LIPIDIC CONJUGATES OF LUTEINIZING-HORMONE-RELEASING HORMONE (LHRH)+ AND THYROTROPIN-RELEASING-HORMONE (TRH)+ THAT RELEASE AND PROTECT THE NATIVE HORMONES IN HOMOGENATES OF HUMAN INTESTINAL EPITHELIAL (CACO-2) CELLS

被引:51
|
作者
TOTH, I [1 ]
FLINN, N [1 ]
HILLERY, A [1 ]
GIBBONS, WA [1 ]
ARTURSSON, P [1 ]
机构
[1] UNIV UPPSALA,BIOMEDICUM,S-75123 UPPSALA,SWEDEN
关键词
LIPIDIC AMINO ACID; LIPIDIC PEPTIDE; DRUG DELIVERY; LHRH; TRH; CACO-2 CELL HOMOGENATE; ENZYME DEGRADATION;
D O I
10.1016/0378-5173(94)90108-2
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The enzymatically labile peptides LHRH and TRH were conjugated to various lipidic peptides. The conjugates and free peptides were incubated with Caco-2 cell homogenates and their respective degradation profiles were studied following incubation. Conjugation to lipidic peptides increased the half-life of LHRH and TRH. The Caco-2 cell homogenates were capable of cleaving the conjugated lipidic peptide, to release the parent LHRH or TRH. The released LHRH or TRH subsequently demonstrated a longer half-life than when present alone in the incubation mixture, suggesting that the cleaved lipidic peptide is capable of inhibiting enzymes.
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页码:241 / 247
页数:7
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