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Volume 98, Issue 7
Displaying 1-22 of 22 articles from this issue
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HIROYASU OGATA, SUMIO SUZUKI, TOSHIO SHIBAZAKI, AKIRA EJIMA, TETSUO IN ...1978 Volume 98 Issue 7 Pages 823-831
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSCorrelation was demonstrated between dissolution and several measures of bioavailability for powder and tablets of isonicotinic acid hydrazide (INH). Aqueous solution, powder, six tablets produced by Japanese manufacturers (A, B, C, D, E, F), and two tablets prepared in the laboratory (G-I, G-II) were examined. Dissolution rate curves, measured by the beaker method (pH 1.0, 75 rpm), were linearized by the Weibull plot and first-order plot applications. Dissolution efficiency was also calculated. In these samples, commercial tablets (A-F) and powder dissolved rapidly. Bioavailability was compared in seven formulations (solution, powder, A, B, C, G-I, G-II) by measuring amount of urinary excretion of INH in four healthy male subjects in cross-over study, by oral administration of 100 mg of each formulation after an overnight fasting. No significant differences were noted among aqueous solution, powder, A, B, C, and G-I in maximum excretion rate or in cumulative amount excreted during 24 hr. The maximum excretion rate time decreased in the order of solution, powder, A, B, C, G-I, and G-II. In vivo dissolution rate in the digestive tract, calculated by the de-convolution method, also showed the same tendency. The correlation between dissolution rate and bioavailability was examined quatitatively. The formulations, of which t50 values were less than 20 min or DE values were more than 50%, showed no difference in their bioavailability. However, the formulations that dissolved more slowly showed poor bioavailability. These results support the use of dissolution test to predict the bioavailability of INH.View full abstractDownload PDF (1006K) -
HISAYOSHI SUGIHARA, TOSHIAKI NIKAI, HUMIHIKO ODA, TETSUNOSUKE TANAKA1978 Volume 98 Issue 7 Pages 832-839
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSA human blood coagulation principle was isolated from the venom of a snake Agkistrodon acutus, by a combination of gel filtration on Sephadex G-75 and chromatographies on DEAE-Sephadex A-50, CM-Sephadex C-50, and DEAE-Sephadex A-50. By these procedures, 17.4 mg purified preparation was obtained from 1 g of crude venom. This coagulation principle hydrolyzed arginine esters, such as tosyl-l-arginine methyl ester (TAME) or benzoyl-arginine ethyl ester (BAEE), but did not digest casein. The coagulation and esterolytic activities were inhibited by diisopropyl fluorophosphate (DEP) or antiserum but not by soy bean trypsin inhibitor (SBTI), ethylene diamine tetra acetic acid (EDTA), cysteine, heparin, or p-chloromercuribenzoate (PCMB). The preparation was homogeneous as judged by disc electrophoresis on polyacrylamide gel and isoelectric focusing. The molecular weight of this protein was determined to be approximately 52000, and the isoelectric point was found to be pH 4.7 by isoelectric focusing with carrier ampholyte. The coagulation and esterolytic activities of this protein were 37.5 and 99.3 unit, respectively. This protein was stable to heat treatment, and between pH 6 and 8. Michaelis constant (Km) and inhibition constant (K1) for this protein were found to be 1.34×10-3 M and 1.92×10-3 M, respectively. This enzyme had some carbohydrates but did not contain any nucleic acids.View full abstractDownload PDF (973K) -
MASAYUKI NAKAGAKI, SHUJI KITAGAWA1978 Volume 98 Issue 7 Pages 840-849
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSAn ion can migrate against its concentration gradient because ionic flux in a mixed electrolyte solution is driven not only by the concentration gradient, but also by the electric potential gradient. Therefore, reverse permeation can occur when ionic flux driven by the electric force is large enough and is in the opposite direction, just as in a reverse diffusion reported for the HCl-CaCl2-H2O ternary system. In the present work ternary systems which contain two kinds of cations and one kind of anion, such as HCl-CaCl2-H2O, NaCl-CaCl2-H2O, HCl-KCl-H2O, and KCl-NaCl-H2O, were studied, and reverse permeation across the cellulose membrane was experimentally observed for both H+ containing systems and non-containing systems. It was concluded that the reverse permeation could occur easily when the mobility of coexisting ions is largely different and the effect of diffusion potential was pronounced. A liner relation between the permeability coefficient and the ratio of concentration gradients, as expected from the theory, was also verified experimentally, but the gradient of the straight line was different from the theoretical values calculated from nonequilibrium thermodynamics. In order to examine the permeation process more precisely, variation of permeation with time was studied for the HCl-KCl-H2O ternary system by using the cells with stirring. It was thus concluded that the reverse permeation was a transient phenomenon and that the permeability coefficients agreed well with theoretical values.View full abstractDownload PDF (981K) -
SHINICHIRO SAKAI, NORIO AIMI, JUNJI ENDO, MASATO SHIMIZU, ETSUJI YAMAN ...1978 Volume 98 Issue 7 Pages 850-862
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe C/D ring closing reaction of optically active 2, 3-seco-2, 3-dihydroakuammigine (II) with Hg (OAc)2-EDTA·2Na was reinvestigated and the isolated products were found to be tetrahydroalstonine (III), insideheteroyohimbine (V), and insidedehydroyohimbine (VI). There was no evidence for the formation of akuammigine (V), and insidedehydroyohimbine (VI). There was no evidence for the formation of akuammigine (IV), different from that of Uskokovic using racemic compound (II) as the starting material. Modified Polonvski reaction of compound II N-oxide (IXa) gives IV, V, and a piperidine derivative Xb. Bond cleavage between N4 and C5 of compound (II) with carbobenzoxy chloride formed an urethane derivative (Xc) as a major product. Compound Xc yielded a piperidine derivative (Xa) by hydrogenolysis. On the other hand, pteropodine (Ia) was transformed to Xa via XIIIc, d. The synthesis of aricine (XIXa) and reserpinine (XIXb) using Xa was achieved by the usual method. Combination of these procedures forms a new general method to synthesize various kinds of aromatic substituted heteroyohimbinoid indole alkaloids.View full abstractDownload PDF (1618K) -
SHIGERU KOBAYASHI, MASARU KIHARA, HIROSHI MATSUMOTO1978 Volume 98 Issue 7 Pages 863-868
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSApogalanthamine analogs (1-4), were prepared by photolysis of the hydrochlorides of halogeno-N-benzyl-β-phenethylamine derivatives (5-8). The yield of 3 and 4 from the halogeno-amines (7, 11 and 8, 12, respectively) having a halogen atom in the benzyl group were found to be better than those of 1 and 2 from the halides (5, 9 and 6, 10, respectively) having a halogen atom in the phenethyl group. On photolysis, the analogs (1-4) seem to be formed via a phenyl radical (I or II) and a cyclohexadienyl radical (III or IV).View full abstractDownload PDF (745K) -
SHOJI TAKEMURA, HIROMI TERAUCHI, KEIKO KOWATA, KEIKO NAKANO, YUICHI OK ...1978 Volume 98 Issue 7 Pages 869-879
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIn order to examine bioactivities, simple amino acid derivatives mainly of DL-phenylalanine were prepared. N-Alkyl or N-aralkyl derivatives of DL-phenylalanine (1-11), DL-alanine (12-13), and DL-leucine (14) were synthesized by two routes ; (a) via Schiff bases prepared from amino acids and carbonyl compounds, and (b) direct reductive alkylation of the amino acids with sodium cyanoborohydride. N-Acetyl- and N-benzoxycarbonyl-phenylalanines were coupled with various amines by the mixed anhydride procedure to give the corresponding amides (15-24). Some of the N-benzoxycarbonyl derivatives were hydrogenolyzed to produce free amino acid amides (25-27). 4-Nitro-(28), 4-amino-(29), and 4-(4-dimethylaminophenyl) azo (30-31) derivatives of phenylalanine were synthesized. N-Phthaloylamino acids were condensed with hydrazobenzene to yield diphenylhydrazides (32-33). Compound 32 was converted to free aminoacyldiphenylhydrazide (48). N-Diphenylacetamino acids (34-40) were prepared by the usual technique using diphenylacetyl chloride. Some cyclized derivatives of the amino acids (41-47) were also prepared. Biological tests, including antibacterial, and the action on central nervous, circulation, muscular systems, etc., of these compounds were examined, but none of them showed much activity.View full abstractDownload PDF (1061K) -
NORIO AWATA, KEIICHI YAMAMOTO, ISAO SUGIMOTO1978 Volume 98 Issue 7 Pages 880-885
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSMetabolic fate of dehydroepiandrosterone sulfate (I-S) was investigated in rabbits after its oral administration. I-S and androst-5-ene-3β, 17α-diol 3-monosulfate (II-S) were isolated from the urine as the major metabolite, demonstrating a predominant direct metabolism (without splitting of the ester linkage) and a selective 17α-hydroxylation. The plasma level of I-S and II-S reached maximum (3.1 and 26μg/ml) at 1 hr after oral administration of I-S (50 mg/kg). On the other hand, cumulative excretion of I-S and II-S in urine during 24 hr was 24 and 17 mg, respectively. Furthermore, II-S, androst-5-ene-3β, 17α-diol 3, 17-disulfate (II-D), androst-5-ene-3β, 17β-diol 3-monosulfate (III-S) and androst-5-ene-3β, 17β-diol 3, 17-disulfate (III-D) were each administered orally to clarify the direct metabolism of I-S. It was found that I-S and II-S were easily interconverted in rabbits.View full abstractDownload PDF (709K) -
MOTOHARU JUICHI, YOSHIKO ANDO, YUKARI YOSHIDA, JUNICHI KUNITOMO, TETSU ...1978 Volume 98 Issue 7 Pages 886-890
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe tertiary phenolic alkaloidal components of the rhizoma of Cocculus trilobus DC. (Menispermaceae) were examined. Two new erythrinan alkaloids, named coccutrine and dihydroerysovine, and two known erythrinan alkaloids, cocculine (V) and cocculolidine (VII), were isolated. The structures of coccutrine and dihydroerysovine were determined by spectroscopic methods as (I) and (III), respectively.View full abstractDownload PDF (729K) -
EISAKU HAYASHI, TAKEO HIGASHINO, SHINICHI SUZUKI1978 Volume 98 Issue 7 Pages 891-897
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESS1-Phenyl-1H-pyrazolo [3, 4-d] pyrimidine-4-carbonitrile (I) is synthesized by the application of potassium cyanide to 4-(p-tolysulfonyl)- (II) or 4-chloro-1-phenyl-1H-pyrazolo [3, 4-d] pyrimidine (III) in dimethyl sulfoxide. Application of a nucleophilic reagent to I results in two kinds of reaction according to the kind of the reagent used. One (A) is the substitution of the -CN group by the attack of the reagent on carbon at 4-position to which -CN is bonded. The other (B) is the addition reaction to -CN group by the attack of the reagent on the carbon atom of -CN group. The reaction (A) occurs with hydroxide ion, alkoxide ion, amines, hydrazines, and carbanions (active methylene compound or ketone in the presence of sodium amide). Reaction (B) occurs in acid hydrolysis and in the reaction with hydrogen peroxide in alkalinity, hydroxylamine, and hydrogen sulfide, resulting in the formation of carboxylic acid, carboxamide, carboxamidoxime, and thiocarboxamide, respectively. Reduction with Raney nickel in formic acid results in two-way reactions ; reduction of -CN group to -CH2NH2 group (B) or replacement of -CN group with a hydride ion (A).View full abstractDownload PDF (888K) -
KEIJI WAKABAYASHI, TAKESHI YAMAMOTO, KUNIRO TSUJI, HIROSHI ZENDA, TAKU ...1978 Volume 98 Issue 7 Pages 898-903
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSAs a part of studies on active principles of tar, antifungal constituents in fish-meal tar were examined. Three active principles, A, B, and C, were isolated by a suitable combination of counter-current distribution, column chromatography, and gel filtlation. The isolated compounds were found to be norharman (A), harman (B), and 4-azaskatole (C). Antifungal activities of 1-alkyl-β-carbolines (R : H-C10) were also discussed.View full abstractDownload PDF (676K) -
KEIJI WAKABAYASHI, TAKESHI YAMAMOTO, KUNIRO TSUJI, HIROSHI ZENDA, TAKU ...1978 Volume 98 Issue 7 Pages 904-909
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSPast studies on active principles in tar has shown that active principles were classified into basic and acidic parts, namely pyrolysis of protein-rich sourses like eggs, nonfat soybean, or fish meal mostly produced N-heteroaromatic compounds, while pyrolysis of carbohydrate-rich sources like wood or rice bran produced acidic compounds. These results prompted clarification of pyrosynthetic mechanisms of fomation of these N-heteroaromatic compounds under pyrolytic conditions. A series of amino acids was pyrolyzed and their antifungal activities were tested to find that pyrolysates of aromatic amino acids (tryptophan, phenylalanine, tyrosine), lysine, and arginine, had a potent antifungal activity. Among them the active principles in the pyrolysate of DL-tryptophan were identified as norharman, harman, and 1-ethyl-β-carboline. It was also found that 1-isobutyl-, 1-isopentyl-, and 1-(2-methylbutyl)-β-carboline, which were isolated from egg tar, were formed from the pyrolysis of DL-tryptophan-leucine and DL-tryptophan-isoleucine mixture.View full abstractDownload PDF (666K) -
KUNIRO TSUJI, TAKESHI YAMAMOTO, HIROSHI ZENDA, TAKUO KOSUGE1978 Volume 98 Issue 7 Pages 910-913
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIsolation and structural determination of antifungal principles from phenylalanine pyrolysate are described. Two antifungal constituents (I and II) were isolated from the basic fraction of pyrolytic product by means of distillation under reduced pressure, countercurrent distribution, and column chromatography. Active principles : (I), liquid, picrate, mp 150-151° ; C11H9N·C6H3N3O7. (II), mp 130-132° ; C11H10N2, UV λMeOHmax nm (log ε) : 268 (4.33), 315 (sh) ; λMeOHmax-HCl nm (log ε) : 262 (4.32), 319 (3.79) ; picrate, mp 270-272°. They were identified as 3-phenylpyridine and 2-amino-5-phenylpyridine, respectively.View full abstractDownload PDF (505K) -
TAKASHI YAZAKI, MASAHIRO MAKINO, TAKESHI YAMAMOTO, KUNIRO TSUJI, HIROS ...1978 Volume 98 Issue 7 Pages 914-922
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIsolation and structure determination of antifungal principles from tyrosine pyrolysate are described. L-Tyrosine was heated at 350-400°and seven antifungal constituents (I-VII) were isolated from the pyrolysate by a suitable combination of distilation, column chromatography, and gel filtration. Active principles ; (I), mp 230° (subl.), C14H14O2 ; (II), mp 265° (dec.), C14H12O2 ; (III), mp 130-131°, C14H14O2 ; (IV), mp 114-115° ; C14H15NO ; (V), mp 193-195°, C11H9NO ; (VI), mp 244-245°, C16H13NO ; (VII), mp 144-145°, C13H13NO. These were found to be identical with 4, 4'-dihydroxy-dibenzyl, 4, 4'-dihydroxy-trans-stilbene, 4-hydroxybenzyl p-tolyl ether, N-phenyltyramine, 3-(p-hydroxyphenyl) pyridine, 3-(p-hydroxyphenyl)-6-methylquinoline, and 4-amino-2'-hydroxydiphenylmethane, respec-tively.View full abstractDownload PDF (977K) -
MAMORU NOGUCHI, MICHINORI KUBO, YORIKO NAKA1978 Volume 98 Issue 7 Pages 923-928
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSTitrimetric determination of alkaloids in commercial ephedra herb was made by three extraction methods, using ether (JP IX), MeOH, or hot water, and the highest content was obtained by hot water extraction. High-speed liquid chromatographic determination was also made on the same samples, using two column materials, Bondapak C18 and μPorasil, with MeOH : NH4OH (400 : 8) as the developing solvent, and a good correlation was found between the values obtained by titrimetry and those by liquid chromatography. The recovery of ephedrine or alkaloids from the decoction of ephedra herb added with glycyrrhiza radix, cinnamon cortex, armeniac seeds, or their mixture (Maoo-to without ephedra herb) ranged between 55 and 83%. The pH of these decoctions were below 7.0, where ephedrine and methylephedrine did not distill out with steam during decoction. It was assumed that the decrease in alkaloid recovery in Maoo-to originated in adsorption of these alkaloids on crude drug materials in the decoction solution.View full abstractDownload PDF (661K) -
TEISUKE OKANO, TAKASHI HORIE, JUNKO OHNO1978 Volume 98 Issue 7 Pages 929-936
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSExaminations were made on the photodynamic action of anthraquinone derivatives on calf thymus DNA and also on the mechanism involved in this reaction. When the aqueous mixture of DNA and anthraquinone derivatives was irradiated by light above 290 nm, melting point and viscosity of DNA decreased in the order of 2-anthraquinonesulfonate, 2-anthraquinonecarboxylic acid, and 1-anthraquinonesulfonate. Such effect was not seen in 1, 5- and 1, 8-anthraquinonedisulfonate. The degree of the photodynamic action of anthraquinones on DNA paralleled the quantity of hydrogen peroxide produced by the photoirradiation of aqueous solution of anthraquinone derivatives. Results of the "i-assay" and sucrose density gradient centrifugation experiments indicated that scission of the DNA chain took place by the photodynamic action of anthraquinone derivatives. Examination of the reaction mechanism revealed that hydroxy radical produced in the aqueous solution of anthraquinone derivatives during photoirradiation played an important role in the photosensitization reaction of DNA.View full abstractDownload PDF (939K) -
HIROSHI ISHIHAMA, HIDEKI KIMATA, MASAHIRO YONEMITSU, SHU MATSUMOTO, TA ...1978 Volume 98 Issue 7 Pages 937-943
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSMetabolic fate of the cyclopropylmethyl group of prazepam (PZ) was studied in rats. After oral administration of [sidechain-14C] PZ, the radioactivity was detected in various tissues, indicating the extensive uptake of this compound. A higher level was seen in the stomach, kidneys, heart, intestine, liver, and lung. The radioactivity in the liver, kidneys, and blood reached a peak level within 1 hr after dosing, but it was delayed in other tissues in reaching a peak level. Thereafter, the radioactivity in the tissues decreased gradually. During 24 hr, 59.7 and 12.4% of the radioactivity were excreted in the urine and feces, respectively. Only 0.26% of the dose was excreted in the expired air during 24 hr, suggesting that there was neither oxidation of the α-methylene of the cyclopropylmethyl group to CO2 nor degradation of the cyclopropane ring. A major urinary metabolite was isolated and identified as N-cyclopropylcarbonylglycine (CPCG). Its mass spectrum was identical with that of the authentic sample. Reverse isotope dilution analysis showed that CPCG was responsible for 95.2% of the radioactivity in the urine. In addition, the acute toxity and effects of a metabolic intermediate, cyclopropanecarboxylic acid (CPCA), on ketone bodies in the blood and urine were tested. These results suggest that CPCA takes little part in the toxicity of PZ.View full abstractDownload PDF (863K) -
SHIGEO KABUTO, TARO TAMAKI, TAKASHI KOIDE, HIROSHI ISHIHAMA1978 Volume 98 Issue 7 Pages 944-949
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSMetabolism of orally administered [5-14C] prazepam was investigated in cynomolgus monkeys. The radioactivity in the plasma reached a peak level at 3-6 hr after dosing, and thereafter declined gradually with a half-life of about 21 hr. Major metabolites in the plasma were desalkylprazepam (DPZ), 3-hydroxyprazepam (3-HPZ) glucuronide and oxazepam (OX) glucuronide. These glucuronides were rapidly excreted, and DPZ accounted for more that 70% of the total plasma metabolites after 12 hr. More than 70% of the radioactivity were excreted mostly in the urine within 3 days. Major metabolites in the urine were OX glucuronide and 3-HPZ glucuronide. The amount of these glucuronides did not decrease markedly until 48 hr after dosing. 4'-Hydroxydesalkylprazepam sulfate accounted for only 2-4% of the total urinary metabolites. In addition, a very small amount of prazepam (PZ) was detected in the plasma and urine. Most of fecal metabolites was unabsorbed PZ, which indicates that the fecal excretion via bile has little significance in monkeys. These results suggest that the PZ metabolism in the monkey resembles that in man, though the rate of metabolism in the monkey is faster than that in man.View full abstractDownload PDF (686K) -
SHINICHIRO SAKAI, NOBUO SHINMA1978 Volume 98 Issue 7 Pages 950-964
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSBy utilizing the C/D ring cleavage reaction with BrCN and its reclosing reaction with NH4OAc/HOAc, chemical conversion of corynanthe-type alkaloids, hirsutine (9a) and geissoschizine methyl ether (6), into C-mavacurine-type alkaloids, 19, 20β-dihydro-16-epipleiocarpamine (25) and 16-epipleiocarpamine (30), was accomplished. This partial synthesis of 30 revealed the absolute configuration of C-mavacurine type alkaloids.View full abstractDownload PDF (1602K) -
SHIGETAKA YOSHINA, MOTOI YOGO1978 Volume 98 Issue 7 Pages 965-968
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSBromination of 4-methylfuro [2, 3-b] quinoline (I) with bromine in carbon tetrachloride afforded 2, 3-dibromo-4-methyl-2, 3-dihydrofuro [2, 3-b] quinoline (II). Dehydrobromination of II yielded two isomeric compounds, 3-bromo-4-methylfuro [2, 3-b] quinoline (III) and 2-bromo-4-methylfuro [2, 3-b] quinoline (IV). On the other hand, treatment of I with N-bromosuccinimide in carbon tetrachloride gave 4-bromomethylfuro [2, 3-b] quinoline (V). The reaction of V with NaCN in DMF gave an unexpected dimeric cyano compound (VI), whereas the reaction with aliphatic secondary amines (diethylamine, piperidine, morphorine, or pyrrolidine) in benzene gave the expected tert-amino compounds (VIIa-VIId).View full abstractDownload PDF (528K) -
TOZABURO KURIHARA, MASAO KIKUCHI1978 Volume 98 Issue 7 Pages 969-972
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSFrom the essential oil of the flower of Cornus controuersa HEMSL., cornusol (3, 7-dimethyl-1, 6-octadien-3, 4-diol, a new compound), ethyl salicylate, methyl salicylate, phenol, cresol (o-, m-, p-), guaiacol, benzyl alcohol, phenethyl alcohol, l-linalool, cis-3-hexen-1-ol, benzaldehyde, benzoic acid, salicylic acid, 12 hydrocarbons, and 14 fatty acids were isolated. 2α-Hydroxyursolic acid, ursolic acid, quercetin, kaempferol, caffeic acid, p-coumaric acid, salicylic acid, 8 hydrocarbons, and 9 alcohols were also identified from the steam distillation residue of the etherial extract.View full abstractDownload PDF (593K) -
KENICHI SASAKI, MASAAKI SAITOH, GIICHI TAKAYANAGI1978 Volume 98 Issue 7 Pages 973-976
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSEffect of egg lectin from Rana japonica (RJ-lectin) on the growth of Ehrlich solid tumor was examined in male ddY mice, using the temporary circulation-stop method as an in vitro model. Lectin was injected intravenously 24 hr after inoculation of Ehrlich ascites carcinoma (1×106 cells) into the right thigh. The upper thigh was tightly ligated to stop blood circulation, and the animals were kept without movement with warming of the leg at 37° for 30 min. The antitumor activity was estimated by weihing the solid tumor on the 10th day after cell inoculation. Intravenous administration of RJ-lectin in the temporary circulation-stop method more strongly suppressed the tumor growth than by intravenous injection of the lectin without any treatment. The inhibitory action of RJ-lectin in the temporary circulation-stop method depended on the number of administrations. The inhibition rate of the lectin at 10 or 20 mg/kg (three intravenous administrations) was 93 and 77%, respectively. In this method the lectin may easily contact with tumor cell as observed in vitro and is able to react with the cells directly for a long time. It is suggested that RJ-lectin suppresses the tumor growth by direct cytotoxic effect on tumor cells.View full abstractDownload PDF (633K) -
OSAMU ISHIKAWA, TSUTOMU HASHIMOTO, TERUMI NAKAJIMA, OSAMU TANAKA, HIDE ...1978 Volume 98 Issue 7 Pages 976-979
Published: July 25, 1978
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSFor the analysis of Coptidis Rhizoma, high-speed liquid chromatography was examined, not only for its major alkaloid, berberine, but also for its minor alkaloids. It was found that under an appropriate condition [on starch gel (LS-170), eluted with the solvent system of H2O : MeCN : AcOH : Et3N=80 : 20 : 0.3 : 0.745, pH 8.5], sufficient separation of berberine, magnoflorine, jatrorrhizine, palmatine, coptisine, and some other unidentified alkaloids was obtained. By means of the present procedure, content of berberine and relative content of palmatine and coptisine to berberine in some of wild and commercial coptis rhizomes were determined. Since the solvent system does not contain any nonvolatile salt, the present technique also offers the possibility of application to rapidpreparative separation of alkaloids of this type by liquid chromatography. The application to analysis of alkaloids of phellodendron-cortex is also described.View full abstractDownload PDF (477K)
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