The invention provides an
octreotide-D-configuration oncolytic
peptide conjugate as well as a preparation method and application thereof, and belongs to the technical field of polypeptide preparation and biological
medicine. The invention designs and synthesizes a pH-responsive
octreotide-D-configuration oncolytic
peptide conjugate aiming at the defects that an L-configuration oncolytic
peptide is poor in stability, low in anti-tumor activity, high in
toxicity to normal cells, only capable of performing intratumor injection and the like. The pH-responsive
octreotide-D-configuration oncolytic
peptide conjugate can significantly improve the anti-tumor activity and stability of the oncolytic peptide, and shows a stronger tumor
cell proliferation inhibition effect. The conjugate provided by the invention has the advantages of lower
toxicity to normal cells, higher activity to high-expression
somatostatin receptor tumor
cell lines and the like, and meanwhile, the administration mode of the oncolytic peptide can be optimized, so that the conjugate has a good practical application value.