Jean-françois Goossens - Academia.edu (original) (raw)
Papers by Jean-françois Goossens
HAL (Le Centre pour la Communication Scientifique Directe), Oct 1, 2016
![Research paper thumbnail of Highly Cytotoxic Benzo[c]pyrido[2,3,4-kl]acridines](https://attachments.academia-assets.com/117238011/thumbnails/1.jpg)
](ChemInform, Jul 29, 2003
Several benzo[c]pyrido[2,3,4-kl]acridines bearing different substituents on the A and E rings wer... more Several benzo[c]pyrido[2,3,4-kl]acridines bearing different substituents on the A and E rings were synthesized and evaluated for their capacity to bind to DNA and to inhibit DNA topoisomerases. Potent cytotoxic compounds were discovered but no strict correlation with their DNA binding affinity and effects on topoisomerases were observed. DNA is one but not the unique target of these compounds.
Letters in Peptide Science, Jul 1, 1999
Chemical modifications were obtained on the dual NK1/NK2 ligand Cbz-Gly-Leu-Trp-OBzl(CF3)2 with a... more Chemical modifications were obtained on the dual NK1/NK2 ligand Cbz-Gly-Leu-Trp-OBzl(CF3)2 with a view to optimizing affinities for both NKI and NK2 receptors. Replacement of the Gly residue by other amino acids increased affinities for NK~/NK2 receptors or induced selectivity for the NK1 receptor.
Journal of Medicinal Chemistry, Sep 12, 2002
ABSTRACT
Neuropeptides, Feb 1, 1993
Tissue transglutaminase (tTG) activity was used to test the potent regulatory role of vasoactive ... more Tissue transglutaminase (tTG) activity was used to test the potent regulatory role of vasoactive intestinal peptide (VIP) on Retinoic Acid-induced effect in human neuroblastoma cell line. The comparison between both differentiation and cell death related to tissue transglutaminase was discussed in this model. VIP alone was a potent differentiating agent in SK-N-SH cells but in the presence of retinoic acid (RA), this peptide rather potentiates RA-induced tTG activity which is now considered as an apoptosis marker in neuroblastoma cell line. This paper demonstrated an additional neuromodulator role for VIP.
Journal of Chromatography B: Biomedical Sciences and Applications, Jul 1, 1994
ABSTRACT
Electrophoresis, Dec 1, 2006
EKC methods for the enantiomeric resolution of homocamptothecin derivatives, potent anticancer ag... more EKC methods for the enantiomeric resolution of homocamptothecin derivatives, potent anticancer agents targeting DNA topoisomerase I selected for clinical trials, were developed using highly sulfated beta-CD as chiral selectors at acidic pH. Optimal electrophoretic conditions, with migration times under 15 min, were as follows: for the neutral homocamptothecin analog 1, a BGE of 75 mM phosphate buffer pH 2.5 (H(3)PO(4) + triethanolamine)/ACN - 95/5 v/v, with 7.5% w/v highly S-beta-CD, an applied field of 0.2 kV/cm and a fused capillary temperature control of 30 +/- 0.1 degrees C (typical current approximately 175 microA); for the cationic homocamptothecin 2, a BGE of 25 mM phosphate buffer pH 2.5 (H(3)PO(4) + TEA)/ACN - 90/10 v/v, with 2.5% w/v highly S-beta-CD, an applied field of 0.15 kV/cm and a fused capillary temperature control of 25 +/- 0.1 degrees C (typical current approximately 45 muA), and both are validated. The best results in terms of LOQ were obtained by EC with fluorescence detection: 10 ng/mL and 20 ng/mL for 1 and 2, respectively (LOQ divided by 150 for 1 and 5 for 2 with respect to UV), thus making this method particularly convenient for enantiomeric purity determination of galenic forms. UV detection appears to be an alternative to fluorescence for the analysis of the main component either for the control of galenic forms or for therapeutic adaptation. Moreover, this method exhibits better performances than HPLC.
Bioorganic & Medicinal Chemistry Letters, Oct 1, 2007
A new series of FTase inhibitors containing a tricyclic moiety--dioxodibenzothiazepine or dibenzo... more A new series of FTase inhibitors containing a tricyclic moiety--dioxodibenzothiazepine or dibenzocycloheptane--has been designed and synthesized. Among them, dioxodibenzothiazepine 18d displayed significant inhibitory FTase activity (IC(50)=17.3 nM) and antiproliferative properties.
Analytical Letters, 2003
A method for the simultaneous determination of di(2-ethylhexyl)-phthalate and its major metabolit... more A method for the simultaneous determination of di(2-ethylhexyl)-phthalate and its major metabolite mono(2-ethylhexyl)phthalate in human plasma by high-performance liquid chromatography is described. The procedure, linear in the concentration range 0.05-5.0 ppm, is simple and ...
Organometallics, Aug 19, 2016
A series of di-nuclear ruthenium arene complexes with TSC ligands ([(η 6-pcymene)Ru(N 1 ,S-TSC)] ... more A series of di-nuclear ruthenium arene complexes with TSC ligands ([(η 6-pcymene)Ru(N 1 ,S-TSC)] 2 Cl 2 , A-type, 1 and 2) and their corresponding analogues ([(η 6-p-cymene)Ru(N 2 ,S-TSC)] 2 Cl 2 , B-type, 3 and 4), in which TSCs act as different coordination mode, have been synthesized and structurally characterized by a variety of physical methods. The molecular structures of 1, 3 and 4 were determined using single-crystal X-ray diffraction analysis. The Gibbs free energy of the two examples of the two types of complexes (1 and 3) and bonding order in their single-crystals were discussed using density functional theory (DFT) calculations. The compounds were further evaluated for their in vitro antiproliferative activities against several cancerous and HEK-293 T noncancerous cell lines, and the results indicate that B-type complexes show stronger cytotoxicity than A-type complexes. Furthermore, the interactions of the compounds with DNA were investigated by electrophoretic mobility spectrometry studies.
Pharmacology, 2014
Background/Aims: The in vivo metabolic profile of a benzopyridooxathiazepine (BPT) derivative, a ... more Background/Aims: The in vivo metabolic profile of a benzopyridooxathiazepine (BPT) derivative, a potent tubulin polymerization inhibitor with a promising in vitro activity, was investigated. Methods: The quantification of the BPT derivative and the identification of metabolites in the plasma of Wistar rats after i.p. and oral administration of 10 mg/kg were performed by the HPLC-mass spectrometry method. Results: Following a single i.p. dose of the BPT derivative, the plasma concentrations showed a biexponential decay (with a rapid decline) followed by a slow decay with a terminal half-life of 77.90 min. The area under the concentration-time curve from time 0 to infinity (AUC0-∞) was 18.90 µg/ml·min. After oral administration, the plasmatic concentrations reached a peak of 0.06 μg/ml at 35 min and then decayed with a half-life of 108 min. The AUC0-∞ was 10.25 µg/ml·min, representing 54.2% of the relative bioavailability. The compound was well distributed in the body, and its elimination seemed to be fast, regardless of the administration route. The major metabolic pathways were demethylation and hydroxylation reactions, both followed by conjugation with glucuronic acid. Conclusion: In rats, the BPT derivative is well distributed and undergoes extensive metabolism, leading to several metabolites. With promising in vitro activity and very good oral bioavailability, this compound seems to be an attractive candidate for further development as an anticancer agent.
Regulatory Peptides, Jul 1, 1994
VIP is a widely distributed neuropeptide of 28 amino acids, whose central part is proposed to be ... more VIP is a widely distributed neuropeptide of 28 amino acids, whose central part is proposed to be an amphiphilic alpha-helix. In order to gain an understanding of the effect of this alpha helix on receptor binding and stimulation, a human VIP analog has been designed in which the residues 12 to 19 were replaced by a spacer of the same length, (gamma-aminobutyryl)2. This peptide altered neither the basal guinea pig tracheal smooth muscle tonus nor the VIP-induced relaxation. Conversely, the VIP analog was found to displace VIP from its binding sites on LA-N-2 human neuroblastoma cells (VIP IC50: 5.4 nM; VIP analog IC50: 52.2 nM) and to inhibit the VIP-induced cyclic AMP production of 58 +/- 15% at 1 microM and 95 +/- 2% at 10 microM. It seems that the alpha helix structure might only play the role of a spacer holding the important residues, at the N- and C-ends, respectively, at an appropriate distance. In the VIP analog structure, the (gamma-aminobutyryl)2 chain introduced in place of the alpha helix plays the role of adequate spacer to bind the LA-N-2 receptors but probably does not induce the active conformation for receptor stimulation. The lack of VIP analog effects on the tracheal receptors related to relaxation argues for a possible heterogeneity of VIP receptors on a pharmacological basis.
Letters in Peptide Science, Jul 1, 1999
Chemical modifications on the NK 1 competitive antagonist L-732,138, with a view to creating a du... more Chemical modifications on the NK 1 competitive antagonist L-732,138, with a view to creating a dual NK 1 /NK 2 ligand, led to the tryptophan derivative 1 possessing the protected Gly-Leu sequence of the C-terminus of substance P and neurokinin A. Modifications in the nature of the carbamate function increased the selectivity for the NK 1 receptor, whereas the inclusion of the indole moiety in β-carboline or carbazole rings decreased the affinity for both receptors. Free indolylmethyl and Cbz carbamate groups were shown to be essential for NK 2 affinity.
Journal of Chromatography A, Jul 1, 2016
Tetrahedron Letters, Apr 1, 2011
Metabolism-clinical and Experimental, Feb 1, 2020
Objective: Bile acids (BAs) are signaling molecules controlling lipid and glucose metabolism. Sin... more Objective: Bile acids (BAs) are signaling molecules controlling lipid and glucose metabolism. Since BA alterations are associated with obesity and insulin resistance, plasma BAs have been considered candidates to predict type 2 diabetes (T2D) risk. We aimed to determine (1) the association of BAs with glucose homeostasis parameters and (2) their predictive association with the risk of conversion from prediabetes to new-onset diabetes (NOD) in a prospective cohort study. Design: 205 patients with impaired fasting glucose (IFG) were followed each year during 5 years in the IT-DIAB cohort study. Twenty-one BA species and 7α-hydroxy-4-cholesten-3-one (C4), a marker of BA synthesis, were quantified by LC/MS-MS in plasma from fasted patients at baseline. Correlations between plasma BA species and metabolic parameters at baseline were assessed by Spearman's coefficients and the association between BAs and NOD was determined using Cox proportional-hazards models. Results: Among the analyzed BA species, total hyocholic acid (HCA) and the total HCA/total chenodeoxycholic acid (CDCA) ratio, reflecting hepatic BA 6α-hydroxylation activity, negatively correlated with BMI and HOMA-IR. The total HCA/total CDCA ratio also correlated negatively with HbA 1C. Conversion from IFG to NOD occurred in 33.7% of the participants during the follow-up. Plasma BA species were not independently associated with the conversion to NOD after adjustment with classical T2D risk factors. Conclusions: Fasting plasma BAs are not useful clinical biomarkers for predicting NOD in patients with IFG. However, an unexpected association between 6α-hydroxylated BAs and glucose parameters was found, suggesting a role for this specific BA pathway in metabolic homeostasis. IT-DIAB study registry number: NCT01218061.
Toxicologie Analytique et Clinique, May 1, 2017
S33 8,5 %) et sévère (4,3 % versus 2,7 %) (p < 0,001) proportionnellement plus fréquente. Discuss... more S33 8,5 %) et sévère (4,3 % versus 2,7 %) (p < 0,001) proportionnellement plus fréquente. Discussion La rapidité et la concordance des réponses des mycologues pour l'identification des champignons impliqués dans les intoxications est une plus-value pour la prise en charge du patient par le médecin. Lorsque la Mycoliste était sollicitée pour des cas d'expositions d'enfants, la gravité des cas était plus fréquemment de PSS0 car il s'agissait d'enfants ayant ingéré un petit morceau de champignon. Pour les adultes, la Mycoliste a été plus fréquemment sollicitée pour des intoxications modérées ou sévères afin de corréler le toxidrome à l'espèce en cause. Cette Mycoliste permettra probablement à terme d'améliorer la connaissance de la toxicité humaine des champignons. Remerciements Nous remercions l'ensemble des mycologues participant à la Mycoliste sans lesquels ce travail n'aurait pas été possible. Déclaration de liens d'intérêts Les auteurs déclarent ne pas avoir de liens d'intérêts.
PubMed, 1992
The conformation of various regions of vasoactive intestinal peptide (VIP) has been analyzed by s... more The conformation of various regions of vasoactive intestinal peptide (VIP) has been analyzed by semiempirical methods, CD, and NMR spectroscopy, indicating that residues 11-21 are most likely to be helical, whereas the amino-terminal portion VIP(1-11) could exhibit two beta-turn structures. VIP(1-11) inhibits 125I-VIP binding to intact guinea pig tracheal epithelial cells and the VIP-induced smooth muscle response. However, the endecapeptide exhibits no effect on the muscle tone. All these data suggest that VIP(1-11) may be a useful tool in studying VIP receptor recognition, its regulation, and cellular functions.
Waste and Biomass Valorization, Jul 10, 2020
In the actual context of food safety and circular economy, the separation of the α137-141 antimic... more In the actual context of food safety and circular economy, the separation of the α137-141 antimicrobial peptide (TSKYR, 653 Da) coming from the hydrolysis of bovine hemoglobin, a non-valorized slaughterhouse by-product, and its reuse as a preservative agent for food products during storage would be of major interest. However, depending on the degree of hydrolysis (DH) of the bovine hemoglobin, the TSKYR peptide environment into the hydrolysate will be different and would impact its recovery yield by electrodialysis with ultrafiltration membranes (EDUF), a hybrid and eco-friendly technology. In this context, five DHs (3, 5, 10, 13 and 18%) were investigated to study the influence of the peptide populations on the α137-141 selective separation by EDUF. It appeared from these results that the most appropriate DH was of 5% since a lower population of peptides between 500 and 1000 Da was present and the subunits of hemoglobin were already digested. Hence, an enrichment factor of about 13 folds for the α137-141 was obtained in comparison with the initial hydrolysate. At our knowledge, it was the first time that the effect of the hydrolysis degree of a protein is demonstrated to impact preferentially the separation of a specific peptide by EDUF.
Journal of Chromatography B, Sep 1, 2018
HAL is a multidisciplinary open access archive for the deposit and dissemination of scientific re... more HAL is a multidisciplinary open access archive for the deposit and dissemination of scientific research documents, whether they are published or not. The documents may come from teaching and research institutions in France or abroad, or from public or private research centers. L'archive ouverte pluridisciplinaire HAL, est destinée au dépôt et à la diffusion de documents scientifiques de niveau recherche, publiés ou non, émanant des établissements d'enseignement et de recherche français ou étrangers, des laboratoires publics ou privés.
HAL (Le Centre pour la Communication Scientifique Directe), Oct 1, 2016
ChemInform, Jul 29, 2003
Several benzo[c]pyrido[2,3,4-kl]acridines bearing different substituents on the A and E rings wer... more Several benzo[c]pyrido[2,3,4-kl]acridines bearing different substituents on the A and E rings were synthesized and evaluated for their capacity to bind to DNA and to inhibit DNA topoisomerases. Potent cytotoxic compounds were discovered but no strict correlation with their DNA binding affinity and effects on topoisomerases were observed. DNA is one but not the unique target of these compounds.
Letters in Peptide Science, Jul 1, 1999
Chemical modifications were obtained on the dual NK1/NK2 ligand Cbz-Gly-Leu-Trp-OBzl(CF3)2 with a... more Chemical modifications were obtained on the dual NK1/NK2 ligand Cbz-Gly-Leu-Trp-OBzl(CF3)2 with a view to optimizing affinities for both NKI and NK2 receptors. Replacement of the Gly residue by other amino acids increased affinities for NK~/NK2 receptors or induced selectivity for the NK1 receptor.
Journal of Medicinal Chemistry, Sep 12, 2002
ABSTRACT
Neuropeptides, Feb 1, 1993
Tissue transglutaminase (tTG) activity was used to test the potent regulatory role of vasoactive ... more Tissue transglutaminase (tTG) activity was used to test the potent regulatory role of vasoactive intestinal peptide (VIP) on Retinoic Acid-induced effect in human neuroblastoma cell line. The comparison between both differentiation and cell death related to tissue transglutaminase was discussed in this model. VIP alone was a potent differentiating agent in SK-N-SH cells but in the presence of retinoic acid (RA), this peptide rather potentiates RA-induced tTG activity which is now considered as an apoptosis marker in neuroblastoma cell line. This paper demonstrated an additional neuromodulator role for VIP.
Journal of Chromatography B: Biomedical Sciences and Applications, Jul 1, 1994
ABSTRACT
Electrophoresis, Dec 1, 2006
EKC methods for the enantiomeric resolution of homocamptothecin derivatives, potent anticancer ag... more EKC methods for the enantiomeric resolution of homocamptothecin derivatives, potent anticancer agents targeting DNA topoisomerase I selected for clinical trials, were developed using highly sulfated beta-CD as chiral selectors at acidic pH. Optimal electrophoretic conditions, with migration times under 15 min, were as follows: for the neutral homocamptothecin analog 1, a BGE of 75 mM phosphate buffer pH 2.5 (H(3)PO(4) + triethanolamine)/ACN - 95/5 v/v, with 7.5% w/v highly S-beta-CD, an applied field of 0.2 kV/cm and a fused capillary temperature control of 30 +/- 0.1 degrees C (typical current approximately 175 microA); for the cationic homocamptothecin 2, a BGE of 25 mM phosphate buffer pH 2.5 (H(3)PO(4) + TEA)/ACN - 90/10 v/v, with 2.5% w/v highly S-beta-CD, an applied field of 0.15 kV/cm and a fused capillary temperature control of 25 +/- 0.1 degrees C (typical current approximately 45 muA), and both are validated. The best results in terms of LOQ were obtained by EC with fluorescence detection: 10 ng/mL and 20 ng/mL for 1 and 2, respectively (LOQ divided by 150 for 1 and 5 for 2 with respect to UV), thus making this method particularly convenient for enantiomeric purity determination of galenic forms. UV detection appears to be an alternative to fluorescence for the analysis of the main component either for the control of galenic forms or for therapeutic adaptation. Moreover, this method exhibits better performances than HPLC.
Bioorganic & Medicinal Chemistry Letters, Oct 1, 2007
A new series of FTase inhibitors containing a tricyclic moiety--dioxodibenzothiazepine or dibenzo... more A new series of FTase inhibitors containing a tricyclic moiety--dioxodibenzothiazepine or dibenzocycloheptane--has been designed and synthesized. Among them, dioxodibenzothiazepine 18d displayed significant inhibitory FTase activity (IC(50)=17.3 nM) and antiproliferative properties.
Analytical Letters, 2003
A method for the simultaneous determination of di(2-ethylhexyl)-phthalate and its major metabolit... more A method for the simultaneous determination of di(2-ethylhexyl)-phthalate and its major metabolite mono(2-ethylhexyl)phthalate in human plasma by high-performance liquid chromatography is described. The procedure, linear in the concentration range 0.05-5.0 ppm, is simple and ...
Organometallics, Aug 19, 2016
A series of di-nuclear ruthenium arene complexes with TSC ligands ([(η 6-pcymene)Ru(N 1 ,S-TSC)] ... more A series of di-nuclear ruthenium arene complexes with TSC ligands ([(η 6-pcymene)Ru(N 1 ,S-TSC)] 2 Cl 2 , A-type, 1 and 2) and their corresponding analogues ([(η 6-p-cymene)Ru(N 2 ,S-TSC)] 2 Cl 2 , B-type, 3 and 4), in which TSCs act as different coordination mode, have been synthesized and structurally characterized by a variety of physical methods. The molecular structures of 1, 3 and 4 were determined using single-crystal X-ray diffraction analysis. The Gibbs free energy of the two examples of the two types of complexes (1 and 3) and bonding order in their single-crystals were discussed using density functional theory (DFT) calculations. The compounds were further evaluated for their in vitro antiproliferative activities against several cancerous and HEK-293 T noncancerous cell lines, and the results indicate that B-type complexes show stronger cytotoxicity than A-type complexes. Furthermore, the interactions of the compounds with DNA were investigated by electrophoretic mobility spectrometry studies.
Pharmacology, 2014
Background/Aims: The in vivo metabolic profile of a benzopyridooxathiazepine (BPT) derivative, a ... more Background/Aims: The in vivo metabolic profile of a benzopyridooxathiazepine (BPT) derivative, a potent tubulin polymerization inhibitor with a promising in vitro activity, was investigated. Methods: The quantification of the BPT derivative and the identification of metabolites in the plasma of Wistar rats after i.p. and oral administration of 10 mg/kg were performed by the HPLC-mass spectrometry method. Results: Following a single i.p. dose of the BPT derivative, the plasma concentrations showed a biexponential decay (with a rapid decline) followed by a slow decay with a terminal half-life of 77.90 min. The area under the concentration-time curve from time 0 to infinity (AUC0-∞) was 18.90 µg/ml·min. After oral administration, the plasmatic concentrations reached a peak of 0.06 μg/ml at 35 min and then decayed with a half-life of 108 min. The AUC0-∞ was 10.25 µg/ml·min, representing 54.2% of the relative bioavailability. The compound was well distributed in the body, and its elimination seemed to be fast, regardless of the administration route. The major metabolic pathways were demethylation and hydroxylation reactions, both followed by conjugation with glucuronic acid. Conclusion: In rats, the BPT derivative is well distributed and undergoes extensive metabolism, leading to several metabolites. With promising in vitro activity and very good oral bioavailability, this compound seems to be an attractive candidate for further development as an anticancer agent.
Regulatory Peptides, Jul 1, 1994
VIP is a widely distributed neuropeptide of 28 amino acids, whose central part is proposed to be ... more VIP is a widely distributed neuropeptide of 28 amino acids, whose central part is proposed to be an amphiphilic alpha-helix. In order to gain an understanding of the effect of this alpha helix on receptor binding and stimulation, a human VIP analog has been designed in which the residues 12 to 19 were replaced by a spacer of the same length, (gamma-aminobutyryl)2. This peptide altered neither the basal guinea pig tracheal smooth muscle tonus nor the VIP-induced relaxation. Conversely, the VIP analog was found to displace VIP from its binding sites on LA-N-2 human neuroblastoma cells (VIP IC50: 5.4 nM; VIP analog IC50: 52.2 nM) and to inhibit the VIP-induced cyclic AMP production of 58 +/- 15% at 1 microM and 95 +/- 2% at 10 microM. It seems that the alpha helix structure might only play the role of a spacer holding the important residues, at the N- and C-ends, respectively, at an appropriate distance. In the VIP analog structure, the (gamma-aminobutyryl)2 chain introduced in place of the alpha helix plays the role of adequate spacer to bind the LA-N-2 receptors but probably does not induce the active conformation for receptor stimulation. The lack of VIP analog effects on the tracheal receptors related to relaxation argues for a possible heterogeneity of VIP receptors on a pharmacological basis.
Letters in Peptide Science, Jul 1, 1999
Chemical modifications on the NK 1 competitive antagonist L-732,138, with a view to creating a du... more Chemical modifications on the NK 1 competitive antagonist L-732,138, with a view to creating a dual NK 1 /NK 2 ligand, led to the tryptophan derivative 1 possessing the protected Gly-Leu sequence of the C-terminus of substance P and neurokinin A. Modifications in the nature of the carbamate function increased the selectivity for the NK 1 receptor, whereas the inclusion of the indole moiety in β-carboline or carbazole rings decreased the affinity for both receptors. Free indolylmethyl and Cbz carbamate groups were shown to be essential for NK 2 affinity.
Journal of Chromatography A, Jul 1, 2016
Tetrahedron Letters, Apr 1, 2011
Metabolism-clinical and Experimental, Feb 1, 2020
Objective: Bile acids (BAs) are signaling molecules controlling lipid and glucose metabolism. Sin... more Objective: Bile acids (BAs) are signaling molecules controlling lipid and glucose metabolism. Since BA alterations are associated with obesity and insulin resistance, plasma BAs have been considered candidates to predict type 2 diabetes (T2D) risk. We aimed to determine (1) the association of BAs with glucose homeostasis parameters and (2) their predictive association with the risk of conversion from prediabetes to new-onset diabetes (NOD) in a prospective cohort study. Design: 205 patients with impaired fasting glucose (IFG) were followed each year during 5 years in the IT-DIAB cohort study. Twenty-one BA species and 7α-hydroxy-4-cholesten-3-one (C4), a marker of BA synthesis, were quantified by LC/MS-MS in plasma from fasted patients at baseline. Correlations between plasma BA species and metabolic parameters at baseline were assessed by Spearman's coefficients and the association between BAs and NOD was determined using Cox proportional-hazards models. Results: Among the analyzed BA species, total hyocholic acid (HCA) and the total HCA/total chenodeoxycholic acid (CDCA) ratio, reflecting hepatic BA 6α-hydroxylation activity, negatively correlated with BMI and HOMA-IR. The total HCA/total CDCA ratio also correlated negatively with HbA 1C. Conversion from IFG to NOD occurred in 33.7% of the participants during the follow-up. Plasma BA species were not independently associated with the conversion to NOD after adjustment with classical T2D risk factors. Conclusions: Fasting plasma BAs are not useful clinical biomarkers for predicting NOD in patients with IFG. However, an unexpected association between 6α-hydroxylated BAs and glucose parameters was found, suggesting a role for this specific BA pathway in metabolic homeostasis. IT-DIAB study registry number: NCT01218061.
Toxicologie Analytique et Clinique, May 1, 2017
S33 8,5 %) et sévère (4,3 % versus 2,7 %) (p < 0,001) proportionnellement plus fréquente. Discuss... more S33 8,5 %) et sévère (4,3 % versus 2,7 %) (p < 0,001) proportionnellement plus fréquente. Discussion La rapidité et la concordance des réponses des mycologues pour l'identification des champignons impliqués dans les intoxications est une plus-value pour la prise en charge du patient par le médecin. Lorsque la Mycoliste était sollicitée pour des cas d'expositions d'enfants, la gravité des cas était plus fréquemment de PSS0 car il s'agissait d'enfants ayant ingéré un petit morceau de champignon. Pour les adultes, la Mycoliste a été plus fréquemment sollicitée pour des intoxications modérées ou sévères afin de corréler le toxidrome à l'espèce en cause. Cette Mycoliste permettra probablement à terme d'améliorer la connaissance de la toxicité humaine des champignons. Remerciements Nous remercions l'ensemble des mycologues participant à la Mycoliste sans lesquels ce travail n'aurait pas été possible. Déclaration de liens d'intérêts Les auteurs déclarent ne pas avoir de liens d'intérêts.
PubMed, 1992
The conformation of various regions of vasoactive intestinal peptide (VIP) has been analyzed by s... more The conformation of various regions of vasoactive intestinal peptide (VIP) has been analyzed by semiempirical methods, CD, and NMR spectroscopy, indicating that residues 11-21 are most likely to be helical, whereas the amino-terminal portion VIP(1-11) could exhibit two beta-turn structures. VIP(1-11) inhibits 125I-VIP binding to intact guinea pig tracheal epithelial cells and the VIP-induced smooth muscle response. However, the endecapeptide exhibits no effect on the muscle tone. All these data suggest that VIP(1-11) may be a useful tool in studying VIP receptor recognition, its regulation, and cellular functions.
Waste and Biomass Valorization, Jul 10, 2020
In the actual context of food safety and circular economy, the separation of the α137-141 antimic... more In the actual context of food safety and circular economy, the separation of the α137-141 antimicrobial peptide (TSKYR, 653 Da) coming from the hydrolysis of bovine hemoglobin, a non-valorized slaughterhouse by-product, and its reuse as a preservative agent for food products during storage would be of major interest. However, depending on the degree of hydrolysis (DH) of the bovine hemoglobin, the TSKYR peptide environment into the hydrolysate will be different and would impact its recovery yield by electrodialysis with ultrafiltration membranes (EDUF), a hybrid and eco-friendly technology. In this context, five DHs (3, 5, 10, 13 and 18%) were investigated to study the influence of the peptide populations on the α137-141 selective separation by EDUF. It appeared from these results that the most appropriate DH was of 5% since a lower population of peptides between 500 and 1000 Da was present and the subunits of hemoglobin were already digested. Hence, an enrichment factor of about 13 folds for the α137-141 was obtained in comparison with the initial hydrolysate. At our knowledge, it was the first time that the effect of the hydrolysis degree of a protein is demonstrated to impact preferentially the separation of a specific peptide by EDUF.
Journal of Chromatography B, Sep 1, 2018
HAL is a multidisciplinary open access archive for the deposit and dissemination of scientific re... more HAL is a multidisciplinary open access archive for the deposit and dissemination of scientific research documents, whether they are published or not. The documents may come from teaching and research institutions in France or abroad, or from public or private research centers. L'archive ouverte pluridisciplinaire HAL, est destinée au dépôt et à la diffusion de documents scientifiques de niveau recherche, publiés ou non, émanant des établissements d'enseignement et de recherche français ou étrangers, des laboratoires publics ou privés.