Journal
BIOTECHNOLOGY LETTERS
Volume 32, Issue 7, Pages 883-890Publisher
SPRINGER
DOI: 10.1007/s10529-010-0242-8
Keywords
Acute toxicity; Alpha-momorcharin; Anti-tumor activity; Immunogenicity; PEGylation
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Funding
- National Science Foundation of China [30770232]
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Alpha-momorcharin (alpha-MMC) is a ribosome-inactivating protein (RIP) with excellent cytotoxicity to tumor cells. However, its strong immunogenicity and short plasma half-life limit its clinical applications. To overcome this, we have to PEGylated alpha-MMC using a branched 20 kDa (mPEG) (2)-Lys-NHS. Homogeneous mono-, di- and tri-PEGylated alpha-MMCs were synthesized, purified and characterized. In vitro and in vivo analysis indicated that the serial PEG-conjugates preserved moderate anti-tumor activity with 36% acute toxicity and at most 66% immunogenicity decrease. These results suggested the potential application of alpha-MMC-PEG conjugates as an anti-tumor agent.
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