DNA-Binding, Photocleavage, and Photodynamic Anti-cancer Activities of Pyridyl Corroles.

The DNA-binding, photocleavage, and antitumor activity of three free base pyridyl corroles 1, 2, and 3 have been investigated. The binding affinity toward CT-DNA decreases with increasing number of pentafluorophenyl, whereas the photocleavage activity toward pBR322 DNA becomes more efficient. Singlet oxygen was demonstrated as active species responsible for DNA cleavage. These corroles exhibited high cytotoxicity against three tested cancer cells (Hela, HapG2, and A549) and the cytotoxicity could be further enhanced under irradiation. Intracellular reactive oxygen species level was also monitored using HeLa Cells upon the combined treatment of corroles and light. These corroles could be absorbed by HeLa cells at low concentration. They can induce the decrease of mitochondrial membrane potential and apoptosis of tumor cells under irradiation.

Cytotoxicity, apoptosis, cell cycle arrest, reactive oxygen species, mitochondrial membrane potential, and Western blotting analysis of ruthenium(II) complexes.

Three new ruthenium(II) complexes-[Ru(bpy)2(adppz)](ClO4)2, [Ru(dmb)2(adppz)](ClO4)2, and [Ru(dmp)2(adppz)](ClO4)2 (bpy is 2,2'-bipyridine, adppz is 7-aminodipyrido[3,2-a:2',3'-c]phenazine, dmb is 4,4'-dimethyl-2,2'-bipyridine, and dmp is 2,9-dimethyl-1,10-phenanthroline)-were synthesized. [Ru(dmp)2(adppz)](ClO4)2 exhibits higher cytotoxicity than cisplatin toward A549, MG-63, and SKBR-3 cells. The apoptosis and cellular uptake were studied by fluorescence microscopy. [Ru(dmp)2(adppz)](ClO4)2 enhances the level of reactive oxygen species (ROS) and decreases the mitochondrial membrane potential. These complexes induce cell cycle arrest in S phase in BEL-7402 cells, and inhibit the antiproliferation of SKBR-3 cells at G0/G1 phase. Western blotting analysis shows that [Ru(dmp)2(adppz)](ClO4)2 induces apoptosis in BEL-7402 cells through activation of caspase 3, caspase 7, and procaspase 7 and ROS-mediated mitochondrial dysfunction pathways.

Two truxinate derivatives and a phenyldilactone from the leaves of Castanopsis eyrei.

Phytochemical investigation of the Leaves of Castanopsis eyrei led to the isolation of two new natural truxinate derivatives and a new phenyldilactone. The structures of the new natural compounds were determined by spectroscopic methods and chemical evidence as 3,3',4,4'-tetrahydroxy-ß-truxillic acid (1), 3,3',4,4'-tetrahydroxy-δ-truxillic acid (2), 3'-hydroxymaysedilactone A (3). Establishment of a Caenorhabditis elegans lipid metabolism model using GFP and mCherry fluorescently labeled lipid droplets to screen compound 3 for its activity in reducing lipid accumulation.

Plasma metabolites associated with physiological and biochemical indexes indicate the effect of caging stress on mallard ducks (Anas platyrhynchos).

OBJECTIVE: Cage rearing has critical implications for the laying duck industry because it is convenient for feeding and management. However, caging stress is a type of chronic stress that induces maladaptation. Environmental stress responses have been extensively studied, but no detailed information is available about the comprehensive changes in plasma metabolites at different stages of caging stress in ducks. We designed this experiment to analyze the effects of caging stress on performance parameters and oxidative stress indexes in ducks. METHODS: Liquid chromatography tandem mass spectrometry (LC/MS-MS) was used to determine the changes in metabolites in duck plasma at 5 (CR5), 10 (CR10), and 15 (CR15) days after cage rearing and traditional breeding (TB). The associated pathways of differentially altered metabolites were analyzed using Kyoto encyclopedia of genes and genomes (KEGG) database. RESULTS: The results of this study indicate that caging stress decreased performance parameters, and the plasma total superoxide dismutase levels were increased in the CR10 group compared with the other groups. In addition, 1,431 metabolites were detected. Compared with the TB group, 134, 381, and 190 differentially produced metabolites were identified in the CR5, CR10, and CR15 groups, respectively. The results of principal component analysis (PCA) show that the selected components sufficiently distinguish the TB group and CR10 group. KEGG analysis results revealed that the differentially altered metabolites in duck plasma from the CR5 and TB groups were mainly associated with ovarian steroidogenesis, biosynthesis of unsaturated fatty acids, and phenylalanine metabolism. CONCLUSION: In this study, the production performance, blood indexes, number of metabolites and PCA were compared to determine effect of the caging stress stage on ducks. We inferred from the experimental results that caging-stressed ducks were in the sensitive phase in the first 5 days after caging, caging for approximately 10 days was an important transition phase, and then the duck continually adapted.

2-(3,5-Dibromo-4-hydroxyphenyl)imidazo[4,5-f][1,10]phenanthrolinoruthenium(II) complexes: synthesis, characterization, cytotoxicity, apoptosis, DNA-binding and antioxidant activity.

A new ligand DBHIP and its two ruthenium(II) complexes [Ru(dmb)(2)(DBHIP)](ClO(4))(2) (1) and [Ru(dmp)(2)(DBHIP)](ClO(4))(2) (2) have been synthesized and characterized. The cytotoxicity of DBHIP and complexes 1 and 2 has been assessed by MTT assay. The apoptosis studies were carried out with acridine orange/ethidium bromide (AO/EB) staining methods. The binding behaviors of these complexes to calf thymus DNA (CT-DNA) were studied by absorption titration, viscosity measurements, thermal denaturation and photoactivated cleavage. The DNA-binding constants of complexes 1 and 2 were determined to be 8.64 +/- 0.16 x 10(4) (s = 1.34) and 2.79 +/- 0.21 x 10(4) (s = 2.17) M(-1). The results suggest that these complexes interact with DNA through intercalative mode. The studies on the mechanism of photocleavage demonstrate that superoxide anion radical (O(2)(*-)) and singlet oxygen ((1)O(2)) may play an important role in the DNA cleavage. The experiments on antioxidant activity show that these compounds also exhibit good antioxidant activity against hydroxyl radical (OH*).

Bis(2,9-dimethyl-1,10-phenanthroline-κN,N')(10,11,12,13-tetra-hydro-dipyrido[3,2-a:2',3'-c]phenazine-κN,N)ruthenium(II) bis-(perchlorate) dihydrate.

The title compound, [Ru(C(14)H(12)N(2))(2)(C(18)H(14)N(4))](ClO(4))(2)·2H(2)O, consists of an Ru(II) complex cation, two perchlorate anions and two uncoordinated water mol-ecules. The Ru(II) ion is chelated by a 10,11,12,13-tetra-hydro-dipyrido[3,2-a:2',3'-c]phenazine ligand and two 2,9-dimethyl-1,10-phenanthroline ligands in a distorted octa-hedral geometry. The two uncoord-inated water mol-ecules are disordered over five positions, with an occupancy factor of about 0.4 for each site. A supra-molecular structure is formed by weak π-π inter-actions between neighbouring mol-ecules, with centroid-centroid distances of 3.618 (2) and 3.749 (2) Å.

RbCa(2)Nb(3)O(10) from X-ray powder data.

Rubidium dicalcium triniobate(V), RbCa(2)Nb(3)O(10), has been synthesized by solid-state reaction and its crystal structure refined from X-ray powder diffraction data using Rietveld analysis. The compound is a three-layer perovskite Dion-Jacobson phase with the perovskite-like slabs derived by termination of the three-dimensional CaNbO(3) perovskite structure along the ab plane. The rubidium ions (4/mmm symmetry) are located in the inter-stitial space.

Isolation, culture, and identification of duck intestinal epithelial cells and oxidative stress model constructed.

Intestinal epithelial cells (IECs) not only have an absorption function but also act as a physical barrier between the body and the intestinal bacterial flora. Damage to IECs leads to the breakdown of this barrier and has negative effects on animal health. Intestinal epithelial damage is frequently associated with long-term acute stress, such as increased temperature and new stress management models. The intestinal epithelial damage caused by environmental stress has been linked to oxidative stress. Until now, the effects of intestinal epithelial antioxidant activity from feed additives and treatments could be tested in ducks only in vivo because of the lack of in vitro cell culture systems. In this study, we describe our protocol for the easy isolation and culture of IECs from the small intestine of duck embryos. Immunofluorescence was used for the cytological identification of IECs. In addition, IEC marker genes (IAP and CDH1) could also be detected in cultured cells. And cell status assessments were performed, and cell proliferation viability was analyzed by CCK-8 assay. Furthermore, we constructed an oxidative stress model to be used to research the oxidative stress response mechanism, and drugs acting on the cell signal transduction pathway. In conclusion, we have developed an effective and rapid protocol for obtaining duck primary IECs and constructed an oxidative stress model. These IECs exhibit features consistent with epithelial cells and could be used to explore the physiological mechanisms of oxidative stress ex vivo.

Synthesis, characterization, DNA interaction, antioxidant and anticancer activity studies of ruthenium(II) polypyridyl complexes.

Two new Ru(II) polypyridyl complexes [Ru(phen)2(adppz)](ClO4)2 (1) and [Ru(dip)2(adppz)](ClO4)2 (2) have been synthesized and characterized. The DNA-binding constants were determined to be 6.54 ± 0.42 × 10(5) and 7.65 ± 0.20 × 10(5)M(-1) for complexes 1 and 2. DNA binding experiments indicated that complexes 1 and 2 interact with DNA through intercalative mode. Antioxidant activity shows that the complexes have significant hydroxyl radical scavenging activity. Cytotoxic activities suggest that the complex 2 exhibits higher cytotoxic activity against BEL-7402, MG-63 and SKBR-3 cells than complex 1 under identical conditions. Complexes 1 and 2 can induce apoptosis of BEl-7402 cells. We have identified several cellular mechanisms induced by 1 and 2 in BEL-7402 cells, including the level detection of ROS, activation of procaspase 3, caspase 7, the expression of antiapoptotic proteins Bcl-x, Bcl-2, proapoptotic proteins Bad, Bax, Bid and cell cycle arrest. Thus, complexes 1 and 2 inhibit growth of BEL-7402 cells through induction of apoptotic cell death, enhancement of ROS levels and S-phase and G0/G1 cell cycle arrest. Further investigations have shown that complex 2 induces apoptosis by regulating the expression of Bcl-2 family proteins.

Synthesis, characterization, cellular uptake, apoptosis, cytotoxicity, dna-binding, and antioxidant activity studies of ruthenium(II) complexes.

Two new ruthenium(II) polypyridyl complexes [Ru(dmb)(2)(HECIP)](ClO(4))(2) (1) (HECIP = N-ethyl-4-[(1,10)-phenanthroline(5,6-f)imidazol-2-yl]carbazole, dmb = 4,4'-dimethyl-2,2'-bipyridine) and [Ru(dmp)(2)(HECIP)](ClO(4))(2) (2) (dmp = 2,9-dimethyl-1,10-phenanthroline) have been synthesized and characterized. The DNA-binding behaviors of the two complexes were investigated by absorption spectra, viscosity measurements, and photoactivated cleavage. The DNA-binding constants for complexes 1 and 2 were determined to be 8.03 (± 0.12) × 10(4) M(-1) (s = 1.62) and 2.97 (± 0.15) × 10(4) M(-1) (s = 1.82), respectively. The results suggest that these complexes interact with DNA through intercalative mode. The photocleavage of pBR322 DNA by Ru(II) complexes was investigated. The cytotoxicity of complexes 1 and 2 has been evaluated by the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide)] method. Complex 1 shows higher anticancer potency than 2 against the four tumor cell lines. Apoptosis and cellular uptake were investigated. The antioxidant activities of the ligand and these complexes were also performed.

Ruthenium(II) polypyridyl complexes: synthesis and studies of DNA binding, photocleavage, cytotoxicity, apoptosis, cellular uptake, and antioxidant activity.

Two ruthenium (II) complexes [Ru(dmb)2(APIP)](ClO4)2 (APIP=2-(2-aminophenyl)imidazo[4,5-f ][1,10]phenanthroline, dmb=4,4'-dimethyl-2,2'-bipyridine; 1) and [Ru(dmb)2(HAPIP)](ClO4)2 (HAPIP=2-(2-hydroxyl-4-aminophenyl)imidazo[4,5-f ][1,10]phenanthroline; 2) were synthesized and characterized. DNA binding was investigated by electronic absorption titration, luminescence spectra, thermal denaturation, viscosity measurements, and photocleavage. The DNA binding constants for complexes 1 and 2 were 4.20 (±0.14)×10(4) and 5.45 (±0.15)×10(4) M(-1). The results suggest that these complexes partially intercalate between the base pairs. The cytotoxicity of complexes 1 and 2 was evaluated by MTT assay. Cellular uptake was observed under fluorescence microscopy; complexes 1 and 2 can enter into the cytoplasm and accumulate in the nuclei. Apoptosis and the antioxidant activity against hydroxyl radicals (•OH) were also explored.

Cytotoxicity, apoptosis, cellular uptake, cell cycle arrest, photocleavage, and antioxidant activity of 1, 10-phenanthroline ruthenium(II) complexes.

Two new ruthenium(II) complexes, [Ru(phen)2(DNPIP)](ClO4)2 (1) and [Ru(phen)2(DAPIP)](ClO4)2 (2), were synthesized and characterized. The DNA-binding properties of these complexes were investigated using UV/vis absorption titration, viscosity measurements, thermal denaturation, and photoactivated cleavage. The DNA binding constants for complexes 1 and 2 are 2.63 ± 0.25×10(5) M(-1) (s=2.45) and 1.51±0.18×10(5) M(-1) (s=1.34). The results indicated that these complexes interacted with DNA through the intercalative mode. The cytotoxicity in vitro of complexes 1 and 2 were assessed against BEL-7402, HepG-2, and MCF-7 cell lines by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Apoptosis was studied with the acridine orange/ethidium bromide staining method. The antiproliferative mechanism was explored with flow cytometry. Cellular uptake studies showed that complexes 1 and 2 can enter into the cytoplasm and accumulate in the nuclei. Cell cycle arrest and antioxidant activity were also investigated.

Synthesis, cellular uptake, apopotosis, cytotoxicity, cell cycle arrest, interaction with DNA and antioxidant activity of ruthenium(II) complexes.

A new ligand and two ruthenium(II) complexes [Ru(bpy)(2)(DNPIP)](ClO(4))(2)1 and [Ru(bpy)(2)(DAPIP)](ClO(4))(2)2 were synthesized and characterized. The DNA-binding constants for complexes 1 and 2 were determined to be 2.24 (±0.30) × 10(5) M(-1) (s = 1.29) and 6.34 (±0.32) × 10(4) M(-1) (s = 2.84). The photocleavage of pBR322 DNA by Ru(II) complexes was investigated. The cytotoxicity of complexes 1 and 2 were assessed against three tumor cell lines. The apoptosis and cellular uptake were studied. The retardation assay of pGL 3 plasmid DNA was explored. The cell cycle arrest was analysized by flow cytometry. The antioxidant activities of the ligand and complexes were also investigated.

Hot-injection synthesis of highly luminescent and monodisperse CdS nanocrystals using thioacetamide and cadmium source with proper reactivity.

Thioacetamide (TAA) has served as an excellent sulfur source to react with cadmium stearate to controllably produce highly luminescent and monodisperse CdS nanocrystals through the hot-injection method in dodecylamine solvent. The kinetics and thermodynamics of nucleation/growth of CdS nanocrystals, as well as their optical properties are controlled by changing synthesis conditions such as reaction time, injection/growth temperatures, TAA concentration and cadmium source with different reactivity. Temperature-dependent release of reactive sulfur species from TAA, together with proper reactivity of cadmium source, facilitates the better separation of nucleation and growth stage, the formation of highly monodisperse CdS nanocrystals with tunable size and further self-assembly into ordered superlattices. When cadmium carboxylates such as cadmium stearate and cadmium oleate are used as cadmium sources, surface trap emission of CdS nanocrystals can be gradually removed to obtain bright pure-blue emission with increasing reaction time. The highest quantum efficiency of up to 33.6% is achieved when using cadmium stearate as cadmium source at the injection/growth temperatures of 230/210 degrees C for 90min.

Synthesis of ruthenium(II) complexes and characterization of their cytotoxicity in vitro, apoptosis, DNA-binding and antioxidant activity.

A new ligand DBHIP and its two ruthenium (II) complexes [Ru(bpy)(2)(DBHIP)](ClO(4))(2) (1) and [Ru(phen)(2)(DBHIP)](ClO(4))(2) (2) have been synthesized and characterized. The binding behaviors of the two complexes to calf thymus DNA were investigated by absorption spectra, viscosity measurements, thermal denaturation and photoactivated cleavage. The DNA-binding constants for complexes 1 and 2 have been determined to be 8.87+/-0.27 x 10(4)M(-1) (s=1.83) and 1.32+/-0.31 x 10(5)M(-1) (s=1.84). The results suggest that these complexes interact with DNA through intercalative mode. The cytotoxicity of DBHIP, complexes 1 and 2 has been evaluated by MTT assay. The apoptosis assay was carried out with acridine orange/ethidium bromide (AO/EB) staining methods. The studies on the mechanism of photocleavage demonstrate that superoxide anion radical (O(2)(-)) and singlet oxygen ((1)O(2)) may play an important role.