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Volume 105, Issue 3
Displaying 1-13 of 13 articles from this issue
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YUKIO SUGIURA1985 Volume 105 Issue 3 Pages 199-209
Published: March 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSBiometallochromophores are involve in some fundamental biological processes such as electron strage and transfer (Fe, Cu), dioxygen binding and activation (Mn, Fe, Cu), and substrate activation and catalysis (Mn, Fe, Co, Ni, Cu, Zn, Mo). The properties of metal ions which play an important role in active sites of biometallochromophores provide a useful information for the relation between the chemical structures and biological function of these metal-containing amino acids, peptides, and proteins. In addition, antitumor antibiotic bleomycin also requires iron ion for its deoxyribonucleic acid cleavage action and indeed bleomycin-iron complex is capable of oxygen activation. This review has been discussed on structures and functions of biometallochromophores.View full abstractDownload PDF (1091K) -
HISASHI YAMAMOTO1985 Volume 105 Issue 3 Pages 210-223
Published: March 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSWith the aid of selected examples an overview is given of the development trends in highly discriminative reactions using main-group metallorganics. 1) A new approach has been demonstrated for the selective synthesis of β-hydroxyl acetylenes with high optical purities. 2) A highly chemo- and stereoselective cleavage of acetals derived from 2 (R), 4 (R)-2, 4-pentanediol with organoaluminum and titanium reagents has been demonstrated. 3) Biogenetic type asymmetric synthesis of limonene and bisabolenes has been accomplished with a high degree of enantioselectivity.View full abstractDownload PDF (872K) -
MINORU UENO, ATSUSHI OHKUMA, HIROSHI KIKUCHI, SHIGEMITSU OHSAWA, KOHIC ...1985 Volume 105 Issue 3 Pages 224-231
Published: March 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSSingle bilayer liposomes (SUV type) were prepared by the injection method of ethanol solution of egg lecithin. Particle sizes of the liposome were measured at 25°C by submicron particle sizer (Malvern) at intervals of a few days to know effects of several additives such as macrogol, soybean oil and DL-α-tocopheryl acetate, under the conditions that homogeneous and stable liposomes are obtained without additives. The particle size became smaller by the addition of macrogol and the liposome became more stable by the addition of soybean oil. The amount of DL-α-tocopheryl acetate in liposome solutions was found to be very high. The peak value at particle size distribution obtained from particle sizer coincided with that from the transmission electron micrographs.View full abstractDownload PDF (922K) -
TOKUNARU HORIE, HIROKI KOURAI, MASAO TSUKAYAMA, MITSUO MASUMURA, MITSU ...1985 Volume 105 Issue 3 Pages 232-239
Published: March 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSSelective dealkylation of the 5-methoxyl group on the 6-hydroxy-5, 7-dimethoxy- and 5, 6, 7-trimethoxyflavones and of the benzyloxyl groups on the 5, 6, 7-tris (benzyloxy) flavones was studied and the following results were obtained. (1) The 5-methoxyl group on the flavones lacking hydroxyl groups or the acetates of the flavones having hydroxyl groups was selectively split with an excess of ca. 5% (w/v) anhydrous aluminum chloride-acetonitrile at 60°C for 1-1.5 h to give quantitatively the corresponding 5-hydroxyflavones. The method is available for the synthesis of 5-hydroxyflavones having 6-hydroxyl or 6-methoxyl groups. (2) The benzyloxyl groups at both the 5- and 6-positions on the 5, 6, 7-tris (benzyloxy) flavones were selectively split with conc hydrochloric acid in acetic acid to give the corresponding 7-benzyloxy-5, 6-dihydroxyflavones. (3) Pectolinarigenin, eupatilin, and 5, 7-dihydroxy-3', 4', 5', 6-tetramethoxyflavone were synthesized from the corresponding 5, 6, 7-trihydroxyflavones by these methods.View full abstractDownload PDF (783K) -
MASAO FUJITA, TAKAO INOUE, MASAHIRO NAGAI1985 Volume 105 Issue 3 Pages 240-248
Published: March 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSO-Methylation effects on carbon-13 nuclear magnetic resonance chemical shifts (in DMSO-d6) of o-, p-disubstituted phenols were investigated. In phenols (7-24), o-substituted phenols with another substituent conjugated to the benzene ring at para position, O-methylation caused downfield shifts by averages 1.1, 1.0 and 0.8 ppm for ipso-C (C-1), substituted ortho-C (C-2) and para-C (C-4) respectively, and upfield shifts by averages 1.1, 0.6 and 4.5 ppm for meta-C's (C-3 and C-5) and ortho-methine C (C-6) respectively. The trend of O-methylation effect on ipso-C (a smaller downfield shift) and meta-C's (larger upfield shifts) was different from that reported on o-substituted phenols with a proton or a nonconjugated substituent at para position ; however this trend was observed also on O-methylation of p-monosubstituted phenols (1-6). The regularity of a downfield shift by about 1.0 ppm for substituted ortho-C and an upfield shift by about 4.1-4.5 ppm for ortho-methine C was found to be held not only on O-methylation of o-monosubstituted phenols but also on that of o-substituted phenols with other substituents at meta and/or para positions. The above results were successfully applied to the 13C-NMR spectral interpretation of some natural products including coumarins (25-35) and flavonoids (36-42).View full abstractDownload PDF (975K) -
JOHJI YAMAHARA, TOKUNOSUKE SAWADA, HAJIME FUJIMURA, MASAO OKAMOTO1985 Volume 105 Issue 3 Pages 249-255
Published: March 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe analgesic and sedative effects of tetrahydropalmatine, tetrahydroberine and tetrahydroisoquinoline derivatives have been recognized. In order to discover new derivatives of tetrahydroisoquinoline with pharmacological properties similar to tetrahydropalmatine and with a simpler, easily synthesizable structure, several new derivatives of tetrahydroisoquinoline were synthesized. They were examined for their anti-inflammatory effect and analgesic effect in mice using Whittle's method and for their antipyretic effect in rats with endotoxin. 2-Amino-1, 2, 3, 4-tetrahydroisoquinoline-1, 3-dione was found to possess equally effective anti-inflammatory and analgesic properties as the reference drug, aminopyrine. It was found that this compound at 25 mg/kg, p. o. was as effective in its antipyretic action as aminopyrine at 100 mg/kg, p. o. Among other 13 new derivatives, 2-dimethylaminoethyl-1, 2, 3, 4-tetrahydroisoquinoline-1, 3-dione was also found to possess a similar degrees of anti-inflammatory and analgesic effect as aminopyrine.View full abstractDownload PDF (545K) -
AYA NITTA1985 Volume 105 Issue 3 Pages 256-270
Published: March 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSFormosan cinnamon bark on Osaka market and cinnamon on Formosan market were examined histologically in comparing with some bark specimens from Formosa, Cinnamomum pseudo-loureirii, and also collected in Japan, 'Yabunikkei', C. insularimontanum, syn. C. japonicum, 'Nikkei', C. sieboldii MEISN., syn. C. loureirii auct. Jap. non NEES, 'Kusunoki', C. camphora, 'Marubanikkei', C. daphnoides and 'Shiba-nikkei', C. daphnoides subsp. Doederleinii. Six kinds of marketed material named 'Yukei', ?? ??, 'Kohkei', ?? ??, 'Keitsu', ?? ??, 'Keishin', ?? ??, 'Keihi', ?? ?? and 'Hai-fang keitsu', ?? ?? ?? ??, were all C. cassia PRESL. Formosan cinnamon had three types, F-3 was identical with C. randaiense, F-2 presumed as C. osmophloeum and F-1 fitted to C. insularimontanum and/or C. sieboldii, which were not able to be distinguished in inner structure only. There was no material which has the same structure as C. pseudo-loureirii sent from Formosa. The difference of intraspecies in C. insularimontanum and in C. sieboldii was also presumed to be bigger than that found in these two species. Inner structure of another bark specimens was discussed in connection with external characters.View full abstractDownload PDF (4576K) -
SHIGEYUKI USUI, AKIRA HARA, TOSHIHIRO NAKAYAMA, HIDEO SAWADA1985 Volume 105 Issue 3 Pages 271-277
Published: March 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSMembrane lipids affecting guinea pig liver microsomal carbonyl reductase were investigated. The reductase in microsomes treated with 67% acetone was activated about three times that of intact microsomes, and inhibited by the addition of acetone-extracted lipids. The fatty acids, such as palmitic acid, stearic acid and oleic acid which were detected in acetone-extracted lipids, strongly inhibited the reductase in acetone-treated microsomes and the purified reductase, and the Ki value of palmitic acid for the purified reductase was 50 μM. These fatty acids may be able to regulate the reductase activity physiologically. On the other hand, the activity of reductase was inactivated by phospholipase treatment and delipidation of microsomes with sodium deoxycholate, and recovered by the addition of phospholipids (e. g. lysophosphatidylcholine, sphingomyelin and phosphatidylcholine) in phospholipase-treated and delipidated microsomes. The purified reductase was reactivated by phospholipids such as lysophosphatidylcholine, phosphatidylserine and phosphatidylcholine. Triton X-100 also gave a similar effect to phospholipid, and was able to be substituted for phospholipid in supporting the reducatse activity. These results indicate that the membrane lipids take part in carbonyl reductase activity.View full abstractDownload PDF (787K) -
YOSHITERU WATANABE, KAZUTOSHI YOKOYAMA, MICHINOBU YAMAJI, FUMIKO TANAK ...1985 Volume 105 Issue 3 Pages 278-283
Published: March 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe hollow cavities of suppositories made from oily-base material (Witepsol H-15) were filled up with indomethacin (IDM) in the following 4 forms : IDM fine powder (I), IDM physically mixed powder with lactose (II), IDM in propylene glycol (PG) suspension (III) and IDM in macrogol 300 solution (IV). The dissolution percentage of IDM and their releasing aspects were observed in vitro. By using I, after melting the base material of hollow type suppositoty, the released powder did not become wet easily and was difficult to diffuse into the solution. Therefore, IDM dissolved into the solution very slightly. By the use of II, IDM mixture powder dissolved into the aqueous solution a little faster than that by the case I, but no considerable improvement could be found. The difficulty in wetting was improved in III, but the dissolution was not perfect. In the case of IV, IDM dissolved more quickly and almost completely. Plasma concentration of IDM was measured in rabbits after the rectal administration of the suppositories including 50 mg of IDM in two kinds of hollow types, one of which had fine powder (I) and the other included macrogol 300 solution (IV) and two kinds of conventional types, one was prepared from oily-base material (V) and the other was made of water soluble base material (VI), with IDM. These data on bioavailability suggested that the hollow type suppository was superior to the conventional one made of the same kind of oily-base material. Furthermore, compared to the conventional type suppository made of water soluble base material (VI), the hollow type one including macrogol 300 solution (IV) could be expected to have an immediate effect, because its tmax was smaller than VI.View full abstractDownload PDF (685K) -
YOSHITERU WATANABE, YOSHITO TONE, MAYUMI SUZUKI, MITSUO MATSUMOTO1985 Volume 105 Issue 3 Pages 284-288
Published: March 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIn the previous report, it was proved that the hollow type suppository contained indomethacin (IDM) with macrogol 300 (M-300) solution had the largest area under the plasma concentration-time curve (AUC) after the rectal administration to rabbits. In this report, the effect of M-300 on bioavailability of hollow type suppositories made of Witepsol H-15, including IDM in their hollow cavities was estimated by changing the amount of M-300 in rabbits. When the content of IDM in suppository was changed to 50 mg, 25 mg and then 12.5 mg while M-300 was being kept at the same amount of 0.5 ml, each of the AUC/dose parameter was similar in value, and no dependency on dose could be seen. Next, when IDM was kept at 25 mg and M-300 increased, AUC augmented depending on the increase of M-300 amount (16.6±3.1 h·μg/ml→29.9±4.8 h·μg/ml), but when M-300 increased more than 0.5 ml, AUC was not enhanced anymore. It was suggested that there is a suitable quantity in using M-300.View full abstractDownload PDF (641K) -
MASAYOSHI INOUE, HIROYOSHI TANAKA, KAZUHIRO SHIMA, KUNIHEI INAZU1985 Volume 105 Issue 3 Pages 289-295
Published: March 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe effect of organic solvent on the growth rate of cephalothin sodium (KF) after seeding in frozen solution was investigated. All of used solvents accelerated crystal growth of KF and it was found that the accelerative effect of solvent increased with an increase in dielectric constant of solvent. KF formed micelle in aqueous solution and the solvent lower the freezing temperature of the micelle and it can be assumed that the lowering of the freezing temperature of the micelle related to the volume of solvent existing in the micelle. Alcohol lower larger the freezing temperature of the micelle than ketone and nitrile, but the accelerative effect of alcohol on the growth rate was less than that of ketone and nitrile. The effect of the concentration of ethanol and acetone was investigated and it seemed that ethanol accelerated nucleation. Nevertheless, the accelerative effect of ethanol on the growth rate was less than that of acetone. These results suggested that simultaneous use of solvent having a different mode of action is effective for crystallization of KF in frozen solution by spontaneous nucleation.View full abstractDownload PDF (749K) -
YOSHINOBU NAKAI, KEIJI YAMAMOTO, KATSUHIDE TERADA, JUNICHI ICHIKAWA1985 Volume 105 Issue 3 Pages 296-299
Published: March 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSSublimation of benzoic acid from a mixture of benzoic acid and porous glass powder (controlled pore glass, CPG) was examined. A large quantity of benzoic acid was retained in the mixture after heating in vacuo depending on heating temperature and mixing ratio. Especially for a low mixing ratio the mixture showed a high remaining percent. It is evident that capillaries of CPG played an important role in the benzoic acid retention since benzoic acid sublimated completely from a mixture of benzoic acid and fine glass beads having no capillaries. CPG-benzoic acid mixture of a low concentration mixture of CPG showed hallow pattern on powder X-ray diffractograms and no heat of melting on thermograms. Since benzoic acid molecules scarcely adsorbed in the aqueous solution, the adsorption of benzoic acid in the CPG-benzoic acid mixture is characteristic in the solidgas phase. The CPG-benzoic acid mixture showed a high dissolution rate of benzoic acid in aqueous solution, especially in initial dissolution stage. From the results described above it is concluded that benzoic acid molecules adsorbed tightly on the wall of capillaries in gas phase and easily released from the mixture in aqueous solution.View full abstractDownload PDF (507K) -
HARUKI OISHI, YASUMICHI HATAYAMA, HIROMI SHIRAISHI, KAZUYA YANAGISAWA, ...1985 Volume 105 Issue 3 Pages 300-303
Published: March 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSAn attempt has been made to develop an automated instrument that measures the turbidity change in gelation reaction of a solution containing endotoxin and Limulus amoebocyte lysate, and quantifies endotoxin by determining gelation time of the sample. This instrument monitors the ratio R (t) of the sequential to the initial transmittance of up to 64 samples simultaneously and independently at 10 s increments. As the samples are stationarily incubated at controlled temperature of 37±0.5°C, the objective judgement of gelation is provided without any disturbance from sample vibration. Defining gelation time as the time required to obtain 5% decrease of R (t), the well correlated calibration curve was obtained for endotoxin concentration from 1 pg/ml to 100 ng/ml. The coefficients of variation of the calculated endotoxin concentration were 5.64 to 14.1%. The judgement of gelation by this method agreed well with that by the conventional gel-clot method when the proper measuring time (about a half of that by the conventional method) was selected.View full abstractDownload PDF (539K)
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