Purine nucleotides are crucial for the effective operation of cell membrane proteins maintaining the neurotransmitter responses of 5-HT. Major protein targets in the treatment of depression include SERT, N/K ATPase an...Purine nucleotides are crucial for the effective operation of cell membrane proteins maintaining the neurotransmitter responses of 5-HT. Major protein targets in the treatment of depression include SERT, N/K ATPase and GPCR. Each protein target is responsive to a specific complement of drugs: antidepressants (SERT), lithium and cardiogenic steroids (N/K ATPase), 5-HT receptor ligands (GPCR). Computational software is useful for comparing molecular similarity within ligand-ligand and ligand-nucleotide structures. Previous studies demonstrate that GPCR ligands of different pharmacologic classes display relative molecular similarity to nucleotide structures. The current study applies this methodology to compound structures modulating SERT and N/K ATPase receptors. Minimum energy conformers of SERT antagonists demonstrate relative molecular similarity to the structural template of GTP nucleotide. GTP template fits of 5-HT and psilocin are similar, whereas a SERT-like fit is one of several for the ketamine structure. Endogenous and pharmaceutical modulators of Na/K ATPase relate to adenine nucleotide. The fits of cardiogenic steroids to a cGMP template demonstrate similarities and differences between compounds. Relative molecular similarity within the structures of hormones, drugs and nucleotides has implications for neurotransmitter transport and cell signal transduction processes.展开更多
为研究盐度渐变对日本囊对虾的机体免疫的影响,实验设置了4个盐度梯度分别为26、22、18和14,统计了各盐度下日本囊对虾累计死亡率,检测了日本囊对虾体内血清总蛋白(TP)含量、碱性磷酸酶(AKP)和酸性磷酸酶(ACP)、血清ATP酶(Na^(+)/K^(+)-...为研究盐度渐变对日本囊对虾的机体免疫的影响,实验设置了4个盐度梯度分别为26、22、18和14,统计了各盐度下日本囊对虾累计死亡率,检测了日本囊对虾体内血清总蛋白(TP)含量、碱性磷酸酶(AKP)和酸性磷酸酶(ACP)、血清ATP酶(Na^(+)/K^(+)-ATPase和T-ATPase)、超氧化物歧化酶(SOD)和多酚氧化酶(PPO)的动态变化。结果显示,盐度渐变胁迫下各盐度组累计死亡率的大小为14>18>22>26,血清蛋白含量随胁迫强度的增加和胁迫时间的延长呈下降趋势,后随着盐度回升而上升。24~72 h ACP和AKP活力表现为盐度组14<18<22<26,且随时间的延长呈下降趋势,Na^(+)/K^(+)-ATPase和T-ATPase活力显示出盐度梯度差异显著,14盐度组显著高于其它盐度组(P<0.05),SOD活力与PPO活力受盐度胁迫强度和胁迫时间的影响显著,盐度胁迫强度越强,SOD活力与对照组的差异越显著(P<0.05),血清PPO活力的变化趋势越明显。日本囊对虾机体免疫受盐度胁迫显著,研究结果为日本囊对虾的健康养殖提供重要的理论指导及借鉴。展开更多
[目的]观察葱白提取物对非酒精性脂肪肝(NAFLD)模型大鼠ATP合酶Fo亚基6(ATPase6)、ATP合酶Fo亚基8(ATPase8)表达的影响,并探讨其作用机制。[方法]将50只雄性SD大鼠随机分为正常组、模型组、葱白低剂量组、葱白中剂量组、葱白高剂量组,每...[目的]观察葱白提取物对非酒精性脂肪肝(NAFLD)模型大鼠ATP合酶Fo亚基6(ATPase6)、ATP合酶Fo亚基8(ATPase8)表达的影响,并探讨其作用机制。[方法]将50只雄性SD大鼠随机分为正常组、模型组、葱白低剂量组、葱白中剂量组、葱白高剂量组,每组10只。采用高脂饮食喂养复制NAFLD模型大鼠,造模10周后,给予葱白提取物连续干预4周后,测定血清中丙氨酸氨基转移酶(ALT)、天门冬氨酸氨基转移酶(AST)和甘油三酯(TG)、胆固醇(TC)的含量;苏木精-伊红(HE)染色法观察肝脏组织结构变化;Real time PCR检测大鼠肝脏组织中ATPase6、ATPase8 mRNA的表达。[结果]与正常组比较,模型组出现明显肝脂肪变性,血清ALT、AST、TC、TG水平明显升高(P<0.05),ATPase6、ATPase8 mRNA的表达明显降低(P<0.05);相较于模型组,葱白低、中、高剂量组肝脂肪变性均不同程度减轻;血清ALT、AST、TC、TG水平均不同程度降低(P<0.05),ATPase6、ATPase8 m RNA表达不同程度升高(P<0.05)。与葱白低剂量组比较,葱白中、高剂量组肝脂肪变性减轻明显,ALT、AST、TC、TG水平明显降低(P<0.05),ATPase6、ATPase8 mRNA水平明显升高(P<0.05),中、高剂量葱白组之间差异无统计学意义。[结论]葱白提取物能够改善肝脂肪变性,可能与提高ATPase6、ATPase8的表达,增加肝线粒体ATP合成有关。展开更多
文摘Purine nucleotides are crucial for the effective operation of cell membrane proteins maintaining the neurotransmitter responses of 5-HT. Major protein targets in the treatment of depression include SERT, N/K ATPase and GPCR. Each protein target is responsive to a specific complement of drugs: antidepressants (SERT), lithium and cardiogenic steroids (N/K ATPase), 5-HT receptor ligands (GPCR). Computational software is useful for comparing molecular similarity within ligand-ligand and ligand-nucleotide structures. Previous studies demonstrate that GPCR ligands of different pharmacologic classes display relative molecular similarity to nucleotide structures. The current study applies this methodology to compound structures modulating SERT and N/K ATPase receptors. Minimum energy conformers of SERT antagonists demonstrate relative molecular similarity to the structural template of GTP nucleotide. GTP template fits of 5-HT and psilocin are similar, whereas a SERT-like fit is one of several for the ketamine structure. Endogenous and pharmaceutical modulators of Na/K ATPase relate to adenine nucleotide. The fits of cardiogenic steroids to a cGMP template demonstrate similarities and differences between compounds. Relative molecular similarity within the structures of hormones, drugs and nucleotides has implications for neurotransmitter transport and cell signal transduction processes.
文摘为研究盐度渐变对日本囊对虾的机体免疫的影响,实验设置了4个盐度梯度分别为26、22、18和14,统计了各盐度下日本囊对虾累计死亡率,检测了日本囊对虾体内血清总蛋白(TP)含量、碱性磷酸酶(AKP)和酸性磷酸酶(ACP)、血清ATP酶(Na^(+)/K^(+)-ATPase和T-ATPase)、超氧化物歧化酶(SOD)和多酚氧化酶(PPO)的动态变化。结果显示,盐度渐变胁迫下各盐度组累计死亡率的大小为14>18>22>26,血清蛋白含量随胁迫强度的增加和胁迫时间的延长呈下降趋势,后随着盐度回升而上升。24~72 h ACP和AKP活力表现为盐度组14<18<22<26,且随时间的延长呈下降趋势,Na^(+)/K^(+)-ATPase和T-ATPase活力显示出盐度梯度差异显著,14盐度组显著高于其它盐度组(P<0.05),SOD活力与PPO活力受盐度胁迫强度和胁迫时间的影响显著,盐度胁迫强度越强,SOD活力与对照组的差异越显著(P<0.05),血清PPO活力的变化趋势越明显。日本囊对虾机体免疫受盐度胁迫显著,研究结果为日本囊对虾的健康养殖提供重要的理论指导及借鉴。
文摘[目的]观察葱白提取物对非酒精性脂肪肝(NAFLD)模型大鼠ATP合酶Fo亚基6(ATPase6)、ATP合酶Fo亚基8(ATPase8)表达的影响,并探讨其作用机制。[方法]将50只雄性SD大鼠随机分为正常组、模型组、葱白低剂量组、葱白中剂量组、葱白高剂量组,每组10只。采用高脂饮食喂养复制NAFLD模型大鼠,造模10周后,给予葱白提取物连续干预4周后,测定血清中丙氨酸氨基转移酶(ALT)、天门冬氨酸氨基转移酶(AST)和甘油三酯(TG)、胆固醇(TC)的含量;苏木精-伊红(HE)染色法观察肝脏组织结构变化;Real time PCR检测大鼠肝脏组织中ATPase6、ATPase8 mRNA的表达。[结果]与正常组比较,模型组出现明显肝脂肪变性,血清ALT、AST、TC、TG水平明显升高(P<0.05),ATPase6、ATPase8 mRNA的表达明显降低(P<0.05);相较于模型组,葱白低、中、高剂量组肝脂肪变性均不同程度减轻;血清ALT、AST、TC、TG水平均不同程度降低(P<0.05),ATPase6、ATPase8 m RNA表达不同程度升高(P<0.05)。与葱白低剂量组比较,葱白中、高剂量组肝脂肪变性减轻明显,ALT、AST、TC、TG水平明显降低(P<0.05),ATPase6、ATPase8 mRNA水平明显升高(P<0.05),中、高剂量葱白组之间差异无统计学意义。[结论]葱白提取物能够改善肝脂肪变性,可能与提高ATPase6、ATPase8的表达,增加肝线粒体ATP合成有关。