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Biomedical subjects

Y Deguchi

Publications and source records attributed to Y Deguchi.

139 records · Page 8Linked to original sources
PubMed1985

Physical fitness of paraplegics in full wheelchair marathon racing.

The wheelchair marathon is one of the most difficult sports for participants with much uncertainty regarding the security of the paraplegics. The physical fitness of paraplegics has been examined regularly since The Oita International Wheelchair Marathon (half marathon) was inaugurated (1981). A full marathon (42.195 km) was adopted at The 3rd Meeting (1983). The individual equations between heart rate (HR) and oxygen consumption VO2 were drawn from the preliminary test on the subjects who were expected to be among the top finishers in these races. VO2 during these races was indirectly estimated and showed a fairly low value (35.0 +/- 3.8 ml/kg/min in the full race, 32.7 +/- 6.3 ml/kg/min in the half race respectively) in comparison with able-bodied elite runners. However, the paraplegic participants had extremely high HR (171.6 +/- 20.5 beats/min, 168.1 +/- 9.8) continuously throughout the race. Though the ratio of active muscle mass of arms to legs in paraplegic athletes may approximate to near equal, paraplegic arms seem to exert physiologically and mechanically less efficient power. There were no significant differences in physical fitness between the full and the half marathon elite finishers. The cardiovascular function of paraplegic athletes may well be ranked among those of able-bodied athletes in their fitness. Full wheelchair marathon seems to be safe if it is held in an appropriate environment.

Adult↗
PubMed1985

Diversity of underlying mechanisms in the production of analgesic and pentobarbital-hypnosis prolonging effects of various analgesic drugs and stresses.

Stressful stimuli, electric footshock (FS), immobilized-water immersion (IW), and cold-water swimming (CWS), produced analgesia and prolonged the pentobarbital hypnosis as well as morphine and clonidine. Naloxone completely antagonized the analgesic effects of morphine and FS and partially that of IW; however, that of clonidine and CWS were not reversed by naloxone. Naloxone eliminated the hypnosis prolonging effect of morphine and FS, but failed to reverse the effect of clonidine, IW and CWS. Differences in the analgesic and hypnosis prolonging effects and also the respective naloxone sensitivity of each drug and stress suggest the diversity of the underlying mechanisms.

Analgesics↗
PubMed1981

Degradation kinetics and mechanism of aminocephalosporins in aqueous solution: cefadroxil.

The degradation kinetics and mechanism of a new, orally effective cephalosporin derivative, cefadroxil, in aqueous solution were investigated at pH 2.51-11.5 at 35 degrees and ionic strength 0.5. The degradation rates were determined by high=pressure liquid chromatography. At constant pH and temperature, the degradation followed first-order kinetics and a log k-pH profile was presented. The shape of the rate-pH profile resembled that for cephalexin or cephradine under the same conditions. Citrate and phosphate buffers enhanced general acid and base catalysis of the degradation. In aqueous solution, cefadroxil was shown to degrade by three parallel reactions: (a) intramolecular aminolysis by the C-7 side-chain amino group on the beta-lactam moiety, (b) water-catalyzed or spontaneous hydrolysis, and (c) beta-lactam cleavage by the nucleophilic attack of hydroxide ion. In neutral and weak alkaline solutions, the main degradation products were two piperazine-2, 5-diones and 3-hydroxy-4-methyl-2(5H)-thiophenone, the former being formed from Reaction a, while the latter arose via the degradation pathways of Reaction b and/or c.

Buffers↗
PubMed1981

Multiple nutritional requirements of lactobacilli: genetic lesions affecting amino acid biosynthetic pathways.

Genetic lesions responsible for amino acid requirements in several species of multiple auxotrophic lactobacilli were investigated. Systematic attempts were made to isolate mutants that could grow in the absence of each of the amino acids required by the parental strains of Lactobacillus plantarum, L. casei, L. helveticus, and L. acidophilus. After treatment with appropriate mutagens, such mutants could be obtained with respect to many but not all required amino acids. Successful isolation of mutants for a given amino acid means that a minor genetic lesion reparable by single-step mutations affects its biosynthesis; a failure to isolate mutants suggests the involvement of more extensive lesions. Analysis of these results as well as the specific requirements exhibited by the parental strains revealed certain regularities; some of the biosynthetic pathways for individual amino acids were virtually unaffected by more extensive lesions in at least species tested, whereas others were affected by more extensive lesions in at least some species. Both the number and the kind of pathways affected by extensive lesions differed appreciably among different species. Furthermore, the growth response of the parental strains to some putative amino acid precursors revealed a clear correlation between the extent of genetic lesions and the occurrence and location of a genetic block(s) for a given pathway. These findings are discussed in relation to the phylogeny, ecology, and evolution of lactic acid bacteria.

Amino Acids↗
PubMedDate not supplied

Retention of biologic activity of human epidermal growth factor following conjugation to a blood-brain barrier drug delivery vector via an extended poly(ethylene glycol) linker.

Human brain gliomas overexpress the receptor for epidermal growth factor (EGF), and radiolabeled EGF is a potential peptide radiopharmaceutical for imaging human brain tumors, should this peptide be made transportable through the blood-brain barrier (BBB) in vivo. Peptide drug delivery to the brain may be facilitated by conjugating peptide radiopharmaceuticals to BBB drug delivery vectors such as the OX26 monoclonal antibody (MAb), which undergoes receptor-mediated transcytosis through the BBB via the brain capillary endothelial transferrin receptor. EGF was biotinylated with NHS-XX-biotin, where NHS = N-hydroxysuccinimide and -XX- = bis (aminohexanoyl) spacer arm. The [125I]EGF-XX-biotin rapidly bound to C6 rat glioma cells transfected with the human EGF receptor. However, no binding to the C6 EGF receptor was detected when the [125I]EGF-XX-biotin was bound to a conjugate of streptavidin (SA) and the OX26 MAb. An alternative linker strategy using poly(ethylene glycol) (PEG) of 3400 Da molecular mass (PEG3400) was evaluated, wherein EGF was monobiotinylated with NHS-PEG3400-biotin. Attachment of the [125I]EGF-PEG3400-biotin to the OX26/SA conjugate did not impair binding of the construct to the EGF receptor in C6 glioma cells. The length of the -PEG- spacer arm and the -XX- spacer arm was >200 atoms and 14 atoms, respectively. These studies demonstrate that the use of the extended PEG linker releases steric hindrance of MAb transport vectors on binding of EGF to its cognate receptor on glioma cells. Attachment of EGF peptide radiopharmaceuticals to BBB drug delivery systems such as the OX26 MAb using extended PEG linkers allows for retention of the bifunctionality of the conjugate with binding to both EGF and transferrin receptors.

Animals↗
PubMedDate not supplied

Epidermal growth factor radiopharmaceuticals: 111In chelation, conjugation to a blood-brain barrier delivery vector via a biotin-polyethylene linker, pharmacokinetics, and in vivo imaging of experimental brain tumors.

Epidermal growth factor (EGF) is a potential peptide radiopharmaceutical for detection of brain tumors, because many human gliomas overexpress the EGF receptor (EGFR). The transport of EGF to the brain, however, is restricted by the blood-brain barrier (BBB). The purpose of the present study was to develop a vector-mediated brain delivery system for radiolabeled EGF. Human EGF was monobiotinylated with NHS-PEG3400-biotin, where NHS is N-hydroxysuccinimide and PEG3400 is poly(ethylene glycol) of 3400 Da molecular mass. EGF-PEG3400-biotin was radiolabeled with either 125I or 111In through the metal chelator, diethylenetriaminepentaacetic acid (DTPA). The radiolabeled EGF was then conjugated to a BBB delivery vector comprised of a complex of the OX26 monoclonal antibody (MAb) to the rat transferrin receptor, which was coupled to streptavidin (SA). Following intravenous injection in rats, the 125I conjugate was rapidly degraded in vivo, while the 111In conjugate was metabolically stable. The brain delivery of [111In]DTPA-EGF-PEG3400-biotin was enabled by conjugation with OX26/SA and was optimized by co-injection of unlabeled EGF to saturate EGF receptors in the liver. The specific binding of the [111In]DTPA-EGF-PEG3400-biotin conjugated to OX26/SA to the EGF receptor was confirmed in C6 rat glioma cells, which had been transfected with a gene encoding for the human EGF receptor under the regulation of a dexamethasone-inducible promoter. In vivo studies of C6-EGFR experimental tumors in Fischer 344 rats demonstrated successful brain imaging only when the peptide radiopharmaceutical was conjugated to the BBB delivery system, although the C6-EGFR tumors did not express EGFR in vivo. In conclusion, these studies describe the molecular formulation of a peptide radiopharmaceutical that can be used for imaging brain tumors behind the BBB.

Animals↗
PubMedDate not supplied

Positively charged gelatin microspheres as gastric mucoadhesive drug delivery system for eradication of H. pylori.

Gastric mucoadhesive drug delivery systems are very promising for eradication of Helicobacter pylori (H. pylori), a spiral bacterium that resides in the gastric mucus layer and at the mucus-epithelial cell interface. New positively charged biodegradable microspheres were prepared using aminated gelatin by surfactant-free emulsification in olive oil, followed by a cross-linking reaction with glutaraldehyde. The amino group contents of the modified gelatin and the microspheres were determined using a 2,4,6-trinitrobenzenesulfonic acid method. With the increase of glutaraldehyde concentration, the amino group content of the microspheres decreased accordingly. The influence of glutaraldehyde concentration, cross-linking reaction time, drug-loading patterns, and type of release media on the in vitro release characteristics of amoxicillin from the microspheres was investigated. Amoxicillin release rate from the modified gelatin microspheres was significantly reduced compared with that from gelatin microspheres. Furthermore, the release was decreased with the increase of glutaraldehyde concentration and/or cross-linking time. On the other hand, a faster release was observed in a lower pH release medium and/or using a lower pH solution for amoxicillin loading. The gastric mucoadhesive properties of the microspheres were evaluated using RITC-labeled microspheres in an isolated rat stomach. The gastric mucoadhesion of the modified gelatin microspheres was markedly improved compared with that of gelatin microspheres. The modified gelatin microsphere proves to be a possible candidate delivery system for the effective eradication of H. pylori.

Adhesives↗