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首页> 外文期刊>International Journal of Environmental Research and Public Health >Synthesis and Structure-Activity Correlation Studies of Metal Complexes of α-N-heterocyclic Carboxaldehyde Thiosemicarbazones in Shewanella oneidensis
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Synthesis and Structure-Activity Correlation Studies of Metal Complexes of α-N-heterocyclic Carboxaldehyde Thiosemicarbazones in Shewanella oneidensis

机译：沙瓦氏假单胞菌中α-N-杂环甲醛甲醛硫半脲酮金属配合物的合成及结构活性相关性研究

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This investigation involved the synthesis of metal complexes to test the hypothesis that structural changes and metal coordination in pyridine thiosemicarbazones affect cell growth and cell proliferation in vitro. Thiosemicarbazones are well known to possess antitumor, antiviral, antibacterial, antimalarial, and other activities. Extensive research has been carried out on aliphatic, aromatic, heterocyclic and other types of thiosemicarbazones and their metal complexes. Due to the pronounced reactivity exhibited by metal complexes of heterocyclic thiosemicarbazones, synthesis and structural characterization of di-2-pyridylketone 4N-phenyl thiosemicarbazone and diphenyl tin (Sn) and platinum (Pt) complexes were undertaken. Shewanella oneidensis MR-1, a metal ion-reducing bacterium, was used as a model organism to explore the biological activity under aerobic conditions. A comparision of the cytotoxic potential of selected ligand and metal-complex thiosemicarbazones on cell growth in wild type MR-1 and mutant DSP-010 Shewanella oneidensis strains at various concentrations (0, 5, 10, 15, 20 or 25 ppm) was performed. The wild type (MR-1) grown in the presence of increasing concentrations of Sn- thiosemicarbazone complexes was comparatively more sensitive (mean cell number = 4.8 X 108 + 4.3 X 107 SD) than the DSP-010, a spontaneous rifampicillin derivative of the parent strain (mean cell number = 5.6 x 108 + 6.4 X 107 SD) under comparable aerobic conditions (p=0.0004). No differences were observed in the sensitivity of the wild and mutant types when exposed to various concentrations of diphenyl Pt- thiosemicarbazone complex (p= 0.425) or the thiosemicarbazone ligand (p=0.313). Growth of MR-1 in the presence of diphenyl Sn- thiosemicarbazone was significantly different among treatment groups (p=0.012). MR-1 cell numbers were significantly higher at 5ppm than at 10 to 20ppm (p = 0.05). The mean number of DSP-010 variant strain cells also differed among diphenyl Sn- thiosemicarbazone complex treated groups (p=0.051). In general, there was an increasing trend in the number of cells from about 5.0 X 108 cells (methanol control group) to about 6.0 X 108 cells (25ppm). The number of cells in methanol control group was significantly lower than cell numbers at 20ppm and 25ppm (p = 0.05), and numbers at 5ppm treatment were lower than at 20 and 25ppm (p = 0.05). Furthermore, a marginally significant difference in the number of MR-1 cells was observed among diphenyl Pt- thiosemicarbazone complex treatment groups (p = 0.077), and an increasing trend in the number of cells was noted from ~5.0 X 108 cells (methanol control group) to ~5.8 X 108 cells (20ppm). In contrast, the DSP-010 variant strain showed no significant differences in cell numbers when treated with various concentrations of diphenyl Pt- thiosemicarbazone complex (p = 0.251). Differences in response to Sn- metal complex between MR-1 and DSP-010 growing cultures indicate that biological activity to thiosemicarbazone metal complexes may be strain specific.
机译：这项研究涉及金属配合物的合成，以检验以下假设：吡啶硫半脲在吡啶中的结构变化和金属配位会影响细胞生长和细胞增殖。众所周知，硫代氨基脲具有抗肿瘤，抗病毒，抗菌，抗疟及其他活性。已经对脂族，芳族，杂环和其他类型的硫代半氨基甲酮及其金属配合物进行了广泛的研究。由于杂环硫代半氨基甲酮的金属配合物表现出显着的反应性，因此进行了二-2-吡啶基酮4N-苯基硫代半脲与二苯基锡（Sn）和铂（Pt）配合物的合成和结构表征。拟南芥Shewanella oneidensis MR-1是一种金属离子还原细菌，被用作模型生物，以研究有氧条件下的生物活性。在不同浓度（0、5、10、15、20或25 ppm）下，比较了所选配体和金属配合物的硫代半氨基甲酰胺对野生型MR-1和突变型DSP-010希瓦氏菌的生长的细胞毒性潜力。 。在浓度不断增加的Sn- thiosemicarbazone复合物存在下生长的野生型（MR-1）相对于DSP-010（DSP的自发利福霉素衍生物）更敏感（平均细胞数= 4.8 X 108 + 4.3 X 107 SD）。亲本菌株（平均细胞数= 5.6 x 108 + 6.4 X 107 SD）在有氧条件下（p = 0.0004）。当暴露于各种浓度的二苯基对-硫代氨基脲复合物（p = 0.425）或硫代氨基脲配体（p = 0.313）时，野生型和突变型的敏感性均未见差异。在治疗组之间，在存在二苯基锡-硫半碳zone的情况下MR-1的生长显着不同（p = 0.012）。 MR-1细胞数在5ppm时显着高于10至20ppm（p = 0.05）。 DSP-010变异株细胞的平均数目在二苯基锡-硫代半碳酸盐复合物治疗组之间也有所不同（p = 0.051）。通常，细胞数量从约5.0 X 108细胞（甲醇对照组）增加到约6.0 X 108细胞（25ppm）有增加的趋势。甲醇对照组的细胞数量明显低于20ppm和25ppm时的细胞数量（p = 0.05），处理5ppm时的细胞数量低于20ppm和25ppm时的细胞数量（p = 0.05）。此外，在二苯基对-硫代半碳酰胺复合物治疗组之间观察到MR-1细胞数量略有显着差异（p = 0.077），并且从〜5.0 X 108细胞中观察到细胞数量呈增加趋势（甲醇对照组）〜5.8 X 108个细胞（20ppm）。相反，当用各种浓度的二苯基对-硫代半碳酰胺复合物处理时，DSP-010变异株在细胞数量上没有显着差异（p = 0.251）。 MR-1和DSP-010生长培养物对Sn-金属配合物的响应差异表明，对thiosemicarbazone金属配合物的生物活性可能是菌株特异性的。

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