SYNTHESIS OF TYROSINE-RELATED PEPTIDE AND THEIR EFFECT ON PROGESTERONE PRODUCTION

Twenty peptides containing hydroxy- amino acids have been synthesized manually by stepwise solid-phase procedure.The chloromethyl resin and MBHA resin were used as solid supports.A new reagent of 0.5 mol·L^-1 DDSi/1.5mol·L^-1 phenol/ DCM was applied for the removal of Na-Boc group.TFMSA was the cleaving reagent.After purification by C-18 column,allproducts were assayed according to amino acid analysis·The bioactivity of synthetic peptides was tested for the effect on progesterone production in uitro.Eight peptides, GlyTyrAiaLys,( SarSer )₂Lys and its metftyl ester,TyrLys,HisTyr-NH2,ThrProTyrLys-NH₂ TyrThrProArgLys and AspHisProThrPheLys showed significant effect on inhibiting hCG-induced progesterone production,and first three of them could also inhibit basal progesterone secretion. However,peptide GlySerTyr exhibited stimulative activity on basal proges- erone secretion,So far,no reasonable relationship between structure and bioactivity was found。