Cylic peptides cyclo[X1-X2-X3-X4-X5-X6] and cyclo[Y6-Y5-Y4-Y3-Y2-Y1] [X1, X2 = independently hydrophobic natural orsynthetic L-amino acid; X3, X5 = independently hydrophilic natural or synthetic L-amino acid or Gly; X4, Y4 = independently natural or synthetic D-amino acid or Gly, or a-methylalanine, a-aminocyclobutanecarboxylic acid, etc.; X6, Y6 = independently natural or synthetic L-amino acid or Gly, or a-methylalanine, a-aminocyclobutanecarboxylic acid, etc.; Y1, Y2 = independently hydrophobic natural or synthetic D-amino acid; Y3, Y5 = independently hydrophilic natural or synthetic D-amino acid or Gly] were prepared as immunosuppressants useful for treating pathologies involving activation of T-lymphocytes. Their immunosuppressant activity was detd. in vitro and in vivo in human or murine mixed lymphocyte cultures by measuring lymphocyte proliferation by [3H]-TdR incorporation assay and the production of interferon g and interleukin-5 by ELISA assay. Thus, cyclo[(b-1-Nal)-(b-1-Nal)-Glu-(D-Pro)-His-Asn] (b-1-Nal = b-1-naphthylalanine), prepared by a solid phase synthesis, significantly decreased lymphocyte proliferation and inhibited prodn. of interferon g and interleukin-5.

New cyclic peptides, their preparation and pharmaceutical use as immunosuppressants

LOMBARDI, ANGELINA;PAVONE, VINCENZO
2001

Abstract

Cylic peptides cyclo[X1-X2-X3-X4-X5-X6] and cyclo[Y6-Y5-Y4-Y3-Y2-Y1] [X1, X2 = independently hydrophobic natural orsynthetic L-amino acid; X3, X5 = independently hydrophilic natural or synthetic L-amino acid or Gly; X4, Y4 = independently natural or synthetic D-amino acid or Gly, or a-methylalanine, a-aminocyclobutanecarboxylic acid, etc.; X6, Y6 = independently natural or synthetic L-amino acid or Gly, or a-methylalanine, a-aminocyclobutanecarboxylic acid, etc.; Y1, Y2 = independently hydrophobic natural or synthetic D-amino acid; Y3, Y5 = independently hydrophilic natural or synthetic D-amino acid or Gly] were prepared as immunosuppressants useful for treating pathologies involving activation of T-lymphocytes. Their immunosuppressant activity was detd. in vitro and in vivo in human or murine mixed lymphocyte cultures by measuring lymphocyte proliferation by [3H]-TdR incorporation assay and the production of interferon g and interleukin-5 by ELISA assay. Thus, cyclo[(b-1-Nal)-(b-1-Nal)-Glu-(D-Pro)-His-Asn] (b-1-Nal = b-1-naphthylalanine), prepared by a solid phase synthesis, significantly decreased lymphocyte proliferation and inhibited prodn. of interferon g and interleukin-5.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11588/196901
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