Multivalent zanamivir-bovine serum albumin conjugate as a potent influenza neuraminidase inhibitor

A multivalent Zanamivir (ZA) conjugate as new anti-influenza agent was prepared. Specifically, multiple copies of ZA with a C7 azido-terminated linker were covalently attached onto alkyne-modified bovine serum albumin (BSA) via copper-free click reaction. The loading number of ZA was determined by MALDI-TOF. Primary neuraminidase (NA) inhibition assay showed that this conjugate retained some NA inhibitory activity compared to its parent ZA monomer. Moreover, the ZA-BSA conjugate was not cytotoxic with concentrations up to 1 µM.