YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
108 巻, 9 号
選択された号の論文の13件中1~13を表示しています
  • 佐藤 雅之
    1988 年 108 巻 9 号 p. 805-823
    発行日: 1988/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Several synthetic methods of 1, 3-dioxin-4-one and its derivatives are described. These dioxinones undergo cycloreversion to formyl- or acylketenes, whose inter- or intramolecular trapping provides efficient routes to a variety of heterocyclic compounds. Use of 6-unsubstituted dioxinones in the so-called de Mayo reaction provides an efficient method for simultaneous introduction of acetic acid and formyl appendages at the vicinal position of alkanes. Chiral spirocyclic dioxinones readily available from l-menthone show remarkable diastereofacial selectivities in a variety of addition reactions, such as photo [2+2] additions, Diels-Alder reactions, and conjugated additions. Thus, use of spirocyclic dioxinones has provided enantioselective synthetic methods of Corey lactone derivatives, carbocyclic analogues of C-nucleoside, and 3-hydroxybutyric acid.
  • 糸川 秀治
    1988 年 108 巻 9 号 p. 824-841
    発行日: 1988/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Sarcoma-180A has been used for screening the antineoplastic components from natural sources, especially from higher plants. The cyclic oligopeptides RA series compounds isolated from Rubia akane are toxic substances against many kinds of tumors. They were studied chemically and biologically. Among of them, RA-VII is the most active compound against animal tumors and adopted to be tested for phase I study after precrinical trials. Sinococuline isolated from Cocculus trilobus, which is an morphinane alkaloid, has also strong antineoplastic activity against many kinds of animal tumors. Some kinds of diterpenes isolated from Casearia sylvestris, a Palaguaian plant, are very toxic for Sarcoma-180A. Moreover, chemical and biological investigations have been applied to the Zingiberaceous plants.
  • 大熊 勝治
    1988 年 108 巻 9 号 p. 842-855
    発行日: 1988/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Lysosomes, which form an important degradative system within eukaryotic cells, have such conspicuous feature that their interior is acidic, providing favorable conditions for various acidic hydrolases. It has been controversial for a long time whether the low internal pH of lysosomes reflected an equilibrium of protons or an active transport mechanism. In our study, we determined the precise pH within lysosomes by establishing a new quantitative and sensitive technique for pH estimation. Furthermore, we showed that the lysosomal pH is influenced by basic substances. An interest in the mechanism of lysosomal acidification has increased with the realization that (1) there are several acidic compartments, besides lysosomes, constituting a vacuolar system within eukaryotic cells and that (2) basic substances also affect a variety of biological reactions. Subsequently, we showed that the lysosomal pH is maintained by an adenosine triphosphate-dependent proton pump. The proton pump is now well recognized to be ubiquitous in vacuolar system. This review summarizes the pH maintenance mechanism and the nature of the proton pump in lysosomes.
  • 茂田 士郎, 細谷 光亮, 望月 忍, 千葉 卓男
    1988 年 108 巻 9 号 p. 856-859
    発行日: 1988/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Various pyridoazoles have been synthesized and tested against respiratory syncytical virus, Flu-V (A-Ishikawa/17/82), and herpes simplex virus (KOS-1). Among these compounds, 2-carboxy-4-ethoxycarbonyl-1-oxo-1H, 5H-pyrido[1, 2-a]benzimidazole (2) and 2-benzamido-4-cyano-1-oxo-1H, 5H-pyrido[1, 2-a]benzimidazole (4) were found to have significant antiviral activity.
  • 平原 敬三, 安藤 直子, 松石 哲郎, 鈴木 信夫, 寺尾 俊彦, 倉田 宗司
    1988 年 108 巻 9 号 p. 860-866
    発行日: 1988/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    The addition of sodium oleate to antithrombin III (ATIII) produced complexes of ATIII and oleic acid by varying the acid concentration. During immunoelectrophoresis, ATIII shifted to the anode in the presence of sodium oleate. The reactivity of ATIII with anti human ATIII serum lowered as the sodium oleate level increased. However the reactivity with antibody obtained by immunization of rabbits with the mixture of sodium oleate and ATIII, was not lost on the immunoelectrophoresis. In acrylamide gel electrophoresis, ATIII separated into 6 bands with an increase in sodium oleate. The binding ratio of ATIII to heparin-Sepharose decresed in the presence of sodium oleate. In acrylamide gel isoelectrofocusing, the subtypes of ATIII having pI 5 showed high affinity to oleic acid. These high affinity subtypes also showed high affinity to heparin and thrombin. In fibrinogen agarose electrophoresis, ATIII lost its antithrombin activity depending on the increase of sodium oleate. By the determination of free fatty acids (FFA) in ATIII purified from normal plasma, we found that FFA would bind to ATIII in the normal plasma. Scatchard plot analysis indicated 7.6 binding sites of oleic acid per ATIII molecule. The results suggested that ATIII lost its activity by conformational change or interference in the thrombin binding site, and that the subtype of ATIII having pI 5 could be a significant carrier of plasma FFA.
  • 平原 敬三, 松石 哲郎, 鈴木 信夫, 寺尾 俊彦, 倉田 宗司
    1988 年 108 巻 9 号 p. 867-871
    発行日: 1988/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    In assaying fibrinogen agarose electrophoresis, we found that oleic acid controlled antithrombin III (ATIII) activity depending on the acid concentration. In our assay with synthetic substrates, the inhibition of ATIII progressive activity (PA) by unsaturated fatty acids was at least 4-fold stronger than that by saturated ones. Specifically, the inhibitory activity of oleic acid was 6.7-fold of palmitic acid, and 13.1-fold of stearic acid. 50% inhibition of both PA and heparin cofactor activity (HCA) in 0.86 μM ATIII significantly decreased in the presence of 13 μM oleic acid. There was no difference in PA and HCA resulting from the order of mixing ATIII, oleic acid and heparin, indicating that heparin did not affect the formation of ATIII-oleic acid complex. However the presence of albumin neutralized the ATIII inhibition activity of oleic acid significantly. The addition of albumin to the mixture of oleic acid and ATIII, however, did not restore the ATIII activity, which indicated that albumin could not dissociate oleic acid from ATIII. These results suggest that unsaturated fatty acids inhibit mainly the regulating function of ATIII on coagulation, and that it may give rise to thrombotic disorders.
  • 山口 啓之, 高田 正昭, 笠井 良次, 松浦 広道, 田中 治, 不破 享
    1988 年 108 巻 9 号 p. 872-875
    発行日: 1988/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    The contents of the individual neutral and acidic saponins in cultivated Ginseng was investigated by high performance liquid chromatographic analysis. In main roots, saponin contents increase with aging and once decrease in 5th years plant due to the marked development of weight of the roots. Then a significant increase was observed in 6th years plant. In case of lateral roots, a remarkable increase of the contents was observed in 3rd years plant and then the contents decrease in 5th and 6th years plant. The content of ginsenoide-Re is relatively higher in this part than others. In the rhizomes, the contents greatly increase between 2nd and 3rd years plant. It is noteworthy that the content of ginsenoside-Ro, the glucuronide saponin of oleanolic acid, is significantly higher in the rhizomes than in the other parts.
  • 谿 忠人, 大野 智子, 井上 一美, 有地 滋
    1988 年 108 巻 9 号 p. 876-885
    発行日: 1988/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Effects of clofibric acid and three kampo-prescription, sho-saiko-to, dai-saiko-to and san-oh-shashin-to on biological responses in betamethasone treated rats were compared especially from hemorheological view points. Dai-saiko-to and san-oh-shashin-to, famous kampo-prescriptions used in traditional Chinese system of medicine, were found to improve the hyperviscosity accompanied with hyperlipemia and hypercoagulative property affected by betamethasone treatment. The activities of clofibric acid which has also improved hyperviscosity and three kampo-prescriptions were found to differ in degree of reacting on serum levels of corticosterone, lipidoperoxide and triglyceride and liver weight in betamethasone treated rats.
  • 廣瀬 智弘, 杉浦 重樹, 柴田 仁美, 長谷 哲, 中西 義信, 正宗 行人
    1988 年 108 巻 9 号 p. 886-893
    発行日: 1988/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Total nucleotide sequence of plasmid pKYM which was isolated from Shigelia sonnei as a multicopy plasmid was determined by the Sanger's method. An open reading frame of 321 amino acid polypeptide (37 kilo dalton) was found in the sequence which corresponded to the rep gene found by the biological experiment. It was also determined that the minimal nucleotide sequence required to initiate replication was 133 bp present in the Hin dII-Hin dII fragment by constructing the plasmids with deletions around the replication origin.
  • 廣瀬 智弘, 柴田 仁美, 長谷 哲, 中西 義信, 正宗 行人
    1988 年 108 巻 9 号 p. 894-903
    発行日: 1988/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Plasmid pKYM is a multicopy plasmid isolated from Shigella sonnei. We have determined the region required for the incompatibility which also controls the copy number. It is partially overlapped with the region required for the initiation of replication. There are two promoters in this region. One promoter synthesizes messenger ribonucleic acid (mRNA) of rep protein (PR promoter) and another one transcribes the opposite strand in the same region (PL promoter). These two RNAs seem to interact through the stem-and-loop structure present in this region. The repression of the synthesis of rep protein which is essential for plasmid replication by the interaction of these two RNAs seems to be the main mechanism of the incompatibility and the regulation of copy number.
  • 石井 康子, 谷澤 久之, 滝野 吉雄
    1988 年 108 巻 9 号 p. 904-910
    発行日: 1988/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    The mechanism of cathartic effect of barbaloin, representative of Aloe, was investigated by using male rats. Barbaloin administered orally was demonstrated to decompose to aloe-emodin-9-anthrone and aloe-emodin in the rat large intestine. And, these decomposed compounds were likely to change each other in the large intestine. Any compound of barbaloin, aloe-emodin-9-anthrone and aloe-emodin administered orally to rats was found to cause an obvious increase of water content in the large intestine, and only aloe-emodin-9-anthrone administered orally caused a significant increase of water content in the small intestine. Furthermore, the clear increase of water content and abnormality of electrolytes (Na+, K+) in the colon segment of rat were observed only by aloe-emodin-9-anthrone when compounds tested were injected directly into the colon segment. Therefore, it seemed that aloe-emodin-9-anthrone, a decomposition product of babaloin in the rat large intestine, caused an increase of water content in the large intestine by a different mechanism from the stimulation of peristalsis and this played an important role in cathartic activity of barbaloin.
  • 高谷 昌弘
    1988 年 108 巻 9 号 p. 911-915
    発行日: 1988/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Upon treatment of 4, 5-dichloro-3(2H)-pyridazinone (II) with 47% hydrobromic acid, 4, 5-dibromo-3(2H)-pyridazinones (III) and 4-bromo-5-chloro-3(2H)-pyridazinones (IV) were obtained. This nucleophilic substitution is a rare example to react preferentially at the 4-position than the 5-position of II.
  • 小山 又次郎, 狐塚 寛
    1988 年 108 巻 9 号 p. 916-920
    発行日: 1988/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    The murexide reactions of uric acid and other xanthine derivatives were investigated to clarify the pathways of the coloration. From the reaction mixture of uric acid with nitric acid, alloxan (3) and parabanic acid (4) were isolated. Alloxan was found to be a key intermediate, since it was converted to a purple colored murexide by treatment with conc. ammonia. From the murexide reaction of theophylline, 3-hydroxy-4, 6-dimetyloxazolo[4, 5-d]pyrimidine-2, 5, 7(3H, 4H, 6H)-trione (1) and 1, 3-dimethylalloxan (2) were isolated, and these compounds were converted to the purple colored murexoin with conc. ammonia. From the murexide reactions of theobromine and xanthine, 5[(hexahydro-1-methyl-2, 4, 6-trioxo-5-pyrimidinyl)imino]-1-methyl-2, 4, 6(1H, 3H, 5H)-pyrimidinetrione monoammonium salt (5) and murexide were obtained as colored substances, respectively, but an attempt to isolate intermediates was unsuccessful. Murexide and 5 were found to occur in the anion delocalized structure in solution from the nuclear magnetic resonance spectral data.
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