Solid-Phase Synthesis and In Vitro Cytotoxicity of New Peptide Functionalized Cyclencarboxymethylen and L-DOPA Hybrids
| Autor: | T Macek, R Jezek, I Maisuradze, N Sulashvili, P Lovecka, L. Arabuli, E Nikoleishvili |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
chemistry.chemical_classification
Kidney Antioxidant 010405 organic chemistry Chemistry medicine.medical_treatment HEK 293 cells Peptide 010402 general chemistry 01 natural sciences High-performance liquid chromatography 0104 chemical sciences chemistry.chemical_compound Solid-phase synthesis medicine.anatomical_structure Cyclen Biochemistry Toxicity medicine |
| Zdroj: | Medicinal Chemistry. 7 |
| ISSN: | 2161-0444 |
| DOI: | 10.4172/2161-0444.1000487 |
| Popis: | The new small peptide functionalized cyclen and DOPA derivatives were synthesized: cyclen-HisHis, cyclen- AspHis, cyclen-GluHis, DOPA-HisHis were prepared. The solid-phase synthesis strategy was used for preparation of new compounds. Synthesized cyclen- and DOPA-oligopeptide hybrid conjugations were purified by HPLC and analyzed using MALDI-TOF MS spectrometer. The toxic effect was determined against mammalian cells human embryonic kidney cell line HEK293T ATCC®CLR-11268TM for each new compound. The inhibition effect of all tested cyclen– dipeptides on kidney cells was approximately about 30% after 24 hours. The minimal rate of toxicity against human liver cells showed all tested dipeptides with DOPA, their inhibition effect was maximal 10%. The acute inhibition effect of sample DOPA-GluHis-DOPA was 14% imme¬diately after adding. The antioxidant and anticancer activity studies will be next part of the ongoing project. |
| Databáze: | OpenAIRE |
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