Change search
ReferencesLink to record
Permanent link

Direct link
Analysis of in vitro toxicity of five cell-penetrating peptides by metabolic profiling
Stockholm University, Faculty of Science, Department of Neurochemistry. University of Tartu, Estonia.ORCID iD: 0000-0001-6107-0844
2009 (English)In: Toxicology, ISSN 0300-483X, E-ISSN 1879-3185, Vol. 265, no 3, 87-95 p.Article in journal (Refereed) Published
Abstract [en]

Cell-penetrating peptides (CPPs) are promising candidates for safe and efficient delivery vectors for a wide range of cargoes. However, any compound that is internalized into cells may affect the cell homeostasis. The plethora of possible biological responses makes large scale “omics” studies appealing approaches for hunting any unsuspected side-effects and evaluate the toxicity of drug candidates. Here we have compared the alterations in cytosolic metabolome of CHO cells caused by five representatives of the most common CPPs: transportan (TP), penetratin (pAntp), HIV Tat derived peptide (pTat), nonaarginine (R9) and model amphipathic peptide (MAP). Analysis was done by liquid chromatography–mass spectrometry techniques, principal component analysis and heatmap displays. Results showed that the intracellular metabolome was the most affected by TP followed by pTat and MAP. Only minor changes could be associated with pAntp or R9 treatment. The cells could recover from a treatment with 5 μM TP, but no recovery was observed at higher concentration. Both metabolomic and control experiments showed that TP affected cellular redox potential, depleted energy and the pools of purines and pyrimidines. In conclusion, we have performed a metabolomic analysis comparing the safety of cell-penetrating peptides and demonstrate the toxicity of one of them.

Place, publisher, year, edition, pages
2009. Vol. 265, no 3, 87-95 p.
Keyword [en]
Metabolomics, Cell-penetrating peptides, Cytotoxicity, Side-effects, Delivery vehicles
National Category
Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy) Neurosciences
Research subject
Neurochemistry with Molecular Neurobiology
URN: urn:nbn:se:su:diva-32176DOI: 10.1016/j.tox.2009.09.016ISI: 000272567700003OAI: diva2:279684
Available from: 2009-12-04 Created: 2009-12-04 Last updated: 2015-04-21Bibliographically approved

Open Access in DiVA

No full text

Other links

Publisher's full text

Search in DiVA

By author/editor
Langel, Ülo
By organisation
Department of Neurochemistry
In the same journal
Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy)Neurosciences

Search outside of DiVA

GoogleGoogle Scholar
The number of downloads is the sum of all downloads of full texts. It may include eg previous versions that are now no longer available

Altmetric score

Total: 22 hits
ReferencesLink to record
Permanent link

Direct link