N - 4909类似物的合成。第一部分。人肝癌G2细胞中载脂蛋白E分泌的刺激剂。

Synthesis of N-4909 analogs. Part I. A stimulant of apolipoprotein E secretion in human hepatoma G2 cells.

作者信息

Yanai M, Suzuki M, Kawamura K, Oshida N, Hiramoto S, Yasuda O, Shingai A, Suguro T

机构信息

Pharmaceutical Research Laboratories, Nisshin Flour Milling Co, Ltd, Iruma-gun, Saitama, Japan.

出版信息

J Antibiot (Tokyo). 2000 Dec;53(12):1385-96. doi: 10.7164/antibiotics.53.1385.

DOI:10.7164/antibiotics.53.1385

PMID:11217804

Abstract

Analogs of N-4909 (1), which had a stimulating activity for apolipoprotein E (apo E) secretion in Human hepatoma Hep G2 cells, were prepared and their activities examined. Cyclic analogs which had different kinds of amino acids or different number of amino acids from N-4909 (1) showed less effect on apo E secretion from Hep G2 cells. The length of acyl chain was found to be an important factor for the activity. Shorter chain reduced the activity. Linear analogs were also prepared. One of their analogs, N-5849 (17), which had six amino acids was found to have strong activity.

摘要

制备了对人肝癌Hep G2细胞中载脂蛋白E（apo E）分泌具有刺激活性的N - 4909（1）类似物，并检测了它们的活性。与N - 4909（1）相比，具有不同种类氨基酸或不同氨基酸数量的环状类似物对Hep G2细胞中apo E分泌的影响较小。发现酰基链的长度是影响活性的一个重要因素。较短的链会降低活性。还制备了线性类似物。发现它们的一种具有六个氨基酸的类似物N - 5849（17）具有较强的活性。