Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Chemistry and Anti-tumor Activity of Sperabillin Polymers
Tsuneaki HIDAShigetoshi TSUBOTANIAkira HORIMorio MURAKAMIHideaki NATSUGARIYoshio KOZAISetsuo HARADA
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JOURNAL FREE ACCESS

1993 Volume 41 Issue 5 Pages 889-893

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Abstract
Sperabillin A, 3-[[(3R, 5R)-3-amino-6-[(2E, 4Z)-2, 4-hexadienoylamino]-5-hydroxyhexanoyl]amino]propanamidine dihydrochloride, was polymerized on standing for several days under a highly humid atmosphere or in the presence of radical initiators. The average molecular weight of the polymers obtained could be regulated by changing the reaction conditions in the latter case. Spectral analyses of the polymers revealed that the 2, 4-hexadienoyl moiety of sperabillins was polymerized in a free radical-initiated reaction. The polymers selectively inhibited the proliferation of human umbilical vein endothelial (HUVE) cells. Polymers having higher molecular weight showed stronger inhibition of HUVE cell proliferation. In addition, the polymers showed anti-tumor activity against B16 melanoma in vivo.
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© The Pharmaceutical Society of Japan
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