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101.
Hirotaka Kashiwagi Yoshiyuki Ono Masateru Ohta Susumu Itoh Fumihiko Ichikawa Suguru Harada Satoshi Takeda Nobuo Sekiguchi Masaki Ishigai Tadakatsu Takahashi 《Bioorganic & medicinal chemistry》2013,21(7):1823-1833
In an extension of our study on gamma hydroxy carboxylic acid analogs, we explored a series of nonsecosteroidal vitamin D receptor (VDR) agonists in which 1,3-diol of 1,25(OH)2D3 had been replaced by aryl acetic acid. These analogs showed very potent activity in vitro compared with 1,25(OH)2D3. An X-ray analysis of 8d showed that the inserted phenyl ring well mimicked the folded methylene linker of the gamma hydroxy carboxylic acid moiety but the carboxylic acid of 8d interacted with VDR in a different manner from gamma hydroxy carboxylic acids. Through our in vivo screening in an osteoporosis rat model using immature rats, we identified a potent active vitamin D3 analog, compound 7e. In mature rats of the same model, compound 7e also showed good PK profiling and excellent ability to prevent bone mineral density loss without severe hypercalcemia. Our nonsecosteroidal VDR agonist 7e (CH5036249) could be a possible new drug candidate for treating osteoporosis in human. 相似文献
102.
Koshi Arai Tetsu Ando Sadahiro Tatsuki Kenji Usui Yoshiko Ohguchi Matsuo Kurihara 《Bioscience, biotechnology, and biochemistry》2013,77(12):3165-3168
Lipoxygenase-3, the major component of the enzyme in rice grain, was purified 2980-fold with a yield of 7% from embryos. The purified enzyme had a specific activity of 280 μmol O2 formed/min per mg protein. This enzyme was inactivated by SH compounds, such as cysteine and glutathione. The inactivation was prevented by the addition of catalase or replacement of the air by N2 gas. These two treatments were also effective for the stable storage of the purified enzyme. The molecular weights measured by sodium dodecyl sulfate gel and gradient gel electrophoresis were 93,000 and 89,000, respectively, indicating that the enzyme is a single polypeptide chain. The purified enzyme contained 0.73 Fe atom per molecule. The absorption spectrum suggested that the enzyme is a non-heme iron protein. Some similarities in amino-acid composition were observed between rice, soybean, and pea lipoxygenases. The purified enzyme specifically produced 9-d-hydroperoxy-10,12(E,Z)-octadecadienoic acid when linoleic acid was used as a substrate. 相似文献
103.
104.
Takeshi Sugai Shigefumi Kuwahara Chimaki Hoshino Noritada Matsuo Kenji Mori 《Bioscience, biotechnology, and biochemistry》2013,77(10):2579-2585
Asymmetric hydrolysis of the acetates of racemic secondary alcohols related to synthetic pyrethroids by Bacillus subtilis var. niger (IFO 3108) yielded optically active acetates and alcohols of varying optical purities. 相似文献
105.
For determining sclerothionine (STH, S-2-hydroxyethylergothioneine), the method of P. C. Jocelyn which determined ergothioneine in blood was applied, and it was shown that STH was necessary to be degraded with 70% KOH for 1 hr at 100°C, in order to get a theoretical amount of trimethylamine. Trimethylamine produced was trapped by picric acid and spectrophotometrically measured as picrate at 410 mμ. By this method and using paper chromatography, STH in Sclerotinia culture could be determined successfully, and it was found that, among Sclerotinia fungi, a strain of Sclerotinia libertiana which can form sclerotium normally only produced STH, and other various strains of the same genus produced ergothioneine. The cultural condition for production of STH by the Sclerotinia libertiana strain was investigated. As a result, in the shaking liquid culture containing wheat bran, 1.0%; glucose, 1.0%; Polypepton, 0.6%; KH2PO4, 0.05%; MgCl2, 0.05% and cystine-HCl, 0.003% as nutrient, the addition of methionine at a later period in about 0.01% concentration was found to stimulate the accumulation of STH in mycelium. 相似文献
106.
Hideyuki Furukawa Hideki Matsuo Takashi Deguchi Akio Shiga Hirotoshi Samejima 《Bioscience, biotechnology, and biochemistry》2013,77(5):617-623
l-Lysine monohydrochloride and d-glucose were allowed to react in a bicarbonate buffer of pH 8.8 under refluxing. The reaction mixture was then chromatographed on a thin-layer plate of Kiesel Gel using n-propanol ethyl-acetate water 25% aqueous ammonia (6: 1: 2: 1 v/v) as a developing agent. Elson-Morgan-reactive spots on the chromatogram were eluted individually, and each of the eluates was incubated with L. bifidus var. pennsylvanicus in a defined medium. A certain fraction on the chromatogram showed remarkably promoting effect on both the acid productivity and the growth of the organism. And such effect of the fraction was much stronger than that of N-acetyl-d-glucosamine which had been known as a “Bifidus Factor” 相似文献
107.
Yoshinari Kobayashi Ryûkichi Matsuo 《Bioscience, biotechnology, and biochemistry》2013,77(5):1333-1335
The degradation of nitrite and the inhibition towards formation of carcinogenic nitrosamines by melanoidins, produced from the glucose-glycine system were investigated at various conditions. The degradation of nitrite was highest at pH 1.2 (29%), when the ratio of melanoidins to nitrite was 1: 3. The inhibition towards formation of nitrosamines by melanoidins had the same tendency as the degradation of nitrite, the inhibition also being highest at pH 1.2 (99%). In addition, melanoidins after nitrite treatment exhibited a little higher mutagenicity and much stronger desmutagenicity than those of the original melanoidins. The change of the structure of melanoidins after treating with nitrite was also investigated by HPLC and CP-MAS NMR. 相似文献
108.
Akira Nakamura Matsuo Ono Hirozo Segawa Tetsuo Takematsu 《Bioscience, biotechnology, and biochemistry》2013,77(4):1009-1016
6-Phenyl- and 5-phenyl-2-pyrazinecarbonitriles with or without a propylamino group at the 3-, 5- or 6-position of the pyrazine ring were prepared together with some related compounds from the corresponding 2,3-pyrazinedicarbonitriles. Their herbicidal activities against barnyardgrass and broadleaf weeds were examined in pot tests. The 6-phenyl-2-pyrazinecarbonitriles were relatively potent compared with the 5-phenyl derivatives. Moreover, the presence of a propylamino group at the 5-position of the 6-phenyl-2-pyrazinecarbonitriles was closely related to an increase in activity. 相似文献
109.
β-Xylosidase was purified 662 fold from a culture filtrate by ammonium sulfate fractionation, gel filtration on Biogel P-100, DEAE-Sephadex chromatography, and gel filtration on Sephadex G-200. With isoelectric focusing, the purified β-xylosidase found to be homogeneous on SDS (sodium dodecyl sulfate) polyacrylamide gel electrophoresis. The molecular weight was estimated by gel filtration to be 240,000, and 116,000 by SDS polyacrylamide gel electrophoresis. The purified β-xylosidase had an isoelectric point at pH 3.25, and contained 4% carbohydrate residue. The optimum pH was found to be in the range of 4.5 ~ 5, and the optimum temperature was 55°C. The enzyme activity was inhibited by Hg2 +, SDS, and N-bromosuccinimide at a concentration of 1 × 10?3 m, and also p-chloromercuribenzoate at a concentration of 1 × 10?4m. The purified enzyme hydrolyzed phenyl β-d-xyloside (ko = 302.6 sec?1),β-nitrophenyl β-d-xyloside (ko = 438.9 sec?1), o-nitrophenyl β-d-xyloside (ko = 431.0 sec?1), p-chlorophenyl β-d-xyloside (ko = 207.9 sec?1), o-chlorophenyl β-d-xyloside (ko = 211.8 sec?1), β-methylphenyl β-d-xyloside ko = 96.5 sec?1), o-methylphenyl β-d-xyloside (ko = 83.1 sec?1), p-methoxyphenyl β-d-xyloside (ko = 99.3 sec?1), o-methoxyphenyl β-d-xyloside (ko= 100.0 sec?1), xylobiose (ko = 992A sec?1), xylotriose (ko = 1321.9 sec?1), xylotetraose (ko = 7S9.1 sec?1) and xylopentaose (ko = 508.0 sec?1). On enzymic hydrolysis of phenyl β-d-xyloside, the reaction product was found to be β-d-xylose with retention of the configuration. The purified β-xylosidase was practically free of a-xylosidase and β-glucosidase activities. 相似文献
110.
Akio Manabe Osamu Kirino Yuji Funaki Yoshio Hisada Hirotaka Takano Shizuya Tanaka 《Bioscience, biotechnology, and biochemistry》2013,77(12):3215-3217
The membrane lipids of six higher plants that differ in salt tolerance were analyzed and compared. The root lipids increased in a ratio of glycolipid/phospholipid with increasing salt- tolerance. A similar increase in the ratio was observed with increasing external salinity when halophytic orach and salt-sensitive cucumber were exposed to varying salinity, although the latter plant was limited to only a little increase. Measurements of ion-transport rates with artificial lipid membranes revealed that the root lipids from a salt-resistant plant formed a more permeable membrane than those from a salt-sensitive species. It was found that the membrane permeability was related to the glycolipid/phospholipid ratio in the membrane lipids, where the glycolipids were stimulative and the phospholipids were repressive for ion-flow. These different effects of the two lipid classes may be attributed to their molecular species and head groups. 相似文献