[Objectives] This study was conducted to understand the biological characteristics of Duoluo goats. [Methods] With male and female Duoluo goats as the research object, related performance indexes were determined and a...[Objectives] This study was conducted to understand the biological characteristics of Duoluo goats. [Methods] With male and female Duoluo goats as the research object, related performance indexes were determined and analyzed after slaughter. [Results] The weights of one-year-old male and female Duoluo goats before slaughter were (25.68±2.37) and (24.51±1.97) kg, respectively;the dressing percentages were (43.55±3.24) % and (43.84±3.42) %, respectively;and the net meat percentages were (33.02±2.32) % and (34.19±2.46) %, respectively. (2) The cooked meat rates of male and female Duoluo goats were (65.49±1.42) % and (65.36±1.55) %, respectively;the shearing force was (5.48±1.24) and (5.65±1.02) N, respectively;and the loin-eye muscle areas were (8.95±1.72) and (8.82±1.15) cm 2, respectively. (3) The protein contents of male and female Duoluo goats were (20.07±0.42) and (19.47±1.22) g/100 g, respectively;and the fat contents were (1.30±0.80) % and (2.92±0.55) %, respectively;and the cholesterol contents were (71.76±11.47) and (74.83±2.68) mg/100 g, respectively;(4) The Ca contents of male and female Duoluo goats were (69.53±10.89) and (63.00±4.56) mg/kg, respectively;the Fe contents were (16.73±1.83) and (14.77±0.58) mg/kg, respectively;and the Zn contents were (38.47±3.68) and (31.83±2.22) mg/kg, respectively. (5) In the muscles of male and female Duoluo goats, the contents of essential amino acids were (7.44±0.24) and (7.26±0.41) g/100 g , respectively;the contents of non-essential amino acids were (11.81±0.33) and (11.42±0.67) g/100 g, respectively;and the contents of flavor amino acids were (8.79±0.27) and (8.42±0.57) g/100 g, respectively. [Conclusions] This study lays a foundation for the excavation and utilization of the resource, Duoluo goats.展开更多
We have discovered and synthesized a series of indole-based derivatives as novel sigma-2(σ_(2))receptor ligands.Two ligands with high σ_(2) receptor affinity and subtype selectivity were then radiolabeled with F-18 ...We have discovered and synthesized a series of indole-based derivatives as novel sigma-2(σ_(2))receptor ligands.Two ligands with high σ_(2) receptor affinity and subtype selectivity were then radiolabeled with F-18 in good radiochemical yields and purities,and evaluated in rodents.In biodistribution studies in male ICR mice,radioligand[18F]9,or 1-(4-(5,6-dimethoxyisoindolin-2-yl)butyl)-4-(2-[18F]fluoroethoxy)-1H-indole,was found to display high brain uptake and high brain-to-blood ratio.Pretreatment of animals with the selective σ_(2) receptor ligand CM398 led to significant reductions in both brain uptake(29%-54%)and brain-to-blood ratio(60%-88%)of the radioligand in a dose-dependent manner,indicating high and saturable specific binding of[18F]9 to σ_(2) receptors in the brain.Further,ex vivo autoradiography in male ICR mice demonstrated regionally heterogeneous specific binding of[18F]9 in the brain that is consistent with the distribution pattern of σ_(2) receptors.Dynamic positron emission tomography imaging confirmed regionally distinct distribution and high levels of specific binding for[18F]9 in the rat brain,along with appropriate tissue kinetics.Taken together,results from our current study indicated the novel radioligand[18F]9 as the first highly specific and promising imaging agent for σ_(2) receptors in the brain.展开更多
Monoacylglycerol lipase(MAGL) is a pivotal enzyme in the endocannabinoid system, which metabolizes 2-arachidonoylglycerol(2-AG) into the proinflammatory eicosanoid precursor arachidonic acid(AA). MAGL and other endoge...Monoacylglycerol lipase(MAGL) is a pivotal enzyme in the endocannabinoid system, which metabolizes 2-arachidonoylglycerol(2-AG) into the proinflammatory eicosanoid precursor arachidonic acid(AA). MAGL and other endogenous cannabinoid(EC) degrading enzymes are involved in the fibrogenic signaling pathways that induce hepatic stellate cell(HSC) activation and ECM accumulation during chronic liver disease. Our group recently developed an;F-labeled MAGL inhibitor([18F]MAGL-4-11)for PET imaging and demonstrated highly specific binding in vitro and in vivo. In this study, we determined [18F]MAGL-4-11 PET enabled imaging MAGL levels in the bile duct ligation(BDL) and carbon tetrachloride(CCl_(4)) models of liver cirrhosis;we also assessed the hepatic gene expression of the enzymes involved with EC system including MAGL, NAPE-PLD, FAAH and DAGL that as a function of disease severity in these models;[18F]MAGL-4-11 autoradiography was performed to assess tracer binding in frozen liver sections both in animal and human. [18F]MAGL-4-11 demonstrated reduced PET signals in early stages of fibrosis and further significantly decreased with disease progression compared with control mice. We confirmed MAGL and FAAH expression decreases with fibrosisseverity, while its levels in normal liver tissue are high;in contrast, the EC synthetic enzymes NAPE-PLD and DAGL are enhanced in these different fibrosis models. In vitro autoradiography further supported that[18F]MAGL-4-11 bound specifically to MAGL in both animal and human fibrotic liver tissues. Our PET ligand [18F]MAGL-4-11 shows excellent sensitivity and specificity for MAGL visualization in vivo and accurately reflects the histological stages of liver fibrosis in preclinical models and human liver tissues.展开更多
基金Supported by Sichuan Provincial Mutton Sheep Innovation Team(CXTD2019-14)Special Fund Factor Method Transfer Payment Project of Sichuan Science and Technology Program(220017)。
文摘[Objectives] This study was conducted to understand the biological characteristics of Duoluo goats. [Methods] With male and female Duoluo goats as the research object, related performance indexes were determined and analyzed after slaughter. [Results] The weights of one-year-old male and female Duoluo goats before slaughter were (25.68±2.37) and (24.51±1.97) kg, respectively;the dressing percentages were (43.55±3.24) % and (43.84±3.42) %, respectively;and the net meat percentages were (33.02±2.32) % and (34.19±2.46) %, respectively. (2) The cooked meat rates of male and female Duoluo goats were (65.49±1.42) % and (65.36±1.55) %, respectively;the shearing force was (5.48±1.24) and (5.65±1.02) N, respectively;and the loin-eye muscle areas were (8.95±1.72) and (8.82±1.15) cm 2, respectively. (3) The protein contents of male and female Duoluo goats were (20.07±0.42) and (19.47±1.22) g/100 g, respectively;and the fat contents were (1.30±0.80) % and (2.92±0.55) %, respectively;and the cholesterol contents were (71.76±11.47) and (74.83±2.68) mg/100 g, respectively;(4) The Ca contents of male and female Duoluo goats were (69.53±10.89) and (63.00±4.56) mg/kg, respectively;the Fe contents were (16.73±1.83) and (14.77±0.58) mg/kg, respectively;and the Zn contents were (38.47±3.68) and (31.83±2.22) mg/kg, respectively. (5) In the muscles of male and female Duoluo goats, the contents of essential amino acids were (7.44±0.24) and (7.26±0.41) g/100 g , respectively;the contents of non-essential amino acids were (11.81±0.33) and (11.42±0.67) g/100 g, respectively;and the contents of flavor amino acids were (8.79±0.27) and (8.42±0.57) g/100 g, respectively. [Conclusions] This study lays a foundation for the excavation and utilization of the resource, Duoluo goats.
基金supported by the National Natural Science Foundation of China(No.21876013)Beijing Natural Science Foundation(7212203,China)。
文摘We have discovered and synthesized a series of indole-based derivatives as novel sigma-2(σ_(2))receptor ligands.Two ligands with high σ_(2) receptor affinity and subtype selectivity were then radiolabeled with F-18 in good radiochemical yields and purities,and evaluated in rodents.In biodistribution studies in male ICR mice,radioligand[18F]9,or 1-(4-(5,6-dimethoxyisoindolin-2-yl)butyl)-4-(2-[18F]fluoroethoxy)-1H-indole,was found to display high brain uptake and high brain-to-blood ratio.Pretreatment of animals with the selective σ_(2) receptor ligand CM398 led to significant reductions in both brain uptake(29%-54%)and brain-to-blood ratio(60%-88%)of the radioligand in a dose-dependent manner,indicating high and saturable specific binding of[18F]9 to σ_(2) receptors in the brain.Further,ex vivo autoradiography in male ICR mice demonstrated regionally heterogeneous specific binding of[18F]9 in the brain that is consistent with the distribution pattern of σ_(2) receptors.Dynamic positron emission tomography imaging confirmed regionally distinct distribution and high levels of specific binding for[18F]9 in the rat brain,along with appropriate tissue kinetics.Taken together,results from our current study indicated the novel radioligand[18F]9 as the first highly specific and promising imaging agent for σ_(2) receptors in the brain.
基金supported by MGH Research Scholars Program(to Raymond.T.Chung,USA)。
文摘Monoacylglycerol lipase(MAGL) is a pivotal enzyme in the endocannabinoid system, which metabolizes 2-arachidonoylglycerol(2-AG) into the proinflammatory eicosanoid precursor arachidonic acid(AA). MAGL and other endogenous cannabinoid(EC) degrading enzymes are involved in the fibrogenic signaling pathways that induce hepatic stellate cell(HSC) activation and ECM accumulation during chronic liver disease. Our group recently developed an;F-labeled MAGL inhibitor([18F]MAGL-4-11)for PET imaging and demonstrated highly specific binding in vitro and in vivo. In this study, we determined [18F]MAGL-4-11 PET enabled imaging MAGL levels in the bile duct ligation(BDL) and carbon tetrachloride(CCl_(4)) models of liver cirrhosis;we also assessed the hepatic gene expression of the enzymes involved with EC system including MAGL, NAPE-PLD, FAAH and DAGL that as a function of disease severity in these models;[18F]MAGL-4-11 autoradiography was performed to assess tracer binding in frozen liver sections both in animal and human. [18F]MAGL-4-11 demonstrated reduced PET signals in early stages of fibrosis and further significantly decreased with disease progression compared with control mice. We confirmed MAGL and FAAH expression decreases with fibrosisseverity, while its levels in normal liver tissue are high;in contrast, the EC synthetic enzymes NAPE-PLD and DAGL are enhanced in these different fibrosis models. In vitro autoradiography further supported that[18F]MAGL-4-11 bound specifically to MAGL in both animal and human fibrotic liver tissues. Our PET ligand [18F]MAGL-4-11 shows excellent sensitivity and specificity for MAGL visualization in vivo and accurately reflects the histological stages of liver fibrosis in preclinical models and human liver tissues.
