A novel 4/6-type alpha-conotoxin ViIA selectively inhibits nAchR α3β2 subtype
作者：
Li, Liang;Liu, Na;Ding, Rong;Wang, Shuo;Liu, Zhuguo;...
期刊：
生物化学与生物物理学报 ,2015年47(12):1023-1028 ISSN：1672-9145
通讯作者：
Dai, Qiuyun
作者机构：
[Li, Liang; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;[Wang, Shuo; Dai, Qiuyun; Liu, Na; Li, Liang; Liu, Zhuguo; Li, Haiying; Ding, Rong] Beijing Inst Biotechnol, Beijing 100071, Peoples R China.
通讯机构：
[Dai, Qiuyun] B;Beijing Inst Biotechnol, Beijing 100071, Peoples R China.
关键词：
α-conotoxin;ViIA;cloning;synthesis;α3β2 nAChR subtype
摘要：
Conotoxins (CTxs) are typically small peptides composed of 12-50 amino acid residues with 2-5 disulfide bridges. Most of them potently and selectively target a wide variety of ion channels and membrane receptors. They are highly valued as neuropharmacological probes and in pharmaceutical development. In this work, a novel α4/6-CTx named ViIA (RDCCSNPPCAHNNPDC-NH2) was identified from a cDNA library of the venom ducts of Conus virgo (C. virgo). ViIA was then synthesized chemically and its disulfide connectivity was identified as 'C1-C3, C2-C4'. Its molecular targets were further assessed using two-electrode voltage clamping. The results indicated that ViIA selectively inhibited nicotinic acetylcholine receptor (nAChR) α3β2 subtype with an IC50 of 845.5 nM, but did not target dorsal root ganglion sodium (Na+)-, potassium (K+)- or calcium (Ca2+)-ion channels. Further structure-activity relationship analysis demonstrated that Arg1 and His11 but not Asp2 were the functional residues. To the best of our knowledge, ViIA is the first 4/6 α-CTx that selectively inhibits nAChR α3β2 subtype. This finding expands the knowledge of targets of α4/6-family CTxs. © The Author 2015. Published by ABBS Editorial Office in association with Oxford University Press on behalf of the Institute of Biochemistry and Cell Biology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences.
语种：
英文
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PCSK9/LDLR通路介导姜黄素烟酸酯促进HepG2摄取脂质
作者：
Zhang Cai-Ping;Sun Shao-Wei;Gong Yong-Zhen;Ou Lu;Lin Li-Mei;...
期刊：
生物化学与生物物理进展 ,2015年42(9):825-832 ISSN：1000-3282
通讯作者：
Liao Duan-Fang
作者机构：
[Zhang Cai-Ping] Univ South China, Coll Med, Hengyang 421001, Peoples R China.;[Lin Li-Mei; Tuo Qin-Hui; Sun Shao-Wei; Gong Yong-Zhen; Liao Duan-Fang] Hunan Univ Chinese Med, State Key Lab Chinese Med Powder & Med Innovat Hu, Div Stem Cell Regulat & Applicat, Changsha 410205, Hunan, Peoples R China.;[Zhang Cai-Ping; Zheng Xing; Sun Shao-Wei; Ou Lu; Lei Xiao-Yong] Univ South China, Coll Pharm & Biol Sci, Hengyang 421001, Peoples R China.;[Tuo Qin-Hui; Gong Yong-Zhen; Liao Duan-Fang] Hunan Univ China, Sinoluxembourg Cooperat Res Ctr Chinese Med, Med, Changsha 410208, Hunan, Peoples R China.
通讯机构：
[Liao Duan-Fang] H;Hunan Univ Chinese Med, State Key Lab Chinese Med Powder & Med Innovat Hu, Div Stem Cell Regulat & Applicat, Changsha 410205, Hunan, Peoples R China.
关键词：
姜黄素烟酸酯(CurTn);低密度脂蛋白受体(LDLR);低密度脂蛋白(LDL);前蛋白转化酶枯草杆菌蛋白酶9型(PCSK9);胆固醇调节元件结合蛋白2型(SREBP2)
摘要：
为研究PCSK9/LDLR通路介导姜黄素烟酸酯(CurTn)降低血浆低密度脂蛋白胆固醇(LDL-C),减少动脉内膜下脂质沉积的分子机制,用5、10、15 μmo/L姜黄素烟酸酯与25 mg/L LDL共孵育HepG2细胞24 h,分别采用油红O染色、胆固醇荧光定量试剂盒、DiI-LDL摄取检测细胞内胆固醇含量及LDL摄取情况,用逆转录定量聚合酶链反应(RT-Q-PCR)检测LDLR及SREBP2的mRNA表达,蛋白质印迹检测LDLR、SREBP2及PCSK9蛋白表达.随姜黄素烟酸酯作用浓度的增高细胞内脂滴显著增多,细胞内游离胆固醇(FC)、总胆固醇(TC)含量增高,细胞内胆固醇摄取增多;RT-Q-PCR和蛋白质印迹检测发现,与对照组(Control)比较,5、10、15 μmo/L姜黄素烟酸酯处理组LDLR蛋白表达增高,SREBP2 mRNA表达水平升高, PCSK9蛋白表达降低,但对LDLR mRNA及SREBP2蛋白表达无影响.结果表明:姜黄素烟酸酯通过降低PCSK9、减少LDLR降解、升高LDLR蛋白表达,促进HepG2细胞胆摄取胆固醇.初步说明CurTn可能通过抑制PCSK9介导LDLR溶酶体降解,促进肝脏清除血浆LDL-C水平.
语种：
中文
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烷氧染料木黄酮衍生物的合成及其抗癌活性研究
作者：
姚旭;郑自通;郭玉;余柳英;魏云;...
期刊：
中南医学科学杂志 ,2014年(4):336-338 ISSN：2095-1116
作者机构：
南华大学药学系,湖南 衡阳,421001;南华大学附属第二医院药剂科;[郑兴; 余柳英; 郭玉; 姚旭; 魏云] 南华大学;[郑自通] 南华大学第二附属医院
关键词：
染料木黄酮;衍生物;抗癌活性
摘要：
目的：研究烷氧染料木黄酮衍生物的体外抗癌活性。方法在催化剂的作用下,染料木黄酮与卤代烃发生取代反应,生成了一系列染料木黄酮衍生物,并通过MTT法检测其对人急性粒细胞性白血病( HL-60)细胞、人结肠癌(HT-29)细胞和人胃癌(SGC-7901)细胞的增殖抑制作用。结果合成了4个烷氧取代染料木黄酮衍生物,其中化合物3a(4′,5,7-三甲基染料木黄酮)对HL-60、HT-29和SGC-7901细胞增殖的抑制作用均强于5-氟尿嘧啶(5-Fu)。结论染料木黄酮衍生物3a具有潜在的抗癌活性。
语种：
中文
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替普瑞酮对阿司匹林致胃黏膜损伤的保护作用分析
作者：
周湘华;郑兴;赵其辉
期刊：
中国医药指南 ,2014年(29):146-146 ISSN：1671-8194
作者机构：
南华大学药学院;[赵其辉] 湖南环境生物职业技术学院;[郑兴; 周湘华] 南华大学
关键词：
替普瑞酮;阿司匹林;胃黏膜损伤
摘要：
目的：分析探讨替普瑞酮对阿司匹林致胃黏膜损伤的保护作用。方法选取来我院就诊的需要长期服用阿司匹林的186例患者，随机分为观察和对照组，每组93例，对照组患者给予阿司匹林肠溶片，100 mg/d，观察组患者在服用阿司匹林的基础上给予替普瑞酮50 mg次，每天3次。分析比较两组患者3、6及12个月后的消化道症状及胃黏膜损伤情况。结果服药3、6、12个月后，观察组患者的消化道症状发生率及胃镜评分与对照组比较具均有显著性差异，P＜0.05，具有统计学意义。结论替普瑞酮对阿司匹林所致得胃黏膜损伤具有一定的保护作用，使阿司匹林所引发的不良反应率降低，值得在临床上推广使用。
语种：
中文
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烟酸联合姜黄素对高脂大鼠血脂及肝脏炎症因子表达的影响
作者：
郑自通;庹勤慧;姚旭;阳巍;郑兴;...
期刊：
海峡药学 ,2014年(8):13-16 ISSN：1006-3765
作者机构：
南华大学附属第二医院药剂科衡阳421001;南华大学药学系 衡阳 421001;湖南中医药大学中药粉体与创新药物国家重点实验室培育基地 长沙420108;[阳巍; 庹勤慧; 郑兴; 姚旭; 廖端芳] 南华大学;[郑自通] 南华大学第二附属医院
关键词：
烟酸;姜黄素;联合用药;降脂;炎症因子
摘要：
目的：探讨烟酸联合姜黄素对高脂血症大鼠的降脂作用及肝脏TNF-α与IL-6表达的影响。方法50只SD大鼠随机分为溶剂对照组、高脂模型组、烟酸组〔100mg/（kg· d）〕、姜黄素组〔200mg/（kg· d）〕、联合用药组〔姜黄素200mg/（kg· d）＋烟酸100mg/（kg· d）〕。8周后检测大鼠血脂，处死，取其肝脏，HE染色，免疫组化检测肝脏TNF-α与IL-6的表达情况。结果与对照组相比，高脂模型组的TC、LDL均明显升高（P＜0.05），肝脏TNF-α与IL-6表达明显增高。与高脂模型组相比，烟酸组能降低TG、LDL含量（P＜0.05），姜黄素组与联合用药组均能显著降低TC、TG、LDL含量（P＜0.05），肝脏TNF-α与IL-6表达明显降低。结论烟酸与姜黄素联合用药可增强降脂作用，且较两者单独用药效果更佳；联合用药能够明显降低肝脏TNF-α与IL-6的表达。
语种：
中文
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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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普通高校药学专业“三级平台”式实践教学体系的构建
作者：
刘运美;雷小勇;郭玉;郑兴;唐国涛;...
期刊：
中国高等医学教育 ,2014年(1):41-42 ISSN：1002-1701
作者机构：
南华大学药学与生物科学学院药学系,湖南衡阳,421001;[郑兴; 黄红林; 雷小勇; 刘运美; 郭玉; 唐国涛] 南华大学
关键词：
药学专业;三级平台式;实践教学体系
摘要：
本文在充分研究药学教育国内外现状与发展趋势基础上,提出了以知识、能力和素质协调发展为宗旨,创建药学专业“三级平台式”特色实践教学体系的研究思路.改革药学专业人才培养模式,主动适应社会经济发展和科技进步对人才的需要.
语种：
中文
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烟酸联合姜黄素对高脂大鼠血脂及肝脏炎症因子表达的影响
作者：
郑自通;庹勤慧;姚旭;阳巍;郑兴;...
期刊：
中国药事 ,2014年(12):1348-1351 ISSN：1002-7777
作者机构：
南华大学附属第二医院，衡阳 421001;南华大学药学系;湖南中医药大学中药粉体与创新药物国家重点实验室培育基地;[阳巍; 庹勤慧; 郑兴; 姚旭; 廖端芳] 南华大学;[郑自通] 南华大学第二附属医院
关键词：
烟酸;姜黄素;联合用药;降脂;炎症因子;合理用药研究
摘要：
目的：探讨烟酸联合姜黄素对高脂血症大鼠的降脂作用及肝脏 TNF-α与 IL-6表达的影响。方法50只SD大鼠随机分为溶剂对照组、高脂模型组、烟酸组[100 mg·(kg·d)-1]、姜黄素组[200 mg·(kg·d)-1]、联合用药组[姜黄素200 mg·(kg·d)-1+烟酸100 mg·(kg·d)-1]。8周后检测大鼠血脂,处死,取其肝脏,HE染色,免疫组化检测肝脏TNF-α与IL-6的表达情况。结果与对照组相比,高脂模型组的TC、LDL均明显升高(P<0.05),肝脏TNF-α与 IL-6表达明显增高。与高脂模型组相比,烟酸组能降低TG、LDL含量(P<0.05),姜黄素组与联合用药组均能显著降低 TC、TG、LDL 含量(P<0.05),肝脏TNF-α与IL-6表达明显降低。结论烟酸与姜黄素联合用药可增强降脂作用,且较两者单独用药效果更佳；联合用药能够明显降低肝脏TNF-α与IL-6的表达。
语种：
中文
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Synthesis and anti-hepatocellular carcinoma activity of gem-difluoromethylenated Oleanolic acid
作者：
Guan Wang;Qutong Zheng;Yun Wei;Ya Liu;Hongquan Zhang;...
作者机构：
[Guan Wang; Hongquan Zhang; Qiuxia Huang; Liqiu Quan; zongbao Wang; Xing Zheng] Research Interest Group, University of South China, Hengyang 421001, China;[Qutong Zheng; Yun Wei; Ya Liu] Institute of Pharmacy & Pharmacology, University of South China, Hengyang 421001, China;[Jichang Xiao] Key Laboratory of Organofluorine Chemistry, Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032, China;[zongbao Wang; Xing Zheng] Institute of Pharmacy & Pharmacology, University of South China, Hengyang 421001, China
会议名称：
中国化学会全国第十一届有机合成化学学术研讨会
会议时间：
2014-10-16
会议地点：
上海
会议主办单位：
中国化学会
会议论文集名称：
中国化学会全国第十一届有机合成化学学术研讨会论文集
关键词：
Oleanolic acid;gem-Difluoromethylenated oleanolic acid;Hepatocellular carcinoma
摘要：
A novel gem-difluoromethylenated oleanolic acid was synthesized and its anti-hepatocellular carcinoma activity in vitro was tested.The results of biological test showed that gem-difluoromethylenated oleanolic acid possessed potential anticancer activity.
语种：
英文
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发挥药师职能加强药品采购管理与安全用药
作者：
周湘华;郑兴
期刊：
临床研究 ,2014年(4):163-163 ISSN：2096-1278
作者机构：
[周湘华] 湖南环境生物职业技术学院;[郑兴] 南华大学
关键词：
药师职能;药品采购;安全用药
摘要：
药品是一种特殊的商品，对于保证患者的生命安全有重要的作用，药师是医院一线工作人员，不仅是药品的管理人员，也是药品的监督与协调人员，对于保证医院用药安全用药有着重要的作用。但是由于各种因素的影响，在长期工作中，很多医院都未意识到药师的重要性，只是将药师作为医生工作的协助人员，本文主要分析医院药品采购工作中存在的问题并提出相应的管理措施。
语种：
中文
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Decarboxylative Julia- Kocienski gem- Difluoro- Olefination of 2-Pyridinyl Sulfonyldifluoroacetate
作者：
Wang, Xiao-Ping;Lin, Jin-Hong;Xiao, Ji-Chang* ;Zheng, Xing
期刊：
European Journal of Organic Chemistry ,2014年2014(5):928-932 ISSN：1434-193X
通讯作者：
Xiao, Ji-Chang
作者机构：
[Lin, Jin-Hong; Xiao, Ji-Chang; Wang, Xiao-Ping] Chinese Acad Sci, Key Lab Organofluorine Chem, Shanghai Inst Organ Chem, Shanghai 200032, Peoples R China.;[Wang, Xiao-Ping; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.;[Xiao, Ji-Chang] Chinese Acad Sci, Key Lab Organofluorine Chem, Shanghai Inst Organ Chem, 345 Lingling Rd, Shanghai 200032, Peoples R China.
通讯机构：
[Xiao, Ji-Chang] C;Chinese Acad Sci, Key Lab Organofluorine Chem, Shanghai Inst Organ Chem, 345 Lingling Rd, Shanghai 200032, Peoples R China.
关键词：
Fluorine;Decarboxylation;Sulfur;Olefination;Aldehydes
摘要：
The decarboxylation of potassium 2-pyridinyl sulfonyldifluoroacetate and its subsequent reaction with aldehydes was found to be an efficient approach for the Julia-Kocienski reaction under mild conditions to give gem-difluoro olefins in moderate to excellent yields. Owing to its high stability in the pure state and its easy decarboxylation in polar solvents, potassium 2-pyridinyl sulfonyldifluoroacetate is expected to be an efficient gem-difluoro-olefination reagent. The decarboxylation of potassium 2-pyridinyl sulfonyldifluoroacetate and its subsequent reaction with aldehydes is an efficient approach for the Julia-Kocienski reaction under mild conditions to give gem-difluoro olefins in moderate to excellent yields. Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
语种：
英文
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初步探讨社区药事管理的建设和发展
作者：
周湘华;郑兴
期刊：
现代养生(下半月版) ,2014年(04):289-289 ISSN：1671-0223
作者机构：
南华大学药学系;[郑兴] 湖南环境生物职业技术学院;[周湘华] 南华大学
关键词：
社区药事管理;建设;发展
摘要：
目的:研究并分析社区药事管理的建设和发展方法。方法:分析我社区服务中心药师管理中存在的不足,并制定出针对性的整改措施。结果:来患者数量也逐渐增多,改革工作初见成效。结论:为了为社区居民提供更好的服务,还需要不断提升药师的专业技能水平与责任意识,加强对患者的用药指导。
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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2010—2012年解放军第169医院抗高血压药应用分析
作者：
陆国忠;郑兴
期刊：
中国医院用药评价与分析 ,2014年14(2):119-122 ISSN：1672-2124
作者机构：
南华大学药学院,湖南衡阳421002;解放军第169医院,湖南衡阳421002;解放军第169医院,湖南衡阳,421002;[郑兴] 中国人民解放军联勤保障部队第922医院;[陆国忠] 南华大学
关键词：
抗高血压药;销售金额;用药频度;分析
摘要：
目的:了解2010—2012年我院抗高血压药使用情况,为临床合理用药、药品采购提供参考。方法:调取2010—2012年我院抗高血压药的出库数据,统计抗高血压药的销售金额、用药频度（DDDs）、限定日费用（DDC）及药物利用指数（DUI）。结果:我院抗高血压药品种多样、价格低廉、销售金额持续增长;其中钙通道阻滞剂（CCB）的销售金额和DDDs排序均居于首位;单品种硝苯地平缓、控释片的DDDs排序居前2位。结论:我院抗高血压药的使用符合当地居民实际情况,使用基本合理。
语种：
中文
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Synthetic derivatives of chrysin and their biological activities
作者：
Liu, Yunmei* ;Song, Xiudao;He, Jun;Zheng, Xing;Wu, Houlv
期刊：
Medicinal Chemistry Research ,2014年23(2):555-563 ISSN：1054-2523
通讯作者：
Liu, Yunmei
作者机构：
[Liu, Yunmei; Wu, Houlv; Song, Xiudao; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421101, Peoples R China.;[He, Jun] Univ South China, Inst Chem & Chem Engn, Hengyang 421101, Peoples R China.
通讯机构：
[Liu, Yunmei] U;Univ South China, Inst Pharm & Pharmacol, Hengyang 421101, Peoples R China.
关键词：
Chrysin derivatives;Anticancer activity;Anti-inflammatory activity;NO donors;Antimicrobial activity;Aromatase inhibitors
摘要：
Chrysin is one of flavones constituents of Orocylumineicum vent. It has been a hot spot as a potential chemopreventive agent and as a natural molecule with numerous biological activities such as antioxidant, antitumor, antiviral, anti-hypertension, anti-diabetic, antibacterial, and so on in recent years. Because of its poor solubility, small intestinal absorption, and the rapid metabolism of glycosylation, a large number of efforts had been made by domestic and foreign researchers on designing its analogs and conjugates to obtain compounds with improved efficacy and selectivity for developing more active drugs for clinic. This article reviews the current research of studying on chrysin derivatives including their properties and possible applications. Additionally, this article also presents the basic information concerning chemical reactivity of chrysin, relevant to the synthesis of its derivatives.
语种：
英文
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Synthesis and Anti-cancer Activities of Apigenin Derivatives
作者：
Zheng, Xing* ;Yu, Liuying;Yang, Jing;Yao, Xu;Yan, Wenna;...
期刊：
MEDICINAL CHEMISTRY ,2014年10(7):747-752 ISSN：1573-4064
通讯作者：
Zheng, Xing
作者机构：
[Yan, Wenna; Wei, Yun; Bo, Shaowei; Yao, Xu; Yu, Liuying; Zheng, Xing; Liu, Ya] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;[Yang, Jing; Zheng, Xing] Bur Commod Qual Supervis & Inspect, Hengyang 421001, Peoples R China.;[Wang, Guan; Wu, Zhiyi] Univ South China, Res Interest Grp, Hengyang 421001, Peoples R China.
通讯机构：
[Zheng, Xing] U;Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.
关键词：
Anti-cancer activities;apigenin;baker-venkataraman reaction;flavonoids;MTT method;SAR.
摘要：
A novel series of apigenin derivatives with phloroglucinol or resorcinol as raw materials were synthesized according to Baker-Venaktaraman reaction and their in vitro inhibitory activities on colorectal adenocarcinoma (HT-29) and leucocythemia (HL-60) cell lines were evaluated by the standard methyl thiazole tetrazolium (MTT) method. The results of biological test showed that some of apigenin derivatives possessed stronger anti-cancer activities than apigenin. Compound 6 showed the strongest activity against colorectal adenocarcinoma (HT-29) and leucocythemia (HL-60) cell lines with IC50 valure of 2.03±0.22 µM, 2.25±0.42 µM, it was better than 5-FU (12.92±0.61 µM, 9.56±0.16 µM), which shows a potential compound for colorectal adenocarcinoma and leucocythemia.
语种：
英文
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Copper-catalyzed trifluoromethylation of alkenes with an electrophilic trifluoromethylating reagent
作者：
Wang, Xiao-Ping;Lin, Jin-Hong;Zhang, Cheng-Pan;Xiao, Ji-Chang* ;Zheng, Xing
期刊：
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY ,2013年9(1):2635-2640 ISSN：1860-5397
通讯作者：
Xiao, Ji-Chang
作者机构：
[Lin, Jin-Hong; Xiao, Ji-Chang; Wang, Xiao-Ping; Zhang, Cheng-Pan] Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem, Shanghai 200032, Peoples R China.;[Wang, Xiao-Ping; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.;[Xiao, Ji-Chang] Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem, 345 Lingling Rd, Shanghai 200032, Peoples R China.
通讯机构：
[Xiao, Ji-Chang] C;Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem, 345 Lingling Rd, Shanghai 200032, Peoples R China.
关键词：
alkenes;catalysis;copper;electrophilic trifluoromethylating reagent;trifluoromethylation
摘要：
An efficient method for the copper-catalyzed trifluoromethylation of terminal alkenes with an electrophilic trifluoromethylating reagent has been developed. The reactions proceeded smoothly to give trifluoromethylated alkenes in good to excellent yields. The results provided a versatile approach for the construction of Cvinyl-CF3 bonds without using prefunctionalized substrates. © 2013 Wang et al.
语种：
英文
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Synthesis and Anticancer Activity of Mono-Carbonyl Analogues of Curcumin
作者：
Song Yin;Xing Zheng;Xu Yao;Yuhong Wang;Duanfang Liao;...
期刊：
癌症治疗(英文) ,2013年4(1):113-123 ISSN：2151-1934
作者机构：
Division of Stem Cell Regulation and Application, State Key Laboratory of Chinese Medicine Powder and Medicine Innovation in Hunan (Incubation), Hunan University of Chinese Medicine, Changsha, China;Institute of Pharmacy and Pharmacology, University of South China, Hengyang, China
关键词：
Curcumin;Mono-Carbonyl Analogues;Anticancer Activity;SAR
摘要：
Curcumin has been reported to possess multifunctional bioactivities with low toxicity. However, the clinical application of curcumin has been significantly limited by its instability and poor metabolic property. Up to now, multiple approaches are being sought to overcome these limitations to obtaining “super curcumin”, and many analogues of curcumin have been designed and synthesized. In all of those analogues, a series of mono-carbonyl curcumin analogues deleting the β-diketone draw our attention. Since the seven-carbon β-diketone linker in curcumin may be responsible for its instability, the series of mono-carbonyl curcumin analogues deleting the β-diketone may be potential prodrug with improved pharmacokinetic and pharmacodynamic properties. This review just focuses on these more stable mono-carbonyl analogues of curcumin, and shows the new class of active structure by introducing the synthesis and anticancer activity of them.
语种：
英文
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Copper-Mediated Trifluoromethylation of Terminal Alkynes by S-(Trifluoromethyl)diarylsulfonium Salt
作者：
Wang, Xiaoping;Lin, Jinhong;Zhang, Chengpan;Xiao, Jichang* ;Zheng, Xing
期刊：
中国化学 ,2013年31(7):915-920 ISSN：1001-604X
通讯作者：
Xiao, Jichang
作者机构：
[Lin, Jinhong; Zhang, Chengpan; Xiao, Jichang; Wang, Xiaoping] Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem, Shanghai 200032, Peoples R China.;[Wang, Xiaoping; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.;[Xiao, Jichang] Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem, 345 Lingling Lu, Shanghai 200032, Peoples R China.
通讯机构：
[Xiao, Jichang] C;Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem, 345 Lingling Lu, Shanghai 200032, Peoples R China.
关键词：
copper;alkynes;trifluoromethylation;S-(trifluoromethyl)diarylsulfonium salt
摘要：
The copper-mediated trifluoromethylation of terminal alkynes with S-(trifluoromethyl)diarylsulfonium salt has been carefully investigated. The reactions proceeded smoothly to afford trifluoromethylated acetylenes in moderate to good yields. This approach is a convenient method to synthesize a variety of functional trifluoromethylated acetylenes.
语种：
英文
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柱层析法纯化灯盏乙素的研究
作者：
肖俊辉;姚旭;刘运美;王小平;唐昌云;...
期刊：
中国医药指南 ,2012年10(7):2,12 ISSN：1671-8194
作者机构：
南华大学附属第二医院,湖南,衡阳,421001;南华大学药学科研兴趣小组,湖南,衡阳,421001;[唐昌云; 周洋] 南华大学;[郑兴; 肖俊辉; 刘运美; 姚旭; 王小平] 南华大学第二附属医院
关键词：
柱层析;灯盏乙素;纯化
摘要：
目的 优选灯盏乙素的柱层析纯化条件.方法 采用高效液相色谱法检测纯度,考察了不同固定相和流动相对灯盏乙素分离效果的影响.结果 灯盏乙素的最佳纯化工艺条件为:固定相200~300 目的 硅胶柱,流动相V(CH2Cl2):V(CH3OH)=5:1,常压洗脱.结论 该方法操作简单,分离效果好,使用成本低.
语种：
中文
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