name	title	fuMetaTitel	body	fuDCcreator	fuDCcreatorLinks	fuDCpublisher	fuDCpublisherLocation	fuDCSizeOrDuration	fuDCdateYear	fuDCdateMonth	fuDCdateDay	fuDCsubject	fuDCrelationPartOf	fuDCrelation	fuDClanguage	fuDCsource	fuDCcontributor	fuDCtype	fuDCformat	fuDCidentifier	fuDCcoverage	fuDCrights	fuDCdescriptionDE	fuDCdescriptionEN	fuDCIdentifierBibliographicCitation	fuBild	fuDCBibtex	fuLinksZumThema
KA960	Noncharged and Charged Monodendronised Perylene Bisimides as Highly Fluorescent Labels and their Bioconjugates			"Huth, K.; Heek, T.; Achazi, K.; Kuhne, C.; Urner, L. H.; Pagel, K.; Dernedde, J.; Haag, R."		Chemistry			2017	4	6	"bioconjugates; biolabelling; fluorescent labels; ionic charge effects; perylene bisimides"				https://doi.org/10.1002/chem.201605847		journalArticle		1521-3765 (Electronic) 0947-6539 (Linking)				A series of water-soluble, hydroxylated and sulphated, polyglycerol (PG) dendronised, monofunctional perylene bisimides (PBIs) were synthesised in three generations. Their photophysical properties were determined by absorption and emission spectroscopy and their suitability as potential biolabels examined by biological in vitro studies after bioconjugation. It could be shown that the photophysical properties of the PBI labels can be improved by increasing the sterical demand and ionic charge of the attached dendron. Thereby, charged labels show superior suppression of aggregation over charge neutral labels owing to electrostatic repulsion forces on the PG-dendron. The ionic charges also enabled a reduction in dendron generation while retaining the labels' outstanding fluorescence quantum yields (FQYs) up to 100 %. These core-unsubstituted perylene derivatives were successfully applied as fluorescent labels upon bioconjugation to the therapeutic antibody cetuximab. The dye-antibody conjugates showed a strongly enhanced aggregation tendency compared to the corresponding free dyes. Biological evaluation by receptor-binding, cellular uptake, and cytotoxicity studies revealed that labelling did not affect the antibody's function, which renders the noncharged and charged dendronised PBIs suitable candidates as fluorescent labels in biological imaging.				
KA961	Fullerene Polyglycerol Amphiphiles as Unimolecular Transporters			"Donskyi, I. S.; Achazi, K.; Wycisk, V.; Licha, K.; Adeli, M.; Haag, R."		Langmuir			2017	7	5					https://doi.org/10.1021/acs.langmuir.7b00183		journalArticle		1520-5827 (Electronic) 0743-7463 (Linking)				Due to their unique structure and properties, water-soluble fullerene derivatives are of great interest for various biomedical purposes. In this work, solution behavior, encapsulation and release properties, biocompatibility, and cellular uptake pathways of fullerene-polyglycerol amphiphiles (FPAs) with defined structures are investigated. The number of polyglycerol branches attached to the surface of fullerene affects the physicochemical properties of FPAs dramatically but not their cellular uptake. Release of encapsulated hydrophobic dyes from FPAs strongly depends on the number of their branches. Conjugation of a pH-sensitive dye to the FPAs as a probe showed that their self-assemblies are taken up through endocytotic pathways. It was observed that FPAs are able to transfer small molecules into cells both above and below their critical aggregation concentration. Taking advantage of the water solubility, biocompatibility, and transfer-ability of FPAs, they might find use as unimolecular carriers for future biomedical applications.				
KA962	Highly Efficient Multivalent 2D Nanosystems for Inhibition of Orthopoxvirus Particles			"Ziem, B.; Thien, H.; Achazi, K.; Yue, C.; Stern, D.; Silberreis, K.; Gholami, M. F.; Beckert, F.; Groger, D.; Multhaup, R.; Rabe, J. P.; Nitsche, A.; Haag, R."		Adv Healthc Mater			2016	11		"Animals; Antiviral Agents/*administration & dosage/*chemistry; Carbon/administration & dosage/chemistry; dendritic polyglycerol sulfate; Glycerol/administration & dosage/chemistry; Graphite/administration & dosage/chemistry; Heparan Sulfate/administration & dosage/chemistry; heparin analogue; Nanoparticles/*administration & dosage/*chemistry; orthopoxvirus; Orthopoxvirus/*drug effects; Oxides/administration & dosage/chemistry; Polymers/administration & dosage/chemistry; Swine; thermally reduced graphene oxide; virus inhibitors"				https://doi.org/10.1002/adhm.201600812		journalArticle		2192-2659 (Electronic) 2192-2640 (Linking)				"Efficient inhibition of cell-pathogen interaction to prevent subsequent infection is an urgent but yet unsolved problem. In this study, the synthesis and functionalization of novel multivalent 2D carbon nanosystems as well as their antiviral efficacy in vitro are shown. For this reason, a new multivalent 2D flexible carbon architecture is developed in this study, functionalized with sulfated dendritic polyglycerol, to enable virus interaction. A simple ""graft from"" approach enhances the solubility of thermally reduced graphene oxide and provides a suitable 2D surface for multivalent ligand presentation. Polysulfation is used to mimic the heparan sulfate-containing surface of cells and to compete with this natural binding site of viruses. In correlation with the degree of sulfation and the grafted polymer density, the interaction efficiency of these systems can be varied. In here, orthopoxvirus strains are used as model viruses as they use heparan sulfate for cell entry as other viruses, e.g., herpes simplex virus, dengue virus, or cytomegalovirus. The characterization results of the newly designed graphene derivatives demonstrate excellent binding as well as efficient inhibition of orthopoxvirus infection. Overall, these new multivalent 2D polymer nanosystems are promising candidates to develop potent inhibitors for viruses, which possess a heparan sulfate-dependent cell entry mechanism."				
KA963	Complex Assembly of Polymer Conjugated Mesoporous Silica Nanoparticles for Intracellular pH-Responsive Drug Delivery			"Yang, Y.; Achazi, K.; Jia, Y.; Wei, Q.; Haag, R.; Li, J."		Langmuir			2016	11	29	"*Drug Delivery Systems; A549 Cells; Cross-Linking Reagents; Drug Carriers/*chemistry; Endocytosis; Fluorescent Dyes/administration & dosage/pharmacokinetics; Glycerol/chemistry; Humans; Hydrogen-Ion Concentration; Microscopy, Confocal; Microscopy, Electron, Transmission; Nanoparticles/*chemistry/ultrastructure; Nanotechnology; Neoplasms/drug therapy; Polymers/chemistry; Rhodamines/administration & dosage/pharmacokinetics; Schiff Bases/chemistry; Silicon Dioxide/chemistry; Tumor Microenvironment"				https://doi.org/10.1021/acs.langmuir.6b01845		journalArticle		1520-5827 (Electronic) 0743-7463 (Linking)				There is a great challenge in constructing pH-responsive drug delivery systems in biomedical application research. Many nanocomposites are intended to be pH-responsive as drug carriers because of a tumorous or intracellular mildly acidic environment. However, it is always difficult to find an appropriate system for quick response and release before the carrier is excreted from the living system. In this work, hyperbranched polymer, hyperbranched polyglycerol (hPG), and conjugated mesoporous silica nanoparticles (MSNs) were assembled as complexes to serve as drug carriers. Herein, the conjugated polymer-MSNs interacted through the Schiff base bond, which possessed a mildly acidic responsive property. Interestingly, the assembled system could rapidly respond and release guest molecules inside cancer cells. This would make the entrapped drug released before the carriers escape from the endosome counterpart. The results show that the assembled composite complexes can be considered to be a drug delivery system for cancer therapy.				
KA964	Responsive Contrast Agents: Synthesis and Characterization of a Tunable Series of pH-Sensitive Near-Infrared Pentamethines			"Wycisk, V.; Achazi, K.; Hillmann, P.; Hirsch, O.; Kuehne, C.; Dernedde, J.; Haag, R.; Licha, K."		ACS Omega			2016	11	30	"biological applications; cells; cyanine dyes; fluorescent-probes; growth-factor receptor; labeling reagents; lysosomal ph; mediated endocytosis; monoclonal-antibody; succinimidyl esters"				https://doi.org/10.1021/acsomega.6b00182		journalArticle		2470-1343 (Print) 2470-1343 (Electronic) 2470-1343 (Linking)				The demand for responsive dyes in optical imaging is high to achieve a better signal-to-noise ratio and, more specifically, to visualize acidic compartments of the endocytic pathway. Herein, we present a new synthetic route, with a step-by-step synthesis of water-soluble pH-sensitive cyanine dyes exhibiting pK(a) values in the region of physiological pH, as confirmed by absorption and fluorescence spectra. Moreover, modification of pK(a) values was achieved by two different substitution patterns, creating tunable pH-sensitive dyes. We demonstrated the functionality of the pH-sensitive dyes and their suitability as contrast agents for cellular uptake studies by preparing dye-labeled cetuximab and transferrin conjugates. Sulfonated head chains increased water solubility and prevented the formation of dimers, even in the context of dye-labeled bioconjugates. Confocal microscopy images of living cells revealed their pH-responsiveness, as specific fluorescence signal enhancements were observed in acidic compartments of the endocytic pathway (endosomes and lysosomes), although the background signal was low in a pH-neutral environment. Using mixtures of conjugates labeled with either a pH-sensitive or non-pH-sensitive dye for the uptake studies, we could follow the receptor binding and distinguish it from the endocytic uptake process of the conjugates in a simultaneous manner. Moreover, we used flow cytometry to quantify the fluorescence and observed a 3-fold signal enhancement for the pH-sensitive dye conjugates over a period of 3 h.				
KA965	Surface-Independent Hierarchical Coatings with Superamphiphobic Properties			"Schlaich, C.; Cuellar Camacho, L.; Yu, L.; Achazi, K.; Wei, Q.; Haag, R."		ACS Appl Mater Interfaces			2016	10	26	"hierarchical coatings; mussel-inspired adhesives; protein-resistant surfaces; self-cleaning; superamphiphobic surfaces"				https://doi.org/10.1021/acsami.6b08487		journalArticle		1944-8252 (Electronic) 1944-8244 (Linking)				Facile approaches for the fabrication of substrate independent superamphiphobic surfaces that can repel both water and organic liquids have been limited. The design of such super-repellent surfaces is still a major challenge of surface chemistry and physics. Herein, we describe a simple and efficient dip-coating approach for the fabrication of highly hierarchical surface coatings with superamphiphobic properties for a broad range of materials based on a mussel-inspired dendritic polymer (MI-dPG). The MI-dPG coating process provides a precise roughness control, and the construction of highly hierarchical structures was achieved either directly by pH-controlled aggregation or in combination with nanoparticles (NP). Moreover, the fabrication of coatings with a thickness and roughness gradient was possible via simple adjustment of the depth of the coating solution. Subsequent postmodification of these highly hierarchical structures with fluorinated molecules yielded a surface with superamphiphobic properties that successfully prevented the wetting of liquids with a low surface tension down to about 30 mN/m. The generated superamphiphobic coatings exhibit impressive repellency to water, surfactant containing solutions, and biological liquids, such as human serum, and are flexible on soft substrates.				
KA966	Chemo-Enzymatic Synthesis of Perfluoroalkyl-Functionalized Dendronized Polymers as Cyto-Compatible Nanocarriers for Drug Delivery Applications			"Parshad, B.; Kumari, M.; Achazi, K.; Bottcher, C.; Haag, R.; Sharma, S. K."		Polymers			2016	8	18	"drug encapsulation; enzymatic release; fluorinated amphiphilic polymers; nanocarriers; self-assembly"				https://doi.org/10.3390/polym8080311		journalArticle		2073-4360 (Electronic) 2073-4360 (Linking)				Among amphiphilic polymers with diverse skeletons, fluorinated architectures have attracted significant attention due to their unique property of segregation and self-assembly into discrete supramolecular entities. Herein, we have synthesized amphiphilic copolymers by grafting hydrophobic alkyl/perfluoroalkyl chains and hydrophilic polyglycerol [G2.0] dendrons onto a co-polymer scaffold, which itself was prepared by enzymatic polymerization of poly[ethylene glycol bis(carboxymethyl) ether]diethylester and 2-azidopropan-1,3-diol. The resulting fluorinated polymers and their alkyl chain analogs were then compared in terms of their supramolecular aggregation behavior, solubilization capacity, transport potential, and release profile using curcumin and dexamethasone drugs. The study of the release profile of encapsulated curcumin incubated with/without a hydrolase enzyme Candida antarctica lipase (CAL-B) suggested that the drug is better stabilized in perfluoroalkyl chain grafted polymeric nanostructures in the absence of enzyme for up to 12 days as compared to its alkyl chain analogs. Although both the fluorinated as well as non-fluorinated systems showed up to 90% release of curcumin in 12 days when incubated with lipase, a comparatively faster release was observed in the fluorinated polymers. Cell viability of HeLa cells up to 95% in aqueous solution of fluorinated polymers (100 mug/mL) demonstrated their excellent cyto-compatibility.				
KA967	Synthesis, Photophysical, and Biological Evaluation of Sulfated Polyglycerol Dendronized Perylenebisimides (PBIs)--A Promising Platform for Anti-Inflammatory Theranostic Agents?			"Heek, T.; Kuhne, C.; Depner, H.; Achazi, K.; Dernedde, J.; Haag, R."		Bioconjug Chem			2016	3	16	"*Theranostic Nanomedicine; Anti-Inflammatory Agents/*therapeutic use; Glycerol/*chemistry; Imides/*chemistry; Perylene/*analogs & derivatives/chemistry; Polymers/*chemistry; Sulfates/*chemistry"				https://doi.org/10.1021/acs.bioconjchem.5b00683		journalArticle		1520-4812 (Electronic) 1043-1802 (Linking)				A set of four water-soluble perylene bisimides (PBI) based on sulfated polyglycerol (PGS) dendrons were developed, their photophysical properties determined via UV/vis and fluorescence spectroscopy, and their performance as possible anti-inflammatory agents evaluated via biological in vitro studies. It could be shown that in contrast to charge neutral PG-PBIs the introduction of the additional electrostatic repulsion forces leads to a decrease in the dendron generation necessary for aggregation suppression, allowing the preparation of PBIs with fluorescence quantum yields of >95% with a considerable decreased synthetic effort. Furthermore, the values determined for L-selectin binding down to the nanomolar range, their limited impact on blood coagulation, and their minor activation of the complement system renders these systems ideal for anti-inflammatory purposes.				
KA968	Synthesis, self-assembly, and photocrosslinking of fullerene-polyglycerol amphiphiles as nanocarriers with controlled transport properties			"Donskyi, I.; Achazi, K.; Wycisk, V.; Bottcher, C.; Adeli, M."		Chem Commun (Camb)			2016	3	21	"*Drug Carriers; *Nanostructures; Fullerenes/*chemistry; Glycerol/*chemistry; Microscopy, Electron, Scanning; Polymers/*chemistry; Spectrophotometry, Ultraviolet"				https://doi.org/10.1039/c5cc08369a		journalArticle		1364-548X (Electronic) 1359-7345 (Linking)				In this work, we report a new, simple, gram-scale method for synthesizing water-soluble fullerene-polyglycerol amphiphiles (FPAs) that self-assemble into partially and fully crosslinked nanoclusters with the ability to controllably transport hydrophobic and hydrophilic agents.				
KA969	Boronate cross-linked ATP- and pH-responsive nanogels for intracellular delivery of anticancer drugs			"Zhang, X.; Achazi, K.; Haag, R."		Adv Healthc Mater			2015	3	11	"*Drug Delivery Systems; Adenosine Triphosphate/*chemistry; Antineoplastic Agents/*pharmacology; ATP-responsiveness; Boronic Acids/*chemistry; Cell Death/drug effects; Chemical Precipitation; Cross-Linking Reagents/*chemistry; Dynamic Light Scattering; Endocytosis/drug effects; Endosomes/drug effects/metabolism; HeLa Cells; Humans; Hydrogen-Ion Concentration; Intracellular Space/*metabolism; Lysosomes/drug effects/metabolism; MCF-7 Cells; Methotrexate/pharmacology; Nanogels; organelle permeation; Particle Size; Permeability/drug effects; pH degradation; Polyethylene Glycols/*chemistry/toxicity; Polyethyleneimine/*chemistry/toxicity; polyglycerol nanogels"				https://doi.org/10.1002/adhm.201400550		journalArticle		2192-2659 (Electronic) 2192-2640 (Linking)				A novel adenosine-5'-triphosphate (ATP) and pH dual-responsive degradable nanogel (NG) system are developed based on the complexation of 1,2-diols in dendritic polyglycerol (dPG), and boronic acids, which are conjugated with dPG as the macromolecular cross-linker. The NG is formed by a mild and surfactant-free inverse nanoprecipitation method. An anticancer drug, methotrexate (MTX), is coprecipitated with the macromolecular precursors and cross-linkers to form MTX-loaded NG (NG-MTX) with a loading capacity of 13 wt%. The size of NG is controllable from 100 to 300 nm, which is suitable for the enhanced permeation and retention (EPR) effect and can be degraded into small fragments that are within the clearance limitation in the presence of 5 x 10(-3) m ATP or at pH 4 after 24 h. Increasing ATP concentrations and decreasing pH values of the release medium accelerate the release of MTX. Both the real-time cell analysis (RTCA) and MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) results show no cytotoxic effect of NG and a dose-dependent effect of NG-MTX on HeLa cells as well as MCF-7 cells. The fluorescein isothiocyanate (FITC)-labeled NG (FITC-NG) exhibits a time-dependent intracellular uptake tendency and cell organelle permeability as determined by confocal laser scanning microscopy (CLSM) or flow cytometry.