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脱氢姜酮、查耳酮和异丁香酚类似物作为体外抗癌剂。

Dehydrozingerone, chalcone, and isoeugenol analogues as in vitro anticancer agents.

作者信息

Tatsuzaki Jin, Bastow Kenneth F, Nakagawa-Goto Kyoko, Nakamura Seiko, Itokawa Hideji, Lee Kuo-Hsiung

机构信息

Natural Products Research Laboratories, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599-7360, USA.

出版信息

J Nat Prod. 2006 Oct;69(10):1445-9. doi: 10.1021/np060252z.

DOI:10.1021/np060252z
PMID:17067159
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2532514/
Abstract

Twenty-eight compounds related to dehydrozingerone (1), isoeugenol (3), and 2-hydroxychalcone (4) were synthesized and evaluated in vitro against human tumor cell replication. Except for isoeugenol analogues 27-35, most compounds exhibited moderate or strong cytotoxic activity against KB, KB-VCR (a multidrug-resistant derivative), and A549 cell lines. In particular, chalcone 15 showed significant cytotoxic activity against the A549 cell line with an IC50 value of 0.6 microg/mL. Furthermore, dehydrozingerone analogue 11 and chalcones 16 and 17 showed significant and similar cytotoxic activity against both KB (IC50 values of 2.0, 1.0, and 2.0 microg/mL, respectively) and KB-VCR (IC50 values of 1.9, 1.0, and 2.0 microg/mL, respectively) cells, suggesting that they are not substrates for the P-glycoprotein drug efflux pump.

摘要

合成了28种与脱氢姜酮（1）、异丁香酚（3）和2-羟基查耳酮（4）相关的化合物，并对其进行体外抗人肿瘤细胞复制活性评估。除异丁香酚类似物27 - 35外，大多数化合物对KB、KB - VCR（一种多药耐药衍生物）和A549细胞系表现出中度或强细胞毒性活性。特别是，查耳酮15对A549细胞系表现出显著的细胞毒性活性，IC50值为0.6μg/mL。此外，脱氢姜酮类似物11以及查耳酮16和17对KB（IC50值分别为2.0、1.0和2.0μg/mL）和KB - VCR（IC50值分别为1.9、1.0和2.0μg/mL）细胞均表现出显著且相似的细胞毒性活性，表明它们不是P - 糖蛋白药物外排泵的底物。

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