Nickel-Catalyzed Difluoroalkylation-Alkylation of Enamides
作者:
Xu, Chang;Yang, Zhi-Fang;An, Lun;Zhang, Xingang*
期刊:
ACS Catalysis ,2019年9(9):8224-8229 ISSN:2155-5435
通讯作者:
Zhang, Xingang
作者机构:
[An, Lun; Xu, Chang; Zhang, Xingang] Univ Chinese Acad Sci, Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem,Ctr Excellence Mol Sy, 345 Lingling Lu, Shanghai 200032, Peoples R China.;[Yang, Zhi-Fang] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.
通讯机构:
[Zhang, Xingang] U;Univ Chinese Acad Sci, Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem,Ctr Excellence Mol Sy, 345 Lingling Lu, Shanghai 200032, Peoples R China.
关键词:
cross-coupling;dialkylzinc reagent;fluorine;nickel;tandem reaction
摘要:
Nickel-catalyzed carbodifunctionalization of alkenes is an efficient strategy for the construction of C-C bonds. However, applications of the strategy in dialkylation of alkenes remain underdeveloped due to the difficulties in suppressing competitive side reactions. We now describe a nickel-catalyzed tandem reaction by difluoroalkylation-alkylation of N-vinyl 2-pyrrolidinone with difluoroalkyl bromides and dialkylzinc reagents. The reaction can also extend to N-vinyloxazolidinone and N-vinylacetamide. This carbodifunctionalization reaction proceeds smoothly under mild reaction conditions with good functional group tolerance, providing a straightforward access to gem-difluoroalkylated 2-pyrrolidinone derivatives that are of interest in medicinal chemistry. © 2019 American Chemical Society.
语种:
英文
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Peptidic Monodisperse PEG "combs" with Fine-Tunable LCST and Multiple Imaging Modalities
作者:
Zhu, Junfei;Xiao, Yan;Zhang, Huaibin;Li, Yu;Yuan, Yaping;...
期刊:
Biomacromolecules ,2019年20(3):1281-1287 ISSN:1525-7797
通讯作者:
Jiang, Zhong-Xing
作者机构:
[Li, Yu; Jiang, Zhong-Xing; Zhu, Junfei; Zhang, Huaibin; Yang, Zhigang] Wuhan Univ, Sch Pharmaceut Sci, Hubei Prov Engn & Technol Res Ctr Fluorinated Pha, Wuhan 430071, Peoples R China.;[Xiao, Yan; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;[Zhou, Xin; Chen, Shizhen; Yuan, Yaping] Chinese Acad Sci, Wuhan Inst Phys & Math, State Key Lab Magnet Resonance & Atom & Mol Phys, Natl Ctr Magnet Resonance Wuhan, Wuhan 430071, Peoples R China.
通讯机构:
[Jiang, Zhong-Xing] W;Wuhan Univ, Sch Pharmaceut Sci, Hubei Prov Engn & Technol Res Ctr Fluorinated Pha, Wuhan 430071, Peoples R China.
摘要:
Thermosensitive and imaging-traceable materials with fine-tunable lower critical solution temperature (LCST) around body temperature are highly valuable in biomedicine. However, such materials are rare because it is challenging to fine-tune the LCST and incorporate suitable imaging modalities. Herein, peptidic monodisperse polyethylene glycol (M-PEG) "combs" with fine-tunable LCST, "hot spot" fluorine-19 magnetic resonance imaging (19F MRI), thermoresponsive fluorescent imaging, and drug loading ability were developed through accurately programming their structures during solid phase peptide synthesis (SPPS). The easy availability, structural accuracy, biocompatibility, and versatility provide the M-PEG "combs" with promising prospects as thermoresponsive and imaging-traceable biomaterials for controlled drug delivery. © 2019 American Chemical Society.
语种:
英文
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One-pot synthesis of monodisperse dual-functionalized polyethylene glycols through macrocyclic sulfates
作者:
Lv, Xiaoyan;Zheng, Xing;Yang, Zhigang;Jiang, Zhong-Xing*
期刊:
Organic & Biomolecular Chemistry ,2018年16(44):8537-8545 ISSN:1477-0520
通讯作者:
Jiang, Zhong-Xing
作者机构:
[Jiang, Zhong-Xing; Lv, Xiaoyan; Yang, Zhigang] Wuhan Univ, Sch Pharmaceut Sci, Hubei Prov Engn & Technol Res Ctr Fluorinated Pha, Wuhan 430071, Hubei, Peoples R China.;[Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.
通讯机构:
[Jiang, Zhong-Xing] W;Wuhan Univ, Sch Pharmaceut Sci, Hubei Prov Engn & Technol Res Ctr Fluorinated Pha, Wuhan 430071, Hubei, Peoples R China.
摘要:
Dual-functionalization of monodisperse oligoethylene glycols, especially hetero-functionalization, provides a series of highly valuable intermediates for life and materials sciences. However, the existing methods for the preparation of these compounds suffer excessive protecting and activating group manipulation as well as tedious purification. Here, a one-pot dual-substitution strategy with macrocyclic sulfates of polyethylene glycols as the key intermediates was developed for the convenient and scalable preparation of a series of homo-functionalized and hetero-functionalized oligoethylene glycols in just 1 step. A high synthetic efficacy was achieved by avoiding the protecting and activating group manipulation and the intermediate purification.
语种:
英文
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A Novel Color Modulation Analysis Strategy through Tunable Multiband Laser for Nanoparticle Identification and Evaluation
作者:
Cao, Xuan;Lei, Gang;Feng, Jingjing;Pan, Qi;Wen, Xiaodong;...
期刊:
Analytical Chemistry ,2018年90(4):2501-2507 ISSN:0003-2700
通讯作者:
He, Yan
作者机构:
[He, Yan; Cao, Xuan] Hunan Univ, Coll Biol, State Key Lab Chemo Biosensing & Chemometr, Coll Chem & Chem Engn, Changsha 410082, Hunan, Peoples R China.;[Wen, Xiaodong; Pan, Qi; He, Yan; Lei, Gang; Feng, Jingjing] Tsinghua Univ, Dept Chem, Beijing 100084, Peoples R China.;[Cao, Xuan] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.
通讯机构:
[He, Yan] H;[He, Yan] T;Hunan Univ, Coll Biol, State Key Lab Chemo Biosensing & Chemometr, Coll Chem & Chem Engn, Changsha 410082, Hunan, Peoples R China.;Tsinghua Univ, Dept Chem, Beijing 100084, Peoples R China.
摘要:
Creating color difference and improving the color resolution in digital imaging is crucial for better application of color analysis. Herein, a novel color modulation analysis strategy was developed by using a homemade tunable multiband laser illumination device, in which the portions of R, G, and B components of the illumination light are discretionarily adjustable, and hence the sample color could be visually modulated continuously in the RGB color space. Through this strategy, the color appearance of single gold nanorods (AuNRs) under dark-field microscopy was migrated from the spectrally insensitive red region to the spectrally sensitive green-yellow region. Unlike the traditional continuous-wave light source illumination, wherein the small spectral variations in the samples within a narrow spectral range are averaged by the whole spectrum of the light source, leading to little color difference, the application of sharp, multiband laser illumination could enlarge the color separation between samples, thus resulting in high spectral sensitivity in color analysis. By comparing the corresponding color evolution processes of different samples as the multiband combination of the laser illumination was changed, more efficient color separation of AuNRs was achieved. With this instrument and single Ag@AuNRs as the sulfide probe, we achieved high throughput and highly sensitive detection of sulfide at a detection limit of 0.1 nM, a more than 2 orders of magnitude improvement compared to the previous color sensing scheme. This strategy could be utilized for nanoparticle identification, evaluation, and determination in biological imaging and biochemical analysis. © 2018 American Chemical Society.
语种:
英文
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Ginnalin A from Kujin tea (: Acer tataricum subsp. ginnala) exhibits a colorectal cancer chemoprevention effect via activation of the Nrf2/HO-1 signaling pathway
作者:
Bi, Wu;He, Chun-nian;Li, Xiao-xiao;Zhou, Liu-ying;Liu, Rui-jie;...
期刊:
Food & Function ,2018年9(5):2809-2819 ISSN:2042-6496
通讯作者:
Zhang, Peng-fei
作者机构:
[Liu, Rui-jie; Bi, Wu; Li, Xiao-xiao; Zhang, Sai; Zhou, Liu-ying; Zhang, Peng-fei; Chen, Zhu-chu] Cent S Univ, Xiangya Hosp, Chinese Minist Hlth, Key Lab Canc Prote, Changsha 410008, Hunan, Peoples R China.;[He, Chun-nian] Chinese Acad Med Sci, Minist Educ, Inst Med Plant Dev, Key Lab Bioact Subst & Resources Utilizat Chinese, Beijing 100193, Peoples R China.;[He, Chun-nian] Peking Union Med Coll, Beijing 100193, Peoples R China.;[Li, Guo-qing] Univ South China, Sch Pharm & Life Sci, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Hunan, Peoples R China.
通讯机构:
[Zhang, Peng-fei] C;Cent S Univ, Xiangya Hosp, Chinese Minist Hlth, Key Lab Canc Prote, Changsha 410008, Hunan, Peoples R China.
摘要:
Ginnalin A (also known as acertannin) is one of the most important phenolic compounds of several beverage Acer plants. In this study, it is reported for the first time that ginnalin A is an activator of the Nrf2 signaling pathway in human colon cancer cells. Ginnalin A, isolated from the leaves of Acer tataricum subsp. ginnala, exhibited promising preventive activity against colon cancer cells (HCT116, SW480 and SW620) with IC50 values of 24.8 μM, 22.0 μM and 39.7 μM, respectively. In addition, it significantly reduced the colony formation of these cells. Flow cytometry analysis indicated that ginnalin A suppressed cancer proliferation via the induction of cell cycle arrest at the S-phase. Real time PCR analysis demonstrated that ginnalin A can upregulate the mRNA expression levels of Nrf2-related antioxidant genes Nrf2, HO-1 and NQO1. Western blotting analysis revealed that ginnalin A promoted the Nrf2 nuclear translocation and upregulated the proteins Nrf2, HO-1 and NQO1. Moreover, the upregulation of p62 and the inhibition of Keap1 were also found by Western blotting analysis. Therefore, the activation of the Nrf2 signaling pathway was probably induced through the upregulation of p62 and the inhibition of Keap1. © 2018 The Royal Society of Chemistry.
语种:
英文
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Facile fabrication of a novel hybrid nanoparticles by self-assembling based on pectin-doxorubicin conjugates for hepatocellular carcinoma therapy
作者:
Ye, Peng-Ju;Huang, Can;Yang, Sa;Gao, Pei;Li, Zhi-Ping;...
期刊:
Artificial Cells, Nanomedicine and Biotechnology ,2018年46(sup3):S661-S670 ISSN:2169-1401
通讯作者:
Yu, Cui-Yun
作者机构:
[Huang, Can; Li, Zhi-Ping; Ye, Peng-Ju; He, Dong-Xiu; Xiang, Ya; Tang, Si-Yue; Chen, Yu-Ping; Yang, Sa; Liu, Yu-Feng; Yu, Cui-Yun] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.;[Ye, Peng-Ju; Yu, Cui-Yun; Gao, Pei] Univ South China, Inst Pharm & Pharmacol, Hengyang, Peoples R China.
通讯机构:
[Yu, Cui-Yun] U;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.
关键词:
Drug delivery system;doxorubicin;hepatocellular carcinoma;macromolecular pro-drug;pectin-doxorubicin conjugates;solution self-assembling
摘要:
Hepatocellular carcinoma (HCC) is one of the greatest public health problems worldwide, and chemotherapy remains the major approach for the HCC treatment. Doxorubicin (DOX) is one of the anthracycline antibiotics but its clinical use is limited due to its severe cardiotoxicity. In this study, novel hybrid nanoparticles by self-assembling based on pectin-doxorubicin conjugates (PDC-NPs) were fabricated for HCC treatment. The stabilized structure of the PDC-NPs was characterized by methylene blue absorption, the size, zeta potential and the morphology, which was investigated by Zetasizer nanoparticle analyzer and transmission electron microscope (TEM), of nanoparticles. The PDC-NPs achieved a sustained and prolonged release ability, which was illustrated with in vitro drug release profiles, anti-cell proliferation study, cellular uptake assay and in vivo pharmacokinetics analysis. Biocompatibility of the PDC-NPs was assessed with bovine serum albumin (BSA) adsorption test, hemolysis activity examination and viability evaluation of human umbilical vein endothelial cells. Importantly, in vivo studies of the PDC-NPs, which were performed in the athymic BALB/c nude mice, demonstrated that the PDC-NPs significantly reduced the lethal side effect of DOX. Additionally, the H&E staining and serum biochemistry study further confirmed the excellent biological security of the PDC-NPs. © 2018, © 2018 Informa UK Limited, trading as Taylor & Francis Group.
语种:
英文
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Design, synthesis and biological evaluation of flavonoid salicylate derivatives as potential anti-tumor agents
作者:
Deng, Xiangping;Wang, Zhe;Liu, Juan;Xiong, Shujuan;Xiong, Runde;...
期刊:
RSC Advances ,2017年7(61):38171-38178 ISSN:2046-2069
通讯作者:
Tang, Guotao
作者机构:
[Wang, Zhe; Deng, Xiangping; Liu, Juan; Xiong, Shujuan; Tang, Guotao; Xiong, Runde; Cao, Xuan; Zheng, Xing] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.;[Chen, Yanming] Mudanjiang Youbo Pharmaceut Co Ltd, Mudanjiang, Peoples R China.
通讯机构:
[Tang, Guotao] U;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.
摘要:
A series of flavonoid salicylate derivatives containing trimethoxybenzene and a series of chrysin salicylate derivatives were synthesized for use as anti-tumor agents, and evaluated for antiproliferative activity using three human tumor cells: MCF-7 (breast carcinoma cells), HepG2 (liver carcinoma cells), MGC-803 (gastric carcinoma cells) and the mice tumor cells MFC (forestomach carcinoma cells). A substituent group of a suitable size and the trimethoxybenzene had a certain influence on the bioactivity of the flavonoid salicylate derivatives. Compound 2 and its salicylate derivatives 7a-7g containing the trimethoxybenzene exhibited more antiproliferative activity. Among them, compound 7g displayed the most potent antiproliferative activity against MGC-803 cells and MFC cells with the concentration causing 50% inhibition of cell growth (IC50) values of 11.05 ± 1.58 μM and 13.73 ± 2.04 μM, respectively. The flow cytometry results showed that compound 7g caused the cell cycle to be arrested in the G0/G1 phase and induced apoptosis of MFC cells in a dose-dependent manner. Furthermore, compound 7g showed good anti-tumor activity in vivo. These results suggested that compound 7g could be a new, potent anti-tumor candidate which should be optimized and evaluated further. © 2017 The Royal Society of Chemistry.
语种:
英文
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Synthesis and antitumor activity of novel N-(5-benzyl-4-(tert-butyl)thiazol-2-yl)-2-(piperazin-1-yl)acetamides
作者:
Wu, Zhilin;Ding, Na;Tang, Yuting;Ye, Jiao;Peng, Junmei;...
期刊:
Research on Chemical Intermediates ,2017年43(8):4833-4850 ISSN:0922-6168
通讯作者:
Hu, Aixi
作者机构:
[Ye, Jiao; Ding, Na; Peng, Junmei; Wu, Zhilin; Tang, Yuting; Hu, Aixi] Hunan Univ, Coll Chem & Chem Engn, Changsha, Hunan, Peoples R China.;[Wu, Zhilin] Univ South China, Sch Chem & Chem Engn, Hengyang, Hunan, Peoples R China.;[Peng, Junmei] Univ South China, Inst Pharm & Pharmacol, Hengyang, Hunan, Peoples R China.
通讯机构:
[Hu, Aixi] H;Hunan Univ, Coll Chem & Chem Engn, Changsha, Hunan, Peoples R China.
关键词:
Thiazole;Piperazinylacetamide;Antitumor activity;Cell cycle;Double staining
摘要:
A series of novel N-(5-benzyl-4-(tert-butyl) thiazol-2-yl)-2-(piperazin-1yl) acetamides were designed, synthesized and evaluated for their antitumor activities in vitro. The structures of the synthesized compounds were characterized by H-1 NMR, C-13 NMR and elemental analysis. In general, compounds 5a, 5c and 6a showed potent antiproliferative activity against HeLa (human cervical cancer) and A549 (human lung cancer) cell lines. Compound 6a, with the best inhibitory activity against HeLa cells (IC50 = 1.6 +/- 0.8 mu M), was selected to investigate the induced changes of cell morphology in the HeLa cell line by means of acridine orange (AO)/ethidium bromide (EB) double staining and cell cycle analysis using flow cytometry. The results indicated that compound 6a could induce cell apoptosis and cause G1-phase arrest in the cell division cycle.
语种:
英文
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Hydrogen sulfide alleviates uranium-induced acute hepatotoxicity in rats: Role of antioxidant and antiapoptotic signaling
作者:
Yuan, Yan;Zheng, Jifang* ;Zhao, Tingting;Tang, Xiaoqing;Hu, Nan
期刊:
Environmental Toxicology ,2017年32(2):581-593 ISSN:1520-4081
通讯作者:
Zheng, Jifang
作者机构:
[Zheng, Jifang; Yuan, Yan; Zhao, Tingting] Univ South China, Sch Pharmaceut & Biol Sci, Inst Biol, Dept Biol, Changsheng West Rd 28, Hengyang City 421001, Hunan, Peoples R China.;[Tang, Xiaoqing] Univ South China, Coll Med, Inst Neurosci, Dept Physiol, Changsheng West Rd 28, Hengyang City 421001, Hunan, Peoples R China.;[Hu, Nan] Univ South China, Key Discipline Lab Natl Def Biotechnol Uranium Mi, Changsheng West Rd 28, Hengyang City 421001, Hunan, Peoples R China.
通讯机构:
[Zheng, Jifang] U;Univ South China, Sch Pharmaceut & Biol Sci, Inst Biol, Dept Biol, Changsheng West Rd 28, Hengyang City 421001, Hunan, Peoples R China.
关键词:
hydrogen sulfide;uranium;hepatotoxicity;oxidative stress;apoptosis
摘要:
As an endogenous gaseous mediator, H2S exerts antioxidative, antiapoptotic, and cytoprotective effects in livers. This study was designed to investigate the protective role of H2S against uranium-induced hepatotoxicity in adult SD male rats after in vivo effect of uranium on endogenous H2S production was determined in livers. The levels of endogenous H2S and H2S-producing enzymes (CBS and CSE) were measured in liver homogenates from uranium -intoxicated rats. In rats injected intraperitoneally (i.p.) with uranyl acetate or NaHS (an H2S donor) alone or in combination, we examined biochemical parameters to assess liver function, revealed hepatic histopathological alteration, investigated oxidative stress markers, and explored apoptotic signaling in liver homogenates. The results suggest that uranium-intoxication in rats decreased CBS and CSE protein expression, H2S synthesis capacity, and endogenous H2S generation. NaHS administration in uranium-intoxicated rats produced amelioration in liver biochemical indices and histopathological effects, decreased MDA content, and increased GSH level and antioxidative enzymes activities like SOD, CAT, GPx, and GST. NaHS administration in uranium-intoxicated rats attenuated uranium-activated phosphorylation state of JNK. NaHS treatment in uranium-intoxicated rats increased antiapoptotic Bcl-2 but decreased pro-apoptotic Bax, resulting in the rise of Bcl-2/Bax ratio. NaHS treatment in uranium-intoxicated rats reduced the apoptosis mediator caspase-3 and cytochrome c release and elevated ATP contents. Taken together, these data implicate that H2S can afford protection to rat livers against uranium-induced adverse effects mediated by up-regulation of antioxidant and antiapoptotic signaling. The anti-apoptotic property of H2S may be involved, at least in part, in inhibiting JNK signaling. © 2016 Wiley Periodicals, Inc. Environ Toxicol 32: 581–593, 2017. © 2016 Wiley Periodicals, Inc.
语种:
英文
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Diastereoselective Synthesis of CF3 -Containing Vicinal Diamines
作者:
Huang, Qiu-xia;Zheng, Qu-tong;Duan, Yaya;Lin, Jin-Hong* ;Xiao, Ji-Chang* ;...
期刊:
The Journal of Organic Chemistry ,2017年82(15):8273-8281 ISSN:0022-3263
通讯作者:
Xiao, Ji-Chang;Zheng, Xing;Lin, Jin-Hong
作者机构:
[Xiao, Ji-Chang; Zheng, Xing; Huang, Qiu-xia; Zheng, Qu-tong] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.;[Lin, JH; Xiao, Ji-Chang; Zheng, Xing; Huang, Qiu-xia; Duan, Yaya; Lin, Jin-Hong; Zheng, Qu-tong] Univ Chinese Acad Sci, Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem, 345 Lingling Rd, Shanghai 200032, Peoples R China.
通讯机构:
[Xiao, JC; Zheng, X; Lin, JH] U;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.;Univ Chinese Acad Sci, Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem, 345 Lingling Rd, Shanghai 200032, Peoples R China.
摘要:
The highly diastereoselective synthesis of CF3-containing vicinal diamines by a convenient two-step procedure without the need to isolate the intermediate products is described.
语种:
英文
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Simultaneous fluorescence analysis of the different carbohydrates expressed on living cell surfaces using functionalized quantum dots
作者:
He, Dongxiu* ;Wang, Danxia;Shi, Xiaoxin;Quan, Wenjie;Xiong, Runde;...
期刊:
RSC Advances ,2017年7(20):12374-12381 ISSN:2046-2069
通讯作者:
He, Dongxiu
作者机构:
[Huang, Honglin; Yua, Cui-yun; He, Dongxiu; Wang, Danxia] Univ South China, Inst Pharm & Pharmacol, Hengyang, Hunan, Peoples R China.;[Quan, Wenjie; Shi, Xiaoxin; Yua, Cui-yun; He, Dongxiu; Xiong, Runde] Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Hunan, Peoples R China.
通讯机构:
[He, Dongxiu] U;[He, Dongxiu] H;Univ South China, Inst Pharm & Pharmacol, Hengyang, Hunan, Peoples R China.;Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Hunan, Peoples R China.
摘要:
The aberrant expression of carbohydrates has been associated with the occurrence, growth, progression and metastasis of tumors. Tumor-associated carbohydrates may have great potential as tumor markers for the early diagnosis of hepatocellular carcinoma (HCC). Therefore, characterizing HCC-associated carbohydrate expression is of great importance to assist the early diagnosis of HCC. A fluorescence method for characterizing carbohydrates expressed on both normal human cells (LO2 cells and endothelial cells) and HCC cells (HepG2 cells) using functionalized quantum dots (QDs) has been proposed in this study. The QDs were successfully fabricated and covalently conjugated with Datura stramonium agglutinin (DSA) or Lens culinaris agglutinin (LCA) via 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) coupling reaction. The formed functionalized QDs (lectin–QDs conjugates) were characterized using ultraviolet and fluorescence spectra, agarose gel electrophoresis, hemagglutination activity tests, lectin competitive-binding assay and carbohydrate inhibition assays. The functionalized QDs were found to retain stable fluorescence and carbohydrate recognition abilities. Significant differences of carbohydrates expressed between on the normal cells and the HepG2 cells were evaluated by fluorescence imaging and flow cytometric analysis. The experimental results illustrate that the functionalized QDs could be used as promising tools for monitoring in situ cell surface carbohydrate expression and evaluating the differences in the carbohydrates expressed on normal cells and tumor cells surfaces, which is very important for helping the early diagnosis of HCC.
语种:
英文
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Direct Imaging of Single Plasmonic Metal Nanoparticles in Capillary with Laser Light-Sheet Scattering Imaging
作者:
Cao, Xuan;Feng, Jingjing;Pan, Qi;Xiong, Bin;He, Yan* ;...
期刊:
Analytical Chemistry ,2017年89(5):2692-2697 ISSN:0003-2700
通讯作者:
He, Yan
作者机构:
[Xiong, Bin; He, Yan; Cao, Xuan] Hunan Univ, Coll Chem & Chem Engn, Coll Biol, State Key Lab Chemobiosensing & Chemometr, Changsha 410082, Hunan, Peoples R China.;[Pan, Qi; He, Yan; Feng, Jingjing] Tsinghua Univ, Dept Chem, Beijing 100084, Peoples R China.;[Cao, Xuan] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.;[Yeung, Edward S.] Iowa State Univ, Dept Chem, Ames, IA 50011 USA.
通讯机构:
[He, Yan] H;[He, Yan] T;Hunan Univ, Coll Chem & Chem Engn, Coll Biol, State Key Lab Chemobiosensing & Chemometr, Changsha 410082, Hunan, Peoples R China.;Tsinghua Univ, Dept Chem, Beijing 100084, Peoples R China.
摘要:
Understanding the heterogeneous distribution of the physical and chemical properties of plasmonic metal nanoparticles is fundamentally important to their basic and applied research. Traditionally, they are obtained either indirectly via bulk spectroscopic measurements plus electron microscopic characterizations or through single molecule/particle imaging of nanoparticles immobilized on planar substrates. In this study, by using light-sheet scattering microscopy with a supercontinuum white laser, highly sensitive imaging of individual metal nanoparticles (MNPs) flowing inside a capillary, driven by either pressure or electric field, was achieved for the first time. We demonstrate that single plasmonic nanoparticles with different size or chemical modification could be differentiated through their electrophoretic mobility in a few minutes. This technique could potentially be applied to high throughput characterization and evaluation of single metal nanoparticles as well as their dynamic interactions with various local environments. © 2017 American Chemical Society.
语种:
英文
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功能化磁性载体固定耐辐射奇球菌及其对铀的吸附行为与机理
作者:
肖方竹;何淑雅;彭国文;唐艳;戴益民
期刊:
中国有色金属学报 ,2016年26(7):1568-1575 ISSN:1004-0609
通讯作者:
Peng, Guo-Wen(pgwnh@sohu.com)
作者机构:
[肖方竹; 何淑雅; 唐艳] Support Discipline Laboratory of National Defence for Biochemistry and Molecular biology, University of South China, Hengyang, 421001, China;[戴益民] The Key Laboratory of Powder and Transport Materials Protection in Hunan Province, College of Chemistry and Chemical Engineering, Changsha University of Science &, Technology, Changsha, 410004, China;[彭国文] School of Resources and Safety Engineering, Central South University, Changsha, 410083, China;[彭国文] School of Chemistry and Chemical Engineering, University of South China, Hengyang, 421001, China
通讯机构:
School of Chemistry and Chemical Engineering, University of South China, Hengyang, China
关键词:
功能化;磁性载体;耐辐射奇球菌;铀;吸附机理
摘要:
为了解决耐辐射奇球菌(DR)容易以悬浮态生长,菌体与水的密度差较小,吸附铀后难以分离等问题,首先使用氯化亚砜对羧基化磁性纳米Fe_3O_4粒子进行酰氯功能化,以此作为DR菌固定载体,再与二乙烯三胺化学修饰的DR菌进行固定化,得到一种新型功能化磁性耐辐射奇球菌吸附剂NFGDR,并通过红外光谱仪和扫描电镜分别表征吸附剂NFGDR的结构。考察溶液pH值、吸附时间、铀初始浓度和吸附剂投加量等因素对吸附剂NFGDR吸附铀的影响,对吸附动力学模型和吸附等温模型进行分析。结果表明:吸附剂NFGDR表面具有大量吸附铀的基团,吸附铀后表面形态发生变化;吸附铀的最佳条件是pH值为5、吸附时间为80 min、铀初始浓度为10 mg/L和吸附剂投加量为5 mg。吸附剂NFGDR对铀的吸附动力学过程符合准二级动力学模型,吸附等温线符合Langmuir等温线模型,说明该吸附体系是一个单层吸附过程。同时,使用3种不同的解析剂对吸附剂NFGDR解析再生6次后,其对铀的吸附率均在80%以上,说明其具有良好的再生性能。
语种:
中文
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Target-based metabolomics for the quantitative measurement of 37 pathway metabolites in rat brain and serum using hydrophilic interaction ultra-high-performance liquid chromatography-tandem mass spectrometry
作者:
Chen, Jiahui;Hou, Waner;Han, Bo;Liu, Guanghui;Gong, Jin;...
期刊:
Analytical and Bioanalytical Chemistry ,2016年408(10):2527-2542 ISSN:1618-2642
通讯作者:
Liao, Qiongfeng;Xie, Zhiyong
作者机构:
[Chen, Jiahui; Gong, Jin; Liao, Qiongfeng; Liu, Guanghui; Hou, Waner] Guangzhou Univ Chinese Med, Sch Chinese Mat Med, Guangzhou 510407, Guangdong, Peoples R China.;[Han, Bo] Shihezi Univ, Sch Pharm, Shihezi 832000, Peoples R China.;[Zhong, Danmin; Li, Yemeng; Xie, Zhiyong] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China.;[Xie, Zhiyong] Univ South China, Cooperat Innovat Ctr Mol Target New Drug Study, Hengyang 421001, Hunan, Peoples R China.
通讯机构:
[Liao, Qiongfeng] G;[Xie, Zhiyong] S;[Xie, Zhiyong] U;Guangzhou Univ Chinese Med, Sch Chinese Mat Med, Guangzhou 510407, Guangdong, Peoples R China.;Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China.
关键词:
Amino acids;HILIC-MS;Quantitative;Target-based metabolomics;neurotransmitters;purines and pyrimidines
摘要:
Amino acids, neurotransmitters, purines, and pyrimidines are bioactive molecules that play fundamental roles in maintaining various physiological functions. Their metabolism is closely related to the health, growth, development, reproduction, and homeostasis of organisms. Most recently, comprehensive measurements of these metabolites have shown their potential as innovative approaches in disease surveillance or drug intervention. However, simultaneous measurement of these metabolites presents great difficulties. Here, we report a novel quantitative method that uses hydrophilic interaction ultra-high-performance liquid chromatography-tandem mass spectrometry (HILIC-UPLC-MS/MS), which is highly selective, high throughput, and exhibits better chromatographic behavior than existing methods. The developed method enabled the rapid quantification of 37 metabolites, spanning amino acids, neurotransmitters, purines, and pyrimidines pathways, within 6.5 min. The compounds were separated on an ACQUITY UPLC® BEH Amide column. Serum and brain homogenate were extracted by protein precipitation. The intra- and interday precision of all of the analytes was less than 11.34 %, and the accuracy was between -11.74 and 11.51 % for all quality control (QC) levels. The extraction recoveries of serum ranged from 84.58 % to 116.43 % and those of brain samples from 80.80 % to 119.39 %, while the RSD was 14.61 % or less for all recoveries. This method was used to successfully characterize alterations in the rat brain and, in particular, their dynamics in serum. The following study was performed to simultaneously test global changes of these metabolites in a serotonin antagonist p-chlorophenylalanine (PCPA)-induced anxiety and insomnia rat model to understand the effect and mechanism of PCPA. Taken together, these results show that the method is able to simultaneously monitor a large panel of metabolites and that this protocol may represent a metabolomic method to diagnose toxicological and pathophysiological states. © Springer-Verlag Berlin Heidelberg 2016.
语种:
英文
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Hydrogen Sulfide and Cellular Redox Homeostasis
作者:
Xie, Zhi-Zhong* ;Liu, Yang;Bian, Jin-Song*
期刊:
Oxidative Medicine and Cellular Longevity ,2016年2016:6043038 ISSN:1942-0900
通讯作者:
Xie, Zhi-Zhong;Bian, Jin-Song
作者机构:
[Xie, Zhi-Zhong; Liu, Yang] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.;[Xie, Zhi-Zhong; Liu, Yang] Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Hunan, Peoples R China.;[Bian, Jin-Song] Natl Univ Singapore, Yong Loo Lin Sch Med, Dept Pharmacol, Singapore 117597, Singapore.
通讯机构:
[Xie, Zhi-Zhong] U;[Xie, Zhi-Zhong] H;[Bian, Jin-Song] N;Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.;Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Hunan, Peoples R China.
摘要:
Intracellular redox imbalance is mainly caused by overproduction of reactive oxygen species (ROS) or weakness of the natural antioxidant defense system. It is involved in the pathophysiology of a wide array of human diseases. Hydrogen sulfide (H2S) is now recognized as the third "gasotransmitters" and proved to exert a wide range of physiological and cytoprotective functions in the biological systems. Among these functions, the role of H2S in oxidative stress has been one of the main focuses over years. However, the underlying mechanisms for the antioxidant effect of H2S are still poorly comprehended. This review presents an overview of the current understanding of H2S specially focusing on the new understanding and mechanisms of the antioxidant effects of H2S based on recent reports. Both inhibition of ROS generation and stimulation of antioxidants are discussed. H2S-induced S-sulfhydration of key proteins (e.g., p66Shc and Keap1) is also one of the focuses of this review.
语种:
英文
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Difluoromethylation of N-arylsulfonyl hydrazones with difluorocarbene leading to difluoromethyl aryl sulfones
作者:
Zheng, Qu-Tong;Wei, Yun;Zheng, Jian;Duan, Ya-ya;Zhao, Gang;...
期刊:
RSC Advances ,2016年6(85):82298-82300 ISSN:2046-2069
通讯作者:
Zheng, Xing;Xiao, Ji-Chang;Lin, Jin-Hong
作者机构:
[Wang, Zong-Bao; Wei, Yun; Xiao, Ji-Chang; Zheng, Qu-Tong; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.;[Wang, Zong-Bao; Wei, Yun; Xiao, Ji-Chang; Zheng, Qu-Tong; Zheng, Xing] Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.;[Duan, Ya-ya; Wei, Yun; Lin, Jin-Hong; Xiao, Ji-Chang; Zheng, Jian; Zheng, Qu-Tong; Lin, JH; Zhao, Gang] Univ Chinese Acad Sci, Chinese Acad Sci, Key Lab Organofluorine Chem, Shanghai Inst Organ Chem, 345 Lingling Rd, Shanghai 200032, Peoples R China.
通讯机构:
[Zheng, X; Xiao, JC; Lin, JH] U;[Zheng, X; Xiao, JC] H;Univ South China, Inst Pharm & Pharmacol, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.;Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.;Univ Chinese Acad Sci, Chinese Acad Sci, Key Lab Organofluorine Chem, Shanghai Inst Organ Chem, 345 Lingling Rd, Shanghai 200032, Peoples R China.
摘要:
The difluoromethylation of N-arylsulfonyl hydrazones with difluorocarbene generated from difluoromethylene phosphobetaine (Ph<inf>3</inf>P<sup>+</sup>CF<inf>2</inf>CO<inf>2</inf><sup>-</sup>) to give various difluoromethyl aryl sulfones is described. ©2016 The Royal Society of Chemistry.
语种:
英文
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Nanohydroxyapatite/cellulose nanocrystals/silk fibroin ternary scaffolds for rat calvarial defect regeneration
作者:
Chen, Xiaoming;Zhou, Runmei;Chen, Bin;Chen, Jianting*
期刊:
RSC Advances ,2016年6(42):35684-35691 ISSN:2046-2069
通讯作者:
Chen, Jianting
作者机构:
[Chen, Jianting; Chen, Xiaoming] Southern Med Univ, Nanfang Hosp, Dept Orthoped Spinal Surg, Guangzhou 510515, Guangdong, Peoples R China.;[Chen, Xiaoming] Univ South China, Affiliated Hosp 2, Dept Orthoped Spinal Surg, Hengyang 421001, Peoples R China.;[Zhou, Runmei] Univ South China, Affiliated Hosp 2, Dept Pharm, Hengyang 421001, Peoples R China.;[Chen, Bin] Chenzhou 1 Peoples Hosp, Dept Orthoped Spinal Surg, Chenzhou 423000, Peoples R China.
通讯机构:
[Chen, Jianting] S;Southern Med Univ, Nanfang Hosp, Dept Orthoped Spinal Surg, Guangzhou 510515, Guangdong, Peoples R China.
摘要:
The purpose of this study was to design and characterise a novel biomimetic scaffold for the repair of critical size calvarial defects. In this study, we developed a new hydroxyapatite/cellulose nanocrystals/silk fibroin (HA/CNC/SF) scaffold by mixing a solution of SF with HA and CNC nanoparticles. The scaffold was fabricated by freeze-drying. The average pore size and porosity of the HA/CNC/SF scaffolds were 110 ± 7.3 μm and 90 ± 6.2%, respectively. The thermostability and mechanical properties of the scaffolds were significantly better than those of either SF, CNC/SF or HA/SF scaffolds. Additionally, the composite scaffold exhibited excellent biocompatibility and superior osteoconductivity. Hence, the efficacy of the HA/CNC/SF scaffold was evaluated for bone regeneration in the rat calvarial defect model. The results demonstrated that the rat calvarial defect healed with new-formed bone within 12 weeks of implantation and the degradation rate of the scaffold was a good match to the bone regeneration rate. Therefore, the HA/CNC/SF scaffold is considered to be a strong candidate for the repair of bone defects in bone tissue engineering.
语种:
英文
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A near-infrared BODIPY-based fluorescent probe for the detection of hydrogen sulfide in fetal bovine serum and living cells
作者:
Zhang, Jian;Zhou, Junliang;Dong, Xiaochun* ;Zheng, Xing;Zhao, Weili
期刊:
RSC Advances ,2016年6(56):51304-51309 ISSN:2046-2069
通讯作者:
Dong, Xiaochun
作者机构:
[Dong, Xiaochun; Zhang, Jian; Zhao, Weili] Fudan Univ, Sch Pharm, Shanghai 200120, Peoples R China.;[Zhou, Junliang; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.
通讯机构:
[Dong, Xiaochun] F;Fudan Univ, Sch Pharm, Shanghai 200120, Peoples R China.
摘要:
A near-infrared (NIR) "off-on" fluorescent probe BDP-680 was developed by taking advantage of the Michael addition reaction of unsaturated double bonds in conformationally restricted BODIPY to allow detection of H<inf>2</inf>S. The new probe possesses a highly selective and sensitive response to H<inf>2</inf>S. Such a NIR probe has been applied successfully to detect H<inf>2</inf>S in 10% deproteinized fetal bovine serum (FBS). The detection limit of the probe for NaSH in 10% deproteinized FBS sample was calculated to be about 1 μM which is consistent with the value obtained from serum free solutions (0.5 μM). The probe is of low toxicity and has been successfully used to detect H<inf>2</inf>S in living cells. ©2016 The Royal Society of Chemistry.
语种:
英文
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Fabrication of galactosylated chitosan-5-fluorouracil acetic acid based nanoparticles for controlled drug delivery
作者:
Yu, Cui-Yun* ;Li, Na-Mei;Yang, Sa;Ning, Qian;Huang, Can;...
期刊:
Journal of Applied Polymer Science ,2015年132(40):- ISSN:0021-8995
通讯作者:
Yu, Cui-Yun
作者机构:
[He, Zi-Ning; Huang, Wen; Huang, Can; He, Dong-Xiu; Tan, Xiang-Wen; Li, Na-Mei; Sun, Li-Chun; Yang, Sa; Yu, Cui-Yun; Ning, Qian] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.;[Yu, Cui-Yun] Univ South China, Inst Pharm & Pharmacol, Learning Key Lab Pharmacoprote Hunan Prov, Hengyang 421001, Peoples R China.;[Sun, Li-Chun] Tulane Univ, Dept Med, Hlth Sci Ctr, New Orleans, LA 70112 USA.
通讯机构:
[Yu, Cui-Yun] U;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.
关键词:
biomaterials;biomedical applications;drug‐delivery systems;nanostructured polymers
摘要:
ABSTRACT In this study, a novel type of macromolecular prodrug, N‐galactosylated chitosan (GC)−5‐fluorouracil acetic acid (FUA) conjugate based nanoparticles, was designed and synthesized as a carrier for hepatocellular carcinoma drug delivery. The GC–FUA nanoparticles were produced by an ionic crosslinking method based on the modified ionic gelation of tripolyphosphate with GC–FUA. The structure of the as‐prepared GC–FUA was characterized by Fourier transform infrared and 1H‐NMR analyses. The average particle size of the GC–FUA nanoparticles was 160.1 nm, and their drug‐loading content was 21.22 ± 2.7% (n = 3). In comparison with that of the freshly prepared nanoparticles, this value became larger after 7 days because of the aggregation of the GC–FUA nanoparticles. An in vitro drug‐release study showed that the GC–FUA nanoparticles displayed a sustained‐release profile compared to 5‐fluorouracil‐loaded GC nanoparticles. All of the results suggest that the GC–FUA nanoparticles may have great potential for anti‐liver‐cancer applications. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015, 132, 42625.
语种:
英文
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Design and Synthesis of Fluorinated Dendrimers for Sensitive 19F MRI
作者:
Yu, Weijiang;Yang, Yuqi;Bo, Shaowei;Li, Yu;Chen, Shizhen;...
期刊:
The Journal of Organic Chemistry ,2015年80(9):4443-4449 ISSN:0022-3263
通讯作者:
Jiang, Zhong-Xing
作者机构:
[Li, Yu; Yu, Weijiang; Jiang, Zhong-Xing; Yang, Zhigang] Wuhan Univ, Key Lab Combinatorial Biosynth & Drug Discovery, Minist Educ, Wuhan 430071, Peoples R China.;[Li, Yu; Yu, Weijiang; Jiang, Zhong-Xing; Yang, Zhigang] Wuhan Univ, Sch Pharmaceut Sci, Wuhan 430071, Peoples R China.;[Yang, Yuqi; Zhou, Xin; Chen, Shizhen] Chinese Acad Sci, Wuhan Inst Phys & Math, Natl Ctr Magnet Resonance Wuhan, Key Lab Magnet Resonance Biol Syst,State Key Lab, Wuhan 430071, Peoples R China.;[Jiang, Zhong-Xing; Bo, Shaowei; Zheng, Xing] Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hunan Prov Educ Dept, Hengyang 421001, Peoples R China.;[Bo, Shaowei; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.
通讯机构:
[Jiang, Zhong-Xing] W;Wuhan Univ, Key Lab Combinatorial Biosynth & Drug Discovery, Minist Educ, Wuhan 430071, Peoples R China.
摘要:
To achieve high sensitivity for 19F MRI, a class of novel dendritic molecules with multiple pseudosymmetrical fluorines was designed and efficiently synthesized. Through iterative bromination and Williamson ether synthesis under mild conditions, a fluorinated dendrimer with 540 pseudosymmetrical fluorines was conveniently prepared without performing the group protection in a convergent way. The dendrimer is characterized by a strong 19F NMR peak and short relaxation times. Eventually, an appreciably enhanced 19F MRI at an extremely low concentration (18.5 μM) was achieved, which demonstrated the potential utility of such dendritic molecules in highly sensitive 19F MRI.
语种:
英文
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