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学科主题: 药学
题名:
Novel N-(3-carboxyl-9-benzylcarboline-1-yl) ethylamino acids: synthesis, anti-proliferation activity and two-step-course of intercalation with calf thymus DNA
作者: Wu, Jianhui; Cui, Guohui; Zhao, Ming; Cui, Chunying; Peng, Shiqi
刊名: MOLECULAR BIOSYSTEMS
发表日期: 2007
DOI: 10.1039/b712092n
卷: 3, 期:12, 页:855-861
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemistry & Molecular Biology
研究领域[WOS]: Biochemistry & Molecular Biology
关键词[WOS]: BOVINE SERUM-ALBUMIN ; BETA-CARBOLINE ; ANTINEOPLASTIC AGENTS ; BIOLOGICAL-ACTIVITY ; CYTOTOXIC ACTIVITY ; CRYSTAL-STRUCTURE ; ANTITUMOR AGENTS ; IN-VITRO ; BINDING ; DERIVATIVES
英文摘要:

To explore the intercalating mechanism of beta-carbolines, four novel N-(3-carboxyl-9-benzylcarboline-1-yl)ethylamino acids [-phenylalanine (6a), -alanine (6b), -isoleucine (6c) and -glycine (6d)] were prepared here. Their in vitro anticancer activities were examined by their anti-proliferation for 5 human carcinoma cell lines. The average IC(50)s against 5 human carcinoma cell lines are 53.54 mu M, 118.77 mu M, 147.34 mu M and greater than 291.63 mu M for 6a, 6b, 6c and 6d, respectively. The DNA intercalating mechanism of 6a-d was approved by the comparison of the parameters and signals of UV, CD and fluorescence spectra of calf thymus DNA (CT DNA) alone and the CT DNA/6a-d system. Using fluorescence titration based kinetic analysis a two-step-course consisting of stacking and intercalating was described and the stacking was considered as the key step to the CT DNA intercalating mechanism of 6a-d. Using fluorescence titration based thermomechanical analysis, the stacking complexes of 6a-d with CT DNA were described to be formed spontaneously and to be stabilized predominantly by their hydrophobic interactions. The intercalation itself goes very fast and only has limited contribution to their anticancer activities.

语种: 英语
WOS记录号: WOS:000250932100014
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/67390
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
2.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100069, Peoples R China

Recommended Citation:
Wu, Jianhui,Cui, Guohui,Zhao, Ming,et al. Novel N-(3-carboxyl-9-benzylcarboline-1-yl) ethylamino acids: synthesis, anti-proliferation activity and two-step-course of intercalation with calf thymus DNA[J]. MOLECULAR BIOSYSTEMS,2007,3(12):855-861.
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