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半田 哲郎, 小松 裕明, 掛江 敦之, 宮嶋 孝一郎
1990 年 38 巻 8 号 p.
2079-2082
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Cosonication of egg yolk lecithin and triolein with apolipoproteins isolated from pig high density lipoprotein (apoHDL) gave us reconstituted high density lipoprotein particles (r-HDLs) of 9 nm in average diameter. They were smaller than microemulsion particles (MEs) composed of the lipids (35 nm). The protein/ egg yolk lecithin ratio in the fractionated r-HDLs was higher in the smaller particles. Binding of a hydrophobic probe, 2-p-toluidinylnaphthalene-6-sulfonate (TNS), to MEs, r-HDLs and apoHDL were evaluated on the basis of Halfman and Nishida's method. The reconstitution of apoHDL into MEs led to a 68% reduction in the binding of TNS and a small increase in the α-helix content as compared with free apoHDL. The binding experiments also showed the condensation of lecithin molecules at the r-HDL surface. The amphipathic helixes of apoHDL are located in the surface monolayer of egg yolk lecithin surrounding the triolein core. The intercalation of the hydrophobic residues of apoHDL between egg yolk lecithin molecules brings about a pronounced curvature of the surface and a decrease in the particle diametri.
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鈴木 和夫, 小林 理香, 古畑 公夫, 小倉 治夫
1990 年 38 巻 8 号 p.
2083-2087
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
6-O-(5-Acetamido-3, 5-dideoxy-D-glycero-α- and -β-D-galacto-nonulopyranosylonic acid)-(2→6)-O-β-D-galacto-pyranosyl-(1→4)-1-(5-cholesten-3β-yloxy)-β-D-glucopyranose was synthesized under various conditions through a Koenigs-Knorr-like reaction. The stereochemistry of the products was confirmed by analysis of the nuclear magnetic resonance and circular dichroism spectra.
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川村 清, 大田 富夫, 大谷 元治
1990 年 38 巻 8 号 p.
2088-2091
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Treatment of 2-(2, 3-epoxy)propylphenyl acetate derivatives with catalytic amounts of NaI in organic solvent gave directly the corresponding 3-chromanyl acetate derivatives in good yields (86.6-98.0%). Similar treatment of 2-(2, 3-epoxy)propyl-6-methoxyphenyl N-mesyl-L-phenylalanylate gave a diastereomeric mixture of 8-methoxy-3-chromanyl N-mesyl-L-phenylalanylate, which was fractionated into both diatereomers by silica gel column chromatography. Subsequent hydrolysis of these isomers afforded the enantiomers of 8-methoxy-3-chromanol.
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川村 清, 大田 富夫, 大谷 元治
1990 年 38 巻 8 号 p.
2092-2096
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
An efficient synthesis of all four optical isomers of nipradilol has been achieved. Thus, 8-methoxy-3-chromanone was reduced enantioselectively with baker's yeast to afford (3R)-8-methoxy-3-chromanol, which, after derivation to (3R)-8-acyloxy-3-chromanol, was led to (3S)- or (3R)-8-hydroxy-3-chromanyl nitrate (7 or 9) by selecting a reaction with retention (using acetyl nitrate) or inversion (using Bu
4N
+NO
3-) of configuration. Futher, (3S)- and (3R)-8-methoxy-3-chromanol, prepared via chemical resolution of 8-methoxy-3-chromanyl N-mesyl-L-phenylalanylate, were also led to 7 or 9 in the same manner. Using 7 and 9, four optically active glycidyl ether derivatives (11-14) were synthesized by using a novel Me
4N
+Cl
--catalyzed etherification reaction of phenol with (S)- and (R)-epichlorohydrin. Subsequent amination of 11-14 with isopropylamine afforded the four optical isomers of nipradilol.
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野瀬 敦子, 工藤 忠宏
1990 年 38 巻 8 号 p.
2097-2101
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
The reduction of a variety of functional groups with the nickel(II) chloride-zinc system was investigated. This system reduced aldehydes, ketones, olefins, nitriles, oxime, nitro and heterocyclic compounds under mild conditions in good yields. It is of interest that some cases of reduction of ketones afforded the corresponding olefins and the saturated products, and the reduction of nitriles afforded the corresponding primary alcohols with the primary and secondary amines. The selective reduction of olefin and nitro functionalities in some compounds bearing carbonyl, ester and carboxyl functionalities was observed with this system.
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井藤 千裕, 水野 豊子, 棚橋 志穂, 古川 宏, 十一 元晴, 井上 真美, 邑口 美樹, 大村 三男, / , Andrew T. M ...
1990 年 38 巻 8 号 p.
2102-2107
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Bisosthenon (1), a new dimeric coumarin, was isolated from the roots of some Citrus plants (Rutaceae), and the structure was elucidated to be 1, correspoding to a head-to-head dimer of osthenon (4), which was previously obtained from Citrus plants. The photodimerization of 4 gave 1 as well as two other dimeric products, 2 and 3.
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伊藤 喬, 岡田 真弥子, 永田 和弘, 山口 健太郎, 大沢 昭緒
1990 年 38 巻 8 号 p.
2108-2111
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Monocyclic 1, 2, 3-triazines reacted with electron rich dienophiles to give pyridines and pyridazines. 4, 6-Disubstituted 1, 2, 3-triazine was denitrogenated to the azete intermediate, which afforded isomeric pyridines. 2, 5-Dihydrotriazines were oxidized by m-chloroperbenzoic acid to give 1, 2, 3-triazoles. Ring transformations of other triazine derivatives are also reported.
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西山 泰弘, 中山 茂, 岡田 芳男, 閔 庚善, 小野坂 敏見, 田中 慶一
1990 年 38 巻 8 号 p.
2112-2117
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
A pentacosapeptide corresponding to the entire amino acid sequence of Agaricus bisporus metallothionein (MT) and related cysteine-containing peptides were prepared by the conventional solution method and their heavy metal-binding properties were examined. The Cu
2+- or Cu
+-binding activities of various peptides were not greatly dependent on the peptide structure, so far as examined, although the pentacosapeptide, A. bisporus MT, exhibited slightly higher binding activity than the other peptides. On the contrary, the Cd
2+-binding activities of these peptides were fairly structure-dependent.
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石井 永, 杉浦(旧姓萩原) 孝夫, 秋山(旧姓近藤) 洋子, 市川 佳重, 渡辺 敏子, 村上 泰興
1990 年 38 巻 8 号 p.
2118-2126
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
In order to clarify the mechanism of the abnormal Fischer indolization of 2-methoxyphenylhydrazones the Fischer indolization of ethly pyruvate 2-(2, 6-dimethoxyphenyl)phenylhydrazone (6) was undertaken using ethanolic hydrogen chloride and zinc chloride as an acid catalyst. The cyclization was found to take place predominantly on the 2, 6-dimethoxyphenyl nucleus to give the corresponding indoles, although the yields of indoles formed were low. Some non-indolic by-products were also produced which might give information about the mechanism of Fischer indolization. In particular, the formation of 3, 5-dimethoxy-4-anilinobenzaldehyde (15) suggests that the first cyclization step in Fischer indolization could take place at the para position of phenylhydrazone as a side reaction.
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阿部 フミ子, 長尾 常敦, 岡部 光, 山内 辰郎, 丸林 信洋, 上田 幾彦
1990 年 38 巻 8 号 p.
2127-2129
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Parsonsianine, a 14-membered macrocyclic pyrrolizidine alkaloid, composed of retronecine, (2S, 3R)-2, 3-dihydroxy-2-ethylbutanoic acid and (2R, 3S)-2, 3-dihydroxy-2-isopropylbutanedioic acid, was isolated from the leaves of Parsonsia laevigata and the structure was determined by means of nuclear magnetic resonance and X-ray analysis.
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釜谷 ルミ子, 田中 順子, 檜山 理恵, 上田 博之
1990 年 38 巻 8 号 p.
2130-2132
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Eight triterpenoid hydrocarbons were characterized from the fresh leaves of Cheiropleuria bicuspis. They consist of hop-22(29)-ene, neohop-13(18)-ene, fern-7-ene, (18R)-dammara-13(17), 21-diene, eupha-7, 21-diene, 13α(H)-malabaricatriene, γ-polypodatetraene and squalene, all of which have different carbon skeletons, A new triterpenoid alcohol was isolated and established as 1α, 11α, 30-trihydroxyhopane. We also detected friedelin, hydroxyhopane, dryocrassol, lupeol, fernenol, 1α, 11α, 22-trihydroxyhopane, a mixture of sterols and a mixture of fatty acid esters of cycloartanoids, methylsterols and sterols. These findings suggest that Cheiropleuria bicuspis is related to Microsorium (Polypodiaceae), but are nevertheless consistent with the independency of Cheiropleuriaceae.
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富岡 清, 親見 裕一, 椎名 邦彦, 中島 誠, 古賀 憲司
1990 年 38 巻 8 号 p.
2133-2135
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Enantioselective dihydroxylation of E-stilbene afforded (1S, 2S)-1, 2-diphenyl-1, 2-ethanediol in 70% ee by employing a stoichiometric amount of osmium tetroxide-chiral amine 5, prepared from N-methylephedrine and 2-bromopyridine.
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津田 喜典, 酒井 由紀, 中井 章, 大島 武, 細井 深造, 礒部 公明, 佐野 武弘
1990 年 38 巻 8 号 p.
2136-2142
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Several 2, 8-dioxo-1, 7-cycloerythrinan drivatives (bearing a 6β-ethoxycarbonyl or 6β-hydrogen substituent) were prepared in good yields from the reported 2, 8-dioxo-7β or 7α-hydroxyerythrinan derivatives by a base-catalyzed intramolecular alkylation of the corresponding O-mesylates, and they were shown to be useful intermediates for synthesizing natural erythrinan alkaloids. The C-1 of these compounds has been suitably protected for further manipulation at C-3 and the cyclopropane ring can be readily cleaved in a reductive or a non-reductive manner to give C-1 methylene or C-1 olefin derivatives. The latter process is discussed in detail with reference to several examples of ionic and radical opening. The reactivity of the carboxylate ester group on the cyclopropane ring bearing an electro-negative substituent was unusually high.
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阿部 フミ子, 山内 辰郎
1990 年 38 巻 8 号 p.
2143-2145
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Three new tetrahydrofuranoid-lignan glycosides, tanegosides A, B and C, were isolated from Trachelospermum liukiuense HATSUSIMA, along with 8 lignan glycosides already known in T. asiaticum, and the structures were elucidated by spectral and chemical methods.
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藤井 澄三, 斎藤 徹, 森 繁治
1990 年 38 巻 8 号 p.
2146-2150
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
The first total synthesis of the 8-oxopurine 8, a constituent of the marine sponge Hymeniacidon sanguinea GRANT, has been achieved via two alternative routes starting from 8-bromo-9-methyladenine (11), which is obtainable from 9-methyladenine (10) by bromination. The first route includes methylation of 11 with MeI to give the 1-methylated product 13·HI, conversion of 13·HI into the free base 13, and treatment of 13 with NaOAc in boiling AcOH to produce 8 in 25% overall yield (from 10). The second route includes treatment of 11 with boiling 1 N aqueous NaOH and methylation of the resulting 8-oxo derivative 12 with MeI, affording 8 in 63% overall yield (from 10). The rearranged isomer 15 and the N
6 -acetyl derivative 9 have also been synthesized.
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野中 源一郎, 酒井 孝, 田中 隆, 三橋 國英, 西岡 五夫
1990 年 38 巻 8 号 p.
2151-2156
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
The structures of the C-glycosidic ellagitannins, castalagin, vescalagin, casuarinin and stachyurin, have been revised to 1-4 respectively, on the basis of two-dimensional nuclear Overhauser effect (NOE) spectroscopy and NOE difference spectroscopy. Furthermore, the structures of some related C-glycosidic tannins were re-examined by using similar techniques, and it was concluded that the configuration at the glucose C-1 position in all hitherto known C-glycosidic tannins must be revised.
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佐野 武弘, 堀口 よし江, 神戸 末孝, 津田 喜典
1990 年 38 巻 8 号 p.
2157-2161
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Photocycloaddition of 5-aryl-4-ethoxycarbonyl-1H-pyrrole-2, 3-dione 1 with isoprene and thermolysis of the resulting exo-vinyl cyclobutanes 6 caused a ring enlargement reaction due to a 1, 3-shift, giving rise to the hydroindoles 9, which were found to be regioisomeric to the hydroindoles 14 obtained as a major cycloadduct by the Diels-Alder reaction of the same addends. Thus, the two-step hydroindole synthesis, i.e., dioxopyrroline-diene photoannulation and thermolysis of the resulting vinyl cyclobutane, has a synthetic value in giving the product with the reverse regiochemistry to that of the Diels-Alder adduct.
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林 哲輝, 田中 隆, 野中 源一郎, 西岡 五夫, 陳 益昇
1990 年 38 巻 8 号 p.
2162-2171
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Together with ten hydolyzable tannins and related compounds (1-10), three novel dimeric ellagitannins, excoecarianin (11), and excoecarinins A (13) and B (16), possessing a dehydrohexahydroxydiphenoyl or an elaeocarpusinoyl group, have been isolated from the leaves of Excoecaria kawakamii HAYATA (Euphorbiaceae). The structures of these tannins were established on the basis of spectroscopic and chemical evidence.
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Jean-Francois LAGORCE, Anne-Catherine JAMBUT-ABSIL, Jacques BUXERAUD, ...
1990 年 38 巻 8 号 p.
2172-2174
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
It has been demonstrated spectroscopically that many nitrogen-containing heterocyclic compounds can from charge transfer complexes with iodine. The complexes of morpholine with iodine were shown to be of the n-σ type with a 1 : 1 stoichiometry. A strong donor-acceptor interaction was found (K
c=1261±12 mol
-1 at 20°C in CCl
4), considerably higher than those of complexes of anomatic compounds with iodine. The high value of the formation constant for this complex indicated that morpholine could serve as a starting point for the synthesis of novel anti-thyroid drugs.
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安藤 章, 品田 哲郎, 木下 進司, 有村 典子, 小山 まゆみ, 永井 隆文, 三木 卓一, 熊懐 稜丸, 佐藤 治男
1990 年 38 巻 8 号 p.
2175-2178
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
With the aim of obtaining a porphyrin derivative useful for diagnosis and therapy of cancer, fluorine analogues of protoporphyrin, in which the vinyl group(s) were replaced by difluorovinyl group(s), were synthesized by the reaction of the formylporphyrins with sodium chlorodifluoroacetate in the presence of triphenylphosphine. Some improvements in the reported procedures for the synthesis of formylporphyrins are also described. Preliminary results of biological tests of the products showed that 8
2, 8
2-difluoroprotoporphyrin accumulates to gastric cancer more selectively than other fluorine analogues and that 3
2, 3
2, 8
2, 8
2-tetrafluoroprotoporphyrin is taken up by rat hepatoma cells more readily than the others.
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野本 裕二, 小場瀬 宏之, 高井 春樹, 寺西 正行, 中村 譲治, 久保 和博
1990 年 38 巻 8 号 p.
2179-2183
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
A series of phthalazine and 1, 2, 3-benzotriazine derivatives which have heterocyclylpiperidino groups was synthesized and tested for cardiotonic activity in anesthetized dogs. Several 6, 7-dimethoxyphthalazine derivatives showed relatively potent cardiotonic activity comparable to that of amrinone.
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劉 謙, 広野 修一, 森口 郁生
1990 年 38 巻 8 号 p.
2184-2189
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Using the discriminant analysis method, we completely distinguished 24 calmodulin inhibitors in three groups, as classified by Zimmer et al. The resultant discriminant functions distinguished the three groups in terms of positive potential surface area on the side chain, as well as the total and neutral surface areas on the ring in the inhibitor molecules.Group assignment of additional calmodulin inhibitors from other sources was then estimated according to the discriminant functions. The relationship between structure and inhibitory potency on calmodulin-activated phosphodiesterase for group I inhibitors, together with those estimated, was studied using the adaptive least squares method with several parameters dependent on molecular conformations. A "best conformer" was selected for each inhibitor on the basis of quantitative structure-activity relationship (QSAR). The results of QSAR analysis of group I inhibitors showed that bydrophobicity was important for the ring moiety but not for the side chain. The negative potential surface area of the side chain is necessary for activity. It is desirable for the nitrogen atom in the side chain, which is considered the center of the negative potential area, to be located far from the ring moiety. Thus, the ring moiety and side chain may possibly play different roles in interactions with the receptor system.
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西村 由郎, 広瀬 徹, 岡田 秀継, 柴森 厚一郎, 中野 純次, 松本 純一
1990 年 38 巻 8 号 p.
2190-2196
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
A series of C-7 thio-substituted 1-cyclopropyl-1, 4-dihydro-4-oxoquinoline-3-carboxylic acids were prepared and tested for their antibacterial activity. Structure-activity relationships associated with the C-5 and C-7 substituents were discussed. Among the C-7 substituents including alkylthio, arylthio, heteroarylthio, and cyclic aminothio groups, a 2-aminoethylthio group was the best for enhancing in vitro antibacterial activity. The C-5 variants increased activity in the order OH<F<H<NH
2. Of compounds prepared in this work, 5-amino-7-(2-aminoethyl)thio-1-cyclopropyl-6, 8-difluoro-1, 4-dihydro-4-oxo-quinoline-3-carboxylic acid (18) was the most active.
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藤田 浩毅, 佐々木 有亮, 河野 弘之, 大久保 恭仁, 安保 明博, 鈴木 謙次, 日野 正孝
1990 年 38 巻 8 号 p.
2197-2200
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Nine analogs based on a structure of Tyr-D-Arg-Phe-X (X=alkylamides or alkylhydrazide containing electoron-withdrawing atoms or groups) were newly synthesized and their biological properties were examined by the opioid receptor binding properties of μ-, δ- and κ-receptors, guinea-pig ileum (GPI) assay and analgesic activity in the tail pinch test after subcutaneous administration in mice. Analogs with X=NHCH
2CF
3, Sar-ol, or NH(CH
2)
2CN showed potent activities in the GPI and analgesic assays and high affinity for μ-receptor. An analog with X=taurinamide was found to possess 4-fold higher μ-receptor selectivity than that of [D-Ala
2, MePhe
4, Gly-ol
5]enkephalin (DAGO). The receptor binding properties of previously reported analogs [Chem. Pharm. Bull., 33, 1528 (1985); ibid., 33, 4865 (1985); ibid., 36, 4834 (1988)] were also examined for overall discussion of the structure-activity relationships of this series of tripeptide amides.
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伊藤(旧姓染谷) まゆみ, 志村 洋史, 渡辺 修治, 玉井 正晴, 花田 和紀, 高橋 晶子, 田中 善孝, 新井 巌, 張 佩玲, 〓 ...
1990 年 38 巻 8 号 p.
2201-2203
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Successive purification of the extract from Canarium album and Euphorbia nematocypha, guided by antihepatotoxic activity in primary cultured rat hepatocytes, led to the isolation of brevifolin (1), hyperin (2), ellagic acid (3) and 3, 3'-di-O-methylellagic acid (4) as hepatoprotective compounds. Compounds 1, 3 and 4 also reduced carbon tetrachloride (CCl
4)-induced liver damage in mice. The hapatoprotective activities of 1, 2, 3 and 4 in vitro and in vivo are apparently due to their antioxidative effects, which were exhibited by further studies using 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radicals and CCl
4-induced lipid peroxidation systems.
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三野 芳紀, 宇佐美 秀子, 太田 長世, 武田 美雄, 市原 照由, 藤多 哲朗
1990 年 38 巻 8 号 p.
2204-2207
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Inorganic constituents of the leaves of several kinds of plants growing on different soil types were investigated using energy-dispersive X-ray fluorescence spectrometry.The results can be summarized as follows : (1) Each plant exhibited a characteristic metals profile, even if they were grown on similar soil types. (2) As we would expect, the metals profile of the plant leaves depends on the inorganic constitution of the soil on which it is grown. However, the degree of the influence of the soil types on the metals profile of the plant differs according to the kind of inorganic element; Ca and Cu are almost indepenent of the soil types, but the Ti and Fe content is dependent upon the soil types. (3) Sr content of plant leaves is closely related to the ratio of Sr to Ca of the soil on which the plants are grown. (4) This information should be helpful in identifying the producing district or original plant of a crude drug by its metals profile.
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三野 芳紀, 太田 長世
1990 年 38 巻 8 号 p.
2208-2211
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Energy-dispersive X-ray fluorescence spectrometry following sample decomposition and preconcentration was developed to determine selenium in crude drugs. Samples were decomposed with conc. HNO
3 and conc. H
2SO
4 in a flask with a reflux condenser. Evaporation of HNO
3 had to be avoided to prevent serious loss of this element. Selenium was preconcentrated from the digestion liquid by two-step reduction with 4 M HCl and ascorbic acid, the elemental selenium formed was adsorbed on activated carbon and then collected on a Nuclepore membrane filter for direct irradiation in an X-ray spectrometer.This analytical method (detection limit, 0.03 ppm) was used to determine selenium in many kinds of crude drugs. The analytical results indicated vegetable drugs to be low in selenium content : more than 0.5 ppm in only a limited number of samples and less than detection (0.03 ppm) in nearly all the samples. Animal drugs contain selenium at higher levels, Lumbricus and Cantharis being 7.46 and 1.67 ppm, respectively.
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芳野 恭士, 佐野 満昭, 藤田 雅弘, 富田 勲
1990 年 38 巻 8 号 p.
2212-2215
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
The effects of vitamin E (E) deficiency on the formation of aliphatic aldehydes in rat plasma and liver were studied. Three-week-old Wistar male rats were fed either an E supplemented diet (2-ambo-α-tocopheryl acetate 20 mg/kg diet, designated as E supplemented diet group) or an E deficient diet (E deficient diet group). After 8 weeks, n-hexanal and (E)-4-hydroxy-2-nonenal (4-HN) in the plasma of the E deficient diet group were found to be 2.0 and 2.5-fold greater than those of the E supplemented diet group, respectively. The contents of aldehydes such as n-pentanal, n-hexanal, 4-HN in the liver were also significantly higher in the E deficient diet group than in the E supplemented diet group. These results indicate that some aldehydes, arising possible from lipid peroxides, are produced and detected in the plasma and liver of rats under the condition like E deficiency.In this study we further found that the activity of the liver aldehyde dehydrogenase (ALDH, EC 1.2.1.3) was significantly changed; 5 and 8 weeks after the start it was lower in the E deficient diet group when compared to that in the E supplemented diet group. The decrease of enzyme activity was related to the increase of aldehydes such as n-hexanal in the liver.The aldehyde increase in the plasma of the E deficient diet group was thought to raise the injury of cells, namely, a strong hemolysis on erythrocytes prepared from the blood of rats fed the E deficient diet.
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森 聖一, 山口 正義
1990 年 38 巻 8 号 p.
2216-2218
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
The effect of regucalcin, a calcium-binding protein isolated from rat liver cytosol, on cytosolic Ca
2+/calmodulin-dependent protein kinase activity was investigated. The increase in cytosolic Ca
2+/calmodulin-dependent protein kinase activity with passage of incubation time was clearly prevented by the presence of regucalcin (1.0 μM). An appreciable effect of regucalcin was seen at 0.5 μM. The cytosolic Ca
2+/calmodulin-dependent protein kinase activity was fairly increased by increasing concentrations of added Ca
2+ (0.25-1.0 mM). This increase was clearly blocked by the presence of regucalcin (1.0 μM). The inhibitory effect of regucalcin on the protein kinase activity was also seen with varying concentrations of calmodulin (2.5-15 μg). In the presence of regucalcin (1.0 μM), trifluoperazin (50 μM), an antagonist of calmodulin, significantly decreased the cytosolic Ca
2+/calmodulin-dependent protein kinase activity. These results suggest that regucalcin can regulate the Ca
2+-calmodulin effect in liver cytosol.
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篠原 久実, 大野 尚仁, 宿前 利郎
1990 年 38 巻 8 号 p.
2219-2223
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
We have demonstrated that hot water extracts of sclerotia of Sclerotinia sclerotiorum IFO 9395 (TSHW) show various immunomodulating activities and mitogenic substance(s) were recovered from the β-1, 3-glucanase resistant-fraction (EDF) (Shinohara et al. Chem. Pharm. Bull., 37, 2174 (1989)). In this paper, we examined whether or not the mitogenic substance(s) were also obtained from the other methods, phosphate buffer extraction. Although the native extracts (3S-M) sterilized with a membranse filter showed a slight mitogenicity to murine splenocytes, 3S-M denatured in boiling water (3S-MB) showed significant activity. Treatment of 3S-M for only 1 min in boiling water or 10 min at 70 °C was sufficient to show significant mitogenic activity. After heat treatment of 3S-M in boiling water for 30 s, the main band corresponding to that of 3S-M was not clearly observed. Instead, new bands appeared at the top of the gel in normal-polyacrylamide gel electrophoresis (normal-PAGE), suggesting that many physicochemical changes occurred during that heat treatment. These findings suggest that heat denaturation of substance(s) from sclerotia was one of the triggering mechanisms expressing mitogenic activity to murine splenocytes.
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水田 博彰, 川添 康, 芳賀 慶一郎, 小川 建志
1990 年 38 巻 8 号 p.
2224-2227
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Effects of the amount and the composition of meals on gastric emptying and small intestinal transit times of a suspension were investigated in beagle dogs using acetaminophen and salicylazosulfapyridine as markers.Gastric emptying time was affected both by the amount and the composition of a meal; it was prolonged proportionally to the amount of a solid meal and varied among the 3 kinds of test meals of the same energy content in the following rank order : land>skimmed milk>mashed potatoes.The inter-individual variation of small intestinal transit time in a fed state was smaller than that in a fasted state, whereas the mean transit times in both states were similar. Small intestinal transit time was not affected by the amount of the solid meal. On the other hand, it varied among the 3 kinds of test meals in the following rank order : lard>mashed potatoes>skimmed milk.It is noteworthy that small intestinal transit time in the beagle dog is approximately 2 h shorter than that in humans both in fasted and fed states.
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佐藤 幸夫, 中島谷 浩一, 鈴木 康男
1990 年 38 巻 8 号 p.
2228-2232
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Interaction of liposomes (phospholipid vesicle) with human erythrocytes was studied by means of a spectroscopic method. Transfer of hemoglobin between liposomes and erythrocytes was observed. This transfer was mediated by a migration of band 3 proteins. In this case, a transfer of band 4.5 also was observed by means of electrophoresis. An interaction of lipid monomers from the liposomes with the erythrocyte membranes seemd to be closely correlated to the transfer of these proteins. It was presumed that this interaction induced some changes in the molecular organization of the cell membranes around band 3, resulting in release of the proteins from the erythrocyte membranes.
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/ 米持 悦生, 小口 敏夫, 山本 恵司, 仲井 由宣, Yoshinobu NAKAI
1990 年 38 巻 8 号 p.
2233-2236
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
The effect of grinding on the dehydration of crystal water of theophylline has been studied. It was observed that the water content of theophylline hydrate decreased with increased grinding time. As the grinding time proceeded, the results of differential scanning calorimetry (DSC) indicated that crystal water of ground theophylline hydrate dehydrated in three steps at ca. 58, 44, and 17°C, respectively. Powder X-ray diffraction study revealed that the crystal lattice of theophylline monohydrate collapsed by grinding, and part of the theophylline molecules subsequently rearranged the collapsed lattice to form theophylline anhydrate. The result of Fourier transformed infrared spectroscopy demonstrated that the hydrogen bonds between crystal water molecules and theophylline molecules were weakened or destroyed to some extent by grinding. It was supposed that crystal water in the ground theophylline hydrate might exist at least in three molecular states of different hydrogen-bonding. From DSC study, it was suggested that the ruptured hydrogen bonds of water molecules in the ground theophylline hydrate were strengthened after storage under 96.5% relative humidity at 30°C.
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藤井 まき子, 原田 克弘, 松本 光雄
1990 年 38 巻 8 号 p.
2237-2241
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
We prepared a phenobarbital (PB) solid dispersion (SD) with phosphatidylcholine (PC). PB was present in an amorphous state in SD if its mole fraction was under 0.75. An infrared (IR) spectra study suggested a hydrogen bond between NH in PB and phosphate in PC, with a raito of about 1 : 1. When the mole fraction of PB was less than 0.50, differential scanning calorimetry (DSC) curves showed endothermic peaks at 57, 90 and 145°C, and an exothermic peak at 60°C. The IR spectrum and X-ray diffraction pattern changed after holding at 70°C, so at this point it is considered that the metastable state of SD changed into a ctable, and extra energy was released. When the mole fraction of PB was high, PB also arranged near hydrophobic group because an endothermic peak was observed at 46-52°C, which was lower than fully hydrated PC.PB is similar to indomethacin (IM) in molecular shape and to phenyton (PHT) in chemical structure. Its DSC curve and IR spectra are similar to PHT, and the limit ratio of its amorphous state is the same as IM. It is considered that the chemical structure is an important factor in its interaction to PC, and also, the molecular shape is important to arrange into PC lattice.
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手嶋 大輔, 鈴木 彰人, 大坪 健司, 樋口 駿, 青山 敏信, 下園 雄治, 斉田 勝, 野田 寛治
1990 年 38 巻 8 号 p.
2242-2245
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
The efficacy of both the emetic syrup prepared in the previous report and the United States Pharmacopoeia (USP) ipecac syrup concerning the prevention of drug absorption was investigated in 4 beagle dogs using a randomized and cross-over design. In order to control the intragastric pH of the beagle dogs, the administration of pentagastrin or hydrochloric acid (HCl)-glycine buffer (pH 1.5) was tested. The intragastric pH changed from 7.2 to 1.8 with the intramuscular administration of pentagastrin, but the primary emesis occurred more slowly. On the other hand, the HCl-glycine buffer (pH 1.5) gave the appropriate emesis. Therefore, the HCl-glycine buffer (pH 1.5) was used to control the intragastric pH of the beagle dogs.Acetaminophen (AcA), salicylic acid (SA) and kanamycin (KM) as markers were administered orally after conditioning the intragastric pH at 1.5. The emetic syrup or the USP ipecac syrup was then administered. The recovery rate of AcA and KM from vomit was 42-65%. The emetic syrup and the USP ipecac syrup significantly reduced the absorption of AcA from the calculation of pharmacokinetic parameters compared to the control syrup. It was observed that the absorption of cephaeline (CP) in the emetic syrup was less than that of CP in the USP ipecac syrup.
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谷 覚, 田中 亨
1990 年 38 巻 8 号 p.
2246-2248
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Effects of somatostatin on pepsinogen secretion was investigated in the rat in vivo and in vitro. In the perfused rat stomach, somatostatin inhibited secretagogue-induced acid secretion in dose-dependent manner. However, effects of somatostatin on secretagogue-induced pepsinogen secretion were obscure. To clarify the effects of somatostatin on the chief cells, gastric mucosal cell were isolated by a proteolytic enzyme. Somatostain inhibited carbachol- and cholecystoknin octapeptide-induced pepsinogen secretion from dispersed gastric mucosal cells in a dose-dependent manner. Histamine-induced pepsinogen secretion, which was recovered by culturing, was also inhibited by somatostatin. These results suggest that somatostatin inhibits secretagogue-induced pepsinogen secretion directly.
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横山 祥子, 藤江 忠雄
1990 年 38 巻 8 号 p.
2249-2252
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
The association of 1-octadecanoic acid (C18) in 1, 2-dichloroethane at 40°C has been investigated by measuring the fluorescence spectra and intensities of ammonium 8-anilino-1-naphthalenesulfonate as a probe.As a result, it has been found that C18 begins to associate at a concentration of 1.0-1.2×10
-2 mol·dm
-3 and that the aggregation number is small and constant in the concentration region above about 4×10
-2mol·dm
-3.The mechanism for the formation of fatty acid (FA)-thiamine disulfide (TDS) complexes, (FA)
6(TDS), was also discussed.
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松本 治, 多賀 徹, 松島 正明, 東 常行, 町田 勝之輔
1990 年 38 巻 8 号 p.
2253-2255
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
The crystal of bovine trypsin complexed with a potent inhibitor, 4-[4-(N, N-dimethylcarbamoylmethoxycarbonylmethyl)phenoxycarbonyl]guanidinium methanesulfonate (FOY-305) in the novel orthorhombic from with a low molecular packing density was studied by the X-ray diffraction method. Using synchrotron radiation, the intensity data were collected to 1.8 Å resolution. The structure was solved by molecuar replacement methods, and refined to an R-factor=18.0% for 14364 reflection by the restrained least-squares method. The final difference Fourier maps revealed that hydrolyzed inhibitor fragments bind with the protein at multiple sites around the active center of trypsin. The structural feature in the crystalline state probably corresponds to a statistical average of several complexes which would be formed between the inhibitor and trypsin during the binding and releasing process in solution.
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加多木 豊史, 青木 美砂子, 勝 幸子, 片岡 裕美, 花輪 知子
1990 年 38 巻 8 号 p.
2256-2258
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Flavone was reduced with sodium bis(2-methoxyethoxy)aluminum hydride (SMEAH) to 1-(2-hydroxyphenyl)-3-phenylpropanol (A) and 1-phenylindan-1, 3-diol (B). Product yields depended on the molar ratio of SMEAH/flavone. When the molar ratio of SMEAH was from 1 to 2 in relation to flavone, the main product was compound A, but at a ratio of more than 3, the rearranged compound B was predominant.
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小山 清隆, 会田 須美子, 名取 信策
1990 年 38 巻 8 号 p.
2259-2261
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Epimerization reactions of bis(naphtho-γ-pyrone) derivatives, ustilaginoidin A (2) and dihydroisoustilaginoidin A (6), were examined by refluxing the compounds in acetic and in p-xylene. The epimerization occurred in acetic acid but not in p-xylene. From the reaction mixture in the case of dihydroisoustilaginoidin A, the starting material and the epimer at the biaryl linkage, dihydroustilaginoidin A (7), were isolated and characterized. The circular dichroism Cotton effects due to chiral exciton coupling of biaryl compound is discussed.
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榊 潤一, 小林 聡, 佐藤 雅之, 金子 主税
1990 年 38 巻 8 号 p.
2262-2264
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
A new general one-pot method for high-yield synthesis of S-alkyl β-ketothioesters by heating of 6-mono- and 5, 6-disubstituted 1, 3-dioxin-4-ones and thiols in an appropriate aprotic solvent is described. This procedure is available for large-scale preparation of a variety of β-ketothioesters.
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竹内 靖雄, 町支 臣成, 友実 英雄, 吉田 浩一, 大和 正利
1990 年 38 巻 8 号 p.
2265-2267
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
The Wittig reaction of benzofuran-2, 3-diones (2), cyclic α-ketoesters, was examined. The reaction of 2 having an electron-donating substituent on the aromatic ring with a stable ylide afforded not 3-alkylidene-2(3H)-benzofuranones (4) but 2-alkylidene-3(2H)-benzofuranones (1) with high regioselectivity.
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西口 嘉乃, 多河 典子, 渡邊 富久子, 木口 敏子, 二宮 一彌
1990 年 38 巻 8 号 p.
2268-2270
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
The 4-carboxymethylthio derivatives 8 and 13, new haptens of betamethasone (2) and dexamethasone (1), were prepared for application to enzyme immunoassay.
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坂上 健司, 岩松 勝義, 渥美 国夫, 畠中 稔
1990 年 38 巻 8 号 p.
2271-2273
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Synthesis and antibacterial activity of 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methyl)ethoxyiminoacetamido]-3-(3-hydroxy-4-pyridon-1-yl)-3-cephem-4-carboxylic acid (12) and its related compounds are described. Compound 12 exhibited excellent antibacterial activity against gram-negative bacteria, and its anti-pseudomonal activity was ten to fifteen times greater than that of ceftazidime.
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吉野 博, 荒川 義弘, 中澤 隆弘, 金子 武稔, 松永 学, 荒木 伸, 池田 益啓, 土屋 裕, 山津 清實, 橘 真郎
1990 年 38 巻 8 号 p.
2274-2276
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
The opioid activities of [MeTyr
1]-Dyn(1-7)-NH
2, [MeTyr
1, D-Leu
8]-Dyn(1-8)-NH
2, [MeTyr
1, D-Leu
8]-Dyn(1-9)-NH
2, [MeTyr
1, D-Leu
8]-Dyn(1-10)-NH
2, [MeTyr
1, D-Leu
8]Dyn(1-11)-NH
2, and [MeTyr
1, D-Leu
8, 12]-Dyn(1-13)-NH
2 were examined in the bioassays (guinea pig ileum, mouse vas deferens and rabbit vas deferens). Because [MeTyr
1, D-Leu
8]-Dyn(1-9)-NH
2 showed the most potent opioid activity of the peptides tested, the biological activities of two kinds of Dyn(1-9) analogues, [MeTyr
1, MeArg
7, D-Leu
8]-Dyn(1-9)-NHEt and [D-Cys
2-Cys
5, MeArg
7, D-Leu
8]-Dyn(1-9)-NH
2 were determined and compared with those of [MeTyr
1, MeArg
7, D-Leu
8]-Dyn(1-8)-NHEt and [D-Cys
2-Cys
5, MeArg
7, D-Leu
8]-Dyn(1-8)-NHEt in the three bioassays, in the receptor binding assays, and in the mouse tail pinch test after subcutaneous administration. The results suggest that the extension of the C-terminal in the peptide chain of [MeArg
7, D-Leu
8]-Dyn(1-8)-NH
2 analogues by Arg is ineffective for increasing the κ-opioid activities, κ-receptor selectivity and/or analgesic effects of the peptides.
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加藤 健, 森田 豊
1990 年 38 巻 8 号 p.
2277-2280
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
Six flavone C-glycosides : 2", 6"-di-O-acetylisoorientin (1), 2", 6"-di-O-acetylorientin (2), 2"-O-acetylisoorientin (3), 2"-O-acetylorientin (4), isoorientin (5) and orientin (6) were identified from the aerial parts of Rumex acetosa L .(Polygonaceae), in addition to two flavonol O-glycosides : avicularin (7) and hyperin (8). Of these, 1-3 were new compounds and 4-7 were isolated for the first time from this species. The structures were established by ultraviolet, fast atom bombardment mass and nuclear magnetic resonance spectral data.
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呉 鳳鍔, 小池 一男, 二階堂 保, 石井 清, 大本 太一, 池田 恵二
1990 年 38 巻 8 号 p.
2281-2282
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
A new steroid, 22, 23-dihydrospinasterol plamitate was isolated from the whole plants of Arenaria kansuensis (Caryophyllaceae) and its structure was determined by chemical and spectroscopic means. 22, 23-Dihydrospinasterol, 22, 23-dihydrospinasterone, ergosterol-5, 8-peroxide, 24-methylene-22, 23-dihydrolanosterol, zeorin, fernenone, β-sitosterol 3β-O-β-D-glucopyranoside, tricin, (+)-isoscoparin and (-)-isoscoparin were also isolated.
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清水 岑夫, 正川 仁, 松澤 孝泰, 米澤 咲子, 林 利光, 有澤 宗久, 鈴木 正一, 吉崎 正雄, 森田 直賢, / / , Isa ...
1990 年 38 巻 8 号 p.
2283-2284
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
The anti-inflammatory active fraction of the Paraguayan crude drug, "Alhucema, " Lavandula latifolia VILL. afforded four compounds : coumarin (1), 7-methoxycoumarin (2), trans-phytol (3) and caryophyllene oxide (4). 1 showed a weakly inhibitory effect on carrageenin-induced paw edema in rats on topical application and 4 showed an inhibitory effect on histamine-induced contraction in guinea pig ileum.
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古川 高子, 藤林 靖久, 福永 仁夫, 横山 陽
1990 年 38 巻 8 号 p.
2285-2286
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
To obtain radiogallium labeled immunoglobulin G with a high specific radioactivity for in vitro use, a
67Ga source was purified by extraction from
67Ga-gallium citrate with butyl acetate, and a
67Ga-labeling solution was produced. This solution was then used to label a deferoxamine-immunoglobulin G conjugate. Both a very high specific radioactivity(872±56 MBq/mg) and a high labeling efficiency (94.0%) were achieved.
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佐藤 英助, 古川 美地, 金岡 祐一
1990 年 38 巻 8 号 p.
2287-2289
発行日: 1990/08/25
公開日: 2008/03/31
ジャーナル
フリー
The fluorescence of 9, 10-dioxa-syn-3, 4, 6, 7-tetramethylbimane (bimane) was found to be quenched in the presence of guanosine 5'-monophosphate. By using this phenomenon, the bimane system was used for the fluorophor of substrates for phosphodiesterase I.Bimanes were coupled to 5'-guanylic acid and the resulting compounds were shown to be portent fluorogenic substates for the assay of phosphodiesterase I.
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