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Biomedical subjects

N Ando

Publications and source records attributed to N Ando.

At least 181 records · Page 10Linked to original sources

Antitumor activity of 1-alkoxycarbonylalkylcarbamoyl-5-fluorouracil derivatives by oral administration.

Antitumor activity of seven 5-fluorouracil derivatives having carbamoyl linkage with amino acid was examined against L-1210 leukemia, adenocarcinoma 755, ascites sarcoma 180, Ehrlich ascites carcinoma and Lewis lung carcinoma by oral administration. These compounds showed more than 30% increase in life-span (ILS) against L-1210 at optimal doses when given by oral administration. Therapeutic ratios (ILSmax/ILS30) of 1-methoxycarbonylmethylcarbamoyl and 1-(1-ethoxycarbonyl-3-methylthiopropylcarbamoyl) derivatives of 5-fluorouracil in L-1210 system were 4.8 and 4.7, respectively. 1-Methoxycarbonylmethylcarbamoyl and 1-(2-ethoxycarbonylethylcarbamoyl) derivatives of 5-fluorouracil inhibited completely the growth of adenocarcinoma 755 when given orally, but only 1-methoxycarbonylmethylcarbamoyl derivative inhibited 99 and 98% of the growth of ascites sarcoma 180 and Ehrlich ascites carcinoma, respectively. The latter compound increased the life-span to 48% at optimal dose in Lewis lung carcinoma system.

Adenocarcinoma↗

Sister-chromatid exchanges and chromosomal aberrations in cultured Chinese hamster cells treated with pesticides positive in microbial reversion assays.

The induction of sister-chromatid exchanges (SCEs), chromosomal aberrations and polyploids was investigated in cultured Chinese hamster cells treated with pesticides or a related compound positive in microbial reversion assays. The chemicals tested were captan, captafol, 1,2-dibromoethane (EDB), 1,2-dibromo-3-chloropropane (DBCP), 5-nitro-1-naphrhonitrile (NNN), p-dimethylaminobenzenediazo sodium sulfonate (DAPA), 2-hydrazinoethanol (HEH), vamidothion, dichlorovos (DDVP), N-nitroso-ethylenethiourea (N-nitroso-ETU), and 2,4-dinitrophenyl thiocyanate (NBT). A significant and dose-dependent increase in the frequency of SCEs and chromosomal aberrations was observed in the cell cultures treated with captan, captafol, EDB, DBCP, HEH, DDVP, vamidothion, DAPA or N-nitroso-ETU or NBT produced a significant increase in the frequency of polyploid cells, whereas the other agents did not. When compared with results from microbial reversion assays, a close correlation was observed between the ability to induce SCEs or chromosomal aberrations and the mutagenic potency in bacteria (r:0.71-0.84).

Aneuploidy↗

Antitumor activity of metabolites of 1-hexylcarbamoyl-5-fluorouracil and related compounds against L1210 leukemia in vivo and L5178Y lymphoma cells in vitro.

Antitumor activity of metabolites of 1-hexylcarbamoyl-5-fluorouracil (HCFU) and related compounds was examined in vivo and in vitro. Carboxypentyl and carboxypropyl carbamoyl derivatives of 5-fluorouracil (FU) were moderately active against L1210 by oral administration but less active by intraperitoneal administration. However, 5-hydroxy- and 5-oxo-hexylcarbamoyl derivatives of FU were markedly or moderately active against the leukemia by both oral and intraperitoneal administrations. Therapeutic ratios for the metabolites were less than that for HCFU by both oral and intraperitoneal administrations. Metabolites of HCFU had growth inhibitory activity against L5178Y in vitro similar to alkylcarbamoyl derivatives of FU. Activity of metabolites was lower than that of FU and higher than that of HCFU in vitro. It means that HCFU is converted into FU through active intermediate metabolites in vivo.

Animals↗

Conversion of deoxycorticosterone to 3-keto-4-etienic acid, catalyzed by a partially purified preparation from bovine adrenocortical mitochondria.

Bovine adrenocortical mitochondria were sonicated and subjected to extraction with sodium cholate. The extract contained not only cytochrome P-450 activities, but also an activity which catalyzed the conversion of deoxycorticosterone to an unknown steroid (designated X). The latter activity was concentrated by (NH4)2SO4 fractionation in the presence of sodium cholate, and separated from P-450 by taking advantage of their different solubilities in phosphate buffer without sodium cholate. The specific activity of the partially purified enzyme fraction was 70 times higher than that of sonicated mitochondria. The conversion of deoxycorticosterone to steroid X required NAD or NADP. The conversion rate was dependent on the concentration of deoxycorticosterone. The major product, steroid X, was isolated from the reaction mixture by means of silicic acid and Iatrobeads column chromatography. The steroid was characterized as 3-keto-4-etienic acid (3-oxoandrost-4-ene-17beta-carboxylic acid). This result suggests that an enzyme system for the conversion of deoxycorticosterone to 3-keto-4-etienic acid exists in adrenocortical mitochondria.

Adrenal Cortex↗

67Ga scanning in the evaluation of esophageal carcinoma.

Eighty-nine patients with histologically proved esophageal carcinoma were scanned with 67Ga to screen for extramural tumor extension and lymph-node involvement. Radiation dose and reduction of uptake were correlated. 67Ga accumulation indicated extramural extension with a sensitivity of 67% and a specificity of 93%. Marked uptake in an extraprimary site in the mediastinum or upper abdomen indicated lymph-node involvement with a sensitivity of 27% and a specificity of 100%. Irradiation with more than 20 Gy (2,000 rad) reduced uptake (P less than 0.05). 67Ga scanning appears to be useful in the evaluation of esophageal carcinoma.

Carcinoma, Squamous Cell↗