Synthesis of regioselectively protected forms of cytidine based on enzyme-catalyzed deacetylation as the key step.

N4-Acetylcytidine (77%) and 2',3'-O, N4-triacetylcytidine (95%) were obtained from the hydrolysis of a common precursor, the peracetylated form of cytidine with Aspergillus niger lipase (Amano A) and Burkholderia cepacia esterase (SC esterase S), respectively, under very mild conditions. The experimental procedure for the conversion of triacetylcytidine to a corresponding phosphoramidite (82%), an intermediate for sugar nucleotide synthesis, is also elaborated.

[Fundamental study of the detection of metastatic bone tumors with whole-body MR imaging].

Preliminary studies were performed to evaluate the usefulness of whole-body magnetic resonance imaging (WB-MRI) in the screening of bone metastases. The fast short TI inversion recovery sequence was the most suitable method because of its minimal image distortion and uniformity of fat suppression in a large field of view. In 4 cases of malignant tumor, the localization of all 8 bone metastases detected with bone scintigraphy (BS) could be clarified with WB-MRI.

[Usefulness of percutaneous sclerosing treatment for low-flow vascular lesions].

Peripheral vascular lesions may occur as a result of various clinical problems, cosmetic or dysfunctional causes, or bleeding. In severe cases, coagulopathy and congestive heart failure may occur. Although the efficacy of transarterial embolization (TAE) for arterial vascular lesions is well known, TAE has no effect on low-flow vascular lesions (venous malformations, venous angiomas, and venous components of arteriovenous malformation).

Synthesis of a Neu2en5Ac analog hapten and isolation of monoclonal antibody to Neu2en5Ac.

Neu2en5Ac is a minor component of body fluids and is abundant in sialuria, but no antibody to detect it has been reported. 5-Acetamido-2,6-anhydro-9-glutaramido-3,5,9-trideoxy-D-glycero-D- galacto-non-2-enonic acid has been synthesized and conjugated with keyhole limpet hemocyanin (KLH) for immunization. A hybridoma named SIC172 was obtained that produces a monoclonal antibody (MAb) to Neu2en5Ac.

Enzymatic synthesis of Kdn oligosaccharides by a bacterial alpha-(2-->6)-sialyltransferase.

Synthesis of CMP-deaminoneuraminic acid (CMP-beta-D-Kdn) and its enzymatic transfer reaction using bacterial alpha-(2-->6)-sialyltransferase were examined. CMP-beta-D-Kdn was prepared from methyl 4,5,7,8,9-penta-O-acetyl-3-deoxy-D-glycero-beta-D-galacto-2- nonulopyranosonate (2) in 24% overall yield. Enzymatic synthesis of Kdn oligosaccharide with CMP-beta-D-Kdn (10.

Optimization of agitation and aeration conditions for maximum virginiamycin production.

To maximize the productivity of virginiamycin, which is a commercially important antibiotic as an animal feed additive, an empirical approach was employed in the batch culture of Streptomyces virginiae. Here, the effects of dissolved oxygen (DO) concentration and agitation speed on the maximum cell concentration at the production phase, as well as on the productivity of virginiamycin, were investigated. To maintain the DO concentration in the fermentor at a certain level, either the agitation speed or the inlet oxygen concentration of the supply gas was manipulated.

Synthesis of Immobilized CMP-Sialic Acids and Their Enzymatic Transfer with Sialyltransferase.

A novel immobilization procedure for glycoproteins is based on the reacion of immobilized CMP-NeuAc (CMP-sialic acids) with sialyltransferase (see scheme). The transfer ability was tested under various conditions; a corresponding oligosaccharide or asialoglycoprotein acted as sialyl acceptor. The solid-phase synthesis of CMP-NeuAc is also described.

Association of fatty liver with increased ratio of visceral to subcutaneous adipose tissue in obese men.

We studied the association of fatty liver with subcutaneous and visceral obesity in 46 male and 36 female patients with body mass index (BMI) over 22 kg/m2. The correlation coefficient between the ratio of the visceral adipose tissue to the subcutaneous adipose tissue (V/S) and the computed tomography (CT) number of the liver was -0.299 (P < 0.

Mass production of bacterial alpha 2,6-sialyltransferase and enzymatic syntheses of sialyloligosaccharides.

To supply alpha 2,6-sialyltransferase for the large-scale synthesis of sialoside, we investigated culture conditions for the production of sialyltransferase 0160. The addition of galactose and beef extract, and control of the pH of the culture medium were effective on the production of sialyltransferase 0160. The maximal enzyme productivity reached 550 units/L.

MRI in carcinomatous encephalitis.

We report a rare case of miliary brain metastases presenting with symptoms similar to encephalitis ("carcinomatous encephalitis"). Contrast-enhanced MRI demonstrated miliary metastases more distinctly than other imaging methods and reproduced the pathological features.

Novel aspects of interaction between UDP-gal and GlcNAc beta-1,4-galactosyltransferase: transferability and remarkable inhibitory activity of UDP-(mono-O-methylated gal), UDP-Fuc and UDP-man.

Four mono-O-methylated and one mono-O-acetylated UDP-D-Gal analogues and UDP-L-Fuc were synthesized. 2-O-Methyl-D-galactose residue was enzymatically transferred to give 2'-O-methyllactosaminide in high yield. UDP-Fuc and UDP-Man showed potent inhibitory activities against beta-1,4-galactosyltransferase.

[Pathological evaluation of superselective one-shot intra-arterial infusion chemotherapy for head and neck tumors].

Since 1992, we have treated 43 patients with head and neck tumors by superselective intra-arterial infusion chemotherapy (SIIC) via femoral artery. In 8 patients among then, operation was performed thereafter with/without radiation therapy (RT). CDDP and/or CBDCA were utilized as the chemotherapeutic modality.

Purification and characterization of a marine bacterial beta-galactoside alpha 2,6-sialyltransferase from Photobacterium damsela JT0160.

A bacterial sialyltransferase, named sialyltransferase 0160, was purified from a marine bacterium that had been isolated from seawater from Sagami Bay, Kanagawa. This strain has been identified as Photobacterium damsela, and named P. damsela JT0160.

Hypoxanthine: a low molecular weight factor essential for growth of erythrocytic Plasmodium falciparum in a serum-free medium.

A low molecular weight factor in a basal medium essential for erythrocytic Plasmodium falciparum development in a serum-free medium using a cell growth-promoting factor derived from adult bovine serum was detected. The factor was hypoxanthine. The optimal hypoxanthine concentration for parasite growth was between 15 and 120 microM.

Superselective cisplatin (CDDP)-carboplatin (CBDCA) combined infusion for head and neck cancers.

A group of 26 patients with carcinoma of the head and neck region was treated by superselective intra-arterial infusion of cisplatin (CDDP)-carboplatin (CBDCA). The tumor locations included the tongue (n = 4), oral base (n = 2), nasopharynx (n = 2), oropharynx (n = 8), hypopharynx (n = 4) and larynx (n = 4). Using the coaxial technique, a microcatheter was placed in the lingual, ascending pharyngeal, facial and superior thyroidal arteries according to the location of the tumor.

Enzymic transfer of 6-modified D-galactosyl residues: synthesis of biantennary penta- and hepta-saccharides having two 6-deoxy-D-galactose residues at the nonreducing end and evaluation of 6-deoxy-D-galactosyl transfer to glycoprotein using bovine beta-(1-->4)-galactosyltransferase and UDP-6-deoxy-D-galactose.

UDP-6-Deoxy-D-galactose and UDP-6-deoxy-6-fluoro-D-galactose were synthesized and their transfer to 2-acetamido-2-deoxy-D-glucose (N-acetyl-D-glucosamine) by beta-(1-->4)-galactosyltransferase was examined. The transfer rates of 6-deoxy-D-galactose and 6-deoxy-6-fluoro-D-galactose were 1.3 and 0.

Characterization of inhibitory activities and binding mode of synthetic 6'-modified methyl N-acetyl-beta-lactosaminide toward rat liver CMP-D-Neu5Ac: D-galactoside-(2-->6)-alpha-D-sialyltransferase.

6'-Deoxy (12), 6'-thio (13), and 6'-O-tetrahydropyranosyl (14) analogues of methyl N-acetyl-beta-lactosaminide (3), were synthesized from lactose. NOE experiments proved that they adopt the same conformation as that of 3. Inhibition studies using these synthetic analogues, including the disulfide dimer 15, toward (2-->6)-alpha-sialytransferase (EC 2.

Effect of ethanol induced occlusion of the renal artery in rabbit kidney implanted with VX2 carcinoma.

The effects of injection of absolute ethanol into the renal artery were investigated in 13 rabbit kidneys previously implanted with VX2 carcinoma. Eight rabbits with implanted tumors served as controls. The effects were evaluated by angiography and histology.

In vitro fertilization and development of in vitro matured bovine follicular oocytes.

Bovine follicular oocytes matured in vitro were fertilized in vitro using epididymal spermatozoa from five different bulls and then cultured to the blastocyst stage in vitro. The fertilization rate, based on one pair of pronuclei and presence of one sperm tail, ranged from 55.2 to 64.

Pregnancies after co-culture of cumulus cells with bovine embryos derived from in-vitro fertilization of in-vitro matured follicular oocytes.

Bovine follicular oocytes surrounded by cumulus cells for more than one-third of their surface were matured, fertilized and developed in vitro utilizing a co-culture system with bovine cumulus cells. Embryos developed into blastocysts were non-surgically transferred to the uteri of cows at Day 6, 7 or 8 (Day 0 = oestrus). Out of 6 recipient cows (19 blastocysts transferred), 3 became pregnant.