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排序方式: 共有57条查询结果,搜索用时 15 毫秒
1.
N Kubodera H Watanabe T Kawanishi M Matsumoto 《Chemical & pharmaceutical bulletin》1992,40(6):1494-1499
Six analogues of 1 alpha,25-dihydroxy-22-oxavitamin D3 (OCT) (2), 26,27-dimethyl OCT (5), 26,27-diethyl OCT (6), 24-norOCT (7), 24-homoOCT (8), 24-dihomoOCT (9), and 24-trihomoOCT (10) were synthesized from the 20(S)-alcohol (11) as the common starting material. In the activity inducing differentiation of human myeloid leukemia cells (HL-60) into macrophages, 26,27-dimethyl OCT (5) and 24-homoOCT (8) showed the highest activities. The binding properties of these analogues to the chick embryonic intestinal 1 alpha,25-dihydroxyvitamin D3 (1) receptor are also described. 相似文献
2.
The pharmacokinetic study of 67Ga-citrate (67Ga) following intravenous (i.v.), subcutaneous (s.c.) and intraperitoneal (i.p.) injection was performed in anesthetized rats using the repeated blood sampling method by cannulation technique into the external jugular vein. The disappearance of 67Ga from the blood following i.v. and s.c. injection was best fit a three-exponential equation. There was no significant difference between the areas under the curves following i.v. and s.c. injection of 67Ga. In the case of i.p. injection, the disappearance of 67Ga from the blood was described by a two-exponential equation. However, the maximum blood radioactivity was very low, and the disappearance rate of 67Ga from the blood was extremely slow compared to the other routes of injection. The conclusion from these results was that s.c. injection was as suitable as i.v. injection, but i.p. injection was not appropriate for the distribution study of 67Ga such as scintigraphy or autoradiography. However, i.p. route may be available for a special experiment which needs the long-time retention of 67Ga in the blood. 相似文献
3.
Okano T Nakagawa K Kubodera N Ozono K Isaka A Osawa A Terada M Mikami K 《Chemistry & biology》2000,7(3):173-184
BACKGROUND: 1alpha,25-Dihydroxyvitamin D(3) (1alpha,25(OH)(2)D(3)) has been shown to modulate not only proliferation and differentiation, but also apoptosis in malignant cells, indicating that it could be useful for treating cancer. Little information is available concerning the structural motifs of the 1alpha, 25(OH)(2)D(3) molecule responsible for modulation of differentiation and apoptosis, however. We set out to synthesize singly dehydroxylated A-ring analogs of 19-nor-1alpha,25(OH)(2)D(3) in a catalytic asymmetric fashion, and to investigate their biological activities in leukemia HL-60 cells. RESULTS: A series of singly dehydroxylated 19-nor-1alpha,25-dihydroxyvitamin D(3) A-ring analogs were synthesized using a combinatiorial sequence of regioselective propiolate-ene reaction and catalytic asymmetric carbonyl-ene cyclization. Surprisingly, the analogs could be clearly divided into two categories; one group, bearing 1alpha-hydroxy or 3beta-hydroxy groups in the A-ring, were potent differentiators and the second group, bearing 1beta-hydroxy or 3alpha-hydroxy groups, were potent stimulators of apoptosis. CONCLUSIONS: We have clearly identified the structural motifs of 19-nor-1alpha,25(OH)(2)D(3) analogs responsible for differentiation and apoptosis in HL-60 cells. These findings will provide useful information not only for development of therapeutic agents for treatment of leukemia and other cancers, but also for structure-function studies of 1alpha,25(OH)(2)D(3). 相似文献
4.
N Kubodera K Miyamoto M Akiyama M Matsumoto T Mori 《Chemical & pharmaceutical bulletin》1991,39(12):3221-3224
Three vitamin D3 analogues, 1 alpha,25-dihydroxy-23-oxavitamin D3 (3), 1 alpha,25-dihydroxy-23-thiavitamin D3 (4) and 1 alpha,25-dihydroxy-23-azavitamin D3 (5) were synthesized. In the differentiation-inducing activity of human myeloid leukemia cells into macrophages in vitro, the 23-aza analogue (5) showed the least activity, while no remarkable differences were observed between the 23-oxa analogue (3) and the 23-thia analogue (4), which were less active than 1 alpha,25-dihydroxyvitamin D3 (1). 相似文献
5.
6.
S. Nasu T. Sato S. X. Nakamura K. Sumiyoshi F. Myhrer K. Kubodera 《Few-Body Systems》2013,54(7-10):1595-1598
We have investigated the neutrino reactions via deuteron in the surface region of the supernova core. We evaluate the electron capture on deuterons and the neutrino emission from nucleon-nucleon scattering through the deuteron formation and found an important role of neutrino reactions with deuteron. 相似文献
7.
Higashiguchi T. Hirata T. Koga M. Rajyaguru C. Sasaki W. Kubodera S. 《Applied physics. B, Lasers and optics》2004,79(5):587-590
We investigated characteristics of the soft X-ray emission in the wavelength range of 6–16 nm using various rare-gas cryogenic solid targets irradiated with a nanosecond laser pulse. Suprathermal ions having a maximum velocity of the order of 107 cm/s were detected for three rare-gas targets (Ar, Kr, and Xe). The spatial distributions of the soft X-rays and the suprathermal ions were measured for Xe cryogenic solid targets and found to vary as cos2 and cos5, respectively, where is the angle to the target normal. By integrating the observed cos2 spatial distribution, the conversion efficiency of the soft X-ray emission in the wavelength range from 6 to 16 nm was evaluated to be 0.2%/pulse. PACS 52.38.ph; 52.50.Jm 相似文献
8.
We observed a small-signal gain of Ar2* emission at 126 nm by use of a hollow fiber to guide the high-intensity laser propagation in high-pressure Ar. The small-signal gain coefficient was measured to be 0.05 cm(-1) at 126 nm. Kinetic analysis revealed that the electrons produced by the high-intensity laser through an optical-field-induced ionization process initiated the Ar2* production processes. The increase in the emission intensity was measured to be exp(2.5), with an increase in the fiber length. 相似文献
9.
10.
Optical third-harmonic generation from some high-index glasses was investigated. The highest χ(3) was obtained from As2S3 glass 2.2 × 10−12 esu/ This value was 100 times higher than that of pure SiO2 glass and comparable with that of the polymer with monomer-doping, which are known as organic materials with quite high χ(3). From the relationship between χ(3) and composition, sulfide glasses were found to have higher χ(3) than oxide or semiconductor-doped oxide glasses with similar refractive indices. 相似文献