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北原 一太, 松本 陽子, 上田 甫, 上岡 龍一
1992 年 40 巻 8 号 p.
2208-2209
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
The antioxidation effect was remarkably enhanced in the case of natural phenol derivatives (sesamol and eugenol) as compared with synthesized butylated hydroxyanisol (BHA).
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小濱 靖弘, 飯田 健太郎, 仙波 太郎, 三村 務, 稲田 昭, 田中 啓詞, 中西 勤
1992 年 40 巻 8 号 p.
2210-2211
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
A new cytotoxic substance designated as BS-1 was isolated from the autolysate and culture filtrate of Bacillus stearothermophilus UK563. On the basis of spectral data, the structure of BS-1 was determined as bis(2-hydroxyethyl) trisulfide and confirmed by direct comparison with the synthetic compound. BS-1 exhibited potent cytotoxicity against leukemia P388-D1, leukemia P388, mastocytoma P815, lymphoma EL4 and lymphoma MOLT4.
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木方 正, 塩瀬 能伸, 永井 勝幸, 佐久嶋 美穂, 鵜飼 茂夫
1992 年 40 巻 8 号 p.
2212-2214
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
An antitumor polysaccharide containing peptide moieties AT-HW ([α]
D + 31° in water) and an antitumor polysaccharide AT-AL ([α]
D + 209° in 1 M sodium hydroxide) were isolated from hot-water extract and the alkaline extract of the fruiting bodies of Armillariella tabescens, respectively. Chemical structures of AT-HW and AT-AL were investigated by a combination of chemical and spectroscopic methods. The results indicate that the major constituent of AT-HW (molecular weight, 105000), a heteroglycan, is composed primarily of β-(1→6)-linked D-glucopyranosyl and D-galactopyranosyl residues, and contains their branched residues and terminal sugar (gluco-, manno-, and fucopyranose) residues, in addition to β-(1→3)-linked D-glucopyranosyl residues, while AT-AL molecular weight, 93000) is chiefly composed of α-(1→3)-linked D-glucopyranosyl residues.
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大野 尚仁, 三浦 敏秀, 斉藤 和夫, 西島 基弘, 宮崎 利夫, 宿前 利郎
1992 年 40 巻 8 号 p.
2215-2218
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
Physicochemical properties and antitumor activities of a fungal (1→3)-β-D-glucan, OL-2, isolated from Leiwan (Omphalia lapidescens) were examined. OL-2 showed sharp signals on carbon-13 nuclear magnetic resonance spectrum in dimethylsulfoxide-d
6 as a solvent, and these signals were significantly reduced by the addition of distilled water to the concentration of 20%. This phenomenon is consistent with the general property of the gel forming (1→3)-β-D-glucan. Binding of OL-2 to Congo red induced a significant change of λ
max to a longer wavelength, and the concentration to induce gel to sol transition was about 0.7 N; in contrast, the concentration was about 0.2 N in the cases of SPG and curdlan. These observations suggested that the gel structure would be significantly stabilized in the case of OL-2. OL-2 showed no or low antitumor activity against the solid form of Sarcoma 180 by intraperitoneal and intralesional administrations; however, it was effective on the ascites form of Sarcoma 180. Of interest, OL-2 also showed significant antitumor activity against the ascites form of MH-134 when administered with 5-fluorouracil. These results indicated that OL-2 showed characteristic features regarding its physicochemical properties and antitumor activity.
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友田 正司, 淺原 初木, 権田 良子, 高田 勝利
1992 年 40 巻 8 号 p.
2219-2221
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
The controlled Smith degradation of MVS-VI, the major acidic polysaccharide having remarkable anti-complementary activity isolated from the seeds of Malva verticillata L., was performed. Methylation analysis of both the primary and the secondary Smith degradation products indicated that the core structural features of MVS-VI include a backbone chain composed of β-1, 3-linked D-galactose residues. The majority of galactose units in the backbone carry side chains composed of β-1, 3- and β-1, 6-linked D-galactosyl residues at position 6. The controlled Smith degradation products showed considerable anti-complementary activity.
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山田 健二, 丸山 和容, 最上 理, 宮川 尚訓, 坪井 實
1992 年 40 巻 8 号 p.
2222-2223
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
The influence of melatonin on reproductive behavior was examined by administering it to pinealectomized male rats for 30 consecutive days. After the 30-d administration of melatonin or vehicle, each male rat was introudced into a female rat's cage on the day of proestrus and allowed to mate overnight. All rats administered the vehicle and the pinealectomized rats copulated; five of the twelve melatonin (8.0 mg/kg)-treated rats did not copulate. These findings suggest that melatonin inhibits the reproductive behavior of male rats.
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宮崎 正三, 大川 裕, 高田 昌彦 /, David ATTWOOD
1992 年 40 巻 8 号 p.
2224-2226
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
Pluronic F-127 (PLF-127) gels were evaluated as a sustained-release vehicle for intraperitoneal administration of mitomycin C (MMC) in order to enhance the therapeutic effects of MMC against a Sarcoma-180 ascites tumor in mice. Tumor cell injections were made on day 0 and injections of MMC in 25% (w/w) PLF-127 on day 1, both intraperitoneally. A prolongation of the life span of tumor-bearing mice following injection of therapeutic PLF-127 was noted, and PLF-127 containing MMC was therapeutically more active than free drug. The high chemotherapeutic efficiency of MMC in PLF-127 was striking at high doses, which would be toxic in the case of the drug alone.PLF-127 gels exhibit reverse thermal behavior and are fluid at refrigerator temperature, but are soft gels at body temperature. The in vitro release experiments indicated that Pluronic gel might serve as a rate-controlling barrier and be useful as a vehicle for sustained-release preparations of MMC to be administered intraperitoneally. These results suggest that sustained-release occurs in the peritoneum and that effective drug concentrations can be maintained by the preparation.
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永井 葉月, 塩沢 竜志, 阿知波 一雄, 寺尾 良保
1992 年 40 巻 8 号 p.
2227-2229
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
Optically active β-lactams were obtained conveniently by lipase-catalyzed enantioselective hydrolysis of 1-acyloxymethyl-2-azetidinones and esterification of 1-hydroxymethyl-3, 3-dimethyl-2-azetidinone with vinyl acetate in organic solvent.
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朱 永智, 呂 曙〓, 岡田 嘉仁, 高田 光正, 奥山 徹
1992 年 40 巻 8 号 p.
2230-2232
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
Two new cycloartane-type glucosides, mongholicoside I (1) and II (2), were isolated from the aerial part of Astragalus mongholicus Bunge and characterized as 9, 19-cyclolanost-24E__--ene-1α, 3β, 16β, 27-tetraol 27-O__--β-D-glucopyranoside and 3β-acetoxy-9, 19-cyclolanost-24E__--ene-1α, 3β, 12β, 16β, 27-pentaol 27-O__--β-D-glucopyranoside based on the chemical and spectral evidence.
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菊地 和也, 早川 宏, 長野 哲雄, 平田 恭信, 杉本 恒明, 広部 雅昭
1992 年 40 巻 8 号 p.
2233-2235
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
Nitric oxide (NO) reacts with H
2O
2 to produce a rise in potent luminol-dependent chemiluminescence under neutral pH conditions. We applied this reaction to the continuous detection of NO released from the rat isolated perfused kidney with simultaneous pressure changes. Acetylcholine increased NO release dose-dependently with the pressure reduction. An NO synthesis inhibitor, N
G-monomethyl-L-arginine, abolished the release. This inhibition was reversed by the addition of L-arginine.
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合田 幸広, 鈴木 淳子, 米谷 民雄, 義平 邦利, 武田 明治, 内山 充
1992 年 40 巻 8 号 p.
2236-2238
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
An aniline derivative which corresponds to UV-5 in the preceding paper was isolated from the case L-tryptophan sample associated with eosinophilia-myalgia syndrome (EMS). By spectroscopic analyses, the structure was identified as 3-anilinoalanine. The compound was optically active, and the stereochemistry of alanine moiety was determined as L, by comparing the specific rotation with a synthesized 3-anilino-L-alanine.
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吉川 雅之, 畠山 祥子, 谷口 久美子, 松田 久司, 山原 條二
1992 年 40 巻 8 号 p.
2239-2241
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
By monitoring the effects on HCI / ethanol-induced gastric lesions in rats, a new anti-ulcer principle named 6-gingesulfonic acid was isolated from Zingiberis Rhizoma, the dried rhizome of Zingiber officinale ROSCOE (cultivated and processed in Taiwan) together with three new monoacyldigalactosylglycerols named gingerglycolipids A, B and C. Their chemical structures were elucidated on the basis of chemical and physicochemical evidence. 6-Gingesulfonic acid showed more potent anti-ulcer activity than 6-gingerol and 6-shogaol.
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森田 哲生, 本屋敷 敏雄, 鶴薗 保幸, 金川 麻子, 冨永 伸明, 植木 寛
1992 年 40 巻 8 号 p.
2242-2244
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
Sodium orthovanadate increased inositol 1, 4, 5-trisphosphate content in rat adipose tissue in a time-dependent manner up to 30 s; its maximal effect was two-fold higher than the basal level of IP
3, and it probably consequently causes elevation of the intracellular Ca
2+.
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井上 誠, 永津 裕子, 若林 啓造, 沈 逸容, 荻原 幸夫
1992 年 40 巻 8 号 p.
2245-2247
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
The relation among circulating monocytes, serum cholesterol and LDL cholesterol in manifestation of atherosclerosis was investigated in hypercholesterolemic rabbits. Serum cholesterol increased sharply and reached a plateau at 12 weeks after the start of cholesterol diet feeding; LDL cholesterol gradually increased until 24 weeks, and the number of monocytes in blood started to decrease abruptly around 12 weeks and resulted in less than 1% total white blood cells at 24 weeks, as reflected by a severe progression of atheroma formation. This result indicated that the decrement of monocyte number in blood was predictive of the presence of severe atherosclerotic plaques.
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吉川 雅之, 内田 英美子, 川口 敦弘, 北川 勲, 山原 條二
1992 年 40 巻 8 号 p.
2248-2250
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
Five new antioxidative glycosides named galloyl-oxypaeoniflorin, suffruticosides A, B, C, and D, and a new paeonol glycoside named suffruticoside E have been isolated from Chinese Moutan Cortex, the root cortex of Paeonia suffruticosa ANDREWS, together with antioxidative galloyl-paeoniflorin. Their structures were elucidated on the basis of chemical and physicochemical evidences. Galloyl-oxypaeoniflorin, galloyl-paeoniflorin, suffruticosides A, B, C, and D showed more potent radical scavenging and antioxidative effects than α-tocopherol.
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三本 勤, 今井 順也, 木佐貫 純嗣, 榎本 裕志, 服部 直子, 赤路 健一, 木曽 良明
1992 年 40 巻 8 号 p.
2251-2253
発行日: 1992/08/25
公開日: 2008/03/31
ジャーナル
フリー
Selective and potent HIV protease inhibitors containing allophenylnorstatine [Apns; (2S, 3S)-3-amino-2-hydroxy-4-phenylbutyric acid] as a transition-state mimic were designed and synthesized. Among them, conformationally constrained tripeptide derivatives, kynostatin (KNI)-227 and -272 (Fig.1), exhibited highly potent antiviral activities against a wide spectrum of HIV isolates. Ready availability due to the simple synthetic procedure and the excellent antiviral properties indicate that KNI-227 and KNI-272 are promising candidates as selective anti-AIDS drugs.
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