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胀果甘草中甘草查尔酮A和E的拓扑异构酶I抑制作用及细胞毒性

Topoisomerase I inhibition and cytotoxicity of licochalcones A and E from Glycyrrhiza inflata.

作者信息

Yoon Goo, Kang Bok Yun, Cheon Seung Hoon

机构信息

College of Pharmacy and Research Institute of Drug Development, Chonnam National University, 300 Yongbong-Dong, Buk-Gu, Gwangju 500-757, Korea.

出版信息

Arch Pharm Res. 2007 Mar;30(3):313-6. doi: 10.1007/BF02977611.

DOI:10.1007/BF02977611
PMID:17424936
Abstract

Licochalcones A (1) and E (2), retrochalcones or reversely constructed chalcones, isolated from the roots of Glycyrrhiza inflata, were evaluated for their cytotoxicities against four different human tumor cell lines; A549 (lung), SK-OV-3 (ovarian), SK-MEL-2 (melanoma) and HCT-15 (colon), using the sulforhodamine B (SRB) assay. The effects of these compounds toward the DNA topoisomerase I (topo I) inhibitory activity were also measured using the supercoiled DNA unwinding assay. All compounds showed moderate cytotoxicities against the four different human tumor cell lines and inhibited the topo I activity in dose-dependent manners. The inhibition of topo I by licochalcones A (1) and E (2) may explain the cytotoxicities of these compounds against the human tumor cell lines.

摘要

从胀果甘草根部分离得到的甘草查耳酮A(1)和E(2),即反式查耳酮或反向构建的查耳酮,采用磺酰罗丹明B(SRB)法评估了它们对四种不同人类肿瘤细胞系;A549(肺癌)、SK-OV-3(卵巢癌)、SK-MEL-2(黑色素瘤)和HCT-15(结肠癌)的细胞毒性。还使用超螺旋DNA解旋试验测量了这些化合物对DNA拓扑异构酶I(拓扑异构酶I)抑制活性的影响。所有化合物对四种不同人类肿瘤细胞系均表现出中等程度的细胞毒性,并以剂量依赖性方式抑制拓扑异构酶I活性。甘草查耳酮A(1)和E(2)对拓扑异构酶I的抑制作用可能解释了这些化合物对人类肿瘤细胞系的细胞毒性。

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