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Volume 35, Issue 12
Displaying 1-50 of 59 articles from this issue
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SABURO SHIMABAYASHI, HIDEJI TANAKA, MASAYUKI NAKAGAKI1987 Volume 35 Issue 12 Pages 4687-4694
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSConcentrations of phosphate ion ([Pi] f) and calcium ion ([Ca2+] f), liberated from the surface of synthetic hydroxyapatite (Ca10 (PO) 4) 6 (OH) 2; HAP) during the adsorption of cetylpyridinium ion (CP+) or cetyltrimethylammonium ion (CTA+), were determined as a function of the equilibrium concentrations of these surface active ions ([CP+] f or [CTA+] f). A part of CP+ or CTA+ was adsorbed by ion-exchange with calcium ion (Ca2+) on the surface of HAP, and the rest was adsorbed together with its counterion (Cl- or Br-). In the region below the critical micelle concentration (cmc), [Ca2+]f increased with an increase in the adsorbed amount of the surface active ion. On the other hand, [Pi] f decreased with an increase in [Ca2+] f to keep the solubility product of HAP (Ksp) constant. However, in the region above the cmc, [Pi] f increased with [CP+] f or [CTA+] f through the binding of phosphate ion (Pi) to the cationic micelles. The electroneutrality on the surface phase of HAP, the solubility product of HAP in the solution phase, and the counterion binding by micelles determined the relationship between [Pi] f and [Ca2+] f. The species of counterion of the surfactant (Cl- or Br-) affected the adsorbing and releasing behaviors : the release of Ca2+ due to the adsorption of CP+ and the release of Pi through its binding to CP+-micelles are more pronounced with cetylpyridinium chloride than with cetylpyridinium bromide. This result can be explained in terms of the affinity of the halide ion for CP+ in the micellar and adsorbed phases (Br->Cl-).View full abstractDownload PDF (1284K) -
YOSHIKAZU MATSUSHIMA, YOSHIKO NAGATA, YUKO TAMANO, SETSURO SUGATA, TAD ...1987 Volume 35 Issue 12 Pages 4695-4699
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSMetal chelate formation of N-pyridoxylidenehydrazine-N ', N '-diacetic acid (1) and related hydrazines in solution was studied by means of absorption spectroscopy. Compound 1 and N-pyridoxylidene-N'-methylhydrazine (2) in methanol formed Cu (II) chelates of the same spectral character, which indicated the chelation of the phenolate oxygen and the hydrazine nitrogen atoms to Cu (II). The compositions of the chelates were 1 : 1 for 1 and 1 : 2 for 2, indicating that 1 acts as a tri- or tetradentate ligand. N- (3-Hydroxy-4-pyridylmethylene) hydrazine-N', N'-diacetic acid formed a Cu (II) chelate similar to that of 1 but N-pyridoxylidene-N', N'-dimethylhydrazine and N-pyridoxylidene-N', N'-diphenylhydrazine did not form chelates under similar conditions. Addition of an equimolar or excess amount of Co (II), Ni (II), Zn (II), Cd (II) or La (III) salt to 1 in methanol gave rise to absorption assignable to the chelate of 1, whereas 2 did not form metal chelates under the same conditions. It was concluded that the iminodiacetic acid moiety of 1 coordinated to the metal ions and enhanced the stability constant of the metal chelates.View full abstractDownload PDF (793K) -
KIYOSHI YOSHIDA, JIRO GOTO, YOSHIO BAN1987 Volume 35 Issue 12 Pages 4700-4704
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSOxidation of cycloalkan [b] indoles (3) with iodine pentoxide (I2O5) in 80% aqueous tetrahydrofuran (THF) at room temperature regioselectively afforded 6-oxocycloalkan [b] indoles (4) in various yields. The yield of this oxidation depends on the size of the ring fused with the indole nucleus. The essential reaction species is I2O5, not HIO3, which might be generated by hydrolysis of I2O5 in the aqueous reaction medium. Oxidation of 1-hydroxytetrahydrocarbazole (5) under the above conditions afforded spiro oxindoles 6 and 7 in 36 and 39% yields, respectively, accompanied with only a trace of 1-oxotetrahydrocarbazole (4a).View full abstractDownload PDF (659K) -
MASAHARU OKI, SADAKATSU SHIMADA1987 Volume 35 Issue 12 Pages 4705-4710
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSDiels-Alder addition of N-phenylmaleimide (2) to 1, 2, 4-triazines (1) occurred across carbons 3 and 6 of the triazines to give 1 : 1 adducts. After losing nitrogen, they gave dihydropyridines, which underwent a variety of further reactions. Pyridine derivatives (3) and bis-adducts (4) containing a 2-azabicyclo [2.2.2] oct-2-ene residue were obtained.View full abstractDownload PDF (795K) -
IWAO MORITA, MASAMI TSUDA, MASAHIRO KISE, MAKOTO SUGIYAMA1987 Volume 35 Issue 12 Pages 4711-4716
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSTreatment of various cyclic phosphites (1), e.g., 2-methoxy-1, 3, 2-dioxaphosphorinane (1a), 2-methoxy-5, 5-dimethyl-1, 3, 2-dioxaphosphorinane (1b) and 2-methoxy-1, 3, 2-dioxaphosphorane (1c), with haloacetones (2) gave cyclic Arbuzov products (3), cyclic Perkow products (4), cyclic methylphosphonates (5), and acyclic products (6-8). Compound 1a gave all of the products (3a, 4a, 5a, 6ag, 7ag, 8ag). However, cyclic phosphites with substituents in the ring (1b, 1d) gave only the cyclic products (3-5). The five-membered ring phosphite (1c) yielded only the acyclic products (6cg, 7cg). Treatment of 1a with chloroacetone gave only the Perkow products (4a, 7ah). Cyclic phosphite (1f) with a 2-benzyloxy substituent afforded simply the cyclic products (3a, 4a, 9). A mechanistic interpretation of these reactions is presented.View full abstractDownload PDF (1070K) -
SATOSHI MORIMOTO, GEN-ICHIRO NONAKA, ITSUO NISHIOKA1987 Volume 35 Issue 12 Pages 4717-4729
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA chemical examination of the seed shells of Aesculus hippocastanum L. has led to the isolation of proanthocyanidins A-6 (10) and A-7 (11), and aesculitannins A (12), B (13), C (14), D (15), E (16), F (17) and G (18). On the basis of chemical and spectroscopic evidence, proanthocyanidins A-6 (10) and A-7 (11) have been determined to be A-type dimers each possessing a C-4, C-6 interflavanoid linkage, while aesculitannins A (12), B (13), C (14), D (15), E (16), F (17) and G (18) have been characterized as oligomeric proanthocyanidins possessing A-type unit (s) in each molecule. In addition, the presence of (-) -epicatechin (1), proanthocyanidins B-2 (2), B-5 (3), A-2 (4), A-4 (5) and C-1 (6), epicatechin- (4β → 6) -epicatechin- (4β → 6) -epicatechin (7), and cinnamtannins B1 (8) and B2 (9) was also demonstrated.View full abstractDownload PDF (1902K) -
TAKEHIRO SANO, MIYUKI HIROSE, YOSHIE HORIGUCHI, HIROAKI TAKAYANAGI, HA ...1987 Volume 35 Issue 12 Pages 4730-4735
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSPhotocycloaddition of the dioxopyrroline 1 to 2, 3-dihydrofurans gave dihydropyridones 7 and 2, 4-dioxa-10-azatricyclo [6.3.0.03, 7] undecanes 8. The structure of 8a was determined by X-ray crystallographic analysis. The mechanisms of formation of the adducts are discussed from stereochemical point of view.View full abstractDownload PDF (905K) -
YASUMITSU TAMURA, HIROKAZU ANNOURA, MASAHIRO FUJI, TAKAYUKI YOSHIDA, R ...1987 Volume 35 Issue 12 Pages 4736-4746
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSNucleophilic addition of organometallic reagents (Grignard reagents and organolithium reagents) to three chiral α-keto acetals (1a-c) in open-chain systems was studied. The reactions of the chiral a-keto acetals (1a, 1b) having a chiral auxiliary as a ketone equivalent with Grignard reagents proceeded in a highly diastereoselective manner (> 94% diastereomeric excess (de)). As an application of the reaction, the syntheses of the key intermediates (6, 8) for (R) -and (S) -mevalolactone were achieved from the product obtained by the reaction of 1a and vinylmagnesium bromide. On the other hand, in the reactions of the chiral α-keto acetal (1c) having a chiral auxiliary as an aldehyde equivalent, lower stereoselectivity was observed even when Grignard reagents were used as addends. The difference of stereoselectivity among the three chiral α-keto acetals (1a-c) is discussed.View full abstractDownload PDF (1931K) -
HIDEAKI SASAKI, TOKUJIRO KITAGAWA1987 Volume 35 Issue 12 Pages 4747-4756
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe one-pot coupling reactions of bis (2-isocyano-2-tosylethyl) benzenes (5) with phthalaldehydes (11) afforded dioxazolo [32] cyclophanes (12a, 12d, 12e, 12f, and 12h), bis (naphth [2, 1-d] -oxazol-4-yl) benzenes (13a-c), and tetraoxazolo [34] parametacyclophane (14) as 1 : 1, 1 : 2, and 2 : 2 adducts, respectively. On the basis of the variable-temperature nuclear magnetic resonance (VT-NMR) spectra of dioxazolo [32] metacyclophane (12e), 12e in solution at room temperature exists in a syn form and the energy barrier to the conformational change (ΔG_??_) at the coalescence temperature (Tc = 38 °C) is determined to be 64.5 kJ/mol, which is higher than that of parent [32] metacyclophane (1). Therefore, it was suggested that the annelations of two oxazole rings to the two methylene bridges of 1 significantly affected the mobility of the benzene rings of 12e.View full abstractDownload PDF (1323K) -
HIROSHI WADA, HIROYUKI FUJITA, TAKAO MURAKAMI, YASUHISA SAIKI, CHIU-MI ...1987 Volume 35 Issue 12 Pages 4757-4762
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSChemical studies of three representatives of the genus Pseudophegopteris (Thelypteridaceae) revealed that the genus is characterized by the occurrence of unusual flavonoids with a modified B-ring related to protogenkwanin (VII). From P. hirtirachis HOLTT., three novel compounds, protogenkwanone (I), tetrahydroprotogenkwanone (II) and tetrahydroprotogenkwanin (III), were isolated, along with protogenkwanin 4'-O-β-D-glucoside (VI). From P. subaurita CHING, two new acylated glucosides of protogenkwanin, protogenkwanin 4'-O- (2-O-acetyl) -β-D-glucoside (IV) and 4'-O- (6-O-acetyl) -β-D-glucoside (V), were obtained, together with I, II and VI. From P. bukoensis HOLTT., IV, V and VI were isolated, in addition to apigenin 7-O-α-L-rhamnoside and kaempferol. The structures of the new compounds were determined by means of spectroscopic methods and chemical transformations.View full abstractDownload PDF (1052K) -
MITSUTERU NUMAZAWA, MASAO NAGAOKA, AYAKO MUTSUMI1987 Volume 35 Issue 12 Pages 4763-4768
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSWhen 16β-hydroxy-5α-androstan-17-one (2a) and its 16α-deuterio derivative (2a-16-d) were separately treated with H2SO4 or NaOH, compound 2a was rearranged to the 17β-hydroxy-16-oxo isomer (3a) with a marked kinetic deuterium isotope effect at the 16-position (kH/kD= 4.5 or 3.0). The product 3a obtained from compound 2a-16-d retained deuterium at C-17 to the extent of 16-65% while no significant loss of the isotope from the substrate was observed during the reaction. Isotope-labeling experiments showed that the intramolecular 1, 2-hydride shift is principally involved in the ketol rearrangement, and that the 16-oxo function of compound 3a enolizes preferentially toward the C-17 position rather than the C-15 position under the above conditions.View full abstractDownload PDF (873K) -
NOBUTAKA FUJII, TOSHIHIRO WATANABE, AKIRA OTAKA, KIYOSHI BESSHO, ITSUO ...1987 Volume 35 Issue 12 Pages 4769-4776
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA 37-residue peptide corresponding to the entire amino acid sequence of second human calcitonin gene-related peptide (β-hCGRP) was synthesized by assembling seven peptide fragments, followed by two successive treatments; i.e., first with thallium (III) trifluoroacetate to establish the disulfide bond between two Cys (Ad) residues and then with 1 M trimethylsilyl trifluoromethane-sulfonate/trifluoroacetic acid in the presence of diphenyl sulfide and ammonium iodide to remove all protecting groups employed and at the same time to reduce Met (O) to Met. The result was compared with that obtained by the usual air-oxidation procedure.
Synthetic β-hCGRP exhibited a weak inhibitory action against bone Ca-resorption stimulated by [1-34] -parathyroid hormone in vitro and lowered the Ca and Pi levels in rat serum.View full abstractDownload PDF (3003K) -
TAKUSHI KURIHARA, KAZUNORI SANTO, SHINYA HARUSAWA, RYUJI YONEDA1987 Volume 35 Issue 12 Pages 4777-4788
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe utility of the cyanohydrin diethylphosphates derived from aldehydes (arylaldehydes, crotonaldehyde, and cinnamaldehyde) as an acyl anion equivalent was examined. Deprotonation of cyanophosphates with n-butyllithium in the presence of tetramethylethylenediamine in tetrahydrofuran at -78°C followed by reactions with alkyl (acyl) halides, carbonyl compounds, and α, β-unsaturated nitriles or esters, as well as cyanophosphates themselves, afforded alkylated (acylated) products, mixed benzoin and acyloin phosphates, polysubstituted cyclopropanes, and diarylfumaronitriles in moderate yields, respectively.View full abstractDownload PDF (1737K) -
MASARU KOBAYASHI, HIROSHI MITSUHASHI1987 Volume 35 Issue 12 Pages 4789-4792
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe Chinese Umbelliferae plant Ligusticum wallichii was found to contain all the new components previously found in Cnidium officinale, which is closely related with L. wallichii and is used as the source plant of the crude drug “senkyu” in Japan. Three ligustilide derivatives, senkyunolide K (2), senkyunolide L (3), and senkyunolide M (4) were isolated simultaneously and their structures were elucidated as 4β-hydroxylsenkyunolide A (2), 6-hydroxy-7-chloro-6, 7-dihydroligustilide (3) and 6-butyryl-7-hydroxy-6, 7-dihydroligustilide (4) on the basis of the spectral properties. Treatment of ligustilide 6, 7-epoxide with hydrochloric acid readily gave 3 and thus 3 was considered to have been formed during the extraction of the plant.View full abstractDownload PDF (772K) -
TAKUSHI KURIHARA, TATSUYA TERADA, SHINYA HARUSAWA, RYUJI YONEDA1987 Volume 35 Issue 12 Pages 4793-4802
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA new and simple method for a formal synthesis of (±) -lysergic acid (1), via a four-step sequence starting from the aldehyde (13), is described. A very high yield of the product was obtained after purification by column chromatography at the end of the process, without isolation of intermediates.View full abstractDownload PDF (1862K) -
TAKEO HIGASHINO, SUSUMU SATO, AKIRA MIYASHITA, TATSUHIKO KATORI1987 Volume 35 Issue 12 Pages 4803-4812
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSAmong various Lewis acids, aluminium chloride (AlCl3) was the most effective catalyst for the formation of the Reissert compound (21a, 5-benzoyl-4, 5-dihydro-1-phenyl-1H-pyrazolo [3, 4-d] pyrimidine-4-carbonitrile) of 1-phenyl-1H-pyrazolo [3, 4-d] pyrimidine (11) by using benzoyl chloride and trimethylsilyl cyanide (TMSCN) in anhydrous methylene chloride (CH2Cl2).
Application of this method to derivatives of the following condensed pyrimidines, 1H-pyrazolo [3, 4-d] pyrimidine (1), 9H-purine (3), 3H-1, 2, 3-triazolo [4, 5-d] pyrimidine (5), and quinazoline (7), gave the corresponding new series of Reissert compounds (2, 4, 6, 8, and 9), which could not be prepared by the standard method using potassium cyanide and acid chloride in aqueous media.View full abstractDownload PDF (1351K) -
TATSUO YAMAUCHI, FUMIKO ABE, ALFRED S.C. WAN1987 Volume 35 Issue 12 Pages 4813-4818
Published: December 25, 1987
Released on J-STAGE: February 12, 2010
JOURNAL FREE ACCESSGlucos-3-ulosyl-thevetosides of 17α-digitoxigenin and 17α-tanghinigenin were obtained from air-dried leaves of Cerbera manghas and C. odollam. From fresh leaves, oleagenin glucosylthevetoside and digitoxigenin gentiotriosyl-thevetoside were isolated besides known glycosides, glucosyl-thevetosides of digitoxigenin and tanghinigenin The difference between the cardenolide glycosides of the air-dried leaves and of the fresh leaves, and the glycosides patterns in the two species are discussedView full abstractDownload PDF (760K) -
IWAO MORITA, Yuko HARUTA, TOSHIO TOMITA, MASAMI TSUDA, KAZUHISA KANDOR ...1987 Volume 35 Issue 12 Pages 4819-4828
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSVarious 1-and 2-substituted and 1, 2-fused 1, 4-dihydropyridine-5-phosphonate derivatives were designed and synthesized as analogues of 1, 4-dihydropyridine-3, 5-dicarboxylate, and their antihypertensive activities were examined. Several compounds proved to be equal or superior to nifedipine in lowering blood pressure in normotensive and spontaneously hypertensive rats. Among these compounds, 1-substituted 1, 4-dihydropyridine derivatives showed potent antihypertensive activities. The structure-activity relationships are discussed.View full abstractDownload PDF (1438K) -
SHUNJI IZUTA, MINEO SANEYOSHI1987 Volume 35 Issue 12 Pages 4829-4838
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSEight kinds of 5-substituted 1-β-D-arabinofuranosyluracil 5 '-triphosphates ((E) - (3-nitrostyryl) (6), (E) - (3-aminostyryl) (9), (E) - (4-nitrostyryl) (7), (E) - (4-aminostyryl) (10), (E) -styryl (8), phenethyl (11), (RS) - (3-azido-2-hydroxypropyl) (17), and (RS) - (3-amino-2-hydroxypropyl) (18) derivatives) were synthesized. Among these analogs, araUTPs bearing strongly hydrophobic styryl groups at the 5-position (6-10) were shown to have selective and strong inhibitory action on deoxyribonucleic acid (DNA) polymerase α purified from cherry salmon (Oncorhynchus masou) testes. The 5-azidopropyl derivative (17) also inhibited this polymerase. The compounds with a nitro and an amino group on the 5-styryl substituent showed essentially the same activity, but the 5-phenethyl derivative (11) and the 5-aminopropyl derivative (18) showed greatly reduced inhibitory action. On the other hand, in the case of DNA polymerase β, all the analogs showed similar inhibitory effects. The influence of hydrophobic and steric effects of substituents at the 5-position of araUTP on DNA polymerases α and β are discussed.View full abstractDownload PDF (1729K) -
YOSHIYUKI KAWAKAMI, YASUSHI NAGAI, YUKUO NEZU, TADASHI SATO, TOSHINOBU ...1987 Volume 35 Issue 12 Pages 4839-4845
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe stereostructures of four furanoditerpenes which were isolated from Arcangelisia flava MERR., 6-hydroxyarcangelisin, 2-dehydroarcangelisinol, tinophyllol, and 6-hydroxyfibleucin, were elucidated by a differential nuclear Overhauser effect (NOE) method and two-dimensional nuclear magnetic resonance (2D NMR). The stereostructures of two franoditerpenes, fibraurin and 6-hydroxyfibraurin, which had not been completely determined, were also elucidated.View full abstractDownload PDF (932K) -
JUN-EI KINJO, JUN-ICHI FURUSAWA, JUNKO BABA, TAKASHI TAKESHITA, MASAKI ...1987 Volume 35 Issue 12 Pages 4846-4850
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSTwo new isoflavone glycosides, the 8-C-apiosyl (1→6) glucosides of daidzein and genistein, were isolated from the roots and the voluble stems of Pueraria lobata (WILLD.) OHWI. Thirteen known isoflavonoids and related compounds were also found.View full abstractDownload PDF (744K) -
HARUKI YAMADA, MASAMI YOSHINO, TSUKASA MATSUMOTO, TAKAYUKI NAGAI, HIRO ...1987 Volume 35 Issue 12 Pages 4851-4855
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSSeveral phytosterols, stigmasterol, campesterol and β-sitosterol, were shown to have potent anti-complementary activities. Stigmasterol was the most potent. A marked consumption of C4 was observed to have occurred when serum was incubated with these phytosterols, and β-sitosterol and stigmasterol showed higher C4 consumption than campesterol. After the incubation of serum with these phytosterols in the absence of Ca2+ ions, cleavage of C3 in the serum was detected by immunoelectrophoresis. Stigmasterol caused greater C3 cleavage than the other two compounds. Stigmasterol also showed higher consumption of complement than campesterol and β-sitosterol when rabbit erythrocytes were used in the assay system in the absence of Ca2+ ions. These results indicate that these phytosterols activate complement via both the alternative and classical pathways.View full abstractDownload PDF (3334K) -
HIROSHI HOSODA, REIKO TSUKAMOTO, MAKIKO SHISHIDO, WATARU TAKASAKI, TOS ...1987 Volume 35 Issue 12 Pages 4856-4861
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSEnzyme labeling of a steroid with glucose oxidase by the N-succinimidyl ester method was investigated. The activated ester of a testosterone derivative was treated with glucose oxidase to give a labeled antigen. Various molar ratios of steroid to enzyme, ranging from 2 to 100, were employed; the degrees of hapten substitution were found to be 0.7-13. Satisfactory immunoreactivities with an anti-testosterone antiserum in the enzyme immunoassay procedure were obtained with the labeled antigens prepared at molar ratios higher than 4. The effect of steroid/enzyme molar ratio in the labeling on the sensitivity of the testosterone assay was then examined. It was found that the sensitivity of the assay is significantly influenced by the molar ratio, and a higher ratio results in a decrease in assay sensitivity. A dose-response curve with a high sensitivity could be obtained by the use of the labeled antigen prepared at a molar ratio of 6. The active ester method proved to be useful for the preparation of glucose oxidase-labeled antigens as well as for alkaline phosphatase, β-galactosidase and horseradish peroxidase labelings, because of its simplicity and excellent reproducibility.View full abstractDownload PDF (938K) -
GENJIRO KUSANO, AKIRA TAKAHASHI, KAZUHIRO SUGIYAMA, SHIGEO NOZOE1987 Volume 35 Issue 12 Pages 4862-4867
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe antifungal activities of several solanum alkaloids and their derivatives were examined against a variety of fungal strains such as Candida albicans and Trichophyton spp. Solacongestidine (I) showed the strongest activity (minimum inhibitory concentration) against C. albicans (0.8 μg/ml), T. rubrum (0.4 μg/ml) and Cryptococcus albidus (0.78 μg/ml), and also showed lesser activities against a wide range of fungi. Solafloridine (II) and verazine (VII) showed activities against C. albicans (3.1 and 6.2 μg/ml, respectively) and T. rubrum (25 and 3.1 μg/ml, respectively), while other alkaloids such as solasodine (III), tomatidine (IV), tomatillidine (V) and solanocapsine (VI) and related compounds (VIII-XIX) showed much lower activities. Solacongestidine also prolonged the survival time of mice infected with C. albicans.View full abstractDownload PDF (982K) -
SUSUMU IMAOKA, YOSHIHIKO FUNAE1987 Volume 35 Issue 12 Pages 4868-4871
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSCytochrome P-450 (P-450) isozymes are well separated by high-performance liquid chromatography with an ion-exchange column using buffer containing 0.4% Emulgen 911 (polyphenyl ether) as a detergent. However, it is impossible to monitor the elution profile of protein at 280 nm in the presence of Emulgen. Thus, we have developed a technique for determining the elution profile of protein in the presence of Emulgen. The absorption maximum and minimum of Emulgen 911 were at 276 and 244 nm, respectively. At 244 nm, the elution profile of 0.5 nmol (35 μg) of P-450 was detected as a peak in the presence of 0.4% Emulgen 911. The peak area increased linearly with increasing amount of P-450 up to 5 nmol (350 μg). Identification and estimation of the purity of the eluted P-450 are possible by dual monitoring at 244 and 417 nm, the wavelength for the detection of hemoprotein.View full abstractDownload PDF (535K) -
TAKAKO YOKOZAWA, HIKOKICHI OURA, YUJI KAWASHIMA1987 Volume 35 Issue 12 Pages 4872-4877
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSIn order to study the mechanism of hypoglycemic action of ginsenoside-Rb2 in diabetic rats, experiments were performed to determine carbohydrate metabolites and the levels of lipid constituents. The rats treated with ginsenoside-Rb2 showed a significant decrease of glucose in the hepatic tissue. The level of hepatic glycogen was slightly increased after ginsenoside-Rb2 administration. The glucose-6-phosphate level tended to increase, the pyruvate level was unchanged, and the lactate level tended to decrease. There was, however, no accumulation of total lipid in hepatic tissue. In rats given ginsenoside-Rb2, the levels of triglyceride, non-esterified fatty acid, 3-hydroxybutyrate, and acetoacetate were markedly decreased, showing a trend toward restoration of the normal state and inducing an increase in lipids in the adipose tissue. The hypoglycemic action of ginsenoside-Rb2 is discussed on the basis of the present results.View full abstractDownload PDF (1071K) -
KAZUNOBU MIURA, HIROYUKI KAMIYA, MINEKO TOMINAGA, YASUHIKO INOUE, MORI ...1987 Volume 35 Issue 12 Pages 4878-4882
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA synthetic gene for c-Ha-ras (Val-12) has been modified by cassette mutagenesis using restriction sites, ClaI-BssHII, to encode c-Ha-ras Gly-12. Genes for c-Ha-ras (Leu-61 and Arg-61) have been synthesized by joining newly synthesized oligodeoxyribonucleotides containing appropriate codons, together with previously obtained synthetic fragments. These genes have been expressed in E. coli and the products (p21) isolated. The guanosine diphosphate binding properties and guanosine triphosphatase activities of these p21 derivatives were studied.View full abstractDownload PDF (675K) -
HITOSHI SASAKI, JUNZO NAKAMURA, JUICHIRO SHIBASAKI, YOSHIO ISHINO, KAZ ...1987 Volume 35 Issue 12 Pages 4883-4890
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSTransdermal absorption of flurbiprofen (FP) from a cataplasm (CFP) and its antiinflammatory effect were investigated in the rat under various skin temperature conditions. As the skin temperature was raised, the plasma concentration of FP after application of the cataplasm increased significantly. It was demonstrated by a release and in vitro penetration experiment that skin penetration is the rate-determining step for absorption, and both release and penetration increased with a rise of temperature. Moreover, the in vivo transdermal absorption behavior was estimated by a deconvolution method from the plasma concentration data after intravenous administration and topical application of FP.
The Arrhenius plot of the in vitro penetration data at various temperature gave a nearly straight line and the activation energy calculated from the slope was 16.7 kcal/mol. The skin accumulation of FP decreased with a rise of temperature in the in vivo experiment while no significant change was seen in the in vitro experiment, suggesting participation of the increase of blood flow in the former experiment.
Though the anti-inflammatory effect was demonstrated at the normal skin temperature and under cooling, the effect was not found under warming. In addition, a considerable effect was observed with a control CFP which is free from FP when used under cooling.
From these results, it is suggested that the transdermal absorption of FP from CFP increased with a rise of skin surface temperature, and both factors, the concentration of FP absorbed and topical cooling, contribute to the anti-inflammatory effect.View full abstractDownload PDF (1177K) -
SHIGEO YANAI, YUICHI SUGIYAMA, DONG CHOOL KIM, HIROAKI SATO, TOHRU FUW ...1987 Volume 35 Issue 12 Pages 4891-4897
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA study on binding of human epidermal growth factor (hEGF) to various rat tissue homogenates showed the existence of specific binding in the liver, kidney, small intestines (duodenum, jejunum and ileum), stomach, lung and heart. The extent of the specific binding in the liver was at least ten times as large as those in other tissues. However, no specific binding was observed in the spleen, muscle or brain. Binding kinetic analyses using tissue homogenates of the liver, kidney and small intestines showed that the binding capacities (n) differed remarkably among the tissues, whereas the tissue differences in the dissociation constants (Kd) were minimal (1-6 nm). In our previous report on the contributions of various tissues to hEGF removal from the systemic circulation in rats after i.v. administration, the uptakes of hEGF by the liver, kidney, small intestines, stomach and spleen showed remarkable saturation, which may represent the operation of a receptor-dependent uptake mechanism. In the present in vitro experiment, specific bindings in these tissues except the spleen were indeed identified, suggesting that specific binding plays an important role in the tissue distribution of hEGF. Some other mechanism may be involved in the hEGF distribution to the spleen, because specific binding to this tissue was not detected in vitro. Comparing hEGF binding kinetic data (at 4 °C) for isolated rat hepatocytes with those for the homogenate, the binding parameters showed little difference between the two preparations, indicating that, at least under normal conditions, EGF receptors are not down-regulated and most of them exist on the cell surface.View full abstractDownload PDF (1113K) -
TOSHIYUKI KAKUTANI, YUMI SUEMATSU, WING YIN CHEAH, ETSUKO SUMIMOTO, MI ...1987 Volume 35 Issue 12 Pages 4898-4906
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA new experimental system was applied to obtain information about the local disposition of lipophilic mitomycin C (MMC) prodrugs after intra-arterial injection. Rabbit hind leg was perfused in situ using a single-pass technique and the outflow concentration-time curves of drugs following pulse injection were evaluated by using statistical moment analysis. Moment parameters (moments) were transformed to disposition parameters which express local disposition characteristics together with respect to elimination, distribution, and dispersion. Six lipophilic derivatives of MMC were tested together with the parent drug. Dimethylsulfoxide (DMSO) was used as a model injection vehicle that can be mixed with blood. Using this system, the following results were obtained. 1) Local disposition of the drug is decided by the balance of its affinities for intravascular and extravascular components. 2) Disposition can be modified by derivation of the drug to a more lipophilic prodrug. 3) Higher lipophilicity of a drug results in a larger organ clearance in the absence of albumin, but a smaller clearance in albumin-containing perfusate. 4) In the case of DMSO injection, intermediate clearance values are obtained regardless of the lipophilicity of drugs, and it was suggested that DMSO decreases both partitioning from the injection vehicle to the tissue and plasma protein binding.View full abstractDownload PDF (1406K) -
TOSHIYUKI KAKUTANI, RYO ATSUMI, ETSUKO SUMIMOTO, MITSURU HASHIDA1987 Volume 35 Issue 12 Pages 4907-4914
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA new experimental system was developed to elucidate the local characteristics of regeneration of drugs from prodrugs and was applied to propyloxycarbonyl mitomycin C (propyl-MMC), a lipophilic prodrug of mitomycin C (MMC). Rabbit hind leg was perfused with a single-pass technique and outflow concentration-time curves of propyl-MMC and regenerated MMC after pulse injection of propyl-MMC were evaluated by using statistical moment analysis. The outflow concentration-time profile after injection of MMC was also analyzed. Through Laplace transformation of the convolution function for the regeneration process, the first three moment parameters (moments) were led to secondary parameters which express the regeneration and sequestration characteristics of the prodrug such as the regeneration and sequestration ratios of the prodrug, mean regeneration time, and variance of the regeneration time. The pharmacokinetic behavior of propyl-MMC and MMC was thus expressed from the viewpoints of distribution, sequestration, regeneration, and dispersion, as well as extent and rate. It was confirmed that lipophilic derivation produced a larger tissue distribution and that rapid regeneration of the drug from the prodrug resulted in large local bioavailability of the parent drug.View full abstractDownload PDF (1100K) -
JAN PRÍBORSKÝ, KOZO TAKAYAMA, TSUNEJI NAGAI, DANU&Scaron ...1987 Volume 35 Issue 12 Pages 4915-4920
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe permeability characteristics of newborn pig skin and adult rat skin, either fresh or stored, to model drugs were examined and compared. Special attention was paid to the design to a new experimental system suitable for evaluation of skin permeability to various substances. Two types of model substances were used; insulin, a poorly absorbable substance with high molecular weight as a representative of peptide drugs, and brilliant blue, a low- molecular, relatively well absorbable substance. In vitro experiments performed with both substances in pig and rat gave comparable values of skin permeability. Maximum insulin concentration in the receiver solution was very similar in all experiments (164.5- 180.5μU/ml/24h when Azone® was used and 136.5- 178.0 μU/ ml/24 h when N-methyl- 2- pyrrolidone (NMP) was used as a penetration enhancer). The donor side concentration of insulin was 2.5 mg/ml.
The optimum concentrations of vehicle and penetration enhancer were 40.0% propylene glycol (PG) and 0.1% Azone® or 12.0% NMP, respectively. Brilliant blue experiments performed with the three skin preparations with 40.0% PG and 12.0% NMP gave similar values of the flux JT and permeability P of 1.38- 1.97 μg/cm 2/h and 1.56 × 10 -5- 2.22 × 10-5 cm/h, respectively. The concentration of brilliant blue in the donor compartment was 50 mg/ml. There were differences between the lag time in pig and rat skin experiments : about 3 h in the case of rat skin but 15 min in pig skin. In comparison to in vitro experiments, in situ studies gave much lower penetration of both test substances expressed as concentration in the receiver compartment. In the case of insulin with Azone® or NMP in the formulation, 30 times or 17 times lower concentration was found, and in brilliant blue experiments almost 5 times lower levels were observed. This new experimental system should be useful for examination of potential drug candidates as well as drug formulations for transdermal use.View full abstractDownload PDF (878K) -
KOZO TAKAYAMA, TSUNEJI NAGAI1987 Volume 35 Issue 12 Pages 4921-4927
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSInterpolymer complex formation of polyvinylpyrrolidone (PVP) with carboxyvinyl polymer (CP) was examined by turbidity measurement, a binding isotherm study and Fourier-transform infrared spectroscopy. The interpolymer complex of PVP with CP was found to be formed in the unit molecular ratio of 1 : 1 under ideal conditions, though the ratio of PVP in the solid complex was lower than 1 : 1 under practical conditions. Hydrogen bonding might be the driving force for the complexation, and the degree of hydrogen bonding was calculated to be about 40 to 50%.
The slowest dissolution rate of chlorpheniramine maleate from tablets, which consisted of a blend of PVP and CP was observed when the polymer combination ratio was 1 : 1. In the case of indomethacin, the longest lag time for the dissolution was observed at the polymer ratio of 1 : 1. Therefore, the drug dissolution behavior from PVP/CP tablets is dependent on the complex formation of PVP and CP.View full abstractDownload PDF (984K) -
YUJI TATEOKA, TOSHIYUKI KIMURA, KAZUHITO WATANABE, IKUO YAMAMOTO, ING ...1987 Volume 35 Issue 12 Pages 4928-4934
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSN-Allyl derivatives of uracil (U), thymine (T) and 6-methyluracil (6-MU) were prepared, and their pharmacological activities (hypnotic activity and anticonvulsant activity against pentylenetetrazol (PTZ) -induced seizures) and interactions with three sedative-hypnotics [pentobarbital (PB), barbital (B) and diazepam (DZ)] were investigated in mice. N1, N3-Diallyluracil (DAU) alone exhibited hypnotic and anticonvulsant activities. None of the other allyl derivatives showed both pharmacological activities. As regards interactions, most of the compounds tested prolonged PB-induced sleep at either 80 or 160 mg/kg, i.p. Further, U, T, and 6-MU (160 mg/kg, i.p.) also prolonged the PB-induced sleeping time. DAU showed a prolonging effect on PB-induced sleep when given by intracerebroventricular (i.c.v.) injection. DAU, N1, N3-diallylthymine (DAT) and N1-monoallyluracil (N1-MAU) significantly prolonged the B-induced sleeping time at a dose of 160 mg/kg, i.p. Further, DAU and DAT (40 mg/kg, i.p.) enhanced DZ-induced motor incoordination. These results indicate that U and related compounds possess central nervous system (CNS) - depressant effects and DAU is the most potent among the N-allyl derivatives tested.View full abstractDownload PDF (890K) -
TSUTOMU MIMURA, SUSUMU ITOH, KAZUTAKE TSUJIKAWA, HIROSHI NAKAJIMA, YAS ...1987 Volume 35 Issue 12 Pages 4935-4939
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSImmunoglobulin G from human serum was digested with papain to give an Fc fragment, which was carboxamidemethylated [carboxamidemethylated Fc (CM-Fc), M.W. about 25000].
Types I, III and IV allergic reactions were significantly depressed by the administration of CM-Fc.View full abstractDownload PDF (811K) -
TSUTOMU MIMURA, SUSUMU ITOH, KAZUTAKE TSUJIKAWA, HIROSHI NAKAJIMA, YAS ...1987 Volume 35 Issue 12 Pages 4940-4945
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe mechanism of the anti-allergic activity of carboxamidemethylated Fc (CM-Fc) was examined in vitro. CM-Fc had no effect on the proliferation of lymphocytes induced by concanavalin A (Con A), lipopolysaccharide (LPS), T cell-dependent mitogen or T cell-independent mitogen.
CM-Fc inhibited the activation of glycogen-stimulated guinea pig macrophages by FMLP and A23187, but not by phorbol 12-myristate 13-acetate (PMA).View full abstractDownload PDF (839K) -
TETSUO KOMURO, TOSHIMI MURAI, HIRONOSHIN KAWASAKI1987 Volume 35 Issue 12 Pages 4946-4952
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe effect of sonication on the particle size of lipopolysaccharide (LPS) in aqueous media was studied, in order to examine the relation of particle size to pyrogenicity in rabbits, by the sucrose density gradient ultracentrifugation technique. LPS extracted from E. coli UKT-B according to the phenol/water method showed a polydispersed profile on the gradients, but after sonication for 3 min it formed a single peak in the lower density regions. From the results of electron micrographic observations, partial specific volume, viscosity and turbidity measurements, and density gradient data, it was revealed that sonication produced a decrease in the particle size of LPS. A more marked pyrogenicity in rabbits was observed in the LPS fractions in the lower density regions than in the higher ones, or in the fractions having smaller-sized particles of LPS than in the fractions having larger particles.View full abstractDownload PDF (2531K) -
SACHIKO MINE, EIJI WAKABAYASHI, AKIHIRO SANDA, YOSHIO TAKIZAWA, KAZUKO ...1987 Volume 35 Issue 12 Pages 4953-4959
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSIn order to clarify the reason for the variation in specific activities of ribonuclease preparations from Rhizopus sp. ribonuclease (RNase Rh), low specific activity species (RNase Rh') were separated from native RNase Rh by DEAE Toyopearl 650 column chromatography and characterized. When RNase Rh' was subjected to gel electrophoresis in the absence of 2- mercaptoethanol, it gave a 24 kilodalton (kDa) protein band, but in the presence of the reducing agent it gave 17 and 7 kDa bands. These two peptides were separated by gel filtration and their NH2-terminal amino acid sequences were determined. The results indicated that RNase Rh' was an enzyme species cleaved at about the 50th residue of native RNase Rh by proteases during the course of purification, but the two fragments were still covalently joined by S-S bridges. RNase Rh' retained about 70% of the native activity and has a similar conformation to the native enzyme.View full abstractDownload PDF (4845K) -
HIDENOBU OHMORI, TOSHIKATSU TAKANAMI, MASAICHIRO MASUI1987 Volume 35 Issue 12 Pages 4960-4963
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSElectrochemical oxidation of triphenylphosphine in dichloromethane at a graphite anode in the presence of olefins has been shown to be a convenient method for the preparation of 1-alkenyltriphenylphosphonium perchlorates under mild conditions.View full abstractDownload PDF (574K) -
KAZUKO KIDO, YASUO WATAINABE1987 Volume 35 Issue 12 Pages 4964-4966
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA direct preparation of fully aromatized 3-alkylisoquinolines (3e-p), was achieved by cyclodehydrogenation with chlorosulfonic acid of N-benzyl-α-alkylaminoacetals (2e-p) which were prepared by addition of Grignard reagent to N-benzyliminoacetals (1a-d).View full abstractDownload PDF (408K) -
KATSUHIDE MATOBA, TAKAO YAMAZAKI1987 Volume 35 Issue 12 Pages 4967-4971
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe structure of the product from the reaction of diazomethane and 4, 5, 6, 7-tetrahydro-4', 4', 6, 6-tetramethylspiro [1, 3-benzoxaselenole-2, 1'-cyclohexane] -2', 4, 6'-trione (I), which was prepared by the oxidation of dimedone with selenium dioxide, was proved by X-ray analysis to be 1, 2, 3, 4, 8, 9, 10, 11-octahydro-3, 3, 10, 10-tetramethyl-1, 8-dioxodibenzo [b, e] [1, 4, 7] dioxaselenocine (II). Several 1, 3-oxaselenoles (IV) derived from bicyclo [3.3.1] nonane-2, 4-diones (III) were treated with diazomethane in ether to give the corresponding dioxaselenocines (V) in good yields.View full abstractDownload PDF (761K) -
KEN-ICHI TANJI, HARUMI KUBOTA, YUMI YAMAMOTO, TAKEO HIGASHINO1987 Volume 35 Issue 12 Pages 4972-4976
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe reactions of 2-chloro-9-phenyl-9H-purine (1) with sodium methoxide, ethoxide, and phenoxide as O-nucleophiles, with butylamine and piperidine as N-nucleophiles, and with sodium methylsulfide as an S-nucleophile, afforded 2-methoxy- (3a), 2-ethoxy- (3b), 2-phenoxy- (3c), 2-butylamino- (4a), 2-piperidino- (4b), and 2-methylthio-9-phenyl-9H-purine (5), respectively. Compound 1 also reacted with ethyl cyanoacetate and phenylacetonitrile as C-nucleophiles in the presence of sodium hydroxide in dimethyl sulfoxide to give ethyl H-cyano-9-phenyl-9H-purine-2-acetate (6a) and α, 9-diphenyl-9H-purine-2-acetonitrile (6b). However, 1 did not react with other active methylene compounds, ketones or potassium cyanide.
On the other hand, 2- (methylsulfonyl) -9-phenyl-9H-purine (2), prepared easily from 1, smoothly reacted not only with active methylene compounds but also with ketones and potassium cyanide. When active methylene compounds, such as ethyl cyanoacetate and phenylacetonitrile, were used, 2 gave 6a and 6b in good yields. In the cases of ketones and potassium cyanide, the substitution reactions of 2 proceeded to give the corresponding 2-substituted 9H-purines (7 and 8a-d), as expected.View full abstractDownload PDF (860K) -
TAKASHI HARAYAMA, HIDETO FUKUSHI, KAZUHIRO OGAWA, TETSUYA ARATANI, SAT ...1987 Volume 35 Issue 12 Pages 4977-4980
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSReaction of gem-dibromocyclopropanes (1) with a higher-order organocuprate prepared from cuprous thiocyanate and methyllithium, followed by the addition of methyl iodide in situ, readily afforded dimethylcyclopropanes (2) in good to excellent yields regardless of the functional group in 1.View full abstractDownload PDF (698K) -
NORIKO SHIMIZU, MASASHI TOMODA1987 Volume 35 Issue 12 Pages 4981-4984
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe major neutral polysaccharide, designated as MVS-I, was isolated from the seeds of Malva verticillata L. It was homogeneous on electrophoresis and gel chromatography. It is composed of L-arabinose : D-galactose : D-glucose in the molar ratio of 3 : 6 : 7. Methylation analysis, carbon-13 nuclear magnetic resonance, and periodate oxidation studies enabled elucidation of its structural features.View full abstractDownload PDF (652K) -
HIROYUKI AKITA, HIROKO MATSUKURA, KENJI SONOMOTO, ATSUO TANAKA, TAKESH ...1987 Volume 35 Issue 12 Pages 4985-4987
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSAsymmetric reduction of α-methyl β-keto esters using microbial cells immobilized by the prepolymer method was examined. It was found that by a proper selection of the prepolymer in the stage of immobilization, the chemical and optical yields were both improved appreciably in some cases compared to those obtained by reduction with the native microorganisms.View full abstractDownload PDF (309K) -
YASUO KIKUGAWA1987 Volume 35 Issue 12 Pages 4988-4989
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSDimethylamine-borane was synthesized in good yield from sodium borohydride and dimethylamine hydrochloride by using dimethoxyethane as a solvent.View full abstractDownload PDF (227K) -
NORIYUKI TAKATSU, MASAYO NOGUCHI, SHIGERU OHMIYA, HIROTAKA OTOMASU1987 Volume 35 Issue 12 Pages 4990-4992
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESS2-Hydroxy-3- (2'-piperidyl) quinolizidine (5), an intermediate for the synthesis of (±) -leontiformidine (1a), was converted into (±) -sparteine (7) by a three-step procedure of oxidation, Mannich reaction and deoxygenation.View full abstractDownload PDF (342K) -
TATSUO YAMAUCHI, FUMIKO ABE, ALFRED S. C. WAN1987 Volume 35 Issue 12 Pages 4993-4995
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESS17α-Digitoxigenin apiosyl-glucosyl-thevetoside and cellobiosyl-thevetoside were isolated, together with known biosides and triosides, from the stems of Cerbera manghas L.View full abstractDownload PDF (402K) -
KAZUTAKE SHIMADA, JAI SEUP RO, CHIYOMI KANNO, TOSHIO NAMBARA1987 Volume 35 Issue 12 Pages 4996-4999
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSThe occurrence of two new bufogenin conjugates, desacetylcinobufagin 3-succinyl-L-arginine ester and cinobufagin 3-sulfate, together with two known gamabufotalitoxin homologs and resibufogein 3-sulfate, in the skin of Korean toad, Bufo bufo gargarizans CANTOR, is reported. Their structures were elucidated by degradative means and/or direct comparison with authentic samples. These bufogenin conjugates were assayed for inhibitory activity towards guinea pig heart Na+, K+-adenosine triphosphatase.View full abstractDownload PDF (563K) -
ATSUSHI SUGII, NAOTAKE OGAWA, TAKURO KAWANISHI, TERUHISA UMEDA, TATSUO ...1987 Volume 35 Issue 12 Pages 5000-5003
Published: December 25, 1987
Released on J-STAGE: October 19, 2009
JOURNAL FREE ACCESSA one-step synthesis of a cortisol derivative for radioiodination is presented. The radioimmunoassay for cortisol using the bridge heterologous 125I-labeled antigen was more sensitive than that using a bridge homologous antigen. Cortisol levels in saliva and serum were easily determined by direct radioimmunoassay with the proposed 125I-labeled antigen.View full abstractDownload PDF (653K)