A synthesis of 3′,4-́dideoxykanamycin B

3′,4′-Dideoxykanamycin B, the kanamycin B derivative that is active against resistant bacteria, was prepared from kanamycin B viaN-tosylation, 3′,4′-O-sulphonylation, 3′,4′-unsaturation, and hydrogenation. The unsaturated intermediate was obtained from the 3′,4′-di-O-sulphonyl derivatives by the action of sodium iodide in N,N-dimethylformamide; if zinc dust was added in this reaction, aziridine derivatives were formed, Removal of the tosyl group was successfully performed by using sodium in ammonia-ethylamine.     

The effect of nasal obstruction on the susceptibility of mice to noxious gases (author's transl)]

The effect of nasal obstruction on mice--the maice were forced to breathe through the mouth--was studied when the animals were exposed to noxious gases. It was noted that the forced mouth breathing made the mice less vulnerable to hydrogen sulfide, carbon monoxide and toluen vapor when expressed by the time interval before they lost righting reflex or showed respiratory arrest. The levels of the gases which could induce these sings within 5-10 minutes were significantly elevated with the "mouth breathing" mice. Possible mechanisms for this phenomenon and its application for men were discussed.     

Circular Thin-layer Chromatography of Oligosaccharides

The physicochemical properties and chemical constituents of the blue protein from rice bran were investigated. The blue protein was a copper-containing glycoprotein, the molecular weight of which was found to be 18,300 Daltons by the sedimentation equilibrium method assuming the partial specific volume 0.72 cm³ g^?1. The hexose and pentose contents were 5.49 and 4.01 g per 100 g protein respectively. The copper content was 0.38% which corresponded to 1.09 atoms per one molecule of the protein. The electron spin resonance spectrum showed that the copper was in a cupric state. The standard oxidation-reduction potential of the copper was found to be +275 mV at 20°C and at pH 7.39. The visible and near infrared absorption maxima were found at 450, 600 and 890 mμ, and the 450 mμ band was optically active in the optical rotatory dispersion exhibiting a large Cotton effect.     

Protein-Calcium-Phytic Acid Relationships in Soybean

This paper constitutes the first report in a research series undertaken in order to clarify the interactive relationships among soybean meal protein, calcium and phytic acid in solution and in precipitate.

Data presented are mainly concerned with solubility characteristics of soybean meal proteins as a function of pH. The results support the suggestion as follows; phosphorus and calcium give the remarkable effects on solubility characteristics of protein, the complex containing protein, calcium and phosphorus is formed above isoelectric point of protein and the combinations are labile above at pH 8, especially by heating.     

Immunocytochemical localization of cathepsin B in degenerating rat skeletal muscle induced by a local anesthetic, bupivacaine

Experimental acute degenerative changes in skeletal muscle accompanied by a drastic increase in cathepsins B&L were induced in rats by intramuscular injection of a local anesthetic, bupivacaine. Cathepsins B&L have been implicated in the rapid disappearance of muscle fibers. Degenerating muscle showed a spotty fluorescence when stained with antibodies against cathepsin B, indicating that the increased cathepsin B did not originate from the muscle itself, but from invading phagocytes. We report here results showing that cathepsin B of nonmuscle cell origin is involved in the breakdown of myofibrillar proteins in acute bupivacaine-induced muscle degeneration.     

Biodeposit production by the mussel Mytilus edulis L. on rocky shores

Seasonal changes in the amount of biodeposit (faeces and pseudofaeces) produced by the mussel Mytilus edulis L., which is one of the representative suspension-feeders in the rocky intertidal and shallow subtidal regions of Mutsu Bay, were studied in the laboratory. The effects of water temperature, light, food concentration, flow rate, body size, age, and spawning on biodeposit production were investigated. More biodeposit was produced in summer than in other seasons. Throughout the year, the amount of biodeposit was positively correlated with body size. Relatively more biodeposit was produced by smaller than by larger individuals. A M. edulis population living in one square meter was estimated to produce 9.20 kg of faeces and 2.71 kg of pseudofaeces per year (dry wt). More biodeposit was produced at water temperatures of 17.6–20.2° C than at 4.5–7.6° C and 25.2–26.0° C. The optimum temperature for biodeposit production was found to be ≈ 20.0 °C. When kept in the dark, M. edulis produced more biodeposit than in the light. When food concentration is increased, more psuedofaeces are produced; the amount of faeces, however, remains constant. With increasing flow rate, the amount o f biodeposit per h increased but the biodeposition rate decreased. Larger amounts of faeces and smaller amounts of pseudofaeces were produced by younger mussels than by older ones of a similar size. Spawning also affected biodeposit production.     

Decrease in bacterial production over the past three decades in the north basin of Lake Biwa,Japan

Limnology - In Lake Biwa, the largest lake in Japan, external pollutant loads have decreased since the 1980s, leading to improved water quality, such as reduction in biochemical oxygen demand (BOD)...     

Involvement of intracellular caveolin‐1 distribution in the suppression of antigen‐induced mast cell activation by cationic liposomes

Cationic liposomes are commonly used as vectors to effectively introduce foreign genes into target cells. In another function, we recently showed that cationic liposomes bound to the mast cell surface suppress the degranulation induced by the cross‐linking of high‐affinity immunoglobulin E receptor in a time‐ and dose‐dependent manner. This suppression is mediated by the impairment of the sustained level of intracellular Ca²⁺ concentration ([Ca²⁺]_i) via the inhibition of store‐operated Ca²⁺ entry. Further, we revealed that the mechanism underlying an impaired [Ca²⁺]_i increase is the inhibition of the activation of the phosphatidylinositol 3‐kinase (PI3K)‐Akt pathway. Yet, how cationic liposomes inhibit the PI3K‐Akt pathway is still unclear. Here, we focused on caveolin‐1, a major component of caveolae, which is reported to be involved in the activation of the PI3K‐Akt pathway in various cell lines. In this study, we showed that caveolin‐1 translocated from the cytoplasm to the plasma membrane after the activation of mast cells and colocalized with the p85 subunit of PI3K, which seemed to be essential for PI3K activity. Meanwhile, cationic liposomes suppressed the translocation of caveolin‐1 to the plasma membrane and the colocalization of caveolin‐1 with PI3K p85 also at the plasma membrane. This finding provides new information for the development of therapies using cationic liposomes against allergies.     

Structural requirement of C‐terminal region of chicken lysozyme signal peptide

Abstract

The mechanisms of signal peptide cleavage has not been fully elucidated yet. In previous investigation, we have examined the effect of chicken lysozyme signal peptide mutations on the secretion of human lysozyme. During this study, we determined that the hydrophobic bulky amino acid Val at position ‐1 inhibited the function of signal peptide. To determine why the ‐1Val suppressed the function of signal peptide, turn‐promoting amino acids Pro and Gly were introduced after ‐lVal to prevent the signal peptide from forming α‐helix and induce β‐turn around the cleavage site. This mutation resulted in no processing of signal peptide and no secretion of human lysozyme. However, the replacement of ‐1Val with Ala permitted a functional signal. Based on these results, three dimensional models around the cleavage site of each signal peptide were made, which show that bulky side chain at ‐1 residue of signal peptide limits the reaction space for signal peptidase and suppresses cleavage by steric hindrance. We suggest that the bulky side chain at ‐1 residue suppresses the signal peptide cleavage by its local steric hindrance and not by a change in whole structure around the cleavage site. On the other hand, introduction of Pro at position +1 did not inhibit signal cleavage completely resulting in poor secretion and processing efficiency although Pro in position +1 has been recently reported to block cleavage of the prokaryotic signal peptide. The mechanism of cleavage of prokaryotic signal may be different than that of eukaryotic signal.     

Crystal Structure of Silkworm Bombyx mori JHBP in Complex With 2-Methyl-2,4-Pentanediol: Plasticity of JH-Binding Pocket and Ligand-Induced Conformational Change of the Second Cavity in JHBP

Juvenile hormones (JHs) control a diversity of crucial life events in insects. In Lepidoptera which major agricultural pests belong to, JH signaling is critically controlled by a species-specific high-affinity, low molecular weight JH-binding protein (JHBP) in hemolymph, which transports JH from the site of its synthesis to target tissues. Hence, JHBP is expected to be an excellent target for the development of novel specific insect growth regulators (IGRs) and insecticides. A better understanding of the structural biology of JHBP should pave the way for the structure-based drug design of such compounds. Here, we report the crystal structure of the silkworm Bombyx mori JHBP in complex with two molecules of 2-methyl-2,4-pentanediol (MPD), one molecule (MPD1) bound in the JH-binding pocket while the other (MPD2) in a second cavity. Detailed comparison with the apo-JHBP and JHBP-JH II complex structures previously reported by us led to a number of intriguing findings. First, the JH-binding pocket changes its size in a ligand-dependent manner due to flexibility of the gate α1 helix. Second, MPD1 mimics interactions of the epoxide moiety of JH previously observed in the JHBP-JH complex, and MPD can compete with JH in binding to the JH-binding pocket. We also confirmed that methoprene, which has an MPD-like structure, inhibits the complex formation between JHBP and JH while the unepoxydated JH III (methyl farnesoate) does not. These findings may open the door to the development of novel IGRs targeted against JHBP. Third, binding of MPD to the second cavity of JHBP induces significant conformational changes accompanied with a cavity expansion. This finding, together with MPD2-JHBP interaction mechanism identified in the JHBP-MPD complex, should provide important guidance in the search for the natural ligand of the second cavity.