This invention relates to the field of
biopharmaceutical technology, providing a self-assembled
peptide-rhein conjugate, its formulation, preparation method, and applications. The MMP-9-responsive self-assembled
peptide-rhein conjugate of this invention, with the sequence Rhein-GFFPLGLAGACE, can respond to abnormally activated MMP-9 in atherosclerotic plaques, self-assembling in situ into a stable
nanofiber structure at the
lesion site. The rhein in this conjugate exhibits significant anti-inflammatory and
antioxidant functions, but its water
solubility and oral
bioavailability are low. These are significantly improved after conjugation with the
peptide, achieving targeted delivery and prolonging
retention time. The introduction of the
tripeptide ACE, which mimics the function of
glutathione, further enhances the conjugate's ability to
resist oxidative stress. Furthermore, this conjugate exhibits excellent anti-inflammatory and
antioxidant effects,
scavenging ROS, inhibiting
inflammatory pathways, regulating macrophage
phenotype, and inhibiting
apoptosis, providing a new strategy for the treatment of atherosclerosis.