The title compound 1-（3-amino-[1,2,4]triazol-1-yl）-3,3-dimethyl-butan-2-one（3） was synthesized by Hofmann-alkylation reaction of 1-chloro-3,3-dimethyl-butan-2-one（1） and ~1H-[1,2,4]triazol-3-ylamine（2） with eq...The title compound 1-（3-amino-[1,2,4]triazol-1-yl）-3,3-dimethyl-butan-2-one（3） was synthesized by Hofmann-alkylation reaction of 1-chloro-3,3-dimethyl-butan-2-one（1） and ~1H-[1,2,4]triazol-3-ylamine（2） with equal amount of K_2CO_3 as acid acceptor. The structure of compound 3 was characterized by ~1H NMR, 13 C NMR, HRMS and single-crystal X-ray diffraction. The compound crystallizes in the monoclinic system, space group P21/n with a = 5.7227（8）, b = 27.924（4）, c = 6.2282（7） ？, β = 101.892（11）°, V = 973.9（2） ？~3, Z = 4, T = 180.00（10） K, μ（MoKα） = 0.087 mm^（-1）, Dc = 1.243 g/cm^3, 3832 reflections measured（3.648≤θ≤26.022°）, 1916 unique reflections（Rint = 0.0359, Rsigma = 0.0572） used in all calculations. The final R = 0.0557（I 〉 2σ（I）） and w R = 0.1276（all data）. Bioassay showed that 3 displayed excellent activity as plant growth regulator with inducing lateral root formation and enhancing primary root elongation at 0.27 mmol/L（50 ppm） in soybeen（He Feng-50）. Good water solubility was found with 50 mg in 1 m L of water. Therefore, application of 3 in agriculture is more environmentally friendly due to cosolvent-free condition, and results in improved abiotic-stress tolerance by affecting the root growth. And furthermore, it can be used as a precursor to investigate the function of regulating plant root growth.展开更多
旨在证明miR-324-3p可以通过调控其预测的靶基因MC1R及其下游基因的表达从而对羊驼皮肤黑色素的合成产生影响。本研究在体外培养的羊驼皮肤黑色素细胞中转染miR-324-3p过表达载体,应用qRT-PCR与Western blotting分析比较各试验组中MC1R...旨在证明miR-324-3p可以通过调控其预测的靶基因MC1R及其下游基因的表达从而对羊驼皮肤黑色素的合成产生影响。本研究在体外培养的羊驼皮肤黑色素细胞中转染miR-324-3p过表达载体,应用qRT-PCR与Western blotting分析比较各试验组中MC1R基因与毛色相关基因小眼畸形相关转录因子(Microphthalmia-associtated transcription factor,Mitf)、酪氨酸酶(Tyrosinase,Tyr)、酪氨酸相关蛋白2(Tyrosinase related protein 2,Tyrp2)的表达差异性,利用酶标仪检测黑色素产量的变化。结果显示:(1)miR-324-3p在棕色与白色羊驼皮肤中均有表达,且在棕色羊驼皮肤中极显著表达(P<0.01),其相对表达量是白色的1.64倍;(2)黑色素细胞被转染了miR-324-3p过表达载体后,处理组靶基因MC1R及其下游调控基因Mitf、Tyr和Tyrp2的表达量与黑色素产量较空白对照组均有下调,且以Mitf基因表达量极显著下调(P<0.01)。综上表明,羊驼皮肤中miR-324-3p可能通过调控MC1R基因的表达,顺势下调MC1R基因下游调控基因Mitf、Tyr与Tyrp2的表达,最终对羊驼皮肤黑色素细胞中黑色素的类型及合成量产生影响。展开更多
The interactions between several peptides with low molecular weight (guest, NH2 Arg Arg Trp Trp H 2; NH2 Arg Trp Arg Trp H 3; NH2 Trp Arg Arg Trp H 4; NH2 Arg Arg Trp Trp Trp Trp H 5; NH2 Trp Trp Arg Arg Trp Trp H 6; ...The interactions between several peptides with low molecular weight (guest, NH2 Arg Arg Trp Trp H 2; NH2 Arg Trp Arg Trp H 3; NH2 Trp Arg Arg Trp H 4; NH2 Arg Arg Trp Trp Trp Trp H 5; NH2 Trp Trp Arg Arg Trp Trp H 6; NH2 Arg Arg Trp Trp Trp Trp Trp Trp H 7; NH2 Arg Arg Trp Trp Trp Trp Trp Trp Trp Trp H 8) and β cyclodextrin dimer (host, 1) bridged with the derivative of (1R, 3R) 1 aminocyclobutane cis 1,3 dicar boxylic acid were investigated by using fluorescence polarization method in buffer aqueous solution (pH 7.4) at 298K. The binding constants of the cyclodextrin dimer 1 to the guests 2 8 were determined. It was shown that there was a cooperative action of the two cavities of a cyclodextrin dimer in the binding of large substrates, and that the structure and properties of amino acid in the peptides played very important roles in the synergic complexation between host and guest.展开更多
基金supported by the National Natural Science Foundation of China(No.2012BAD20B04)
文摘The title compound 1-（3-amino-[1,2,4]triazol-1-yl）-3,3-dimethyl-butan-2-one（3） was synthesized by Hofmann-alkylation reaction of 1-chloro-3,3-dimethyl-butan-2-one（1） and ~1H-[1,2,4]triazol-3-ylamine（2） with equal amount of K_2CO_3 as acid acceptor. The structure of compound 3 was characterized by ~1H NMR, 13 C NMR, HRMS and single-crystal X-ray diffraction. The compound crystallizes in the monoclinic system, space group P21/n with a = 5.7227（8）, b = 27.924（4）, c = 6.2282（7） ？, β = 101.892（11）°, V = 973.9（2） ？~3, Z = 4, T = 180.00（10） K, μ（MoKα） = 0.087 mm^（-1）, Dc = 1.243 g/cm^3, 3832 reflections measured（3.648≤θ≤26.022°）, 1916 unique reflections（Rint = 0.0359, Rsigma = 0.0572） used in all calculations. The final R = 0.0557（I 〉 2σ（I）） and w R = 0.1276（all data）. Bioassay showed that 3 displayed excellent activity as plant growth regulator with inducing lateral root formation and enhancing primary root elongation at 0.27 mmol/L（50 ppm） in soybeen（He Feng-50）. Good water solubility was found with 50 mg in 1 m L of water. Therefore, application of 3 in agriculture is more environmentally friendly due to cosolvent-free condition, and results in improved abiotic-stress tolerance by affecting the root growth. And furthermore, it can be used as a precursor to investigate the function of regulating plant root growth.
文摘旨在证明miR-324-3p可以通过调控其预测的靶基因MC1R及其下游基因的表达从而对羊驼皮肤黑色素的合成产生影响。本研究在体外培养的羊驼皮肤黑色素细胞中转染miR-324-3p过表达载体,应用qRT-PCR与Western blotting分析比较各试验组中MC1R基因与毛色相关基因小眼畸形相关转录因子(Microphthalmia-associtated transcription factor,Mitf)、酪氨酸酶(Tyrosinase,Tyr)、酪氨酸相关蛋白2(Tyrosinase related protein 2,Tyrp2)的表达差异性,利用酶标仪检测黑色素产量的变化。结果显示:(1)miR-324-3p在棕色与白色羊驼皮肤中均有表达,且在棕色羊驼皮肤中极显著表达(P<0.01),其相对表达量是白色的1.64倍;(2)黑色素细胞被转染了miR-324-3p过表达载体后,处理组靶基因MC1R及其下游调控基因Mitf、Tyr和Tyrp2的表达量与黑色素产量较空白对照组均有下调,且以Mitf基因表达量极显著下调(P<0.01)。综上表明,羊驼皮肤中miR-324-3p可能通过调控MC1R基因的表达,顺势下调MC1R基因下游调控基因Mitf、Tyr与Tyrp2的表达,最终对羊驼皮肤黑色素细胞中黑色素的类型及合成量产生影响。
基金supported by the National Basic Research and Development Program of China(973 Program,2011CB710800)New Century Excellent Talents in University(NCET-11-0658)+2 种基金Natural Science Foundation of Jiangsu Province(BK2011150)the Program of Introducing Talents of Discipline to Universities(111-2-06)a Project Funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions~~
文摘The interactions between several peptides with low molecular weight (guest, NH2 Arg Arg Trp Trp H 2; NH2 Arg Trp Arg Trp H 3; NH2 Trp Arg Arg Trp H 4; NH2 Arg Arg Trp Trp Trp Trp H 5; NH2 Trp Trp Arg Arg Trp Trp H 6; NH2 Arg Arg Trp Trp Trp Trp Trp Trp H 7; NH2 Arg Arg Trp Trp Trp Trp Trp Trp Trp Trp H 8) and β cyclodextrin dimer (host, 1) bridged with the derivative of (1R, 3R) 1 aminocyclobutane cis 1,3 dicar boxylic acid were investigated by using fluorescence polarization method in buffer aqueous solution (pH 7.4) at 298K. The binding constants of the cyclodextrin dimer 1 to the guests 2 8 were determined. It was shown that there was a cooperative action of the two cavities of a cyclodextrin dimer in the binding of large substrates, and that the structure and properties of amino acid in the peptides played very important roles in the synergic complexation between host and guest.
