具有 N-乙酰葡萄糖胺的三萜皂苷的合成及细胞毒性活性。

Synthesis and cytotoxic activity of the N-acetylglucosamine-bearing triterpenoid saponins.

机构信息

School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.

出版信息

Carbohydr Res. 2010 Mar 30;345(5):607-20. doi: 10.1016/j.carres.2010.01.002. Epub 2010 Jan 7.

DOI:10.1016/j.carres.2010.01.002

PMID:20116049

Abstract

Fourteen ursolic acid and oleanolic acid saponins with N-acetyl-beta-D-glucosamine, and (1-->4)-linked and (1-->6)-linked N-acetyl-beta-D-glucosamine oligosaccharide residues were synthesized in a convergent manner. The structures of all compounds were confirmed by (1)H NMR and (13)C NMR spectroscopy and by mass spectrometry, and their cytotoxic activities were assayed in three cancer cell lines. Only oleanolic acid-3-yl beta-D-GluNAc showed significant cytotoxicity against HL-60 and BGC-823.

摘要

十四种齐墩果酸和熊果酸皂苷与 N-乙酰-β-D-葡萄糖胺以及（1-->4）-连接和（1-->6）-连接的 N-乙酰-β-D-葡萄糖胺低聚糖残基以汇聚方式合成。所有化合物的结构均通过（1）H NMR 和（13）C NMR 光谱以及质谱法得到确认，并在三种癌细胞系中测定了它们的细胞毒性。只有齐墩果酸-3-基-β-D-GluNAc 对 HL-60 和 BGC-823 具有显著的细胞毒性。