[Structure and diversity of nirK-type denitrifying microbial community in marsh soils at different invasion stages of Spartina alterniflora in the Minjiang River estuary, China.] / é—½æ±Ÿæ²³å£äº’èŠ±ç±³è‰ä¸åŒå ¥ä¾µé˜¶æ®µæ¹¿åœ°åœŸå£¤nirKåž‹åç¡åŒ–å¾®ç”Ÿç‰©ç¾¤è½ç»“æž„åŠå¤šæ ·æ€§.

To explore the differences in structure and diversity of nirK-type denitrifying microbial community in marsh soils at different invasion stages of Spartina alterniflora, the mudflat (MF, before invasion) and the S. alterniflora marsh after seaward invasion for 1-2 years (SAN) and 6-7 years (SA) in Shanyutan of the Minjiang River estuary were investigated by high-through put sequencing method. Results showed that the seaward invasion of S. alterniflora reduced the richness and diversity of nirK-type denitrifying microbial community in marsh soils. The nirK-type denitrifying microbial community in soils at different invasion stages included Proteobacteria and Actinobacteria, with Proteobacteria as the dominant one. The seaward invasion of S. alterniflora greatly altered the composition of nirK-type denitrifying microbial community in marsh soils. The highest relative abundance of genus in soils from different invasion stages were Bradyrhizobium, Mesorhizobium and Alcaligenes, respectively. The seaward invasion of S. alterniflora increased the spatial heterogeneity of nirK-type denitrifying microbial community composition in marsh soils. In SAN plot, the enhancement of spatial heterogeneity was primarily due to higher environmental disturbances in plots and the increased spatial heterogeneity of environmental variables caused by the seaward invasion of S. alterniflora. The seaward invasion of S. alterniflora altered the physico-chemical properties (e.g., grain composition, pH and moisture) and N nutrient conditions (total N, NH4+-N and NO3--N) in marsh soils, which greatly altered the structure and diversity of nirK-type denitrifying microbial community. Our findings reveal the microbial mechanism of denitrification process in marsh soils during the seaward invasion of S. alterniflora.

[Phosphorus forms in marsh soils with different years of Spartina alterniflora invasion in the Minjiang River estuary, China]. / é—½æ±Ÿæ²³å£äº’èŠ±ç±³è‰ä¸åŒå ¥ä¾µå¹´é™æ¹¿åœ°åœŸå£¤ç£·èµ‹å­˜å½¢æ€.

We examined the effects of Spartina alterniflora invasion on phosphorus forms of marsh soils, based on the method of space-for-time substitution by selecting S. alterniflora marshes with different invasion years (SA1, 5-6 years; SA2, 8-10 years; and SA3, 12-14 years) in Shanyutan of the Minjiang River estuary. The results showed that in marsh soils of different invasion years, the proportion of hardly decomposable phosphorus (HCl-Pi and Residual-P) was the highest (46.4%-46.7%), followed by moderately decomposable phosphorus (NaOH-Pi, NaOH-Po and Sonic-Pi) (40.0%-44.0%), and the easily decomposable phosphorus (Resin-Pi, NaHCO3-Pi and NaHCO3-Po) was the lowest (9.5%-13.3%). With increasing invasion years of S. alterniflora, soil phosphorus forms and their spatial distributions were greatly altered. The contents of moderately decomposable phosphorus, hardly decomposable phosphorus, and total phosphorus (TP) generally increased, while easily decomposable phosphorus content generally decreased. Compared with SA1, the contents of moderately decomposable phosphorus, hardly decomposable phosphorus and TP in SA2 increased by 11.5%, 9.7% and 10.5%, while those in SA3 increased by 24.8%, 13.2% and 13.5%, respectively. The distribution of phosphorus forms was greatly altered with increasing invasion years, which was dependent on the variations of key factors such as EC, pH value and grain composition. The implementation of regular mowing activities for S. alterniflora in the Minjiang River estuary in recent years, to some extent, reduced the return of phosphorus from residues to soils and decreased the availability of the easily decomposable phosphorus in soils.

[Sulfur oxidation-reduction process and its coupling effects with other elements in marsh soil: A review]. / 湿地土壤硫氧化-è¿˜åŽŸè¿‡ç¨‹åŠå ¶ä¸Žå ¶ä»–å ƒç´ çš„è€¦åˆä½œç”¨ç ”ç©¶è¿›å±•.

Sulfur oxidation-reduction process (SORP) in marsh soil is an important link in sulfur cycle, which plays an important role in maintaining the stability and health of marsh. We summarized the SORP in marsh soil and its influencing factors, and analyzed the research progress of its coupling effects with other elements. The influencing factors of SORP in marsh soil mainly involved biotic (plants, microorganisms, zoobenthos, human activities, etc.) and abiotic factors (physical factors such as temperature, moisture and particle size, and chemical factors such as pH, salinity, organic matter, etc.). Related research on the coupling effects of SORP and other elements in marsh soil mainly involved in biogenic elements such as carbon (C), nitrogen (N) and phosphorus (P), and metal elements such as iron (Fe) and manganese (Mn). Currently, the underlying mechanism of SORP was not deeply explored, the research on coupling effects was unbalance, and the ecological effects were insufficient. In the future, key functional microorganisms involved in SORP should be strengthened, the coupling mechanism between SORP and micro-elements should be enhanced, and the ecological effects produced by the coupling effects of SORP with other elements should be emphasized.

[Mechanism of Huanglian Wendan Decoction in improving impaired glucose tolerance based on skeletal muscle NLRP3/caspase-1/IL-1ß, IL-18 pathway].

This study investigated the mechanism of improving impaired glucose tolerance(IGT) of rats by Huanglian Wendan Decoction from the perspective of the skeletal muscle Nod-like receptor protein 3(NLRP3)/cysteinyl aspartate specific proteinase-1(caspase-1)/interleukin-1ß(IL-1ß), interleukin-18(IL-18) pathway. Healthy male SD rats were fed with the diet containing 45% fat for 20 weeks, accompanied by a high-temperature and high-humidity environment and an inactive lifestyle, for the establishment of the IGT rat model. The rats were divided into the blank control group, model control group, metformin hydrochloride group(positive drug group, 0.05 g·kg~(-1)·d~(-1)) and Huanglian Wendan Decoction group(7.8 g·kg~(-1)·d~(-1)). After continuous intragastric administration for 4 weeks, the obesity and glycemic indexes of all the rats were measured. The fasting serum insulin(FINS) level was determined by ELISA, with the insulin sensitivity index(ISI) and insulin resistance index(IRI) calculated. The mRNA and protein expression le-vels of nuclear factor kappaB(NF-κB), NLRP3, caspase-1, IL-1ß and IL-18 in skeletal muscle tissue were detected by real-time polymerase chain reaction(PCR), Western blot and immunofluorescence. Compared with the blank control group, the model control group witnessed significantly increased mRNA and protein expression of NF-κB, NLRP3, caspase-1, IL-1ß and IL-18. As revealed by the comparison with the model control group, Huanglian Wendan Decoction could effectively regulate the obesity status, reduce body weight, correct the abnormal levels of 2-hour plasma glucose(2 hPG), insulin resistance index(IRI), insulin sensitivity index(ISI), and lower the mRNA and protein expression of NF-κB, NLRP3, caspase-1, IL-1ß and IL-18 in the skeletal muscle tissue of IGT rats. Combined with previous studies, the above results showed that the occurrence and development of IGT was closely related to inflammatory response and the classic pyroptosis pathway in skeletal muscle, such as NLRP3/caspase-1/IL-1ß, IL-18. It is inferred that the mechanism of Huanglian Wendan Decoction was to alleviate insulin resistance(IR) and then reverse the course of IGT lies in the regulation of the abnormal insulin receptor signaling pathway based on the NLRP3 inflammasome pathway.

Copy number variation in the CES1 gene and the risk of non-alcoholic fatty liver in a Chinese Han population.

A recent genome-wide copy number variations (CNVs) scan identified a 16q12.2 deletion that included the carboxylesterase 1 (CES1) gene, which is important in the metabolism of fatty acids and cholesterol. We aimed to investigate whether CES1 CNVs was associated with susceptibility to non-alcoholic fatty liver disease (NAFLD) in a Chinese Han population. A case-control study was conducted among 303 patients diagnosed with NAFLD and 303 age (± 5) and sex-matched controls from the Affiliated Nanping First Hospital of Fujian Medical University in China. The copy numbers of CES1 were measured using TaqMan quantitative real-time polymerase chain reaction (qPCR) and serum CES1 was measured using enzyme-linked immunosorbent assays. The Chi-squared test and a logistic regression model were used to evaluate the association between CES1 CNVs and NAFLD susceptibility. The distribution of CES1 CNVs showed a higher frequency of CNVs loss (< 2) among patients; however, the difference was not significant (P = 0.05). After controlling for other known or suspected risk factors for NAFLD, CES1 CNVs loss was significantly associated with greater risk of NAFLD (adjusted OR = 2.75, 95% CI 1.30-5.85, P = 0.01); while CES1 CNVs gain (> 2) was not. There was a suggestion of an association between increased CES1 serum protein levels and CNVs losses among cases, although this was not statistically significant (P = 0.07). Copy number losses (< 2) of CES1 contribute to susceptibility to NAFLD in the Chinese Han population.

Cyclometalated iridium(III) complexes as mitochondria-targeted anticancer and antibacterial agents to induce both autophagy and apoptosis.

Mitochondrial damage will hinder the energy production of cells and produce excessive ROS (reactive oxygen species), resulting in cell death through autophagy or apoptosis. In this paper, four cyclometalated iridium(III) complexes (Ir1: [Ir(piq)2L]PF6; Ir2: [Ir(bzq)2L]PF6; Ir3: [Ir(dfppy)2L]PF6; Ir4: [Ir(thpy)2L]PF6; piq = 1-phenylisoquinoline; bzq = benzo[h]quinoline; dfppy = 2-(2,4-difluorophenyl)pyridine;thpy = 2-(2-thienyl)pyridine; L = 1,10-phenanthroline-5-amine) were synthesized and characterized. Cytotoxicity tests show that these complexes have excellent cytotoxicity to cancer cells, and mechanism studies indicatethat these complexes can specifically target mitochondria. Complexes Ir1 and Ir2 can damage the function of mitochondria, subsequently increasing intracellular levels of ROS, decreasing MMP (mitochondrial membrane potential), and interfering with ATP energy production, which leads to autophagy and apoptosis. Furthermore, autophagy induced by Ir1 and Ir2 can promote cell death in coordination with apoptosis. Surprisingly, these four complexes also showed moderate antibacterial activity to S. aureusand P. aeruginosa.

Mitochondria-targeted Re(I) complexes bearing guanidinium as ligands and their anticancer activity.

As the "powerhouse" of a cell, mitochondria maintain energy homeostasis, synthesize ATP via oxidative phosphorylation, generate ROS signaling molecules, and modulate cell apoptosis. Herein, three Re(I) complexes bearing guanidinium derivatives have been synthesized and characterized. All of these complexes exhibit moderate anticancer activity in HepG2, HeLa, MCF-7, and A549 cancer cells. Mechanism studies indicate that complex 3, [Re(CO)3(L)(Im)](PF6)2, can selectively localize in the mitochondria and induce cancer cell death through mitochondria-associated pathways. In addition, complex 3 can effectively depress the ability of cell migration, cell invasion, and colony formation.

Silver Single Atom in Carbon Nitride Catalyst for Highly Efficient Photocatalytic Hydrogen Evolution.

Single atom catalysts (SACs) with the maximized metal atom efficiency have sparked great attention. However, it is challenging to obtain SACs with high metal loading, high catalytic activity, and good stability. Herein, we demonstrate a new strategy to develop a highly active and stable Ag single atom in carbon nitride (Ag-N2 C2 /CN) catalyst with a unique coordination. The Ag atomic dispersion and Ag-N2 C2 configuration have been identified by aberration-correction high-angle-annular-dark-field scanning transmission electron microscopy (AC-HAADF-STEM) and extended X-ray absorption. Experiments and DFT calculations further verify that Ag-N2 C2 can reduce the H2 evolution barrier, expand the light absorption range, and improve the charge transfer of CN. As a result, the Ag-N2 C2 /CN catalyst exhibits much better H2 evolution activity than the N-coordinated Ag single atom in CN (Ag-N4 /CN), and is even superior to the Pt nanoparticle-loaded CN (PtNP /CN). This work provides a new idea for the design and synthesis of SACs with novel configurations and excellent catalytic activity and durability.

The effect of apatinib on pharmacokinetic profile of buspirone both in vivo and in vitro.

OBJECTIVE: In this study, we aimed to investigate the potential interaction of apatinib and buspirone and underlying mechanism. METHODS: UPLC-MS/MS assay was applied to determine the concentrations of buspirone and its main metabolites (1-PP and 6-OH buspirone) after incubated with liver microsomes. Moreover, the connection of in vitro and in vivo was further determined. Sprague Dawley rats were randomly divided into two groups: group A (20 mg/kg buspirone) and group B (buspirone vs 40 mg/kg apatinib). Tail vein blood was collected and subjected to the UPLC-MS/MS detection. KEY FINDINGS: Apatinib inhibited the generations of 1-PP and 6-OH buspirone dose-dependently with IC50 of 1.76 and 2.23 µm in RLMs, and 1.51 and 1.48 µm in HLMs, respectively. There was a mixed mechanism underlying such an inhibition effect. In rat, AUC(0- t ) , AUC(0-∞) , Tmax and Cmax of buspirone and 6-OH buspirone increased significantly while co-administering with apatinib, but Vz/F and CLz/F decreased obviously while comparing group A with group B . CONCLUSIONS: Apatinib suppresses the CYP450 based metabolism of buspirone in a mixed mechanism and boosted the blood exposure of prototype drug and 6-OH buspirone dramatically. Therefore, extra caution should be taken when combining apatinib with buspirone in clinic.

[Effects of spatial expansion of Phragmites australis and Cyperus malaccensis on distributions and stocks of phosphorus in marshes in the Minjiang River estuary, China.] / 闽江河口芦苇与短叶茳芏空间扩展对湿地系统磷赋存特征的影响.

To investigate the distributions and stocks of total phosphorus (TP) in plant-soil systems of marshes in Shanyutan of the Minjiang River estuary and explore its influencing factors, Phragmites australis (PA) marsh and Cyperus malaccensis (CM) marsh before spatial expansion and ecotonal marsh (EM, P. australis and C. malaccensis in EM were denoted by PA' and CM', respectively) during spatial expansion were studied. Results showed that, as affected by spatial expansion, the contents of TP in both plant and soil in different marshes showed great variations. Compared with PA and CM marshes, soil TP in EM increased by 20.0% and 7.1%, respectively. The variation of soil TP in EM might be attributed to the alteration of soil particle composition, plant bio-mass and root/shoot ratio during spatial expansion. Except for leaves, TP in organs of P. australis in P. australis-C. malaccensis community (PA') was lower than that in C. malaccensis in P. australis-C. malaccensis community (CM'), due to the differences in absorption, utilization and translocation way of P among organs between the two species. The competition effect caused by spatial expansion greatly changed plant P allocation ratio of the two species. Compared with PA and CM, the allocations of P in roots and leaves of PA' increased, while only that in roots of CM' rose. During spatial expansion, the two species might adopt different adaptation strategies for P absorption and utilization to maintain their competitiveness. The PA might compete primarily by strengthening the P accumulation capacities of its roots and promoting leaf photosynthesis, whereas the CM might resist the spatial expansion of PA by increasing its underground biomass to enhance P absorption.

[Discharge and Contents of Exosome from Leukocyte-Reduced Apheresis Platelet Stored for Different Storage Time].

OBJECTIVE: To explore the effect of storage time on discharge and content of exosome from leukocyte-reduced apheresis platelets (LRA-Plt). METHODS: Exosome (EXO) from LRA-Plt were acquired by ExoQuick, and its' morphology, immunological marker and particle size distribution were detected by transmission electron microscopy (TEM), Western blotting and dynamic light scattering (DLS), respectively. The changes in particle size distribution of EXO from LRA-Plt with different storage time were detected by DLS. The changes in content of protein and RNA of EXO from LRA-Plt with different storage time were detected by Nanodrop® ND-2000. RESULTS: EXO from LRA-Plt was acquired successfully, which was characterized by cup-like shape, CD63/TSG101 enriched and Calnexin negative, and the particle size of which ranged from 30 to 200 nm. At early stored stage (stored for 1 day and 2 days), particle size of EXO from LRA-Plt was small and ranges from 30 to 40 nm. Meanwhile, the contents of protein and RNA were low. The particle size distribution, contents of protein and RNA of EXO from LRA-Plt were not significanty different ammg groups (P＞0.05). At middle-late stored stage (stored for 3, 4 and 5 days), the particle size of EXO from LRA-Plt was larger than that of early stored stage, which ranges was from 130 to 200 nm. Meanwhile, the contents of protein and RNA were higher than those of early stored stage. Particle size distribution, contents of protein and RNA of EXO from LRA-Plt stored for middle-late stage were significant higher than those of early stored stage (P＜0.05). CONCLUSION: Morphology of EXO from LRA-Plt stored for middle-late stage was different from that stored for early stored stage. Moreover, the particle size distribution, contents of protein and RNA of EXO from LRA-Plt stored for middle-late stage were higher than those of early stored stage. A large amount of protein and RNA contained in EXO from LRA-Plt may participate in the multiple functions caused by platelet transfusion.

[Effects of Spartina alterniflora invasion in a seaward direction on variations of inorganic sulfur forms in marsh soils of the Minjiang River estuary, China]. / é—½æ±Ÿæ²³å£äº’èŠ±ç±³è‰æµ·å‘å ¥ä¾µå¯¹æ¹¿åœ°åœŸå£¤æ— æœºç¡«èµ‹å­˜å½¢æ€çš„å½±å“.

To explore the effects of Spartina alterniflora invasion in a seaward direction on variations of inorganic sulfur forms in marsh soils, the levels of inorganic sulfur forms (H2O-S, Adsorbed-S, HCl-Soluble-S and HCl-Volatile-S) were determined in bare flat (BF, before invasion), S. alterniflora marsh after seaward invasion for one year (SA') and S. alterniflora marsh after seaward invasion for three years (SA) in Shanyutan of the Minjiang River estuary with the method of space-for-time substitution. Results showed that the seaward invasion of S. alterniflora altered the stocks and distribution of inorganic sulfur form in marsh soils. Compared with BF, the contents of H2O-S, Adsorbed-S and HCl-Volatile-S in soils of SA increased by 52.6%, 78.2% and 21.0%, respectively, while that of HCl-Soluble-S decreased by 3.4%. In contrast, the levels of H2O-S, Adsorbed-S and HCl-Soluble-S in soils of SA' increased by 43.9%, 70.6% and 29.6%, respectively, whereas that of HCl-Volatile-S decreased by 11.6%. The contents of total inorganic sulfur (TIS) in soils of SA and SA' increased by 40.7% and 37.8%, while the stocks of TIS increased by 26.8% and 31.4%, respectively. The key factors affecting different forms of inorganic sulfur in marsh soils had changed due to the seaward invasion of S. alterniflora. In particular, the key factors affecting the variations of H2O-S contents changed from soil grain composition and bulk density in BF to soil organic matter in SA' and SA. The seaward invasion of S. alterniflora significantly increased the content of TIS in marsh soils, which was mainly contributed by H2O-S and Adsorbed-S. Thus, it was concluded that the seaward invasion of S. alterniflora significantly increased the supply capacity of available sulfur in marsh soils, which, to some extent, accelerated its seaward invasion.

Optimization of Low-Dimensional Components of Quasi-2D Perovskite Films for Deep-Blue Light-Emitting Diodes.

Compared to efficient green and near-infrared light-emitting diodes (LEDs), less progress has been made on deep-blue perovskite LEDs. They suffer from inefficient domain [various number of PbX6 - layers (n)] control, resulting in a series of unfavorable issues such as unstable color, multipeak profile, and poor fluorescence yield. Here, a strategy involving a delicate spacer modulation for quasi-2D perovskite films via an introduction of aromatic polyamine molecules into the perovskite precursor is reported. With low-dimensional component engineering, the n1 domain, which shows nonradiative recombination and retarded exciton transfer, is significantly suppressed. Also, the n3 domain, which represents the population of emission species, is remarkably increased. The optimized quasi-2D perovskite film presents blue emission from the n3 domain (peak at 465 nm) with a photoluminescence quantum yield (PLQY) as high as 77%. It enables the corresponding perovskite LEDs to deliver stable deep-blue emission (CIE (0.145, 0.05)) with an external quantum efficiency (EQE) of 2.6%. The findings in this work provide further understanding on the structural and emission properties of quasi-2D perovskites, which pave a new route to design deep-blue-emissive perovskite materials.

Association between nut intake and non-alcoholic fatty liver disease risk: a retrospective case-control study in a sample of Chinese Han adults.

OBJECTIVES: Nut consumption has been associated with a lower risk of type 2 diabetes, metabolic syndrome and insulin resistance. However, its effect on the risk of non-alcoholic fatty liver disease (NAFLD) is unknown. Therefore, we investigated the relationship between nut consumption and NAFLD risk. SETTING AND PARTICIPANTS: We conducted a retrospective case-control study including 534 patients diagnosed with NAFLD and 534 controls matched by sex and age (±5 years) from the Affiliated Nanping First Hospital of Fujian Medical University in China. MAIN OUTCOME MEASURES: Information on dietary intake was collected using a semiquantitative food frequency questionnaire and nut consumption was calculated. Nut consumption was categorised using quartiles based on the distribution of daily nut intake of the controls. Binary logistic regression models were used to estimate ORs and the 95% CIs for the association between nut consumption and NAFLD risk. RESULTS: After adjusting for potential confounding variables, nut consumption was not associated with NAFLD risk in the overall sample. When the fully adjusted model was stratified by sex, a significant inverse association was found between high nut consumption and NAFLD only among the men in the highest quartile (OR=0.43; 95% CI 0.26 to 0.71; Ptrend = 0.01). The inverse association of nut consumption with NAFLD risk in men remained significant after controlling for other known or suspected risk factors for NAFLD. CONCLUSIONS: Diets with a higher intake of nuts may be associated with a decreased risk of NAFLD, particularly in men.

Guanidine-modified cyclometalated iridium(III) complexes for mitochondria-targeted imaging and photodynamic therapy.

PDT is a well-established therapeutic modality for many types of cancer. Photoluminescent cyclometalated iridium(III) complexes are one of the most commonly used classes of organometallic compounds with potential beneficial applications in bioimaging and as promising anticancer agents. In the present study, three new cyclometalated iridium(III) complexes (Ir1-Ir3) containing guanidinium ligands were found to exert excellent cytotoxic effects on different types of cancer cells upon light irradiation at 425 nm. Notably, Ir1 conferred almost no dark toxicity (IC50 > 100 µM) to HepG2 cells, but the value decreased by 387-fold to 0.36 µM following 10 min of light irradiation (425 nm). Further mechanistic investigation revealed that complex Ir1 could induce apoptosis via the activation of reactive oxygen species (ROS)-mediated mitochondrial signaling pathways in the presence or absence of light irradiation. In vivo studies demonstrated that Ir1 significantly inhibited tumor growth in HepG2 xenograft-bearing mice under light irradiation at 425 nm. Taken together, these findings indicate that designing PDT-based Ir(III) complexes may hold a great deal of promise for anticancer drug development.

Gushukang exerts osteopreserve effects by regulating vitamin D and calcium metabolism in ovariectomized mice.

Calcium homeostasis plays vital roles in the management of bone health. Traditional herbal formula Gushukang (GSK) was clinically applied to treat primary osteoporosis. This study aimed to explore the osteoprotective effects of GSK and its roles in maintaining calcium homeostasis in ovariectomized (OVX) mice. The OVX mice were orally treated with low (0.38 g/kg), middle (0.76 g/kg) and high (1.52 g/kg) dose of GSK for 8 weeks. GSK treatment dramatically increased serum calcium level and decreased urinary calcium excretion as well as enhanced calcium content in bone of OVX mice. Serum level of 25-hydroxyvitamin D was significantly increased in OVX mice with exposure to GSK. Treatment with GSK improved bone mass and micro-structure of trabecular bone at distal metaphysis of femur and proximal metaphysis of tibia in OVX mice shown by safranin O staining and micro-CT measurement. GSK treatment at all doses up-regulated mRNA expression of calcium-binding protein-28k and vitamin D receptor in kidney of OVX mice, and dose-dependently decreased mRNA expression of claudin-14 and elevated mRNA expression of claudin-16 in duodenum of OVX mice. Taken together, GSK exerted beneficial effects on trabecular bone of OVX mice by improving calcium homeostasis via regulating paracellular calcium absorption in duodenum and transcellular calcium reabsorption in kidney.

Cyclometalated iridium(III)-guanidinium complexes as mitochondria-targeted anticancer agents.

Guanidinium-functionalized molecules are commonly studied for their use as pharmaceutically active compounds and drugs carriers. Herein, four cyclometalated iridium(III) complexes containing guanidinium ligands have been synthesized and characterized as potential anticancer agents. These complexes exhibit moderate antitumor activity in HeLa, MCF-7, HepG2, CNE-2, and A549 human tumor cells. Interestingly, all complexes showed higher cytotoxicity than cisplatin against a cisplatin-resistant cell line A549R, and less cytotoxicity on the nontumorigenic LO2 cells. Intracellular distribution studies suggest that these complexes are selectively localized in the mitochondria. Mechanism studies indicate that these complexes arrested the cell cycle in the G0/G1 phase and can influence mitochondrial integrity, inducing cancer cell death through reactive oxygen species (ROS)-dependent pathways.

2,3,5,4'-Tetrahydroxystilbene-2-O-ß-d-glucoside exerted protective effects on diabetic nephropathy in mice with hyperglycemia induced by streptozotocin.

2,3,5,4'-Tetrahydroxystilbene-2-O-ß-d-glucoside (TSG), an active component from the functional and medicinal herb Polygonum multiflorum Thunb, has the capacity of blocking angiotensin II (ANG II) signaling, a pathway within the renin-angiotensin system (RAS) which plays a critical role in the development of diabetic nephropathy (DN), and blockade of the RAS is currently used for the treatment of DN. Here we investigated the beneficial effect of TSG therapy on renal damage in the streptozotocin (STZ)-induced diabetes model. The STZ-treated C57BL/6J diabetic mice developed progressive albuminuria and renal tubular interstitial fibrosis within 10 weeks, accompanied by increased production of ANG II, fibronection, TGF-ß, CTGF, TNF-α, RANTES and MCP-1 and decreased expression of slit diaphragm proteins in the kidney. The treatment of the diabetic mice with a TSG ameliorated kidney mass increase prevented albuminuria, and reduced tubular interstitial fibrosis. The TSG treatment suppressed the induction of fibronection, CTGF, TGF-ß, and MCP-1 and reversed the decline of slit diaphragm proteins Neph-1, ZO-1, and FAT-1. These were accompanied by blockade of renal renin and ANG II accumulation induced by hyperglycemia. These data demonstrated that the inhibition of the RAS with TSG effectively prevented renal injury in diabetic nephropathy.

[Effect of Weifuchun on inhibiting inflammation of Helicobacter pylori-infected GES-1 cells and NF-kappaB signaling pathway].

OBJECTIVE: To study the effect of Weifuchun on inflammation of Helicobacter pylori (Hp)-infected gastric epithelial cells (GES-1) and its correlation with NF-kappaB signaling pathway. METHODS: Hp standard home-made strain (CagA +, VacA +) NCTCI 1637 infected GES-1 cells were used. Weifuchun was used as intervention. Weifuchun of different concentrations (5,10, and 20 microg/mL) were screened by MTT assay. A blank group and the model group were set up. Then the growth inhibition rate of drugs on gastric epithelial GES-1 cells was detected with MTT assay. Cell cycle was detected using flow cytometry. The supernatant liquid was separated to detect the contents of IL-8 and IL-4 by ELISA.The protein expression level of NF-kappaB was detected by Western blot analysis. RESULTS: MTT assay indicated significantly inhibitory effect of Weifuchun on GES-1 cells [5% inhibiting concentration (IC5)] was 10 microg/ml in the Weifuchun group. After GES-1 and Hp were cultured together,the contents of IL-8 in the supernatant were more obviously higher in the model group than in the blank group (P < 0.05), and then gradually decreased. After treatment with different concentrations of Weifuchun, the levels of IL-8 in the supernatant were less when compared with the model group at 12, 24, 48, and 72 h (P < 0.05). The decrement was the most significant in the high dose Weifuchun group. The IL-4 level in the supernatant was obviously lower in the model group than in the blank group. It obviously increased in the high concentration Weifuchun group (P < 0.05). There was no statistical difference in the IL-4 level between middle, low concentration Weifuchun group and the blank group (P > 0.05). The protein expression of intranuclear P65 increased and that of IkBalpha decreased 60 min after Hp infection. But the protein expression of intranuclear P65 decreased and the protein expression of IkBalpha increased after intervention of Weifuchun. CONCLUSIONS: Weifuchun adjusted H. pylori induced IL-8 and IL-4 production by gastric epithelial cells through blocking NF-kappaB pathways. Its mechanisms might possibly lie in inhibiting p65 from entry into nucleus and the degradation of IkBalpha. Weifuchun was an effective drug for treatment of Hp correlated chronic gastritis.