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Volume 35, Issue 10
Displaying 1-50 of 62 articles from this issue
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OSAMU NAKAGUCHI, TERUO OKU, MASASHI HASHIMOTO, TAKASHI KAMIYA1987 Volume 35 Issue 10 Pages 3979-3984
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESS3-Aminonocardicinic acid (3-ANA, 2) was prepared by removal of the N-acyl group of nocardicin A (1). Reacylation of 2 with some typical side-chain acids gave the corresponding semisynthetic nocardicins 6.View full abstractDownload PDF (943K) -
OSAMU NAKAGUCHI, TERUO OKU, HIDEKAZU TAKENO, MASASHI HASHIMOTO, TAKASH ...1987 Volume 35 Issue 10 Pages 3985-3994
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSMonocyclic β-lactams related to nocardicins were enantioselectively synthesized from phthal-imidoacetyl chloride and hexahydro-1, 3, 5-triazines (4) via a [2+2] cycloaddition reaction. The preparation and biological activity of some typical acyl derivatives are also described.View full abstractDownload PDF (1467K) -
HIROYUKI SETOI, HIROSHI KAYAKIRI, HIDEKAZU TAKENO, MASASHI HASHIMOTO1987 Volume 35 Issue 10 Pages 3995-3999
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSPolyhydroxylated pyrrolidine derivatives, 7, 11, 15, and 18, were synthesized from 4, a. key intermediate for our total synthesis of swainsonine (1). The immunostimulating activities of these new derivatives were found to be moderate and less than that of swainsonine.View full abstractDownload PDF (666K) -
KOICHI KOJIMA, SHIGEO AMEMIYA, KAZUO KOYAMA, SHINICHI SAITO, TAKESHI O ...1987 Volume 35 Issue 10 Pages 4000-4015
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSOptically active 3-hetero analogues of isocarbacyclin (34a, 38, 39, 40 and 42) as well as ω-chain analogues have been synthesized from the bicyclic alcohol (1). Compound 34d had more potent anti-platelet aggregating activity than prostacyclin in human platelet-rich plasma.View full abstractDownload PDF (2892K) -
NOBUTOSHI TANAKA, HIROSHI WADA, MASAAKI KOJIMA, TAKAO MURAKAMI, YASUHI ...1987 Volume 35 Issue 10 Pages 4016-4021
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThree new hopane-type triterpenes, 1, 2 and 3, were isolated from the fronds of Cheiropleuria bicuspis (BL.) PR. The structures were determined as 22, 25-dihydroxyhopan-1-one, 1α, 11α, 22-trihydroxyhopane and 1α, 11α, 22, 25-tetrahydroxyhopane, respectively, on the basis of spectral data, X-ray analysis and chemical correlations.View full abstractDownload PDF (845K) -
EMAKO SUZUKI, MARIKO OSABE, MASATAKA MOCHIZUKI, YUKO WAKABAYASHI, MASA ...1987 Volume 35 Issue 10 Pages 4022-4030
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSDirectly acting mutagens formed from N-nitroso-N- (formylmethyl) alkylamines (3) were isolated and identified as N-nitroso-N-alkyl-1-hydroxyimino-2-oxoethylamines (4). Their structures were elucidated on the basis of nuclear magnetic resonance spectra and confirmed by derivatization to the crystalline 2, 4-dinitrophenylhydrazones (5). Compounds 4 (alkyl =ethyl and butyl) were strongly mutagenic to Salmonella typhimurium TA 1535 and Escherichia coli WP2 hcr- without metabolic activation, while 4 with a tert-butyl group was not mutagenic. The formation of 4 is considered to proceed by the nitrosation of 3, indicating a possible involvement of the formylmethyl metabolite in carcinogenesis by N-nitrosamines with a 2-hydroxyethyl group.View full abstractDownload PDF (1589K) -
TAISEI UEDA, TSUNEYASU ADACHI, JINSAKU SAKAKIBARA, MASAHISA ASANO, JOZ ...1987 Volume 35 Issue 10 Pages 4031-4038
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSNovel heterocycles, purino [7, 8-g] -6-azapteridines and [1, 2, 4] triazino [3, 2-f] purines, were synthesized and their biological activities were examined. Heating of 7, 8-diamino-1, 3-dimethylxanthine (2), which was obtained by the reaction of 8-aminotheophylline with hydroxylamine-Ο-sulfonic acid, with hydrochloric acid gave 2, 4, 7, 9-tetramethylpurino [7, 8-g] -6-azapteridine-1, 3, 8, 10 (2H, 4H, 7H, 9H) -tetrone (4) in 96% yield; this product was identical with the compound obtained by the reaction of 2 with alloxan followed by methylation. Treatment of 4 with alkylamines gave 3-alkylamino-2-alkylcarbamoyl-6, 8-dimethyl [1, 2, 4] triazino [3, 2-f] purine-7, 8 (6H, 8H) -diones (10a-g) in 63-95% yields. Compound 4 was active against P 388 leukemia. Vascular relaxing effects of some of the triazino [3, 2-f] purines (10a, b, e, f) were examined, but none showed potent activity.View full abstractDownload PDF (1194K) -
MITSUAKI KODAMA, YOSHINORI SHIOBARA, HISAKO SUMITOMO, KAZUKO MITANI, K ...1987 Volume 35 Issue 10 Pages 4039-4042
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSZerumbone (1), an eleven-membered ring sesquiterpene isolated from Zingiber zerumbet, was synthesized by means of an intramolecular Wittig-type reaction of the keto-phosphonate 2.View full abstractDownload PDF (747K) -
SHINGO SATO, SYUJI FUJITA, KIMIO FURUHATA, HARUO OGURA, SHOJI YOSHIMUR ...1987 Volume 35 Issue 10 Pages 4043-4048
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESS2-(5-Cholesten-3β-yloxy)α- and β-glycosides of N-acetyl-D-neuraminic acid were prepared 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.View full abstractDownload PDF (886K) -
KIYOTAKA KOYAMA, SHINSAKU NATORI, YOICHI IITAKA1987 Volume 35 Issue 10 Pages 4049-4055
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe absolute configuration of chaetochromin A (1) was established by X-ray analysis of the 6-Ο-p-bromobenzoate (15) of the 5, 5', 6', 8, 8'-pentamethyl ether (14). The stereochemistry of the 9-9' bond was proved to be S, in agreement with the result obtained by the application of the exciton chirality method. From the circular dichroism spectra, the absolute configurations of chaetochromins B, C and D (2-4) and cephalochromin (8) were proved to be S, while those of ustilaginoidins A, B, and C (5-7) were R. The stereochemistry of other bis (naphtho-γ-pyrones) is discussed.View full abstractDownload PDF (1028K) -
MASAHIRO SUZUKI, HIROMICHI TANAKA, TADASHI MIYASAKA1987 Volume 35 Issue 10 Pages 4056-4063
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSSeveral 5-carbon-substituted 1-β-D-ribofuranosylimidazole-4-carboxamides were synthesized via the direct C-5 lithiation of a protected 4-carboxamide derivative as the key reaction step. Wittig reaction of a 5-formyl derivative was also examined.View full abstractDownload PDF (1567K) -
ERIC POSTAIRE, CLAUDE VIEL, DIDIER MARTINEZ, JOSEPH LIKFORMAN, MICHEL ...1987 Volume 35 Issue 10 Pages 4064-4067
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSPapaverine 1 was oxidized by vanadium pentoxide in 2.5 M aqueous sulfuric acid media to give four new compounds : 4-hydroxy-6-demethylpapaveraldine (3), 4-hydroxy-4'-demethylpapaveraldine (4), 3-hydroxy-6-demethylpapaveraldine (5) and 3-hydroxy-4'-demethylpapaveraldine (6). The structures were established on the basis of mass spectrometry, ultraviolet-infrared spectrometry, nuclear magnetic resonance measurements and also chemical correlation with papaveraldine 2.View full abstractDownload PDF (674K) -
HIROYUKI NAGANO, YOSHIHARU NAWATA, MASATOMO HAMANA1987 Volume 35 Issue 10 Pages 4068-4077
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSIn order to elucidate the mechanism of the 2-acetylation in the reaction of nicotinic acid 1-oxide (2a) with boiling acetic anhydride, thermal reactions and reactions with hot acetic anhydride have been explored with 3-X-pyridine 1-oxides (2). The former reactions of 2d (X =CONHAc), 2f (X = CONMeAc), 2h (X = CH2OAc) and 2j [X = CH (OAc) 2] result in recovery or decomposition. The latter reactions of 2c (X =CONH2), 2d, 2e (X =CONHMe), 2h and 2j bring about mainly deoxygenative α-acetoxylation, no 2-acetylation being noticed. However, the reaction of 2f with acetic anhydride affords 6, 7-dihydro-6-methyl-7-methylene-5H-pyrrolo [3, 4-b] pyridin-5-one 1-oxide (7) as an initial product, which further undergoes deoxygenative β-acetoxylation to give 7-acetoxy-7-acetoxymethyl-6, 7-dihydro-6-methyl-5H-pyrrolo [3, 4-b] pyridin-5-one (8) and 7-acetoxymethylene-6, 7-dihydro-6-methyl-5H-pyrrolo [3, 4-b] pyridin-5-one (9). On the basis of these results we propose a new electrophilic pathway for the 2-acetylation of 2a and 2f.View full abstractDownload PDF (1936K) -
TAKEO HIGASHINO, SUSUMU SATO, AKIRA MIYASHITA, TATSUHIKO KATORI1987 Volume 35 Issue 10 Pages 4078-4086
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe anion (A) of the Reissert compound (1, 5-benzoyl-4, 5-dihydro-1-phenyl-1H-pyrazolo [3, 4-d] pyrimidine-4-carbonitrile) was found to react with electrophiles in two ways. One is nucleophilic attack of the anion A. The other is self-decomposition of the anion A.
Thus, A underwent nucleophilic attack with aromatic and aliphatic aldehydes (4a-j), resulting in the formation of the corresponding α-aryl (or alkyl)-1-phenyl-1H-pyrazolo [3, 4-d] pyrimidin-4-ylmethyl benzoates (6a-j) together with 1-phenyl-1H-pyrazolo [3, 4-d] pyrimidine (2), the 4, 4'-dimer (7) of 2, Ο-benzoylaroins (8a-d), and Ο-benzoylcyanohydrins (9e-j). Nucleophilic substitution took place in the reaction of A with 2, 4-dinitrochlorobenzene (14a) and methyl iodide (14d), giving the 4- (2, 4-dinitrophenyl) derivative (17a) of 2 and 5, 7-dibenzoyl-4-methyl-l-phenyl-4-(1-phenyl-1H-pyrazolo [3, 4-d] pyrimidin-4-yl)-4, 5, 6, 7-tetrahydro-1H-pyrazolo [3, 4-d] pyrimidine-6-carbonitrile (19), respectively.
However, the anion A did not react with other aryl (or alkyl) halides (14b, c, e), ketones (11a, b), 2-alkenonitriles (21a, b), and dimethyl acetylenedicarboxylate (22), and underwent the known self-decomposition, resulting in the formation of products such as 2, 7, the cyano derivative (18) of 2, and the ester 6a.View full abstractDownload PDF (1481K) -
FUMIKO ABE, TSUNEATSU NAGAO, YUJIRO MORI, TATSUO YAMAUCHI, YASUHISA SA ...1987 Volume 35 Issue 10 Pages 4087-4092
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThree piscicidal pregnanes including two known defense substances of water beetles and four pregnane glycosides having the same aglycone as that of teikaside A were isolated from the roots of Apocynum venetum L. var.basikurumon HARA and their structures were determined.View full abstractDownload PDF (886K) -
HIROYUKI NAGANO, YOSHIHARU NAWATA, MASATOMO HAMANA1987 Volume 35 Issue 10 Pages 4093-4100
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSNicotinic acid 1-oxide (1) reacts with hot propionic anhydride to give 4-aza-3-ethyl-3-propionyloxy-1 (3H) -isobenzofuranone 4-oxide (2), 5-aza-3-methyl-4-propionyloxyisocoumarin (3), 4-aza-3-ethyl-3-propionyloxy-1 (3H) -isobenzofuranone (4), 4-aza-3-ethyl-3, 5-dipropionyloxyl (3H) -isobenzofuranone (5) and a mixture of 2- and 6-hydroxynicotinic acids (6 and 7). Product 2 is a 2-propionylation product of 1, and 3, 4 and 5 arise from further action of the anhydride on 2. Phenylacetic anhydride undergoes oxidative decarboxylation with 1 to give benzaldehyde and nicotinic acid. The reaction of 1 with benzoic anhydride affords a 2-benzoylation product, 4-aza-3- benzoyloxy-3-phenyl-1 (3H) -isobenzofuranone 4-oxide (12).View full abstractDownload PDF (1114K) -
HIROYUKI SAWANISHI, KAYOKO TAJIMA, TAKASHI TSUCHIYA1987 Volume 35 Issue 10 Pages 4101-4109
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSPhotolysis of 2-unsubstituted (5a-f) and 2, 4-disubstituted (5k, l) 3-azidopyridines in the presence of sodium methoxide resulted in ring expansion to give the 4-methoxy-5H-1, 3-diazepines (8 and 18), presumably via the azirine intermediates 6 and 17 derived from the initially formed singlet 3-pyridylnitrenes by cyclization at the 2-position of the pyridine ring. On the other hand, in the photolysis of 2-substituted 3-azidopyridines (5g-j), the cyclization of the nitrenes occurred predominantly at the vacant 4-position giving rise to the 3-methoxy-2H-1, 4-diazepines (13).View full abstractDownload PDF (1704K) -
HARUKI SASHIDA, AKIRA FUJII, TAKASHI TSUCHIYA1987 Volume 35 Issue 10 Pages 4110-4116
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSIrradiation of the 3-azidoquinolines (6a-c) in the presence of sodium methoxide resulted in ring expansion to give the fully unsaturated 3-methoxy-3H-1, 4-benzodiazepines (8). Further treatment of the 2-unsubstituted 3H-1, 4-benzodiazepine (8a) with sodium methoxide in methanol gave the solvent adduct 7, which reverted to 8a on being refluxed in benzene, whereas the 2- substituted 3H-1, 4-benzodiazepines (8b, c), upon treatment with sodium methoxide, underwent tautomerization to afford the 5H-1, 4-benzodiazepines (15). Some reactions of the new 1, 4- benzodiazepines (8 and 15) thus obtained were also examined.View full abstractDownload PDF (1161K) -
HIROSHI OHTAKA, GORO TSUKAMOTO1987 Volume 35 Issue 10 Pages 4117-4123
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe quantitative structure-activity relationships of 1-benzyl-4-diphenylmethylpiperazines for cerebral vasodilating activity and duration of action were examined. The analyses indicate that increase of the electron density on the benzylic nitrogen atom and the introduction of sterically small substituents at the para position of the diphenylmethyl moiety bring about strong interactions of the molecule with the active site and result in high potency as well as prolonged action.View full abstractDownload PDF (987K) -
HIROSHI OHTAKA, TOSHIRO KANAZAWA, KEIZO ITO, GORO TSUKAMOTO1987 Volume 35 Issue 10 Pages 4124-4129
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSAs a lead development based on the previous quantitative structure-activity relationship (QSAR) results on cerebral vasodilating activities of 1-benzyl-4-diphenylmethylpiperazines, 1- cinnamyl-4-diphenylmethylpiperazines having electron-donating groups on the cinnamyl moiety were designed. Two methods of synthesis were developed. As expected from the QSAR results, these compounds exhibited stronger potency and longer-lasting effect than cinnarizine and flunarizine.View full abstractDownload PDF (764K) -
KAZUO OGAWA, TADAFUMI TERADA, YOSHIYUKI MURANAKA, TOSHIHIRO HAMAKAWA, ...1987 Volume 35 Issue 10 Pages 4130-4136
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESS2- (1, t- and c-4-Dialkylcyclohex-r-1-yl) -2-oxoethyl arenesulfonates, 2- (4, 4-dialkylcyclohex-1-yl) -2-oxoethyl arenesulfonates and related compounds were synthesized and evaluated for esteraseand chymotrypsin-inhibitory activities in vitro and for hypolipidemic effect in vivo. The transisomers of 2- (1, 4-dialkylcyclohex-1-yl) -2-oxoethyl arenesulfonates showed much more potent esterase-inhibitory action (about 13 to 6200 times) than the cis-isomers as well as more potent hypolipidemic action (about 1.5 to 10 times) but the chymotrypsin-inhibitory actions of the two isomers were similarly low. On the other hand, the 2-oxoethyl arenesulfonates having a 4, 4- disubstituted cyclohexane ring mostly exhibited potent esterase-inhibitory action (order of IC50; 10-8 to 10-9M) and marked hypolipidemic effect (78% to 95% reductions of plasma triglyceride).View full abstractDownload PDF (1074K) -
SUHAIL AHMAD, SHOICHIRO OZAKI, TOSHIO NAGASE, MASAAKI IIGO, REIKO TOKU ...1987 Volume 35 Issue 10 Pages 4137-4143
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSAntitumor-active derivatives of 5-fluorouracil were prepared via a new method by introducing an acyloxymethyl group at the 1-, 3-, or 1, 3-position (s). These derivatives were obtained by condensing 1, 3-bis (hydroxymethyl) -5-fluorouracil with various short-/long-chain carboxylic acids or their derivatives, in the presence of dicyclohexylcarbodiimide and a catalytic amount of N, N-dimethylaminopyridine. Some of the derivatives showed strong antitumor activity against the leukemia L1210 system when administered orally.View full abstractDownload PDF (1120K) -
IWAO MORITA, KATSUTOSHI KUNIMOTO, MASAMI TSUDA, SHIN-ICHI TADA, MASAHI ...1987 Volume 35 Issue 10 Pages 4144-4154
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA series of 1, 4-dihydropyridine-5-cyclic phosphonate derivatives, designed as analogues of 1, 4- dihydropyridine-3, 5-dicarboxylate calcium antagonists, was synthesized and examined for antihypertensive activity. Several compounds were proved to have activities superior or comparable to that of nifedipine in lowering blood pressure in normotensive and spontaneously hypertensive rats (SHR). Among these compounds, methyl 2, 6-dimethyl-5- (2-oxo-1, 3, 2-dioxaphosphorinan-2-yl) -4- (2-nitrophenyl) -1, 4-dihydropyridine-3-carboxylate (31, DHP-218) was approximately 7 times more active than nifedipine in SHR and was selected for further development and clinical evaluation. The structure-activity relationships are discussed.View full abstractDownload PDF (2072K) -
TENJI KONISHI, YOKO NARUMI, KAZUAKI WATANABE, SHIU KIYOSAWA, JUNZO SHO ...1987 Volume 35 Issue 10 Pages 4155-4161
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSTwo iridoid glucosides, namely boschnaloside (1), and boschnaside (2), (+) -pinoresinol-β-D-glucopyranoside (3), a new oligosaccharide (=β-D-glucopyranosyl (1→4) -α-L-rhamnopyranosyl- (1→3) -D- (4-O-caffeoyl) -glucopyranose) (4), and a new phenylpropanoid glycoside named rossicaside A (5) have been isolated from Boschniakia rossica FEDTSCH. et FLEROV (Orobanchaceae) and their structures have been determined.View full abstractDownload PDF (1223K) -
MARIKO TANOGUCHI, MASAO ARIMOTO, HIDEYUKI SAIKA, HIDEO YAMAGUCHI1987 Volume 35 Issue 10 Pages 4162-4168
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThree kinds of lignans, including a new lignan, named hernolactone, were isolated from the seeds of Hernandia ovigera L. besides six previously reported lignans, desoxypodophyllotoxin (DPT), desoxypicropodophyllin, bursehernin, podorhizol, hernandin and dehydro-DPT. The structure of hernolactone was determined as (2R, 3R) -3- (4′-hydroxy-3′, 5′-dimethoxybenzyl) -2- (3″, 4″, 5″-trimethoxybenzyl) -γ-butyrolactone (IV) and the other two lignans were identified as (-) -yatein ((-) -deoxypodorhizon) (V) and dehydropodophyllotoxin (IX).View full abstractDownload PDF (1106K) -
TOSHIO TASHIMA, URAO KAWAKAMI, MICHIKO HARADA, TOORU SAKATA, NOBUKATSU ...1987 Volume 35 Issue 10 Pages 4169-4180
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSCommercially available aqueous solutions of glutaraldehyde (GA) sometimes contain GA polymers as impurities which can cause undesirable effects. We found new type oligomers present in a GA solution as impurities and isolated them by reverse-phase high performance liquid chromatography. These compounds were identified as GA trimer, pentamer and heptamer having a 1, 3, 5-trioxane skeleton. In particular, GA trimer, 2, 4, 6-tris (4-oxobutyl) -1, 3, 5-trioxane, was named “paraglutaraldehyde” (para-GA). These compounds showed absorption maxima at 280 nm (the same position as GA), and hence could not be distinguished from GA itself by the conventional ultraviolet absorption method. These impurities were not detected in highly purified GA solution after storage under the conditions of practical use. Accordingly, these oligomers seemed to be formed by the intermolecular cyclization of GA monomer during the processes of synthesis.View full abstractDownload PDF (1823K) -
MASAMI HORIKOSHI, YOSHINOBU NAKANISHI, SHOJI HIRASHIMA, MASAHIKO OHTSU ...1987 Volume 35 Issue 10 Pages 4181-4187
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSRecently, casein kinase II was suggested to play a role in accurate transcription in vitro (R. Zandomeni, M. C. Zandomeni, D. Shungar, and R. Weinmann, J. Biol. Chem., 261, 3414 (1986)). In the present study, we examined whether transcription factor S-II is a target of casein kinase II, because the phosphorylated form of S-II, termed S-II', is known to be present in vivo. We found that S-II was phosphorylated by casein kinase II purified from Ehrlich ascites tumor cells, and showed that this reaction was inhibited by 5, 6-dichloro-1-β-D-ribofuranosylbenzimidazole (DRB). DRB also inhibited accurate transcription of the adenovirus major late gene in a nuclear lysate of Ehrlich ascites tumor cells, as it has been found to do in a HeLa cell lysate. This inhibition of transcription was partly restored by addition of purified casein kinase II, but not S-II', to the reaction mixture.View full abstractDownload PDF (5003K) -
SATOSHI ISHII, HIDEMI ISHII, TAKAFUMI WATANABE, TETSUYA SUGA1987 Volume 35 Issue 10 Pages 4188-4193
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSHepatic peroxisomes from 20-d-old chick embryo were purified by sucrose density gradient centrifugation. The specific activities of catalase and D-amino acid oxidase (DAAO) in the peroxisomal fraction were 24- and 32-fold, respectively, higher than those in the homogenate. The isolated peroxisomes included activities of 85.5 and 416 nmol/min/mg protein of carnitine palmitoyltransferase (CPT) and carnitine acetyltransferase (CAT), respectively. CPT was easily solubilized by treatment with Tween 20 or sonication from the peroxisomes, being similar in this respect to catalase. On the other hand, CAT was more resistant to solubilization, behaving similarly to DAAO. These results indicate that CPT as well as catalase is located in the peroxisomal matrix in a soluble form, and that CAT as well as DAAO is weakly associated with some insoluble components.View full abstractDownload PDF (898K) -
YOSHIO INOUYE, MOTOHIRO NISHIMURA, YASUCHIKA MATSUDA, HIDEMI HOSHIKA, ...1987 Volume 35 Issue 10 Pages 4194-4202
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSSarcosine oxidase (EC 1.5.3.1) produced by Streptomyces sp. KB210-8SY was purified by ion exchange chromatography on DEAE-sepharose CL-6B, affinity chromatography on sarcosyl-AH-sepharose 4B and gel filtration on sephadex G-150 to electrophoretic homogeneity.
The molecular weight of the enzyme was estimated to be 44000 by sodium dodecyl sulfate (SDS) -polyacrylamide gel electrophoresis and gel filtration on Sephadex G-150. The enzyme showed the maximum activity at pH 8 and was stable at pH 7-9. In addition to sarcosine, the enzyme oxidized N-methyl-L-leucine, N-methyl-DL-alanine and N-methyl-DL-valine to lesser extents. The apparent Km values for sarcosine, N-methyl-L-leucine, N-methyl-DL-alanine and N-methyl-DL-valine were 0.91, 0.58, 1.6 and 6.7 mM, respectively. The enzyme was inactivated by N-bromosuccinimide, hydroxylamine hydrochloride, SDS, Zn2+, Ni2+ and Hg2+ but not by ethylenediaminetetraacetate, p-chloromercuribenzoate or p-toluenesulfonyl chloride.
The taxonomic characteristics of strain KB210-8SY are closely related to those of Streptomyces flavovirens and S. misakiensis.View full abstractDownload PDF (3291K) -
RYOTA KUROKI, NAOE KANESAKA, HIDENORI YAMADA, TAIJI IMOTO1987 Volume 35 Issue 10 Pages 4203-4207
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSReactivities of various amines in the modifications of acetic acid and Asp-101 of hen egg-white lysozyme in the carbodiimide (1-ethyl-3 [3- (dimethylamino) propyl]carbodiimide hydrochloride (EDC)) reaction were investigated at pH 5.0 and room temperature. The reactivity of an amine towards EDC-activated Asp-101 was at least 50 times higher than that towards EDC-activated acetic acid. Such a high efficiency of modification of Asp-101 could not be explained only by the EDC-binding mechanism in which the EDC molecule binds to the active site cleft of lysozyme close to Asp-101 to activate Asp-101 selectively [R. Kuroki, H. Yamada, and T. Imoto, J. Biochem. (Tokyo), 99, 1493 (1986)]. Therefore, in addition to the above mechanism, an amine-binding mechanism in which an amine molecule binds to lysozyme close to the EDC-activated Asp-101 residue so as to increase the effective concentration of the amine by more than 50 times is proposed.View full abstractDownload PDF (811K) -
TAKAKO YOKOZAWA, TAEKO KOBAYASHI, HIKOKICHI OURA, YUJI KAWASHIMA1987 Volume 35 Issue 10 Pages 4208-4214
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe effects of ginsenoside-Rb2 on nitrogen compounds in streptozotocin-diabetic rats were investigated. A marked decrease in blood urea nitrogen level was observed in the ginsenoside-Rb2 administered group. Administration of ginsenoside-Rb2 induced increases of total protein and Lys, Gly, Glu, Arg, etc. in serum, while no significant change of serum albumin was observed. In the liver, the urea content was decreased with a concomitant increase of ribonucleic acid content. A quantitative study on the distribution of free and membrane-bound ribosomes indicated that the increase in ribosomes caused by the Administration of ginsenoside-Rb2 is mainly due to the increase in membrane-bound ribosomes. Ginsenoside-Rb2 exhibited a normalizing action on the hepatic concentrations of Glu, Thy, Phe, and Tyr. Furthermore, body weight significantly increased in diabetic rats receiving ginsenoside-Rb2, even though they took less food than the control group. Ginsenoside-Rb2 remarkably improved diabetic symptoms such as over-eating, polyuria, etc.View full abstractDownload PDF (1028K) -
MASAYOSHI YAMAGUCHI, NAOMI OGAWA1987 Volume 35 Issue 10 Pages 4215-4220
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe effect of calcitonin (CT) on adenosine-5'-triphosphate (ATP) synthesis in the hepatic mitochondria of rats was investigated. Administration of CT (80 MRC mU/100 g body weight) produced a marked elevation of ATP content in the hepatic cytosol. This increase was completely inhibited by administration of 2, 4-dinitrophenol (0.1 mg/100 g), an inhibitor of oxidative phosphorylation of mitochondria. Verapamil (1.0 mg/100 g) also inhibited the hormonal effect on hepatic ATP content. Moreover, administration of calcium chloride (2.0 and 4.0 mg Ca2+/100 g) elevated the cytosolic ATP content by about 1.8-and 2.3-fold, respectively. Meanwhile, administration of CT produced a remarkable increase of ATPase activity in the hepatic mitochondria. Calcium contents in both the liver and the mitochondria were raised by CT administration. The removal of the mitochondrial calcium by washing with 10 mM ethyleneglycol-bis (2-aminoethylether) -N, N, N', N'-tetraacetic acid (EGTA, pH 7.4) caused complete loss of the increase in mitochondrial adenosine triphosphatase (ATPase) activity induced by CT administration. The CT-increased ATPase activity was appreciably increased by addition of 10 and 50 μM Ca2+, but this increase was not altered by addition of 10 μM trifluoperazine or calmodulin (2.5 μg/ml). These results suggest that CT stimulates ATP synthesis in the hepatic mitochondria, and that the hormonal effect may be mediated through calcium, but not calmodulin.View full abstractDownload PDF (1013K) -
SHINGO NIIMI, TAKAO HAYAKAWA, TADASHI OSHIZAWA, ERIKO UCHIDA, TSUTOMU ...1987 Volume 35 Issue 10 Pages 4221-4228
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe efficient purification and characterization of the product of chemically synthesized human growth hormone (hGH) gene expressed in Escherichia coli are described. The product was purified from the cell lysates of the E. coli by means of ammonium sulfate precipitation, DE-52 chromatography, chromatofocusing chromatography and Ultrogel AcA 54 chromatography. The purified hGH gene product was homogeneous on sodium dodecyl sulfate-polyacrylamide gel electrophoresis, non-denaturing polyacrylamide gel electrophoresis, gel electrofocusing and high-performance liquid chromatography (HPLC). The purified product and an authentic methionyl hGH (m-hGH) showed identical behavior in these systems. The structural features of the purified product were examined by means of amino acid composition analysis, NH2-terminal sequence analysis and tryptic peptide mapping. The experimental values of the amino acid composition of the purified product were in agreement with the theoretical values for m-hGH. Its NH2-terminal sequence (39 amino acid residues) was identical with that of the published sequence of hGH, except for an additional amino-terminal methionine residue immediately preceding phenylalanine at residue 1. The elution profile of the tryptic peptides of the purified product on HPLC was identical with that of authentic m-hGH. These elution profiles were nearly identical with that of a pituitary-derived hGH, with the exception of one peak due to NH2-terminal peptide. On the basis of these results, the purified product was identified as m-hGH.View full abstractDownload PDF (2463K) -
GUI-MIN LUO, WEI LI, LIAN-XING ZHENG, YU-HUA CHENG, SUSUMU FUNAKOSHI, ...1987 Volume 35 Issue 10 Pages 4229-4234
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSIn a cell-free extract of Azotobacter vinelandii-230, at least four electromorphologically different components possessing superoxide dismutase activity were detected. One component was purified to homogeneity. The purified enzyme (molecular weight 43000) consists of two noncovalently interacting subunits of equal size. Metal analysis indicated the presence of iron, 2 mol/mol-dimer. The amino acid composition (ca. 153 residues) was determined.View full abstractDownload PDF (1834K) -
MASAYOSHI YAMAGUCHI, MASAJI IMASE1987 Volume 35 Issue 10 Pages 4235-4240
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe regulatory effect of calcitonin (CT) on succinate dehydrogenase in the hepatic mitochondria of rats was investigated. Administration of CT (80 MRC mU/100 g body weight) produced a significant increase in calcium content and a corresponding elevation of succinate dehydrogenase activity in the hepatic mitochondria. These increases were dose-dependent. CT also increased succinate dehydrogenase activity and calcium content in the hepatic mitochondria of thyroparathyroidectomized rats. The CT-induced increase in enzyme activity was completely reversed by treatment with 1.0 mM ethylene glycol bis- (2-aminoethylether) N, N, N', N'-tetraacetic acid (EGTA). The increased activity was restored by addition of Ca2+ (2.5-25 μM). Trifluoperazine (25 and 50 μM), a calmodulin inhibitor, completely prevented the increase in succinate dehydrogenase activity caused by CT. Insulin (1.0 U/100 g) also increased succinate dehydrogenase activity in the hepatic mitochondria by about 30% (p<0.01), while the enzyme activity was not elevated by thyroxine (10 μg/100 g). The effect of insulin on the enzyme activation was attributed to the elevation of mitochondrial calcium. The present result indicates that succinate dehydrogenase activity is regulated by CT, and that the effect may be mediated through an increase of calcium in the mitochondria.View full abstractDownload PDF (1053K) -
SEIJI MIYAUCHI, YUICHI SUGIYAMA, YASUFUMI SAWADA, TATSUJI IGA, MANABU ...1987 Volume 35 Issue 10 Pages 4241-4248
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSBy means of the multiple indicator dilution (MID) method, the sequestration process of 4-methylumbelliferone (4-MU), which is well known to be conjugated to glucuronide (4-MUG) and sulfate (4-MUS) in the rat liver, was found to be saturated as the dose was increased J. Pharmacokin. Biopharm., 15, 25 (1987). This observation might be attributed to the saturation of the conjugative metabolism. In the present study, using an in vivo tissue sampling single injection technique, we determined whether the sequestration process obtained by means of the MID method reflected the conjugative metabolism process. When the dose of 4-MU was increased from a low dose (110μg/rat) to a high dose (3200 μg/rat), FDapp, 4-MUS and FDapp, 4-MUG, which represent the fractions of the amounts of the formed 4-MUG and 4-MUS remaining in the liver, respectively, remarkably decreased. Since 4-MUG and 4-MUS formed from 4-MU have low diffusional clearances between the blood and hepatocytes, they are effectively trapped in the hepatocytes and therefore FDapp, 4-MUS and FDapp, 4-MUG represent the extents of the conjugative metabolism of 4-MU. Therefore, the dose-dependent change in the sequestration process was found to be attributable to the saturation of the conjugative metabolism. This observation confirms our previous hypothesis that the saturation of the sequestration process observed by using the MID method reflected that of the conjugative metabolism. Furthermore, according to the “sinusoidal” model, we simulated the time profiles of the amounts of drugs remaining in the liver, using parameters obtained from the MID data. The model, which has 20 sinusoidal compartments and can be regarded as identical to a “parallel tube” model, could reliably predict the time profiles of the amounts of drugs remaining in the liver.View full abstractDownload PDF (1187K) -
TOSHIAKI NAKAJIMA, YASUJI TAKASHIMA, KIN-ICHI IIDA, HARUMI MITSUTA, AT ...1987 Volume 35 Issue 10 Pages 4249-4254
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe absorption of indomethacin (IM) from suppositories containing surface-modified IM microcapsules (MC) after rectal administration in rabbits was investigated with the aim of producing sustained-release suppositories. The IM-MC were prepared by phase separation of ethylcellulose (EC) from cyclohexane, and the IM surface was modified with a carboxy-vinyl polymer (Hiviswako® 104, HW) by a dry blend technique before encapsulation.
As a sustained plasma level of IM was not obtained when IM-MC-containing suppositories which showed a zero-order release profile were administered, the factors affecting the IM absorption, that is, the EC and HW contents in the MC, and the suppository base and type, were investigated. The EC and HW contents in the MC affected the IM release rate but had little effect on the IM absorption. When the IM-MC were directly administered, the IM plasma level was significantly lower than that after administration of the macrogol base suppository containing the IM-MC. The area under the concentration-time curve (AUC) in the case of the Witepsol® base was smaller than that in the case of the macrogol one. The plasma concentration-time curve of the hollow-type suppository showed a lag time, and the Tmax was delayed by 1 h compared with that of the conventional suppository. Thus, it was found that a suitable kind and amount of suppository base and an appropriate suppository type should be selected to prepare sustained-release suppositories containing IM-MC.View full abstractDownload PDF (923K) -
YOSHINOBU NAKAI, KEIJI YAMAMOTO, KATSUHIDE TERADA, MANABU SAKAI1987 Volume 35 Issue 10 Pages 4255-4262
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSAcid-base properties of excipient surfaces have been studied by photoacoustic spectroscopy (PAS) in the visible absorption range using seven acid-base indicators. The acid strength (H0) of each excipient was determined from the PA spectral patterns of the indicators. The H0 values of silica-alumina, silica-magnesia and crystalline cellulose were determined to be between 3.3 and-3.0, between 4.8 and 2.0, and between 4.8 and 3.3, respectively. In the cases of some excipients, the acid strength measured by PAS was weaker than the value which was measured from the color changes of the indicators on the surface of the excipients in benzene solution. These differences are ascribed to water adsorption on the surface during PAS sample preparation. In the case of crystalline cellulose, the hydrogen bonding network was so tight in benzene solution that the indicators could not enter the network.View full abstractDownload PDF (925K) -
TARO OGISO, YOSHIMASA ITO, MASAHIRO IWAKI, HIDEHIKO ATAGO, CHIKAKO TAN ...1987 Volume 35 Issue 10 Pages 4263-4270
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSTo investigate quantitatively the percutaneous absorption of dexamethasone acetate (DA) and palmitate (DP), gel and petrolatum ointments were prepared and applied to rat skin. DA in the presence of absorption enhancers (Azone® and sorbitan monooleate) was rapidly absorbed, in the form of dexamethasone, through the skin, whereas the absorption after application of DA ointment without enhancers was relatively poor. DP was also efficiently absorbed in the presence and absence of enhancers, with bioavailability of 5.3 and 4.1%, respectively. The absorbed DP was slowly hydrolyzed in the systemic circulation. The percutaneous absorption of drugs from the petrolatum ointments with enhancers was slower than that from the gel ointments. The in vitro release rates of DA and DP from the gel ointments with enhancers were 7.3 and 6.1 mg/h1/2, respectively and were much higher than those from the petrolatum ointments. The partition coefficient of DP was much larger than that of DA. Thus, it is suggested that DA and DP gel ointments with enhancers are effective in terms of high absorption into the circulation.View full abstractDownload PDF (1211K) -
TOSHIAKI NISHIHATA, YUHKO NAKANO, MASARU YAMAZAKI1987 Volume 35 Issue 10 Pages 4271-4276
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSSustained-release tablets (SR-tablet), prepared with hydrogenated soya phospholipids, gave slow release of theophylline and sodium diclofenac into a solvent at pH 6.8, in an in vitro study. The release profile of theophylline from the SR-tablet remained unchanged at pH values between 2.0 and 6.8. However, the release of diclofenac from the SR-tablet into a solvent at pH 2.0 was very slight, due to the low solubility at pH 2.0. The release of both drugs seems to occur predominantly by a leaching mechanism, as proposed by Higuchi. The oral administration of SR-tablets to dogs avoided a transient peak of drug concentration in the plasma and maintained plasma drug concentrations at higher levels for a longer period, in comparison with the oral administration of theophylline in suspension form or a commercial tablet of sodium diclofenac.View full abstractDownload PDF (922K) -
CHIHIRO ITO, HIROSHI FURUKAWA1987 Volume 35 Issue 10 Pages 4277-4285
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSEight new coumarins, peroxyauraptenol (1b), cis-dehydroosthol (2), murraol (3), murranganon (4a), isomurranganon senecioate (5), murrangatin acetate (6b), isomurralonginol acetate (7b), and chloticol (8), were isolated from leaves of Murraya exotica L. (Rutaceae), and their structures were elucidated. Seventeen known coumarins were also characterized. However, no alkaloid was detected.View full abstractDownload PDF (1670K) -
TADASHI KIHO, MASAHIKO ITO, KATSUYUKI NAGAI, CHIHIRO HARA, SHIGEO UKAI1987 Volume 35 Issue 10 Pages 4286-4293
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA water-insoluble glucan (N-5P), [α] 23D +2.3° (c= 0.51, 0.5 M sodium hydroxide), was isolated from the alkaline extract of the fruit bodies of Yu er (Chinese name) (Auricularia species). N-5P was homogeneous as judged by gel filtration and electrophoresis. By gel filtration, the molecular weight of N-5P was estimated to be 5.6 × 105. The 13C-nuclear magnetic resonance and infrared spectra, together with the result of chromium trioxide oxidation, indicated that glucosidic linkages in N-5P have the β-D configuration. From the results of methylation analysis, periodate oxidation, Smith degradation (complete, as well as partial), partial acetolysis, and enzymic hydrolysis, it was concluded that N-5P has a main chain composed of β- (1→3) -linked D-glucopyranosyl residues, with single, β- (1→6) -linked D-glucopyranosyl groups attached as side chains, which account for a quarter of the total sugar residues. In addition, the results of enzymic hydrolysis indicated that the β- (1→6) -linked D-glucosyl side chains are mainly localized in the neighborhood of the nonreducing end of the main chain. Furthermore, N-5P showed potent antitumor activity against the solid form of sarcoma 180 in mice, and exhibited significant carbon clearance-enhancing activity in mice.View full abstractDownload PDF (1363K) -
TOKUJIRO KITAGAWA, HIROKO KURODA, HIDEAKI SASAKI, KOICHI KAWASAKI1987 Volume 35 Issue 10 Pages 4294-4301
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSAliphatic, aromatic, and heteroaromatic carboxylic acids react with 1, 1'-oxalyldiimidazole (1) or 1, 1'-oxalyldi (1, 2, 4-triazole) (2) in acetonitrile for 40min at 40 °C to give the corresponding 1-acylazole intermediates (11), which promptly undergo aminolysis and alcoholysis to form amides (13) including dipeptides (14), esters (16), and thioesters (19). These findings show that both 1 and 2 can be utilized as condensing reagents for the synthesis of carboxylic acid derivatives.View full abstractDownload PDF (936K) -
YOSHIO NIIMI, TAKAHIKO TSUYUKI, TAKEYOSHI TAKAHASHI, KAZUHIRO MATSUSHI ...1987 Volume 35 Issue 10 Pages 4302-4306
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSTwo new quassinoid glycosides, shinjuglycosides E and F, were isolated from the root bark of Ailanthus altissima SWINGLE and their structures were established to be 2-O- (β-D-glucopyranosyl)-2α, 11α, 12α-trihydroxypicrasane-1, 16-dione and 2-O- (β-D-glucopyranosyl) -2α, 12β-dihydroxy-picrasane-1, 11, 16-trione, respectively.View full abstractDownload PDF (685K) -
KOJI IUCHI, MASAHIRO NITTA, TAKASHI TANAKA, KEIZO ITO, YASUO MORIMOTO, ...1987 Volume 35 Issue 10 Pages 4307-4313
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSEleven C-terminal fragment peptides of cholecystokinin (CCK) which contain a O-sulfated tyrosine residue [CCK (27-32), CCK (27-31), CCK (27-31) amide, CCK (27-30), CCK (27-30) amide, CCK (27-29), CCK (27-29) amide, CCK (26-27), CCK (26-27) amide, CCK (25-27) and CCK (25-27) amide] were prepared by the solution method. The syntheses of these peptides were carried out by stepwise condensation in combination with fragment condensation. Analgesic effects of these fragment peptides were measured by means of the writhing test. The ED50 value of CCK (27-32) was 9.1 mg/kg and that of CCK (25-27) was 7.5 mg/kg, but the other synthetic peptides produced no statistically significant response at a dose of 8 or 10 mg/kg.View full abstractDownload PDF (1222K) -
TADATAKA NORO, KAZUKO NORO, TOSHIO MIYASE, MASANORI KUROYANAGI, KAORU ...1987 Volume 35 Issue 10 Pages 4314-4316
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSInhibitory activities of nine anthraquinone derivatives against xanthine oxidase (EC 1.2.3.2) were assayed in vitro. Anthragallol (1, 2, 3-trihydroxyanthraquinone, 8) was the most active inhibitor among them. The concentration of 8 in the assay mixture required to give 50% inhibition (IC50) was 1.2 × 10 -5 M. The type of inhibition by 8 with respect to xanthine as a substrate was uncompetitive.View full abstractDownload PDF (441K) -
ATSUSHI HIRAOKA, KUNIJIRO YOSHITAMA, TAKASHI HINE, TSUGUO TATEOKA, TAK ...1987 Volume 35 Issue 10 Pages 4317-4320
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA new system for the rapid and microscale analysis of flavonoids has been established using capillary isotachophoresis. Under the conditions employed, authentic flavonoids examined were clearly separated into individual zones, and the compounds in plant extracts could also be identified on the basis of enhancement of the appropriate zones in runs involving mixed charging of extracts with the authentic samples. This new technique seems to be useful for the detection of rutin (quercetin-3-O-rhamnoglucoside), which is a taxonomical marker in the genus Calamagrostis (Poaceae), in large numbers of plant specimens of this taxa on a micro scale.View full abstractDownload PDF (613K) -
GENJIRO KUSANO, AKIRA TAKAHASHI, SHIGEO NOZOE, YOSHIKO SONODA, YOSHIHI ...1987 Volume 35 Issue 10 Pages 4321-4323
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe effects of several solanum steroidal alkaloids on cholesterol biosynthesis from 24, 25- dihydrolanosterol by 10000 × g supernatant fluid of rat liver were examined. Solacongestidine (I), solafloridine (II) and solasodine (III) (40 μM each) exhibited considerable inhibitory effects (59, 51, 37% inhibition, respectively) on the synthesis of cholesterol from [24, 25-3H] -24, 25-dihydrolanosterol (18 μM). The biological importance of the inhibitory properties of the steroidal alkaloids is discussed.View full abstractDownload PDF (513K) -
TOSHIHIRO FUJII, HARUO ASAI, YUKIHIRO MIYASAKA, TATSUO SUZUKI, YOSHIYU ...1987 Volume 35 Issue 10 Pages 4324-4327
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSS100 protein exhibited an inhibitory effect on the adenosine triphosphatase activity of brain microtubule proteins in a concentration-dependent manner. In the presence of Ca2+, maximal inhibition was about 90% (only about 10% of the original activity remained), while the maximum inhibition in the presence of Mg2+ was about 30%. Zn2+, which can bind both microtubule proteins and S100 protein, had little effect on the inhibitory action of S100 protein in the presence or absence of Ca2+. The inhibition by S100 protein was reduced by chlorpromazine.View full abstractDownload PDF (546K) -
MAKOTO BANNAI, TOSHIO MAZDA, YOSHIHIDE ISHIKAWA, SHIGERU SASAKAWA1987 Volume 35 Issue 10 Pages 4328-4331
Published: October 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSRecovery of adenosine diphosphate aggregability of stored platelets took place after incubation at 37°C with Tyrode/bovine serum albumin solution as well as with fresh plasma. However, recovery with plasma from platelet concentrate (PC) stored in ordinary polyvinyl chloride bags was less, and the extent of the decrease depended upon the length of storage. The level of recovery with stored PC plasma, containing leached di- (2-ethylhexyl) phthalate (DEHP), was the same as that of fresh plasma to which DEHP had been added at the same concentration as found in the stored PC plasma. These results indicate that DEHP leached into the plasma of stored PC suppresses aggregability recovery. This suppression by DEHP is reversible.View full abstractDownload PDF (607K)