Artificial joint replacement surgery is the orthopedic procedure of choice to relieve pain, correct joint deformities, and help patients resume everyday activities. However, the detailed mechanisms regulating peri-imp...Artificial joint replacement surgery is the orthopedic procedure of choice to relieve pain, correct joint deformities, and help patients resume everyday activities. However, the detailed mechanisms regulating peri-implant bone remodeling at the bone-prosthesis interface remain elusive. To address this gap in knowledge, we evaluated the natural postoperative course of bone metabolism by using [18F] NaF positron emission tomography (PET)/computed tomography in 57 patients (104 joints) who underwent asymptomatic total knee arthroplasty (TKA). First, we measured total tracer uptake around TKA to determine the total bone metabolism (TBM) and used the ischial tuberosity as the reference tissue for normalization of PET images. Second, we calculated the TBM ratio (TBMR) by dividing the TBM by tracer uptake in the reference tissue. A moderate increase in TBMR was observed 4 - 5 days after implantation, and its intensity reached the maximum on the seventh postoperative day. The TBMR showed no differences until 12 weeks, after which it decreased slowly and returned to the basal levels. The new parameter TBMR and the unique pattern of postoperative metabolic changes in the bone around the prosthesis may help set accurate interpretation criteria to diagnose complications such as loosening or infections.展开更多
Differences between the inhibitory activities of specific compounds on analogous enzymes isolated from different animal species are one of the critical issues to evaluate when exploring structure-activity relationship...Differences between the inhibitory activities of specific compounds on analogous enzymes isolated from different animal species are one of the critical issues to evaluate when exploring structure-activity relationships. The activity of acarbose is about ten times stronger in rat than in human, and that of neosalacinol is similar in both species. Binding affinities of acarbose and neosalacinol to four catalytic domains of alpha-glucosidases in human and rat were compared to investigate the cause of activity differences among species. Species difference was brought about complicatedly by the balance of interaction with four domains, and the result was indicated that larger ligand would show larger species difference in activity.展开更多
Maltase-glucoamylase (MGAM) and sucrase-isomaltase (SI) belong to human intestinal alpha-glucosidase and their N-terminal side catalytic domains are called NtMGAM and NtSI, and their C-terminal side catalytic domains ...Maltase-glucoamylase (MGAM) and sucrase-isomaltase (SI) belong to human intestinal alpha-glucosidase and their N-terminal side catalytic domains are called NtMGAM and NtSI, and their C-terminal side catalytic domains are called CtMGAM and CtSI. As an antidiabetic, alpha-glucosidase inhibitor is required to bind to all of these domains to inhibit disaccharides hydrolysis. Salacinol and kotalanol isolated from Salacia reticulata are novel seed compounds for al-pha-glucosidase inhibitor. Even though the complex structures of NtMGAM or NtSI have been determined experimen-tally, those of CtMGAM and CtSI have not been revealed. Thus, homology modeling for CtMGAM and CtSI has been performed to predict the binding mode of salacinol and its derivatives for each domain. The binding affinities for these compounds were also calculated to explain the experimental structure-activity relationships (SARs). After a docking study of the derivatives to each catalytic domain, the MM/PBSA method has been applied to predict the binding affinities. The predicted binding affinities were almost consistent with the experimental SARs. The comparison of the complex structures and binding affinities provided insights for designing novel compounds, which inhibit all catalytic domains.展开更多
A lot of phenomena related to propagating various waves are seen when the high-speed train goes through the tunnel,the gas pipeline is broken due to an accident or the air brake of the wagon operates.For instance,a co...A lot of phenomena related to propagating various waves are seen when the high-speed train goes through the tunnel,the gas pipeline is broken due to an accident or the air brake of the wagon operates.For instance,a compression wave generated ahead of a high-speed train entering a tunnel propagates to the tunnel exit and spouts as a micro pressure wave,which causes an exploding sound.In order to estimate the magnitude correctly,the mechanism of the attenuation and distortion of a compression wave propagating along a very long tunnel must be understood and the experimental information on these phenomena is required.An experimental investigation is carried out to clarify the attenuation and distortion of the propagating compression wave in a very long tube.Experimental results show that the strength of a compression wave decreases with distance.The attenuation and distortion of compression waves are affected by the initial waveform of the compression wave and by the unsteady boundary layer induced by the propagating wave.The shape of a compression wave becomes different with the propagating distance;that is,a shock wave appears just head of a wavefront and an overshoot on pressure distribution is observed behind a shock wave due to the transition of the unsteady boundary layer.展开更多
文摘Artificial joint replacement surgery is the orthopedic procedure of choice to relieve pain, correct joint deformities, and help patients resume everyday activities. However, the detailed mechanisms regulating peri-implant bone remodeling at the bone-prosthesis interface remain elusive. To address this gap in knowledge, we evaluated the natural postoperative course of bone metabolism by using [18F] NaF positron emission tomography (PET)/computed tomography in 57 patients (104 joints) who underwent asymptomatic total knee arthroplasty (TKA). First, we measured total tracer uptake around TKA to determine the total bone metabolism (TBM) and used the ischial tuberosity as the reference tissue for normalization of PET images. Second, we calculated the TBM ratio (TBMR) by dividing the TBM by tracer uptake in the reference tissue. A moderate increase in TBMR was observed 4 - 5 days after implantation, and its intensity reached the maximum on the seventh postoperative day. The TBMR showed no differences until 12 weeks, after which it decreased slowly and returned to the basal levels. The new parameter TBMR and the unique pattern of postoperative metabolic changes in the bone around the prosthesis may help set accurate interpretation criteria to diagnose complications such as loosening or infections.
文摘Differences between the inhibitory activities of specific compounds on analogous enzymes isolated from different animal species are one of the critical issues to evaluate when exploring structure-activity relationships. The activity of acarbose is about ten times stronger in rat than in human, and that of neosalacinol is similar in both species. Binding affinities of acarbose and neosalacinol to four catalytic domains of alpha-glucosidases in human and rat were compared to investigate the cause of activity differences among species. Species difference was brought about complicatedly by the balance of interaction with four domains, and the result was indicated that larger ligand would show larger species difference in activity.
文摘Maltase-glucoamylase (MGAM) and sucrase-isomaltase (SI) belong to human intestinal alpha-glucosidase and their N-terminal side catalytic domains are called NtMGAM and NtSI, and their C-terminal side catalytic domains are called CtMGAM and CtSI. As an antidiabetic, alpha-glucosidase inhibitor is required to bind to all of these domains to inhibit disaccharides hydrolysis. Salacinol and kotalanol isolated from Salacia reticulata are novel seed compounds for al-pha-glucosidase inhibitor. Even though the complex structures of NtMGAM or NtSI have been determined experimen-tally, those of CtMGAM and CtSI have not been revealed. Thus, homology modeling for CtMGAM and CtSI has been performed to predict the binding mode of salacinol and its derivatives for each domain. The binding affinities for these compounds were also calculated to explain the experimental structure-activity relationships (SARs). After a docking study of the derivatives to each catalytic domain, the MM/PBSA method has been applied to predict the binding affinities. The predicted binding affinities were almost consistent with the experimental SARs. The comparison of the complex structures and binding affinities provided insights for designing novel compounds, which inhibit all catalytic domains.
文摘A lot of phenomena related to propagating various waves are seen when the high-speed train goes through the tunnel,the gas pipeline is broken due to an accident or the air brake of the wagon operates.For instance,a compression wave generated ahead of a high-speed train entering a tunnel propagates to the tunnel exit and spouts as a micro pressure wave,which causes an exploding sound.In order to estimate the magnitude correctly,the mechanism of the attenuation and distortion of a compression wave propagating along a very long tunnel must be understood and the experimental information on these phenomena is required.An experimental investigation is carried out to clarify the attenuation and distortion of the propagating compression wave in a very long tube.Experimental results show that the strength of a compression wave decreases with distance.The attenuation and distortion of compression waves are affected by the initial waveform of the compression wave and by the unsteady boundary layer induced by the propagating wave.The shape of a compression wave becomes different with the propagating distance;that is,a shock wave appears just head of a wavefront and an overshoot on pressure distribution is observed behind a shock wave due to the transition of the unsteady boundary layer.