状细胞患者尿酸与代谢综合征的关系
Pub Date : 2021-05-11 DOI: 10.4236/ABC.2021.113010
Kandji Pape Matar, Djité Moustapha, Barry Nene Oumou Kesso, Sagne René Ngor, Thioune Marême, Mbacke Ndoumbé Mame, N. H. Malick, G. Fatou, Lopez-Sall Philomène, C. Aynina, D. Amadou, Gueye Papa Madièye
The objective of this study was to assess the association between uric acid and the metabolic syndrome and its components in homozygous sickle cell patients. This is a prospective case/control study of sickle cell SS patients. Each patient was matched to a control of the same sex and age ± 2 years. In our framework, we used the criteria for defining metabolic syndrome according to International Diabetes Federation (IDF) 2009. Assay of all biological parameters was performed with the ARCHITECT ci4100, Abbot (Chicago, Illinois, USA). Data were collected with Excel 2016 software and statistical analysis was done using XLSTAT 2019 software. Student’s T test was used to compare means and a p-value less than 0.05 was considered significant. The study population consisted of 100 homozygous sickle cell patients with an average age of 26 years with a sex ratio of 0.58. The prevalence of metabolic syndrome in our population according to the IDF 2009 was 2%. In our study 28% of patients presented with hyperuricemia. Uricaemia was significantly elevated in patients with components of the metabolic syndrome, in particular in 33% of patients with a large waist circumference, in 25% of hypertensive patients, in 50% of patients with hypertriglyceridemia and in 60% of patients with hypertriglyceridemia and low HDL-cholesterol levels. Significant correlations were found between uricemia and certain components of the metabolic syndrome, in particular the level of triglycerides (r = 0.31, p = 0.002), blood sugar (r = 0.16; p = 0.012), around size (r = 0.071; p ≤ 0.05), HDL-Cholesterol (r = ﹣0.01; p = 0.018), PAS (r = 0.076; p = 0.035) and PAD (r = ﹣0.18; p = 0.0015).
本研究的目的是评估尿酸与纯合子镰状细胞患者代谢综合征及其成分之间的关系。这是一项镰状细胞SS患者的前瞻性病例/对照研究。每名患者与一名同性别、同年龄±2岁的对照组相匹配。在我们的框架中,我们使用了根据国际糖尿病联合会(IDF) 2009年定义代谢综合征的标准。使用ARCHITECT ci4100, Abbot (Chicago, Illinois, USA)进行所有生物学参数的测定。数据采集采用Excel 2016软件,统计分析采用XLSTAT 2019软件。使用学生T检验比较均值和p值小于0.05被认为是显著的。研究人群包括100名平均年龄为26岁、性别比为0.58的纯合子镰状细胞患者。根据IDF 2009,我国人口中代谢综合征的患病率为2%。在我们的研究中,28%的患者表现为高尿酸血症。代谢综合征患者的尿毒症显著升高,特别是33%的大腰围患者、25%的高血压患者、50%的高甘油三酯血症患者和60%的高甘油三酯血症和低hdl -胆固醇水平患者。尿酸血症与代谢综合征的某些组成部分之间存在显著相关性,特别是甘油三酯水平(r = 0.31, p = 0.002)、血糖水平(r = 0.16;P = 0.012),大约大小(r = 0.071;p≤0.05),hdl -胆固醇(r = -0.01;p = 0.018), PAS (r = 0.076;p = 0.035)和PAD (r = -0.18;P = 0.0015)。
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引用次数: 1
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