Jean-Pierre Majoral

Publications (161)709.77 Total impact

• Article: Original Multivalent Copper(II)-Conjugated Phosphorus Dendrimers and Corresponding Mononuclear Copper(II) Complexes with Antitumoral Activities.

  Nabil El Brahmi, Saïd El Kazzouli, Serge M Mignani, El Mokhtar Essassi, Geneviève Aubert, Régis Laurent, Anne-Marie Caminade, Mosto M Bousmina, Thierry Cresteil, Jean-Pierre Majoral
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  ABSTRACT: Novel multivalent copper(II)-conjugated phosphorus dendrimers and their corresponding mononuclear copper(II) complexes were synthesized, characterized, and screened for antiproliferative activity against human cancer cell lines. Selected copper ligands were grafted on the surface of phosphorus dendrimers of generation Gn (n = 1 to 3): N-(pyridin-2-ylmethylene)ethanamine for dendrimers 1Gn, N-(di(pyridin-2-yl)methylene)ethanamine for dendrimers 2Gn, and 2-(2-methylenehydrazinyl)pyridine for dendrimers 3Gn. The results indicated that the most potent derivatives are 1Gn and 1Gn-Cu versus 2Gn, 2Gn-Cu, and 3Gn, 3Gn-Cu. A direct relationship between the growth inhibitory effect and the number of terminal moieties or the amount of copper complexed to the dendrimer was observed in copper-complexed 1 series and noncomplexed 1 series. These data clearly suggested that cytotoxicity increased with the number of terminal moieties available and was boosted by the presence of complexed Cu atoms. Importantly, no cytotoxic effect was observed with CuCl2 at the same concentrations. Finally, 1G3 and 1G3-Cu have been selected for antiproliferative studies against a panel of tumor cell lines: 1G3 and 1G3-Cu demonstrated potent antiproliferative activities with IC50 values ranging 0.3-1.6 μM. Interestingly, the complexation of the terminal ligands of 1G3 dendrimers by copper(II) metal strongly increased the IC50 values in noncancer cells lines referred to as "safety" cell lines.
  Molecular Pharmaceutics 03/2013; · 4.78 Impact Factor
• Article: Low temperature synthesis of ordered mesoporous stable anatase nanocrystals: the phosphorus dendrimer approach.

  Younes Brahmi, Nadia Katir, Mykhailo Ianchuk, Vincent Collière, El Mokhtar Essassi, Armelle Ouali, Anne-Marie Caminade, Mosto Bousmina, Jean Pierre Majoral, Abdelkrim El Kadib
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  ABSTRACT: The scarcity of low temperature syntheses of anatase nanocrystals prompted us to explore the use of surface-reactive fourth generation phosphorus-dendrimers as molds to control the nucleation and growth of titanium-oxo-species during the sol-gel mineralization process. Unexpectedly, the dendritic medium provides at low temperature, discrete anatase nanocrystals (4.8 to 5.2 nm in size), in marked contrast to the routinely obtained amorphous titanium dioxide phase under standard conditions. Upon thermal treatment, heteroatom migration from the branches to the nanoparticle surface and the ring opening polymerization of the cyclophosphazene core provide stable, interpenetrating mesoporous polyphosphazene-anatase hybrid materials (-P[double bond, length as m-dash]N-)(n)-TiO(2). The steric hindrance of the dendritic skeleton, the passivation of the anatase surface by heteroatoms and the ring opening of the core limit the crystal growth of anatase to 7.4 nm and prevent, up to 800 °C, the commonly observed anatase-to-rutile phase transformation. Performing this mineralization in the presence of similar surface-reactive but non-dendritic skeletons (referred to as branch-mimicking dendrimers) failed to generate crystalline anatase and to efficiently limit the crystal growth, bringing thus clear evidence of the virtues of phosphorus dendrimers in the design of novel nanostructured materials.
  Nanoscale 02/2013; · 5.91 Impact Factor
• Article: Pyrene-Tagged Dendritic Catalysts Noncovalently Grafted onto Magnetic Co/C Nanoparticles: An Efficient and Recyclable System for Drug Synthesis.

  Michel Keller, Vincent Collière, Oliver Reiser, Anne-Marie Caminade, Jean-Pierre Majoral, Armelle Ouali
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  ABSTRACT: Hold on to your palladium! Phosphines have been grafted on magnetic Co/C nanoparticles through π-π interactions. The resulting Pd complexes showed high activity for Suzuki couplings and the system involving a dendritic ligand was recyclable, allowing the preparation of the drug Felbinac over 12 consecutive runs with minimal Pd leaching. After extraction with CH(2) Cl(2) , Felbinac met the requirements of the pharmaceutical industry (<5 ppm Pd).
  Angewandte Chemie International Edition 02/2013; · 13.45 Impact Factor
• Article: Expand classical drug administration ways by emerging routes using dendrimer drug delivery systems: A concise overview.

  Serge Mignani, Saïd El Kazzouli, Mosto Bousmina, Jean-Pierre Majoral
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  ABSTRACT: Drugs are introduced into the body by numerous routes such as enteral (oral, sublingual and rectum administration), parenteral (intravascular, intramuscular, subcutaneous and inhalation administration), or topical (skin and mucosal membranes). Each route has specific purposes, advantages and disadvantages. Today, the oral route remains the preferred one for different reasons such as ease and compliance by patients. Several nanoformulated drugs have been already approved by the FDA, such as Abelcet®, Doxil®, Abraxane® or Vivagel®(Starpharma) which is an anionic G4-poly(l-lysine)-type dendrimer showing potent topical vaginal microbicide activity. Numerous biochemical studies, as well as biological and pharmacological applications of both dendrimer based products (dendrimers as therapeutic compounds per se, like Vivagel®) and dendrimers as drug carriers (covalent conjugation or noncovalent encapsulation of drugs) were described. It is widely known that due to their outstanding physical and chemical properties, dendrimers afforded improvement of corresponding carried-drugs as dendrimer-drug complexes or conjugates (versus plain drug) such as biodistribution and pharmacokinetic behaviors. The purpose of this manuscript is to review the recent progresses of dendrimers as nanoscale drug delivery systems for the delivery of drugs using enteral, parenteral and topical routes. In particular, we focus our attention on the emerging and promising routes such as oral, transdermal, ocular and transmucosal routes using dendrimers as delivery systems.
  Advanced drug delivery reviews 02/2013; · 11.96 Impact Factor
• Article: Viologen-Phosphorus Dendrimers Inhibit α-Synuclein Fibrillation.

  Katarzyna Milowska, Justyna Grochowina, Nadia Katir, Abdelkrim El Kadib, Jean-Pierre Majoral, Maria Bryszewska, Teresa Gabryelak
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  ABSTRACT: Inhibition of α-synuclein (ASN) fibril formation is a potential therapeutic strategy in Parkinson's disease and other synucleinopathies. The aim of this study was to examine the role of viologen-phosphorus dendrimers in the α-synuclein fibrillation process and to assess the structural changes in α-synuclein under the influence of dendrimers. ASN interactions with phosphonate and pegylated surface-reactive viologen-phosphorus dendrimers were examined by measuring the zeta potential, which allowed determining the number of dendrimer molecules that bind to the ASN molecule. The fibrillation kinetics and the structural changes were examined using ThT fluorescence and CD spectroscopy. Depending on the concentration of the used dendrimer and the nature of the reactive groups located on the surface, ASN fibrillation kinetic can be significantly reduced and even, in the specific case of phosphonate dendrimers, the fibrillation can be totally inhibited at low concentrations. Presented results indicate that viologen-phosphorus dendrimers are able to inhibit ASN fibrils formation and may be used as fibrillar regulating agents in neurodegenerative disorders.
  Molecular Pharmaceutics 02/2013; · 4.78 Impact Factor
• Article: Phosphorus Dendrimers as Carriers of siRNA-Characterisation of Dendriplexes.

  Malgorzata Ferenc, Elzbieta Pedziwiatr-Werbicka, Katarzyna E Nowak, Barbara Klajnert, Jean-Pierre Majoral, Maria Bryszewska
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  ABSTRACT: There are many types of dendrimers used as nanomolecules for gene delivery but there is still an ongoing search for ones that are able to effectively deliver drugs to cells. The possibility of gene silencing using siRNA gives hope for effective treatment of numerous diseases. The aim of this work was to investigate in vitro biophysical properties of dendriplexes formed by siRNA and cationic phosphorus dendrimers of 3rd and 4th generation. First, using the ethidium bromide intercalation method, it was examined whether dendrimers have an ability to form complexes with siRNA. Next, the characterisation of dendriplexes formed at different molar ratios was carried out using biophysical methods. The effects of zeta potential, size and changes of siRNA conformation on the complexation with dendrimers were examined. It was found that both phosphorus dendrimers interacted with siRNA. The zeta potential values of dendriplexes ranged from negative to positive and the hydrodynamic diameter depended on the number of dendrimer molecules in the complex. Furthermore, using circular dichroism spectroscopy it was found that cationic phosphorus dendrimers changed only slightly the shape of siRNA CD spectra, thus they did not induce significant changes in the nucleic acid secondary structure during complex formation.
  Molecules 01/2013; 18(4):4451-4466. · 2.39 Impact Factor
• Article: Effect of viologen-phosphorus dendrimers on acetylcholinesterase and butyrylcholinesterase activities.

  Karol Ciepluch, Monika Weber, Nadia Katir, Anne-Marie Caminade, Abdelkrim El Kadib, Barbara Klajnert, Jean Pierre Majoral, Maria Bryszewska
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  ABSTRACT: The inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) is the first step in checking whether new compounds can be considered as drugs for treating neurodegenerative diseases. The effect of viologen-phosphorus dendrimers on AChE and BChE activities was studied. The results show that the effects on the cholinesterase activities depend on dendrimer type and size. Viologen dendrimers can interact with the enzymes in two ways: they can bind either to a peripheral site of the enzyme or to amino acids located near the active site, inhibiting catalysis by both cholinesterases. All tested non-toxic viologen-phosporus dendrimers inhibited the activities of both cholinesterases, showing their potential as new drugs for treating neurodegenerative diseases.
  International journal of biological macromolecules 12/2012; · 2.37 Impact Factor
• Article: From Graftable Biphotonic Chromophores to Water-Soluble Organic Nanodots for Biophotonics: The Importance of Environmental Effects.

  Cédric Rouxel, Marina Charlot, Olivier Mongin, Tathavarathy Rama Krishna, Anne-Marie Caminade, Jean-Pierre Majoral, Mireille Blanchard-Desce
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  ABSTRACT: The photophysical and two-photon absorption (TPA) properties of biphotonic chromophores with one or two phenol pendant units were studied and compared with that of a model biphotonic quadrupolar chromophore. A water-soluble dendritic structure was then synthesized by using the pendant moieties as starting points for the construction of dendritic branches. We show that the polarity of the environment significantly modulates both the fluorescence and the TPA responses of the different chromophoric derivatives. This extends to more subtle effects that involve phenol pendant moieties that were found to act as discrete solvating units and to modify both the photophysics and the TPA response of the chromophore. This demonstrates the high sensitivity of the TPA response of quadrupolar derivatives to minute alterations in the environment. Moreover, the dendritic branches were found to behave as a peculiar cybotactic environment that was able to tune the fluorescence and TPA response of the inner chromophore by creating a polar environment. This reveals a new direction for exploiting such effects by playing on the dendritic architecture (e.g., the nature and shape of the building blocks, the geometry and position of the chromophore) to modulate the TPA responses.
  Chemistry 11/2012; · 5.93 Impact Factor
• Article: Cytotoxicity and genotoxicity of cationic phosphorus-containing dendrimers.

  Paulina Gomulak, Barbara Klajnert, Maria Bryszewska, Jean Pierre Majoral, Anne Marie Caminade, Janusz Blasiak
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  ABSTRACT: Cationic phosphorus-containing dendrimers (CPDs) are a class of a highly-branched polymers with potential medical relevance. However, little is known about CPD modes of interactions with cells and its components, including DNA. In the present work we investigated cytotoxicity and genotoxicity of CPDs generation 3 and 4 (CPD G3 and CPD G4), in human mononuclear blood cells, A549 human cancer cells and human gingival fibroblasts (HGFs). CPD G3 and CPD G4 at concentrations up to 10 µM induced a concentration-dependent decrease in cell viability as assessed by flow cytometry. Both compounds did not induce breaks in isolated DNA as evaluated by the plasmid relaxation assay but they induced DNA cross-links in the cells, as examined by comet assay. CPD G3 and 4 induced slight perturbations in the cell cycle leading to a decrease in the G2/M cell population accompanied by an increase in the S cell population. Upon treatment with CPDs, the cells showed changes in their morphology, including loss of cell attachment, disruption of cell membrane and nucleus condensation. Our results indicate that CPD G3 and G4 are cytotoxic and genotoxic for assorted human cells. Therefore, CPDs may form stable complexes with DNA and interfere with cellular processes.
  Current Medicinal Chemistry 10/2012; · 4.86 Impact Factor
• Article: From Metallodrugs to Metallodendrimers for Nanotherapy in Oncology: a Concise Overview.

  Saïd El Kazzouli, Nabil El Brahmi, Serge Mignani, Mosto Bousminab, Maria Zablockac, Jean-Pierre Majoral
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  ABSTRACT: Metallodrugs (organometallic complexes) bearing at least one metal-carbon bond - represent original and powerful tools for diverse therapeutic applications based on the development of "bioorganometallic chemistry". To date, various metallodrugs were described with very interesting biological activities as antimalarials, antibacterials, neuroprotectors, against arthritis, for chemotherapy etc. Anticancer Pt-based drugs are the main complexes used in the treatment of several cancers, but unfortunately these complexes show elicit and severe toxicities and resistance effects. The remarkably unique and tunable properties of dendrimers have made them promising tools for diverse biomedical applications such as diagnostics, gene therapy and drug delivery including in oncology. Recent studies have shown that well designed dendritic carriers overcome such as poor solubility, permeability, biocompatibility, bioavailability and toxicity of the native drug. This review reports on the recent advances for the use of metallodrugs and dendritic based carriers (drug-dendrimer conjugates and drug encapsulation) in oncology. Advantages, limitations and opportunities in oncology of such materials are discussed and compared.
  Current Medicinal Chemistry 09/2012; · 4.86 Impact Factor
• Source

  Available from: Ricardo Madrid

  Article: Validation of a Generation 4 Phosphorus-Containing Polycationic Dendrimer for Gene Delivery against HIV-1.

  Verónica Briz, M Jesús Serramía, Ricardo Madrid, Aurelien Hameau, Anne-Marie Caminade, Jean Pierre Majoral, M Angeles Muñoz-Fernández
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  ABSTRACT: Gene therapy, in which oligomeric genetic material is carried into cells by nano-sized gene delivery vehicles to interfere with gene expression, represents a promising approach for preventive therapy against HIV/AIDS pandemic. Herein, we evaluate the usefulness of a phosphorus-containing dendrimer G4(NH+Et2Cl-)96 as a delivery agent of ODNs and siRNAs. G4(NH+Et2Cl-)96 formed stable complexes with ODNs or siRNAs and exhibited very low cytotoxicity in Sup T1 cells or PBMC. Functional validation was performed by using specific siRNA against HIV-1 Nef, siNEF to interfere in HIV-1 replication. G4(NH+Et2Cl-)96/siNEF dendriplex showed a high efficiency in Nef silencing. Furthermore, in vitro treatment of HIV-infected PBMC with G4(NH+Et2Cl-)96/siNEF dendriplex significantly reduced the viral replication. Our results prove the usefulness of phosphorus-containing dendrimers to deliver and transfect siRNA into CD4-T cells as a potential alternative therapy in the HIV-1 infection.
  Current Medicinal Chemistry 09/2012; · 4.86 Impact Factor
• Article: Dendritic phosphoramidite ligands for Rh-catalyzed [2+2+2] cycloaddition reactions: unprecedented enhancement of enantiodiscrimination.

  Lídia Garcia, Anna Roglans, Régis Laurent, Jean-Pierre Majoral, Anna Pla-Quintana, Anne-Marie Caminade
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  ABSTRACT: Phosphorus dendrimers containing terminal phosphoramidite ligands have been found to be highly effective and recoverable catalysts for the rhodium(I) catalyzed [2+2+2] cycloaddition reactions. A strong positive dendritic effect is observed both in the activity and enantiodiscrimination leading to axially chiral biaryl compounds.
  Chemical Communications 08/2012; 48(74):9248-50. · 6.17 Impact Factor
• Article: Organocatalysis with dendrimers.

  Anne-Marie Caminade, Armelle Ouali, Michel Keller, Jean-Pierre Majoral
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  ABSTRACT: This review gives an overview of the use of dendrimers and dendrons as organocatalysts, i.e. as catalysts in the absence of any metal. A large variety of dendrimeric structures have already been used for such a purpose, varying in size (generation), type and location (core or surface) of the organocatalytic entities, and overall chemical composition. The main types of reactions catalyzed concern bond formation (in particular C-C bonds), bond cleavage (in particular of esters), reductions and oxidations. In many cases, good to excellent enantioselectivities have been observed, in some cases associated with a positive dendritic effect (better properties when the generation of the dendrimer increases). Due to their large size compared to products, the dendrimeric organocatalysts can be often recovered and reused several times.
  Chemical Society Reviews 04/2012; 41(11):4113-25. · 28.76 Impact Factor
• Article: Gold-Containing dendrimers: A new class of macromolecules

  Oriol Rossell, Miquel Seco, Anne-Marie Caminade, Jean-Pierre Majoral
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  ABSTRACT: The synthesis of dendrimers possessing gold atoms on the surface or inside the internal layers is reported. They have been shown to be precursors to mixed gold-transition metal cluster-containing dendrimers, which represent a new class of hybrid materials. The latter species are rather soluble in common solvents and can be characterized by spectroscopic methods. Moreover, gold-containing dendrimers are useful for making gold nanoparticles, which have very interesting electronic, optical, and catalytic properties.
  Gold bulletin 04/2012; 34(3):88-94. · 3.52 Impact Factor
• Source

  Available from: Katarzyna Milowska

  Article: Phosphorus-containing dendrimers against α-synuclein fibril formation.

  Katarzyna Milowska, Teresa Gabryelak, Maria Bryszewska, Anne-Marie Caminade, Jean-Pierre Majoral
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  ABSTRACT: The aim of this work was to study the effect of phosphorus-containing dendrimers (generations G3 and G4) on the fibrillation of α-synuclein (ASN). The inhibition of fibril formation (filamentous and aggregates) is a potential therapeutic strategy for neurodegenerative disorders such as Parkinson's and other motor disorder neurodegenerative diseases. The interaction between phosphorus-containing dendrimers and ASN was studied by fluorescence spectroscopy. The decrease in the fluorescence intensity of intrisinic tyrosine was the most marked change in the fluorescence intensity observed upon addition of dendrimers. Furthermore, the effect of dendrimers on ASN fibril formation was studied using circular dichroism (CD) spectroscopy and CD studies were complemented by fluorescence assays using the dye thioflavin T (ThT). The results showed that phosphorus-containing dendrimers G3 and G4 inhibited fibril formation, when they were used in the ASN/dendrimer ratios 1:0.1 and 1:0.5. However, the higher concentrations of dendrimers did not show this effect.
  International journal of biological macromolecules 02/2012; 50(4):1138-43. · 2.37 Impact Factor
• Article: Biological properties of new viologen-phosphorus dendrimers.

  Karol Ciepluch, Nadia Katir, Abdelkrim El Kadib, Aleksandra Felczak, Katarzyna Zawadzka, Monika Weber, Barbara Klajnert, Katarzyna Lisowska, Anne-Marie Caminade, Mostapha Bousmina, Maria Bryszewska, Jean Pierre Majoral
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  ABSTRACT: Some biological properties of eight dendrimers incorporating both phosphorus linkages and viologen units within their cascade structure or at the periphery were investigated for the first time. In particular cytotoxicity, hemotoxicity, and antimicrobial and antifungal activity of these new macromolecules were examined. Even if for example all these species exhibited good antimicrobial properties, it was demonstrated that their behavior strongly depends on several parameters as their size and molecular weight, the number of viologen units and the nature of the terminal groups.
  Molecular Pharmaceutics 01/2012; 9(3):448-57. · 4.78 Impact Factor
• Article: An efficient and recyclable dendritic catalyst able to dramatically decrease palladium leaching in Suzuki couplings

  Michel Keller, Aurélien Hameau, Grégory Spataro, Sonia Ladeira, Anne-Marie Caminade, Jean-Pierre Majoral, Armelle Ouali
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  ABSTRACT: A series of novel monomeric and dendritic thiazolyl phosphines (generations 1 and 3) was prepared and the activity these ligands conferred to palladium in Suzuki couplings was evaluated. The heteroaryl ligands were revealed to be very efficient and were able to perform the reactions in mild conditions. Besides, their efficiency was compared to that of the corresponding triphenylphosphines. Moreover, the possibility to reuse both families of dendritic ligands was explored and the thiazolyl phosphine-based catalytic systems could be successfully recycled for five consecutive reactions without loss of activity, contrary to their triphenylphosphine counterparts. Remarkably, the palladium leaching was found to be dramatically reduced by using the dendrimer-supported thiazolylphosphines instead of the monomeric ligand and only trace amounts of metal (<0.55 ppm) could be found in the coupling product before any purification.
  Green Chemistry 01/2012; 2012(10):2807-2815. · 6.32 Impact Factor
• Article: Number of terminal groups versus generation of the dendrimer, which criteria influence the catalytic properties?

  Paul Servin, Regis Laurent, Hanna Dib, Luca Gonsalvi, Maurizio Peruzzini, Jean-Pierre Majoral, Anne-Marie Caminade
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  ABSTRACT: We report the synthesis of a dense dendrimer ended by the PTA ligand (1,3,5-triaza-7-phosphaadamantane), and the use of the corresponding Rh and Ru complexes for catalysis. The catalytic properties of these dendrimers are compared with those of two other dendrimers: a dendrimer of the same generation but having half the number of ligands, and a dendrimer of the next generation, but having the same number of ligands. The positive influence of the density of catalytic sites on the surface of these dendrimers for alcohol isomerization in water has been evidenced. (C) 2012 Elsevier Ltd. All rights reserved.
  Tetrahedron Letters 01/2012; 53(30):3876-3879. · 2.68 Impact Factor
• Article: Organophosphorus chemistry for the synthesis of dendrimers.

  Anne-Marie Caminade, Régis Laurent, Maria Zablocka, Jean-Pierre Majoral
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  ABSTRACT: Dendrimers are multifunctional, hyperbranched and perfectly defined macromolecules, synthesized layer after layer in an iterative manner. Besides the nature of the terminal groups responsible for most of the properties, the nature of the internal structure, and more precisely of the branching points, is also of crucial importance. For more than 15 years, we have demonstrated that the presence of phosphorus atom(s) at each branching point of the dendrimeric structure is particularly important and highly valuable for three main reasons: (i) the versatility of phosphorus chemistry that allows diversified organochemistry for the synthesis of dendrimers; (ii) the use of 31P-NMR, which is a highly valuable tool for the characterization of dendrimers; (iii) some properties (in the fields of catalysis, materials, and especially biology), that are directly connected to the nature of the internal structure and of the branching points. This review will give an overview of the methods of synthesis of phosphorus-containing dendrimers, as well on the ways to graft phosphorus derivatives as terminal groups, with emphasis on the various roles played by the chemistry of phosphorus.
  Molecules 01/2012; 17(11):13605-21. · 2.39 Impact Factor
• Article: Phosphorus dendrimers affect Alzheimer's (Aβ1-28) peptide and MAP-Tau protein aggregation.

  Tomasz Wasiak, Maksim Ionov, Krzysztof Nieznanski, Hanna Nieznanska, Oxana Klementieva, Maritxell Granell, Josep Cladera, Jean-Pierre Majoral, Anne Marie Caminade, Barbara Klajnert
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  ABSTRACT: Alzheimer's disease (AD) is characterized by pathological aggregation of β-amyloid peptides and MAP-Tau protein. β-Amyloid (Aβ) is a peptide responsible for extracellular Alzheimer's plaque formation. Intracellular MAP-Tau aggregates appear as a result of hyperphosphorylation of this cytoskeletal protein. Small, oligomeric forms of Aβ are intermediate products that appear before the amyloid plaques are formed. These forms are believed to be most neurotoxic. Dendrimers are highly branched polymers, which may find an application in regulation of amyloid fibril formation. Several biophysical and biochemical methods, like circular dichroism (CD), fluorescence intensity of thioflavin T and thioflavin S, transmission electron microscopy, spectrofluorimetry (measuring quenching of intrinsic peptide fluorescence) and MTT-cytotoxicity assay, were applied to characterize interactions of cationic phosphorus-containing dendrimers of generation 3 and generation 4 (CPDG3, CPDG4) with the fragment of amyloid peptide (Aβ(1-28)) and MAP-Tau protein. We have demonstrated that CPDs are able to affect β-amyloid and MAP-Tau aggregation processes. A neuro-2a cell line (N2a) was used to test cytotoxicity of formed fibrils and intermediate products during the Aβ(1-28) aggregation. It has been shown that CPDs might have a beneficial effect by reducing the system toxicity. Presented results suggest that phosphorus dendrimers may be used in the future as agents regulating the fibrilization processes in Alzheimer's disease.
  Molecular Pharmaceutics 12/2011; 9(3):458-69. · 4.78 Impact Factor