Biflavones of Decussocarpus rospigliosii as Phosphodiesterases Inhibitors
University of Strasbourg, Strasburg, Alsace, France Planta Medica
(Impact Factor: 2.15).
11/2007; 73(12):1284-6. DOI: 10.1055/s-2007-990218
A phytochemical study of an ethyl acetate extract of Decussocarpus rospigliosii leaves led to the isolation of six 3'-8''-biapigenin derivatives identified as amentoflavone (1), podocarpusflavone A (2), sequoiaflavone (3), podocarpusflavone B (4), 7,7''-di-O-methylamentoflavone (5) and heveaflavone (6). Biflavones 1-4 showed strong inhibitory activity on several PDE isoforms. Biflavone (5) showed selective and potent inhibition of the PDE4 isoform (IC50=1.48+/-0.21 microM) and was almost as active as the reference drug Rolipram (IC50=1.1+/-0.2 microM).
Available from: Gustavo P. Amarante-Mendes
- "Some of the pharmacological properties attributed to biflavonoids include antiviral, anti-inflammatory, antimicrobial and anti-cancer activities (Mkounga et al., 2009; Pang et al., 2009). Biflavonoids are also known as cyclic nucleotide phosphodiesterase inhibitors (Chaabi et al., 2007; Harborne, 1986). "
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ABSTRACT: The leaves of the Cashew plant (Anacardium occidentale L.) are used by the folk medicine in South America and West Africa. This plant is rich in flavonoids, which are polyphenolic compounds widespread in plants, and that have diverse physiological effects. In a sub-acute toxicity assay it was found that an ethanolic extract of Cashew leaves elicited lymphopenia in rats. The extract was also found to be cytotoxic and to induce apoptosis in Jurkat (acute lymphoblastic leukemia) cells. The crude ethanolic extract was fractionated and resolved by HPLC. One of the four fractions obtained led to the isolation of the biflavonoid agasthisflavone. [(3)H]-thymidine incorporation assays and flow cytometry analysis showed that the isolated compound displayed a high anti-proliferative effect in Jurkat cells with an IC(50) of 2.4 μg/ml (4.45 μM). The effect of agathisflavone on the acute promyelocytic leukemia cell line HL60, Burkitt lymphoma Raji cells and Hep-2 laryngeal carcinoma cells was also tested. The two latter ones were only mildly affected by agathisflavone. It is also shown that agathisflavone induces apoptosis in Jurkat cells and it this proposed that this is the likely mechanism of agathisflavone specific cytotoxicity.
Experimental and toxicologic pathology: official journal of the Gesellschaft fur Toxikologische Pathologie 11/2010; 64(5):435-40. DOI:10.1016/j.etp.2010.10.010 · 1.86 Impact Factor
Drug Discovery Today Disease Mechanisms 06/2008; 5(2). DOI:10.1016/j.ddmec.2008.08.001
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ABSTRACT: The present work describes the phytochemical investigation of the aerial parts of Amanoa almerindae Leal (Euphorbiaceae). After fractionation of the organic extracts, four pentacyclic triterpenes (friedelin, lupeol, betulin, betulinic acid), three steroids (β-sitosterol, sitostenone, daucosterol), a lignan (49-demethyl- deoxypodophyllotoxin) and for first time in this genus the presence of the biflavones amentoflavone, sequoiaflavone, and putraflavone were identified. The structures of isolated compounds were established by spectroscopic methods and confirmed by comparison with reference samples and literature data. No previous phytochemical study of Amanoa almerindae has been reported, and to the best of our knowledge, this is the first report of biflavonoids in the Amanoa genus.
Pharmaceutical Biology 05/2009; 47(6):496-499. DOI:10.1080/13880200902838717 · 1.24 Impact Factor
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