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Volume 105, Issue 2
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NAKAO ISHIDA1985 Volume 105 Issue 2 Pages 91-108
Published: February 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe causes that lead malignant tumors to be lethal are not completely understood. However, patients are known to reach a state of immunosuppression in the late stages of the diseases. This impairment of immune responses in patients or animals bearing cancer is believed to be one of the most plausible causes of death. To explain this impairment, the presence of immunosuppressive factors with a wide variety of molecular sizes have been investigated. One factor was found to be IAP (immunosuppressive acidic protein), a kind of α1-acid glycoprotein. In mice, an increase in the amount of IAP in the serum paralleled with the appearance of suppressor macrophages. In humans, many clinical reports tell us that after a surgical operation an increase in IAP in the serum clearly indicates the unfavourable prognosis of patients, while a decrease in IAP, followed by no later elevation, means a favourable prognosis. Other low-molecular weight immunosuppressive factors were looked for in ascites of tumor-bearing mice, based upon the evidence that the components of malignant cells which cause them to differ qualitatively from normal cells are transfer ribonucleic acids (RNAs). The breakdown products of these RNAs were examined by means of high performance liquid chromatography in mouse ascites and 1-methyladenosine (m1A) was detected, in addition to uric acid, uracil and pseudouridine. It was found that the administration of a μg order of m1A to mice two or three days before i.v. infection with Listeria monocytogenes caused a definite acceleration in the number of deaths due to infection. Both of these markers will be useful in the prognosis of cancer patients and monitoring the effectiveness of therapy. However, further knowledge of these immunosuppressive factors will be necessary in order to effectively diagnose the immunological status of cancer patients and establish a therapeutic policy for them. Because, without enough knowledge of these immunosuppressive factors, one can not deal with the real immunological status of cancer patients nor establish a therapeutic policy for them.View full abstractDownload PDF (2007K) -
HIROSHI HIKINO1985 Volume 105 Issue 2 Pages 109-118
Published: February 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThere are a variety of crude drugs which are reputed to be effective for liver disorders. To evaluate liver-protective activity and to elucidate active constituents of those drugs, it is essential that appropriate assay methods are provided. Antihepatotoxic activity has hitherto been assessed by in vivo assay methods employing whole animals which, however, are costly in animals, require fairly large amounts of samples and give marked variation and poor reproducibility of the results, and, therefore, are not suitable for activity-guided fractionation of plant extracts. For primary screening of antihepatotoxic activity of extracts, fractions and constituents of liver-protective crude drugs, carbon tetrachloride-, D-galactosamine-, peroxide- and ionophore-produced cytotoxicity models utilizing primary cultured rat hepatocytes have been established. The antihepatotoxic effects of the known natural products have been evaluated using these methods thus devised. A number of crude drugs have been screened by means of the in vitro assay methods using carbon tetrachloride- and D-galactosamine-induced cytotoxicity models to reveal that some exhibited significant antihepatotoxic effects. A survey for the antihepatotoxic constituents in the active drugs has been conducted and the antihepatotoxic actions of the active constituents of Artemisia capillaris buds, Salvia plebeia herbs, Curcuma longa rhizomes, Zingiber officinale rhizomes, Schizandra chinensis fruits, Atractylodes rhizomes, Swertia japonica herbs, Tetrapanax papyriferum leaves, Dianthus superbus var. longicalycinus herbs, Panax ginseng roots, Aeginetia indica herbs and Ephedra roots have been assessed. The mechanisms of antihepatotoxic actions of glycyrrhizin, atractylon and wuweizisu C have been examined.View full abstractDownload PDF (1188K) -
ETSUO OISHI, HIDEKI MATSUBARA, EISAKU HAYASHI1985 Volume 105 Issue 2 Pages 119-128
Published: February 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESS4, 7-Dichioro-1-phenyl-1H-pyrazolo [3, 4-d] pyridazine (I) reacted with active methylene compounds i.e. ethyl cyanoacetate (IIa), ethyl acetoacetate (IIb), diethyl malonate (IIc), malononitrile (IId) and phenylacetonitrile (IIe) in the presence of sodium hydride in refluxing benzene to afford the corresponding 4-substituted (R1) 7-chloro-1-phenyl-1H-pyrazolo [3, 4-d] pyridazine (III) or 7-substituted (R2) 4-chloro-1-phenyl-1H-pyrazolo [3, 4-d]-pyridazine (IV) i.e. IIIa (R1=NC-CH-CO2C2H5), IVa (R2=NC-CH-CO2C2H5), IVb (R2=CH8CO-CH-CO2C2H5), IVc (R2=CH (CO2C2H5)2), IIId (R1=CH (CN)2), IIIe (R1=NC-CH-Ph). Compound I also reacted with ketones having an active methylene group i.e. acetophenone (IIf), propiophenone (IIg), acetone (IIh) and diethyl ketone (IIi) in the presence of sodium hydride in refluxing toluene to afford the corresponding 4-substituted (R1) 7-chloro-1-phenyl-1H-pyrazolo [3, 4-d] pyridazine (IX), 7-substituted (R2) 4-chloro-1-phenyl-1H-pyrazolo [3, 4-d] pyridazine (X) or 4, 7-disubstituted (R3) 1-phenyl-1H-pyrazolo [3, 4-d] pyridazine (XI) i.e. IXa (R1=CH2COPh), Xa (R2=CH2COPh), XIa (R3=CH2COPh), XIb (R3=CH3-CH-COPh), IXc (R1=CH2COCH3), Xc (R2=CH2COCH3), XIc (R3=CH2COCH3), IXd (R1=CH3-CH-COC2H5).View full abstractDownload PDF (935K) -
ETSUO OISHI, TAKESHI ENDO, YOSHIKAZU ASAHINA, EISAKU HAYASHI1985 Volume 105 Issue 2 Pages 129-141
Published: February 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSChemical properties of 7-methoxy-1-phenyl-1H-pyrazolo [3, 4-d] pyridazine 5-oxide (V) obtained in the reaction of 7-methoxy-1-phenyl-1H-pyrazolo [3, 4-d] pyridazine (IV) with m-chloroperbenzoic acid were studied. Compound V reacted with nucleophiles to give 4 (R2), 7 (R1)-disubstituted 1-phenyl-1H-pyrazolo [3, 4-d] pyridazine or the ring fission product, methyl 4 (R8)-substituted 1-phenyl-1H-pyrazole-5-carboxylate. The reaction of V with each of phosphoryl chloride and sulfuryl chloride gave VI (R2=Cl, R1=OCH3) and XI (R2=Cl, R1=OH). In the case of the reaction of V with tosyl chloride, XII (R3=CH (-Cl)-p-tosyl) was obtained together with VI and XI. The reaction of V with potassium hydroxide solution gave IX (R2=H, R1=OH, 5-oxide). The reaction of V with ethyl cyanoacetate in acetic anhydride gave XIII (R2=NC-CH-CO2C2H5, R1=OCH3). The Grignard reaction of V with methylmagnesium iodide and ethylmagnesium bromide gave XIVa (R2=CH3, R1=OCH3) and XIVb (R2=C2H5, R1=OCH3), respectively. Application of the Reissert reaction to V resulted in the formation of XVI (R3=CH=C (-OCH3)-(4-formyl-1-phenyl-1H-pyrazol-5-yl). The reaction of V with acetic anhydride afforded XVII (R2=OH, R1=OCH3), XVIII (R3=CH (-COCH3)-O-COCH3), and XIX ((R3=CH=)2). The reaction of V with acetyl chloride afforded XI, XXa (R3=CH (-COCH3)-R4, R4=4-chloro-6, 7-dihydro-7-oxo-1-phenyl-1H-pyrazolo [3, 4-d] pyridazin-6-yl) and XXI (R3=CH2-R4). A similar ring fission occurred in the reaction of V with benzoly chloride to afford XXb (R3=CH (-COPh)-R4), XXI, and XIX. The reaction of V with dimethyl acetylenedicarboxylate afforded 7-methoxy-1-phenyl-1H-pyrazolo [3, 4-d] pyridazinium 3-methoxy-1-methoxycarbonyl-2, 3-dioxopropylide (XXII), trimethyl 9-methoxy-1-phenyl-1H-pyrazolo [3, 4-d] pyrrolo [1, 2-b] pyridazine-4, 5, 6-tricarboxylate (XXIII), and methyl 5-methoxycarbonyl-6-methoxy-α-oxo-1-phenyl-1, 5H-cyclopenta [c]-pyrazol-5-ethanoate (XXIV). It is considered that the ring fission products are formed by the cleavage of pyridazine ring accompanied with the liberation of nitrogen.View full abstractDownload PDF (1156K) -
MASAO KIKUCHI, YOUKO YAMAUCHI1985 Volume 105 Issue 2 Pages 142-147
Published: February 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThree new secoiridoid glucosides, named ligustrosidic acid (V), oleuropeinic acid (VI) and neonuezhenide (VIII), have been isolated from the fruits of Ligustrum japonicum and Ligustrum lucidum, and their structures have been elucidated on the basis of chemical and spectral evidence. Compound IX has been presumed to be the substance as Gl 3 which was obtained from Fraxinus americana.View full abstractDownload PDF (566K) -
TSUYOSHI TOMIMORI, HISANORI JIN, YUKINORI MIYAICHI, SHINGO TOYOFUKU, T ...1985 Volume 105 Issue 2 Pages 148-155
Published: February 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSHigh-performance liquid chromatographic procedure was established for the quantitative method of flavonoids in Scutellaria root ("Huangqin", the root of Scutellaria baicalensis GEORGI). Eleven flavonoids, baicalein (I), baicalin (II), baicalein 7-O-glucoside (III), oroxylin A (IV), oroxylin A 7-O-glucuronide (V), wogonin (VI), wogonin 7-O-glucuronide (VII), chrysin (VIII), skullcapflavone II (IX), 5, 7, 2', 6'-tetrahydroxyflavanone (X) and dihydrooroxylin A (XI), were separated by the combined use of both operating conditions of 1 and 2 shown in Fig. 2 and 3, respectively. This method is considered to be useful for the chemical evaluation of commercially available Scutellaria root.View full abstractDownload PDF (682K) -
AKIRA TAKADATE, NAONORI YOSHIMURA, SHUJIRO GOYA, HITOSHI MATSUMOTO1985 Volume 105 Issue 2 Pages 156-160
Published: February 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe fluorescence characteristics of amino- and anilino-derivatives of isocarbostyril, isocoumarin and 4-quinazolinone were examined comparatively in connection with their molecular structures. The fluorescence maxima of these compounds significantly depended upon the partial structures in molecules such as lactam structure for isocarbostyrils and 4-quinazolinones, lactone for isocoumarins, and guanidino for amino- and anilino-4-quinazolinones. Stereochemical configuration of anilino-substituted compounds was estimated from changes in fluorescence maxima. These derivatives other than 2-anilino-4-quinazolinone (IIIc) were highly fluorescent in ethanol. In contrast, IIIc exhibited extremely low fluorescence in ethanol and was practically non-fluorescent in aqueous solution ; in less-polar solvents and aqueous protein solution, the fluorescence significantly increased. 2-Anilino-4-methoxyquinazoline (V) has also similar characteristics to those of IIIc. Therefore, IIIc and V seemed to be applicable as fluorescence probes for the investigation of hydrophobic regions in protein.View full abstractDownload PDF (614K) -
KEISUKE KITAMURA, EIJI MORITA, KEIICHIRO HOZUMI1985 Volume 105 Issue 2 Pages 161-165
Published: February 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSA personal computer (NEC PC-8001) based spectral data acquisition system was constituted and a BASIC program to calculate the second derivative spectra by Savitzky-Golay method was composed. The analogue output from a recorder output terminal of a spectrophotometer was acquired through an analogue-to-digital converter of 12-bit and the sampling rate, i.e., the acquisition interval was controlled by a programable interrupt routine provided in a peripheral I/O unit (PC-8013). The acquisition with the interval of 125ms corresponded to four data points per 1 nm at the scan speed of 120 nm/min. The absorption spectra of a didymium filter and a salicylic acid in ethanol solution were measured as samples for sharp and broad peaks respectively. Their second derivative spectra were calculated on the program by using two kinds of 17 points-convolution integers derived from approximations to polynomials of the third and fifth degree. The second derivative signal shapes did not show considerable large differences between the third and fifth degree in both samples. However, the signal-to-noise ratios were appreciably better in the third degree than in the fifth.View full abstractDownload PDF (547K) -
YASUJI TAKASHIMA, SHIGEO TANAKA, SATOSHI HOSONO, ICHIRO KAWAMATA, HIRO ...1985 Volume 105 Issue 2 Pages 166-170
Published: February 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIn order to clarify the factors which enhance the efficacy of drug in cream, the correlation between the release of isothipendyl (IP) and the distribution of IP in the oil and aqueous phases of cream was investigated for creams with varied pHs. The distribution of IP in the phases of creams was measured by using ultracentrifugation and ultrafiltration methods. The release test of IP from cream was performed by using cellulose or dimethyl polysiloxane membrane. The release of IP through cellulose membrane was dependent on the amount of total IP in the aqueous phase of cream. On the other hand, the release of IP through dimethyl polysiloxane membrane showed the present of optimum pH value of cream, and the release was dependent on the product of amounts of the total IP and of free form IP in the aqueous phase. The results showed that it is necessary to use dimethyl polysiloxane membrane for the evaluation of the release of ionic drug from creams, and in order to obtain maximum release of drug, the pH of cream must be adjusted to the optimum pH value.View full abstractDownload PDF (546K) -
KOJI DAIGO, CHIAKI YAMADA, MANABU YAMAJI, NOBUO NAKAGIRI, MASAYUKI OKA ...1985 Volume 105 Issue 2 Pages 171-182
Published: February 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe effects of sodium alginate on the adhesion and aggregation of rat and human platelets were examined to investigate the role of this material in haemostasis. The adhesion of the rat and human platelets on the surface of glass beads, as well as the platelet aggregation in vitro, were enhanced in the presence of sodium alginate. This effect was dependent of the molecular weight and concentration of sodium alginate in the medium. The scanning and transmission electron microscopic observations revealed that the aggregated platelets, in the presence of sodium alginate, lost their discoid shape and formed irregular spheres with extended pseudopods. The number of microfibrils in the cytoplasm of these platelets markedly increased. These findings demonstrated that the aggregation of platelets was apparently enhanced in the presence of sodium alginate. Sodium alginate did not inhibit the aggregation of platelets induced by adenosine diphosphate or collagen, but instead, accelerated the action of these agents. Sodium alginate had no direct effects upon the release of serotonin from platelets and arachidonic acid cascade. The results of the present study suggest that the enhancing effect of sodium alginate on the adhesion and aggregation of platelets may have a significant role in haemostasis.View full abstractDownload PDF (2721K) -
SABURO SUGAI, YOSHIO KAJIWARA, KAZUHIKO KUBOTA1985 Volume 105 Issue 2 Pages 183-187
Published: February 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIn order to examine how quaternization of atropine changes its pharmacological profile, five atropinium compounds (1a-e) were synthesized and subjected to examination for acute toxicity, mydriatic activity and antispasmodic activity by using the isolated guinea pig ileum and in situ ileum. The five atropinium compounds (1a-e) had lower anticholinergic activity than parent atropine. Among the five compounds, those introduced less bulky hydroxyalkyl groups to their nitrogen atom showed higher anticholinergic activity or larger pA2 values than the others. It was of special interest that spasmolytic activity of the atropinium derivatives evaluated by use of in situ ileum was much higher than that expected from their anticholinergic activity obtained by the isolated ileum, and even close to that of atropine. Toxicity of the atropinium compounds was somewhat similar to that of atropine. These results are suggestive that the quaternization of atropine does not favor reduction of toxicity and enhancement of anticholinergic activity but seems to introduce ganglion blocking activity. This study also suggests us that spasmolytic activity of drugs should be evaluated on the basis of their activity of inhibiting in situ ileum motility.View full abstractDownload PDF (560K) -
ETSUO ITO, SUGURU TAKEO, HISAO KADO, HISAO YAMAMOTO, NOBUHIRO WATANABE ...1985 Volume 105 Issue 2 Pages 188-193
Published: February 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSAn antitumor polysaccharide, RBS (rice bran saccharide), has been prepared from rice bran with hot water extraction. Potent antitumor activities against sarcoma-180 solid tumors were observed not only by intraperitoneal administration but also by oral administration of purified RBS (RBS30F1). Physico-chemical properties of RBS30F1 are as follows ; (1) it is a white powder and soluble in water, (2) pH of the aqueous solution is neutral, (3) it is a glucan constructed by glucose as a sole sugar component, (4) it has α-1→6-glucosidic bond as a main frame including a small amount of α-1→4-glucosidic bond, (5) it contains a small amount of protein and minerals connecting to the polysaccharide, and (6) its molecular weight is over one million. Since it has been known little that α-glucan has potent antitumor activities, the fact mentioned above would be interesting to think about the relationship between structure and biological activities of polysaccharides. Antitumor activities of RBS30F1 are thought to be a kind of host mediated action that stimulates the immunological activities of the host, because the substance had no cytocidal activity against an animal cell line in vitro. No acute toxicity against rats was observed in the case of oral administration of crude RBS (RBS30).View full abstractDownload PDF (660K) -
YUKI NAKAJIMA, TAKAFUMI OKUTOMI, SYUNJI NATORI, MASATOSHI YAMAZAKI, DE ...1985 Volume 105 Issue 2 Pages 194-197
Published: February 25, 1985
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSTo know the role of animal lectins, we examined their participation in tumor recognition and rejection in cooperation with phagocytic cell cascade. We report here that Sarcophaga peregrina lectin induced in the hemolymph of larvae on injury can lyse MM46 tumor cells in cooperation with bone marrow cells. Carbohydrate moieties on cell membranes were recognized in cytolytic process. We had already reported the inhibition of tumor development in vivo by this lectin. This may be due to a phagocytic cell cascade reaction in which S. peregrina lectin can lyse tumor cells in cooperation with immature bone marrow cells, polymorphonuclear leukocytes and finally with macrophages.View full abstractDownload PDF (498K)
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