Solid-Phase Synthesis of Mimosine Tetrapeptides and Their Inhibitory Activities on Neuraminidase and Tyrosinase

• DOI: 10.1021/jf203494t
• Publication Date: 2011-11-02T17:18:12Z
• Authors: Atul Upadhyay; Jamnian Chompoo; Nozomi Taira; Masakazu Fukuta; Shinichi Gima; Shinkichi Tawata
• Keywords: Mimosine; Neuraminidase inhibitor

Neuraminidase is a rational target for influenza inhibition, and the search neuraminidase inhibitors has been intensified. Mimosine, nonprotein amino acid, was first time identified as inhibitor with an IC(50) of 9.8 ± 0.2 μM. It found that mimosine had slow, time-dependent competitive inhibition against neuraminidase. Furthermore, small library tetrapeptides (M-A(1)-A(2)-A(3)) synthesized by solid-phase synthesis assayed to evaluate their tyrosinase inhibitory properties. Most showed better activities than mimosine. Mimosine-FFY best compound, it exhibited 50% at low micromolar range 1.8 μM, whereas 18.3 0.5 The kinetic studies all peptides inhibited noncompetitively K(i) values ranging from 1.9 -to 7.2 These results suggest could be used source bioactive compounds may have possibilities in design drugs inhibitors.