Porphyrin-Based Metal-Organic Framework Compounds as Promising Nanomedicines in Photodynamic Therapy
作者：
Yu, Wenmei;Zhen, Wenqiang;Zhang, Qizhi;Li, Yanchun;Luo, Hongyu;...
期刊：
ChemMedChem ,2020年15(19):1766-1775 ISSN：1860-7179
通讯作者：
Liu, Yunmei
作者机构：
[Liu, Yunmei; Yu, Wenmei; Zhang, Qizhi; Li, Yanchun; Luo, Hongyu] Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hunan Prov Key Lab Tumor Microenvironment Respons, Hengyang City 421001, Hunan, Peoples R China.;[He, Jun; Zhen, Wenqiang] Univ South China, Inst Chem & Chem Engn, Hengyang City 421001, Hunan, Peoples R China.
通讯机构：
[Liu, Yunmei] U;Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hunan Prov Key Lab Tumor Microenvironment Respons, Hengyang City 421001, Hunan, Peoples R China.
关键词：
porphyrin-MOF nanomedicines;photodynamic therapy;synergistic therapy;nitric oxide
摘要：
Porphyrin photosensitizers are widely used in photodynamic therapy (PDT) because of their unique diagnostic and therapeutic functions. However, many factors such as poor water solubility and instability of porphyrin compounds have limited its clinical application . The metal- organic framework has the characteristics of versatility, high porosity and excellent biocompatibility. The porphyrin-MOF nanomaterials have attracted full attention from researchers because MOF can effectively suppress the quenching caused by the self-aggregation of porphyrin compounds and promote drug delivery. This article reviews the latest applications of porphyrin-MOF nanomedicine in type II photodynamic therapy by increasing tumour cell oxygen concentration, depleting tumour cell functional molecules and releasing signal molecules . The current potential limitations and future application trends have also been emphasized and discussed.
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A promising anticancer drug: a photosensitizer based on the porphyrin skeleton
作者：
Zhang, Qizhi;He, Jun;Yu, Wenmei;Li, Yanchun;Liu, Zhenhua;...
期刊：
RSC Medicinal Chemistry ,2020年11(4):427-437 ISSN：2632-8682
通讯作者：
Liu, Yunmei
作者机构：
[Liu, Yunmei; Yu, Wenmei; Zhang, Qizhi; Li, Yanchun; Zhou, Binning; Liu, Zhenhua] Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang City 421001, Hunan, Peoples R China.;[Liu, Yunmei; Yu, Wenmei; Zhang, Qizhi; Li, Yanchun; Zhou, Binning; Liu, Zhenhua] Hunan Prov Key Lab Tumor Microenvironm Respons Dr, 28 Western Changshen Rd, Hengyang City 421001, Hunan, Peoples R China.;[He, Jun] Univ South China, Inst Chem & Chem Engn, Hengyang City 421001, Hunan, Peoples R China.
通讯机构：
[Liu, Yunmei] H;Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang City 421001, Hunan, Peoples R China.;Hunan Prov Key Lab Tumor Microenvironm Respons Dr, 28 Western Changshen Rd, Hengyang City 421001, Hunan, Peoples R China.
摘要：
Photodynamic therapy (PDT) is a minimally invasive combination of treatments that treat tumors and other diseases by using photosensitizers, light and oxygen to produce cytotoxic reactive oxygen species (ROS) inducing tumor cell apoptosis. Photosensitizers are the key part of PDT for clinical application and experimental research, and most of them are porphyrin compounds at present. Due to their unique affinity for tumor tissues, porphyrins are not only excellent photosensitizers, but also good carriers to transport other active drugs into tumor tissues, which can exert synergistic anticancer effects of PDT and chemotherapy. This article reviews the clinical development of porphyrin photosensitizers and the research status of porphyrin containing bioactive groups. Finally, future perspectives and the current challenges of photosensitizers based on the porphyrin skeleton are discussed.
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英文
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Novel photosensitizing properties of porphyrin–chrysin derivatives with antitumor activity in vitro
作者：
Liu, Ding;Zhang, Qizhi;Zhang, Lang;Yu, Wenmei;Long, Huizhi;...
期刊：
Journal of Chemical Research ,2020年44(7-8):494-504 ISSN：1747-5198
通讯作者：
Liu, Yunmei
作者机构：
[Liu, Yunmei; Yu, Wenmei; Liu, Ding; Zhang, Qizhi; Long, Huizhi] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;[Liu, Yunmei; Yu, Wenmei; Liu, Ding; Zhang, Qizhi; Long, Huizhi] Hunan Prov Key Lab Tumor Microenvironm Respons Dr, Hengyang, Peoples R China.;[Zhang, Lang; He, Jun] Univ South China, Inst Chem & Chem Engn, Hengyang, Peoples R China.
通讯机构：
[Liu, Yunmei] U;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.
关键词：
porphyrins;chrysins;porphyrin-chrysin derivatives;synthesis;antitumor
摘要：
Photodynamic therapy is a promising cancer treatment with the advantages of low toxicity, high efficiency, and noninvasiveness. In this study, 23 novel porphyrin–chrysin derivatives are synthesized using alkyl carbon chains as bridges. We use human gastric cancer cells (MGC-803) and human cervical cancer cells to evaluate the in vitro antitumor activity of all the porphyrin–chrysin derivatives, with 5-fluorouracil (5-Fu) as a positive control. Several of the prepared compounds showed effective photodynamic killing effects, among which 5-hydroxy-2-phenyl-7-(2-(4-(10,15,20-tris(4-hydroxyphenyl)porphyrin-5-yl)phenoxy)ethoxy)-4H-chromen-4-one shows the highest antiproliferation activity on human cervical cancer cells, with a half maximal inhibitory concentration of 26.51 ± 1.15 µM. Flow cytometry analysis showed that human cervical cancer cell apoptosis might be induced by G1 phase arrest. © The Author(s) 2020.
语种：
英文
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Synthesis and biological evaluation of amino acid derivatives containing chrysin that induce apoptosis
作者：
Li, Yang;Zhang, Qizhi;He, Jun;Yu, Wenmei;Xiao, Jie;...
期刊：
Natural Product Research ,2019年35(4):529-538 ISSN：1478-6419
通讯作者：
Liu, Yunmei
作者机构：
[Li, Yang; Zhang, Qizhi; Yu, Wenmei; Xiao, Jie; Guo, Yu; Liu, Yunmei] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang, Peoples R China;[He, Jun] Univ South China, Inst Chem & Chem Engn, Hengyang, Peoples R China;[Zhu, Xiaoming] Hengyang Normal Univ, Inst Chem & Mat Sci, Hengyang, Peoples R China
通讯机构：
[Liu, Yunmei] U;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang, Peoples R China.
关键词：
Chrysin derivatives;amino acid;apoptosis;breast cancer;cell viability
摘要：
A series of chrysin amino acid derivatives were synthesized to evaluate for their antiproliferative activities against several cancer cell lines. Among the compounds tested, N-(2-((5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yl)oxy)octanoyl)-L-leucine methyl ester(5d) presented a good anti-proliferative activity in MDA-MB-231 and MCF-7 cells. Flow cytometry analysis showed that 5d induced apoptosis and prolonged cell cycle progression in MDA-MB-231 and MCF-7 cells. Western blot analysis showed that 5d significantly inhibited Akt phosphorylation (Ser473) in MDA-MB-231 and MCF-7 cells. In addition, 5d treatment markedly downregulated Bcl-2 and upregulated Bax in a dose-dependent manner. In vitro caspase activation assay showed that 5d induced apoptosis of MDA-MB-231 cells by enhancing caspase 3/7 activity. The regulatory effect of 5d on apoptosis of MDA-MB-231 and MCF-7 cells may be induced by mitochondrial apoptosis pathway. This study is of great significance for designing and developing more effective chrysin amino acid derivatives. [GRAPHICS] .
语种：
英文
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The Relationship between Pharmacological Properties and Structure- Activity of Chrysin Derivatives
作者：
Li, Yang;Li, Yan-peng;He, Jun* ;Liu, Ding;Zhang, Qi-zhi;...
期刊：
MINI-REVIEWS IN MEDICINAL CHEMISTRY ,2019年19(7):555-568 ISSN：1389-5575
通讯作者：
He, Jun;Liu, Yunmei
作者机构：
[Liu, Yunmei; Li, Kang; Guo, Yu; Liu, Ding; Li, Yan-peng; Tang, Guo-Tao; Zhang, Qi-zhi; Li, Yang; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.;[He, Jun] Univ South China, Inst Chem & Chem Engn, Hengyang 421001, Peoples R China.;[He, J; Liu, YM] Univ South China, Inst Pharm & Pharmacol, 28 Changshcng West Rd, Hengyang 421001, Peoples R China.
通讯机构：
[He, J; Liu, YM] U;Univ South China, Inst Pharm & Pharmacol, 28 Changshcng West Rd, Hengyang 421001, Peoples R China.
关键词：
Chrysin;chrysin derivatives;synthesis;biological activities;structure-activity relationships;drug target.
摘要：
Chrysin is a natural product of a flavonoid compound. Chemically, chrysin consists of two phenyl rings (A and B) and a heterocyclic ring (C). Biologically, chrysin exerts many different physiological activities. In recent years, with the in-depth development for more active drugs, the synthesis and biological activities of chrysin derivatives have been well studied. Besides, structure-activity relationship of chrysin revealed that the chemical construction meets the critical chemical structural necessities of flavonoids for numerous pharmacological activities. It is generally believed that modified chrysin could be more potent than unmodified chrysin. Different modification in the rings of chrysin could possess various degrees of biological activities. This review aims to summarize the mechanism for the activities of chrysin and its derivatives in different rings. We also explored the relationship between biological function and structure-activity of substituted chrysin derivatives with different functional groups. The influence of chrysin derivatives on the proliferation and apoptosis of cancer cells is also investigated. Development of novel drugs based on the biological functions of chrysin could better improve clinical outcomes of affected population, especially for tumor patients and diabetic patients.
语种：
英文
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The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton
作者：
Li, Yang;Xiao, Jie;Zhang, Qizhi;Yu, Wenmei;Liu, Mengqin;...
期刊：
Bioorganic & Medicinal Chemistry ,2019年27(3):568-577 ISSN：0968-0896
通讯作者：
Liu, Yunmei;He, Jun
作者机构：
[Xiao, Jie; Liu, Yunmei; Yu, Wenmei; Guo, Yu; Zhang, Qizhi; Li, Yang] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;[He, Jun] Univ South China, Inst Chem & Chem Engn, Hengyang 421001, Peoples R China.;[Liu, Mengqin] Hengyang Normal Univ, Inst Chem & Mat Sci, Hengyang 421001, Peoples R China.
通讯机构：
[Liu, Yunmei; He, Jun] U;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;Univ South China, Inst Chem & Chem Engn, Hengyang 421001, Peoples R China.
关键词：
Anti-tumor;Drug target;Inhibitors of protein kinases;Quinazoline derivatives;Structure-activity relationship
摘要：
Quinazoline was originally utilized as an anti-tumor treatment, and its various derivatives can be directly extracted from plants. In recent years, protein kinases (PK) have been well recognized in the development of tumor drugs. Functionally, PK serves a vital role in the apoptosis, proliferation, differentiation, migration and cell cycle of tumor cells. Due to its good physicochemical properties, quinazoline skeleton, a superior type of PK inhibitor, has been extensively used in anti-tumor drug design. An increasing number of studies on quinazoline synthesis have been reported and used by different groups to effectively develop novel derivatives. Thus, several studies have been approved for the use of quinazoline derivatives as inhibitors of other kinases, including Src and histone deacetylase. The aim of the present review was to summarize the mechanism of quinazoline compounds as PK inhibitors, their biological structure-activity relationship such as the substituted quinazoline compounds with different functional groups in the apoptotic process, and their effect on the proliferation of tumor cells. The development of novel agents based on the antitumor functions of quinazoline molecular compounds may improve the clinical outcomes of the affected population, particularly in patients with cancer. © 2019 Elsevier Ltd
语种：
英文
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Research Advances in Syntheses and Properties of Porphyrin Derivatives
作者：
刘鼎;成林;何军;郭玉;刘运美
期刊：
化学通报 ,2018年81(9):780-791 ISSN：0441-3776
作者机构：
Institute of Pharmacy & Pharmacology,Hunan Province Cooperative innovation Center for Molecular Target New Druge Study,University of South China, Hengyang, 421101;Institute of Chemistry & Chemical Engineering,University of South China, Hengyang, 421101;[刘鼎; 成林; 郭玉; 刘运美] Institute of Pharmacy & Pharmacology,Hunan Province Cooperative innovation Center for Molecular Target New Druge Study,University of South China, Hengyang, 421101;[何军] Institute of Chemistry & Chemical Engineering,University of South China, Hengyang, 421101
关键词：
取代卟啉;缩环卟啉;扩环卟啉;合成;性质
摘要：
卟啉化学是有机化学研究中不可或缺的一个方向。由于卟啉在结构上具有一个大的共轭体系,从而具有典型的芳香性。其具有优异的光电性能、独特的光动力治疗作用、高效的催化活性,并且广泛存在于血红素、叶绿素、维生素B12、过氧化氢酶等有机生物分子中,所有这一切都吸引着科学家们进行深入研究。本文从取代卟啉、缩合卟啉以及扩环卟啉三个方面分别讨论了卟啉的研究进展,通过列举一系列经典的反应以及卟啉衍生物,总结了卟啉衍生物的合成方法及其发展方向。另外,文中还对于卟啉的一些特殊物理、化学和光电性质,做了重点介绍。本文旨在为卟啉的研究者们提供参考。
语种：
中文
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新型卟啉-白杨素复合物的合成及其体外抗肿瘤MCF-7细胞的研究
作者：
刘鼎;何军;成林;张奇志;刘运美
期刊：
广东化工 ,2018年45(7):51-52,88 ISSN：1007-1865
作者机构：
南华大学药学与生物科学学院,湖南衡阳,421001;南华大学化学与化工学院,湖南衡阳,421001
关键词：
卟啉;白杨素;抗肿瘤;合成
摘要：
目的:合成一类新型的抗肿瘤活性化合物,以期获得更高效,低毒,靶向性好的抗肿瘤先导药物。方法:通过先合成两类合适的卟啉分子,再通过不同长度的碳链桥利用分子间成醚键的方法将之与白杨素分子有机地结合,从而形成一类新型的卟啉-白杨素复合物。通过核磁共振氢谱,紫外-可见光谱确证化合物结构。然后利用标准的MTT方法检测化合物体外抗乳腺癌MCF-7细胞的活性。结果:成功合成了4个新型卟啉-白杨素复合物;利用MTT法检测其具有优于母体化合物的抗肿瘤活性。结论:本课题合成了一类具有深入研究价值的新型抗肿瘤先导化合物。
语种：
中文
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基于复式分子印迹膜识别的左奥硝唑传感器
作者：
钱多;王红娟;何军;邓健
期刊：
分析试验室 ,2017年36(4):466-470 ISSN：1000-0720
作者机构：
[钱多; 王红娟; 何军; 邓健] 南华大学化学化工学院, 衡阳, 421001
关键词：
奥硝唑;复式分子印迹膜;电化学传感器
摘要：
建立了基于导电聚合物-硅氧缩聚物复式分子印迹膜的左奥硝唑(S-ONZ)对映体检测方法。以3 -(苯氨基)丙基三甲氧基硅烷和2 -氨基苯硼酸为电聚合单体,在碳糊电极表面电沉积连有Si(OCH_3)_3和B(OH)_2基团的聚苯胺型导电膜;以3 -氨丙基三甲氧基硅烷为功能单体、四乙氧基硅烷为交联剂,模板分子S-ONZ存在的条件下经溶胶-凝胶法在导电膜表面共价连接形成硅氧缩聚物分子印迹膜。B(Ⅲ)的引入使印迹位点嵌入路易斯酸中心,由此形成的配位相互作用使印迹位点对模板分子具有更高的对映识别性和更强的结合能力。最优实验条件下,在6.0×10~(-8)~3.5 ×10~(-4) mol/L浓度范围内S-ONZ的还原峰电流与其浓度呈良好的线性关系,检测限为11 nmol/L。传感器已用于检测片剂、血清及尿液中S-ONZ含量,回收率为95.1% ~106%,RSD为3.3% ~4.2%。
语种：
中文
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异丙酰基为桥合成白杨素氨基酸衍生物及其抗癌活性研究
作者：
刘容芳;何军;沈洪秀;刘鼎;李洋;...
期刊：
肿瘤药学 ,2017年7(4):395-400+411 ISSN：2095-1264
作者机构：
南华大学药物药理研究所,湖南衡阳,421001;南华大学化学化工学院,湖南衡阳,421001;[郑兴; 刘运美; 郭玉; 李洋; 沈洪秀; 刘鼎; 刘容芳; 何军; 唐国涛] 南华大学
关键词：
白杨素;氨基酸;抗癌
摘要：
目的 为改善天然产物白杨素的活性,利用氨基酸类物质特性,以异丙酰基为桥合成一系列白杨素氨基酸类衍生物,以期得到活性更高的衍生物。方法 采用烷基化、水解、酰胺缩合等药物合成方法在白杨素的7位引入不同类型的氨基酸,得到一系列衍生物,运用1H-NMR和13C-NMR等方法对其结构进行确证;采用MTT法,以白杨素母体、5-FU为对照,检测其抗人肝癌细胞Hep G2和人乳腺癌细胞MCF-7活性。结果 1H-NMR和13C-NMR等数据显示,烷酰基、氨基酸等基团被成功地引入到白杨素分子的7位。活性测试结果显示,化合物2,5b,5d抑制Hep G2细胞的IC50值低于母体化合物白杨素,化合物2,3,4b,4c,4d,5a和5c抑制MCF-7细胞的IC50值低于白杨素。结论 通过实验能成功地将烷酰基、氨基酸等基团引入白杨素的7位,且得到的大多数衍生物,相较于天然产物白杨素母体,具有更好的抗人肝癌细胞Hep G2和人乳腺癌细胞MCF-7的活性。
语种：
中文
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Carbon paste electrode modified with duplex molecularly imprinted polymer hybrid film for metronidazole detection
作者：
Xiao, Ni;Deng, Jian* ;Cheng, Jianlin;Ju, Saiqin;Zhao, Haiqing;...
期刊：
Biosensors and Bioelectronics ,2016年81:54-60 ISSN：0956-5663
通讯作者：
Deng, Jian
作者机构：
[Xiao, Ni; Zhao, Haiqing; He, Jun; Deng, Jian; Qian, Duo; Ju, Saiqin; Xie, Jin] Univ South China, Sch Chem & Chem Engn, Hengyang 421001, Hunan, Peoples R China.;[Cheng, Jianlin] Univ South China, Sch Publ Hlth, Hengyang 421001, Hunan, Peoples R China.
通讯机构：
[Deng, Jian] U;Univ South China, Sch Chem & Chem Engn, Hengyang 421001, Hunan, Peoples R China.
关键词：
Anilinomethyltriethoxysilane;Duplex molecularly imprinted polymer;Electrochemical sensor;Electropolymerization;Metronidazole
摘要：
A novel electrochemical sensor based on duplex molecularly imprinted polymer (DMIP) hybrid film modified carbon paste electrode (CPE) has been developed for highly sensitive and selective determination of metronidazole (MNZ). A conductive poly(anilinomethyltriethoxysilane) film is firstly electrodeposited on the surface of a CPE, and then a molecularly imprinted polysiloxane (MIPS) membrane is covalently covered on the film via sol-gel process. The as-constructed DMIP hybrid film, combining the advantages of MIPS and conducting MIP, can make feasible the direct and efficient signal transformation between the target analyte and the transducer, as well as enhance the imprinting recognition capability, mass transfer efficiency and the detection sensitivity. Under optimized conditions, the reduction peak currents of MNZ are linear to MNZ concentrations in the range from 4.0×10-7 to 2.0×10-4 mol L-1 with a detection limit of 9.1×10-8 mol L-1. The RSD values vary from 2.9% to 4.7% for intra-day and from 3.4% to 4.2% for inter-day precision. The DMIP-based sensor has been successfully applied for the determination of MNZ in biological and pharmaceutical samples. The accuracy and reliability of the method is further confirmed by high performance liquid chromatography. © 2016 Elsevier B.V.
语种：
英文
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独立学院基础化学实验教学的创新模式与成效分析
作者：
龙威;王榆元;何军
期刊：
萍乡学院学报 ,2015年32(6):87-90 ISSN：2095-9249
作者机构：
[龙威; 王榆元; 何军] 南华大学船山学院;南华大学化学化工学院
关键词：
基础化学;实验教学;独立学院;创新模式
摘要：
独立学院的基础化学实验教学开展模式因不同高校而开设形式不同,但传统的模式已较大地阻碍了学生创新思维的发展.本文提出以学生为主体,提出“自选实验”—“自主完成”—“自我总结”的创新模式,获得了广大学生的欢迎,通过实践调研表明:此种创新模式能较大程度调动学生积极性,成效性分析良好,在高等教育中切实可行.
语种：
中文
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7-0-羧烷基化白杨素衍生物的合成及其抗癌活性
作者：
宋秀道;何军;马锦;郑兴;雷小勇;...
期刊：
合成化学 ,2015年23(2):93-97 ISSN：1005-1511
作者机构：
[宋秀道; 马锦; 郑兴; 雷小勇; 刘运美; 郭玉] 南华大学药物药理研究所;[何军] 南华大学化学化工学院
关键词：
白杨素;烷基化;衍生物;合成;抗癌活性
摘要：
以白杨素(1)为起始原料,与溴代羧酸乙酯经取代反应制得中间体7-0-乙氧羰基烷基白杨素(3a~3d);3a~3d经水解反应合成了7-0-羧烷基化的白杨素衍生物(4a~4d),其中4b~4d为新化合物,其结构经~1H NMR,~(13)C NMR,IR和ESI-MS表征。初步的体外抗癌活性实验结果表明,3和4对人肝癌细胞HepG2和人胃癌细胞MGC-803具有一定的抗癌活性,且大多数化合物的抗癌活性比母体化合物1强,其中6-(5-羟基-2-苯基-4H-苯并吡喃酮-7-氧)己酸(4d,IC_(50)4.04 μmol·L~(-1))对MGC-803细胞的活性抑制作用强于阳性药物DDP(IC_(50)4.40 μmol·L~(-1))。
语种：
中文
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二茂铁-肽Fc-Lys-Leu—Val-OCH3的合成及电化学性质
作者：
魏传晚;王晓娟;何军
期刊：
南华大学学报(自然科学版) ,2015年(3):92-95+98 ISSN：1673-0062
作者机构：
南华大学 化学化工学院,湖南 衡阳,421001;[何军; 魏传晚; 王晓娟] 南华大学
关键词：
二茂铁-肽;液相合成;电化学
摘要：
以二茂铁、亮氨酸、缬氨酸和赖氨酸为原料,苯并***-1-四甲基六氟磷酸酯( HBTU)及1-羟基苯并***( HOBt)为缩合剂,采用液相合成法,合成了Fc-Lys-Leu-Val-OCH3(简称Fc-KLV,其中Fc：ferrocenoyl,二茂铁).用柱层析分离纯化得到目标化合物,并对目标化合物进行紫外和核磁表征以确证其结构. Fc-KLV的循环伏安扫描结果表明,在0.4~0.8 V范围内出现了一对可逆的氧化还原峰,氧化峰和还原峰电位分别为624 mV和546 mV,峰电位之差ΔEp为78 mV,峰电流密度之比Ipa/Ipc =1.12,扩散系数D=1.782×10-6 cm2/s,表明相应的电化学过程主要受扩散控制.
语种：
中文
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Synthesis of novel amino acid derivatives containing chrysin as anti-tumor agents against human gastric carcinoma MGC-803 cells
作者：
Song, Xiudao;Liu, Yunmei* ;Ma, Jin;He, Jun;Zheng, Xing;...
期刊：
Medicinal Chemistry Research ,2015年24(5):1789-1798 ISSN：1054-2523
通讯作者：
Liu, Yunmei
作者机构：
[Liu, Yunmei; Lei, Xiaoyong; Song, Xiudao; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;[Zhang, Lurong; Song, Xiudao; Jiang, Guorong] Suzhou Acad Wumen Chinese Med, Suzhou Hosp Tradit Chinese Med, Suzhou 215003, Peoples R China.;[Ma, Jin] Soochow Univ, Affiliated Childrens Hosp, Suzhou 215003, Peoples R China.;[He, Jun] Univ South China, Inst Chem & Chem Engn, Hengyang 421001, Peoples R China.
通讯机构：
[Liu, Yunmei] U;Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.
关键词：
Chrysin;Amino acid derivatives;Apoptotic;Anti-proliferative
摘要：
Abstract Two series of amino acid derivatives containing chrysin were prepared from 7-O-carboxymethyl chrysin (4a) and 7-O-carboxypropyl chrysin (4b) and amino acid methyl esters by treatment with 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride and N-hydroxybenzotriazole as coupling reagents. The anti-proliferative activities of these derivatives in vitro against human gastric carcinoma MGC-803 cells were evaluated by the standard MTT method. The results showed that among these derivatives tested, compound N-[4-(5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yloxy)butyryl]-l-isoleucine methyl ester (7c) exhibited the most potent inhibitory activity against the growth of MGC-803 cells with IC50 value of 3.78 μmol/L, comparable to the positive control cisplatin. The preliminary apoptotic mechanism of compound 7c was also investigated by flow cytometry (FCM) and Western blot analysis. Results form the FCM assay demonstrated that compound 7c could induce the apoptosis of MGC-803 cells in a dose-dependent manner. And further Western blot assay indicated that 7c could induce the apoptosis through increasing protein expression of Bax and decreasing protein expression of Bcl-xl. In summary, these results suggest that compound 7c may serve as an effective chemotherapeutic candidate. © 2014 Springer Science+Business Media New York.
语种：
英文
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白杨素甘氨酸类化合物的合成及抗癌活性
作者：
Song Xiudao;He Jun;Ma Jin;Liu Yunmei* ;Zheng Xing;...
期刊：
高等学校化学学报 ,2014年35(7):1465-1470 ISSN：0251-0790
通讯作者：
Liu Yunmei
作者机构：
[Guo Yu; Liu Yunmei; Song Xiudao; Ma Jin; Zheng Xing; Lei Xiaoyong] Univ South China, Inst Pharm & Pharmacol, Key Lab Hunan Prov Pharmacoprote, Hengyang 421001, Peoples R China.;[He Jun] Univ South China, Inst Chem & Chem Engn, Hengyang 421001, Peoples R China.
通讯机构：
[Liu Yunmei] U;Univ South China, Inst Pharm & Pharmacol, Key Lab Hunan Prov Pharmacoprote, Hengyang 421001, Peoples R China.
关键词：
白杨素;衍生物;甘氨酸;抗肿瘤
摘要：
以白杨素为起始原料,通过卤代和水解反应制得中间产物7-O-羧烷基化的白杨素衍生物(6 ~ 9); 然后以1-乙基-3-(3-二甲氨基丙基)碳二亚胺(EDCI)、1-羟基苯并三氮唑(HOBt)和4-二甲氨基吡啶(DMAP)为催化体系,4个中间产物分别与甘氨酸甲酯盐酸盐进行酰胺缩合反应,制得白杨素甘氨酸甲酯类化合物12 ~ 15; 化合物12 ~ 15在pH = 10 ~ 11和室温下水解得到相应的白杨素甘氨酸类化合物(16 ~ 19). 所有目标化合物的结构均经~1H NMR,~(13)C NMR,IR 以及MS 确认. 以顺铂为阳性对照药物,采用噻唑蓝比色(MTT)法检测了目标化合物对人肝癌细胞HepG2和人胃癌细胞MGC-803的体外增殖抑制作用. 结果表明,目标化合物14 ~ 16,18和19的体外抗肿瘤活性明显强于白杨素,且化合物18(IC_(50) = 4. 36 μmol /L)对MGC-803细胞的增殖抑制作用强于阳性药物顺铂(IC_(50) = 4. 40 μmol /L).
语种：
中文
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医用有机化学理论教学改革的探索与实践
作者：
梁俊;邓健;罗虹;魏传晚;何军
期刊：
山西医科大学学报 ,2014年16(6):437-439 ISSN：1007-6611
作者机构：
南华大学化学化工学院基础化学教研室,衡阳,421001
关键词：
医用有机化学;教学改革;教学方法
摘要：
为了提高医学专业学生的学习兴趣和培养学生的创新能力,全面提升医用有机化学的教学质量。通过医用有机化学理论教学改革,从注重理论联系实际,精心组织教学内容;优化教学设计,合理使用多媒体课件进行教学;培养学生的自主性学习等方面进行了探索和实践。
语种：
中文
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新型吗啉类化合物的合成及抗实验性抑郁活性研究
作者：
梁俊;肖新荣;何军
期刊：
南华大学学报(自然科学版) ,2014年(3):87-91 ISSN：1673-0062
作者机构：
南华大学 化学化工学院,湖南 衡阳,421001
关键词：
吗啉类化合物;合成;抗抑郁药理模型;抗抑郁活性
摘要：
设计合成了7个未见报道的新型吗啉类化合物,通过IR、NMR、ESI-MS和元素分析对目标化合物结构进行了表征.利用小鼠强迫游泳及悬尾两个抗抑郁药理模型对所合成的化合物进行抗抑郁药理活性筛选,进行了初步的药效评价研究.结果表明这些化合物显示了不同程度的抗抑郁活性,同等剂量下部分化合物的体内抗抑郁作用显著强于空白组,其中芳香环的3位上具有氟取代基的化合物,抗抑郁活性最高,有进一步研究的价值.
语种：
中文
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研讨式教学方法在医用有机化学教学中的应用
作者：
何军;梁俊;魏传晚;王宏青;邓健;...
期刊：
广州化工 ,2014年(17):211-212,218 ISSN：1001-9677
作者机构：
南华大学化学化工学院化学教研室,湖南 衡阳,421001
关键词：
研讨式教学法;医学有机化学;启发式知识传授;互动式讨论
摘要：
有机化学是医学专业重要基础课程。随着教育教学改革的发展,使得医学有机化学的教学面临不少困境。本文从分析教学现状入手,分析问题,提出具体的解决方法,尝试用研讨式教学方法进行医学有机化学的教学改革。采取启发式知识传授、互动式讨论、课题式研讨、研究性实验、归纳性总结等几个环节,激发学生的学习兴趣,提高学生的综合素质。取得了良好的教学效果。
语种：
中文
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Synthesis of New 7-O-Modified Chrysin Derivatives and Their Anti-proliferative and Apoptotic Effects on Human Gastric Carcinoma MGC-803 Cells
作者：
Liu Yunmei* ;Song Xiudao;Ma Jin;He Jun;Zheng Xing;...
期刊：
高等学校化学研究：英文版 ,2014年30(6):925-930 ISSN：1005-9040
通讯作者：
Liu Yunmei
作者机构：
[Liu Yunmei; Zhao Zihao; Song Xiudao; Zheng Xing; Lei Xiaoyong; Pan Xia] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;[Jiang Guorong; Song Xiudao] Suzhou Hosp Tradit Chinese Med, Suzhou Acad Wumen Chinese Med, Suzhou 215003, Peoples R China.;[Ma Jin] Soochow Univ, Affiliated Childrens Hosp, Suzhou 215003, Peoples R China.;[He Jun] Univ South China, Inst Chem & Chem Engn, Hengyang 421001, Peoples R China.
通讯机构：
[Liu Yunmei] U;Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.
关键词：
7-O-Modified chrysin;Anti-proliferative effect;Apoptotic effect;Flavanoid
摘要：
Two series of 7-O-modified chrysin derivatives were prepared from 7-O-carboxymethyl chrysin(2a), 7-O-carboxypropylchrysin(2b) and short-chain alcohols by using 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride(EDCI), N-hydroxybenzotriazole(HOBt) and 4-dimethylamiopryidine(DMAP) as coupling reagents. Taking cisplatin as a reference substance, their anti-proliferative activities in vitro against human gastric carcinoma MGC-803 cells were evaluated by the standard 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide(MTT) method. The results showed that among the compounds tested, compound hepty 4-(5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yloxy) acetate(3f) displayed the most potent growth-inhibitory effect on MGC-803 cells with half maximal inhibitory concentration(IC50) value of 3.23 μmol/L. The preliminary mechanism of inhibitory effect of compound 3f was also detected by flow cytometry(FCM), and the compound exerted anticancer activity via inducing the apoptosis of MGC-803 cells in a dose dependent manner, which suggested that compound 3f would be a potential anti-cancer agent. © 2014, Jilin University, The Editorial Department of Chemical Research in Chinese Universities and Springer-Verlag GmbH.
语种：
英文
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