罗米肽 A 的简便制备与晶体结构。

A facile preparation and crystal structure of romipeptide A.

机构信息

Life Science and Biotechnology Research Center, School of Life Science, Northeast Agricultural University, Harbin, 150030, China.

Taizhou Vocational College of Science and Technology, Taizhou, 318000, China.

出版信息

J Antibiot (Tokyo). 2022 Jan;75(1):48-50. doi: 10.1038/s41429-021-00487-2. Epub 2021 Nov 26.

DOI:10.1038/s41429-021-00487-2

PMID:34824376

Abstract

A double disulfide tethering depsipeptide dimer, romipeptide A (1) was prepared by NaOH catalyzed dimerization of romidepsin. Its structure was determined by analysis of NMR and HR-ESI-MS data as well as single crystal X-ray diffraction. Bioassay results showed that 1 exhibited good cytotoxic activity against two tumor cell lines B16 and HCT116. This study reported the single crystal data of 1 for the first time. The facile preparation of 1 afforded enough amount for its further biological evaluations.

摘要

一种双硫键连接的二聚肽二聚体罗米肽 A（1）是通过罗米地辛的 NaOH 催化二聚化制备的。其结构通过 NMR 和 HR-ESI-MS 数据以及单晶 X 射线衍射分析确定。生物测定结果表明，1 对两种肿瘤细胞系 B16 和 HCT116 表现出良好的细胞毒性活性。本研究首次报道了 1 的单晶数据。1 的简便制备方法提供了足够的量，可用于进一步的生物学评估。