Liancai Zhu

DNA binding, cytotoxicity, apoptotic inducing activity, and molecular modeling study of quercetin zinc(II) complex

DNA cleavage activity of quercetin zinc(II) complex has been studied, but little attention has been devoted to the relationship between antitumor activity of this complex and DNA-binding properties. DNA-binding properties of quercetin zinc(II) complex were studied using UV-vis spectra, fluorescence measurements, and viscosity measurements. The results obtained indicate that quercetin zinc(II) complex can intercalate into the stacked base pairs of DNA, and compete with the strong intercalator ethidium bromide for the intercalative binding sites with Stern-Volmer quenching constant, K(sq)=1.24. The complex was subjected to biological tests in vitro using three tumor cell lines (HepG2, SMMC7721, and A549), which showed significant cytotoxicity against three tumor cell lines. Moreover, Hoechst33258 staining showed HepG2 cells underwent the typical morphologic changes of apoptosis characterized by nuclear shrinkage, chromatin condensation, or fragmentation after exposure to the complex. In addition, Molecular modeling was performed to learn the complex could be preferentially bound to DNA in GC region. Our results suggest that antitumor activity of quercetin zinc(II) complex might be related to its intercalation into DNA.

DNA binding and oxidative DNA damage induced by a quercetin copper(II) complex: potential mechanism of its antitumor properties.

The interaction of a quercetin copper(II) complex with DNA was investigated using UV–vis spectra, fluorescence measurement, viscosity measurement, agarose gel electrophoresis, and thiobarbituric acid reactive substances assay. The results indicate that the quercetin copper(II) complex can promote the cleavage of plasmid DNA, producing single and double DNA strand breaks, and intercalate into the stacked base pairs of DNA. Moreover, the complex can induce oxidative DNA damage involving generation of reactive oxygen species such as H2O2 and Cu(I)OOH. In addition, the cytotoxicity experiments carried out with A549 cells confirmed its apoptosis-inducing activity. And we also demonstrate that the levels of survivin protein expression in A549 cells decreased, and that relative activity of caspase-3 increased significantly after treatment with the complex. So our results suggest that the antitumor mechanism of the quercetin copper(II) complex involves not only its oxidative DNA damage with generation of reactive oxygen species but also its specific interaction with DNA.

Preparation of Eudragit L 100-55 enteric nanoparticles by a novel emulsion diffusion method.

In this study, a novel emulsion diffusion method was used to prepare enteric Eudragit L100-55 nanoparticles by ultrasonic dispersion and diffusion solidification. Omeprazole was selected as the model drug. The prepared nanoparticles were in spherical shape and exhibited negative zeta potential. The Fourier transform infrared spectroscopy results indicated that no molecular interaction occurred between the drug molecule and polymer chain. In addition, the nanoparticles showed a strong pH-sensitive release in vitro. A mild cytotoxicity of nanoparticle was observed in the subsequent studies, and the particle cellular uptake study showed that the nanoparticles could be taken up by Caco-2 cells after 0.5h incubation. Our results indicated that the enteric Eudragit L 100-55 nanoparticle could be synthesized successfully via this ultrasonic solidification method, which also could be applied to prepare other pH-sensitive polymer nanoparticles.

Regulation of survivin and Bcl-2 in HepG2 cell apoptosis induced by quercetin.

Quercetin, a widely distributed bioflavonoid, has been shown to induce growth inhibition in a variety of human cancer cells. However, the regulation of survivin and Bcl‐2 on the quercetin‐induced cell‐growth inhibition and apoptosis in cancer cells remains unclear. In the present study, we report that quercetin can inhibit proliferation and induce apoptosis in HepG2 cells in dose‐ and time‐dependent manner. Hoechst 33258 and acridine orange/ethidium bromide (AO/EB) staining showed that HepG2 cells underwent the typical morphologic changes of apoptosis characterized by nuclear shrinkage, chromatin condensation, or fragmentation after exposure to quercetin. Cell‐cycle analysis reveals a significant increase of the proportion of cells in G0/G1 phase. We also demonstrate that the levels of survivin and Bcl‐2 protein expression in HepG2 cells decreased concurrently, and the levels of p53 protein increased significantly after treatment with quercetin by immunocytochemistry analysis. Relative activity of caspase‐3 and caspase‐9 increased significantly. These data clearly indicate that quercetin‐induced apoptosis is associated with caspase activation, and the levels of survivin and Bcl‐2. Our results indicate that the expression of survivin may be associated with Bcl‐2 expression, and the inhibition expression of survivin, in conjunction with Bcl‐2, might cause more pronounced apoptotic effects. Together, concurrent down‐regulated survivin and Bcl‐2 play an important role in HepG2 cell apoptosis induced by quercetin.

Antioxidant activities of aqueous extract from Agrimonia pilosa Ledeb and its fractions.

Agrimonia pilosa Ledeb is used as the tonic for asthenia and fatigue in China. Considering that the energizing effect might be correlated with antioxidant properties, we investigated the antioxidant activities of aqueous extract (AE) from Agrimonia pilosa Ledeb by assessing radical‐scavenging and anti‐lipid‐peroxidation abilities. We found that AE shows a moderate antioxidant activity to scavenge DPPH., O

A novel improved therapy strategy for diabetic nephropathy: targeting AGEs.

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Influence of Harvest Season on Antioxidant Activity and Constituents of Rabbiteye Blueberry (Vaccinium ashei) Leaves

, and .OH and inhibit β‐carotene bleaching with IC50 values of 13.0, 33.2, 351, and 11.9 μg/ml, respectively, while its AcOEt‐soluble fraction (ESF) and BuOH soluble fraction (BSF) exhibit remarkable efficiencies. The ESFs IC50 values of scavenging DPPH., O

Cyclodipeptides from metagenomic library of a japanese marine sponge

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Formulation of porous poly(lactic-co-glycolic acid) microparticles by electrospray deposition method for controlled drug release.

, and .OH, and inhibiting β‐carotene bleaching are 5.6, 5.8, 171, and 7.6 μg/ml, respectively, and those of BSF are 7.5, 8.4, 82.0, and 6.2 μg/ml, respectively. In addition, we found that there is a significant correlation between total phenol content and the antioxidant activity determined by O

Selective binding of small molecules to DNA: application and perspectives.

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