来自……的细胞毒性肽抗生素
Cytotoxic Peptaibols from .
作者信息
Park Yun Seo, Kim Eun-Sook, Deyrup Stephen T, Lee Jin Woo, Shim Sang Hee
机构信息
Natural Products Research Institute, College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea.
College of Pharmacy, Duksung Women's University, Seoul 01369, Republic of Korea.
出版信息
J Nat Prod. 2024 Aug 23;87(8):2081-2094. doi: 10.1021/acs.jnatprod.4c00590. Epub 2024 Jul 22.
Five new lipopeptaibols (-) and eight new 19-residue peptaibols (-) along with two known lipopeptaibols, lipovelutibols C () and D () were isolated from . The planar structures of the newly discovered peptaibols (-, -) were elucidated using 1D and 2D NMR, and UPLC-MS/MS data. The absolute configurations for new peptaibols (-, -) were elucidated using the advanced Marfey's method and GITC (2,3,4,6-tetra--acetyl-β-d-glucopyranosyl isothiocyanate) derivatization. Through analysis of CD spectra, these peptabols were found to have right-handed helical conformations. While most of the new compounds were significantly more active than the positive control, , , , and containing Ser and Leu at positions 10 and 11, respectively, were the most cytotoxic against MDA-MB-231, SNU449, SKOV3, DU145, and HCT116 cancer cell lines, and the 19-residue peptaibols were generally more potent than lipopeptaibols.
从……中分离出了5种新的脂肽抗生素（-）和8种新的19个残基的肽抗生素（-），以及两种已知的脂肽抗生素，脂velutibols C（）和D（）。利用一维和二维核磁共振以及超高效液相色谱-串联质谱数据阐明了新发现的肽抗生素（-，-）的平面结构。使用先进的马尔费方法和GITC（2,3,4,6-四-O-乙酰基-β-D-吡喃葡萄糖基异硫氰酸酯）衍生化阐明了新肽抗生素（-，-）的绝对构型。通过对圆二色谱的分析，发现这些肽抗生素具有右手螺旋构象。虽然大多数新化合物的活性明显高于阳性对照，但分别在第10位和第11位含有丝氨酸和亮氨酸的……、……、……和……对MDA-MB-231、SNU449、SKOV3、DU145和HCT116癌细胞系的细胞毒性最强，并且19个残基的肽抗生素通常比脂肽抗生素更有效。
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