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Preparation of a monoPEGylated derivative of cyanovirin-N and its virucidal effect on acyclovir-resistant strains of herpes simplex virus type 1

Lookup NU author(s): Dr Long Xie


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© 2019, Springer-Verlag GmbH Austria, part of Springer Nature. The long-term administration of acyclovir (ACV) for therapy against herpes simplex virus type 1 (HSV-1) infections can result in the emergence of ACV-resistant HSV strains. It is therefore urgent to develop new anti-herpetic compounds with mechanisms that differ from that of ACV. Cyanovirin-N (CV-N) is an antiviral agent that has an inhibitory effect on HSV-1 infections, and PEGylation of CV-N is potentially useful for pharmaceutical applications. Here, a (Gly 4 Ser) 3 linker molecule was attached to the N-terminus of CV-N, and the resulting compound, linker-CV-N (LCV-N), was produced on a pilot scale with purity up to 95%. Then, PEG 10k -LCV-N was synthesized by modifying at the α-amine group of the N-terminus of LCV-N with 10-kDa polyethylene glycol propionaldehyde (mPEG-ALD). CV-N, LCV-N and PEG 10k -LCV-N were all found to have potent inhibitory activity against ACV-resistant HSV strains with IC 50 values in the nM range. LCV-N was the most potent of these three compounds against both normal and ACV-resistant HSV strains. Although PEG 10k -LCV-N showed less antiviral activity than CV-N and LCV-N, it still exhibited significant and universal virucidal activity against drug-resistant viruses. The toxicity and immunogenicity of PEG 10k -LCV-N were dramatically lower than those of CV-N and LCV-N. In conclusion, we suggest that LCV-N and PEG 10k -LCV-N are promising and safe microbicides for the control and/or treatment of ACV-resistant HSV infection.

Publication metadata

Author(s): Lei Y, Chen W, Liang H, Wang Z, Chen J, Hong H, Xie L, Nie H, Xiong S

Publication type: Article

Publication status: Published

Journal: Archives of Virology

Year: 2019

Volume: 164

Issue: 5

Pages: 1259-1269

Print publication date: 01/05/2019

Online publication date: 23/03/2019

Acceptance date: 13/11/2018

ISSN (print): 0304-8608

ISSN (electronic): 1432-8798

Publisher: Springer Vienna


DOI: 10.1007/s00705-018-04118-4


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