设计环戊烯酮前列腺素衍生物作为促进中枢神经系统大鼠儿茶酚胺能神经元细胞系CAD细胞神经突生长的化合物。

Designed cyclopentenone prostaglandin derivatives as neurite outgrowth-promoting compounds for CAD cells, a rat catecholaminergic neuronal cell line of the central nervous system.

作者信息

Satoh T, Furuta K, Tomokiyo K, Suzuki M, Watanabe Y

机构信息

Department of Neuroscience, Osaka Bioscience Institute, Suita-shi, 565-0874, Osaka, Japan.

出版信息

Neurosci Lett. 2000 Sep 22;291(3):167-70. doi: 10.1016/s0304-3940(00)01403-8.

DOI:10.1016/s0304-3940(00)01403-8

PMID:10984633

Abstract

Here we reported the effects of neurite outgrowth-promoting prostaglandins (NEPP's) on neurons of the central nervous system (CNS). Serum deprivation promoted neurite outgrowth from CAD cells, a CNS-derived cathecholaminergic neuronal cell line. NEPP's (0.05-0.2 microM) accelerated the neurite outgrowth from CAD cells in serum-free medium but didn't in serum-containing medium. Through the study of structure-function relationship with the NEPP's 1-10, NEPP 10 (13,14-dihydro-15-epi-Delta(7)-prostaglandin A(1) (methyl ester) revealed the best compound, exhibiting potent neurite outgrowth-promoting activity with minimal cytotoxicity, suggesting that it is the best compound for drug development.

摘要

在此，我们报告了促神经突生长前列腺素（NEPP）对中枢神经系统（CNS）神经元的影响。血清剥夺促进了CAD细胞（一种源自中枢神经系统的儿茶酚胺能神经元细胞系）的神经突生长。NEPP（0.05 - 0.2微摩尔）在无血清培养基中加速了CAD细胞的神经突生长，但在含血清培养基中则没有。通过对NEPP 1 - 10的结构-功能关系研究，NEPP 10（13,14 - 二氢-15 - 表-Δ(7)-前列腺素A(1)（甲酯）显示出最佳的化合物特性，具有强大的促神经突生长活性且细胞毒性最小，表明它是药物开发的最佳化合物。