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SENSORS AND ACTUATORS B-CHEMICAL · 2014 · IF 3.84

A novel surface modification strategy of CdTe/CdS QDs and its application for sensitive detection of ct-DNA

Wanjun Liang,Zhengqing Liu,Shaopu Liu,Jidong Yang,Youqiu He

A kind of novel Glyp-functionalized-CdTe/CdS Quantum dots (QDs) was successfully synthesized by coating Glyp on the surface of the CdTe/CdS QDs. The fluorescence emission of the modified QDs was enhanced greatly but with a low resonance Rayleigh scattering (RRS). When it interacted with calf thymus DNA (ct-DNA), the fluorescence intensity of the system was obviously quenched and the RRS was enhanced, both in good linear relations. Based on the above, a novel fluorescence biosensor for simple, sensitive and selective detection of ct-DNA was developed. Under the optimized conditions, the linear ranges of the functionalized QDs fluorescence intensity and RRS intensity versus the concentration of ct-DNA were 0.109–70   μg   mL −1 and 0.482–90   μg   mL −1 , respectively. The corresponding detection limits by fluorescence quenching and by RRS enhancing methods were 0.0327   μg   mL −1 and 0.146   μg   mL −1 , respectively. The proposed method was applied to detect ct-DNA in synthetic sample with satisfactory results.

研究领域: 生物传感器 · 分子生物学 · 分析化学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2023 · IF 8.2

Design, synthesis, antitumor activity and ct-DNA binding study of photosensitive drugs based on porphyrin framework

Qizhi Zhang,Wenmei Yu,Zhenhua Liu,Hui Li,Yihui Liu,Xin Liu,Zhaoshun Han,Jun He,Yaofu Zeng,Yu Guo,Yunmei Liu

Photodynamic therapy is a promising novel tumor treatment method. In this study, novel porphyrin-chrysin photosensitizer derivatives were synthesized. Most of the compounds showed antitumor activity against human cervical cancer HeLa cells and human lung cancer A549 cells, among which compound 4c had the best photodynamic therapy effect on HeLa cells and A549 cells, with IC 50 values of 6.26 μM and 23.37 μM, respectively. Free-base porphyrin-chrysin derivatives bind to DNA through surface self-stacking, and zinc metalloporphyrin-chrysin derivatives bind to ct-DNA through intercalation. Notably, the tightness of compound binding to ct-DNA was positively correlated with its antitumor activity. What's more, three-dimensional quantitative conformation studies have shown that increasing the positive charge of the porphyrin ring and introducing a strong electron-withdrawing group at the meso position of the porphyrin ring at the para-position of the benzene ring or reducing the space volume of the compound can enhance the antitumor activity.

CAS / MDL: 480-40-0
研究领域: 药理学 · 肿瘤学 · 生物化学
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JOURNAL OF INORGANIC BIOCHEMISTRY · 2011 · IF 3.317

Synthesis and biological studies of 4′, 7, 8-trihydroxy-isoflavone metal complexes

Li-Jun Tang,Xiang Chen,Yu-Na Sun,Jia Ye,Jing Lu,Ying Han,Xing Jiang,Chan-Chan Cheng,Cheng-Cheng He,Pei-Hong Qiu,Xiao-Kun Li

A new series of complexes of a ligand 4′, 7, 8-trihydroxy-isoflavone with transition metal (zinc, copper, manganese, nickel, cobalt) and selenium have been synthesized and characterized with the aid of elemental analysis , IR, electron ionization mass spectrum (EI-MS) and 1 H NMR spectrometric techniques . The compounds were evaluated for their in vitro antibacterial activities and antitumor properties. The metal complexes were found to be more active than the free ligand. Investigation on the interaction between the complexes and calf-thymus DNA (CT DNA) showed that the absorbance of CT DNA increased and the maximum peak (λ max   =   260   nm) red-shifted, while the intensity of fluorescence spectra of Epstein-Bart DNA (EB-DNA) gradually weakened, which indicated that all of these metal complexes tightly combined with CT DNA.

研究领域: 生物化学 · 药物化学 · 分子生物学
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CHINESE JOURNAL OF STRUCTURAL CHEMISTRY · 2022 · IF 0.847

Syntheses, Crystal Structures and DNA-Binding Properties of Zn(II) and Mn(II) Complexes Based on Imidazole Derivatives and Carboxylic Acid

Hui-Chao GUAN,Xiao-Tong SONG,Gui-Bao LIU,Shu-Mei YUE

Complexes [Zn(pbm)(5-hip)3] ( 1 ), [Zn(pbm)(5-nip) 3 ] ( 2 ), [Mn(pbm)(H 3 btc) 2 (H 2 O)] ( 3 ) and [Mn(pbm)(5-nip) 3 ] ( 4 ), where H 2 HIPA = 5-hydroxyisophthalic acid, H 2 nip = 5-nitroisophthalic acid, H 3 btc = trimesic acid and pbm (pyridine benzene chelate material) = 2-(2-pyridyl)benzimidazole, were identified via single-crystal XRD analyses. 1, 2 and 4 pertain to the monoclinic space group C 2/ c , while 3 belongs to the triclinic space group P ① . The interplay of CT-DNA with those complexes was delineated using ultraviolet, fluorescence, and circular dichroism (CD) spectroscopy and viscosity measurements. Complexes 1, 2, 3 and 4 interact with CT-DNA in an electrostatic or grooving mode. We wish to offer a theory-wise foundation for developing anti-tumor medicines.

研究领域: 无机化学 · 生物化学 · 药学
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Frontiers in Pharmacology · 2021 · IF 5.811

Novel Hybrid CHC from β-carboline and N-Hydroxyacrylamide Overcomes Drug-Resistant Hepatocellular Carcinoma by Promoting Apoptosis, DNA Damage, and Cell Cycle Arrest

Miao Jiefei,Meng Chi,Wu Hongmei,Shan Wenpei,Wang Haoran,Ling Changchun,Zhang Jinlin,Yang Tao

A novel hybrid CHC was designed and synthesized by conjugating β-carboline with an important active fragment N-hydroxyacrylamide of histone deacetylase (HDAC) inhibitor by an amide linkage to enhance antitumor efficacy/potency or even block drug resistance. CHC displayed high antiproliferative effects against drug-sensitive SUMM-7721, Bel7402, Huh7, and HCT116 cells and drug-resistant Bel7402/5FU cells with IC50 values ranging from 1.84 to 3.27 μM, which were two-to four-fold lower than those of FDA-approved HDAC inhibitor SAHA. However, CHC had relatively weak effect on non-tumor hepatic LO2 cells. Furthermore, CHC exhibited selective HDAC1/6 inhibitory effects and simultaneously augmented the acetylated histone H3/H4 and α-tubulin, which may make a great contribution to their antiproliferative effects. In addition, CHC also electrostatically interacted with CT-DNA, exerted remarkable cellular apoptosis by regulating the expression of apoptosis-related proteins and DNA damage proteins in Bel7402/5FU cells, and significantly accumulated cancer cells at the G2/M phase of the cell cycle by suppressing CDK1 and cyclin B protein with greater potency than SAHA-treated groups. Finally, CHC displayed strong inhibitory potency to drug-resistant hepatic tumors in mice. Our designed and synthetic hybrid CHC could be further developed as a significant and selective anticancer agent to potentially treat drug-resistant hepatocellular carcinoma.

研究领域: 药理学 · 肿瘤学 · 分子生物学
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BIOORGANIC CHEMISTRY · 2024 · IF 4.5

Rational design and synthesis of triazene-amonafide derivatives as novel potential antitumor agents causing oxidative damage towards DNA through intercalation mode

Ping Sun,Na Xu,Xue Zhang,Yun-Fei Gao,Jia-Yin Zhang,Qi-Ming Zhang,Chen Liang,Ri-Lei Yu,Ya-Mu Xia,Wei-Wei Gao

In this work, we rationally designed and synthesized two novel triazene-amonafide derivatives 2-(2-(diisopropylamino)ethyl)-5-(3,3-dimethyltriaz-1-en-1-yl)-1H-benzo[ de ]isoquinoline-1,3(2H)-dione ( D-11 ) and 5-(3,3-diethyltriaz-1-en-1-yl)-2-(2-(diisopropylamino)ethyl)-1H-benzo[ de ]isoquinoline-1,3(2H)-dione ( D-12 ) as potential antitumor agents. The DNA damage induced by the intercalation mode of D-11 ( D-12 ) towards DNA was electrochemically detected through the construction of efficient biosensors. The consecutive processes of reversible redox of naphthylimide ring and irreversible oxidation of triazene moiety were elucidated on the surface of glassy carbon electrode (GCE) by CV, SWV, and DPV methods. Electrochemical biosensors were obtained through the immobilization of ct DNA, G-quadruplexes, poly(dG), and poly(dA), respectively, on the clean surface of GCE. After the incubation of biosensors with D-11 or D-12 , the peaks of dGuo and dAdo decreased prominently, and the peak of 8-oxoGua appeared at +0.50 V, suggesting that the interaction between D-11 ( D-12 ) and DNA could result in the oxidative damage of guanine. Unexpected, the as-prepared DNA biosensor possessed satisfactory anti-interference property and good practicability in real samples. UV–vis and fluorescence spectra, and gel electrophoresis assays were employed to further confirm the intercalation mode of D-11 ( D-12 ) towards DNA base pairs. Moreover, D-11 was proved to exhibit stronger anti-proliferation activity than mitionafide and amonafide against both A549 and HeLa cell lines.

CAS / MDL: 50-81-7 63-91-2
研究领域: 药物化学 · 生物化学 · 分子生物学 · 癌症研究
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JOURNAL OF COORDINATION CHEMISTRY · 2019 · IF 1.685

A hydroxyquinoline-appended ruthenium(II)-polypyridyl complex that induces and stabilizes G-quadruplex DNA

Xuexue Xu,Shuang Wang,Yaxuan Mi,Huaqian Zhao,Zebao Zheng,Xiaolong Zhao

A polypyridyl ruthenium(II) complex with hydroxyquinoline-derived ligand has been synthesized and characterized. The ability to act as telomeric quadruplex inducer and stabilizer, and quadruplex-binding properties of the complex have been evaluated by absorption and emission analyses, fluorescent intercalator displacement (FID) titrations, circular dichroism (CD) spectroscopy, polymerase chain reaction (PCR) stop assay, color reaction studies, fluorescence resonance energy transfer (FRET) melting assay, Job plot, and molecular modeling. Observations revealed that the complex could well induce and stabilize the formation of antiparallel G-quadruplex of telomeric DNA in the presence or absence of metal cations, and showed superior G-quadruplex selectivity over duplex DNA with remarkable ΔTm value of 18.0 °C even at 50-fold excessive supplies of calf thymus (ct) DNA. The complex exhibited high interaction affinity of 2.56 × 106 M−1 with G-quadruplex DNA and evident luminescence enhancements of 3.1 and 4.2 times for quadruplex binding in Na+ and K+ buffer, respectively. In addition, the 1:1 [quadruplex]/[complex] binding mode ratio was determined. The results suggest that the complex can be developed as potential anticancer reagent through binding and stabilization of G-quadruplex DNA.

研究领域: 化学 · 生物化学 · 分子生物学 · 癌症研究
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