SYNTHESIS AND ANTITUMOR-ACTIVITY OF 6-O-CARBOXYMETHYL CHITIN FIXING 5-FLUOROURACILS THROUGH PENTAMETHYLENE, MONOMETHYLENE SPACER GROUPS VIA AMIDE, ESTER BONDS

被引:12
作者
OHYA, Y
INOSAKA, K
OUCHI, T
机构
[1] Department Of Applied Chemistry, Faculty Of Engineering, Kansai University, Osaka 564, Suita
关键词
6-O-CARBOXYMETHYL CHITIN; 5-FLUOROURACIL; DRUG DELIVERY SYSTEM; MACROMOLECULAR PRODRUG; ANTITUMOR ACTIVITY; P388; LYMPHOCYTIC-LEUKEMIA;
D O I
10.1248/cpb.40.559
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In order to provide the water-soluble and biodegradable macromolecular prodrug of 5-fluorouracil (5FU), the fixation of 5FUs to 6-O-carboxymethyl chitin(CM-chitin) through pentamethylene, monomethylene spacer groups via amide, ester bonds was carried out. The obtained CM-chitin/5FU conjugate showed the slow release of 5FU and exhibited remarkable antitumor activity against P388 lymphocytic leukemia in mice by intraperitoneal(i.p.) implantation / i.p. injection.
引用
收藏
页码:559 / 561
页数:3
相关论文
共 10 条
[1]  
BOSCH L, 1958, CANCER RES, V18, P335
[2]  
BOUNOUS G, 1978, INT J CLIN PHARM BI, V16, P519
[3]  
MYERS CE, 1981, PHARMACOL REV, V1, P33
[4]  
OHYA Y, 1991, REACT POLYM, V15, P156
[5]  
Ouchi T, 1990, Drug Des Deliv, V6, P281
[6]  
OUCHI T, 1989, MAKROMOL CHEM, V190, P1817
[7]  
Ouchi T., 1989, J BIOACT COMPAT POLY, V4, P362
[8]  
SIRICA AE, 1971, J NATL CANCER I, V47, P377
[9]   EFFECT OF N-ACETYLCHITO-OLIGOSACCHARIDES ON ACTIVATION OF PHAGOCYTES [J].
SUZUKI, K ;
TOKORO, A ;
OKAWA, Y ;
SUZUKI, S ;
SUZUKI, M .
MICROBIOLOGY AND IMMUNOLOGY, 1986, 30 (08) :777-787
[10]  
WAXMAN S, 1982, CLIN INTERPRETATION, P32