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Abstract：
Anithiactin D (1), a 2-phenylthiazole class of natural products, was isolated from marine mudflat-derived actinomycetes Streptomyces sp. 10A085. The chemical structure of 1 was elucidated based on the interpretation of NMR and MS data. The absolute configuration of 1 was determined by comparing the experimental and calculated electronic circular dichroism (ECD) spectral data. Anithiactin D (1) significantly decreased cancer cell migration and invasion activities at a concentration of 5 μM via downregulation of the epithelial-to-mesenchymal transition (EMT) markers in A549, AGS, and Caco-2 cell lines. Moreover, 1 inhibited the activity of Rho GTPases, including Rac1 and RhoA in the A549 cell line, suppressed RhoA in AGS and Caco-2 cell lines, and decreased the mRNA expression levels of some matrix metalloproteinases (MMPs) in AGS and Caco-2 cell lines. Thus 1, which is a new entity of the 2-phenylthiazole class of natural products with a unique aniline-indole fused moiety, is a potent inhibitor of the motility of cancer cells.
摘要：
AnithiactinD(1)，2-苯基噻唑类天然产物，是从海洋泥滩衍生的放线菌链霉菌中分离出来的。10A085.基于NMR和MS数据的解释阐明1的化学结构。通过比较实验和计算的电子圆二色性(ECD)光谱数据来确定1的绝对构型。AnithiactinD（1）通过下调A549，AGS中的上皮-间质转化（EMT）标志物，在5μM的浓度下显着降低了癌细胞的迁移和侵袭活性，和Caco-2细胞系。此外，1抑制RhoGTPases的活性，包括A549细胞系中的Rac1和RhoA，在AGS和Caco-2细胞系中抑制RhoA，并降低了AGS和Caco-2细胞系中某些基质金属蛋白酶（MMPs）的mRNA表达水平。因此，1是具有独特的苯胺-吲哚稠合部分的2-苯基噻唑类天然产物的新实体，是癌细胞运动性的有效抑制剂。
