{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,12]],"date-time":"2025-10-12T19:04:28Z","timestamp":1760295868924,"version":"build-2065373602"},"reference-count":35,"publisher":"MDPI AG","issue":"1","license":[{"start":{"date-parts":[[2020,12,22]],"date-time":"2020-12-22T00:00:00Z","timestamp":1608595200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100001871","name":"Funda\u00e7\u00e3o para a Ci\u00eancia e a Tecnologia","doi-asserted-by":"publisher","award":["UIDB\/50006\/2020","IF\/00092\/2014\/CP1255\/CT0004","PD\/BD\/106035\/2015"],"award-info":[{"award-number":["UIDB\/50006\/2020","IF\/00092\/2014\/CP1255\/CT0004","PD\/BD\/106035\/2015"]}],"id":[{"id":"10.13039\/501100001871","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Membranes"],"abstract":"<jats:p>Conjugation of TP10, a cell-penetrating peptide with intrinsic antimalarial activity, to the well-known antimalarial drugs chloroquine and primaquine has been previously shown to enhance the peptide\u2019s action against, respectively, blood- and liver-stage malaria parasites. Yet, this was achieved at the cost of a significant increase in haemolytic activity, as fluorescence microscopy and flow cytometry studies showed the conjugates to be more haemolytic for non-infected than for Plasmodium-infected red blood cells. To gain further insight into how these conjugates distinctively bind, and likely disrupt, membranes of both Plasmodium-infected and non-infected erythrocytes, we used dynamic light scattering and surface plasmon resonance to study the interactions of two representative conjugates and their parent compounds with lipid model membranes. Results obtained are herein reported and confirm that a strong membrane-disruptive character underlies the haemolytic properties of these conjugates, thus hampering their ability to exert selective antimalarial action.<\/jats:p>","DOI":"10.3390\/membranes11010004","type":"journal-article","created":{"date-parts":[[2020,12,22]],"date-time":"2020-12-22T20:39:29Z","timestamp":1608669569000},"page":"4","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":5,"title":["Insights into the Membranolytic Activity of Antimalarial Drug-Cell Penetrating Peptide Conjugates"],"prefix":"10.3390","volume":"11","author":[{"given":"Lu\u00edsa","family":"Aguiar","sequence":"first","affiliation":[{"name":"LAQV-REQUIMTE, Departamento de Qu\u00edmica e Bioqu\u00edmica, Faculdade de Ci\u00eancias, Universidade do Porto, Rua do Campo Alegre 687, P-4169-007 Porto, Portugal"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6931-1355","authenticated-orcid":false,"given":"Marina","family":"Pinheiro","sequence":"additional","affiliation":[{"name":"LAQV-REQUIMTE, Departamento de Ci\u00eancias Qu\u00edmicas, Faculdade de Farm\u00e1cia, Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, P-4050-313 Porto, Portugal"}]},{"given":"Ana Rute","family":"Neves","sequence":"additional","affiliation":[{"name":"Centro de Qu\u00edmica da Madeira, Universidade da Madeira, Campus da Penteada, Ilha da Madeira, P-9020-105 Funchal, Portugal"}]},{"given":"Nuno","family":"Vale","sequence":"additional","affiliation":[{"name":"OncoPharma Research Group, Center for Health Technology and Services Research (CINTESIS), Rua Dr. Pl\u00e1cido da Costa, P-4200-450 Porto, Portugal"},{"name":"Faculdade de Medicina, Universidade do Porto, Alameda Prof. Hern\u00e2ni Monteiro, P-4200-319 Porto, Portugal"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3106-458X","authenticated-orcid":false,"given":"Sira","family":"Defaus","sequence":"additional","affiliation":[{"name":"Proteomics and Protein Chemistry Group, Department of Experimental and Health Sciences, Pompeu Fabra University, Dr. Aiguader 88, E-08003 Barcelona, Spain"}]},{"given":"David","family":"Andreu","sequence":"additional","affiliation":[{"name":"Proteomics and Protein Chemistry Group, Department of Experimental and Health Sciences, Pompeu Fabra University, Dr. Aiguader 88, E-08003 Barcelona, Spain"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0736-2835","authenticated-orcid":false,"given":"Salette","family":"Reis","sequence":"additional","affiliation":[{"name":"LAQV-REQUIMTE, Departamento de Ci\u00eancias Qu\u00edmicas, Faculdade de Farm\u00e1cia, Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, P-4050-313 Porto, Portugal"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6018-4724","authenticated-orcid":false,"given":"Paula","family":"Gomes","sequence":"additional","affiliation":[{"name":"LAQV-REQUIMTE, Departamento de Qu\u00edmica e Bioqu\u00edmica, Faculdade de Ci\u00eancias, Universidade do Porto, Rua do Campo Alegre 687, P-4169-007 Porto, Portugal"}]}],"member":"1968","published-online":{"date-parts":[[2020,12,22]]},"reference":[{"key":"ref_1","unstructured":"World Health Organization (2019). 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