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Novel lysosome-targeted anticancer fluorescent agents used in zebrafish and nude mouse tumour imaging

《化学科学与工程前沿（英文）》 2022年 第16卷 第1期   页码 112-120 doi: 10.1007/s11705-021-2075-5

摘要： The design of three novel fatty nitrogen mustard-based anticancer agents with fluorophores incorporated into the alkene structure (CXL 118, CXL121, and CXL122) is described in this report. The results indicated that these compounds are selectively located in lysosomes and exhibit effective antitumour activity. Notably, these compounds can directly serve as both reporting and imaging agents in vitro and in vivo without the need to add other fluorescent tagging agents.

关键词： fluorescent drug     lysosomal     anticancer     zebrafish     nude-mouse tumour imaging    

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Progress in tumor vascular normalization for anticancer therapy: challenges and perspectives

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《医学前沿（英文）》 2012年 第6卷 第1期   页码 67-78 doi: 10.1007/s11684-012-0176-8

摘要：

Antitumor angiogenic therapy has been shown promising in the treatment of several advanced cancers since the approval of the first antiangiogenic drug Avastin in 2004. Although the current antiangiogenic drugs reduce the density of tumor blood vessels and result in tumor shrinkage at the early stage of treatment, recent studies have shown that antiangiogenic therapy has transient and insufficient efficacy, resulting in tumor recurrence in patients after several months of treatment. Blockage of blood and oxygen supplies creates a hypoxic and acidic microenvironment in the tumor tissues, which fosters tumor cells to become more aggressive and metastatic. In 2001, Jain proposed tumor vascular normalization as an alternative approach to treating cancers based on the pioneering work on tumor blood vessels by several other researchers. At present, normalizing the disorganized tumor vasculature, rather than disrupting or blocking them, has emerged as a new option for anticancer therapy. Preclinical and clinical data have shown that tumor vascular normalization using monoclonal antibodies, proteins, peptides, small molecules, and pericytes resulted in decreased tumor size and reduced metastasis. However, current tumor vascular normalizing drugs display moderate anticancer efficacy. Accumulated data have shown that a variety of vasculogenic/angiogenic tumor cells and genes play important roles in tumor neovascularization, growth, and metastasis. Therefore, multiple-targeting of vasculogenic tumor cells and genes may improve the efficacy of tumor vascular normalization. To this end, the combination of antiangiogenic drugs with tumor vascular normalizing therapeutics, as well as the integration of Western medicine with traditional Chinese medicine, may provide a good opportunity for discovering novel tumor vascular normalizing drugs for an effective anticancer therapy.

关键词： angiogenesis     vasculogenesis     neovascularization     tumor     vasculature     normalization     traditional Chinese medicine    

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Synthesis and anticancer activity of (+)-nopinone-based 2-amino-3-cyanopyridines

Shengliang LIAO,Shibin SHANG,Minggui SHEN,Xiaoping RAO,Hongyan SI,Jie SONG,Zhanqian SONG

《农业科学与工程前沿（英文）》 2015年 第2卷 第4期   页码 335-340 doi: 10.15302/J-FASE-2015079

摘要： Twelve (+)-nopinone-based 2-amino-3-cyanopyridines 4a–l were synthesized from (–)-β-pinene. The structures of these compounds were characterized by FT-IR, H NMR, and ESI-MS. All the compounds were tested for their anticancer activity against lung cancer cell line A549, gastric cancer cell line MKN45 and breast cancer cell line MCF7 by MTT method, respectively. The results showed that compounds 4f, 4j and 4k had promising anticancer activity against these cancer cell lines, in particular, compound 4f exhibited broad-spectrum and highly efficient anticancer activity against cell lines A549, MKN45 and MCF7 with IC of 23.78, 67.61 and 53.87 µmol·L , respectively. The preliminary analysis of the structure activity relationship implied that the Br or Cl substituted group of the benzene ring in these derivatives significantly contributed to the anticancer activity.

关键词： b-pinene     nopinone     synthesis     2-amino-3-cyanopyridine     anticancer    

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Ozonation of the 5-fluorouracil anticancer drug and its prodrug capecitabine: Reaction kinetics, oxidation

Siyu Chen, Lee Blaney, Ping Chen, Shanshan Deng, Mamatha Hopanna, Yixiang Bao, Gang Yu

《环境科学与工程前沿（英文）》 2019年 第13卷 第4期 doi: 10.1007/s11783-019-1143-2

摘要：

Specific second-order rate constants were determined for 5-FU and CAP with ozone.

Reaction sites were confirmed by kinetics, Fukui analysis, and products.

The olefin moiety was the main ozone reaction site for 5-FU and CAP.

Carboxylic acids comprised most of the residual TOC for 5-FU.

Ozonation removed the toxicity associated with 5-FU and products but not CAP.

关键词： Ozone     5-fluorouracil     Capecitabine     Hydroxyl radicals     Chemotherapy agents     Toxicity    

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Product identification and toxicity change during oxidation of methotrexate by ferrate and permanganate in water

《环境科学与工程前沿（英文）》 2022年 第16卷 第7期 doi: 10.1007/s11783-021-1501-8

摘要：

• Oxidation of methotrexate by high-valent metal-oxo species was first explored.

关键词： Anticancer drugs     High-valent metal-oxo species     Oxidation kinetics     Reaction mechanisms     Multi-endpoint toxicity    

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标题 作者 时间 类型 操作

Novel lysosome-targeted anticancer fluorescent agents used in zebrafish and nude mouse tumour imaging

期刊论文

Progress in tumor vascular normalization for anticancer therapy: challenges and perspectives

null

期刊论文

Synthesis and anticancer activity of (+)-nopinone-based 2-amino-3-cyanopyridines

Shengliang LIAO,Shibin SHANG,Minggui SHEN,Xiaoping RAO,Hongyan SI,Jie SONG,Zhanqian SONG

期刊论文

Ozonation of the 5-fluorouracil anticancer drug and its prodrug capecitabine: Reaction kinetics, oxidation

Siyu Chen, Lee Blaney, Ping Chen, Shanshan Deng, Mamatha Hopanna, Yixiang Bao, Gang Yu

期刊论文

Product identification and toxicity change during oxidation of methotrexate by ferrate and permanganate in water

期刊论文