Anévrysme et Pseudo-anévrysme du ventricule gauche

La gravité de l’infarctus du myocarde réside dans ses complications. Certainement, on avait une importante réduction dans leurs incidences grâce  à  l’amélioration de la prise en charge médicale et l’avènement des méthodes de reperfusion précoce, mais il persiste un taux considérable de complications qui posent un problème diagnostic mais surtout thérapeutique. Parmi eux, il existe l’anévrysme et le pseudo-anévrysme du ventricule gauche. Ces deux complications relativement rares sont souvent méconnues, d’où l’intérêt d’en connaître les modalités de prise en charge diagnostique et thérapeutiques

Viability-reducing activity of Coryllus avellana L. extracts against human cancer cell lines

The increasing rate of cancer incidence has encouraged the search for novel natural sources of anticancer compounds. The presence of small quantities of taxol and taxanes in Corylus avellana L. has impelled new potential applications for this plant in the field of biomedicine. In the present work, the cell viability-reducing activity of stems and leaves from three different hazel trees was studied against three human-derived cancer cell lines (HeLa, HepG2 and MCF-7). Both leaf and stem extracts significantly reduced viability of the three cell lines either after maceration with methanol or using taxane extraction methods. Since maceration reduced cell viability to a greater extent than taxane extraction methods, we scaled up the maceration extraction process using a method for solid/liquid extraction (Zippertex technology). Methanol leaf extracts promoted a higher reduction in viability of all cell lines assayed than stem extracts. Fractionation of methanol leaf extracts using silica gel chromatography led to the purification and identification of two compounds by HPLC-MS and NMR: (3R,5R)-3,5-dihydroxy-1,7-bis(4-hydroxyphenyl) heptane 3-O-β-d-glucopyranoside and quercetin-3-O-rhamnoside. The isolated compounds decreased viability of HeLa and HepG2 cells to a greater extent than MCF-7 cells. Our results suggest a potential use of C. avellana extracts in the pharmacotherapy of cervical cancer and hepatocarcinoma and, to a lesser extent, breast cancer

2-Butyl-5-pentyl­benzene-1,3-diol

In the title compound, C15H24O2, a natural dialkyl­resorcinol commonly named stemphol, the mol­ecules are linked into C(6) and C 2 2(4) chains and R 4 4(16) rings by inter­molecular O—H⋯O hydrogen bonds, creating mol­ecular sheets parallel to the (010) plane. The alkyl chains are directed orthogonally away from these planes in almost complete extension

Approche globale pour la gestion et l'élimination des polluants organiques (application aux rejets aqueux issus des procédés de synthèses du 5007-TDS et du 12911)

L approche globale est un concept multidisciplinaire développé au laboratoire de microbiologie appliquée depuis une dizaine d années, dans le but de répondre à un problème industriel. Il a été appliqué, dans le cadre de cette thèse, sur des effluents aqueux rejetés lors de la synthèse de deux médicaments phares des laboratoires Servier : L Arcalion, médicament antiasthénie et le Protelos, utilisé pour la lutte contre l ostéoporose. La première étape du sujet concerne l analyse et la caractérisation des polluants organiques présents dans les deux effluents étudiés. Les deux familles de polluants contiennent soit un squelette thiophénique, soit un noyau aminopyrimidine, exclusivité de la vitamine B1 et un pont disulfure. Des méthodes de dégradation par voies chimique microbiologique et enzymatique ont été mises en place pour étudier d une part l épuration des effluents en question, et d autre part les mécanismes mis en œuvre sur les molécules cibles et modèles appartenant aux familles de polluants étudiés. Les PAO, et plus particulièrement le Fenton et le procédé de ZEA se sont montrés efficaces pour la dépollution des deux effluents. Le métabolisme de chaque molécule cible a également été étudié chez les microorganismes et les mammifères. Enfin, l approche globale contient une partie valorisation, dans laquelle sont testés les différents métabolites en tant que piégeurs de méthylglyoxal, entité responsable des complications du diabète.Global approach was a multidisciplinary concept developed in the laboratory of applied microbiology, since a decade. The aim was to answer to an industrial problem. It was applied, under this Ph-D, to aqueous effluents released during the syntheses of two headlight drugs of Servier laboratories: Arcalion, drug antiastheny and Protelos, used against osteoporosis. The first step or the subject concerned analysis and characterization of organic pollutants present in studied effluents. The two family of pollutants contained either thiophenic skeleton, or aminopyrimidin moiety, exclusive of vitamin B1 and a disulfide bond. Some methods of degradation by chemical, microbiological and enzymatic ways were established for the study the purification of the effluent, and mechanisms implemented on target or pattern molecules belonging to the families of pollutants. AOPs, in particular Fenton and ZEA process have shown their efficiencies for the cleanup of the two effluents. The metabolism of each molecule was also studied in microorganisms and mammals. Finally, global approach contain an evaluation part, in which were tested different metabolites as methylglyoxal scavengers, entity responsible for diabetes complications.ORSAY-PARIS 11-BU Sciences (914712101) / SudocSudocFranceF

Natural hydrazine-containing compounds: Biosynthesis, isolation, biological activities and synthesis.

International audienceHydrazine, hydrazone and hydrazide derivatives are nitrogen-nitrogen bond containing compounds. Such molecules are relatively scarce in nature and have been isolated from plants, marine organisms and microorganisms. These compounds exhibit remarkable structural diversity and relevant biological activities. The enzymes involved in the formation of the N-N bond are still unknown, but many lines of evidence support the involvement of N-nitrosation and N-hydroxylation activating steps. Beside the challenging N-N bond, N-acylases catalyzing the C-N bond formation contribute to the chemical diversity of N-N-containing natural products (N2NP). This review examines the state of knowledge regarding the biosynthesis of N2NP, for which only two biosynthetic gene clusters have been investigated. Biological properties and chemical synthesis of hydrazines, hydrazones and hydrazides are also reported

Horse liver esterase catalyzed enantioselective hydrolysis of N,O-diacetyl-2-amino-1-arylethanol

N,O-Diacetyl-2-amino-1-arylethanol can be efficiently resolved by horse liver esterase (HLE). A remarkable org. co-solvent effect on the enantioselectivity of HLE was obsd. [on SciFinder (R)

Efficient Piancatelli rearrangement on a large scale using the Zippertex technology under subcritical water conditions

International audiencePiancatelli rearrangement of furyl carbinols is a relevant reaction to produce cyclopentenone derivatives. However, on large scale, Piancatelli rearrangement suffers several serious drawbacks such as long reaction period, high dilution conditions, moderate yields and the formation of dark brown polymeric materials. We described here the first use of Zippertex, an innovative technology reaching the subcritical water conditions (100-150 °C and 100 bars). In these conditions, this rearrangement proceeds smoothly to provide clean crude reaction mixtures without the formation of side-products and dark brown polymeric materials. Thus, a series of simple furyl carbinols directly obtained from bio-sourced furfural, and more challenging non-symmetrical furan-2,5-dicarbinol substrates, also obtained from bio-sourced raw material (HMF), were efficiently transformed into cyclopentenone derivatives in good yields. This technology could be applied successfully on challenging substrates substituted by an aliphatic group and also performed on 500 mmol scale.logy under subcritical water conditions

Management of hyperglycemia during and in the immediate follow-up of acute coronary syndrome

Diabetes is a serious, frequent, and insidious morbidity and mortality risk factor in patients with coronary artery disease. It has been shown that carbohydrate metabolism disorders are common in acute coronary syndromes (ACSs): 30–40% of patients have diabetes, 25–36% have an intolerance to carbohydrates, and only 30–40% have a normal carbohydrate profile. Hyperglycemia occurring either in diabetic or nondiabetic patients is strongly associated with a poor prognosis. It increases the extent of myocardial necrosis, and the risk of recurrence acute coronary syndrome and hemodynamic complications, particularly heart failure and cardiogenic shock, reflecting the importance of optimal management of glucose metabolism abnormalities. The objective of this article is to suggest a screening and management guide for carbohydrate metabolism disorders during and in the immediate follow-up of ACS in diabetic and nondiabetic patients. Screening must be systematic in any patient admitted for ACS, and based on hemoglobin A1c and oral glucose tolerance testing. Treatment of hyperglycemia in the cardiology intensive care unit is recommended in any patient admitted with hyperglycemia >1.80 g/L or postfeeding blood glucose level >1.40 g/L, and should be based on intravenous insulin with concomitant infusion of glucose solution under strict monitoring. Once the patient is no longer in intensive care, intravenous insulin therapy is no longer recommended, and the passage to a fixed insulin therapy regimen or to oral antidiabetics should be considered in consultation with diabetologists. During the rehabilitation phase, good glycemic control improves both prognosis and survival. Keywords: Diabetes, Hyperglycemia, Acute coronary syndrome, Oral antidiabetics, Intravenous insulin therap

Sporochartines A-E, A New Family of Natural Products from the Marine Fungus Hypoxylon monticulosum Isolated from a Sphaerocladina Sponge

Four new sporochartines B-E were isolated from the marine fungus Hypoxylon monticulosurn CLL-205, isolated from a sponge belonging to the Sphaerocladina order and collected in Tahiti coast. Sporochartine A (1), the first representative of this family was previously isolated from the same fungus. The structures of sporochartines B-E were elucidated using 1D and 2D NMR, HRMS and IR data. Their configurations were established according to ROE correlations and comparison with the absolute configuration of sporochartine A (1) previously obtained from X-ray analysis. Sporochartines A-D (2-4) may be derived from endo Diels-Alderase type catalysis and sporochartine E (5) from an exo Diels-Alderase catalysis. The spatial conformation of sporochartines drastically influences the results of the cytotoxic bioassay against HCT-116, PC-3, and MCF-7 human cancer cell lines

Chemoenzymic synthesis of enantiomerically pure 4-fluoro-3-nitro and 3-fluoro-4-nitro phenylalanine

Enantiomerically pure L- and D-4-fluoro-3-nitrophenylalanines and L- and D-3-fluoro-4-nitrophenylalanines were obtained from their corresponding racemates via enzymic resoln. [on SciFinder (R)