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Biomedical subjects

Y Shimauchi

Publications and source records attributed to Y Shimauchi.

35 records · Page 2Linked to original sources

PS-6 and PS-7, new beta-lactam antibiotics. Isolation, physicochemical properties and structures.

Antibiotics PS-6 and PS-7 which are shown to be 5R,6R-3-(2-acetamido)ethylthio-6-isopropyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene- 2-carboxylic acid and 5R,6R-3-(E)-(2-acetamido) vinylthio-6-ethyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid respectively, are new beta-lactam compounds isolated from fermentation broths of Streptomyces cremeus subsp. auratilis A271, S. fulvoviridis A933, S. olivaceus ATCC 31126 and S. flavogriseus NRRL 8139. Fermentation, isolation, physicochemical properties and structures of antibiotics PS-6 and PS-7 are described.

Anti-Bacterial Agents↗

Chemical modification of anthracycline antibiotics. I. Demethoxycarbonylation, 10-epimerization and 4-o-methylation of aclacinomycin A.

Demethoxycarbonyl derivatives of aclacinomycin A and of its 7-epimer, 10-epi-aclacinomycin A and 4-O-methylaclacinomycin A were chemically derived from aclacinomycin A. The cytotoxicity and inhibitory effects of RNA and DNA synthesis in cultured L1210 leukemia cells of the 4-O-methyl derivative approximated that of aclacinomycin A, while the demethoxycarbonyl derivatives and 10-epi-aclacinomycin A exhibited decreased activities in comparison with the parent compound.

Aclarubicin↗

Chemical modification of deltamycins. I. 4''-O-acyl analogs of deltamycins.

Using 4''-O-deacyldeltamycin as a starting material, various 4''-O-acyl derivatives were chemically synthesized by the following scheme: 2'-O-acetylation leads to 4''-O-acylation leads to 2'-O-deacetylation. 4''-O-Deacyldeltamycin is produced during the fermentation of deltamycin producing organisms or can be prepared by the biological deacylation of the deltamycins. 4''-O-Phenylacetyl-4''-O-deacyldeltamycin (PAD) showed good activity against various bacteria and mycoplasma. Among para-substituted PAD derivatives, NPAD (p-nitrophenylacetyl-) and SPAD (p-methylsulfonylphenylacetyl-) showed increased potency as compared to PAD against certain bacteria. The PAD was evaluated by in vivo experiments for plasma levels in mice and dogs and curative activity on the infected mice with Staphylococcus aureus Smith by subcutaneous or oral administration.

Administration, Oral↗

Deltamycins, new macrolide antibiotics. III. Chemical structures.

The structures of deltamycins A1,A2,A3 and A4 belonging to the basic macrolide family of antibiotics were determined mainly from their spectral properties. Deltamycin A4 was identified as carbomycin A having an isovaleryl group on the mycarose moiety of the molecule. Deltamycin A1,A2 and A3 possess similarities to the structure of deltamycin A4, but they have acetyl, propionyl and n-butyryl group, respectively, in the place of isovaleryl group of deltamycin A4. These structures were confirmed by chemical synthesis from deltamycin X (4''-O-deacyldeltamycin) and the corresponding acyl chlorides.

Chemical Phenomena↗

Deltamycins, new macrolide antibiotics. I. Producing organism and fermentation.

A streptomycete strain, P3409, which produced new basic macrolide antibiotics, deltamycins A1, A2 and A3 and carbomycin A (deltamycin A4) was considered to be a new subspecies for which the name Streptomyces halstedii subsp. deltae was proposed. Deltamycins A1, A2, A3 and A4 which were active against Gram-positive bacteria were produced in organic complex media.

Anti-Bacterial Agents↗

A simultaneous monitoring of Lens culinaris agglutinin A-reactive alpha-fetoprotein and des-gamma-carboxy prothrombin as an early diagnosis of hepatocellular carcinoma in the follow-up of cirrhotic patients.

To elucidate the risk factors for developing hepatocellular carcinoma (HCC) during the follow-up of patients with liver cirrhosis (LC), outpatients with LC were examined periodically by means of serum biochemical assessments, ultrasonography, and computed tomography. Risk factors for HCC were statistically analyzed. We also examined an efficacy of Lens culinaris agglutinin A-reactive profiles of alpha-fetoprotein (AFP-L3%) and des-gamma-carboxy prothrombin (DCP) value using a highly sensitive DCP determination kit (ED036) for the early recognition of HCC. The AFP-L3% and the ED036 value were retrospectively determined with stored serum samples. HCC was diagnosed in 21 of the 78 patients with LC during the follow-up period (mean follow-up period: 42 months). The estimated cumulative incidence of HCC was 25% with 3 years and 48% with 5 years. The most significant risk factor for the development of HCC in LC patients was found to be the mean serum AFP concentration from the year before the HCC detection (p=0.02). At the time of the recognition of HCC, the positive rates of the tumor markers were: serum AFP concentration 14%, serum DCP value 5%, AFP-L3% was 33%, and that of ED036 43%. The positive rate in collaborative use of AFP-L3% and ED036 was 67%. The simultaneous determination of the AFP-L3% and the ED036 value was shown to be effective for the early detection of HCC.

Aged↗

Bright loop appearance; a characteristic ultrasonography sign of early hepatocellular carcinoma.

Ultrasonography (US) and computed tomography (CT) are the most effective screening methodologies for hepatocellular carcinoma (HCC). In our US screening, 20% of small HCC nodules less than 20 mm in diameter were detected as hyperechoic tumors. Among these hyperechoic HCC nodules, we have often observed (BL) which is defined as hypoechoic nodules in the hyperechoic tumor. In this study, we report that the BL is a sign of dedifferentiation of early stage of HCC with fatty change by US. From 1994 to 1998, we performed tumor targeting needle biopsy in 938 hepatic nodular lesions. Among them, 284 nodules <20 mm in diameter, histologically diagnosed as HCC, were studied. BL is defined as a hyperechoic tumor containing a hypoechoic nodule >4 mm in diameter by US. Among 284 nodules, well, moderately and poorly differentiated HCC were 183 (64.4%), 100 (35.2%) and 1 (0.4%), respectively. On US, hypoechoic, isoechoic, and hyperechoic nodules were 188 (66.2%), 32 (11.3%) and 64 (22.5%), respectively. Forty-seven nodules of 64 hyperechoic HCC nodules <20 mm in diameter, 47 nodules (73.4%) showed fatty changes. Of 64 hyperechoic HCC nodules, we recognized 22 nodules (34.4%) as BL. The proportion of BL type hyperechoic nodules increased with the tumor size. Two hyperechoic nodules followed by US changed to BL with tumor enlargement. Histologic examination of a resected HCC with BL showed that hyperechoic HCC nodule represented well-differentiated HCC with fatty change and inner hypoechoic lesion represented moderately differentiated HCC without fatty change. In US screening for HCC, BL was often observed in HCC nodules from 11 to 20 mm in diameter. Histologic examination revealed that BL of HCC on US was associated with tumor progression and indicated dedifferentiation showing moderately differentiated HCC in well-differentiated HCC with fatty change.

Adult↗

Successful treatment for bronchial bleeding from invasive pulmonary metastasis of hepatocellular carcinoma: a case report.

Pulmonary metastasis is frequently seen in patients with advanced hepatocellular carcinoma. However, information is limited concerning life-threatening complications and effective treatment of pulmonary metastasis because of the poor prognosis of patients with advanced hepatocellular carcinoma. Recent remarkable progress in detection and treatment of hepatocellular carcinoma has improved prognosis, making management of pulmonary metastasis an important clinical issue. We describe a 68-year-old man with pulmonary metastasis of hepatocellular carcinoma and sudden onset of hemoptysis from bronchial invasion. Transcatheter embolization was performed successfully via the bronchial artery with disappearance of bloody sputum. Peribronchial pulmonary metastasis of hepatocellular carcinoma can cause life-threatening hemoptysis. Transcatheter arterial embolization may be one of therapeutics for hemoptysis from invasive pulmonary metastasis of hepatocellular carcinoma.

Aged↗