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Biomedical subjects

H Kasai

Publications and source records attributed to H Kasai.

At least 343 records · Page 19Linked to original sources

[Pharmacological studies of guanabenz: effects of the central nervous system].

The general pharmacological properties of guanabenz (Wy-8678), a new centrally acting antihypertensive agent, on the central nervous system were studied in mice, rats and rabbits, and they were compared with those of clonidine. In mice, guanabenz (1-30 mg/kg, i.p.) showed overt sedation dose-dependently, like clonidine (0.3 or 1 mg/kg, i.p.). At doses (2.5-20 mg/kg, p.o.) not causing muscle relaxant action, guanabenz impaired rotarod performance, inhibited conditioned avoidance responses and maximum electroshock seizure, prolonged thiopental sleeping time, and lowered body temperature in rats. These central depressant effects were observed following oral administration of clonidine at much lower dose levels. In rabbits, neither guanabenz (5-20 mg/kg, p.o.) nor clonidine (0.5 or 1 mg/kg, p.o.) affected body temperature. These findings suggest that the central depressant activities of guanabenz, qualitatively very similar to clonidine, are much less potent than those of clonidine.

Animals↗

Identification of novel 7,12-dimethylbenz[a]anthracene adducts in cellular ribonucleic acid.

The interaction of guanosine with 7,12-dimethylbenz[a]anthracene (DMBA) 5,6-oxide under alkaline conditions resulted in the formation of six derivatives. These six compounds were cochromatographed with nucleosides obtained by hydrolysis of RNA isolated from rat liver cells treated with [3H]DMBA. The cochromatography showed that three of these adducts were formed in cellular RNA. The three products constituted less than 5% of the total nucleoside-DMBA adducts as shown by chromatography on Sephadex LH-20 and high-pressure liquid chromatography. In one of them, the 2'-hydroxy group of the ribose moiety of guanosine was linked to the C-5, and in the second, to the C-6 position of the DMBA 5,6-oxide residue. In the third derivative, the C-8 position of guanosine was linked to the C-5 of the DMBA 5,6-oxide moiety. These results show, for the first time, modifications of the ribose moiety and of the guanine residue at the C-8 position in the cellular RNA by a metabolite of a polycyclic hydrocarbon.

9,10-Dimethyl-1,2-benzanthracene↗

Effect of methyl substitution on mutagenicity of 2-amino-3-methylimidazo[4,5-f]quinoline, isolated from broiled sardine.

2-Amino-3-methylimidazo[4,5-f]quinoline [I] is a potent mutagen isolated from broiled sun-dried sardine. [I] and its seven of derivatives, (two isomers, one demethylated derivative and four methyl-substituted derivatives), were tested for mutagenicity on Salmonella typhimurium TA98 and TA100 in the presence of S9 mix. 2-Amino-1,4-dimethylimidazo[4,5-f]quinoline was the strongest mutagen of these 8 compounds on TA98, giving 159,000 revertants/nmol (750,000 revertants/micrograms). The demethylated derivative, 2-aminoimidazo[4,5-f]-quinoline, had very weak mutagenicity, inducing only 55 revertants/nmol (200 revertants/micrograms). Compounds having a methyl group at position N-1 or N-3 of 2-aminoimidazo[4,5]f]quinoline were strong mutagens. The 1,5-dimethy-derivative was more mutagenic than 3,5-dimethyl-derivative. Introduction of a methyl group at position 4 and position 5 enhanced and reduced the mutagenicity, respectively. All the compounds tested were more mutagenic to TA98 than to TA100, but their relative orders of mutgenicity with TA98 and TA100 were the same.

Animals↗

Formation of mutagens in cooked foods. III. Isolation of a potent mutagen from beef.

The major mutagenic component of fried beef has been isolated using a series of chromatographic steps. The pure compound has been analyzed by low and high resolution mass spectroscopy and nuclear magnetic resonance spectroscopy. The results indicate that the molecular weight of this extremely mutagenic compound is 198, with an elemental composition of C11H10N4. The compound is different from the known mutagenic pyrolysis products of amino acids or proteins.

Animals↗

Detection of potent mutagens, Trp-P-1 and Trp-P-2, in broiled fish.

The potent mutagens Trp-P-1 (3-amino-1, 4-dimethyl-5H-pyrido-[4,3-b]-indole) and Trp-P-2 (3-amino-1-methyl-5H-pyrido[4,3-b]indole) are known to be produced by pyrolysis of tryptophan [8]. To determine whether such mutagens are produced by cooking foods, the fractions obtained from broiled sardines cooked in the ordinary way were analysed by gas chromatography/mass spectrometry. The results showed that 13.3 ng of Trp-P-1 and 13.1 ng of Trp-P-2 were, in fact, present per gram of broiled sardines.

Animals↗

Purification and characterization of calcium-binding protein containing gamma-carboxyglutamic acid from rat bone.

A gamma-carboxyglutamic acid (Gla)-containing protein was purified from rat femur cortical bone. The presence of 4 Gla residues in the rat protein was shown by amino acid analysis on alkaline and acid hydrolysates. The protein was extracted from rat cortical bone with 0.5 M EDTA (pH 7.6) and purified from the EDTA extracts by gel filtration on Sephadex G-100 and ion-exchange chromatography on DEAE-Sephadex A-25. The protein has a molecular weight of about 6,000 on the basis of amino acid composition. The protein had 56 amino acid residues containing significant amounts of Asp, Glu, and Gla (acidic amino acids). The protein showed calcium-binding activity with Kd = 0.2 mM and calcium-dependent electrophoretic mobility.

1-Carboxyglutamic Acid↗

Under-modified Y base in a tRHAPhe isoacceptor observed in tumor cells.

A fluorescent wye (Ye) was isolated from tRHAPhe specific to Ehrlich ascites cells. The structure was determined to be alpha-amino-beta-hydroxy-4,9,-dihydro-4,6-dimethyl-9-oxo-1-H-imidazo(1,2-alpha)purine-7-butyric acid: namely the compound lacking methyl carboxyl and methyl groups and thus is an under-modified precursor of hydroxy-Y base present in normal liver tRNAPhe.

Animals↗

Three-dimensional structure of hyper-modified nucleoside Q located in the wobbling position of tRNA.

The hyper-modified nucleoside Q (queuosine) is exclusively located in the wobbling position of anticodons of tRNATyr tRNAHis, tRNAAsn and tRNAAsp that recognise codons NAUC (ref. 1). Queuosine and its hexose-containing derivatives are widely distributed in microorganisms, animals and plants. We confirm here the chemical structure of queuosine as 7-(3, 4-trans-4, 5-cis-dihydroxy-1-cyclopenten-3-ylaminomethyl)-7-deazaguanosine (Fig. 1). The unique structural features of Q are the unusual cyclopentenediol side chain and the 7-deazaguanine ring. Queuosine is one of the most complicated modified nucleosides found thus far.

Anticodon↗

Specific fluorescent labeling of 7-(aminomethyl)-7-deazaguanosine located in the anticodon of tRNATyr isolated from E. coli mutant.

Under-modified E. coli tRNATyr that contains 7-(aminomethyl)-7-deazaguanosine in place of Q nucleoside can be chemically modified by dansyl chloride under neutral conditions. Fluorescent labelling specifically occurred only in the 7-(aminomethyl)-7-deazaguanine moiety. The modified tRNATyr was found to be active both in aminoacylation and in binding to ribosomes.

Anticodon↗

Novel mechanism of post-transcriptional modification of tRNA. Insertion of bases of Q precursors into tRNA by a specific tRNA transglycosylase reaction.

The guanine insertion enzyme isolated from Escherichia coli (tRNA transglycosylase) catalyzed the incorporation of bases of Q (queuosine) precursors into E. coli undermodified tRNAAsn and tRNATyr. These bases of Q precursors were inserted in the first position of the anticodon of tRNASn and tRNATyr, replacing guanine originally located in that position. This is a novel type of post-transcriptional modification, inserting a modified base into the polynucleotide chain by cleavage of the N--C glycoside bond without breakage of the phosphodiester bond. One of the bases of Q precursors, 7-(aminomethyl)-7-deazaguanine, was found in the acid-soluble fraction of E. coli cells, supporting the conclusion that formation of Q, 7-(3,4-trans-4,5-cis-dihydroxy-1-cyclopenten-3-ylaminomethyl)-7-deazaguanosine, in tRNA in vivo actually proceeds by the tRNA transglycosylase reaction.

Escherichia coli↗

Fractionation of a mutagenic principle from broiled fish by high-pressure liquid chromatography.

A mutagenic principle present in the basic fraction of broiled sardines cooked in the ordinary way was fractionated by high-pressure liquid chromatography using a reversed-phase column. Results indicated that the major mutagenic principle is not identical with any of the mutagens previously isolated from amino acid pyrolysis products, and that a new, unidentified mutagen exists in broiled sardines.

Amino Acids↗

Isolation of hydroxy-Y base from rat liver tRNAPhe.

A Y-base derivative was isolated from rat liver tRNAPhe and its structure was assigned to be alpha-(carboxyamino)-beta-hydroxy-4,9-dihydro-4,6-dimethyl-9-oxo-1H-imidazol[1,2-a]purine-7-butyric acid dimethyl ester (hydroxy-Y), based on the results of mass spectrometry and chemical degradation. This modified base seems to be the major fluorescent component of rat liver tRNAPhe; the peroxy-Y base previously isolated from rat liver tRNAPhe and characterized by Nakanishi and his coworkers (1,2) was not present in our preparation.

Animals↗