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Integrative development of smart drug-vector nanostructures for adaptive delivery to target cells

Deliverables

A set of pH- and redox-sensitive nanoparticles based on self-assembling copolymers developed and validated in lab

Report on preparation and validation in lab of pH- and redox-sensitive nanoparticles based on self-assembling copolymers

Synthetic platform for obtaining of INMs developed and validated in lab

Report on validation of a synthetic platform for obtaining of INMs at the laboratory scale

Water soluble zerumbone and ellipticine derivatives provided

Report on synthesis of water soluble zerumbone and ellipticine derivatives

Theoretical study of INMs and their interaction with PhACs published

Open Access publication on theoretical studies of INMs and their interaction with PhACs

Docking and DFT modelling of protein-ligand interactions concluded and list of the most promising structures provided

Report on docking and DFT modelling of protein-ligand interactions and selection of the most promising structures

The best PhACs to target the secretory pathway selected and transferred to WP3 and WP4 for DVN optimisation

Report on selection of the best PhACs to target the secretory pathways

Inorganic and inorgano-organic DVN preparation technology optimised and validated in the relevant environment

Report on validation of inorganic and inorganoorganic DVN preparation technology in the relevant environment

Samples of synthetic ellipticine provided for quality control and subsequent use as PhAC

Quality control report on samples of synthetic ellipticine provided for use as PhAC

Progress report, 1st year

Progress report for the first project year submitted to the EU

Progress report, 3rd year

Progress report for the third project year submitted to the EU

Data Management Plan elaborated and approved
Technology of pH- and redox-sensitive nanoparticles manufacturing validated in the relevant environment

Report on validation in the relevant environment of pH and redoxsensitive nanoparticle manufacturing technology

Study on stimuli-responsive drug release, biocompatibility, and cellular uptake of polymer nanoparticles concluded

Report on stimuli-responsive drug release from polymer nanoparticles, their biocompatibility and cellular uptake

The best DVN-PhAC formulations determined in vitro and proposed for in vivo studies

Report on selection of the best DVN-PhAC formulations determined in vitro, which will be proposed for in vivo studies

Summer school organised and held

Summer school will be organised and held during month 14 - 17. (exact date will be established by consensus of the Partners)

Organisation of the Project Workshops

Organisation of the Project Workshops on months 2, 15, 26, 36, 45

Mid-term meeting

Mid-term project review meeting between the Consortium and REA

Publications

Caralluma europaea (Guss.) N.E.Br.: Anti-Inflammatory, Antifungal, and Antibacterial Activities against Nosocomial Antibiotic-Resistant Microbes of Chemically Characterized Fractions

Author(s): F.E.Z.Amrati, M.Bourhia, H.Saghrouchni, M.Slighoua, A.Grafov, R.Ullah, E.Ezzeldin, G.A.Mostafa, A.Bari, S.Ibenmoussa, D.Bousta.
Published in: Molecules, 2021, ISSN 1420-3049
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules26030636

New 2,3-Benzodiazepine Derivative: Synthesis, Activity on Central Nervous System, and Toxicity Study in Mice

Author(s): Amal Amaghnouje; Serhii Bohza; Nathalie Bohdan; Imane Es-Safi; Andrii Kyrylchuk; Sanae Achour; Hinde El Fatemi; Dalila Bousta; Andriy Grafov
Published in: Pharmaceuticals, 2021, ISSN 1424-8247
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/ph14080814

Ethnobotanical survey about the management of diabetes with medicinal plants used by diabetic patients in Region of Fez-Meknes, Morocco

Author(s): Hamza Mechchate, Imane Es-safi, Fatima Zahra Jawhari, Amina Bari, Andriy Grafov, Dalila Bousta
Published in: Ethnobotany Research and Applications, Issue 19, 2020, ISSN 1547-3465
Publisher: University of Hawaii Press
DOI: 10.32859/era.19.12.1-28

Stable Carbenes as Structural Components of Partially Saturated Sulfur-Containing Heterocycles

Author(s): Rozhenko AB, Horbenko YS, Kyrylchuk AA, Zarudnitskii EV, Mykhaylychenko SS, Shermolovich YG, Grafov AV
Published in: Molecules, 2022, ISSN 1420-3049
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules27051458

Phytochemical Study on Antioxidant and Antiproliferative Activities of Moroccan Caralluma europaea Extract and Its Bioactive Compound Classes

Author(s): Fatima ez-zahra Amrati, Mohammed Bourhia, Meryem Slighoua, Samir Ibnemoussa, Ahmed Bari, Riaz Ullah, Amal Amaghnouje, Francesca Di Cristo, Mohammed El Mzibri, Anna Calarco, Laila Benbacer, Dalila Bousta
Published in: Evidence-Based Complementary and Alternative Medicine, Issue 2020, 2020, Page(s) 1-9, ISSN 1741-427X
Publisher: Oxford University Press
DOI: 10.1155/2020/8409718

Well-Defined Thermo-Responsive Copolymers Based on Oligo(Ethylene Glycol) Methacrylate and Pentafluorostyrene for the Removal of Organic Dyes from Water

Author(s): F.Zuppardi, M.Malinconico, F.D’Agosto, G.G.D’Ayala, P.Cerruti
Published in: Nanomaterials, 2020, ISSN 2079-4991
Publisher: MPDI
DOI: 10.3390/nano10091779

In vitro and in silico evaluation of cholinesterase inhibition by alkaloids obtained from branches of Abuta panurensis Eichler

Author(s): R.S.Mesquita, A.Kyrylchuk, A.Cherednichenko, I.S.C.Sá, LM. Bastos, FM.A.Silva, R.C.S. Nunomura, A.Grafov
Published in: Molecules, 2022, ISSN 1420-3049
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules27103138

Anticancer and Immunomodulatory Activities of a Novel Water-Soluble Derivative of Ellipticine

Author(s): Regiane Costa de Oliveira, Gemilson Soares Pontes, Aleksandr Kostyuk, Gabriel B. Coutinho Camargo, Anamika Dhyani, Tetiana Shvydenko, Kostiantyn Shvydenko, Andriy Grafov
Published in: Molecules, Issue 25/9, 2020, Page(s) 2130, ISSN 1420-3049
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules25092130

Alkaloids of Abuta panurensis Eichler: In silico and in vitro study of acetylcholinesterase inhibition, cytotoxic and immunomodulatory activities

Author(s): Rochelly da Silva Mesquita, Andrii Kyrylchuk, Regiane Costa de Oliveira, Ingrity Suelen Costa Sá, Gabriel Coutinho Borges Camargo, Gemilson Soares Pontes, Felipe Moura Araújo da Silva, Rita de Cássia Saraiva Nunomura, Andriy Grafov
Published in: PLOS ONE, Issue 15/9, 2020, Page(s) e0239364, ISSN 1932-6203
Publisher: Public Library of Science
DOI: 10.1371/journal.pone.0239364

In-Vivo Antidiabetic Activity and In-Silico Mode of Action of LC/MS-MS Identified Flavonoids in Oleaster Leaves

Author(s): Hamza Mechchate, Imane Es-Safi, Mohammed Bourhia, Andrii Kyrylchuk, Abdelfattah El Moussaoui, Raffaele Conte, Riaz Ullah, Essam Ezzeldin, Gamal A. Mostafa, Andriy Grafov, Hicham Bekkari, Dalila Bousta
Published in: Molecules, Issue 25/21, 2020, Page(s) 5073, ISSN 1420-3049
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/molecules25215073

Antileukemic Activity and Molecular Docking Study of a Polyphenolic Extract from Coriander Seeds

Author(s): Hamza Mechchate; Regiane Costa de Oliveira; Imane Es-Safi; Emmily Myrella Vasconcelos Mourão; Mohamed Bouhrim; Andrii Kyrylchuk; Gemilson Soares Pontes; Gemilson Soares Pontes; Dalila Bousta; Andriy Grafov
Published in: Pharmaceuticals, 2021, ISSN 1424-8247
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/ph14080770

Cationic Polymer Nanoparticles-Mediated Delivery of miR-124 Impairs Tumorigenicity of Prostate Cancer Cells

Author(s): Raffaele Conte, Anna Valentino, Francesca Di Cristo, Gianfranco Peluso, Pierfrancesco Cerruti, Anna Di Salle, Anna Calarco
Published in: International Journal of Molecular Sciences, Issue 21/3, 2020, Page(s) 869, ISSN 1422-0067
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/ijms21030869

Ethnobotanical Survey of Medicinal Plants Used in the Traditional Treatment of Depression and Anxiety in Fez-Meknes Region

Author(s): A. Amaghnouje, M. Slighoua, I. Es-safi, R. El Jaoudi, A. Elyoubi, D. Bousta, A. Grafov
Published in: Phytothérapie, 2020, ISSN 1624-8597
Publisher: Springer Verlag
DOI: 10.3166/phyto-2020-0225

Synthesis, molecular docking studies, and larvicidal activity evaluation of new fluorinated neonicotinoids against Anopheles darlingi larvae

Author(s): Rochelly da Silva Mesquita, Andrii Kyrylchuk, Iryna Grafova, Denys Kliukovskyi, Andriy Bezdudnyy, Alexander Rozhenko, Wanderli Pedro Tadei, Markku Leskelä, Andriy Grafov
Published in: PLOS ONE, Issue 15/2, 2020, Page(s) e0227811, ISSN 1932-6203
Publisher: Public Library of Science
DOI: 10.1371/journal.pone.0227811

Cellular Uptake of Mildly Oxidized Nanographene for Drug-Delivery Applications

Author(s): M. Mugnano, G. C. Lama, R. Castaldo, V. Marchesano, F. Merola, D. del Giudice, A. Calabuig, G. Gentile, V. Ambrogi, P. Cerruti, P. Memmolo, V. Pagliarulo, P. Ferraro, S. Grilli
Published in: ACS Applied Nano Materials, Issue 3/1, 2019, Page(s) 428-439, ISSN 2574-0970
Publisher: American Chemical Society
DOI: 10.1021/acsanm.9b02035

pH-Responsive Resveratrol-Loaded Electrospun Membranes for the Prevention of Implant-Associated Infections

Author(s): Irene Bonadies, Francesca Di Cristo, Anna Valentino, Gianfranco Peluso, Anna Calarco, Anna Di Salle
Published in: Nanomaterials, Issue 10/6, 2020, Page(s) 1175, ISSN 2079-4991
Publisher: MPDI
DOI: 10.3390/nano10061175

In Vivo and In Vitro Antidiabetic and Anti-Inflammatory Properties of Flax (Linum usitatissimum L.) Seed Polyphenols

Author(s): Mechchate, H.; Es-safi, I.; Conte, R.; Hano, C.; Amaghnouje, A.; Jawhari, F.Z.; Radouane, N.; Bencheikh, N.; Grafov, A.; Bousta, D.
Published in: Nutrients, 2021, ISSN 2072-6643
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/nu13082759

Optimized Antibacterial Effects in a Designed Mixture of Essential Oils of Myrtus communis, Artemisia herba-alba and Thymus serpyllum for Wide Range of Applications

Author(s): Ouedrhiri W, Mechchate H, Moja S, Baudino S, Saleh A, Al Kamaly OM, Grafov A, Greche H.
Published in: Foods, 2022, ISSN 2304-8158
Publisher: MPDI
DOI: 10.3390/foods11010132

Thermoresponsive Copolymer Nanovectors Improve the Bioavailability of Retrograde Inhibitors in the Treatment of Leishmania Infections

Author(s): E.Craig, A.Calarco, R.Conte, V.Ambrogi, G.G.d'Ayala, P.Alabi, J.K.Sello, P.Cerruti, P.E.Kima.
Published in: Frontiers in Cellular and Infection Microbiology, 2021, ISSN 2235-2988
Publisher: Frontiers Media S. A.
DOI: 10.3389/fcimb.2021.702676

Intellectual Property Rights

1,5-Bis-(4-aminodiphenoxy)-2,2,3,3,4,4-hexafluoropentane dihydrochloride

Application/Publication number: UA 116830
Date: 2018-05-10
Applicant(s): INSTITUTE OF ORGANIC CHEMISTRY OF NATIONAL ACADEMY SCIENCES OF UKRAINE

Bioactive Inorganic Nanomatrices Based on Hydrated Polyvalent Transition Metal Oxides : Preparation Process and Applications

Application/Publication number: BR 10 2019 005007 1
Date: 2019-03-14

1,5-Bis-(4-aminodiphenoxy)-3,3-difluoropentane dihydrochloride

Application/Publication number: UA 116492
Date: 2018-03-26
Applicant(s): INSTITUTE OF ORGANIC CHEMISTRY OF NATIONAL ACADEMY SCIENCES OF UKRAINE

1,5-Bis-(4-aminodiphenoxy)-3,3-difluoropentane dihydrochloride

Application/Publication number: UA 116492
Date: 2018-03-26

1,5-Bis-(4-aminodiphenoxy)-2,2,3,3,4,4-hexafluoropentane dihydrochloride

Application/Publication number: UA 116830
Date: 2018-05-10

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