{"entity": "researcher", "timestamp": "2026-04-11T09:02:09.595Z", "family": "Marinelli", "given": "Lisa", "initials": "L", "orcid": "0000-0001-8611-6538", "affiliations": ["Department of Pharmacy, University \"G. D'Annunzio\" of Chieti-Pescara, Chieti Scalo, Chieti, Italy."], "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/researcher/97c00bbd21584fd7a44200f607877276.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/researcher/97c00bbd21584fd7a44200f607877276"}}, "publications": [{"entity": "publication", "iuid": "aafba9b1723a4576ad65c4fde1e93ddc", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/aafba9b1723a4576ad65c4fde1e93ddc.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/aafba9b1723a4576ad65c4fde1e93ddc"}}, "title": "Development of l-Dopa-containing diketopiperazines as blood-brain barrier shuttle.", "authors": [{"family": "Cornacchia", "given": "Catia", "initials": "C"}, {"family": "Marinelli", "given": "Lisa", "initials": "L", "orcid": "0000-0001-8611-6538", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/97c00bbd21584fd7a44200f607877276.json"}}, {"family": "Di Rienzo", "given": "Annalisa", "initials": "A", "orcid": "0000-0002-9994-6968", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/21b8ecd7e661415bbec3d6cc141a2ddf.json"}}, {"family": "Dimmito", "given": "Marilisa Pia", "initials": "MP"}, {"family": "Serra", "given": "Federica", "initials": "F"}, {"family": "Di Biase", "given": "Giuseppe", "initials": "G"}, {"family": "De Filippis", "given": "Barbara", "initials": "B"}, {"family": "Turkez", "given": "Hasan", "initials": "H", "orcid": "0000-0002-7046-8990", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/cf2f1748757d45cabfe56fdfaccead6a.json"}}, {"family": "Mardinoglu", "given": "Adil", "initials": "A", "orcid": "0000-0002-4254-6090", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/ca58bf2d214047e0ae5e38a42a0f2808.json"}}, {"family": "Bellezza", "given": "Ilaria", "initials": "I"}, {"family": "Di Stefano", "given": "Antonio", "initials": "A", "orcid": "0000-0002-3042-2234", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/413d1857e18c4eef8929bb9ceedc5af0.json"}}, {"family": "Cacciatore", "given": "Ivana", "initials": "I", "orcid": "0000-0001-6253-0443", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/31661d5900cc4711923f4bf51cf47a93.json"}}], "type": "journal article", "published": "2022-12-05", "journal": {"title": "Eur J Med Chem", "issn": "1768-3254", "volume": "243", "pages": "114746", "issn-l": "0223-5234"}, "abstract": "In our overall goal to develop anti-Parkinson drugs, we designed novel diketopiperazines (DKP1-6) aiming to both reach the blood-brain barrier and counteract the oxidative stress related to Parkinson's Disease (PD). The anti-Parkinson properties of DKP 1-6 were evaluated using neurotoxin-treated PC12 cells, as in vitro model of PD, while their cytotoxicity and genotoxicity potentials were investigated in newborn rat cerebral cortex (RCC) and primary human whole blood (PHWB) cell cultures. The response against free radicals was evaluated by the total antioxidant capacity (TAC) assay. Comet assay was used to detect DNA damage while the content of 8-hydroxyl-2'-deoxyguanosine (8-OH-dG) was determined as a marker of oxidative DNA damage. PAMPA-BBB and Caco-2 assays were employed to evaluate the capability of DKP1-6 to cross the membranes. Stability studies were conducted in simulated gastric and intestinal fluids and human plasma. Results showed that DKP5-6 attenuate the MPP + -induced cell death on a nanomolar scale, but a remarkable effect was observed for DKP6 on Nrf2 activation that leads to the expression of genes involved in oxidative stress response thus increasing glutathione biosynthesis and ROS buffering. DKP5-6 resulted in no toxicity for RCC neurons and PHWB cells exposed to 10-500 nM concentrations during 24 h as determined by MTT and LDH assays and TAC levels were not altered in both cultured cell types. No significant difference in the induction of DNA damage was observed for DKP5-6. Both DKPs resulted stable in simulated gastric fluids (t1/2 > 22h). In simulated intestinal fluids, DKP5 underwent immediate hydrolysis while DKP6 showed a half-life higher than 3 h. In human plasma, DKP6 resulted quite stable. DKP6 displayed both high BBB and Caco-2 permeability confirming that the DKP scaffold represents a useful tool to improve the crossing of drugs through the biological membranes.", "doi": "10.1016/j.ejmech.2022.114746", "pmid": "36099749", "labels": {"Adil Mardinoglu": null, "SciLifeLab Fellow": null}, "xrefs": [{"db": "pii", "key": "S0223-5234(22)00648-1"}], "notes": [], "created": "2023-12-04T14:58:09.279Z", "modified": "2025-04-29T07:06:35.664Z"}, {"entity": "publication", "iuid": "9da9a80f2d2f4eb081de73a7584fe558", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/9da9a80f2d2f4eb081de73a7584fe558.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/9da9a80f2d2f4eb081de73a7584fe558"}}, "title": "Toxicity of Glycyl-l-Prolyl-l-Glutamate Pseudotripeptides: Cytotoxic, Oxidative, Genotoxic, and Embryotoxic Perspectives.", "authors": [{"family": "Turkez", "given": "Hasan", "initials": "H", "orcid": "0000-0002-7046-8990", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/cf2f1748757d45cabfe56fdfaccead6a.json"}}, {"family": "Ozdemir Tozlu", "given": "Ozlem", "initials": "O", "orcid": "0000-0002-5472-8174", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/3f64b15273ce49348b9ffebf5230ea11.json"}}, {"family": "Tatar", "given": "Arzu", "initials": "A", "orcid": "0000-0002-4486-2695", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/3b34bfb83ab14a95bc03c974d39f816c.json"}}, {"family": "Arslan", "given": "Mehmet Enes", "initials": "ME", "orcid": "0000-0002-1600-2305", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/6c5dd8a766b948efa5f040ceb43e60a6.json"}}, {"family": "Cadirci", "given": "Kenan", "initials": "K", "orcid": "0000-0002-2765-4288", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/305106d191054c26a2de64f9ca54437f.json"}}, {"family": "Marinelli", "given": "Lisa", "initials": "L", "orcid": "0000-0001-8611-6538", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/97c00bbd21584fd7a44200f607877276.json"}}, {"family": "Yapca", "given": "Omer Erkan", "initials": "OE", "orcid": "0000-0002-5578-0126", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/4ea9b4f98ad24d549984a2c9e00a58d9.json"}}, {"family": "Cacciatore", "given": "Ivana", "initials": "I", "orcid": "0000-0001-6253-0443", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/31661d5900cc4711923f4bf51cf47a93.json"}}, {"family": "Di Stefano", "given": "Antonio", "initials": "A", "orcid": "0000-0002-3042-2234", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/413d1857e18c4eef8929bb9ceedc5af0.json"}}, {"family": "Mardinoglu", "given": "Adil", "initials": "A", "orcid": "0000-0002-4254-6090", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/ca58bf2d214047e0ae5e38a42a0f2808.json"}}], "type": "journal article", "published": "2022-11-19", "journal": {"title": "J Toxicol", "issn": "1687-8191", "volume": "2022", "pages": "3775194", "issn-l": null}, "abstract": "The tripeptide H-Gly-Pro-Glu-OH (GPE) and its analogs began to take much interest from scientists for developing effective novel molecules in the treatment of several disorders including Alzheimer's disease, Parkinson's disease, and stroke. The peptidomimetics of GPEs exerted significant biological properties involving anti-inflammatory, antiapoptotic, and anticancer properties. The assessments of their hematological toxicity potentials are critically required for their possible usage in further preclinical and clinical trials against a wide range of pathological conditions. However, there is so limited information on the safety profiling of GPE and its analogs on human blood tissue from cytotoxic, oxidative, and genotoxic perspectives. And, their embryotoxicity potentials were not investigated yet. Therefore, in this study, measurements of mitochondrial viability (using MTT assay) and lactate dehydrogenase (LDH) release as well as total antioxidant capacity (TAC) assays were performed on cultured human whole blood cells after treatment with GPE and its three novel peptidomimetics for 72 h. Sister chromatid exchange (SCE), micronucleus (MN), and 8-oxo-2-deoxyguanosine (8-OH-dG) assays were performed for determining the genotoxic damage potentials. In addition, the nuclear division index (NDI) was figured out for revealing their cytostatic potentials. Embryotoxicity assessments were performed on cultured human pluripotent NT2 embryonal carcinoma cells by MTT and LDH assays. The present results from cytotoxicity, oxidative, genotoxicity, and embryotoxicity testing clearly propounded that GPEs had good biosafety profiles and were trouble-free from the toxicological point of view. Noncytotoxic, antioxidative, nongenotoxic, noncytostatic, and nonembryotoxic features of GPE analogs are worthwhile exploring further and may exert high potentials for improving the development of novel disease-modifying agents.", "doi": "10.1155/2022/3775194", "pmid": "36444193", "labels": {"Adil Mardinoglu": null, "SciLifeLab Fellow": null}, "xrefs": [{"db": "pmc", "key": "PMC9701129"}], "notes": [], "created": "2023-12-04T14:53:09.961Z", "modified": "2023-12-04T14:53:10.249Z"}]}