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101.
Characterization of the estrogenic activities of zearalenone and zeranol in vivo and in vitro 总被引:1,自引:0,他引:1
Takemura H Shim JY Sayama K Tsubura A Zhu BT Shimoi K 《The Journal of steroid biochemistry and molecular biology》2007,103(2):170-177
In the present study, we compared the estrogenic activity of zearalenone (ZEN) and zeranol (ZOL) by determining their relative receptor binding affinities for human ERalpha and ERbeta and also by determining their uterotropic activity in ovariectomized female mice. ZOL displayed a much higher binding affinity for human ERalpha and ERbeta than ZEN did. The IC(50) values of ZEN and ZOL for binding to human ERalpha were 240.4 and 21.79nM, respectively, and the IC(50) values for binding to ERbeta were 165.7 and 42.76nM, respectively. In ovariectomized female ICR mice, s.c. administration of ZEN at doses >or=2mg/kg/day for 3 consecutive days significantly increased uterine wet weight compared with the control group, and administration of ZOL increased the uterine wet weight at lower doses (>or=0.5mg/kg/day for 3 days). Based on available X-ray crystal structures of human ERalpha and ERbeta, we have also conducted molecular modeling studies to probe the binding characteristics of ZEN and ZOL for human ERalpha and ERbeta. Our data revealed that ZEN and ZOL were able to occupy the active site of the human ERalpha and ERbeta in a strikingly similar manner as 17beta-estradiol, such that the phenolic rings of ZEN and ZOL occupied the same receptor region as occupied by the A-ring of 17beta-estradiol. The primary reason that ZOL and ZEN is less potent than 17beta-estradiol is likely because 17beta-estradiol could bind to the receptor pocket without significantly changing its conformation, while ZOL or ZEN would require considerable conformational alterations upon binding to the estrogen receptors (ERs). 相似文献
102.
Teno N Miyake T Ehara T Irie O Sakaki J Ohmori O Gunji H Matsuura N Masuya K Hitomi Y Nonomura K Horiuchi M Gohda K Iwasaki A Umemura I Tada S Kometani M Iwasaki G Cowan-Jacob SW Missbach M Lattmann R Betschart C 《Bioorganic & medicinal chemistry letters》2007,17(22):6096-6100
Pyrrolopyrimidine, a novel scaffold, allows to adjust interactions within the S3 subsite of cathepsin K. The core intermediate 10 facilitated the P3 optimization and identified highly potent and selective cathepsin K inhibitors 11-20. 相似文献
103.
Namiki K Nakamura A Furuya M Mizuhashi S Matsuo Y Tokuhara N Sudo T Hama H Kuwaki T Yano S Kimura S Kasuya Y 《Journal of receptor and signal transduction research》2007,27(2-3):99-111
We investigated how p38alpha mitogen-activated protein kinase (p38) is related to kainate-induced epilepsy and neuronal damages, by using the mice with a single copy disruption of the p38 alpha gene (p38alpha(+/-)). Mortality rate and seizure score of p38alpha(+/-) mice administered with kainate were significantly reduced compared with the case of wild-type (WT) mice. This was clearly supported by the electroencephalography data in which kainate-induced seizure duration and frequency in the brain of p38alpha(+/-) mice were significantly suppressed compared to those of WT mice. As a consequence of seizure, kainate induced delayed neuronal damages in parallel with astrocytic growth in the hippocampus and ectopic innervation of the mossy fibers into the stratum oriens in the CA3 region of hippocampus in WT mice, whose changes were moderate in p38alpha(+/-) mice. Likewise, kainate-induced phosphorylation of calcium/calmodulin-dependent kinase II in the hippocampus of p38alpha (+/-) mice was significantly decreased compared to that of WT mice. These results suggest that p38alpha signaling pathway plays an important role in epileptic seizure and excitotoxicity. 相似文献
104.
Fluxomics: mass spectrometry versus quantitative imaging 总被引:1,自引:0,他引:1
105.
Masamichi Takahashi Hitomi Furusawa Pitayakon Limtong Vanlada Sunanthapongsuk Dokrak Marod Samruan Panuthai 《Ecological Research》2007,22(1):160-164
We have examined the surface (0–10 cm) soil characteristics of sites after bamboo (Cephalostachyum pergracile) mass flowering and death (DB sites) in comparison with sites with living bamboo (Bambusa tulda) (LB sites) in a seasonal tropical forest in Thailand. One year after bamboo flowering the DB sites were acidic with lower
concentrations of exchangeable Ca and Mg and soil nitrogen than the LB sites. Therefore, although leaf and root litter of
the dead bamboo was deposited in the DB sites after bamboo flowering, soil nutrient status decreased. 相似文献
106.
Kunisawa Kazuo Shan Jiajing Lu Qiaohui Yang Yang Kosuge Aika Kurahashi Hitomi Saito Kuniaki Zou Libo Nabeshima Toshitaka Mouri Akihiro 《Neurochemical research》2022,47(9):2880-2889
Neurochemical Research - Major depressive disorder (MDD) is the most prevalent and serious psychiatric disease involving inflammation. Loureirin C and Xanthoceraside are extracts of dragon’s... 相似文献
107.
Paired box gene 5 isoforms A and B have different functions in transcriptional regulation of B cell development‐related genes in immature B cells
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108.
109.
Influence of Prostate Stem Cell Antigen Gene Polymorphisms on Susceptibility to Helicobacter pylori‐associated Diseases: A Case‐control Study
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110.
Harada T Kobayashi R Wada K Nishihara R Kondo A Akimitsu O Noji T Taniwaki N Nakade M Krejci M Takeuchi H 《Chronobiology international》2011,28(7):638-642
Several studies suggest that season of birth differentially affects the physiological characteristics of humans. Those living at relatively high latitude, such as Canada, Spain, and Italy (44°N-45°N), and born in the fall tended to be "morning-type" persons in comparison to those born in other seasons. There are relatively little data on the affect of season of birth on people residing at low latitude. Here the authors show that at low latitude, Kochi, Japan (33°N), the effect of season of birth on the morningness chronotype is confined to young children aged 1-12 yrs, disappearing in elderly persons. Only female participants aged 2-12 yrs born in the fall, especially in November, were significantly morning-typed (p < .001) in comparison to those born in the other seasons, whereas there were no such significant season-of-birth differences in morningness-eveningness preference among male participants. Moreover, both female and male participants aged 13-25 yrs showed no significant seasonal differences in morningness-eveningness preference. The small effects detected in this study might be due to smaller seasonal change in day length at the relatively lower latitude of Kochi. 相似文献