鲨烯环氧酶抑制剂，一种新型细胞毒环壬肽。

Sclerin, a New Cytotoxic Cyclononapeptide from .

机构信息

Faculty of Bioanalysis, Veracruz University, Iturbide s/n, Veracruz 91700, Mexico.

Food Research and Development Unit, Tecnológico Nacional de México-I T Veracruz-UNIDA. M.A. de Quevedo 2779, Col. Formando Hogar Veracruz Ver. C.P., Mexico 91860, Mexico.

出版信息

Molecules. 2019 Feb 3;24(3):554. doi: 10.3390/molecules24030554.

DOI:10.3390/molecules24030554

PMID:30717439

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6384883/

Abstract

A new cytotoxic cyclononapeptide, sclerin, cyclo(⁻Dab⁻Ser⁻Tyr⁻Gly⁻Thr⁻Val⁻Ala⁻ Ile⁻Pro⁻) (), was isolated from the methanol extract of the seeds of , together with the known metabolite, cyclosenegalin A, cyclo(⁻Pro⁻Gly⁻Leu⁻Ser⁻Ala⁻Val⁻Thr⁻) (). The planar structures for the two compounds were established by comprehensive analysis of NMR and ESI-HRMS data, and the absolute stereochemistry was stablished by Marfey's method. Compound showed moderate cytotoxic activity against the human prostate carcinoma cell line DU-145 at µM concentration.

摘要

一种新的细胞毒性环壬肽，sclerin，环（⁻Dab⁻Ser⁻Tyr⁻Gly⁻Thr⁻Val⁻Ala⁻Ile⁻Pro⁻）（），是从的种子甲醇提取物中分离出来的，同时还分离到了已知的代谢产物环森那格列林 A，环（⁻Pro⁻Gly⁻Leu⁻Ser⁻Ala⁻Val⁻Thr⁻）（）。这两个化合物的平面结构通过 NMR 和 ESI-HRMS 数据的综合分析确定，绝对立体化学通过 Marfey 法确定。化合物在 µM 浓度下对人前列腺癌细胞系 DU-145 表现出中等的细胞毒性活性。