Solid-Phase Synthesis of Cyclic Heptapeptide Stylissatin A

摘要

The present study achieves the total synthesis of a new proline-rich cyclic heptapeptide as an inhibitor of nitric oxide production in LPS-stimulated murine macrophage RAW264.7 cells, where all the amino acids are of L-configuration. A general method was described to synthesize the cyclic peptide by a two-step solid-phase/solution synthesis strategy. The linear octapeptide was assembled by standard Fmoc chemistry in the solid phase. Subsequently cyclization was achieved by the solution method. The final product was purified by preparative RP-HPLC, and its structure was identified by HR-QTOF-MS, H-1 NMR, and C-13 NMR.