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标题：Effect of Modification of the Carboxyl Groups of the Sialic Acid Binding Lectin from Bullfrog (Rana catesbeiana) Oocyte on Anti-tumor Activity
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作者：Masanori IWAMA ; Yuko OGAWA ; Noriko SASAKI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2001
卷号：24
期号：9
页码：978-981
DOI：10.1248/bpb.24.978
出版社：The Pharmaceutical Society of Japan
摘要：The sialic acid binding lectin from bullfrog Rana catesbeiana oocyte (cSBL) is known to have anti-tumor activity. In order to investigate the relationship between the net charge of cSBL and its anti-tumor effect, cSBL was modified with a water-soluble carbodiimide (EDC) in the presence of three kinds of nucleophiles, taurine, glycine methylester and ethylenediamine. cSBL having four carboxyl groups was partially modified (ca. 2 residues). The anti-tumor activity of modified cSBLs was in the order of ethylenediamine-modified cSBL>glycine methylester-modified cSBL>taurine modified cSBL≥native cSBL. The results suggested that anti-tumor activity seems to increase with the increase in positive net charge, possibly enhancing the interaction of cSBL with sialoglycoprotein on the surface of tumor cells. The ribonuclease activity of ethylenediamine-modified cSBL decreased with the progress of the reaction, but the number of internalized molecules in the tumor cell increased. Thus, for anti-tumor activity, a higher incorporation of cSBL with reasonable RNase activity seems to be more important than total RNase activity.
关键词：anti-tumor agent;ribonuclease;sialic acid binding protein;carbodiimide;chemical modification;carboxyl group