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学者姓名：钟儒刚
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摘要 ：
氯乙基亚硝基脲(CENUs)是临床上重要的抗肿瘤药物,该类药物通过诱导形成DNA股间交联(dG-dC交联)发挥抗肿瘤作用.但O6-烷基鸟嘌呤-DNA烷基转移酶(O6-alkylguanine-DNA alkyltransferase,AGT)介导的细胞耐药性及明显的毒副作用降低了其抗癌效果.合成了一种肿瘤靶向性多功能亚硝基脲,该化合物由具有低氧选择活性的偶氮苯衍生物、能够抑制AGT活性的O6-苄基鸟嘌呤衍生物和氯乙基亚硝基脲3部分组成.该化合物能够特异性地在低氧肿瘤区域被还原,释放AGT抑制剂和氯乙基亚硝基脲,从而发挥靶向抗肿瘤作用.多功能亚硝基脲及其各中间产物的化学结构经高分辨质谱、1HNMR、13CNMR及IR数据确证.通过CCK-8法评价了上述化合物对人脑神经胶质瘤SF763细胞的增殖抑制活性;并用荧光成像法评价了该化合物对SF763细胞的促凋亡活性.结果表明,与临床一线亚硝基脲类抗肿瘤药物尼莫司汀相比,多功能亚硝基脲能够更有效地抑制肿瘤细胞增殖、促进肿瘤细胞凋亡,并具有明显的低氧靶向性.
关键词 ：
氯乙基亚硝基脲 氯乙基亚硝基脲 肿瘤靶向性 肿瘤靶向性 耐药 耐药 化疗药物 化疗药物 肿瘤低氧 肿瘤低氧
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| GB/T 7714 | 刘琪 , 王娇娇 , 赵丽娇 et al. 肿瘤靶向性多功能亚硝基脲的合成及抗肿瘤活性评价 [J]. | 化学试剂 , 2021 , 43 (6) : 775-782 . |
| MLA | 刘琪 et al. "肿瘤靶向性多功能亚硝基脲的合成及抗肿瘤活性评价" . | 化学试剂 43 . 6 (2021) : 775-782 . |
| APA | 刘琪 , 王娇娇 , 赵丽娇 , 孙国辉 , 任婷 , 张娜 et al. 肿瘤靶向性多功能亚硝基脲的合成及抗肿瘤活性评价 . | 化学试剂 , 2021 , 43 (6) , 775-782 . |
| 导入链接 | NoteExpress RIS BibTex |
摘要 ：
三维细胞培养近年来正被逐渐广泛地应用于抗肿瘤药物筛选,与传统二维细胞培养相比,三维细胞培养模型中的细胞形态、结构和功能与实体瘤更加接近,有利于模拟肿瘤微环境,从而提高药物筛选的准确度.以壳聚糖和透明质酸为原料制备了一种三维多孔支架,并使用该支架构建了人脑胶质瘤SF763细胞的三维肿瘤模型.在此基础上,使用该三维肿瘤球和普通二维细胞评价了尼莫司汀(ACNU)与替拉扎明(TPZ)的体外抗肿瘤活性;并探讨了在常氧和低氧条件下两种药物的活性差异.结果表明,不论在常氧还是低氧条件下,经ACNU处理的三维细胞均比二维细胞表现出更强的耐药性,这说明三维细胞在抗癌药物耐药性评价中具有更高的灵敏性.对于肿瘤低氧敏感药物TPZ,其对三维细胞的毒性与低氧条件下二维细胞的毒性接近,且显著高于在常氧条件下对二维细胞的毒性,这说明三维肿瘤球模拟了肿瘤组织的低氧微环境,使TPZ发生低氧启动从而发挥了抗肿瘤活性.三维细胞培养可作为抗肿瘤药物体外活性评价的有效模型,为抗肿瘤药物筛选提供了更加可靠的方法.
关键词 ：
壳聚糖-透明质酸支架 壳聚糖-透明质酸支架 低氧靶向抗癌药物 低氧靶向抗癌药物 耐药性 耐药性 三维细胞培养 三维细胞培养
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| GB/T 7714 | 李君 , 刘琪 , 赵丽娇 et al. 壳聚糖-透明质酸支架用于低氧靶向性抗癌药物筛选的研究 [J]. | 化学试剂 , 2021 , 43 (6) : 767-774 . |
| MLA | 李君 et al. "壳聚糖-透明质酸支架用于低氧靶向性抗癌药物筛选的研究" . | 化学试剂 43 . 6 (2021) : 767-774 . |
| APA | 李君 , 刘琪 , 赵丽娇 , 孙国辉 , 张娜 , 任婷 et al. 壳聚糖-透明质酸支架用于低氧靶向性抗癌药物筛选的研究 . | 化学试剂 , 2021 , 43 (6) , 767-774 . |
| 导入链接 | NoteExpress RIS BibTex |
摘要 ：
在"三全育人"的大格局下,要充分发挥教师队伍"主力军"、课程建设"主阵地"和课堂教学"主渠道"作用,进一步落实研究生课程思政建设要求,全面推进研究生课程思政的高质量建设,将思政工作体系贯通人才培养体系全过程,是培养中国特色社会主义建设者和接班人的重要基础.癌生物学是北京工业大学环境与生命学部生物学一级学科的研究生课程思政示范课程.结合自身教学实践,浅谈癌生物学课程思政教学模式,旨在提升研究生思想政治教育水平、知识创新和实践创新能力.
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| GB/T 7714 | 孙国辉 , 赵丽娇 , 张娜 et al. 研究生癌生物学课程思政教学模式的初步探索 [J]. | 现代职业教育 , 2021 , (42) : 72-73 . |
| MLA | 孙国辉 et al. "研究生癌生物学课程思政教学模式的初步探索" . | 现代职业教育 42 (2021) : 72-73 . |
| APA | 孙国辉 , 赵丽娇 , 张娜 , 任婷 , 钟儒刚 . 研究生癌生物学课程思政教学模式的初步探索 . | 现代职业教育 , 2021 , (42) , 72-73 . |
| 导入链接 | NoteExpress RIS BibTex |
摘要 ：
亚硝胺是一类对人体危害极大的致癌物,是引发肝癌、肺癌和食管癌等癌症的重要因素.植物源提取物近年来逐渐成为抗癌研究的热点,例如黄酮类、多酚类、维生素类以及生物碱类化合物都具有良好的抗肿瘤效果.一些植物源提取物可以通过清除亚硝酸盐或阻断亚硝化反应来抑制亚硝胺在体内的形成;还可以通过抑制亚硝胺代谢活化、促进肿瘤细胞凋亡、抑制肿瘤细胞增殖和调节肿瘤细胞周期来阻断亚硝胺的致癌作用.对近年来国内外关于植物源提取物抑制亚硝胺诱导癌症的研究进展进行了综述,为植物源提取物的临床应用及癌症防治提供参考.
关键词 ：
癌症防治 癌症防治 亚硝胺 亚硝胺 植物源提取物 植物源提取物 致癌作用 致癌作用
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| GB/T 7714 | 陈玉贺 , 尹方正 , 赵丽娇 et al. 植物源提取物抑制亚硝胺致癌作用的研究进展 [J]. | 化学试剂 , 2021 , 43 (6) : 757-766 . |
| MLA | 陈玉贺 et al. "植物源提取物抑制亚硝胺致癌作用的研究进展" . | 化学试剂 43 . 6 (2021) : 757-766 . |
| APA | 陈玉贺 , 尹方正 , 赵丽娇 , 孙国辉 , 张娜 , 任婷 et al. 植物源提取物抑制亚硝胺致癌作用的研究进展 . | 化学试剂 , 2021 , 43 (6) , 757-766 . |
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摘要 ：
新药研发往往是一件过程漫长且人力物力投入极大的事情.随着日益严重的环境污染问题对人类生命健康形成的挑战,快速研发高效低毒的药物成为当务之急.定量构效关系(QSAR)在历经几十年的发展后,广泛应用于药物科学领域中,作为药物筛选及其生物活性预测的高效工具,在药物活性、毒性和渗透性预测以及作用机制等研究中发挥重要作用.重点介绍了QSAR建模过程及其近年来在抗病毒药物设计与筛选中的研究进展,并对现阶段QSAR应用的局限性问题进行了分析,展望了其未来的发展方向.
关键词 ：
人类免疫缺陷病毒 人类免疫缺陷病毒 定量构效关系 定量构效关系 抗病毒药物设计 抗病毒药物设计 新型冠状病毒 新型冠状病毒 肝炎病毒 肝炎病毒
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| GB/T 7714 | 陈硕 , 李非凡 , 孙国辉 et al. QSAR建模及其在抗病毒药物设计与筛选中的研究进展 [J]. | 化学试剂 , 2021 , 43 (7) : 895-905 . |
| MLA | 陈硕 et al. "QSAR建模及其在抗病毒药物设计与筛选中的研究进展" . | 化学试剂 43 . 7 (2021) : 895-905 . |
| APA | 陈硕 , 李非凡 , 孙国辉 , 赵丽娇 , 钟儒刚 . QSAR建模及其在抗病毒药物设计与筛选中的研究进展 . | 化学试剂 , 2021 , 43 (7) , 895-905 . |
| 导入链接 | NoteExpress RIS BibTex |
摘要 ：
Aliphatic amines as common constituents of dissolved organic nitrogen (DON) exhibit high reactivity during ozonation; however, our understanding of their degradation mechanisms is very limited. In this study, methylamine (MA) and ethylamine (EA), as well as their secondary and tertiary amines (DMA, DEA, TMA and TEA) were chosen as aliphatic amine models and their degradation mechanisms during ozonation were investigated by using the DFT method. The oxygen-transfer reaction occurs initially and rapidly in the ozonation of all the above amines with a ΔG≠ value of 8-10 kcal mol-1 in great agreement with the experimental rate constant of 104 to 107 M-1 s-1. Moreover, N-oxide as the main degradation product for tertiary amines directly forms after oxygen-transfer, while nitroalkanes as main products for secondary and primary amines are yielded after a series of reactions mediated by hydroxylamine and nitrosoalkane with a ΔG≠ value of 10-13 kcal mol-1. Regarding the minor N-dealkylated products for all amines, alkylamino alcohol is an important intermediate possibly generated via a radical reaction pathway with a ΔG≠ value of 21-34 kcal mol-1. Additionally, comparison of the reactivity of aliphatic amines, hydroxylamines and alkylamino alcohols with ozone was made and elucidated in this study. The results are expected to expand our understanding of the degradation mechanisms for nitrogenous compounds during ozonation.
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| GB/T 7714 | Shen Qunfang , Liu Yong Dong , Zhong Rugang . Degradation mechanisms of simple aliphatic amines under ozonation: a DFT study. [J]. | Environmental science. Processes & impacts , 2021 , 23 (3) : 480-490 . |
| MLA | Shen Qunfang et al. "Degradation mechanisms of simple aliphatic amines under ozonation: a DFT study." . | Environmental science. Processes & impacts 23 . 3 (2021) : 480-490 . |
| APA | Shen Qunfang , Liu Yong Dong , Zhong Rugang . Degradation mechanisms of simple aliphatic amines under ozonation: a DFT study. . | Environmental science. Processes & impacts , 2021 , 23 (3) , 480-490 . |
| 导入链接 | NoteExpress RIS BibTex |
摘要 ：
The inositol polyphosphate-5-phosphatase E (Inpp5e) gene is located on chromosome 9q34.3. The enzyme it encodes mainly hydrolyzes the 5-phosphate groups of phosphatidylinositol (3,4,5)-trisphosphate (PtdIns (3,4,5) P3) and phosphatidylinositol (4,5)-bisphosphate (PtdIns (4,5)P2), which are closely related to ciliogenesis and embryonic neurodevelopment, through mechanisms that are largely unknown. Here we studied the role of Inpp5e gene in ciliogenesis during embryonic neurodevelopment using inositol-deficiency neural tube defects (NTDs) mouse and cell models. Confocal microscopy and scanning electron microscope were used to examine the number and the length of primary cilia. The dynamic changes of Inpp5e expression in embryonic murine brain tissues were observed during Embryonic Day 10.5-13.5 (E 10.5-13.5). Immunohistochemistry, western blot, polymerase chain reaction (PCR) arrays were applied to detect the expression of Inpp5e and cilia-related genes of the embryonic brain tissues in inositol deficiency NTDs mouse. Real-time quantitative PCR (RT-qPCR) was used to validate the candidate genes in cell models. The levels of inositol and PtdIns(3,4) P2 were measured using gas chromatography-mass spectrometry (GC-MS) and enzyme linked immunosorbent assay (ELISA), respectively. Our results showed that the expression levels of Inpp5e gradually decreased in the forebrain tissues of the control embryos, but no stable trend was observed in the inositol deficiency NTDs embryos. Inpp5e expression in inositol deficiency NTDs embryos was significantly decreased compared with the control tissues. The expression levels of Inpp5e gene and the PtdIns (3,4) P2 levels were also significantly decreased in the inositol deficient cell model. A reduced number and length of primary cilia were observed in NIH3T3 cells when inositol deficient. Three important cilia-related genes (Ift80, Mkks, Smo) were down-regulated significantly in the inositol-deficient NTDs mouse and cell models, and Smo was highly involved in NTDs. In summary, these findings suggested that down-regulation of Inpp5e might be associated with abnormal ciliogenesis during embryonic neurodevelopment, under conditions of inositol deficiency.
关键词 ：
cilia cilia embryonic development embryonic development gene expression gene expression inositol inositol neural tube defects neural tube defects phosphoinositide 5-phosphatase phosphoinositide 5-phosphatase
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| GB/T 7714 | Yue, Huixuan , Li, Shen , Qin, Jiaxing et al. Down-Regulation of Inpp5e Associated With Abnormal Ciliogenesis During Embryonic Neurodevelopment Under Inositol Deficiency [J]. | FRONTIERS IN NEUROLOGY , 2021 , 12 . |
| MLA | Yue, Huixuan et al. "Down-Regulation of Inpp5e Associated With Abnormal Ciliogenesis During Embryonic Neurodevelopment Under Inositol Deficiency" . | FRONTIERS IN NEUROLOGY 12 (2021) . |
| APA | Yue, Huixuan , Li, Shen , Qin, Jiaxing , Gao, Tingting , Lyu, Jianjun , Liu, Yu et al. Down-Regulation of Inpp5e Associated With Abnormal Ciliogenesis During Embryonic Neurodevelopment Under Inositol Deficiency . | FRONTIERS IN NEUROLOGY , 2021 , 12 . |
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摘要 ：
Chloroethylnitmsoureas (CENUs) are an important family of chemotherapies in clinical treatment of cancers, which exert antitumor activity by inducing the formation of DNA interstrand crosslinks (dG-dC ICLs). However, the drug resistance mediated by O-6-alkylguanine-DNA alkyltransferase (AGT) and absence of tumor-targeting ability largely decrease the antitumor efficacy of CENUs. In this study, we synthesized an azobenzene-based hypoxia-activated combi-nitrosourea prodrug, AzoBGNU, and evaluated its hypoxic selectivity and antitumor activity. The prodrug was composed of a CENU pharmacophore and an O-6-benzylguanine (O-6-BG) analog moiety masked by a N,N-dimethyl-4-(phenyldiazenyl)aniline segment as a hypoxia-activated trigger, which was designed to be selectively reduced via azo bond break in hypoxic tumor microenvironment, accompanied with releasing of an O-6-BG analog to inhibit AGT and a chloroethylating agent to induce dG-dC ICLs. AzoBGNU exhibited significantly increased cytotoxicity and apoptosis-inducing ability toward DU145 cells under hypoxia compared with normoxia, indicating the hypoxia-responsiveness as expected. Predominant higher cytotoxicity was observed in the cells treated by AzoBGNU than those by traditional CENU chemotherapy ACNU and its combination with O-6--BG. The levels of dG-dC ICLs in DU145 cells induced by AzoBGNU was remarkably enhanced under hypoxia, which was approximately 6-fold higher than those in the AzoBGNU-treated groups under normoxia and those in the ACNU-treated groups. The results demonstrated that azobenzene-based combinitrosourea prodrug possessed desirable tumor-hypoxia targeting ability and eliminated chemoresistance compared with the conventional CENUs.
关键词 ：
chloroethylnitrosoureas chloroethylnitrosoureas DNA interstrand crosslinks DNA interstrand crosslinks drug resistance drug resistance hypoxia-activated prodrug hypoxia-activated prodrug O-6-alkylguanine DNA alkyltransferase O-6-alkylguanine DNA alkyltransferase tumor targeting tumor targeting
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| GB/T 7714 | Liu, Qi , Wang, Xiaoli , Li, Jun et al. Development and biological evaluation of AzoBGNU: A novel hypoxia-activated DNA crosslinking prodrug with AGT-inhibitory activity [J]. | BIOMEDICINE & PHARMACOTHERAPY , 2021 , 144 . |
| MLA | Liu, Qi et al. "Development and biological evaluation of AzoBGNU: A novel hypoxia-activated DNA crosslinking prodrug with AGT-inhibitory activity" . | BIOMEDICINE & PHARMACOTHERAPY 144 (2021) . |
| APA | Liu, Qi , Wang, Xiaoli , Li, Jun , Wang, Jiaojiao , Sun, Guohui , Zhang, Na et al. Development and biological evaluation of AzoBGNU: A novel hypoxia-activated DNA crosslinking prodrug with AGT-inhibitory activity . | BIOMEDICINE & PHARMACOTHERAPY , 2021 , 144 . |
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摘要 ：
The information of the acute oral toxicity for most polycyclic aromatic hydrocarbons (PAHs) in mammals are lacking due to limited experimental resources, leading to a need to develop reliable in silico methods to evaluate the toxicity endpoint. In this study, we developed the quantitative structure-activity relationship (QSAR) models by genetic algorithm (GA) and multiple linear regression (MLR) for the rat acute oral toxicity (LD50) of PAHs following the strict validation principles of QSAR modeling recommended by OECD. The best QSAR model comprised eight simple 2D descriptors with definite physicochemical meaning, which showed that maximum atom-type electrotopological state, van der Waals surface area, mean atomic van der Waals volume, and total number of bonds are main influencing factors for the toxicity endpoint. A true external set (554 compounds) without rat acute oral toxicity values, and 22 limit test compounds, were firstly predicted along with reliability assessment. We also compared our proposed model with the OPERA predictions and recently published literature to prove the prediction reliability. Furthermore, the interspecies toxicity (iST) models of PAHs between rat and mouse were also established, validated and employed for filling data gap. Overall, our developed models should be applicable to new or untested or not yet synthesized PAHs falling within the applicability domain (AD) of the models for rapid acute oral toxicity prediction, thus being important for environmental or personal exposure risk assessment under regulatory frameworks.
关键词 ：
Acute oral toxicity Acute oral toxicity Interspecies toxicity model Interspecies toxicity model PAHs PAHs QSAR QSAR Toxicity prediction Toxicity prediction
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| GB/T 7714 | Sun, Guohui , Zhang, Yifan , Pei, Luyu et al. Chemometric QSAR modeling of acute oral toxicity of Polycyclic Aromatic Hydrocarbons (PAHs) to rat using simple 2D descriptors and interspecies toxicity modeling with mouse [J]. | ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY , 2021 , 222 . |
| MLA | Sun, Guohui et al. "Chemometric QSAR modeling of acute oral toxicity of Polycyclic Aromatic Hydrocarbons (PAHs) to rat using simple 2D descriptors and interspecies toxicity modeling with mouse" . | ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY 222 (2021) . |
| APA | Sun, Guohui , Zhang, Yifan , Pei, Luyu , Lou, Yuqing , Mu, Yao , Yun, Jiayi et al. Chemometric QSAR modeling of acute oral toxicity of Polycyclic Aromatic Hydrocarbons (PAHs) to rat using simple 2D descriptors and interspecies toxicity modeling with mouse . | ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY , 2021 , 222 . |
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摘要 ：
Chloropicrin as one of the most frequently detected N-DBPs has drawn great attention due to its high toxicity. However, our understanding of its formation mechanism is still very limited. A combined computational and experimental approach was used in this study to reveal chloropicrin formation mechanism during chlorination. Ethylamine, n-propylamine, alanine and tryptophan along with the above two amines and their four derivatives substituted by -OH or/and -NO2 groups were chosen as computational and experimental model precursors, respectively. The results indicate that primary amines and free amino acids are more likely to share the same chloropicrin formation pathway including N-chlorination, imidization, β-C-alcoholization, N-nitration, α-C-chlorination and dealdehydation processes. Moreover, elimination of hydrochloric acid from N,N-dichloro-amine and electrophilic addition of N-chloroalkylimide with hypochlorous acid were found to be the rate-limiting steps among all the elementary reactions. By skipping over both of the above rate-limiting steps, RCH(OH)CH2NO2 and RCH(OH)CH2NH(OH) compounds were proposed to be potent chloropicrin precursors, and experiments confirmed that 2-nitroethanol and N-methylhydroxylamine have the highest chloropicrin yields in the chlorination among all the precursors reported to date. The findings of this work are helpful for expanding the knowledge of chloropicrin formation mechanisms and predicting the potential chloropicrin precursors.
关键词 ：
Chlorination Chlorination Chloropicrin Chloropicrin DFT DFT Free amino acids Free amino acids Primary amines Primary amines
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| GB/T 7714 | Zhou Yingying , Ye Zhao-Xi , Huang Huang et al. Formation mechanism of chloropicrin from amines and free amino acids during chlorination: A combined computational and experimental study. [J]. | Journal of hazardous materials , 2021 , 416 : 125819 . |
| MLA | Zhou Yingying et al. "Formation mechanism of chloropicrin from amines and free amino acids during chlorination: A combined computational and experimental study." . | Journal of hazardous materials 416 (2021) : 125819 . |
| APA | Zhou Yingying , Ye Zhao-Xi , Huang Huang , Liu Yong Dong , Zhong Rugang . Formation mechanism of chloropicrin from amines and free amino acids during chlorination: A combined computational and experimental study. . | Journal of hazardous materials , 2021 , 416 , 125819 . |
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