Department of Pharmaceutical Sciences, College of Pharmacy, University of Illinois at Chicago, Chicago, IL, 60612, USA.
J Antibiot (Tokyo). 2020 Aug;73(8):526-533. doi: 10.1038/s41429-020-0301-x. Epub 2020 Mar 31.
Two laxaphycin type-B cyclic dodecapeptides, laxaphycins B5 and B6, were obtained from UIC 10484, a freshwater cf. Phormidium sp. Analysis using the 16S rRNA sequence found UIC 10484 to clade with UIC 10045, a known laxaphycin type-A and -B producer, and MS/MS analysis revealed the presence of two novel laxaphycin type-B compounds. The structures of the metabolites were elucidated using 2D NMR and MS/MS. The absolute configurations of the amino acids were determined by advanced Marfey's analysis. Both metabolites were evaluated against the same three cancer cell lines. The IC of both laxaphycins B5 and B6 was near 1 μM against breast cancer MDA-MB-231, melanoma MDA-MB-435, and ovarian cancer OVCAR3 cell lines.
从淡水 cf. 藻属 UIC 10484 中获得了两种松弛素 B 型环十二肽 laxaphycins B5 和 B6。通过 16S rRNA 序列分析,发现 UIC 10484 与已知的松弛素 A 型和 B 型产生菌 UIC 10045 聚类,MS/MS 分析显示存在两种新型松弛素 B 型化合物。使用 2D NMR 和 MS/MS 阐明了代谢物的结构。通过高级 Marfey 分析确定了氨基酸的绝对构型。两种代谢产物均针对三种相同的癌细胞系进行了评估。松弛素 B5 和 B6 的 IC 对乳腺癌 MDA-MB-231、黑色素瘤 MDA-MB-435 和卵巢癌细胞系 OVCAR3 的抑制作用均接近 1 μM。