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Biomedical subjects

G Meunier

Publications and source records attributed to G Meunier.

At least 19 recordsLinked to original sources

Cyclic dipeptide oxidase from Streptomyces noursei. Isolation, purification and partial characterization of a novel, amino acyl alpha,beta-dehydrogenase.

Cyclic dipeptide oxidase is a novel enzyme that specifically catalyzes the formation of alpha,beta-dehydro-Phe (Delta Phe) and alpha,beta-dehydro-Leu (Delta Leu) residues during the biosynthesis of albonoursin, cyclo(Delta Phe-Delta Leu), an antibiotic produced by Streptomyces noursei. It was purified 600-fold with a 30% overall recovery, and consists of the association of a single type of subunit with a relative molecular mass of 21,066 resulting in a large homopolymer of relative molecular mass over 2,000,000. The enzyme exhibits a typical flavoprotein spectrum with maxima at 343.5 and 447.5 nm, the flavin prosthetic group being covalently bound to the protein. The catalytic reaction of the natural substrate cyclo(L-Phe-L-Leu) occurs in a two-step sequential reaction leading first to cyclo(alpha,beta-dehydro-Phe-L-Leu) and finally to albonoursin. Kinetic parameters for the first step were determined (K(m) = 53 microM; k = 0.69 s(-1)). The enzyme was shown to catalyze the conversion of a variety of cyclo(dipeptides) and can be reoxidized at the expense of molecular oxygen by producing H(2)O(2). This reaction mechanism, which differs from those already described for the formation of alpha,beta-dehydro-amino acids, might consist of the transient formation of an intermediate imine followed by its rearrangement into an alpha,beta-dehydro-residue.

Catalysis↗

Changes in the physiological and agricultural characteristics of peat-based Bradyrhizobium japonicum inoculants after long-term storage.

Commercial soybean inoculants processed with sterilised peat and stored at 20 degrees C for 1-8 years were used as experimental materials to assess the changes in the physiological activity of Bradyrhizobium japonicum after storage. Viable counts decreased and physiological characteristics of the bacterium changed during storage, with an increase in the time taken for colony appearance on a medium without yeast extract, an increase in the lag time for nodule appearance on soybean grown in glass tubes and a decrease in survival on seeds. All the inoculants produced a significant increase in grain yield in a field experiment. The percentage of efficient cells in the field (relative to the plate counts) decreased as the length of storage increased. These results suggest that the physiological activity of B. japonicum cells changes after storage. Practical implications for inoculant quality control are discussed.

Bradyrhizobium↗

Quantitative determination of endotoxins released by bacterial biofilms.

Residual endotoxins, commonly associated with bacterial biofilms colonizing reusable medical devices have been associated with pyrogenic reactions in patients. We have used a quantitative, sensitive and reproducible kinetic chromogenic adaptation of the Limulus Amebocyte Lysate assay to assess endotoxin recovery from an in-vitro bacterial biofilm. The 'recovery method' was based on a combination of physical treatment (vortexing and sonication) and chemical treatment (immersion in recovery solution). Five recovery solutions were investigated. The recovered endotoxin was greater when the biofilm was treated with a 1% SDS solution. The sensitive and reproducible method we have developed should allow the recovery and measurement of biofilm bacterial endotoxins on implanted and colonized medical devices. Moreover, the amount of endotoxin was sufficient (> 1000 endotoxin units/cm2 of substrate) to enable a substantial reduction by sterilization processes, the efficiency of which on biofilm endotoxins has yet to be proven.

Biofilms↗

Influence of skull anisotropy for the forward and inverse problem in EEG: simulation studies using FEM on realistic head models.

For the sake of realism in the description of conduction from primary neural currents to scalp potentials, we investigated the influence of skull anisotropy on the forward and inverse problems in brain functional imaging with EEG. At present, all methods available for cortical imaging assume a spherical geometry, or when using realistic head shapes do not consider the anisotropy of head tissues. However, to our knowledge, no study relates the implication of this simplifying hypothesis on the spatial resolution of EEG for source imaging. In this paper, a method using finite elements in a realistic head geometry is implemented and validated. The influence of erroneous conductivity values for the head tissues is presented, and results show that the conductivities of the brain and the skull in the radial orientation are the most critical ones. In the inverse problem, this influence has been evaluated with simulations using a distributed source model with a comparison of two regularization techniques, with the isotropic model working on data sets produced by a nonisotropic model. Regularization with minimum norm priors produces source images with spurious activity, meaning that the errors in the head model totally annihilate any localization ability. But nonlinear regularization allows the accurate recovery of simultaneous spots of activity, while the restoration of very close active regions is profoundly disabled by errors in the head model. We conclude that for robust cortical source imaging with EEG, a realistic head model taking anisotropy of tissues into account should be used.

Anisotropy↗

Thorium excretion in feces by mineral sands workers.

An attempt has been made to correlate the thorium excreted in the feces of two male workers in the monazite section of a mineral sands dry separation plant over a ten-day period with personal air sampling measurements. The air-borne radioactivity was measured on a daily basis using a total (inspirable) dust filter, an integrating personal dosimeter, and a personal cascade impactor. The thorium content of the feces was measured using inductively coupled plasma mass spectrometry. The results suggest that thorium fecal analyses are able to detect acute and chronic exposures to the inhalation of thorium bearing dusts and to confirm the amount of inhaled thorium predicted from air sampling programs and metabolic models.

Administration, Inhalation↗

The biooxidation of cytotoxic ellipticine derivatives: a key to structure-activity relationship studies?

In the family of ellipticine derivatives, those with an amino-phenol or a masked amino-phenol structure are among the most cytotoxic compounds. Preliminary studies on 9-hydroxy- or 9-methoxyellipticines have shown that these molecules behave as "pro-alkylating" agents. In order to rationalize the "biooxidative alkylation" process for various ellipticine derivatives, we report in the present article (i) their electrochemical oxidation parameters, (ii) their biochemical oxidation, (iii) the ability of the oxidized forms to form adducts with nucleophiles, (iv) the biological activities, and (v) the electronic properties of oxidized forms. We present some possible correlations between the oxidizability, the electrophilicity of the oxidized derivatives, and the biological activities of the corresponding drugs.

Alkaloids↗

Peroxidase-catalysed oxidation of N2,N6-dimethyl-9-hydroxyellipticinium acetate. Evidence for the formation of an electrophilic quinone-iminium derivative.

The activation of N2,N6-dimethyl-9-hydroxyellipticinium acetate (DMHE) by a peroxidase-H2O2 system leads to a reactive orthoquinone, or in the presence of a nucleophile like alanine, to adducts with a proposed benzoxazole structure. The stoichiometric and pH metric studies support the generation of a bicationic electrophilic intermediate, namely a quinone-iminium. Since no N6-demethylation occurs during the oxidation process, DMHE is not a prodrug of Celiptium (N2-methyl-9-hydroxy-ellipticinium acetate), but the high electrophilic properties of the species generated might explain its great cytotoxicity and antitumor properties. These results extend the possibility for N6-methyl ellipticine derivatives of a biooxidative activation which can play a role in their cytotoxicity.

Alanine↗

Oxidative biotransformation of the antitumour agent elliptinium acetate: Structural characterization of its human and rat urinary metabolites.

The electrophilic properties of the antitumour drug N(2)-methyl-9-hydroxyellipticinium acetate (Celiptium) are revealed by the detection of thiol-conjugate metabolites in man and rat urine. Besides the unchanged drug and its glucuronide, the cysteinyl- (in man) and the N-acetylcysteinyl- (in man and rat) conjugates have been unambiguously characterized using NMR, UV and mass spectral data. The urinary excretion profile exhibits total excreted products of 21% (in man) and 9% (in rat) with respect to the administered dose. The unchanged drug is found to be the major excreted compound from urine in both species (17% in man, 6.3% in rat); whereas the glucuronide (2.6% in man, 1.5% in rat), cysteinyl- (1.3% in man) and N-acetylcysteinyl- (0.2% in man, 1.2% in rat) conjugates represent the minor excreted compounds. The presence of the latter thio-conjugates provides an indirect proof of the in vivo generation of an oxidized intermediate form of the administered drug.

Journal Article↗

Ribose as the preferential target for the oxidized form of elliptinium acetate in ribonucleos(t)ides. Biological activities of the resulting adducts.

The covalent binding of the oxidized form of elliptinium acetate, an antitumor drug, to various ribonucleos(t)ides is described. In the absence of a strong nucleophile on the bases, e.g., a sulfhydryl group, the main target of this quinone imine derivative is the sugar moiety. With unmodified regular bases, the first electrophilic addition always occurs on the 2'-oxygen of ribose (more slowly for pyrimidine than for purine); in a second step, cyclization of the reoxidized product leads to a spiro derivative: only one stereoisomer is detected with purine nucleoside; the other stereoisomer appears as a minor product (10-20%) with nucleotides and pyrimidine nucleosides. With modified bases, no change is observed except for bases exhibiting an additional strong nucleophilic center: oxidized elliptinium alkylates thioguanine and thioguanosine on the sulfur atom and in this last case not on the ribose moiety. All spiro derivatives are less cytotoxic than the parent compound even if the base is an antimetabolite (azauridine); however, thio-elliptinium adducts maintain high cytotoxicity.

Alkaloids↗

Peroxidase-catalyzed O-demethylation reactions. Quinone-imine formation from 9-methoxyellipticine derivatives.

Despite numerous reports on the N-demethylation reactions catalyzed by peroxidases, to our knowledge, O-demethylation reactions with the same enzymes seem to be still a questionable matter. Unexpectedly, a peroxidase system (horseradish peroxidase and hydrogen peroxide) is able to effect the O-demethylation of the cytotoxic agents 9-methoxyellipticine and N2-methyl-9-methoxyellipticinium acetate. The reaction leads directly to the formation of the corresponding quinone-imine derivatives with the concomitant formation of one molecule of methanol per molecule of methoxy compound. One hydrogen peroxide molecule is consumed during the process. Experiments in H218O-enriched water clearly indicate that 18O is nearly quantitatively incorporated in the carbonyl group of the generated quinone-imine compound with the concomitant elimination of the methoxy group as methanol. So this peroxidase-catalyzed apparent O-demethylation in fact implies an oxidative demethoxylation step. This enzymatic reaction exhibits normal Michaelis-Menten saturation kinetics. Like the 9-hydroxylated ellipticines, both the 9-methoxylated ellipticines show a good affinity for the peroxidase itself (Km approximately 10 microM) but are slowly transformed to the corresponding quinone-imines. The Vmax values for methoxylated ellipticines are 10(-1)-10(-3) lower than those for hydroxylated compounds. This new route for the in vitro formation of electrophilic derivatives from the cytotoxic 9-methoxyellipticine and N2-methyl-9-methoxyellipticinium might be considered as a novel possible metabolic pathway for these drugs, especially if we bear in mind the "bio-oxidative alkylation" process previously described for at least one of the corresponding hydroxylated ellipticine derivatives (see Bernadou, J., Meunier, B., Meunier, G., Auclair, C., and Paoletti, C. (1984) Proc. Natl. Acad. Sci. U.S.A. 81, 1297-1301; and Monsarrat, B., Maftouh, M., Meunier, G., Dugué, B., Bernadou, J., Armand, J. P., Picard-Fraire, C., Meunier, B., and Paoletti, C. (1983) Biochem. Pharmacol. 32, 3887-3890).

Alkaloids↗

Regioselective arylation of ribose in adenosine and guanosine with the antitumor drug N2-methyl-9-hydroxyellipticinium acetate.

The transformation of the antitumor drug N2-methyl-9-hydroxy-ellipticinium by a peroxidase-hydrogen peroxide system, which has been shown to occur in vivo, leads to an electrophilic quinone-imine derivative. This unstable molecule arylates in vitro purine nucleosides and nucleotides, leading to regioselective adducts substituted only at the 2'-O position of the ribose, as shown by mass spectrometry and NMR. It is likely that an important preliminary step in this reaction is a stacking process between the ellipticinium ion and the purine rings, which might explain this regioselectivity.

Adenosine↗

omicron-Quinone formation in the biochemical oxidation of the antitumor drug N2-methyl-9-hydroxyellipticinium acetate.

The activation of N2-methyl-9-hydroxyellipticinium acetate (4) by a peroxidase--H2O2 system leads to the formation of an omicron-quinone (7a). This omicron-quinone is not directly generated from the starting material but through a quinone imine intermediate (6) which is subsequently oxidized. This reaction is highly dependent on pH values. The omicron-quinone 7a is easily protonated (7b), gives an addition product with methanol (9), and is reduced by cysteine. The omicron-quinone 7b has a rather low inhibitory effect against L1210 leukemia cell multiplication but acts as an electron carrier and dramatically augments the oxygen consumption in xanthine oxidase-NADH and rat liver microsomes-NADPH systems.

Alkaloids↗

Vitamin D metabolism in preterm infants. Serial serum calcitriol values during the first four days of life.

In order to evaluate after birth the changes in circulating vitamin D metabolite levels in preterm babies supplemented with vitamin D (2 100 I.U./d), the serum concentration of 25-hydroxyvitamin D [25-OHD] and 1 alpha,25-dihydroxyvitamin D [1,25(OH)2D] were measured in 22 infants (31 to 35 weeks of gestation) from birth up to 96 hours of age. Compared to cord blood levels, serum calcium decreased significantly during the first 24 hours of life (p less than 0.005) and remained low until day 4. Serum immunoreactive parathyroid hormone (iPTH) levels increased from birth to 24 hours and then plateaued. The 25-OHD levels at birth were 27.5 +/- 2.5 nmol/l and increased to 67.5 +/- 12.5 nmol/l (p less than 0.005) during the four days of the study. During the same period, the 1,25(OH)2D serum levels increased steadily from 84 less than 7 to 343 less than 105 pmol/l (p less than 0.005). At all times, there was a positive correlation between 25-OHD levels and those of 1,25(OH)2D. Our data demonstrate that in preterm infants after 31 weeks of gestation, absorption and activation of vitamin D is present as soon as 24 hours after birth and that early neonatal hypocalcemia is unlikely to be caused by an impairment of either PTH secretion or vitamin D activation.

25-Hydroxyvitamin D 2↗