Antiproliferative activity of a new xanthone derivative from leaves of Garcinia nobilis Engl.

A new xanthone, mboudiexanthone (1), together with five known compounds, euxanthone (2), isogarcinol (3), garcinol (4), betulinic acid (5) and zeorin (6) were isolated from the leaves of Garcinia nobilis Engl. The structures were determined by 1D and 2D NMR techniques and X-ray diffraction for 6. The in vitro antiproliferative properties of isolated compounds were evaluated against the human breast cancer cell line MCF-7. All compounds showed an antiproliferative activity with an IC50 value down to ∼11 µM for isogarcinol.SCOPUS: ar.jinfo:eu-repo/semantics/publishe

Antileishmanial Activity of Dimeric Flavonoids Isolated from <i>Arrabidaea brachypoda</i>

Leishmaniasis are diseases caused by parasites belonging to Leishmania genus. The treatment with pentavalent antimonials present high toxicity. Secondary line drugs, such as amphotericin B and miltefosine also have a narrow therapeutic index. Therefore, there is an urgent need to develop new drugs to treat leishmaniasis. Here, we present the in vitro anti-leishmanial activity of unusual dimeric flavonoids purified from Arrabidaea brachypoda. Three compounds were tested against Leishmana sp. Compound 2 was the most active against promastigotes. Quantifying the in vitro infected macrophages revealed that compound 2 was also the most active against intracellular amastigotes of L. amazonensis, without displaying host cell toxicity. Drug combinations presented an additive effect, suggesting the absence of interaction between amphotericin B and compound 2. Amastigotes treated with compound 2 demonstrated alterations in the Golgi and accumulation of vesicles inside the flagellar pocket. Compound 2-treated amastigotes presented a high accumulation of cytoplasmic vesicles and a myelin-like structure. When administered in L. amazonensis-infected mice, neither the oral nor the topical treatments were effective against the parasite. Based on the high in vitro activity, dimeric flavonoids can be used as a lead structure for the development of new molecules that could be useful for structure-active studies against Leishmania

MOESM1 of Gd-nanoparticles functionalization with specific peptides for ß-amyloid plaques targeting

Additional file 1: Figure S1. Characterization of functionalized nanoparticles. Figure S2. Zeta potential versus pH of AGuIX (black) and AGuIX@PEG (red). Figure S3. Reaction scheme for the synthesis of AGuIX@PEG@[email protected]. Figure S4. Chromatograms obtained with at UV-Visible absorption at λ =295 nm of the AGuIX@PEG, AGuIX@PEG@LPFFD and AGuIX@PEG@KLVFF . Elementary Analyses of grafted nanoparticles: Table S1. Molar ratio deduced from experimental weight percentage; Table S2. Elementary analyses given in weight percent of element in the compound; Table S3. Comparison of the primary amine content evaluated by elementary analysis and TNBS assays. These results allow assessing the molecular formula obtained by elementary analysis. Figure S5. Standard curves of amine quantification in APTES/TEOS equimolar mixture by TNBS assays. Figure S6. The cyanine 5.5 presents characteristic absorption and emission wavelength λexc max Cy5.5 = 675 nm and λem max Cy5.5 = 692 nm. Table S4. The yield of the grafting was calculated thanks to the comparison of the cyanine fluorescence and the DOTA(Gd3+) chelate before and after removal of the ungrafted dye by tangential purification. Figure S7. Effect of nanoparticles on cell viability. Figure S8. PIB derivative synthesis details. Figure S9. Control of the non-binding of Cy5.5 dye to amyloid plaque in brain section of AD mouse model