- PH-responsive dendritic core-multishell nanocarriers
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In this paper we describe novel pH-responsive core-multishell (CMS) nanocarrier (pH-CMS), obtained by introducing an aromatic imine linker between the shell and the core. At a pH of 5 and lower the used imine linker was rapidly cleaved as demonstrated by NMR studies. The CMS nanocarriers were loaded with the dye Nile red (NR) and the anticancer drug doxorubicin (DOX), respectively. The transport capacities were determined using UV/Vis spectroscopy, and the sizes of the loaded and unloaded CMS nanocarriers were investigated using dynamic light scattering (DLS). We could show that CMS nanocarriers efficiently transported NR in supramolecular aggregates, while DOX was transported in a unimolecular fashion. After cellular uptake the DOX-loaded pH-responsive nanocarriers showed higher toxicities than the stable CMS nanocarriers. This is due to a more efficient DOX release caused by the cleavage of the pH-labile imine bond at lower pH within the intracellular compartments.
- Fleige, Emanuel,Achazi, Katharina,Schaletzki, Karolina,Triemer, Therese,Haag, Rainer
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- Preparation method of octadecanedioic acid (by machine translation)
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The method has the advantages that raw materials are cheap and easily available, and 9 - McMMMMMurry Coupling forms a coupling intermediate; and then, the method is cheap and easily available in raw materials, simple in post-treatment steps, and capable of greatly reducing production cost and selling price of octadecanedioic acid. (by machine translation)
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- Cysteine-Targeted Insecticides against A. gambiae Acetylcholinesterase Are Neither Selective nor Reversible Inhibitors
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Acetylcholinesterase cysteine-targeted insecticides against malaria vector Anopheles gambia and other mosquitos have already been introduced. We have applied the olefin metathesis for the preparation of cysteine-targeted insecticides in high yields. The prepared compounds with either a succinimide or maleimide moiety were evaluated on Anopheles gambiae and human acetylcholinesterase with relatively high irreversible inhibition of both enzymes but poor selectivity. The concept of cysteine binding was not proved by several methods, and poor stability was observed of the chosen most potent/selective compounds in a water/buffer environment. Thus, our findings do not support the proposed concept of cysteine-targeted selective insecticides for the prepared series of succinimide or maleimide compounds.
- Gorecki, Lukas,Andrys, Rudolf,Schmidt, Monika,Kucera, Tomas,Psotka, Miroslav,Svobodova, Barbora,Hrabcova, Veronika,Hepnarova, Vendula,Bzonek, Petr,Jun, Daniel,Kuca, Kamil,Korabecny, Jan,Musilek, Kamil
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supporting information
p. 65 - 71
(2019/12/25)
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- Metathesis of renewable polyene feedstocks – Indirect evidences of the formation of catalytically active ruthenium allylidene species
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Cross-metathesis (CM) of conjugated polyenes, such as 1,6-diphenyl-1,3,5-hexatriene (1) and α-eleostearic acid methyl ester (2) with several olefins, including 1-hexene, dimethyl maleate and cis-stilbene as model compounds has been carried out using (1,3-bis-(2,4,6-trimethylphenyl)-2-imidazolidinylidene)-dichloro(o-isopropoxyphenylmethylene)ruthenium (Hoveyda-Grubbs 2nd generation, HG2) catalyst. The feasibility of these reactions is demonstrated by the observed high conversions and reasonable yields. Thus, regardless of the relatively low electron density, =CH–CH= conjugated units of molecules, including compound 2 as a sustainable, non-foodstuff source, can be utilized as building blocks for the synthesis of various value-added chemicals via olefin metathesis. DFT-studies and the product spectrum of the self-metathesis of 1,6-diphenyl-1,3,5-hexatriene suggest that a Ru η1-allylidene complex is the active species in the reaction.
- Kovács, Ervin,Sághy, Péter,Turczel, Gábor,Tóth, Imre,Lendvay, Gy?rgy,Domján, Attila,Anastas, Paul T.,Tuba, Róbert
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supporting information
p. 213 - 217
(2017/09/12)
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- Direct interaction, instrumental for signaling processes, between LacCer and Lyn in the lipid rafts of neutrophil-like cells
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Lactosylceramide [LacCer; β-Gal-(1-4)-β-Glc-(1-1)-Cer] has been shown to contain very long fatty acids that specifically modulate neutrophil properties. The interactions between LacCer and proteins and their role in cell signaling processes were assessed
- Chiricozzi, Elena,Ciampa, Maria Grazia,Brasile, Giuseppina,Compostella, Federica,Prinetti, Alessandro,Nakayama, Hitoshi,Ekyalongo, Roudy C.,Iwabuchi, Kazuhisa,Sonnino, Sandro,Mauri, Laura
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p. 129 - 141
(2015/03/05)
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- Methyl ricinoleate as platform chemical for simultaneous production of fine chemicals and polymer precursors
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The modification of methyl ricinoleate by etherification of the hydroxyl group was accomplished by using a nonclassical ruthenium-catalyzed allylation reaction and also by esterification. Methyl ricinoleate derivatives were engaged in ring-closing metathesis (RCM) reactions leading to biosourced 3,6-dihydropyran and α,β-unsaturated lactone derivatives with concomitant production of polymer precursors. Sequential RCM/hydrogenation and RCM/cross-metathesis were also implemented as a straightforward method for the synthesis of tetrahydropyran and lactone derivatives as well as valuable monomers (i.e., polyamide precursors).
- Dupe, Antoine,Achard, Mathieu,Fischmeister, Cedric,Bruneau, Christian
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p. 2249 - 2254
(2013/01/15)
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- Dynamic assessment of bilayer thickness by varying phospholipid and hydraphile synthetic channel chain lengths
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A library of "hydraphile" synthetic ion channel analogues that differ in overall length from ~28-58 A has been prepared. A new and convenient ion-selective electrode (ISE) method was used to assay Na+ release. Liposomes were formed from three d
- Weber, Michelle E.,Schlesinger, Paul H.,Gokel, George W.
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p. 636 - 642
(2007/10/03)
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- Pyridinecarboxamide derivatives
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Pyridinecarboxamide derivatives of the formula STR1 (wherein n represents an integer of 14-18, and R represents a hydrogen atom or a straight or branched C1 -C4 alkyl group) or physiologically acceptable salts thereof. The compounds have excellent inhibiting activity of cerebral edema, especially ischemic cerebral edema, and inhibiting activity of delayed death of neuronal cells (an inhibiting activity of Ca-influx in neuronal cells). Cerebral edema is a pathologic condition accompanying cerebrovascular disorders, especially the acute stage of cerebrovascular disorders and then the compounds are useful as an agent for inhibiting cerebral edema or a therapeutic agent for cerebrovascular disorders. Moreover, the compounds have no hypotensive action which is considered to be side-effect in treating the acute stage cerebrovascular disorders and hardly show a behavior suppressing action so that they are an excellent therapeutic agent for, in particular, the acute stage cerebrovascular disorders. Moreover, the compounds show a cerebral protective activity (an anti-anoxic activity), an increasing activity of cerebral blood flow, and an inhibiting activity of lipid peroxidation and these activities may lead to the increased utility as a therapeutic agent for cerebrovascular disorders.
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- PREPARATION OF TERMINAL ALKENIC ESTERS BY AN OXIDATIVE RADICAL REACTION
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A general method is described for the conversion of (mono)alkenic esters with the double bond at the nth C atom to terminal alkenic esters of (n-1) C atoms in length, with the double bond at n-2.Ozonolysis, either in methanol or in light petroleum, is followed by reaction with a mixture of ferrous and cupric salts.Methyl 10-undecenoate, methyl oleate (methyl (Z)-9-octadecenoate) and methyl erucate (methyl (Z)-13-docosenoate) were converted to methyl 8-nonenoate, methyl 7-ocotenoate and methyl 11-dodecenoate respectively.An improved preparation of 5-hexenoic acid is also described.
- Cardinale, G.,Laan, J. A. M.,Ward, J. P.
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p. 2899 - 2902
(2007/10/02)
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- Bifunctional compounds from reaction of alkoxy hydroperoxides with metal salts
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Alkoxy hydroperoxides, obtained by ozonizing olefins in alcoholic solution, were treated with ferrous sulfate. C-C bond scission and radical formation was followed by dimerization of the radicals formed. Ozonides reacted similarly. Acyclic and cyclic olefins, including a cyclic enol ether, gave rise to a range of α,ω-disubstituted products in modest yields. By using ferric chloride, ω-chloro esters were obtained from the alkoxy hydroperoxides derived from olefinic esters.
- Cardinale,Laan,Van Der Steen,Ward
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p. 6051 - 6054
(2007/10/02)
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