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Volume 107, Issue 9
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SHOJI INOUE1987 Volume 107 Issue 9 Pages 645-664
Published: September 25, 1987
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThis review deals with the synthesis of surugatoxin, neosurugatoxin and prosurugatoxin, isolated from the toxicated Japanese ivory shell (Babylonia japonica), and the chemical transformation of prosurugatoxin into surugatoxin.View full abstractDownload PDF (1317K) -
TAKUO KOSUGE, HIROSHI ZENDA, KUNIRO TSUJI1987 Volume 107 Issue 9 Pages 665-675
Published: September 25, 1987
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIn September 1965, the Japanese ivory shell, Babylonia japonica harvested from the Ganyudo area of Suruga Bay, Shizuoka Prefecture, caused an outbreak of food poisoning. The causative toxins, designated as neosurugatoxin and prosurugatoxin, were isolated from the digestive gland of the shellfish, and their chemical structures were determined. Pharmacological studies suggested that the toxins have selective affinity for ganglionic nicotine receptors, its affinity constant for these receptors being more than three orders of magnitude greater than that of hexamethonium. Surugatoxin derived from prosurugatoxin was isolated from culture medium of Coryneform bacterium which was isolated from digestive gland of toxic ivory shell, indicating that the origin of the toxins were bacterium.View full abstractDownload PDF (1146K) -
MASAYUKI NAKAGAKI, HIROAKI ICHIHASHI1987 Volume 107 Issue 9 Pages 676-682
Published: September 25, 1987
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSMixed monolayers of egg lecithin (EYPC) with myristyl alcohol (C14OH), cetyl alcohol (C15OH) or stearyl alcohol (C18OH) were spread at air-water interface. The surface pressure mean area (F-A) curves for the mixed monolayers were obtained. F-A curves of the mixed monolayers followed the equations of state of virial type : FA/kT=c+b/A. For C18OH-EYPC and C16OH-EYPC systems except for those of low high alcohol concentration, each FA/kT vs. 1/A plot showed a break point. Limiting areas obtained by extraporating the plots to FA/kT=0 showed that the mixed monolayers of EYPC and C14OH or C16OH were expanded although the mixed monolayers of EYPC and C18OH were rather condensed. It was concluded that attractive force between hydrocarbonchains of C14OH or C16OH was decreased by EYPC. Desorption of C14OH from the monolayers under constant area was studied. The desorption rate of C14OH was enhanced by the addition of a small amount of EYPC and practically depressed by the addition of equal or more moles of EYPC. It was concluded that a small amount of EYPC made C14OH molecules to be in high energy state.View full abstractDownload PDF (674K) -
RIEKO MATSUDA, MUMIO ISHIBASHI, MITSURU UCHIYAMA1987 Volume 107 Issue 9 Pages 683-689
Published: September 25, 1987
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSAn automated system was constructed for the optimization of the experimental conditions of a color developing reaction. This system consists of a laboratory robot system and a spectrophotometer which are connected with a personal computer by a remote control interface through RS-232C and by a GP-IB interface, respectively. The procedure for the color developing reaction was carried out with the robot system while the measurement of the absorbance of a sample and the transmission of the value to the computer were carried out automatically with a spectrophotometer. The personal computer controls the robot system and the spectrophotometer, and calculates the optimal value according to the super modified simplex (SMS) algorithm based on the transmitted absorbance value. This system was applied to the reaction of phosphotungstic acid and the drugs with a phenothiazine ring in the molecule. The optimal conditions were searched for chlorpromazine hydrochloride and levomepromazine maleate.View full abstractDownload PDF (698K) -
MASAYUKI MIKAGE, TSUYAKO USHIYAMA, TSUNEO NAMBA1987 Volume 107 Issue 9 Pages 690-693
Published: September 25, 1987
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIn the previous paper, the quantitative analysis of berberine type alkaloids in Coptidis Rhizoma by means of X-ray microanalyser (XMA) was reported. In this paper, the serial distribution of alkaloids on the analytical lines of transverse sections of Coptidis Rhizoma and Phellodendri Cortex by XMA method are described. The analytical specimens were moved automatically during spot analysis, after treating with 0.2% ammonium reineckate in alcohol for 3 h. The results showed that alkaloids were detected much in the cortex and pith of Coptidis Rhizoma but not in the cork layer, phloem and xylem. On Phellodendri Cortex, inner cortex contained alkaloids more than outer part.View full abstractDownload PDF (670K) -
SUMU MATSUEDA, KUNIHIRO SHINPO, KAORU ABE, HAJIME KARASAWA, YUKI KATSU ...1987 Volume 107 Issue 9 Pages 694-697
Published: September 25, 1987
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSA product (II) hydrolyzed with α-amylase was obtained from an antitumor active glycoprotein (I) isolated from Chlorella vulgaris. Its molecular weight was 4.5×104. It was found to have an antitumor activity against sarcoma 180 implanted in mice and also against mouse lymphemia L-1210/v/c.View full abstractDownload PDF (601K) -
MASAYUKI NADAI, TADASHI HORIUCHI, IKUO JOHNO, SHIKIFUMI KITAZAWA, HIDE ...1987 Volume 107 Issue 9 Pages 698-704
Published: September 25, 1987
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSAn evaluation of three commercial macrolide antibiotic tablets on factors concerning absorption characteristics was conducted. Macrolide tablets selected in this study were erythromycin stearate (EM), midecamycin acetate (MOM) and rokitamycin (RKM), and the factors studied were dissolution characteristics, stability and bioavailability of respective tablets in man. Dissolution characteristics were examined in three test solutions with normal, hypoand anacidity. Although all tablets dissolved rapidly and in a similar manner in normal acidic solution, differences were observed in hypo- and anacidic solutions. RKM still showed rapid and complete dissolution, while EM and MOM showed less than 50% in the same period examined. In the stability test, EM degradated to 41% within 60 min in acidic solution, but MOM and RKM showed satisfactory stability and 79 and 90% of respective drugs remained under the same condition. Bioavailability was evaluated with six healthy volunteers. The test was conducted with MOM and RKM in a crossover manner and gastric acidity test was performed between each test. MOM showed a great difference in subjects having hypo- and normal gastric acidity while RKM showed little difference between subjects. These results suggest that in vitro dissolution characteristics and stability are reflected in bioavailability of these tablets in man.View full abstractDownload PDF (669K) -
MITSUO YAMAZAKI, YASUJI AOKI, HIDEO KATO, YASUO ITO, HITOSHI KONTANI, ...1987 Volume 107 Issue 9 Pages 705-710
Published: September 25, 1987
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe compounds of 2-methyl-3-pyrrolidinopropiophenone structure, in which the p-position of phenyl group is hydrogen, alkyl group (C1-C4), cyclohexyl group or fluoromethyl group, were synthesized and the centrally acting muscle relaxant activities of these compounds were studied after peroral or intraduodenal administration. On the muscle relaxant activity in rotating rod method in mice, compound which contains ethyl, n-propyl, isopropyl or n-butyl group had almost equipotent inhibitory activity, but the inhibitory effect on the anemic decerebrate rigidity in rats of ethyl substituent compound was stronger than other compounds. The muscle relaxant activities of the compound containing cyclohexyl or fluoromethyl group were weaker than those of other compounds. The hexobarbital induced sleeping time was more prolonged by the compound containing hydrogen or butyl group at p-position. Toxicities (body weight decrease or mortality) in mice and rats were potentiated according to the length of alkyl chain. These results suggested that ethyl group would be suitable for the p-substituent of phenyl group of the compounds as a centrally acting muscle relaxant. The pyrroridinopropiophenone derivatives had stronger inhibitory effect on convulsion induced by nicotine, as compared with the piperidinopropiophenone analoges.View full abstractDownload PDF (635K) -
SHINJI USUDA1987 Volume 107 Issue 9 Pages 711-719
Published: September 25, 1987
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSTwenty-seven pyrrolidinyl-benzamides in which substituents at 4 (R1) and 5 (R2) positions on benzoyl moiety and at nitrogen of pyrrolidine rings (3-pyrrolidinyl, cis-2-methylpyrrolidin-3-yl and 2-pyrrolidinylmethyl types) varied, including YM-09151-2 and sulpiride, were evaluated for their activities in inhibiting apomorphine-induced stereotypy and conditioned avoidance response and causing catalepsy in mice and rats by subcutaneous (s.c.) and intracerebroventricular (i.c.v.) administration. 1) In variation of R1 substituents on cis-N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxybenzamides, s.c. activities in inhibition of stereotypy and avoidance and induction of catalepsy increased in the order of CH3NH (V) > (CH3)2N (VI) ≥NH2 (IV) > H (III). After i.c.v. injection, however, the rank of potencies was CH3NH > NH2 ≥ (CH3)2N. Monomethylation of the p-amino substituent on benzoyl moiety was also found to enhance s.c. activities in other benzamides (II > I, VIII > VII, XI > X, XIV > XIII, XXIII > XXII). 2) Chlorine as R2 substituents was more favourable than a methylsulfonyl group for intensifying anti-dopaminergic activity after s.c. administration (IV > VII, V > VIII, XIII > XV, XIX > XXI). Compounds IV and V exhibited more potent anti-dopaminergic activity than VII and VIII, respectively, both by s.c. and i.c.v. routes. In contrast, compound IX and sulpiride bearing R2=NH2SO2 caused anti-dopaminergic activity only after i.c.v. injection. 3) Introduction of a benzyl group at nitrogen on the pyrrolidin ring instead of an ethyl group enhanced anti-dopaminergic activity by s.c. injection. 4) Compounds IV-VIII were more potent in inhibiting stereotypy than in inducing catalepsy after i.c.v. administration, whereas IX and sulpiride were less potent in antistereotypic activity. These results indicate that the introduction of monomethyl-amino, chlorine and benzyl groups at 4 and 5 positions on benzoyl moiety and at nitrogen of pyrrolidine ring, respectively, provides for the optimum anti-dopaminergic activity of pyrrolidinyl-benzamides. In addition, a sulfamoyl substituent is not suitable for the penetration of compounds into the brain.View full abstractDownload PDF (986K) -
MAMORU SUEKAWA, TAKASHI SHIGA, HIDEKO SONE, YUKINOBU IKEYA, HEIHACHIRO ...1987 Volume 107 Issue 9 Pages 720-726
Published: September 25, 1987
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe effects of 15 lignan compounds, which were extracted from schisandra fruits, on the contractions of an isolated mesenteric artery of dog induced by prostaglandin F2α (PGF2α), CaCl2 or norepinephrine (NE) were examined. As a result, all lignan compounds used showed inhibitory effects on the contractions of mesenteric artery induced by PGF2α and CaCl2. However, 6 compounds such as gomisin J (GJ) also showed inhibitory effects on NE-induced contraction. We further examined the actions of GJ with much better activity. Since GJ is not soluble in water, we synthesized GJ-Na (GJN) and further used throughout the experiments. In the isolated mesenteric artery of dog, GJN showed inhibitory effects on the NE-induced contraction (ID50=131.8±0.11×10-6 M), and relaxant effects on PGF2α-induced contractions (ED50=9.72±0.36×10-6 M), and also showed inhibitory effects on CaCl2-induced contraction (ID50=6.96±0.16×10-6 M). Furthermore, GJN showed relaxant effects and an increase in coronary flow on the isolated trachea, ileum, taenia coli and heart in guinea-pigs, GJ (10-4 and 3×10-4 g, i.a.) produced an increase in coronary artery blood flow in anesthetized dog, although its effect was slightly weaker than that in diltiazem, a well known calcium antagonist. As mentioned above, it was confirmed that lignan compounds extracted from schisandra fruits had Ca antagonistic actions in varying degrees, and that GJN had a dilating effect on the coronary artery.View full abstractDownload PDF (721K) -
KYOKO TAKAHASHI, NORIKO MATSUMOTO, TADASHI OKAMOTO, TAKEO KISHI1987 Volume 107 Issue 9 Pages 727-731
Published: September 25, 1987
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe effects of anticarcinogenic antibiotics and psychotherapeutic drugs known to possess cardiotoxic effects were investigated on cellular respiration and beating of isolated and cultured mouse cardiac cells, respectively. Adriamycin (ADM) and antimycin A (AMA) as the antibiotics and chlorpromazine (CPZ), thioridazine (THZ) and imipramine (IMP) as the psychotherapeutic drugs were used in the present study. AMA inhibited the cellular respiration as well as the spontaneous beating of the cells shortly after the addition of a low concentration. ADM also inhibited the beating in parallel with the cellular respiration in the concentration range of 70-520 μM. The concentrations of psychotherapeutic drugs for the 50% inhibition of the beating were extremely low in comparison with those for cellular respiration in the mouse cardiac cells, which were about 10-times as effective as AMA. These results suggested that ADM is entirely different from psychotherapeutic drugs in a manner of inhibition of beating and respiration and that the beat-inhibition caused by psychotherapeutic drugs could not be due to the inhibition of cellular respiration.View full abstractDownload PDF (642K) -
NOBUO YOKOO, EIZOU HATTORI, MITSUTERU HIRATA, KOICHIRO WATANABE, FUMIY ...1987 Volume 107 Issue 9 Pages 732-737
Published: September 25, 1987
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSSynthesis of water-soluble chymotrypsin specific inhibitors was attempted to study the roles of chymotrypsin-like enzymes in vivo. Previously we reported that the esters of carboxylic acid containing a condensed ring showed stronger activity than those containing a single ring system. Then we synthesized 4-substituted phenyl esters of carboxylic acid containing a condensed ring, such as tetralin, naphthalene, indole etc., and their inhibitory activities were compared. Among these compounds, esters of tetralin-1-carboxylic acid (FK-448) and 1-naphthylacetic acid showed the strongest activity, and their IC50 values were 8×10-7, 5×10-7 M, respectively. Tetralin-2-carboxylate and 2-naphthylacetate inhibited weaker than 1-analogues. Esters of basic quinoline carboxylic acid and bulky carboxylic acids containing a three-ring system inhibited poorly. Chymotrypsin produced equimolecular 4-substituted phenol rapidly and thereafter the amount of 4-substituded phenol increased slowly, when incubated with FK-448 at 37°C.View full abstractDownload PDF (584K)
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