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119 results on '"Figadere, B."'

2. Acetogenins from Annonaceae

Author

Cavé, A., Figadère, B., Laurens, A., Cortes, D., Cavé, A., Cortes, D., Figadère, B., Laurens, A., Pettit, G. R., Herz, W., editor, Kirby, G. W., editor, Moore, R. E., editor, Steglich, W., editor, and Tamm, Ch., editor

Published
1997
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3. Synthesis and biological studies of 'Polycerasoidol' and 'trans-delta-Tocotrienolic acid' derivatives as PPARalpha and/or PPARgamma agonists

Author

Vila L, Cabedo N, Villarroel-Vicente C, Garcia A, Bernabeu A, Hennuyer N, Staels B, Franck X, Figadere B, Sanz M, and Cortes D

Abstract

2-Prenylated benzopyrans represent a class of natural and synthetic compounds showing a wide range of significant activities. Polycerasoidol is a natural prenylated benzopyran isolated from the stem bark of Polyalthia cerasoides (Annonaceae) that exhibits dual PPARalpha/gamma agonism and an anti-inflammatory effect by inhibiting mononuclear leukocyte adhesion to the dysfunctional endothelium. Herein, we report the synthesis of three new series of prenylated benzopyrans containing one (series 1), two (series 2, "polycerasoidol" analogs) and three (series 3, "trans-delta-tocotrienolic acid" analogs) isoprenoid units in the hydrocarbon side chain at the 2-position of the chroman-6-ol (6-hydroxy-dihydrobenzopyran) scaffold. Isoprenoid moieties were introduced through a Grignard reaction sequence, followed by Johnson-Claisen rearrangement and subsequent Wittig olefination. hPPAR transactivation activity and the structure activity relationships (SAR) of eleven novel synthesized 2-prenylated benzopyrans were explored. PPAR transactivation activity demonstrated that the seven-carbon side chain analogs (series 1) displayed selectivity for hPPARalpha, while the nine-carbon side chain analogs (polycerasoidol analogs, series 2) did so for hPPARgamma. The side chain elongation to 11 or 13 carbons (series 3) resulted in weak dual PPARalpha/gamma activation. Therefore, 2-prenylated benzopyrans of seven- and nine-carbon side chain (polycerasoidol analogs) are good lead compounds for developing useful candidates to prevent cardiovascular diseases associated with metabolic disorders. Copyright © 2021 Elsevier Ltd. All rights reserved.

Published
2022

4. Synthesis of 2-Prenylated Alkoxylated Benzopyrans by Horner- Wadsworth-Emmons Olefination with PPAR alpha/gamma Agonist Activity

Author

Garcia A, Vila L, Marin P, Bernabeu A, Villarroel-Vicente C, Hennuyer N, Staels B, Franck X, Figadere B, Cabedo N, and Cortes D

Subjects
PPAR alpha/gamma activity, Prenylated benzopyrans, Horner-Wadsworth-Emmons reaction
Abstract

We have synthesized series of 2-prenylated benzopyrans as analogues of the natural polycerasoidol, a dual PPAR alpha/gamma agonist with anti-inflammatory effects. The prenylated side chain consists of five or nine carbons with an alpha-alkoxy-alpha,beta-unsaturated ester moiety. Prenylation was introduced via the Grignard reaction, followed by Johnson-Claisen rearrangement, and the alpha-alkoxy-alpha,beta-unsaturated ester moiety was introduced by the Horner-Wadsworth-Emmons reaction. Synthetic derivatives showed high efficacy to activate both hPPAR alpha and hPPAR gamma as dual PPAR alpha/gamma agonists. These prenylated benzopyrans emerge as lead compounds potentially useful for preventing cardiometabolic diseases.

Published
2021

8. High-resolution bioguided screening of Ganoderma capense for P-GP modulating activity

Author

Ta, Hp, Maciuk, A., Vautier, S., Milane, A., Welti, S., Champy, P., Wainer, I.W., Fernandez, C., Figadere, B., Ta, Hp, Maciuk, A., Vautier, S., Milane, A., Welti, S., Champy, P., Wainer, I.W., Fernandez, C., and Figadere, B.

Abstract

Ganoderma lucidum (Polyporaceae) is commonly used as a panacea e.g. in Traditional Chinese Medicine. Abundant research has shown its activity on several targets related to cancer, but no work assessed its modulating activity on P-gp transporter. We extracted metabolites from a clearly defined cultivated strain using petroleum ether, dichloromethane, acetonitrile, methanol and water. Water fraction was added ethanol to precipitate polysaccharides and separate them from supernatant. The 6 resulting fractions have been tested using three different cellular uptake-efflux tests (calceine, rhodamine and 3H- digoxine) in a 96-well format, using rat brain endothelium cells expressing P-gp exclusively. A systematic approach using multiple controls allowed us to record unequivocal data and gave evidence for the special procedure requirements for testing P-gp modulating activity of natural extracts. Triterpenes from the active dichloromethane fraction were isolated using a semi-preparative column and LC-MS monitoring. Compounds were tested at normalized doses, based on peaks areas detected by ELSD detection. Data are presented along with a literature review on P-gp modulating activity of plant triterpenes. Results give a rationale for the use of Ganoderma lucidum in the treatment of cancer and indicate potential pharmacokinetic interaction or potentiation of Ganoderma lucidum with other drug treatments.

Published
2019

9. Bioelectrochemical monitoring of soluble guanylate cyclase inhibition by the natural beta-carboline canthin-6-one

Author

Domenech-Carbo, A, Rodrigo, R, Marechal, JD, Poupon, E, Fournet, A, Figadere, B, and Cebrian-Torrejon, G

Subjects
ACTIVATION, inorganic chemicals, NITRIC-OXIDE, IDENTIFICATION, ALKALOIDS, BINDING, PROTEIN-LIGAND DOCKING, heterocyclic compounds, DEACTIVATION, NO, AFFINITY, ELECTROCHEMISTRY
Abstract

The inhibition of soluble guanylate cyclase (sGC) by canthin-6-one alkaloid (L1) is presented and the mechanism of deactivation is studied using solution phase and voltammetry of microparticles methodologies. Possible inhibition pathways: oxidation of Fe2+ to Fe3+ coupled to reduction of the naphthyridone motif present by the canthin-6-one and coordinating or reacting of L1 with cysteine units of sGC, are balanced. (C) 2016 Elsevier B.V. All rights reserved.

Published
2017

11. dsDNA, ssDNA, G-quadruplex DNA, and nucleosomal DNA electrochemical screening using canthin-6-one alkaloid-modified electrodes

Author

Domenech-Carbo, A, Cebrian-Torrejon, G, de Miguel, L, Tordera, V, Rodrigues-Furtado, D, Assad-Kahn, S, Fournet, A, Figadere, B, Vazquez-Manrique, RP, and Poupon, E

Subjects
G-quadruplex-DNA, Natural products, Voltammetry of microparticles, DNA screening, Canthin-6-one
Abstract

Microparticulate films of a canthin-6-one alkaloid (L), a natural beta-carboline alkaloid presenting a characteristic naphtyridone motif, on glassy carbon electrodes yield different, separate voltammetric signals for dsDNA, ssDNA, G-quadruplex DNA, different degrees of DNA methylation and the biomimetic nucleosomal DNA with detection limit of 10(-5) M. This multiple-signal electrochemical behavior is in contrast with conventional use of DNA intercalators, only discriminating between different DNA forms by variations in the intensity of a unique signal. Complementary photochemical and scanning electrochemical microscopy (SECM) data suggest that the differences in the voltammetric response of the different DNA forms derive from the intercalating properties of the canthin-6-one. (C) 2013 Elsevier Ltd. All rights reserved.

Published
2014

12. Detection, characterization, and screening of heme-binding molecules by mass spectrometry for malaria drug discovery

Author

Munoz-Durango, K., Maciuk, A., Harfouche, A., Torijano-Gutierrez, S., Jullian, J.C., Quintin, J., Spelman, K., Mouray, E., Grellier, P., Figadere, B., Munoz-Durango, K., Maciuk, A., Harfouche, A., Torijano-Gutierrez, S., Jullian, J.C., Quintin, J., Spelman, K., Mouray, E., Grellier, P., and Figadere, B.

Abstract

Contains fulltext : 110844.pdf (publisher's version ) (Open Access), Drug screening for antimalarials uses heme biocrystallization inhibition methods as an alternative to parasite cultures, but they involve complex processes and cannot detect artemisinin-like molecules. The described method detects heme-binding compounds by mass spectrometry, using dissociation of the drug-heme adducts to evaluate putative antiplasmodial activity. Applied to a chemical library, it showed a good hit-to-lead ratio and is an efficient early stage screening for complex mixtures like natural extracts.

Published
2012

50. Synthesis, Spectroscopy, and Cytotoxicity of Glycosylated Acetogenin Derivatives as Promising Molecules for Cancer Therapy<SUP>1</SUP><BBR RID="jm990568mb00001">

Author

Queiroz, E. F., Roblot, F., Duret, P., Figadere, B., Gouyette, A., Laprevote, O., Serani, L., and Hocquemiller, R.

Abstract

Several glycosyl derivatives of squamocin (1) have been synthesized by glycosylation under Lewis acid catalysis with two different 1-O-acetyl sugars. Separation of these compounds has been achieved by HPLC and centrifugal partition chromatography (CPC). A detailed NMR, ESIMS, and LSIMS study allowed complete structural elucidations. The cytotoxic activity of the glycosyl derivatives was investigated and compared with that of squamocin and dihydrosquamocin against human epidermoid carcinoma cells (KB), African green monkey (Cercopithecus aethiops) kidney epithelial cells (VERO), and mouse lymphocytic leukemia cells (L1210). The antiproliferative effects of some derivatives were studied on cell cycles in mouse lymphocytic leukemia cells (L1210).

Published
2000

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