Synthesis and anti-HIV activity of carboxylated and drug-conjugated multi-walled carbon nanotubes |
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| Affiliation: | 1. Department of Electronic Engineering, Industrial Chemistry and Engineering, University of Messina, Contrada Di Dio, I-98166 Messina, Italy;2. Department of Pharmaceutical Sciences and Health Products, University of Messina, Viale Annunziata, I-98168 Messina, Italy;3. Department of Pharmaceutical and Chemical Sciences, University of Trieste, Piazzale Europa 1, I-34127 Trieste, Italy;4. Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium;1. Raymond and Beverly Sackler Faculty of Exact Sciences, Tel-Aviv University, Tel-Aviv 6997801, Israel;2. Applied Physics Division, Soreq NRC, Yavne 81800, Israel;3. DDR&D, Ministry of Defense, Israel;1. Institut de Chimie des Substances Naturelles, UPR2301, CNRS, Avenue de la Terrasse, 91198 Gif-sur-Yvette, France;2. DISCO Beamline, Synchrotron SOLEIL, L’Orme des Merisiers, Saint-Aubin, 91192 Gif-sur-Yvette, France;3. UAR 1008 CEPIA, INRA, Rue de la Géraudière, F-44316 Nantes, France;1. Department of Physics, Aligarh Muslim University, Aligarh 202002, India;2. Atomic & Molecular Physics Division, Bhabha Atomic Research Centre, Mumbai 400085, India;1. School of Pharmacy, Nankai University, Tianjin 300071, China;2. School of life science, Nankai University, Tianjin 300071, China;3. School of chemistry, Nankai University, Tianjin 300071, China |
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| Abstract: | Carbon nanotubes have attracted particular attention in antiviral therapy and recently have been explored as HIV inhibitors through structure-based design. In order to prove their in vitro ability to interact with viral enzymes and to act as HIV inhibitors, we have studied the antiviral potentiality of highly hydrophilic and dispersible carboxylated multi-walled carbon nanotubes (ox-MWCNT) and the activity exerted by the same nanomaterial bearing antiretroviral drugs and hydrophilic functionalities. The antiretroviral drugs chosen for this study were two newly synthesized benzimidazolones, CHI360 and CHI415, belonging to a series of active non-nucleoside reverse transcriptase inhibitors (RTI), and lamivudine (3TC), a known antiretroviral nucleoside agent, currently used in anti-HIV therapy. From this study, the physicochemical properties of these nanomaterials, namely hydrophilicity and dispersibility, emerged as the most relevant features able to control the antiviral activity. The more hydrophilic and dispersible oxidized samples, ox-MWCNT and MWCNT-C-CHI360, showed the best results with IC50 values of 11.43 μg/mL and 4.56 μg/mL, respectively. |
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