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  1. Article ; Online: Preliminary Evaluation of Iron Oxide Nanoparticles Radiolabeled with 68 Ga and 177 Lu as Potential Theranostic Agents

    Evangelia-Alexandra Salvanou / Argiris Kolokithas-Ntoukas / Christos Liolios / Stavros Xanthopoulos / Maria Paravatou-Petsotas / Charalampos Tsoukalas / Konstantinos Avgoustakis / Penelope Bouziotis

    Nanomaterials, Vol 12, Iss 14, p

    2022  Volume 2490

    Abstract: Theranostic radioisotope pairs such as Gallium-68 ( 68 Ga) for Positron Emission Tomography (PET) and Lutetium-177 ( 177 Lu) for radioisotopic therapy, in conjunction with nanoparticles (NPs), are an emerging field in the treatment of cancer. The present ...

    Abstract Theranostic radioisotope pairs such as Gallium-68 ( 68 Ga) for Positron Emission Tomography (PET) and Lutetium-177 ( 177 Lu) for radioisotopic therapy, in conjunction with nanoparticles (NPs), are an emerging field in the treatment of cancer. The present work aims to demonstrate the ability of condensed colloidal nanocrystal clusters (co-CNCs) comprised of iron oxide nanoparticles, coated with alginic acid (MA) and stabilized by a layer of polyethylene glycol (MAPEG) to be directly radiolabeled with 68 Ga and its therapeutic analog 177 Lu. 68 Ga/ 177 Lu- MA and MAPEG were investigated for their in vitro stability. The biocompatibility of the non-radiolabeled nanoparticles, as well as the cytotoxicity of MA, MAPEG, and [ 177 Lu]Lu-MAPEG were assessed on 4T1 cells. Finally, the ex vivo biodistribution of the 68 Ga-labeled NPs as well as [ 177 Lu]Lu-MAPEG was investigated in normal mice. Radiolabeling with both radioisotopes took place via a simple and direct labelling method without further purification. Hemocompatibility was verified for both NPs, while MTT studies demonstrated the non-cytotoxic profile of the nanocarriers and the dose-dependent toxicity for [ 177 Lu]Lu-MAPEG. The radiolabeled nanoparticles mainly accumulated in RES organs. Based on our preliminary results, we conclude that MAPEG could be further investigated as a theranostic agent for PET diagnosis and therapy of cancer.
    Keywords Gallium-68 ; Lutetium-177 ; iron oxide nanoparticles ; condensed clusters ; MTT ; radiolabeling ; Chemistry ; QD1-999
    Subject code 333
    Language English
    Publishing date 2022-07-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  2. Article ; Online: Amantadine variant – aryl conjugates that inhibit multiple M2 mutant – amantadine resistant influenza a viruses

    Christina Tzitzoglaki / Anja Hoffmann / Andreea L. Turcu / Patrick Schmerer / Chunlong Ma / George Laros / Christos Liolios / Brea José / Jun Wang / Santiago Vázquez / Michaela Schmidtke / Antonios Kolocouris

    European Journal of Medicinal Chemistry Reports, Vol 6, Iss , Pp 100083- (2022)

    2022  

    Abstract: Influenza A viruses can cause a serious future threat due to frequent mutations. Amantadine and rimantadine drugs inhibit influenza A M2 wild-type (WT; bearing in the protein M2 proton channel serine at position-31) viruses by binding and blocking M2 WT ... ...

    Abstract Influenza A viruses can cause a serious future threat due to frequent mutations. Amantadine and rimantadine drugs inhibit influenza A M2 wild-type (WT; bearing in the protein M2 proton channel serine at position-31) viruses by binding and blocking M2 WT channel-mediated proton current. The resistant to these drugs influenza A viruses bearing the S31N mutant in the M2 proton channel can be inhibited by amantadine – aryl conjugates, in which amantadine and an aryl group are linked through a methylene, which block M2 S31N channel-mediated proton current. However, the M2 amantadine/rimantadine resistant viruses bearing one of the four mutations L26F, V27A, A30T, G34E in residues that line the M2 channel pore pose an additional concern for public health.Here, we designed 33 compounds based on the structure of three previously published and potent amantadine-aryl conjugates against M2 S31N virus, by replacing amantadine with 16 amantadine variants. The compounds were tested against M2 WT and the five M2 amantadine resistant viruses aiming at identifying inhibitors against multiple M2 mutant – amantadine resistant viruses.We identified 16 compounds that inhibited in vitro two influenza A viruses with M2 WT or L26F channels. Additionally, compounds 21 or 32 or 33, which are conjugates of the rimantadine variant with CMe2 (instead of CHMe in rimantadine) or the diamantylamine or the 4-(1-adamantyl)benzenamine with the 2-hydroxy-4-methoxyphenyl aryl group, were in vitro inhibitors against three influenza A viruses with M2 WT or L26F or S31N, while compound 21 inhibited also in vitro the M2 G34E virus and compound 32 inhibited also in vitro the M2 A30T virus. Also, using electrophysiology, we showed that compound 21 was an efficient blocker of the M2 WT and M2 L26F channels, compound 32 blocked efficiently the M2 WT channel and compound 33 blocked the M2 WT, L26F and V27A channels. The drug metabolism and pharmacokinetics studies showed that these compounds need further optimization.
    Keywords Amantadine - aryl conjugate ; In vitro antiviral activity ; CPE ; Electrophysiology ; Influenza A M2 protein ; A30T ; Pharmacy and materia medica ; RS1-441 ; Other systems of medicine ; RZ201-999
    Subject code 572 ; 500
    Language English
    Publishing date 2022-12-01T00:00:00Z
    Publisher Elsevier
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  3. Article ; Online: Chemical Composition and Antimicrobial Activity of the Essential Oil of Algerian Phlomis bovei De Noé subsp. bovei

    Christos Liolios / Hocine Laouer / Nacira Boulaacheb / Olga Gortzi / Ioanna Chinou

    Molecules, Vol 12, Iss 4, Pp 772-

    2007  Volume 781

    Abstract: The chemical composition of essential oil obtained by steam distillation of dried aerial parts of Phlomis bovei De Noé subsp. bovei collected from Algeria, was analyzed by GC and GC/MS. Seventy five constituents (corresponding to 86.37% of the total ... ...

    Abstract The chemical composition of essential oil obtained by steam distillation of dried aerial parts of Phlomis bovei De Noé subsp. bovei collected from Algeria, was analyzed by GC and GC/MS. Seventy five constituents (corresponding to 86.37% of the total weight) were identified. The main components were: germacrene D, β-caryophyllene, β-bournonene, thymol and hexahydrofarnesyl acetone. Furthermore, the antimicrobial activity of the oil was evaluated against six Gram (+/-) bacteria and three pathogenic fungi, using the agar dilution technique. It was found that the oil exhibited strong antimicrobial activity against most of the tested microorganisms.
    Keywords Phlomis bovei De Noe ; chemical composition ; essential oil ; antimicrobial activity ; Organic chemistry ; QD241-441 ; Chemistry ; QD1-999 ; Science ; Q ; DOAJ:Organic Chemistry ; DOAJ:Chemistry
    Language English
    Publishing date 2007-04-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

    Full text online

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    Inter-library loan at ZB MED

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  4. Article ; Online: Chemical Composition and Antimicrobial Activity of the Essential Oil of Algerian Phlomis bovei De Noé subsp. bovei

    Ioanna Chinou / Olga Gortzi / Nacira Boulaacheb / Hocine Laouer / Christos Liolios

    Molecules, Vol 12, Iss 4, Pp 772-

    2007  Volume 781

    Abstract: The chemical composition of essential oil obtained by steam distillation of dried aerial parts of Phlomis bovei De Noé subsp. bovei collected from Algeria, was analyzed by GC and GC/MS. Seventy five constituents (corresponding to 86.37% of the total ... ...

    Abstract The chemical composition of essential oil obtained by steam distillation of dried aerial parts of Phlomis bovei De Noé subsp. bovei collected from Algeria, was analyzed by GC and GC/MS. Seventy five constituents (corresponding to 86.37% of the total weight) were identified. The main components were: germacrene D, β-caryophyllene, β-bournonene, thymol and hexahydrofarnesyl acetone. Furthermore, the antimicrobial activity of the oil was evaluated against six Gram (+/-) bacteria and three pathogenic fungi, using the agar dilution technique. It was found that the oil exhibited strong antimicrobial activity against most of the tested microorganisms.
    Keywords Phlomis bovei De Noe ; chemical composition ; essential oil ; antimicrobial activity ; Organic chemistry ; QD241-441
    Language English
    Publishing date 2007-04-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

    Full text online

    More links

    Kategorien

    Inter-library loan at ZB MED

    Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

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