Cyclotides: a novel type of cytotoxic agents
2002 (English)In: Molecular Cancer Therapeutics, ISSN 1535-7163, E-ISSN 1538-8514, Vol. 1, no 6, 365-369 p.Article in journal (Refereed) Published
Cytotoxic activities of three naturally occurring macrocyclic peptides (cyclotides) isolated from the two violets, Viola arvensis Murr. and Viola odorata L., were investigated. A nonclonogenic fluorometric microculture assay was used to examine cytotoxicity in a panel of 10 human tumor cell lines representing defined types of cytotoxic drug resistance. Additionally, primary cultures of tumor cells from patients, and for comparison normal lymphocytes, were used to quantify cytotoxic activity. All three cyclotides, varv A, varv F, and cycloviolacin O2, exhibited strong cytotoxic activities, which varied in a dose-dependent manner. Cycloviolacin O2 was the most potent in all cell lines (IC50 0.1– 0.3 _M), followed by varv A (IC50 2.7–6.35 _M) and varv F (IC50 2.6 –7.4 _M), respectively. Activity profiles of the cyclotides differed significantly from those of antitumor drugs in clinical use, which may indicate a new mode of action. This, together with the exceptional chemical and biological stability of cyclotides, makes them interesting in particular for their potential as pharmacological tools and possibly as leads to antitumor agents.
Place, publisher, year, edition, pages
2002. Vol. 1, no 6, 365-369 p.
Medical and Health Sciences
IdentifiersURN: urn:nbn:se:uu:diva-92805ISI: 000178770300001PubMedID: 12477048OAI: oai:DiVA.org:uu-92805DiVA: diva2:166103
De två första författarna delar på förstaförfattarskapet.2005-04-012005-04-012013-06-10Bibliographically approved