Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards

Tianjin, China

Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards

Tianjin, China
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Wang N.,Beijing Corps First Hospital of Chinese Peoples Armed Police Forces | Xu R.-C.,Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards
Chinese Journal of Pharmacology and Toxicology | Year: 2010

OBJECTIVE: To study the effect of ouabain (strophanthin G) on human vascular endothelial ECV304 apoptosis and the possible mechanism. METHODS: ECV304 cells were treated with ouabain 0.01, 0.05, 0.1, 0.5, 1 and 10 μmol·L-1 for 24,48 and 72 h. The survival rates of cells were detected by MTT assay; cells morphological changes were studied by Hoechst 33342/propidium iodide staining; cell cycle distribution was detected by flow cytometry; and the concentrations of the intracellular free calcium ion ([Ca2+]i) and reactive oxygen species (ROS) in ECV304 cells were measured by the laser confocal microscope. The caspase 3 mRNA and protein expression level on ECV304 cells were detected by RT-PCR and Western blotting, respectively. RESULTS: Ouabain 0.01 - 10 μmol·L-1 was incubated with ECV304 cells for 24,48 and 72 h. The inhibition rate of cell survival was increased in a concentration- and time-dependent manner. The coefficient of concentration-correlation was 0.984, 0.994 and 0.997 (P < 0.05), respectively. IC50 of ouabain at 24,48 and 72 h was 0.624, 0.184 and 0.041 μmol·L-1 and the coefficient of time-correlation was 0.974(P < 0.05). Compared with normal control group, the apoptosis rate of ECV304 cells treated with ouabain 0.1 μmol·L -1, from increased from (4.2 ± 0.5)% to (26.0 ± 3.2)% at 24 h, and from (4.7 ± 0.5)% to (36.5 ± 5.3)% at 48 h, being statistically significant (n = 3, P < 0.01). The cells showed obviously defluxion and nuclear chromatin condensation when treated with ouabain 0.1 μmol·L-1 for 24 and 48 h. The [Ca2+]i and ROS concentration in ECV304 cells significantly increased in a concentration- and time-dependant manner after ECV304 cells were incubated with ouabain 0.01, 0.1 and 0.5 μmol·L-1 for 12, 24 and 36 h, respectively. When ouabain was 0.5 μmol·L-1, the coefficient of time-correlation of [Ca2+]i and ROS concentration were 0.912 and 0.924, respectively. When the ECV304 cells was incubated with ouabain for 36 h, the coefficient of concentration-correlation of [Ca2+]i and ROS concentration were 0.889 and 0.907 (P < 0.05), respectively. The RT-PCR and Western blotting results showed that caspase 3 mRNA expression was up-regulated after ECV304 cells were treated with ouabain 0.1 and 0.5 μmol·L-1 for 24 h, being of statistical significance (P < 0.05); caspase 3 protein expression was up-regulated after ECV304 cells were treated with ouabain 0.01, 0.1 and 0.5 μmol·L -1 for 24 h, statistically significant (P < 0.05). CONCLUSION: Ouabain induces ECV304 apoptosis by increasing [Ca2+]i, ROS concentration and up-regulating caspase 3 expression.


Tian D.-L.,Tianjin Medical University | Luo G.,Tianjin Medical University | Chen H.,Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards
Acta Crystallographica Section E: Structure Reports Online | Year: 2011

In title compound, C 16H 17FN 2O 2, the cyclo-hexane ring adopts a chair conformation. The crystal packing is stabilized by weak π-π stacking inter-actions [centroid-centroid distance = 3.503 (5) Å] and inter-molecular C - H⋯O, N - H⋯O and N - H⋯F hydrogen-bond inter-actions. © Tian et al. 2011.


Tang X.-W.,Tianjin Medical University | Chen H.,Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards | Tian D.-L.,Tianjin Medical University | Shi S.-Y.,Tianjin Medical University
Acta Crystallographica Section E: Structure Reports Online | Year: 2011

In the title compound, C16H20N2O 3, the crystal packing is stabilized by weak π-π stacking interactions [centroid-centroid distances = 3.577 (9) and 3.693 (9) Å] and intermolecular C-H⋯O and N-H⋯O hydrogen-bond interactions. The C atoms of the N-isopropyl group are disordered over two sets of sites with occupancies of 0.61(3) and 0.39(3).


Li Y.,General Hospital | Wang H.,Affiliated Hospital | Chen H.,Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards
Acta Crystallographica Section E: Structure Reports Online | Year: 2011

In the title compound, C31H34N2O 7, the fused tetra-hydro-furan and six-membered rings each display an envelope conformation. The dihedral angles between the benzene ring of the benzo[d][1,3]dioxole and the other two benzene rings are 89.68 (3) and 63.38 (2)°. In the crystal, weak inter-molecular C - H⋯O hydrogen bonds link the mol-ecules.


Chen L.-T.,Tianjin Medical University | Chen H.,Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards | Zhou J.,Tianjin Medical University
Acta Crystallographica Section E: Structure Reports Online | Year: 2011

The title compound, C20H20N2O4, crystallizes with four independent molecules in the asymmetric unit. In the molecules, the dihedral angles between the benzene rings and indole mean planes are 24.5 (1), 22.5 (1), 8.8 (1) and 13.9 (1)°. In the crystal, intermolecular N -H⋯O hydrogen bonds are present between the imino groups and the adjacent carbonyl groups. π-π stacking is also observed with a centroidcentroid distance between nearly parallel pyrrole rings of 3.745 (3) Å.


Liu J.,Tianjin Medical University | Chen H.,Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards
Acta Crystallographica Section E: Structure Reports Online | Year: 2011

In the title compound, C17H20N2O 3, the cyclohexane ring adopts a chair conformation. In the crystal, intermolecular N -H⋯O hydrogen bonds link the molecules into layers parallel to the ac plane.


Luo G.,Tianjin Medical University | Zhou J.,Tianjin Medical University | Tian D.-L.,Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards | Zhang S.,Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards
Acta Crystallographica Section E: Structure Reports Online | Year: 2011

In title compound, C 27H 27NO 8, the dihydrofuran-2(3H)-one ring and the six-membered ring fused to it both display envelope conformations. The dihedral angle between the benzene ring of the benzo[d][1,3]dioxole group and the other benzene ring is 60.59 (2)°. In the crystal, weak Intermolecular C - H⋯O hydrogen bonds link the molecules into a three-dimensional network. The furan ring is disordered over two sets of sites with occupancies of 0.722 (7) and 0.278 (7).


Chen H.,Affiliated Hospital | Chen H.,Medical College | Chen H.,Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards | Tian D.-L.,Medical College | And 2 more authors.
Acta Crystallographica Section E: Structure Reports Online | Year: 2011

In the title compound, C30H32N2O 7·CH4O, the tetra-hydro-furan ring and the six-membered ring fused to it both display envelope conformations, with the ring C atom opposite the carbonyl group and the adjacent bridgehead C atom as the flaps, respectively. In the crystal structure, inter-molecular O - H⋯O hydrogen bonds link all moieties into ribbons along [010]. Weak inter-molecular C - H⋯O inter-actions consolidate the crystal packing further. © Chen et al. 2011.


Zhu T.-L.,Affiliated Hospital | Jin J.-R.,Chinese Peoples Armed Police Force Hospital in Tianjin | Chen H.,Tianjin Key Laboratory for Biomarkers of Occupational and Environmental Hazards | Chen H.,Medical College | And 2 more authors.
Acta Crystallographica Section E: Structure Reports Online | Year: 2011

In the title compound, C29H28ClNO7, the tetra-hydro-furan ring and the six-membered ring fused to it both display envelope conformations. The dihedral angles between the plane of the benzene ring of the benzo[d][1,3]dioxole system and the planes of the other two benzene rings are 80.59 (3) and 63.60 (2)°.


Xu Z.-W.,Medical College | Wang F.-M.,Tianjin 3rd Central Hospital | Gao M.-J.,Medical College | Chen X.-Y.,Medical College | And 6 more authors.
Journal of Steroid Biochemistry and Molecular Biology | Year: 2011

Recent studies revealed the potential of Na+/K +-ATPase as a target for anticancer therapy and showed additional modes of action of cardiotonic steroids (CSs), a diverse family of naturally derived compounds, as inhibitors of Na+/K+-ATPase. The results from epidemiological studies showed significantly lower mortality rates in cancer patients receiving CSs, which sparked interest in the anticancer properties of these drugs. The present study was designed to investigate the anticancer effect of CSs (ouabain or cinobufagin) and to elucidate the molecular mechanisms of CS activity in hepatoma cell lines (HepG2 and SMMC-7721). Ouabain and cinobufagin significantly inhibited cell proliferation by attenuating the phosphorylation of extracellular regulated kinase (ERK) and down-regulating the expression of C-myc. These CSs also induced cell apoptosis by increasing the concentration of intracellular free calcium ([Ca2+]i) and induced S phase cell cycle arrest by down-regulating the expression of Cyclin A, cyclin dependent kinase 2 (CDK2) and proliferating cell nuclear antigen (PCNA) as well as up-regulating the expression of cyclin dependent kinase inhibitor 1A (p21CIP1). Overexpression of ERK reversed the antiproliferation effect of ouabain or cinobufagin in HepG2 and SMMC-7721 cells. Currently, the first generation of CS-based anticancer drugs (UNBS1450 and Anvirzel) are in Phase I clinical trials. These data clearly support their potential use as cancer therapies. © 2011 Elsevier Ltd. All rights reserved.

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