In the search for new drugs with more efficient active ingredients, various transition metals are being explored as potential metallopharmaceuticals. These compounds, which combine drugs with metals, have shown promis...In the search for new drugs with more efficient active ingredients, various transition metals are being explored as potential metallopharmaceuticals. These compounds, which combine drugs with metals, have shown promise as chemotherapeutic agents, akin to the accidental discovery of cisplatin and its organic derivatives in the late 20th century. This discovery transformed the sciences, particularly in the fields of organic and inorganic chemistry, by offering new insights into the compositions and molecular geometries of inorganic complexes through coordination chemistry, while also intersecting with other scientific domains such as pharmacology and medicine. To contribute to the development of new chemotherapeutic compounds through simple and reproducible synthetic processes, this study utilized rhodium(III) chloride hydrate (RhCl3.nH2O) to synthesize a series of compounds with the following organic N-heterocyclic ligands: 4,4'-dimethyl-2,2'-bipyridine, isonicotinamide, and N-(3-pyridyl)-isonicotinamide (3-pina). Two analytical techniques were employed to characterize the resulting materials: spectroscopic analysis in the infrared region, which suggested interactions and substitutions at the metal center by the organic compounds, and thermoanalytical analyses, which led to the proposal of minimum formulas for the compounds as follows: C1 [RhCl2(4,4'-Met-2,2'-bipy)2]Cl∙5/2H2O and C2 [Rh(4,4'-Met-2,2'-bipy)2(Iso)2] Cl3∙1/2H2O. However, the complexation of the third compound could not be confirmed due to the physicochemical characteristics of the resulting complex being very similar to those of the starting material, thereby validating the effectiveness of these techniques in differentiating and characterizing the synthesized salts. Due to their solubility in water and/or alcohol and thermal stability, the complexes were tested in biological media to assess cell viability in peripheral blood mononuclear cells. The solutions of these salts demonstrated favorable cell viability under the tested conditions, according to statistical analysis, obtaining average viability in the range of 95 ≤ x ≤ 100, with standard deviations between 3.29 ≤ x ≤ 4.44 for living cells.展开更多
考察了6种烷基咪唑氟硼酸盐室温离子液体的溶解性能,并通过量子化学计算阐明该离子液体的溶解性、电导率与其分子结构之间的关系。结果表明:[R_1R_2Im]^+[BF_4]^- 和油品中的脂肪族烃类组分不互溶,但对部分含硫含氮组分均有一定的溶解度...考察了6种烷基咪唑氟硼酸盐室温离子液体的溶解性能,并通过量子化学计算阐明该离子液体的溶解性、电导率与其分子结构之间的关系。结果表明:[R_1R_2Im]^+[BF_4]^- 和油品中的脂肪族烃类组分不互溶,但对部分含硫含氮组分均有一定的溶解度,同时还能溶解具有 Lewis 酸性的盐类,如杂多酸。[R_1R_2Im]^+[BF_4]^-的阴离子相同时,N-烷基咪唑阳离子的体积越小,对应的离子液体的电导率越大,对杂多酸络合物的溶解度越大。展开更多
Background Atrial fibrillation （AF） is accompanied by atrial structural remodeling. Calpain activity is induced during AE To test a causal relationship between calpain activation and atrial structural changes, N-ace...Background Atrial fibrillation （AF） is accompanied by atrial structural remodeling. Calpain activity is induced during AE To test a causal relationship between calpain activation and atrial structural changes, N-acetyI-Leu-Leu-Met （ALLM）, a calpain inhibitor, was utilized in a canine AF model. Methods Fifteen dogs were randomly divided into 3 groups： sham-operated group, control group and calpain inhibitor group; each with 5 dogs. Sustained AF was induced by rapid right atrium pacing at 600 beats per minute for 3 weeks. ALLM was administered at a dosage of 1.0 mg-kg-l-d1 in the calpain inhibitor group. Three weeks later, the proteolysis, protein expression of TnT and myosin, calpain I localization and expression and structural changes were examined in left atrial free walls, right atrial free walls and the interatrial septum respectively. Atrial size and contractile function were also measured by echocardiography. Results Long-term rapid atrial pacing induced marked structural changes such as enlarged atrial volume, myolysis, degradation of TnT and myosin, accumulation of glycogen and changes in mitochondrial shape and size, which were paralleled by an increase in calpain activity. The positive correlation between calpain activity and the degree of myolysis （rs=0.90 961, P〈0.0001） was demonstrated. In addition to structural abnormalities, pacing-induced atrial contractile dysfunction was observed in this study. The pacing-induced atrial structural alterations and loss of contractility were partially prevented by the calpain inhibitor ALLM. Conclusions Activation of calpain represents key features in the progression towards overt structural remodeling. Calpain inhibitor, ALLM, suppressed the increased calpain activity and reversed structural remodeling caused by sustained atrial fibrillation in the present model. Calpain inhibition may therefore provide a possibility for therapeutic intervention in AE展开更多
文摘In the search for new drugs with more efficient active ingredients, various transition metals are being explored as potential metallopharmaceuticals. These compounds, which combine drugs with metals, have shown promise as chemotherapeutic agents, akin to the accidental discovery of cisplatin and its organic derivatives in the late 20th century. This discovery transformed the sciences, particularly in the fields of organic and inorganic chemistry, by offering new insights into the compositions and molecular geometries of inorganic complexes through coordination chemistry, while also intersecting with other scientific domains such as pharmacology and medicine. To contribute to the development of new chemotherapeutic compounds through simple and reproducible synthetic processes, this study utilized rhodium(III) chloride hydrate (RhCl3.nH2O) to synthesize a series of compounds with the following organic N-heterocyclic ligands: 4,4'-dimethyl-2,2'-bipyridine, isonicotinamide, and N-(3-pyridyl)-isonicotinamide (3-pina). Two analytical techniques were employed to characterize the resulting materials: spectroscopic analysis in the infrared region, which suggested interactions and substitutions at the metal center by the organic compounds, and thermoanalytical analyses, which led to the proposal of minimum formulas for the compounds as follows: C1 [RhCl2(4,4'-Met-2,2'-bipy)2]Cl∙5/2H2O and C2 [Rh(4,4'-Met-2,2'-bipy)2(Iso)2] Cl3∙1/2H2O. However, the complexation of the third compound could not be confirmed due to the physicochemical characteristics of the resulting complex being very similar to those of the starting material, thereby validating the effectiveness of these techniques in differentiating and characterizing the synthesized salts. Due to their solubility in water and/or alcohol and thermal stability, the complexes were tested in biological media to assess cell viability in peripheral blood mononuclear cells. The solutions of these salts demonstrated favorable cell viability under the tested conditions, according to statistical analysis, obtaining average viability in the range of 95 ≤ x ≤ 100, with standard deviations between 3.29 ≤ x ≤ 4.44 for living cells.
文摘考察了6种烷基咪唑氟硼酸盐室温离子液体的溶解性能,并通过量子化学计算阐明该离子液体的溶解性、电导率与其分子结构之间的关系。结果表明:[R_1R_2Im]^+[BF_4]^- 和油品中的脂肪族烃类组分不互溶,但对部分含硫含氮组分均有一定的溶解度,同时还能溶解具有 Lewis 酸性的盐类,如杂多酸。[R_1R_2Im]^+[BF_4]^-的阴离子相同时,N-烷基咪唑阳离子的体积越小,对应的离子液体的电导率越大,对杂多酸络合物的溶解度越大。
基金This work was supported by grants from the National Natural Science Foundation of China （No. 30470686）, the Science and Technology Specialized Research Fund for Youth of HeiJong,）iang Province （No. QC06C076）, key Scientific and Technological Project in Heilongjiang Province （No. GB07C32401） and the Innovation Grant of Harbin Medical University for Graduate Student （No. 200401059）.
文摘Background Atrial fibrillation （AF） is accompanied by atrial structural remodeling. Calpain activity is induced during AE To test a causal relationship between calpain activation and atrial structural changes, N-acetyI-Leu-Leu-Met （ALLM）, a calpain inhibitor, was utilized in a canine AF model. Methods Fifteen dogs were randomly divided into 3 groups： sham-operated group, control group and calpain inhibitor group; each with 5 dogs. Sustained AF was induced by rapid right atrium pacing at 600 beats per minute for 3 weeks. ALLM was administered at a dosage of 1.0 mg-kg-l-d1 in the calpain inhibitor group. Three weeks later, the proteolysis, protein expression of TnT and myosin, calpain I localization and expression and structural changes were examined in left atrial free walls, right atrial free walls and the interatrial septum respectively. Atrial size and contractile function were also measured by echocardiography. Results Long-term rapid atrial pacing induced marked structural changes such as enlarged atrial volume, myolysis, degradation of TnT and myosin, accumulation of glycogen and changes in mitochondrial shape and size, which were paralleled by an increase in calpain activity. The positive correlation between calpain activity and the degree of myolysis （rs=0.90 961, P〈0.0001） was demonstrated. In addition to structural abnormalities, pacing-induced atrial contractile dysfunction was observed in this study. The pacing-induced atrial structural alterations and loss of contractility were partially prevented by the calpain inhibitor ALLM. Conclusions Activation of calpain represents key features in the progression towards overt structural remodeling. Calpain inhibitor, ALLM, suppressed the increased calpain activity and reversed structural remodeling caused by sustained atrial fibrillation in the present model. Calpain inhibition may therefore provide a possibility for therapeutic intervention in AE
