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Biomedical subjects

F Yamada

Publications and source records attributed to F Yamada.

At least 73 records · Page 4Linked to original sources

Mutagenicity studies on fenitrothion in bacteria and mammalian cells.

The mutagenicity of fenitrothion was determined in strains of Salmonella typhimurium and Escherichia coli. Fenitrothion was found to be non-mutagenic in Salmonella typhimurium strains of TA98, TA1535 and TA1537 and in Escherichia coli WP2uvrA both with and without S9 mix, while weak mutagenicity was observed only in Salmonella typhimurium TA100 and enhanced by the addition of S9 mix. The mutagenicity observed in the TA100 strain was not expressed in a nitroreductase-deficient strain, TA100 NR, and decreased in a transacetylase-deficient strain, TA100 1,8-DNP6. The mutagenicity of fenitrothion was also examined by a gene mutation assay using the gene for hypoxanthine-guanine phosphoribosyltransferase (hgprt) in V79 Chinese hamster lung cells. Fenitrothion did not induce any increment of 6-thioguanine-resistant mutant cells at doses ranging from 0.01 to 0.3 mM regardless of the presence or absence of S9 mix. These results suggest that reduction of fenitrothion by a bacterial nitroreductase of TA100 to an active form is essential for the expression of the mutagenicity of fenitrothion in TA100 and that a bacterial transacetylase of TA100 also has an important role in the process of mutagenic activation.

Animals↗

Estrogen and androgen receptor binding affinity of 10 beta-chloro-estrenen derivatives.

10 beta-Chloroestradien-3-one and its derivatives with chlorine substitution in ring A have been prepared. Efficient synthetic methods for 2-chloro- and 4-chloroestradiol are described. The binding affinity of these chlorinated estrogens to the uterine estrogen receptor was measured by a competitive binding assay using [3H]estradiol as ligand. 4-Chloroestradiol showed high binding affinity for the receptor (110% of that of estradiol). 2-Chloroestradiol, 10 beta-chloroestradien-3-one and 4,10 beta-dichloroestradien-3-one had moderate binding affinity. The structures of 10 beta-chloroestradien-3-one and androst-1,4-dien-3-one are very similar and can almost be superimposed. However, their binding affinities to the estrogen and androgen receptor were different. Androst-1,4-dien-3-one displayed no measurable affinity for the estrogen receptor and measurable affinity for the androgen receptor whereas 10 beta-chloroestradien-3-one had very low affinity for the androgen receptor.

Animals↗

Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives.

Several steroid derivatives having the delta 11-pregnane skeleton with a 17-gamma-spirolactone function were synthesized to evaluate their antialdosterone activity and to elucidate the relation between their binding affinity to mineralocorticoid receptor (MR) and their mineralo- and/or antimineralocorticoid activity. Although many of the synthesized compounds showed strong binding affinity for the MR and aldosterone agonist activity, 3-(17 beta-hydroxy-3-oxoandrosta-1,4,6,11-tetraen-17 alpha-yl)propionic acid gamma-lactone exhibited good aldosterone antagonist activity in an in vivo assay. Its in vivo antiandrogenic activity was also found to be relatively weak.

Adrenalectomy↗

Quantitative measurement of endotoxin in rainbow trout (Salmo gairdneri) serum by the chromogenic substrate method.

The amount of endotoxin in serum collected from normal rainbow trout (Salmo gairdneri) and trout inoculated with viable Vibrio anguillarum or lipopolysaccharide (LPS) extracted from bacteria was determined by the chromogenic substrate method. The mean values of endotoxin in four different groups of normal rainbow trout sera ranged from 31.9 to 65.3 pg/ml. When fish were inoculated with viable bacteria (1 x 10(8], they became septicaemic and a large amount of endotoxin ng/ml) was detected in the sera. In fish inoculated with a smaller number of bacteria the amount of endotoxin was several times higher than that of normal fish in spite of failure of bacterial isolation. Although the endotoxin level in serum increased rapidly (greater than 100 ng/ml) after intraperitoneal inoculation with purified V. anguillarum LPS (540 micrograms), no fish died during the experiment. The high level of endotoxin in normal rainbow trout and the resistance of trout to endotoxin are in striking contrast to those of mammalian and avian species.

Animals↗

Dopamine receptor stimulating effects of chanoclavine analogues, tricyclic ergot alkaloids, in the brain.

The abilities of tricyclic ergot alkaloids, chanoclavine-I and its analogues, and bromocriptine to stimulate dopamine receptors in the brain were investigated. Receptor binding of 3H-spiperone has shown that bromocriptine exhibits clear affinity for this compound. The order of displacement potencies was bromocriptine much greater than ergometrine, KSU-1415 greater than chanoclavine-I, KSU-1118, KSU-1791. In the striatum of mice treated with an amino acid decarboxylase inhibitor, gamma-butyrolactone-induced DOPA accumulation was markedly inhibited by bromocriptine and KSU-1415, but not inhibited by chanoclavine-I. In mice with unilateral striatal 6-hydroxydopamine lesions, bromocriptine and KSU-1415 produced a long-lasting contralateral rotation that was suppressed by prior treatment with (+/-)-sulpiride. These results suggest that a tricyclic ergot alkaloid of the chanoclavine type stimulates D-2 receptors in the brain.

4-Butyrolactone↗

Antimutagenicity of extracts from crude drugs in Chinese medicines.

The antimutagenicity of extracts from crude drugs was studied by the Ames bioassay system. The crude drugs chosen were medical plants used very frequently as Chinese medicines. Each crude drug was extracted with hot water similar to the method of Chinese medical treatment. Antimutagenicity of the extract was found with 4 kinds of crude drugs, Paeoniae radix, Bupleuri radix, Hoelen and Glycyrrhizae radix. Each extract of the crude drug showed a different type of antimutagenic action from the others.

Humans↗

Phagocytic activity of macrophages of rainbow trout against Vibrio anguillarum and the opsonising effect of antibody and complement.

The phagocytosis of Vibrio anguillarum by peritoneal macrophages from normal rainbow trout was enhanced by antibody and complement. Treatment of either macrophages or the bacteria by antibody also enhanced opsonisation. Five weeks after immunisation with V anguillarum, the phagocytic activity of macrophages from rainbow trout was increased significantly compared with the activity of those from unvaccinated fish. Although agglutinin titres did not increase until three weeks after immunisation, seven out of 10 fish challenged one week after immunisation survived, indicating that immunised fish had developed resistance to vibrio infection before significant levels of antibody or phagocytic activity became detectable.

Animals↗

Ferredoxins from the photosynthetic purple non-sulfur bacterium Rhodopseudomonas palustris. Isolation and amino acid sequence of ferredoxin I.

Two ferredoxins, ferredoxins I and II, were prepared from Rhodopseudomonas palustris. They were separated on a Sephadex column after carboxymethylation and ferredoxin I, the major component, was subjected to an amino acid sequence study. The protein was composed of 63 amino acid residues and the sequence was as follows: (sequence; see text). The molecular weight was calculated to be 6,718, excluding iron and sulfur atoms. The distribution of the nine cysteine residues was similar to but clearly distinct from those of ferredoxins of other photosynthetic bacteria. Comparison of this ferredoxin with those of other bacteria suggests that the photosynthetic bacteria evolved on separate lines. Ferredoxin II was also subjected to analyses of amino acid composition and terminal sequences, but no further study was possible due to the limited material. Although the composition was different from that of ferredoxin I, the terminal sequences were exactly the same as those of ferredoxin I.

Amino Acid Sequence↗