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Incorporation of nitric oxide donor into 1,3-dioxyxanthones leads to synergistic anticancer activity.

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收录情况： ◇ SCIE

作者：
Liu Jie[a,d] * ; Zhang Cao[a] ; Wang Huailing[b] ; Zhang Lei[a] ; Jiang Zhenlei[a] ; Zhang Jianrun[a] ; Liu Zhijun[a] ; Chen Heru[a,c,*1] ;
机构： [a]Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China [b]School of Food Sciences and Engineering, South China University of Technology, Guangzhou 510641, China [c]Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Jinan University, Guangzhou 510632, PR China [d]Department of Allergy, The Third Affiliated Hospital of Shenzhen University, Shenzhen 518020, PR China
出处：
DOI： 10.1016/j.ejmech.2018.03.072
ISSN：

关键词： Xanthones Nitrates Ati-Cancer Synergistic effect p53/MDM2

摘要：
Fifty 1,3-dioxyxanthone nitrates (4a ∼ i-n, n = 1-6) were designed and synthesized based on molecular similarity strategy. Incorporation of nitrate into 1,3-dioxyxanthones with electron-donating groups at 6-8 position brought about synergistic anticancer effect. Among them, compound 4g-4 was confirmed the most active agent against HepG-2 cells growth with an IC50 of 0.33 ± 0.06 μM. It dose-dependently increased intramolecular NO levels. This activity was attenuated by either NO scavenger PTIO or mitochondrial aldehyde dehydrogenase (mtADH) inhibitor PCDA. Apoptosis analysis indicated different contributions of early/late apoptosis and necrosis to cell death for different dose of 4g-4. 4g-4 arrested more cells on S phase. Results from Western Blot implied that 4g-4 regulated p53/MDM2 to promote cancer cell apoptosis. All the evidences support that 4g-4 is a promising anti-cancer agent. Copyright © 2018 Elsevier Masson SAS. All rights reserved.

基金：
This research was financially supported by Guangdong Provincial Project of Science and Technology (No. 2015A030311012), the Guangzhou Project of Science and Technology (No. 201607010215), and the Fundamental Research Funds for the Central Universities (11615323).
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外文
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中科院(CAS)分区：
出版当年[2017]版：
大类 | 2 区 化学
小类 | 1 区 药物化学
最新[2025]版：
大类 | 2 区 医学
小类 | 1 区 药物化学
JCR分区：
出版当年[2016]版：
Q1 CHEMISTRY, MEDICINAL
最新[2023]版：
Q1 CHEMISTRY, MEDICINAL

影响因子： 最新[2023版] 最新五年平均 出版当年[2016版] 出版当年五年平均 出版前一年[2015版] 出版后一年[2017版]

第一作者：
第一作者机构： [a]Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China [d]Department of Allergy, The Third Affiliated Hospital of Shenzhen University, Shenzhen 518020, PR China
通讯作者：
通讯机构： [a]Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China [c]Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Jinan University, Guangzhou 510632, PR China [*1]Huangpu Avenue West 601, Institute of Traditional Chinese Medicine and Natural Product, College of Pharmacy, Jinan University Guangzhou 510632, PR China.
推荐引用方式(GB/T 7714)：
Liu Jie,Zhang Cao,Wang Huailing,et al.Incorporation of nitric oxide donor into 1,3-dioxyxanthones leads to synergistic anticancer activity.[J].EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY.2018,151:158-172.doi:10.1016/j.ejmech.2018.03.072.
APA：
Liu Jie,Zhang Cao,Wang Huailing,Zhang Lei,Jiang Zhenlei...&Chen Heru.(2018).Incorporation of nitric oxide donor into 1,3-dioxyxanthones leads to synergistic anticancer activity..EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,151,
MLA：
Liu Jie,et al."Incorporation of nitric oxide donor into 1,3-dioxyxanthones leads to synergistic anticancer activity.".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 151.(2018):158-172

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