[The role of adenine nucleotide and its metabolites in regulating the homeostasis of glucose and lipid metabolism].

Glucose and lipid metabolism is the most fundamental metabolic activity of higher organisms. This process is affected by both genetic polymorphisms and environmental factors. Excessive uptake and accumulation of lipids lead to obesity and disorder of glucose metabolic homeostasis characterized by insulin resistance and hyperglycemia, suggesting that the cross-regulation between lipid and glucose metabolism happens precisely at organ, cellular and molecular levels by known mechanisms. Adenine nucleotides and their metabolites have emerged as mediators in the mutual regulation of glucose and lipid metabolism. This review summarizes the roles of purinergic signaling induced by fatty acids in glucose metabolism and the development of type 2 diabetes.

[Clinical application of testicular aspiration biopsy by continuous negative-pressure puncture].

OBJECTIVE: To investigate the characteristics of testicular aspiration biopsy by continuous negative-pressure puncture (CNPP) and sum up the preliminary experience in employing this strategy. METHODS: Totally, 271 patients underwent testicular aspiration biopsy in our hospital from August 2002 to December 2014, 88 by open testicular extraction (group A), 87 with a biopsy gun needle (group B), and 96 with a CNPP device (group C). We analyzed the clinical data about the patients and compared the operation time, intraoperative blood loss, postoperative complications, and the success rate of sperm retrieval among the three groups. RESULTS: The operation time was significantly longer in group A than in B and C (ï¼»37.0 ± 14.1ï¼½ vs ï¼»7.0 ± 2.1ï¼½ and ï¼»6.0 ± 3.1ï¼½ min, P < 0.05), the intraoperative blood loss markedly less in group C than in A and B (ï¼»1.2 ± 0.6ï¼½ vs ï¼»10.2 ± 4.1ï¼½ and ï¼»3.1 ± 1.2ï¼½ ml, P < 0.05), and the rate of postoperative complications remarkably higher in group A than in B and C (8.0% ï¼»7/88ï¼½ vs 4.6% ï¼»4/87ï¼½ and 0 ï¼»0/96ï¼½, P < 0.05), but with no statistically significant difference in the success rate of sperm retrieval between groups A, B and C (95.4% ï¼»21/22ï¼½ vs 97.2% ï¼»35/36ï¼½ vs 95.0% ï¼»38/40ï¼½, P > 0.05). The success rates of single-extraction sperm retrieval sufficient for intracytoplasmic single-sperm injection (ICSI) in groups A, B and C were 89.4% (59/66), 86.3% (44/51) and 82.1 % (46/56), and those of two-extraction sperm retrieval were 97.0% (64/66), 98.0% (50/51) and 98.2% (55/56), respectively, neither with statistically significant difference between the three groups (P > 0.05). CONCLUSIONS: Testicular aspiration biopsy by CNPP can be completed by one person and yield enough testicular tissue for pathological examination or ICSI. With the advantages of convenient operation, less intraoperative blood loss and few postoperative complications, it has a high clinical application value.

A one-dimensional silver(I) coordination polymer based on the 2-[2-(pyridin-4-yl)-1H-benzimidazol-1-ylmethyl]phenol ligand exhibiting photoluminescence.

A one-dimensional Ag(I) coordination complex, catena-poly[[silver(I)-µ-{2-[2-(pyridin-4-yl)-1H-benzimidazol-1-ylmethyl]phenol-κ(2)N(2):N(3)}] perchlorate monohydrate], {[Ag(C19H15N3O)]ClO4·H2O}n, was synthesized by the reaction of 2-[2-(pyridin-4-yl)-1H-benzimidazol-1-ylmethyl]phenol (L) with silver perchlorate. In the complex, the L ligands are arranged alternately and link Ag(I) cations through one benzimidazole N atom and the N atom of the pyridine ring, leading to an extended zigzag chain structure. In addition, the one-dimensional chains are extended into a three-dimensional supramolecular architecture via O-H···O hydrogen-bond interactions and π-π stacking interactions. The complex exhibits photoluminescence in acetonitrile solution, with an emission maximum at 390 nm, and investigation of the thermal stability reveals that the network structure is stable up to 650 K.

1-(2-Carb-oxy-eth-yl)-3-(carboxyl-atometh-yl)-2-ethyl-benzimidazol-1-ium monohydrate.

In the title compound, C14H16N2O4·H2O, three substituent groups are located on the same side of the benzimidazole ring plane. In the crystal, O-H⋯O hydrogen bonds and π-π stacking between parallel imidazole rings [centroid-centroid distance = 3.858 (4) Å] link the mol-ecules into a three-dimensional supra-molecular structure.

2-[2-(3-Methyl-but-oxy)-5-nitro-benz-amido]-acetic acid dimethyl sulfoxide monosolvate.

In the title compound, C(14)H(18)N(2)O(6)·C(2)H(6)OS, the -C(O)NHCH(2)CO(2)H and -O(CH(2))(2)CH(CH(3))(2) substitutents of the aromatic ring are positioned such that the -NH- group is hydrogen-bond donor to the ether O atom of the other substituent. The dimethyl sulfoxide solvent mol-ecule is linked to the carb-oxy-lic acid group by an O-H⋯O hydrogen bond.

Bis(tetra-methyl-ammonium) thio-sulfate tetra-hydrate.

The anion of the title salt, 2C(4)H(12)N(+)·S(2)O(3) (2-)·4H(2)O, possesses approximate C(3v) symmetry. The water mol-ecules themselves engage in hydrogen bonding, forming a ribbon running along the a axis; adjacent chains are linked to the thio-sulfate anions by hydrogen bonds, forming a three-dimensional network. The cavities in the network are occupied by the tetra-methyl-ammonium counter ions.

4-(4-Hydroxybenzoyl)phenol mono-hydrate.

The aromatic rings of the title compound, C(13)H(10)O(3)·H(2)O, are aligned at dihedral angles of 20.6 (1) and 40.8 (1)° with respect to the triangular C(ar-yl)-C(=O)-C(ar-yl) fragment. The hy-droxy groups are each hydrogen-bond donors to separate water mol-ecules, the water mol-ecule itself being hydrogen-bonded to one hy-droxy group and one carbonyl group. The water mol-ecule exists in an unusual four-coordinate environment in the resulting layer structure.

Bis(tetra-methyl-ammonium) oxalate monohydrate.

In the crystal structure of the title hydrated salt, 2C(4)H(12)N(+)·C(2)O(4) (2-)·H(2)O, the two independent cations, the anion and the water mol-ecule all lie on special positions of m site symmetry. In both cations, the mirror plane passes through the nitrogen atom and two methyl groups; in the anion, the mirror plane passes through two carbon and two oxygen atoms. The anions and water mol-ecules inter-act by O-H⋯O hydrogen bonding, forming a chain running along the b axis.

Tris(tetra-ethyl-ammonium) hydrogen bis-[2-(sulfatosulfan-yl)benzoate].

The reaction between tetra-ethyl-ammonium hydroxide and 2,2'-dithio-benzoic acid yields the title compound, 3C(8)H(20)N·H(C(6)H(4)O(5)S(2))(2) (3-), the trianion of which comprises two 2-(sulfato-sulfan-yl)benzoate dianions linked across a center of inversion by an acid H atom. One of the cations is disordered about another center of inversion.

Tetra-n-propyl-ammonium acetate-boric acid (1/1).

In the crystal structure of the ammonium carboxyl-ate-boric acid cocrystal, (C(3)H(7))(4)N(+)·CH(3)CO(2) (-)·H(3)BO(3), the boric acid forms two O-H⋯O hydrogen bonds to the acetate anion. The acetate-boric acid species is hydrogen bonded to another acetate-boric acid species through the third OH unit of the boric acid about a twofold rotation axis.

Tetra-n-propyl-ammonium chloride monohydrate.

The crystal structure of the title salt hydrate, C(12)H(28)N(+)·Cl(-)·H(2)O, consists of non-inter-acting cations and anions. The water mol-ecule forms hydrogen bonds to two chloride ions, about a center of inversion, generating a planar eight-membered {⋯H-O-H⋯Cl}(2) ring.

[Study on beta-amyloid peptide 1-42 induced chemokine RANTES in U251 cell].

OBJECTIVE: To study the molecular mechanisms of beta-amyloid 1-42 (Abeta1.42) induced the inflammatory response in U251 cells. METHODS: U251 cells were treated with different concentration of Abeta1-42 (0.2-4.0 micromol/L) for 24 h, and the cell survival rate was evaluated by MTT. After treated with 2.0 micromol/L Abeta1-42 for 12, 24, 36, 48 hours, the nitric oxide content of U251 cells were detected with nitrate reductase method. The RANTES expression was tested by dual-antibody sandwich ELISA method. The expression of NF-kappaB and STAT1 were detected by the immunocytochemical staining. RESULTS: Abeta1-42 decreased the survival rate of U251 cells in dose-dependent manner. The NO generated in 2 micromol/L Abeta1-42 treated U251 cells reached its peak at 24 h and gradually decreased thereafter. The expression of RANTES increased 4-fold (P < 0.01). The NF-kappaB P65, the STAT1 moved from the cytoplasm to the nucleus and expressed significantly were also observed in the 2 micromol/L Abeta1-42 treated U251 cells. CONCLUSION: Abeta1-42 decreases the survival rate of U251 cells and induce the releasing of NO and RANTES. This indicates that Abeta1-42 induced chemokine RANTES in U251 cell may be close related to the activation of NF-kappa B and STAT1.

Effects of photoperiod on growth, lipid metabolism and oxidative stress of juvenile gibel carp (Carassius auratus).

A 58-day cultivation experiment was carried out to investigate the effects of photoperiods on growth, lipid metabolism and oxidative stress of juvenile gibel carp. Juveniles (5.41 ±â€¯0.01 g) were cultured under seven light photoperiods (0 h of light (L):24 h of darkness (D), 4L:20D (12:00-16:00 light), 8L:16D (10:00-18:00 light), 12L:12D (8:00-20:00 light), 16L:8D (6:00-22:00 light), 20L:4D (4:00-24:00 light) and 24L:0D) in an indoor recirculating aquaculture system. The light intensity was 1.02 µmol·m-2·s-1 (at the tank bottom in a 0.5-m water depth). The fish were fed to satiety three times daily (8:30, 14:30 and 18:30). At the end of the experiment, final body weight, specific growth rate, feed efficiency and feed intake were significantly higher in 16L:8D, 20L:4D and 24L:0D groups than those in other groups (P < 0.05). Long-day photoperiods (16L:8D, 20L:4D and 24L:0D) simultaneously promoted lipogenesis, lipolysis and fatty acid oxidation. The increases in lipid retention efficiency, whole body lipid concentration and liver lipid content (P < 0.05) indicated that lipogenesis exceeded fatty acid oxidation. Liver oxidative stress was induced in juvenile gibel carp by short day lengths. The hepatic total antioxidant capacity, superoxide dismutase, glutathione peroxidase and the contents of metabolite glutathione were the highest in the short-day-length groups (0L:24D, 4L:20D and 8L:16D) (P < 0.05). Based on the growth performance and health status in the long-term cultivation experiment, the optimal photoperiods were 16L:8D, 20L:4D and 24L:0D in juvenile gibel carp.

[In vitro release study, in vivo evaluation of biodistribution and antitumor activity of HPMA copolymer-5-fluorouracil conjugates].

The in vitro release behavior, in vivo biodistribution and antitumor activity of N-(2-hydroxypropyl) methacrylamide (HPMA) copolymer-5-fluorouracil conjugates (P-FU) were studied. The in vitro release behavior was evaluated by determining the amount of 5-fluorouracil (5-FU) released from P-FU in mice plasma at 37 degrees C. The in vivo biodistribution and therapeutic evaluation were investigated with Kunming mice bearing hepatoma 22 (H22). The in vitro half-life (t1/2) of P-FU in mice plasma was 32.4 h. It appeared that the circulation life time of the conjugates were 166 times longer than that of 5-FU. The AUC and t1/2 of P-FU in tumor were 3.3 times and 2.3 times more than those of 5-FU, respectively. Therapeutic evaluation also demonstrated that the treatment with P-FU displayed stronger inhibition of the tumor growth when compared with that of 5-FU (P < 0.05). HPMA copolymer is a potential carrier for 5-FU for effective treatment of cancer.

Cyclotriphosphazene core-based dendrimers for biomedical applications: an update on recent advances.

This review is focused on the recent use of cyclotriphosphazene-based dendrimers in biomedicine. Since its synthesis for the first time in 1834, cyclotriphosphazene has been an important compound of phosphorus chemistry as a scaffold, and a large number of cyclotriphosphazene derivatives have been synthesized and applied in various fields such as biology, catalysis, fluorescence, nanomaterials, etc. Today, one of the most important uses concerns its biomedical applications. In this review, the recent developments (since 2012) of cyclotriphosphazene for major pharmaceutical applications are highlighted and analyzed.

Enhancing alkaline hydrogen evolution reaction activity through Ni-Mn3O4 nanocomposites.

Developing efficient, stable and cost-effective electrocatalysts towards hydrogen production in alkaline environments is vital to improve energy efficiency for water splitting. In this work, we prepared Ni-Mn3O4 nanocomposites on Ni foam which exhibit an excellent hydrogen evolution reaction catalytic activity with a current density (j) of 10 mA cm(-2) at an overpotential (η) of 91 mV and show good stability in an alkaline medium.

[Antitumor activity of mitoxantrone-nanosphere against murine liver tumor H22].

OBJECTIVE: [corrected] To make a comparison between mitoxantrone (DHAQ) and liver targeting drug delivery system mitoxantrone-polybutylcyanoacrylate-nanosphere (DHAQ-PBCA-NS) in respect to their antitumor activity against experimental liver tumor H22 in mice. METHODS: Drugs were given intravenously on the 1st, 5th, 9th day after planting tumor respectively. Weight of tumor in mouse was determined and the results were compared with those of mitoxantrone (DHAQ). RESULTS: There was relationship of dose-effect for both DHAQ and DHAQ-PBCA-NS, and the median effective dose (ED50) of DHAQ and DHAQ-PBCA-NS was 1.04 mg/kg and 0.34 mg/kg respectively. The lethal dose to 50% of the population (LD50) of DHAQ and DHAQ-PBCA-NS i.v. in mice with the same administration schedule was 3.670 mg/kg and 4.225 mg/kg respectively. Therefore, the calculated value of therapeutic index was 3.53 for DHAQ and 12.43 for DHAQ-PBCA-NS. In addition, the antitumor activity of both drugs with different treatment schedules was reported. The results showed: the earlier the mice were treated, the higher the antitumor activity of the two drugs were seen. However, DHAQ-PBCA-NS presented higher activity than DHAQ did, when the same treatment schedule was followed. CONCLUSION: The results demonstrated that the antitumor activity of DHAQ-PBCA-NS is much higher than that of DHAQ, and DHAQ-PBCA-NS is possessed of liver targeting property.

[Function analysis of Sj34.9 gene based on RNAi and microarray].

OBJECTIVE: To analyze the function of Sj34.9 gene, so as to provide the reference for future studies. METHODS: The Sj34.9 gene was knocked down in Schistosoma japonicum by RNA interference (RNAi), and the microarray was used to analyze the genes'expression of S. japonicum after Sj34.9 knocked down. RESULTS: A total of 378 genes expressed differently including 202 up-regulated genes and 176 down-regulated genes. The pathway analysis indicated that the genes expressed differently were mainly related to organelles, metabolism and signal transduction. The gene ontology category analysis showed that most of these genes might be involved in binding, membrane fomulation and cellular process. CONCLUSION: The gene Sj34.9 might play important roles in the process of growth, development, reproduction and metabolism of S. japonicum.

In vivo biodistribution, anti-inflammatory, and hepatoprotective effects of liver targeting dexamethasone acetate loaded nanostructured lipid carrier system.

We aimed to evaluate whether the enhancement of the liver accumulation and anti-inflammatory activity of dexamethasone acetate (DXMA) could be achieved by incorporating it into nanostructured lipid carrier (NLCs). DXMA-NLCs were prepared using a film dispersion-ultrasonication method and characterized in terms of particle size, PDI, zeta potential, differential scanning calorimetry, drug loading capacity, encapsulation efficiency, and in vitro release. The biodistribution and pharmacokinetics of DXMA-NLCs in mice were significantly different from those of the DXMA solution (DXMA-sol). The peak concentration of DXMA-NLCs was obtained half an hour after intravenous administration. More than 55.62% of the total administrated dose was present in the liver. An increase of 2.57 fold in the area under the curve was achieved when compared with that of DXMA-sol. DXMA-NLCs exhibited a significant anti-inflammatory and hepatoprotective effect on carrageenan-induced rats and carbon tetrachloride-induced mice compared with DXMA-sol. However, the effect was not in proportion to the dosage. The intermediate and low dosages presented better effects than DXMA-sol. All results indicate that NLCs, as a novel carrier for DXMA, has potential for the treatment of liver diseases, increasing the cure efficiency and decreasing the side effects on other tissues.

PCR-based site-specific mutagenesis of peptide antibiotics FALL-39 and its biologic activities.

AIM: To construct PGEX-1lambdaT-FALL-39 expression vector and its mutant vector, and study the relationship of function and structure. METHODS: A cDNA encoding mature FALL-39 was cloned from SPCA-1 cell mRNA and the prokaryotic expression vector PGEX-1lambdaT-FALL-39 was constructed. Two kinds of polymerase chain reaction (PCR) for the site-direction mutagenesis were used to construct FALL-39 mutant expression vector, FALL-39-Lys-32 and FALL-39-Lys-24. Minimal effective concentration, minimal inhibitory concentration, and minimal bactericidal concentration were used to assay the antibacterial activities of these peptides. Effects of different solution on the antibacterial activity of FALL-39 and FALL-39-Lys-32 were observed by CFU determination. The hemolytic effects of these peptides were also examined on human red blood cells. RESULTS: Two site-specific mutants FALL-39-Lys-32 and FALL-39-Lys24 were obtained by PCR-induced mutagenesis. In comparison with two-step PCR which required two pairs of primers, one step PCR which required one pair of primers is a simple and efficient method for the PCR based site-specific mutagenesis. Using the prokaryotic expression system, the E coli-based products of recombinant FALL39 and its mutant peptides were also obtained. The antibacterial assay showed that FALL-39-Lys-32 and FALL-39-Lys24 were more potential in the antibacterial activity against E coli ML35p and Pseudomonas aeruginosa ATCC27853 than that of FALL-39, and no increase in hemolysis was observed at the antibacterial concentrations. The antibacterial activity of FALL-39-Lys-32 against E coli was more potent than that of FALL-39 in NaCl-containing LB medium, while its activity was almost the same as FALL-39 in SO4(2-) containing Medium E. CONCLUSION: PCR-based mutagenesis is a useful model system for studying the structure and function relationship of antimicrobial peptides. Keeping a-helical conformation of FALL-39 and increasing net positive charge can increase the antibacterial activity of FALL-39 without increasing hemolysis at the antibacterial concentrations.