N-乳酰鞘氨醇和N-乳酰二氢鞘氨醇的合成及其强效抗白血病活性

Synthesis and potent antileukemic activities of N-lactylsphingosine and N-lactyldihydrosphingosine.

作者信息

Azuma Hideki, Takao Ryoko, Shikata Keiji, Niiro Hayato, Tachibana Taro, Ogino Kenji

机构信息

Department of Applied & Bioapplied Chemistry, Graduate School of Engineering, Osaka City University, Sugimoto 3-3-138, Sumiyoshi-ku, Osaka 558-8585, Japan.

出版信息

J Med Chem. 2003 Jul 31;46(16):3445-7. doi: 10.1021/jm030125p.

DOI:10.1021/jm030125p

PMID:12877580

Abstract

N-(R)- and N-(S)-lactylsphingosine and their corresponding dihydrosphingosine derivatives were synthesized. The antileukemic activities of these compounds were measured by MTT (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide) assay in human leukemia HL-60 cells. N-(R)- and N-(S)-Lactylsphingosine displayed higher activities than N-acetylsphingosine (C2-ceramide, a well-known apoptosis inducer), and their dihydrosphingosine derivatives had slight activities.

摘要

合成了N-(R)-和N-(S)-乳酰鞘氨醇及其相应的二氢鞘氨醇衍生物。通过MTT（3-(4,5-二甲基-2-噻唑基)-2,5-二苯基-2H-溴化四氮唑）法在人白血病HL-60细胞中测定了这些化合物的抗白血病活性。N-(R)-和N-(S)-乳酰鞘氨醇表现出比N-乙酰鞘氨醇（C2-神经酰胺，一种著名的凋亡诱导剂）更高的活性，并且它们的二氢鞘氨醇衍生物具有轻微活性。