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Oligosaccharide-camptothecin conjugates as potential antineoplastic drugs: Design, synthesis and biological evaluation.

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收录情况： ◇ SCIE

作者：
Li Maolin[1] * ; Ye Wenchong[1] * ; Fu Kaishuo[1] * ; Zhou Cui[1] ; Shi Yonghui[3] ; Huang Weiping[1] ; Chen Wenming[4] ; Hu Jiliang[1] ; Jiang Zhilin[2,5] ; Zhou Wen[1] ;
机构： [1]School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, E. 232, University Town, Waihuan Rd, Panyu, Guangzhou, 510006, China [2]Puer University, Puer, 665000, Yunan, China [3]Department of Pharmacy, Sun Yat-Sen Memorial Hospital, Sun Yat-Sen University, Guangzhou, 510120, Guangdong, China [4]Department of Pharmaceutical Production Center, The First Affiliated Hospital of Hunan University of Chinese Medicine, 95, Shaoshan Rd, Changsha, Hunan, 41007, China [5]Institutes of Integrative Medicine, Fudan University, Shanghai, 200040, China
出处：
DOI： 10.1016/j.ejmech.2020.112509
ISSN：

关键词： Camptothecin Oligosaccharides Aqueous solubility and stability Anti-tumor activity Toxicological assessment

摘要：
Thirty novel 20 (S)-O-linked camptothecin (CPT) glycoconjugates were synthesized. They showed more potent in vitro cytotoxicities over irinotecan, but very weak direct topoisomerase I (Topo I) inhibition was observed at 100.0 μM. Oligosaccharide types, length of a PEG linker and acetyl groups exerted obvious effects on cytotoxicity, selectivity, water solubility and stability of the newly synthesized CPT glycoconjugates. Construct 40, with a bleomycin (BLM) disaccharide linked to diethylene glycol in the introduced ester moiety, demonstrated a superior antitumor activity and a distinct selectivity compared to CPT. No toxicity was detectable in animal acute toxicity intravenously (160 mg/kg). Collectively, attachment of oligosaccharides with tumor targeting to 20 (S)-OH of CPT could offer a solution to the daunting problems posed by current Topo I poisons. Copyright © 2020 Elsevier Masson SAS. All rights reserved.

基金：
The work is partly supported by financial support from National Science Foundation of China (No.21772028) and General Scientific Research Project of Guangzhou (No. 201804010325). “Climbing” Progress of Guangdong Province (No. pdjh2019a0111, pdjh2020b0139).
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外文
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中科院(CAS)分区：
出版当年[2019]版：
大类 | 2 区 医学
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[2018]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[2018版] 出版当年五年平均 出版前一年[2017版] 出版后一年[2019版]

第一作者：
第一作者机构： [1]School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, E. 232, University Town, Waihuan Rd, Panyu, Guangzhou, 510006, China
共同第一作者：
通讯作者：
通讯机构： [2]Puer University, Puer, 665000, Yunan, China [5]Institutes of Integrative Medicine, Fudan University, Shanghai, 200040, China
推荐引用方式(GB/T 7714)：
Li Maolin,Ye Wenchong,Fu Kaishuo,et al.Oligosaccharide-camptothecin conjugates as potential antineoplastic drugs: Design, synthesis and biological evaluation.[J].EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY.2020,202:doi:10.1016/j.ejmech.2020.112509.
APA：
Li Maolin,Ye Wenchong,Fu Kaishuo,Zhou Cui,Shi Yonghui...&Zhou Wen.(2020).Oligosaccharide-camptothecin conjugates as potential antineoplastic drugs: Design, synthesis and biological evaluation..EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,202,
MLA：
Li Maolin,et al."Oligosaccharide-camptothecin conjugates as potential antineoplastic drugs: Design, synthesis and biological evaluation.".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 202.(2020)

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