鉴定 N-羟基肉桂酰胺类似物及其对乳腺癌细胞系的生物评价。
Identification of N-Hydroxycinnamamide analogues and their bio-evaluation against breast cancer cell lines.
机构信息
Department of Chemistry, Babasaheb Bhimrao Ambedkar University (A Central University), Lucknow 226025, UP, India.
Department of Dermatology, University of Wisconsin Madison, WI 53706, USA; Endocrinology Division, CSIR-Central Drug Research Institute (CDRI), Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India; Academy of Scientific and Innovative Research (AcSIR), CSIR-Central Drug Research Institute Campus, Lucknow 226031, India.
出版信息
Biomed Pharmacother. 2018 Nov;107:475-483. doi: 10.1016/j.biopha.2018.08.015. Epub 2018 Aug 11.
The present study demonstrates the identification of N-hydroxycinnamamide derivatives and their anticancer potential against human triple-negative breast cancer cell line MDA-MB‑231, MCF-7 and non-malignant origin cell line, HEK-293 (human embryonic kidney). MTT assay was studied with HEK-293 cell line. Anticancer potential of the N-hydroxycinnamamide derivatives were compared with marked drug Tamoxifen through in vitro study. The compound numbers 3b and 3h exhibit most potent activity against antagonistic breast cancer cells (MDA-MB-231) with IC13μM and 5μM respectively. Compound 3h promotes DNA fragmentation and induction of apoptosis. Furthermore, loss of mitochondrial membrane potential induced by compound 3h. The major mechanism of compound 3h for anti-breast cancer activity was probably initiation of reactive oxygen species (ROS) in cancer cells thereby persuading apoptotic cell deaths in cancer cells.
本研究鉴定了 N-羟基肉桂酰胺衍生物，并研究了它们对人三阴性乳腺癌细胞系 MDA-MB-231、MCF-7 和非恶性起源细胞系 HEK-293（人胚肾）的抗癌潜力。用 HEK-293 细胞系进行了 MTT 测定。通过体外研究，将 N-羟基肉桂酰胺衍生物的抗癌潜力与标记药物他莫昔芬进行了比较。化合物 3b 和 3h 对拮抗乳腺癌细胞（MDA-MB-231）表现出最强的活性，IC13μM 和 5μM 分别。化合物 3h 促进 DNA 片段化和诱导细胞凋亡。此外，化合物 3h 诱导线粒体膜电位丧失。化合物 3h 抗乳腺癌活性的主要机制可能是在癌细胞中引发活性氧（ROS），从而促使癌细胞发生凋亡性细胞死亡。
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