PEGylation of alpha-momorcharin: synthesis and characterization of novel anti-tumor conjugates with therapeutic potential.

Abstract

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.

• Authors: Xiaoxiao Bian, Fubing Shen, Yiwen Chen, Baoning Wang, Mian Deng, Yanfa Meng
• Journal: Biotechnology letters (Biotechnol Lett) Vol. 32 Issue 7 Pg. 883-90 (Jul 2010) ISSN: 1573-6776 [Electronic] Netherlands
• PMID: 20238144 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Polyethylene Glycols
• MMC protein, Momordica charantia
• Ribosome Inactivating Proteins

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, immunology, pharmacology, toxicity)
• Cell Line, Tumor
• Humans
• Lethal Dose 50
• Mice
• Mice, Inbred BALB C
• Polyethylene Glycols (chemistry, pharmacology, toxicity)
• Rabbits
• Ribosome Inactivating Proteins (chemistry, immunology, pharmacology, toxicity)