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A New Ceramide (Rumexamide) and Other Chemical Constituents from Rumex abyssinicus Jacq (Polygonaceae): Isolation, Characterization, Antibacterial Activities and Chemophenetic Significance 一种新的神经酰胺(Rumexamide)及其化学成分:从蓼科(Rumex abyssinicus Jacq)中分离、鉴定、抑菌活性及化学意义
Pub Date : 2021-01-01 DOI: 10.4236/abc.2021.115018
Léonel Donald Feugap Tsamo, Lorette Victorine Yimgang, S. C. N. Wouamba, P. Mkounga, A. Nkengfack, L. Voutquenne-Nazabadioko, D. Ngnokam, B. Lenta, N. Sewald
The chemical study of Rumex abyssinicus Jacp (Polygonaceae) led to the isolation of a new ceramide named (R)-2'-hydroxy-N-[(2S,3S,4R,16E)-1,3,4-trihy-droxyhexacos-16-en-2-yl]hexadecanamide (rumexamide) (1) together with sixteen known compounds: bis-(2-ethylhexyl) phthalate ( 2), chrysophanol (3), physcion bacterial activities of extracts (MeOH, n-BuOH and EtOAc), as well as compounds 9, 11, 12, 15 + 16 and 17 against pathogenic bacteria (Staphylococcus aureus ATCC 43300, Shigella flexneri NR 518, Klebsiella pneumoniae ATCC 700603, Escherichia coli ATCC 25922), were performed using the broth microdilution method and the results show that, extracts were not active (MIC > 1000 µg/mL) while compounds were weakly or not active (MIC ≥ 500 µg/mL) against all bacteria strains. Furthermore, the chemophenetic relationships of the isolated compounds and their significances were discussed.
通过对蓼科植物Rumex abyssinicus Jacp的化学研究,分离出一种新的神经酰胺,命名为(R)-2′-羟基- n- [(2S,3S,4R,16E)-1,3,4-三羟基-16-en-2-基]十六烷酰胺(rumexamide)(1)和16个已知化合物:采用微量肉汤稀释法测定了双-(2-乙基己基)邻苯二甲酸酯(2)、大黄酚(3)、提取物(MeOH、n-BuOH和EtOAc)以及化合物9、11、12、15 + 16和17对病原菌(金黄色葡萄球菌ATCC 43300、福氏志贺氏菌NR 518、肺炎克雷伯菌ATCC 700603、大肠杆菌ATCC 25922)的抑菌活性,结果表明:提取物对所有菌株均无活性(MIC≥1000µg/mL),而化合物对所有菌株均弱或无活性(MIC≥500µg/mL)。此外,还讨论了分离化合物的化学亲缘关系及其意义。
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引用次数: 8
Synthesis and In Vitro Anti-Helicobacter and Anti-Staphylococcal Activities of Novel Diaryldisulfides and Diarylthiosulfonates 新型二芳基二硫化物和二芳基硫代磺酸盐的合成及其体外抗幽门螺杆菌和葡萄球菌活性研究
Pub Date : 2021-01-01 DOI: 10.4236/abc.2021.115017
M. Khan, K. Miller, K. Rawson, Yong Zhou
Arylthiols were reacted with acrylonitrile under basic conditions to form the corresponding aryl sulfides which were oxidised with sodium metaperiodate in aqueous methanol to yield 3-arylsulphinylpropanenitriles that upon thermolysis in refluxing toluene produced a mixture of diarylthiosulfonates and diaryldisulfides. The mixture of the two products was easily separated by flash chromatography and characterized spectroscopically. The diarylthiosulfonates and diaryldisulfides, garlic-like organosulfur compounds, were tested for their antimicrobial properties against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Helicobacter pylori and had been found to have good activity against S. aureas and H. pylori with no activity against the other two organisms.
芳基硫醇在碱性条件下与丙烯腈反应生成相应的芳基硫化物,与偏碘酸钠在甲醇水溶液中氧化生成3-芳基磺胺基丙烷腈,在回流甲苯中热裂解生成二芳基硫磺酸盐和二芳基二硫化物的混合物。两种产物的混合物易于用闪蒸色谱分离和光谱表征。二芳基硫代磺酸盐和二芳基二硫化物是大蒜类有机硫化合物,对大肠杆菌、铜绿假单胞菌、金黄色葡萄球菌和幽门螺杆菌的抗菌性能进行了测试,发现对金黄色葡萄球菌和幽门螺杆菌有良好的活性,对其他两种生物没有活性。
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引用次数: 0
Synthesis Characterization and Biological Activities of an Enamine Derivative and Its Coordination Compounds 一种烯胺衍生物及其配位化合物的合成、表征及生物活性
Pub Date : 2020-12-07 DOI: 10.4236/abc.2020.106013
T. Aiyelabola, J. Jordaan, D. Otto, E. Akinkunmi
The medicinal uses and applications of metal complexes are of increasing clinical and commercial importance; this is as a result of some level of success achieved so far. In this regard, novel enamine free-base ligands were synthesized by the condensation of terephthalaldehyde and 2-(methylamino)ethanol. This afforded a dinegative ONNO donor enamine, free base, characterized using 1H and 13C NMR, Fourier-transformed infrared and UV-vis spectroscopy. Coordination compounds of the enamine were also synthesized using Cu(II), Ni(II), Co(II) and VO(IV) ions. These complexes were characterized by electronic, IR spectrophotometry, mass spectrometry, magnetic susceptibility and EDX. The compounds were thereafter evaluated for their antimicrobial and cytotoxic activities. The data obtained were supportive of an octahedral geometry for the Cu(II) complex, a square-pyramidal geometry for the vanadium complex and a 4-coordinate square-planar geometry for both the cobalt and nickel complexes. The magnetic susceptibility data revealed that the complexes are magnetically dilute and mononuclear with exception of the cobalt complex. The ligands and the complexes did not exhibit significant antimicrobial and cytotoxic assays, indicative of the nontoxicity of the ligand and complexes.
金属配合物的药用和应用具有越来越重要的临床和商业意义;这是迄今为止取得一定程度成功的结果。在这方面,通过对苯甲醛和2-(甲氨基)乙醇的缩合反应合成了新的烯胺游离碱配体。这提供了一种双负ONNO供体烯胺,游离碱,使用1H和13C NMR、傅立叶变换红外和UV-vis光谱进行表征。用Cu(II),Ni(II)、Co(II)和VO(IV)离子合成了烯胺的配位化合物。用电子、红外光谱、质谱、磁化率和EDX对这些配合物进行了表征。随后对这些化合物的抗微生物和细胞毒性活性进行评价。所获得的数据支持Cu(II)配合物的八面体几何结构、钒配合物的方形棱锥几何结构以及钴和镍配合物的4-配位方形平面几何结构。磁化率数据表明,除钴配合物外,这些配合物都是磁稀释的单核配合物。配体和配合物没有表现出显著的抗微生物和细胞毒性测定,这表明配体和复合物的无毒性。
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引用次数: 1
Efficient Production of L-Theanine Using Immobilized Recombinant Escherichia coli Cells Expressing a Modified γ-Glutamyltranspeptidase Gene from Pseudomonas nitroreducens 表达修饰的γ-谷氨酰转肽酶基因的固定化重组大肠杆菌细胞高效生产l -茶氨酸
Pub Date : 2020-12-07 DOI: 10.4236/abc.2020.106012
Putthapong Phumsombat, C. Sano, H. Ikezoe, J. Hayashi, T. Itoh, T. Hibi, M. Wakayama
L-Theanine (γ-glutamylethylamide) is a naturally occurring amino acid derivative known to have several beneficial physiological effects as a diet supplement, and to give an umami taste when used as a food additive. The compound is industrially produced by γ-glutamyltranspeptidase from Pseudomonas nitroreducens (PnGGT). Using recombinant PnGGT, we have shown previously that Trp385, Phe417, and Trp525 are key amino acid residues for recognition of acceptor substrates at the PnGGT active site. Here, we demonstrate that a recombinant W525D mutant of PnGGT produces L-theanine from ethylamine and L-glutamine more efficiently than wild-type PnGGT, attributable to an increased ratio of transfer activity to hydrolysis activity. An efficient production of L-theanine was achieved by immobilizing Escherichia coli cells expressing the W525D PnGGT mutant (E. coli-W525D) using 2% alginate as the supporting material. The highest L-theanine production using immobilized E. coli-W525D, representing a conversion rate of 90%, was achieved in optimal reaction conditions of pH 10, 40°C, and a substrate molar ratio of L-glutamine to ethylamine of 1:10. The immobilized E. coli-W525D retains 85% and 78% relative activity after storage for a month at 4°C and room temperature, respectively. Immobilized E. coli-W525D thus has strong potential for use in the future commercial production of L-theanine on a large scale.
l -茶氨酸(γ-谷氨乙胺)是一种天然存在的氨基酸衍生物,已知作为膳食补充剂具有几种有益的生理作用,并且作为食品添加剂使用时具有鲜味。该化合物是由硝基假单胞菌的γ-谷氨酰转肽酶(PnGGT)工业生产的。利用重组PnGGT,我们已经证明Trp385、Phe417和Trp525是PnGGT活性位点识别受体底物的关键氨基酸残基。在这里,我们证明了重组PnGGT的W525D突变体比野生型PnGGT更有效地从乙胺和l -谷氨酰胺中产生l -茶氨酸,这是由于转移活性与水解活性的比例增加。用2%海藻酸盐作为载体,固定化表达W525D PnGGT突变体(大肠杆菌-W525D)的大肠杆菌细胞,实现了l -茶氨酸的高效生产。固定化大肠杆菌- w525d在pH为10、40℃、l -谷氨酰胺与乙胺的摩尔比为1:10的最佳反应条件下,l -茶氨酸的产量最高,转化率为90%。固定化大肠杆菌- w525d在4℃和室温下保存1个月后,相对活性分别保持85%和78%。因此,固定化大肠杆菌- w525d在未来l -茶氨酸的大规模商业化生产中具有很强的应用潜力。
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引用次数: 2
Synthesis, Characterization and Antibacterial Activities of Polydentate Schiff Bases, Based on Salicylaldehyde 水杨醛类多齿席夫碱的合成、表征及抗菌活性研究
Pub Date : 2020-10-20 DOI: 10.4236/abc.2020.105010
Yosef Bayeh, Fekiya Mohammed, Mamo Gebrezgiabher, Fikre Elemo, Mesfin Getachew, Madhu Thomas
Three Schiff bases L1, L2 and L3 were synthesized by condensing salicylaldehyde with 4-aminoantipyrine, ethylendiamine and 2-aminophenol respectively and subsequently characterized by various physicochemical investigations. All the three compounds were screened for their In-vitro antibacterial activity against two gram positive bacteria, Staphylococcus aureus (S.A), Staphylococcus epidermidis (S.E) and two gram negative bacteria Klebsiella pneumoniae (K.P) and Pseudomonas aeruginosa (P.A) by agar diffusion method. On comparing the results obtained with the activity of commercially available antibiotics such as Ciprofloxacin and Chloramphenicol, the newly synthesized compounds showed comparable antibacterial activities. The solvent methanol exhibit activity against all bacterial species with IZs ranging from 8 ± 0.25 to 17 ± 0.29 mm while the standard antibiotics Ciprofloxacin and Chloramphenicol exhibited an activities with IZs varying from 21.3 ± 0.31 to 28.3 ± 0.32 and 26.3 ± 0.24 mm to 32.3 ± 0.23 mm, respectively. However, the newly synthesized Schiff bases L1, L2 and L3 showed IZs ranging from 7.4 ± 0.23 to 32.5 ± 0.14, 3 ± 0.57 to 12 ± 0.28 and 10 ± 0.20 to 32 ± 0.36 respectively. Among the Schiff bases, L3 showed the activity (32 ± 0.36) against S.E and P.A which is higher than the activity of standard antibiotics Ciprofloxacin and Chloramphenicol against the same bacterial strains. The results obtained revealed that all the synthesized Schiff bases exhibit appreciable antibacterial activity against all the bacteria species which potentially makes them, to apply as wide range antibacterial drugs, after further in-vivo cytotoxicity investigations. Their activity can also be further modified by changing the functionality of precursors for Schiff base condensation.
通过水杨醛与4-氨基安替比林、乙二胺和2-氨基苯酚的缩合反应,合成了三种席夫碱L1、L2和L3,并通过各种物理化学研究对其进行了表征。用琼脂扩散法筛选三种化合物对金黄色葡萄球菌(S.A)、表皮葡萄球菌(S.E)、肺炎克雷伯菌(K.P)和绿脓杆菌(P.A)两种革兰氏阴性菌的抗菌活性。将获得的结果与市售抗生素如环丙沙星和氯霉素的活性进行比较,新合成的化合物显示出相当的抗菌活性。溶剂甲醇对所有细菌的活性范围为8±0.25至17±0.29mm,而标准抗生素环丙沙星和氯霉素的活性范围分别为21.3±0.31至28.3±0.32和26.3±0.24mm至32.3±0.23mm。然而,新合成的席夫碱L1、L2和L3的IZ分别为7.4±0.23至32.5±0.14、3±0.57至12±0.28和10±0.20至32±0.36。在希夫碱中,L3对S.E和P.A的活性为(32±0.36),高于标准抗生素环丙沙星和氯霉素对相同菌株的活性。结果表明,经过进一步的体内细胞毒性研究,所有合成的希夫碱对所有可能产生希夫碱的细菌都表现出明显的抗菌活性,可作为广泛的抗菌药物应用。它们的活性还可以通过改变席夫碱缩合前体的官能度来进一步修饰。
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引用次数: 4
Potential Prebiotic Relevance of Glycine Single Crystals Enclosing Fluid Inclusions: An Experimental and Computer Simulation with Static Magnetic Fields 甘氨酸单晶包裹流体包裹体的潜在益生相关性:静态磁场的实验和计算机模拟
Pub Date : 2020-10-20 DOI: 10.4236/abc.2020.105011
E. Angeles-Camacho, J. Cruz-Castañeda, A. Meléndez, M. Colín-García, K. C. L. Cruz, S. Ramos-Bernal, A. Negrón-Mendoza, G. Garza-Ramos, P. Rodríguez-Zamora, C. Camargo-Raya, A. Heredia
Glycine crystallizes into three different polymorphs called α, β and γ under standard physicochemical conditions. They have different features depending on their structural variations. The possible interaction of glycine with magnetic minerals in meteorites and comets or in the ancient Earth, paves the way to study the self-assembly and molecular behavior under irradiation and magnetic conditions. The magnetic field might induce the formation of a specific polymorph of glycine. To gain insight on the consequences of gamma irradiation with a gradient of static magnetic fields (0.06 T, 0.3 T, 0.42 T and 0.6 T) on the self-assembly of single macroscopic glycine crystals, we gamma irradiated the powdered amino acid and then assembled single crystals from water solutions. The preliminary results showed a stable formation of fluid inclusions in the single crystals and no straightforward effect on the self-assem- bly process after glycine gamma irradiation and interaction with static magnetic fields. The α glycine polymorph single crystals formed at 55° from the magnetic longitudinal axis and seemed to be enhanced by gamma radiation. The γ-glycine single crystals presented L and D circular dichroism signals, whereas the irradiated samples presented no circular dichroism bands. Com- puter simulations suggest different catalytic properties from α and γ glycine crystals.
在标准物理化学条件下,甘氨酸结晶成三种不同的多晶型,称为α、β和γ。根据结构变化,它们有不同的特征。甘氨酸可能与陨石、彗星或古代地球上的磁性矿物相互作用,为研究辐照和磁性条件下的自组装和分子行为铺平了道路。磁场可能诱导甘氨酸的特定多晶型的形成。为了深入了解静态磁场梯度(0.06T、0.3T、0.42T和0.6T)的伽马辐射对单个宏观甘氨酸晶体自组装的影响,我们对粉状氨基酸进行伽马辐射,然后从水溶液中组装单晶。初步结果表明,在甘氨酸γ辐照和与静磁场相互作用后,单晶中稳定形成流体包裹体,对自组装过程没有直接影响。α-甘氨酸多晶型单晶在距离磁纵轴55°处形成,似乎受到伽马辐射的增强。γ-甘氨酸单晶呈现L和D圆二色性信号,而辐照样品不呈现圆二色带。计算机模拟表明α和γ甘氨酸晶体具有不同的催化性能。
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引用次数: 3
Spatial Distribution of Dissolved Inorganic Nutrients and Phytoplankton around Kota Kinabalu Wetland, Sabah, Malaysia 马来西亚沙巴州哥打京那巴鲁湿地溶解无机营养物和浮游植物的空间分布
Pub Date : 2020-08-27 DOI: 10.4236/abc.2020.104009
Sujjat Al Azad, Viearl Jivel Jinau
Kota Kinabalu Wetland is importantly habited of mangrove, diverse aquatic flora and fauna as well as feeding stop for migratory birds. This wetland is inundated with the tidal flow, as connected with a small river and nearby coastal areas, thus. A study was carried out to determine the spatial distribution of dissolved inorganic nutrients and phytoplankton diversity at Kota Kinabalu (KK) Wetlands. Five stations, in which river mouth of Likas Bay, river channel (two stations) and inundated area (two stations) in KK Wetland were selected for this study. In-situ parameters of water, water for nutrients and phytoplankton samples were collected from May 2019 until October 2019. The highest concentration of nitrate (0.115 mg/L) was recorded at inundated area of wetland (S5) while the lowest nitrate concentration (0.0047 mg/L) was found at river (S3) flowing towards wetland. The concentrations of ammonia (0.2004 to 2.311 mg/L) were recorded relatively higher at every station compared to other dissolved inorganic nutrients (DIN). The concentration of phosphate was determined in the ranges of 0.0089 - 0.0513 mg/L. Nitrate, ammonia and phosphate showed no significant difference (P = 0.737) in terms of DIN concentration at all five sampling stations during the study period. Twenty-four genera of phytoplankton were identified, dominated by diatoms (55.29%), followed by dinoflagellates (24.95%), Chrysophyta (11.15%), Spirotrichea (5.28%) and Cyanophyta (3.33%). Dominating species throughout the study period include Chaetoceros sp., Pseduo-nitzschia sp., and Cylindrotheca closterium, Peridinium quinquecorne and Alexandrium sp. Phytoplankton species compositions were observed the highest in river mouth area in July with the highest density of 12.115 × 104 cells/mL. The study showed that nutrient concentration was insignificant (P = 0.614) in altering the phytoplankton density, as influences with the tidal water.
哥打基纳巴鲁湿地是红树林、各种水生动植物以及候鸟觅食地的重要栖息地。这片湿地被潮水淹没,与一条小河和附近的沿海地区相连。进行了一项研究,以确定亚庇(KK)湿地溶解无机营养物质的空间分布和浮游植物多样性。本研究选取了Likas湾河口、KK湿地河道(两个站点)和淹没区(两个站)五个站点进行研究。从2019年5月到2019年10月,采集了水、营养水和浮游植物样本的现场参数。湿地淹没区的硝酸盐浓度最高(0.115 mg/L)(S5),而流向湿地的河流(S3)的硝酸盐含量最低(0.0047 mg/L)。与其他溶解无机营养素(DIN)相比,每个站的氨浓度(0.2004至2.311 mg/L)相对较高。磷酸盐的浓度测定范围为0.0089-0.0513mg/L。在研究期间,所有五个采样站的硝酸盐、氨和磷酸盐的DIN浓度均无显著差异(P=0.737)。浮游植物共鉴定出24属,以硅藻(55.29%)为主,其次是甲藻(24.95%)、金藻(11.15%)、螺旋藻(5.28%)和蓝藻(3.33%)。7月河口区浮游植物种类组成最高,密度最高,为12.115×104个细胞/mL。研究表明,营养物浓度对浮游植物密度的影响不显著(P=0.614),受潮汐水的影响。
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引用次数: 2
Syntheses of Coordination Compounds of 2-Amino-3-Methylbutanoic Acid Their Mixed Ligand Complexes and Antibacterial Activities 2-氨基-3-甲基丁酸配位化合物的合成及其混合配体配合物的抗菌活性研究
Pub Date : 2020-06-03 DOI: 10.4236/abc.2020.103006
T. Aiyelabola, I. E. Okunade, J. Jordaan, D. Otto
Coordination compounds of 2-amino-3-methylbutanoic acid were synthesized with chromium(III) and oxovanadium(IV) ions. M:L; 1:2. Adducts of these complexes using 1,10-phenantroline and ethylenediamine were further synthesized, M:L, (1:2). These compounds were characterized using electronic, infra-red spectrophotometry, magnetic susceptibility measurement and percentage metal analyses. The zones of inhibition and minimum inhibitory concentrations of the compounds against eight microbes were studied. The results obtained indicated an octahedral geometry for the Cr(III) complexes, indicative of additional coordination of two water molecules. On the other hand a square pyramid geometry was obtained for the binary oxovanadium complex and its 1,10-phenantroline adduct. However, for the oxovanadium ethylenediamine adduct a distorted octahedral geometry was proposed. The result for the antibacterial studies indicated that both mixed ligand complexes of 1,10-phenantroline exhibited good antibacterial activity, and in some cases better activity than the standard, streptomycin.
以铬(III)和氧钒(IV)离子为原料合成了2-氨基-3-甲基丁酸配合物。M: L;以1,10-苯并喹啉和乙二胺为原料,进一步合成了这些配合物的加成物,M:L,(1:2)。使用电子、红外分光光度法、磁化率测量和金属百分比分析对这些化合物进行了表征。研究了化合物对8种微生物的抑制区和最低抑制浓度。所获得的结果表明Cr(III)配合物具有八面体几何形状,表明两个水分子的额外配位。另一方面,得到了二元氧钒络合物及其1,10-苯并罗啉加合物的方棱锥几何结构。然而,对于氧钒乙二胺加合物,提出了扭曲的八面体几何结构。抗菌研究结果表明,1,10-苯安曲啉的两种混合配体复合物都表现出良好的抗菌活性,在某些情况下比标准链霉素的活性更好。
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引用次数: 1
Synthesis, Characterization, and Evaluation of Antitumor Potential in MCF-7 Cells of Ruthenium-Derived Compounds 钌衍生化合物的合成、表征及其在MCF-7细胞中抗肿瘤潜力的评估
Pub Date : 2020-06-03 DOI: 10.4236/abc.2020.103007
Moraes Fabricio Tarso, Galvão Anderson Dourado, F. D. Batista, Amorin Kelly Aparecida da Encarnação, Sousa Claudia Cristina, H. Cristina, França Eduardo Luzia, Costa Daniel Tizo, S. Batista
To synthesize, characterize and evaluate the antitumor potential derived from ruthenium compounds was generated in this study, from the precursor K[RuCl4(bipy)] a route in a simple and reproducible synthesis for a novel compound of coordinating Ru+3 with bipy and L-trip. The spectroscopic characterization in the middle infrared region (FTIR) shows the interactions between Ru-(L-trip), evidenced by the displacement of the carboxylate ion band for higher energies, and also by the displacements of aliphatic amine bands, suggesting that bidentate coordination of the L-trip ligand occurred. Analysis of the results obtained with thermoanalytical techniques showed that the minimum formula of the compound, [RuCl2(bipy)(L-trip)]1/2H2O. Evaluation of the antitumor potential of precursor K[RuCl4(bipy)] showed the toxic effects on MCF-7 cell line, but did not show selectivity and not reached PBMC cells to the same extent. The evaluation of the antitumor potential of the newly synthesized compound, [RuCl2(bipy)(L-trip)], demonstrated that the insertion of an L-tryptophan molecule into the precursor coordination sphere made it selective when compared to PBMC cells, for MCF-7 type tumor cells.
为了合成、表征和评估钌化合物的抗肿瘤潜力,本研究从前体K[RuCl4(bipy)]中产生了一种简单且可重复的合成Ru+3与bipy和L-trip配位的新化合物的途径。中红外区(FTIR)的光谱表征显示了Ru-(L-trip)之间的相互作用,通过羧酸根离子带对更高能量的位移以及脂肪胺带的位移证明了这一点,表明L-trip配体发生了双齿配位。用热分析技术获得的结果的分析表明,化合物的最小化学式[RuCl2(bipy)(L-trip)]1/2H2O。对前体K[RuCl4(bipy)]的抗肿瘤潜力的评估显示出对MCF-7细胞系的毒性作用,但没有显示出选择性,并且没有达到相同程度的PBMC细胞。对新合成的化合物[RuCl2(bipy)(L-trip)]的抗肿瘤潜力的评估表明,与PBMC细胞相比,将L-色氨酸分子插入前体配位球使其对MCF-7型肿瘤细胞具有选择性。
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引用次数: 0
Comparison of the Biological Activity and Constituents in Japanese Ambers 日本琥珀的生物活性及成分比较
Pub Date : 2020-06-03 DOI: 10.4236/abc.2020.103008
Eisaku Shimizu, Nozomu Shimoda, Tetsuaki Kawamura, N. Ueda, K. Kimura
Background/Aim: Kuji amber is an interesting natural source for drug discovery because a new anti-allergic compound, named kujigamberol and several new compounds have been isolatated from it. It was important to evaluate the yield, biological activities and constituents of each methanol extract of Kuji, Iwaki, Choshi, Mizunami and Ube ambers in Japan in order to establish if additional new compounds could be identified in these ambers. Materials and Method: Biological activities of each extract were evaluated using growth-restoring activity of the mutant yeast strain involving Ca2+-signal transduction and inhibition activity of degranulation in rat basophilic leukemia (RBL)-2H3 cells. Constituents of each extract were analyzed by high performance liquid chromatography (HPLC). Results: All ambers except Ube amber have growth-restoring activity against the mutant yeast. Both Kuji and Iwaki ambers inhibited the degranulation of RBL-2H3 cells induced by the calcium ionophore A23187 in a dose dependent manner. The main biologically active compound in Kuji amber, kujigamberol, was also isolated from Iwaki amber and analyzed by mass spectrometry (MS) and nuclear magnetic resonance (NMR). Conclusion: Kuji and Iwaki ambers appeared to have the same origin. Choshi, Mizunami, and Ube ambers are valuable sources for biologically active compounds which are different from those of Kuji amber.
背景/目的:苦吉琥珀是一种有趣的天然药物发现来源,因为从中分离出了一种新的抗过敏化合物,名为苦吉琥珀醇和几个新的化合物,日本的Mizunami和Ube琥珀,以确定是否可以在这些琥珀中鉴定出额外的新化合物。材料和方法:利用突变酵母菌株的生长恢复活性(涉及Ca2+-信号转导)和对大鼠嗜碱性白血病(RBL)-2H3细胞脱颗粒的抑制活性来评估每种提取物的生物活性。通过高效液相色谱法(HPLC)分析每种提取物的成分。结果:除乌贝琥珀外,所有琥珀对突变酵母均具有生长恢复活性。Kuji和Iwaki ambers均以剂量依赖的方式抑制由钙离子载体A23187诱导的RBL-2H3细胞的脱颗粒。Kuji琥珀中的主要生物活性化合物kujigamberol也是从岩城琥珀中分离出来的,并通过质谱(MS)和核磁共振(NMR)进行了分析。结论:Kuji和Iwaki琥珀似乎有相同的起源。Choshi琥珀、Mizunami琥珀和Ube琥珀是不同于Kuji琥珀的生物活性化合物的宝贵来源。
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引用次数: 1
期刊
生物化学进展(英文)
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