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Biomedical subjects

J L Bernier

Publications and source records attributed to J L Bernier.

69 records · Page 4Linked to original sources

On the mechanism of the tetrahydropteridine cofactor oxidation in aerobic and H2O2-peroxydase media.

It is commonly postulated that the enzymatic hydroxylation of phenylalanine, tyrosine and tryptophan involves the concomitant oxidation of a tetrahydropteridinic cofactor to an unstable quinonoid product, converted to the initial compound under the catalytic action of dihydropteridine reductase. We now report UV, NMR, mass spectrum and spectroscopic studies of 2-amino-4-hydroxy-6,7-dimethyl-5, 6, 7, 8-tetrahydropteridine oxidation process either by atmospheric O2 or by the H2O2-peroxidase system. No quinonoid form was visualized and, moreover, the spectral characteristics of UV absorbance spectra, initially reported as specific for the quinonoid form, are related to other oxidation products whose formation is explained here.

Hydrogen Peroxide↗

Opiate receptor interaction of a new analgesic drug 2-piperidinoethyl dibenzylglycolate.

The pharmacological properties of a new analgesic drug, 2-piperidinoethyl dibenzylglycolate (PDG), have been demonstrated by classical tests. The technique of iontophoresis was used in order to compare the effects of PDG with those of Tyr-D-Ser-Gly-Phe-Leu-Thr (DSTLE), syndyphalin, morphine and naloxone (NAL) on hypothalamic neurones. PDG as other four substances evoked only inhibitory responses. Some neurones, on which were tested three substances, were sensitive to one, two or three of these substances. The differential responses so obtained suggested that PDG does not act on mu- and delta-receptors but on an unidentified receptor for which morphine and NAL have a high affinity as agonist. Structural requirements for activity on different receptors were also proposed on the basis of crystallographic data and the above results.

Action Potentials↗

Synthesis, DNA binding, and cleaving properties of an ellipticine-salen.copper conjugate.

The synthesis of a DNA-cutting agent that conjugates an ellipticine chromophore and a copper complex of bis(salicylidene)ethylenediamine, referred to as a salen, is reported. The presence of the salen.Cu complex allows cleavage of DNA via oxygen-based radicals, and the ellipticine moiety serves as a DNA anchor. Spectroscopic measurements indicate that the intercalation geometry of the ellipticine chromophore is preserved with the hybrid. The cleavage is much more efficient with the conjugate than with the Schiff base copper complex alone.

Chelating Agents↗

Generation of free radicals by simple prenylated hydroquinone derivatives, natural antitumor agents from the marine urochordate Aplidium californicum.

The redox properties of simple prenylated hydroquinone derivatives with cytotoxic properties have been studied by absorption and ESR spectroscopies. Both methods evidenced an autoxidation process in which the hydroquinones give rise to a semiquinone radical. Molecular oxygen is the electron acceptor, as demonstrated by spin trapping. No secondary radicals were found in the ESR spectra, either in the presence of hydroxyl anion (alkaline medium) or in the presence of glutathione. Nevertheless, a redox cycle can be initiated by glutathione, giving rise to substantial free-radical production. Thus, although not fully elucidated, the antitumor properties of the three hydroquinones described here can be correlated with their redox properties and their reactivity with thiol-containing peptides such as glutathione.

Animals↗