从补骨脂果实中​​分离得到 19 种黄酮类化合物，其中包括一种新型黄烷醇 (3) 和三种新型异黄酮 (12-14)。通过综合光谱数据分析明确确定了它们的化学结构。使用 MTT 测定在体外评估分离的黄酮类化合物的抗增殖作用。采用分子对接和ELISA测定活性化合物对ALK5的抑制作用。通过伤口愈合测定和 Transwell 小室测定，发现异巴伐查尔酮可抑制 A549 细胞中 TGF-β1 诱导的 EMT。免疫荧光和Western blot检测结果显示，IBC能够抑制TGF-β1诱导的A549细胞的细胞骨架重排，降低ALK5、ERK和Smad的磷酸化，下调Snail的表达，上调E-cadherin的表达，从而发挥抗肿瘤作用。对 A549 细胞上皮间质转化 (EMT) 过程的潜在抑制作用。本文提出的研究结果为研究补骨脂素类黄酮在人类非小细胞肺癌中的抗增殖和抗转移特性奠定了基础。版权所有 © 2024。由 Elsevier Inc. 出版。

Nineteen flavonoids were isolated from the fruits of Psoralea corylifolia L., including a novel flavanol (3) and three novel isoflavones (12-14). Their chemical structures were unequivocally determined through comprehensive spectral data analysis. The anti-proliferative effect of the isolated flavonoids was assessed in vitro using the MTT assay. Molecular docking and ELISA were employed to determine the inhibitory effects of the active compounds on ALK5. Isobavachalcone was found to inhibit TGF-β1 induced EMT in A549 cells by Wound healing assay and Transwell chamber assay. Immunofluorescence assay and Western blot assay showed that IBC could inhibit cytoskeleton rearrangement, reduce the phosphorylation of ALK5, ERK, and Smad, down-regulate Snail expression, and up-regulate E-cadherin expression in TGF-β1 induced A549 cells, thereby exerting the potential inhibitory effects on epithelial-mesenchymal transition (EMT) process in A549 cells. The findings presented herein establish a fundamental basis for investigating the anti-proliferative and anti-metastatic properties of psoralen flavonoids in human non-small cell lung cancer.Copyright © 2024. Published by Elsevier Inc.