YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
105 巻, 10 号
選択された号の論文の15件中1~15を表示しています
  • 喜谷 喜徳
    1985 年 105 巻 10 号 p. 909-925
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
    Since the discovery of antitumor activity of cis-Platin by Rosenberg in 1969, various Pt complexes were prepared in order to ameliolate severe kidney toxicity, and vomiting and nausea. Pt complexes have usually high antitumor activity against leukemia L1210. Various antitumor Pt complexes were prepared, with an aim to synthesize the 2nd generation Pt complexes with high and specific antitumor activity without or least toxicity. Various Pt complexes of 1, 2-cyclohexanediamine (dach) and 2-(aminomethyl)-cyclohexylamine (amcha) isomers were prepared as carrier ligands, and mono- and bi-dentate leaving groups. Among the carrier ligands, trans-l-dach, and cis-dl- and trans-dl-amcha are found to be the most antitumor active ligands with 5-membered and 6-membered chelate rings. Water-soluble Pt complexes and lipo-soluble Pt complexes were also prepared by the modification of leaving groups. They are highly antitumor active. Among the Pt complexes prepared so far, Pt (oxalato) (trans-l-dach), as well as Pt (D-glucuronato) (trans-l-dach) nitrate and Pt (D-glucuronato)2 (trans-l-dach) are under development as a new type of the antitumor agent. The interactions of Pt complexes with deoxyribonucleic acid (DNA) were discussed. The mode of action of Pt complexes has been found to be mainly intrastrand crosslinking at N7 of guanine base. The measurements were carried out by the exonuclease enzyme digestion of Pt-DNA complexes, followed by the detection with high performance liquid chromatography. Pt (oxalato) (trans-l-dach) is recommended as the promising 2nd generation Pt complex.
  • 赤池 紀扶
    1985 年 105 巻 10 号 p. 926-936
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
    γ-Aminobutyric acid (GABA)-induced Cl- currents (IC1) were studied in isolated frog sensory neurons after suppression of Na+, K+ and Ca2+ currents under voltage-clamp conditions by using three different kinds of technique such as suction pipette, concentration-clamp and patch-clamp. Noise analyses of IC1 indicated the existence of three subgroups of the receptor-ionophore units. Single channel recordings confirmed the presence of three different GABA-gated conductance. Further, we established 'concentration-clamp' technique in which external solution can be completely exchanged by new test solution with 0.5 ms. By using this technique, we could also separate fast, phasic and tonic currents.
  • 倉石 忠幸, 前橋 はるか, 村上 孝夫, 斎木 保久, 陳 秋明
    1985 年 105 巻 10 号 p. 937-941
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
    From the fronds of Microlepia tenera CHRIST (syn. Oenotrichia tenera TAGAWA) a new ent-pimarane-type diterpene triglycoside was isolated together with hookeroside D (II) previously detected in Scypholepia hookeriana J. SM. (syn. Microlepia hookeriana (WALL.) PRESL). The structure was elucidated as 3α-[O-β-D-fucopyranosyl-(1→2)-α-L-arabinofuranosyloxy]-12α-[β-D-fucopyranosyloxy]-ent-pimara-8 (14), 15-diene (I) on the basis of spectroscopic studies and chemical evidence.
  • 上松瀬 勝男, 梶原 長雄, 林 恭子, 下垣内 秀二, 冨金原 迪, 石河 秀夫, 田村 力
    1985 年 105 巻 10 号 p. 942-947
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
    The clinical evaluation of lyophilized Ganoderma lucidum extract was performed with 53 patients divided into two groups, by oral ingestion of tablets during the evaluation period of six months. Group I consists of essential hypertensive patients. Group II consists of mild hypertensive or normotensive patients. The patients were instructed to take six tablets containing 240 mg of the extract per day. Biochemical and hematological examination were performed for 21 test items, and the following results were obtained. 1) In regard to hypertension, blood pressure significantly decreased in group I, but did not in group II, thus showing that Ganoderma lucidum has an ameliorating effect on hypertension. 2) In regard to biochemical and hematological effects, the oral intake did not result in any change in the values of any of the 21 test items beyond the normal range, except that total cholesterol decreased slightly and fibrinogen increased slightly. It was therefore concluded that Ganoderma lucidum has blood-pressure lowering effect on patients with essential hypertension and will not have any side effects on patients with essential or border line hypertension during six months oral intake.
  • 松田 秀秋, 長谷川 敏代, 久保 道徳
    1985 年 105 巻 10 号 p. 948-954
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
    Effects of 70% methanol extract (I) from Red Ginseng (steamed and dried root of Panax ginseng C. A. MEYER) on the phagocytic activity of mouse reticuloendotherial system were studied by the carbon clearance method in normal mice, carrageenan or cyclophosphamide-treated mice. In normal mice, the clearance-rate of carbon was shortened 1 h after the administration of I (50, 200 or 500 mg/kg, p.o., one time, one time/d for 3 d or one time/d for 5 d). Microscopically, carbon particles were internalized mainly by Kupffer cells in the liver and in the spleen, by macrophage (Mφ) of marginal zones between white and red pulp. I (200 or 500 mg/kg, p.o., one time/d for 3 d) activated the phagocytosis of carbon by Kupffer cells in the liver and Mφ in the spleen. In carrageenan (injurious agent of Mφ)-treated mice, I (200 or 500 mg/kg, p.o.) was not found to show the shortening of the clearance rate of carbon. However, in cyclophosphamide (injurious agent of leukocyte)-treated mice, the clearance-rate of carbon was shortened by the oral administration of I (200 or 500 mg/kg, p.o.). These results suggested that 70% methanol extract from Red Ginseng promotes the phagocytic activity on the reticuloendotherial system in mice and has a stimulatory effect on Mφ.
  • 武田 美雄, 藤多 哲朗, 佐藤 利夫, 掛川 寿夫
    1985 年 105 巻 10 号 p. 955-959
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
    From the aerial part of Stachys sieboldi MIQ. (Labiatae), three glycosides were isolated and characterized as isoscutellarein. 4'-methyl ether 7-O-β-(6'''-O-acetyl-2"-allosyl) glucoside (1), isoscutellarein 7-O-β-(6'''-O-acetyl-2"-allosyl) glucoside (2), and acteoside (8). The effects of these glycosides on the activity of hyarulonidase were also examined.
  • 黒岩 信, 猪爪 信夫, 岩奥 玲子, 中野 真汎
    1985 年 105 巻 10 号 p. 960-965
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
    The possibility of metabolism of clonazepam with fresh stool was investigated because a low correlation had been observed between a clonazepam dose and its serum concentrations, and very low bioavailability had been observed when a single dose of a nonmicronized drug in a gelatin capsule was administered orally. After combination of clonazepam with sterilized broth (pH 7.2), 1% (pH 5.9) or 8% (pH 5.5) sterilized stool culture without further anaerobic precautions, the drug did not degrade in the incubation mixture. This indicates that the drug did not react with the components of broth and stool cultures, and was stable at these pH values. On the other hand, after combination of the drug with 1% or 8% human faecal contents in a broth, the drug disappeared rapidly in the incubation mixture in proportion to stool concentrations. The metabolite was identified to be 7-aminoclonazepam by high performance liquid chromatography (HPLC) and thin-layer chromatography (TLC). The degradation of clonazepam and the appearance of a metabolite, 7-aminoclonazepam were followed by HPLC and TLC.
  • 金庭 延慶, 船木 朋雄, 古田 盛, 渉 信敏
    1985 年 105 巻 10 号 p. 966-972
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
    Because of the absorption of many drugs from the intestine, the gastric emptying rate relates to the time of appearance of drug action. In the present study, the effects of water volume taken with the drugs, atropine, and metoclopramide on the absorption properties of cimetidine were investigated in rats. As a result the following facts were clarified ; 1) the absorption rate of cimetidine was significantly influenced by water volume taken with drug, and in this case the absorption rate decreased with decreasing water volume, 2) atropine (which decreases the gastric emptying rate) decreasing absorption rate constant of cimetidine, and 3) metoclopramide (which increases the gastric emptying rate) increasing absorption rate constant of cimetidine, respectively. On the other hand, it was also clarified that the first-pass effect of cimetidine was negligible and the change of water volume taken with drug and coadministration of atropine and metoclopramide did not decrease the extent of bioavailability of cimetidine in comparison with the control. Although it is reported that an antacid decreased the bioavailability of cimetidine, in the present study the effect of the antacid (formulated to the reported manner) on the absorption of cimetidine was not observed.
  • 野上 真里, 森浦 俊次, 西村 まゆみ, 久保 道徳
    1985 年 105 巻 10 号 p. 973-977
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
    "Zhu", dried rhizomes of Atractylodes species has been used for the treatment of indigestion and stomachache as stomachic in traditional Chinese system of medicine. In previous papers, we reported that among various kinds of "Zhu", 50% methanolic extracts of Atractylodes lancea and Atractylodes lancea var. chinensis showed strong inhibitory activity on most experimental ulceration, while those of Atractylodes ovata and Atractylodes japonica produced a significant inhibition on stress-induced ulceration in rats. In order to explore the mode of anti-ulcerogenic activity of 50% methanolic extract of Atractylodes lancea var. chinensis (AC), in the present study, the inhibitory activity of extract on gastric acid secretion in perfused stomach preparation, on gastric secretion in adrenalectomized rats and cooperative activity with steroidal hormone were investigated. Consequently, it was suggested that the anti-ulcerogenic action of AC was closely related to the movement of steroidal hormone in the plasma.
  • 野上 真里, 森浦 俊次, 久保 道徳
    1985 年 105 巻 10 号 p. 978-982
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
    In the previous paper, we suggested that anti-ulcerogenic activity of 50% methanolic extract of Atractylodes lancea var. chinensis (AC) was due to an action through the function of adrenal grand. In the present study, the effect of AC on a protective factors of gastric mucosa was investigated in experimental animals. As a result, AC increases a content of hexosamine in gastric mucosa and gastric mucosal blood flow in acetic acid-induced ulceration in rats. It was proved that strong anti-ulcerogenic activity of AC was exhibited by increasing the protective function of gastric mucosa.
  • 梶原 良夫, 菅井 三郎, 神原 俊文, 内藤 泰男, 河田 登美枝, 木村 智憲, 栗山 隆, 勝原 徳寛, 寺脇 康文, 久津間 輝雄, ...
    1985 年 105 巻 10 号 p. 983-989
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
  • 菅井 三郎, 梶原 良夫, 河田 登美枝, 神原 俊文, 内藤 泰男, 長谷川 賀洋, 吉田 誠一郎, 赤星 三彌, 久津間 輝雄, 高柳 ...
    1985 年 105 巻 10 号 p. 990-995
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
    An investigation on the structure-activity relationship with respect to spasmolytic activity of 4-acyloxy-1-alkyl-1-(1, 3-dioxolan-2-ylmethyl) piperidinium derivatives (1) has led to the development of 4-acyloxy-1-alkyl-1-(1, 3-dioxolan-2-ylmethyl) piperidinium derivatives (2) having further potent spasmolytic activity. The compounds (1 and 2) have two geometrical stereoisomers (trans and cis) attributable to the difference of the configuration at C4-position and tetravalent nitrogen atom of piperidine ring. The trans isomers of 1 and 2 exhibited potent activity than the corresponding cis ones. From the trans-isomers (2), 4-benziloyloxy-1-(1, 3-dioxolan-2-ylmethyl)-1-methylpiperidinium bromide (2a) and 1-(1, 3-dioxolan-2-ylmethyl)-1-methyl-4-(xanthene-9-carbonyloxy) piperidinium bromide (2b) were selected and subjected to examination for pharmacological properties, acute toxicity, antisialagogic activity, mydriatic activity and spasmolytic activity based on the inhibition of the spontaneous movement by using in situ rabbit stomach. The spasmolytic activity of the trans-2a and 2b were considerably potent than that of atropine sulfate and 8-butylscopolaminium bromide (BSB). Safety range of the trans-2b in terms of the spasmolytic activity for acute toxicity, antisialagogic activity and mydriatic activity could be evaluated larger than that of atropine sulfate and BSB.
  • 早川 順子, 野田 直希, 山田 貞二, 三上 栄一, 宇野 圭一
    1985 年 105 巻 10 号 p. 996-1000
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
    Gardenia fruits and its commercial preparations were evaluated chemically by means of thin layer chromatography and high performance liquid chromatography. Geniposide, one of major constituents, was used as a standard substance. Recoveries of geniposide from model preparations were 98.5%. The methods are considered to be useful for the identification and quantitative determination of geniposide in commercial preparations containing gardenia fruits.
  • 岡戸 三枝, 松本 〓, 濱田 吉通, 日高 良一
    1985 年 105 巻 10 号 p. 1001-1003
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
    The bladder has functions to retain and excrete the urine, differing from other regions. Therefore, when drugs are infused in the bladder, they are excreted during urination, and it is difficult to keep them acting in the affected regions for a long period. We have been studying a drug with a prolonged effect in the bladder, thus enabling topical chemotherapy of bladder cancers and prevention of their reccurrence. This led to research and development work on the intravesical stick (IVS). IVS has a base consisting of witepsol H-15, E-85, polysorbate 80 and bleached beeswax, and mixed drugs in it uniformly, and is formed to the stick-shape, and this semi solid dosage form can be applied into the bladder via urethra. The specific gravity was 0.989-0.998 (25°C), and dysuria develops hardly because of the floating into urine. Moreover, in the dissolution examination of active ingredient, the differences of elution patterns were noted by the type of the prescription of the base, and the active ingredient was detected from the start of the dissolution up to 48-120 h. From the results, the usefulness of this drug was suggested as a prolonged effective one.
  • 今村 順茂, 園田 正信, 小田切 優樹, 一番ヶ瀬 尚
    1985 年 105 巻 10 号 p. 1004-1007
    発行日: 1985/10/25
    公開日: 2008/05/30
    ジャーナル フリー
    The serum protein binding of carbutamide in normal and alloxan diabetic rabbits was examined by using the ultrafiltration method. The serum protein binding of carbutamide in alloxan diabetic rabbits was lower than that in normal rabbits. The glycosylation of serum proteins may become one of factors determining the serum protein binding of carbutamide in alloxan diabetic rabbits.
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