Hiromi Kataoka

Syntheses of macrocycles from l-amino acid and their selective transport of amino ester salts through an organic liquid membrane

Abstract Syntheses of 18-membered macrocycle 17 , 24-membered macrocycles 18 , 19 , and 30-membered macrocycles 20 , 21 , 22 , 23 , 25 , were achieved by using diglycolic acid and amino acids as constituents. Selective transport of amino ester salts through an organic liquid membrane was mediated by their macrocycles and intermediate compounds. The transfer abilities of these carriers containing amino acid moieties were different from that of 18-crown-6.

Ozonated Olive Oil Enhances the Growth of Granulation Tissue in a Mouse Model of Pressure Ulcer

The curative effect of ozonated olive oil was evaluated using mouse models of cut wounds and pressure ulcers (decubitus or bedsores). Although ozonated olive oil did not significantly accelerate or decelerate wound contraction in either model, some histological modifications were observed. Ozonated olive oil induced blood coagulation in the hypodermis and cell infiltration in the dermis 1 day after its application. Moreover, it enhanced the formation of granulation tissue 10 days after application. These results indicate that ozonated olive oil promotes granulation tissue formation and is effective in the healing of wounds and pressure ulcers.

Proinflammatory Event of Ozonized Olive Oil in Mice

Ozonized olive oil inhibited the swelling reaction of 2, 4-dinitrofluorobenzene-induced mouse-contact hypersensitivity, which is a model for chronic skin diseases involved in the initiation and propagation of several inflammatory processes, mainly due to type IV hypersensitivity. On the other hand, ozonized olive oil itself stimulated the development of inflammatory responses, such as vasodilation, swelling and epidermal hyperplasia. When repeatedly applied to the skin, ozonized olive oil caused hair loss at the site and contact hypersensitivity. These findings identify a new biological function for ozonized olive oil and indicate the risk of adverse effects with repeated application.

Reductive degradation of O-acyl oximes under fast-atom bombardment conditions

A degradation phenomenon of O-acyl oximes under fast-atom bombardment (FAB) conditions is described from the point of view of reactivity with the liquid matrix and irradiation time with the xenon neutral beam. Mass spectra of O-acyl oximes were compared with those of the free oxime and hydroxylamine as model compounds, by using two different matrices, m-nitrobenzyl alcohol and DTT/TG12 (a 1:2 mixture of dithiothreitol and thioglycerol). A characteristic fragment ion was observed in the FAB mass spectra of O-acyl oximes and a free oxime only when DTT/TG12 was used. Collision-activated dissociation (CAD) was used to search for the origin and to confirm the structure of the characteristic fragment ion. The CAD spectra of the molecular-related ions, [M – H]+,M+• and [M + H]+, demonstrated that this characteristic fragment ion was not derived from any of these precursor ions. The CAD spectra of the characteristic fragment ion, which originated from O-acyl oximes, were very similar to those from free oximes and these results indicated that the fragment ion had the same structure. It was concluded that the degradation, under FAB conditions, was caused by a reductive reaction of the oxime moiety (–O–N=C) in O-acyl oximes regardless of its acyl moiety and that the degradation was initiated by the thiol group(s) in the matrix. The abundance of the ion originating from reductive degradation increased with increasing irradiation time with the xenon neutral beam.

Identification of Candidate Target Cyp Genes for microRNAs Whose Expression Is Altered by PCN and TCPOBOP, Representative Ligands of PXR and CAR

MicroRNAs (miRNAs) are small non-coding RNAs that are involved in mRNA post-transcriptional regulation. The deregulation of miRNAs affects the expression of drug-metabolizing enzymes, drug transporters, and nuclear receptors, all of which are important in regulating drug metabolism. miRNA expression can be altered by several endogenous or exogenous agents, such as steroid hormones, carcinogens, and therapeutic drugs. However, it is unclear whether hepatic miRNA expression is regulated by nuclear receptors, such as pregnane X receptor (PXR) and constitutive androstane receptor (CAR), which are indispensable for the expression of the CYPs. Here we investigated the effects of the mouse PXR and CAR ligands pregnenolone-16α-carbonitrile (PCN) and 1,4-bis[(3,5-dichloropyridin-2-yl)oxy]benzene (TCPOBOP) on hepatic miRNA expression in mice. We found that the expression of 9 miRNAs was increased (>2-fold) and of 4 miRNAs was decreased (>50%) in response to PCN, while TCPOBOP treatment led to the up-regulation of 8 miRNAs and down-regulation of 6 miRNAs. Using several miRNA target prediction algorithms, we found that the predicted target genes included several lesser known Cyp genes (Cyp1a1, Cyp1b1, Cyp2b10, Cyp2c38, Cyp2u1, Cyp4a12a/b, Cyp4v3, Cyp17a1, Cyp39a1, and Cyp51). We analyzed the expression of these genes in response to PCN and TCPOBOP and found changes in their mRNA levels, some of which were negatively correlated with the expression of their corresponding miRNAs, suggesting that miRNAs may play a role in regulating Cyp enzyme expression. Further studies will be required to fully elucidate the miRNA regulatory mechanisms that contribute to modulating CYP expression.

Synthesis of a cyclic octapeptide

Synthese de cyclo ((L-Lys(Z)) 2 -Gly-(L-Phe) 2 -(Gly) 3 ). Utilisation de ce ionophore modele pour le transport de L-Phe-OMe•HCl a travers une membrane organique liquide

PGE2-receptor subtype EP4-dependent adherence of mastocytoma P-815 cells to matrix components in subcutaneous tissues overlaying inside surface of air pouch cavity in CDF1 mouse

Abstract.Objectives:It remains to be fully clarified how adhesion of mast cells is regulated in vivo. We previously reported that PGE2-receptor EP4 stimulated the adhesion of mouse mastocytoma P-815 cells to plate-bound fibronectin. Our purpose in this study is to evaluate the adhesion using a system, which can mimic the in vivo adhesion.Methods:P-815 cells were transplanted in an air pouch produced in the transplantable mice, CDF1. The number of cells that adhere to the subcutaneous tissues overlaying the inside cavity surface was determined.Results:The number of adhered cells was decreased in mice administered with ibuprofen or an EP4 antagonist, ONO AE3-208. A local administration of PGE2 or a phorbol ester, PMA, increased the number of adhered cells, which was also suppressed in the mice treated with ONO AE3-208.Conclusion:Our results suggest that PGE2-mediated adhesion of P-815 cells in the subcutaneous tissues of the air pouch is mediated by the EP4 subtype.