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1.
Kento Nishikibe Keisuke Nishikawa Momochika Kumagai Matsumi Doe Yoshiki Morimoto 《化学:亚洲杂志》2022,17(1):e202101137
There are marine cytotoxic bromotriterpenoids, named the thyrsiferol family that are structurally characterized by some tetrahydropyran (THP) and tetrahydrofuran (THF) rings. The thyrsiferol family belongs to natural products that are often difficult to determine their stereostructures even by the current, highly advanced spectroscopic methods, especially in acyclic systems including stereogenic tetrasubstituted carbon centers. In such cases, it is effective to predict and synthesize the possible stereostructures. Herein, to elucidate ambiguous stereostructures and unassigned absolute configurations of aplysiol B, laurenmariannol, and saiyacenol A, members of the thyrsiferol family, we carried out their asymmetric chemical syntheses featuring 6-exo and 5-exo oxacyclizations of epoxy alcohol precursors and 6-endo bromoetherification of a bishomoallylic alcohol. In this paper, we report total assignments of their stereostructures through their asymmetric chemical syntheses and also their preliminary cytotoxic activities against some tumor cells. These results could not have been achieved without depending on asymmetric total synthesis. 相似文献
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K Kawasaki T Tsuji K Hirase M Miyano Y Imoto M Iwamoto 《Chemical & pharmaceutical bulletin》1991,39(3):584-589
N-Terminal tripeptide analogs of fibrin alpha-chain were synthesized and their inhibitory effect on fibrinogen/thrombin clotting was examined. A new water-soluble active ester, 3-pyridinium ester, was used for the synthesis. Among the synthetic peptides, H-Gly-Pro-Arg-hexamethyleneimine exhibited the highest inhibitory effect on fibrinogen-thrombin clotting. 相似文献
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We studied the hydrolysis of a neuropeptide kyotorphin (L-Tyr-L-Arg) by an enkephalin-degrading aminopeptidase purified from cytosol of rat brain in vitro. The purified enzyme was homogeneous as judged by sodium dodecyl sulfate (SDS)-polyacrylamide gel electrophoresis (PAGE), gel filtration and isoelectric focusing. The aminopeptidase with an apparent molecular weight (Mr) = 98000 catalyzed the hydrolysis of Leu- and Met-enkephalins with Km values of 125 and 142 microM, respectively. The enzyme activity was inhibited by bestatin, amastatin and puromycin but not by pepstatin, leupeptin and phenylmethanesulfonyl fluoride (PMSF). Kyotorphin was degraded by the aminopeptidase at pH 7.0, and the Vmax and Km values were 9.2 mumol/min/mg protein and 95 microM, respectively. The Km value for kyotorphin was compatible to those for Leu- and Met-enkephalins. Taken together, these results suggest a possible involvement of the enkephalin-degrading aminopeptidase in cytosolic degradation of kyotorphin in neuronal cells of rat brain. 相似文献
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Toshiro Watanabe Tapan Kumar Mazumder Shiro Nagai Keisuke Tsuji Shigeru Terabe 《Analytical sciences》2003,19(1):159-161
A micellar electrokinetic chromatography (MEKC) method was developed for estimating the angiotensin-I converting enzyme (ACE) inhibitory activity by separating the hippuric acid liberated in the ACE reaction mixture in the presence of an inhibitor, captopril. The hippuric acid was successfully separated and detected by MEKC with a 25 mM sodium dodecyl sulfate solution in a 25 mM phosphate-50 mM borate buffer at pH 7.0; the total analysis took about 5 min. A good linear relationship was observed between the inhibitor and the peak area of hippuric acid release. No significant difference in the ACE inhibitory activity (IC50) of captopril (an antihypertensive medicine) or autolyzed-mushrooms (functional foods) was observed between the conventional method and the MEKC method. The MEKC method was found to be a useful technique for a rapid assay of the ACE inhibitory activity. 相似文献
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Kosuke Morita Kouji Morimoto Daiya Kaji Yu Liang Zhao Atsushi Yoshida Toshimi Suda Akira Yoneda Tetsuya Ohnishi Hiromitsu Haba Eiji Ideguchi Hu Shan Xu Tao Zheng Hisaaki Kudo Keisuke Sueki Kenji Katori Isao Tanihata 《Acta Physica Hungarica A》2004,19(1-2):53-60
A gas-filled type of recoil separator for heavy element research was installed at an experimental hall of RIKEN Linear Accelerator facility to realize getting higher intensity of primary beam and long beam time. Performance of the separator was studied using target recoils and various nuclear reactions. The results show the high performance of the separator for heave element research. As an application of the GARIS, production and identification of an isotope of the 110th element 271[110] have been performed using the 208Pb(64Ni,1n)271[110] reaction. Three decay chains coincide well both in decay times and energies with the ones reported by the group of SHIP experiment at GSI, Germany. Our results provide a confirmation of the synthesis of an isotope 271[110] of element 110. 相似文献
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Yasuo Kameda Motoya Sasaki Masahiro Yaegashi Kosuke Tsuji Shingo Oomori Shuji Hino Takeshi Usuki 《Journal of solution chemistry》2004,33(6-7):733-745
Time-of-Flight (TOF) neutron diffraction measurements have been carried out on aqueous 8 mol% sodium acetate solutions in D2O. Scattering cross sections that were observed for sample solutions involving 12C/13C and H/D isotopically substituted acetate ions were used to derive the first-order difference functions, ΔH(Q) and ΔC(Q), and corresponding distribution functions, G H(r;r) and G C(r;r), which describe the environmental structure around the methyl and the carboxyl groups within the acetate ion, respectively. Structural parameters concerning the first hydration shell of the carboxyl group within the acetate ion were obtained through the least squares fit to the observed intermolecular difference function, ΔC inter(Q). The nearest neighbor C O...D W1 (CO: carboxyl carbon atom, DW1: water deuterium atom) distance, r(C O...D W1 ), and the angle, ∠ C O ...D W1 -O W (O W : water oxygen atom), were determined to be 2.63(1) Å and 120(1)°, respectively. The coordination number, n(C O ...D W1 ), was obtained to be 4.0(1). These results are consistent with the hydration structure in which water molecules in the first hydration shell of the carboxyl group are hydrogen-bonded with oxygen atoms of the carboxyl group. 相似文献