Cell-penetrating peptides modulate the vascular action of phenylephrine.
Journal Title: Pharmacological Reports - Year 2011, Vol 63, Issue 1
Abstract
Cell-penetrating peptides (CPP) are a family of peptides able to penetrate the cell membrane. This group of compounds has attracted consideration as potential therapeutic tools for the delivery of various substances into cells. Here, we investigated possible interactions between several CPP synthesized in our laboratory and the vascular action of phenylephrine. We used isolated rat tail artery and examined the influence of pretreatment by seven different CPP on the concentration-response curve induced by the α1 receptor agonist phenylephrine. Peptides were synthesized by solid-phase peptide synthesis (SPPS) using the 9-fluorenylmethoxycarbonyl (Fmoc) method. Among the seven different polypeptides, i.e., TP10 (transportan-10), [Lys(AAc)13]TP, [Lys(CAc)13]TP, [Lys(GAc)13]TP, [Lys(TAc)13]TP, [Lys(UAc)13]TP and [Lys(Ac)13]TP, only TP10 and [Lys(AAc)13]TP, both at a concentration of 1 μM (the lowest concentration inducing a significant change in the contraction of isolated rat stomach in our pilot study), rendered rat tail artery more sensitive to phenylephrine; the relative potency increased significantly. Conversely, [Lys(Ac)13]TP strongly decreased the efficacy of phenylephrine.
Authors and Affiliations
Ivan Kocić, Jarosław Ruczyński, Renata Szczepańska, Mariola Olkowicz, Brygida Parfianowicz, Izabela Rusiecka, Piotr Rekowski
Keywords
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