All issues
Predecessor
Volume 105, Issue 7
Displaying 1-12 of 12 articles from this issue
- |<
- <
- 1
- >
- >|
-
TETSUYA KAMATAKI1985 Volume 105 Issue 7 Pages 607-618
Published: July 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe occurrence of sex specific forms of cytochrome P-450 was discovered. One of each form of cytochrome P-450, namely P-450-male and P-450-female, was purified to electrophoretical homogeneity. The two cytochromes were distinguishable from each other in terms of spectral, catalytic, electrophoretic and immunochemical properties and N-terminal amino acid sequence. By the use of specific antibodies to these hemoproteins, P-450-male and P-450-female were found to be present in liver microsomes of male and female rats, and induced by testosterone and estradiol, respectively. These cytochromes appeared in rats with sexual maturation except that P-450-female appeared in a certain early period in male rats before P-450-male appeared. The synthesis of P-450-male was "imprinted"by neonatal testosterone. In old rats, P-450-female instead of P-450-male appeared in male rats in association with a decrease in the ratio of serum testosterone to estradiol leveles. The results of experiments on the effects of hypophysectomy and treatment with testosterone or estradiol showed that synthesis of P-450-female in female rats terminated by hypophysectomy, and alternatively P-450-male appeared even when estradiol was given to the hypophysectomized female rats. The results also showed the possibility that testosterone and estradiol affected drug metabolizing activities by effecting the actions to the livers although to much less extents.View full abstractDownload PDF (1408K) -
TADASHI NAKATA1985 Volume 105 Issue 7 Pages 619-633
Published: July 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSAcyclic stereoselection based on the stereoselective ketone reduction and its application to natural products synthesis are reviewed. 1) Highly stereoselective reductions of α-methyl-β-keto ester, α-methyl-β-hydroxy ketone, α, β-epoxy ketone, and α-hydroxy ketone with Zn (BH4)2 and α-silyloxy ketone with NaAlH2 (OCH2CH2OMe)2 are described. The relation between substitution pattern of ketone and stereoselectivity of the reduction are extensively studied. 2) Highly stereocontrolled method for the synthesis of 1, 3-syn and anti-polyols has been developed based on the stereoselective reduction of six-membered β-keto acetal and successive transthioacetalization. 3) The new methods developed in 1) and 2) have been successfully applied for the synthesis of natural products or related compounds : erythronolide A seco-acid derivative (43), oudemansin (46), antimycin A3 (47), blastmycinone (48), four synthons having three consecutive chiral centers (69-72), bicyclic acetal (75), and pederin (76).View full abstractDownload PDF (1066K) -
SHUNICHI NORO, FUMIYOSHI ISHII, YUKARI HARAGUCHI1985 Volume 105 Issue 7 Pages 634-639
Published: July 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSLecithin is a useful surfactant in many diverse fields, such as food, pharmaceutical, and cosmetic products. However, it has a few weakness properties, for example, as an easily oxidizable and change of brown color for a long stored time. In this study, egg phosphatide saturated by hydrogenation was selected as a surfactant instead of regular egg phosphatide and its emulsifying activity was examined for pharmaceutical emulsion bases. The emulsion stability was evaluated in terms of (1) particle size and its distribution, (2) rheological properties, (3) zeta potential and (4) separated rate of dispersed phase. The following results were obtained. (1) the particle size of emulsion prepared with phosphatide saturated by hydrogenation was smaller than that with usual phosphatide, and (2) phosphatide saturated by hydrogen has a better stability action on emulsion than un-saturated phosphatide.View full abstractDownload PDF (548K) -
TAKAO MURAKAMI, HARUKA MAEHASHI, NOBUTOSHI TANAKA, TOSHIKO SATAKE, TAD ...1985 Volume 105 Issue 7 Pages 640-648
Published: July 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe investigation of several species of genus Pteris (Pteris tremula R. BR., P. dactylina HOOK., P. angustipinna TAGAWA P. multifida POIR., P. grevilleana WALL. and P. cretica L.) afforded a new ent-kaurane type diterpene and two new indanone type sesquiterpenes in addition to the previously known compounds. Their structures were elucidated to be 12β-hydroxy-15-oxo-ent-kaur-16-en-19-oic acid β-D-glucopyranosylester (I), pterosin S 3-O-β-D-glucoside (III) and pterosin S 3-O-β-D-(4'-caffeoyl) glucoside (IV) mainly by spectroscopic methods.View full abstractDownload PDF (983K) -
TAKAO MURAKAMI, HIROSHI WADA, NOBUTOSHI TANAKA, TADAYUKI KURAISHI, YAS ...1985 Volume 105 Issue 7 Pages 649-654
Published: July 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSFrom the fronds of Davallia divaricata BLUME three new (-)-epicatechin glycosides were isolated and shown to be (-)-epicatechin 3-O-β-D-allopyranoside (I), (-)-epicatechin 3-O-β-D-(2"-trans-cinnamoyl) allopyranoside (II) and (-)-epicatechin 3-O-β-D-(3"-trans-cinnamoyl) allop ranoside (III), respectively. From the fronds of Nephrolepis auriculata (L.) TRIMEN and N. biserrata (SW.) SCHOTT, sequoyitol was isolated.View full abstractDownload PDF (633K) -
TAKAO MURAKAMI, NOBUTOSHI TANAKA, TOSHIKO SATAKE, YASUHISA SAIKI, CHIU ...1985 Volume 105 Issue 7 Pages 655-658
Published: July 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSUracil and uridine were isolated from the air-dried fronds of Colysis hemionitidea (WALL) PRESL. and Microsorium fortunei (MOORE) CHING. Their contents in the former fern were 1.6% and 1.3%, respectively. The latter fern contained also 3-carboxyesculetin, fern-9 (11)-ene, 24-methylenecycloartanyl acetate and 24-methylenecycloartanone.View full abstractDownload PDF (518K) -
MITSURU TANEMURA, SHINICHI KAIHO, KOJI MIZUNO, ISAO MATSUNAGA, SHUNICH ...1985 Volume 105 Issue 7 Pages 659-664
Published: July 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESS2, 2'-Iminodibenzoic acid derivatives (3) were synthesized and their hydroxyl radical scavenging action was measured. Compounds (3a, b, e, f and h) were found to have an excellent inhibitory effect on the accumulation of liver triglycerides induced by ethanol in rats. Energies of the highest occupied molecular orbitals of these compounds were calculated.View full abstractDownload PDF (603K) -
MASATO HORIUCHI, HIDEO TAKASHINA, TERUMICHI IWATANI, TADASHI ISO1985 Volume 105 Issue 7 Pages 665-670
Published: July 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSBiotransformation of N-(2-mercapto-2-methylpropanoyl)-L-cysteine (SA96), a dithiol compound developed as an anti-rheumatic, was studied in rats by oral administration. The two S-methylated compounds were isolated from urinary extract by chromatographic methods. By their nuclear magnetic resonance spectra and by comparison with authentic samples, they were identified as N-[2-methyl-2-(methylthio) propanoyl]-L-cysteine (SA679 : S-methylated compound at 2-mercapto-2-methylpropanoic acid moiety of SA96) and as S-methyl-N-[2-methyl-2-(methylthio) propanoyl]-L-cysteine (SA672 : S-methylated compound at both mercapto groups of SA96). However, it was demonstrated that N-(2-mercapto-2-methylpropanoyl)-S-methyl-L-cysteine (SA680), a compound S-methylated only at cysteine moiety of SA96, was absent in the urine. Additionally, (4R)-7, 7-dimethyl-6-oxo-tetrahydro-3H-1, 2, 5-dithiazepine-4-carboxylic acid (SA981 : intramolecular disulfide of SA96), was also detected in the blood and urine. On the basis of these results, the characteristics of metabolic fate of SA96 were discussed.View full abstractDownload PDF (649K) -
HIDEO TAKASHINA, MASATO HORIUCHI, SHOGO MIYAGI, OSAMU UEMURA, TADASHI ...1985 Volume 105 Issue 7 Pages 671-676
Published: July 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSMetabolism of N-(2-mercapto-2-methylpropanoyl)-L-cysteine (SA96), a dithiol compound developed as an anti-rheumatic, was studied in rats and dogs by quantitative determination of SA96 and some metabolites in the blood and urine, by using gas chromatographic and high performance liquid chromatographic techniques. 1) In both dogs and rats, when administering SA96 orally, SA96 and its metabolites appeared in the blood within 30 min, indicating rapid absorption of SA96 through the digestive tract. N-[2-Methyl-2-(methylthio) propanoyl]-L-cysteine (SA679), S-methyl-N-[2-methyl-2-(methylthio) propanoyl]-L-cysteine (SA672) and (4R)-7, 7-dimethyl-6-oxo-tetrahydro-3H-1, 2, 5-dithiazepine-4-carboxylic acid (SA981) were found in both species as metabolites in the blood and urine. 2) In both species, approximately 40% of the dose was recovered in the urine as unchanged SA96, SA679, SA672, SA981 and unknown disulfides within 24 h after oral administration. 3) There was found a species difference in the ratio of these metabolites. In rats, SA679 was the principal metabolite in both the blood and urine, while, in dogs, SA981 was the principal metabolite in the blood and unknown disulfides of SA96 in the urine.View full abstractDownload PDF (701K) -
SHIZUO NAKAJIN, MASAYUKI TAKAHASHI, MASATO SHINODA1985 Volume 105 Issue 7 Pages 677-684
Published: July 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe comparative study of activities of two enzymes, which were well known as a cleaving enzyme of C17-C20 bond of C21-steroids, one was a Δ16-C19-steroid synthetase and the other was a 17α-hydroxylase/lyase, located on testicular microsomes of neonatal pig, were achieved to clarify the property of Δ16-C19-steroid synthetase. Their activities were considerably inhibited by cytochrome P-450-inhibiting compounds such as SU 4885, SU 8000 and SU 10603, but were not inhibited by SKF 525A, o, P'DDD, aminoglutethimide. Furthermore, their activities were remarkably inhibited by CO, various inhibiting agents and temperature of preincubation. Under these experimental conditions, their enzyme activities were inhibited in the same degree. However, on optima for pH and ionic strength, Δ16-C19-steroid synthetase activity was apparently different from 17α-hydroxylase/lyase activity.View full abstractDownload PDF (1015K) -
TAKESHI KATO, HARUMITSU ISHII, MASAKAZU FUNADO, TAKAYUKI DOI, KIYOHISA ...1985 Volume 105 Issue 7 Pages 685-689
Published: July 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe analgesic and morphine-like properties of TAI-998 were compared with those of codeine. TAI-998 was slightly more potent than codeine in the phenylquinone writhing test, but was less potent than codeine in the hot plate test in mice. Unlike the situation with codeine, the analgesic action of TAI-998 was not antagonized by a narcotic antagonist, and TAI-998 showed additive effects to the analgesic activities of morphine and codeine in the hot plate test. The IC50 value of TAI-998, in competing for 3H-naloxone binding to rat brain homogenates was much higher than that of codeine. Codeine affected respiration, gastro-intestinal transfer of charcoal and body temperature, but TAI-998 did not.View full abstractDownload PDF (604K) -
TOSHIO YOKOI, TOHRU KIKUCHI1985 Volume 105 Issue 7 Pages 690-693
Published: July 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSFriedelan-3β, 28-diol was isolated from Pachysandra terminalis SIEB. et ZUCC. and identified as its diacetate.View full abstractDownload PDF (450K)
- |<
- <
- 1
- >
- >|