巻号一覧
114 巻, 3 号
選択された号の論文の7件中1～7を表示しています
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森口 郁生1994 年 114 巻 3 号 p. 135-146
発行日: 1994/03/25
公開日: 2008/05/30
ジャーナル フリーRecent development of quantitative structure-activity relationships (QSARs) and computer-aided drug design contributed by the author and his coworkers was briefly reviewed. Fuzzy adaptive least-squares (FALS), a pattern recognition method for analysing structure-activity rating data to generate QSAR models was developed. A novel feature of FALS is that the degree to which each sample belongs to its activity class is given by a fuzzy membership function. Using FALS, non-congeneric QSAR analyses of carcinogenicity, mutagenicity, and six kinds of pharmacokinetic properties of miscellaneous organic chemicals were performed to construct predictive models for drug design. In these QSAR analyses, the values of log P (partition coefficient in octanol/water) calculated by the simple method of Moriguchi et al. were used as the descriptor for hydrophobicity. The method of Moriguchi et al. is not only simple and convenient but also reliable in the application to 22 drugs selected by Rekker et al. compared to the Rekker method and the Hansch-Leo method. Lastly, a heulistic search method for active conformers using molecular mechanical confor-mational analysis and principal component analysis was proposed.抄録全体を表示PDF形式でダウンロード (1134K) -
田坂 賢二1994 年 114 巻 3 号 p. 147-159
発行日: 1994/03/25
公開日: 2008/05/30
ジャーナル フリーHistamine release from mast cells is intimately related with degranulation. When basic histamine releasers such as compound 48/80 were applied extracellularly to isolated rat mast cells by means of microelectrophoresis, localized degranulation was evoked near the tip of micropipet in a few seconds. In response to the second electrophoretic application at the opposite side of the membrane of the same mast cells, similar local degranulation was induced. This fact clearly indicates that local degranulation does not damage mast cells to the extent of blocking following degranulation. As intracellular electrophoretic application of compound 48/80 caused a swelling of mast cell, although no degranulation was elicited. When antigen-antibody reaction was induced in a single rat mesentery mast cell by means of microelectrophoresis, the application of antigen was made extracellularly or intracellularly. At the site of extracellular application, localized degranulation and histamine release were evoked. Histamine release was evidenced by the disappearance of histamine fluorescence in the degranulated area. Neither degranulation nor histamine release was induced by intracellular application of antigen. In freeze-fracture electronmicroscopy of the resting rat mast cells, intra-membrane particles (IMPs) were randomly distributed on the plasma membrane. When sensitized cells were exposed to antigen, IMPs were markedly dispersed so as to surround bulging regions of the membrane elicited by swollen granules. As the particles gathered at the periphery of the bulges, actually no particle was seen on the protuberant region. When rat mast cells loaded with quin 2 were exposed compound 48/80 in a Ca-free medium, a marked increase of quin 2 fluorescence was noticed, indicating that Ca2+ was released from intracellular Ca store. The binding of 45Ca was at its peak in the fractions where the highest activity of glucose-6-phosphatase, a marker enzyme for the endoplasmic reticulum, when organelles of mast cells were fractionated. This may indicate that intracellular Ca store is endoplasmic reticulum. It has been shown that microfilaments, and microtubules play some important roles in histamine release from rat mast cells. When permeabilized mast cells were stimulated with Ca2+, a translocation of protein kinase C from cytosol to membrane fraction was observed. This leads to phosphorylation of vimentin, one of intermediate filaments. In membrane skeletons of rat mast cells, α-and β-fodrin, ankyrin and actin were found by means of western blotting analysis. It was supposed that membrane skeleton may be useful as a barrier between the plasma membrane and the granule membrane.抄録全体を表示PDF形式でダウンロード (2218K) -
金子 主税, 豊田 朱見, 千葉 淳1994 年 114 巻 3 号 p. 160-170
発行日: 1994/03/25
公開日: 2008/05/30
ジャーナル フリーSome recent topics concerning the addition of molecular fluorine to C=C bonds are discussed together with the mechanistic clarification of the syn-addition and the formation of the rearrangement products. The entire scheme for the addition reaction is the formation of a perpendicular π-complex at the initial stage, which leads to a tight ion pair as the transition state. The tight ion pair then either collapses directly to the syn-addition product, or affords indirectly the carbocation rearrangement product. It is postulated that the direct precursor of the rearrangement products is not a free carbocation but a loose ion pair which is formed from the tight ion pair.抄録全体を表示PDF形式でダウンロード (912K) -
北村 龍一, 佐藤 俊幸, 前田 昌子, 辻 章夫1994 年 114 巻 3 号 p. 171-175
発行日: 1994/03/25
公開日: 2008/05/30
ジャーナル フリーAn enzyme immunoassay for the determination of potassium oxonate in the plasma has been developed. The procedure is based on a competitive enzyme-linked immunosorbent assay using the second antibody solid phase method. The antiserum for potassium oxonate was prepared using oxonic acid 6-carboxypentylamide-BSA conjugate as immunogen. The specific antibody for oxonic acid was isolated from the antiserum using oxonic acid 6-carboxypentylamide immobilized immunosorbent gel. The purified antibody resulted in high sensitivity and low cross-reactivity as compared with the unpurified antiserum. Potassium oxonate in the plasma could be assayed in the range from 20 to 1000 ng/mI by the proposed EIA. The recovery was ranged from 82 to 117% and the coefficient of variation was from 6.6 to 14.7% (n=6).抄録全体を表示PDF形式でダウンロード (593K) -
吉川 雅之, 茶谷 展安, 原田 英美子, 西野 由貴江, 山原 條二, 村上 啓寿1994 年 114 巻 3 号 p. 176-181
発行日: 1994/03/25
公開日: 2008/05/30
ジャーナル フリーIn order to characterize the chemical change of the constituents during the processing of Hydrangeae Dulcis Folium, quantitative analyses of phyllodulcin, hydrangenol, and their 8-O-glucosides were developed by means of high performance liquid chromatography. As an application of this HPLC method, the distribution of those dihydroisocoumarins in different parts of Hydrangea macrophylla var. thunbergii was investigated. It was found that these dihydroisocoumarins were contained at the highest concentration in the leaves. Furthermore, the seasonal fluctuation of these compounds in the leaves, together with the height of the plant and total dry weight of the leaves, were clarified and so that, the suitable period for the harvest of Hydrangea macrophylla var. thunbergii was deduced to be from Oct. to Nov.抄録全体を表示PDF形式でダウンロード (658K) -
呉 立軍, 孫 苓苓, 李 麦香, 楊 〓, 江 沢榮, 呂 揚, 田 之悦, 鄭 啓泰, 宮瀬 敏男, 上野 明1994 年 114 巻 3 号 p. 182-185
発行日: 1994/03/25
公開日: 2008/05/30
ジャーナル フリーA new tricyclic sesquiterpene, named calamenone (1), and two known sesquiterpenes, calamendiol (2) and isocalamendiol (3), were isolated from the roots of Acorus calamus L. The structure of the new compound was elucidated on the basis of spectral and X-ray diffraction data.抄録全体を表示PDF形式でダウンロード (450K) -
宮一 諭起範, 瀬木 幾, 富森 毅1994 年 114 巻 3 号 p. 186-199
発行日: 1994/03/25
公開日: 2008/05/30
ジャーナル フリーFrom the leaves of Phellodendron japonicum MAXIM. (Rutaceae), six new flavonoid glycosides (I-VI) were isolated, together with eight known compounds. The structures of I-VI were shown to be 8-prenyl-3, 4', 5-trihydroxy-flavone 7-O-β-D-(6-O-malonyl) glucopyranoside, (2R, 3R)-8-prenyl-3, 4', 5-trihydroxyflavanone 7-O-β-D-(6-O-malonyl) glucopyranoside, 8-[(S)-2, 3-dihydroxy-3-methylbutyl]-3, 4', 5-trihydroxyflavone 7-O-β-D-glucopyranoside, 8-[(R)-2, 3-dihydroxy-3-methylbutyl]-3, 4', 5-trihydroxyflavone 7-O-β-D-glucopyranoside, (2R, 3R)-8-[(S)-2, 3-dihydroxy-3-methylbutyl]-3, 4', 5-trihydroxyflavanone 7-O-β-D-glucopyranoside and (2R, 3R)-8-[(R)-2, 3-dihydroxy-3-methylbutyl]-3, 4', 5-trihydroxyflavanone 7-O-β-D-glucopyranoside, respectively, on the basis of the chemical and spectral data.抄録全体を表示PDF形式でダウンロード (1311K)
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