Comparison of the clinical outcomes between proximal femoral nail anti-rotation with cement enhancement and hemiarthroplasty among elderly osteoporotic patients with intertrochanteric fracture.

BACKGROUND: The proximal femoral nail anti-rotation (PFNA) with cement enhancement enhances the anchorage ability of internal fixation in elderly with osteoporotic intertrochanteric fracture. However, whether it is superior to hemiarthroplasty is still controversial. The present study aimed to determine which treatment has better clinical outcomes among older patients. METHODS: We retrospectively analyzed 102 elderly patients with osteoporosis who developed intertrochanteric fractures and underwent PFNA combined with cement-enhanced internal fixation (n = 52, CE group), and hemiarthroplasty (n = 50, HA group) from September 2012 to October 2018. All the intertrochanteric fractures were classified according to the AO/OTA classification. Additionally, the operative time, intraoperative blood loss, intraoperative and postoperative blood transfusion rates, postoperative weight-bearing time, hospitalization time, Barthel Index of Activities Daily Living, Harris score of hip function, visual analog (VAS) pain score, and postoperative complications were compared between the two groups. RESULTS: The CE group had significantly shorter operative time, lesser intraoperative blood loss, lower blood transfusion rate, and longer postoperative weight-bearing time than the HA group. The CE group had lower Barthel's Index of Activities of Daily Living, lower Harris' score, and higher VAS scores in the first and third months after surgery than the HA group, but no difference was observed between the two groups from 6 months to 12 months. There was no significant difference in the total post-operative complications between the two groups. CONCLUSION: The use of PFNA combined with a cement-enhanced internal fixation technique led to shorter operative time and lesser intraoperative blood loss and trauma in elderly patients as compared to HA.

Expression of Concern: Conjugation of substituted naphthalimides to polyamines as cytotoxic agents targeting the Akt/mTOR signal pathway.

Expression of Concern for 'Conjugation of substituted naphthalimides to polyamines as cytotoxic agents targeting the Akt/mTOR signal pathway' by Zhi-Yong Tian et al., Org. Biomol. Chem., 2009, 7, 4651-4660, https://doi.org/10.1039/B912685F.

Growth, Physiological, and Photosynthetic Responses of Xanthoceras sorbifolium Bunge Seedlings Under Various Degrees of Salinity.

Xanthoceras sorbifolium Bunge is priced for its medical and energetic values. The species also plays a key role in stabilizing ecologically fragile areas exposed to excess soil salinity. In this study, the effects of salinity on the growth, physiological, and photosynthetic parameters of X. sorbifolium Bunge were investigated. The X. sorbifolium seedlings were subjected to five salt treatments: 0 (control, CK), 70, 140, 210, and 280 mM of sodium chloride (NaCl) solutions. NaCl caused a decrease in plant height, specific leaf area, biomass, and root parameters. Leaf wilting and shedding and changes in root morphology, such as root length, root surface area, and root tips were observed. This study found that X. sorbifolium is tolerant to high salinity. Compared with the CK group, even if the concentration of NaCl was higher than 210 mM, the increase of the relative conductivity was also slow, while intercellular CO2 concentration had a similar trend. Moreover, NaCl stress caused an increase in the malondialdehyde (MDA), soluble proteins, and proline. Among the enzymes in the plant, the catalase (CAT) activity increases first and decreased with the increase in the intensity of NaCl stress, but the salt treatment had no significant effect on superoxide dismutase (SOD) activity. The peroxidase (POD) showed an increasing trend under salt stress. It was found that the photosynthesis of X. sorbifolium was notably impacted by saline stress. NaCl toxicity induced a noticeable influence on leaf net photosynthetic rate (Pn), stomatal conductance (Gs), intercellular CO2 concentration (Ci), transpiration rate (E), and water use efficiency (Wue). As salt concentration increased, the content of chlorophyll decreased. It can be found that a low concentration of NaCl induced the increase of photosynthetic capacity but a high-intensity exposure to stress resulted in the reduction of photosynthetic efficiency and SOD activity, which had a positive correlation. In summary, salt-induced ionic stress primarily controlled root morphology, osmotic adjustment, and enzyme activities of salt-treated X. sorbifolium leaves, whereas the low salt load could, in fact, promote the growth of roots.

Synthesis and biological evaluation of genistein-O-alkylamine derivatives as potential multifunctional anti-Alzheimer agents.

A series of genistein derivatives were synthesized and evaluated as multifunctional anti-Alzheimer agents. The results showed that these derivatives had significant acetylcholinesterase (AChE) inhibitory activity; compound 5a exhibited the strongest inhibition to AChE with an IC50 value (0.034 µM) much lower than that of rivastigmine (6.53 µM). A Lineweaver-Burk plot and molecular modeling study showed that compound 5a targeted both the catalytic active site and the peripheral anionic site of AChE. These compounds also showed potent peroxy scavenging activity and metal-chelating ability. The compounds did not show obvious effect on HepG2 and PC12 cell viability at the concentration of 100 µM. Therefore, these genistein derivatives can be utilized as multifunctional agents for the treatment of AD.

Spectroscopic Study on the Interaction between Naphthalimide-Polyamine Conjugates and Bovine Serum Albumin (BSA).

The effect of a naphthalimide pharmacophore coupled with diverse substituents on the interaction between naphthalimide-polyamine conjugates 1-4 and bovine serum albumin (BSA) was studied by UV absorption, fluorescence and circular dichroism (CD) spectroscopy under physiological conditions (pH = 7.4). The observed spectral quenching of BSA by the compounds indicated that they could bind to BSA. Furthermore, caloric fluorescent tests revealed that the quenching mechanisms of compounds 1-3 were basically static type, but that of compound 4 was closer to a classical type. The Ksv values at room temperature for compound-BSA complexes-1-BSA, 2-BSA, 3-BSA and 4-BSA were 1.438 × 104, 3.190 × 104, 5.700 × 104 and 4.745 × 105, respectively, compared with the value of MINS, 2.863 × 104 at Ex = 280 nm. The obtained quenching constant, binding constant and thermodynamic parameter suggested that the binding between compounds 1-4 with BSA protein, significantly affected by the substituted groups on the naphthalene backbone, was formed by hydrogen bonds, and other principle forces mainly consisting of charged and hydrophobic interactions. Based on results from the analysis of synchronous three-dimensional fluorescence and CD spectra, we can conclude that the interaction between compounds 1-4 and BSA protein has little impact on the BSA conformation. Calculated results obtained from in silico molecular simulation showed that compound 1 did not prefer either enzymatic drug sites I or II over the other. However, DSII in BSA was more beneficial than DSI for the binding between compounds 2-4 and BSA protein. The binding between compounds 1-3 and BSA was hydrophobic in nature, compared with the electrostatic interaction between compound 4 and BSA.

Study on the synthesis, biological activity and spectroscopy of naphthalimide-diamine conjugates.

Eleven novel naphthalimide-diamine conjugates were synthesized and their structures were confirmed by elemental analysis, 1H-NMR, 13C-NMR and MS. Their in vitro antitumor activities were assessed using MTT assays on two cancerous cell lines K562, HCT116, and one normal hepatoma cell line QSG 7701. Compound 7f exhibited potent antitumor activity on HCT116 cells and favorable cell selectivity toward QSG 7701 compared with the positive control, amonafide. Moreover, 7f could block HeG2 cells in the G2/M phase and induce HeG2 cells apoptosis. The interaction of compound 7f with herring sperm DNA was studied by UV/vis absorption and fluorescence spectroscopy under physiological conditions (pH = 7.4). The observed spectral quenching of compound 7f by DNA and the displacement of EB from DNA-EB complex by compound 7f indicated that compound 7f could intercalate into DNA base pairs, which was also corroborated by the effect of KI on compound-DNA interaction. Further caloric fluorescent tests revealed that the quenching mechanism was a static type. Meanwhile, the binding constants, thermodynamic parameters and the effect of NaCl on compound-DNA interaction showed that the type of interaction force was mainly hydrogen bonds and the binding process was driven by hydrogen and van der Waals bonding.

Antitumor effects and preliminary systemic toxicity of ANISpm in vivo and in vitro.

Polyamines as a vector to ferry toxic agents have attracted attention, and naphthalimide-polyamine conjugates show potent activity and tumor cell selectivity. The present study was carried out to evaluate the antitumor effects and preliminary systemic toxicity of ANISpm, a novel 3-amino-naphthalimide-spermine conjugate. The polyamine transport system recognition of ANISpm, supported by α-difluoromethylornithine (DFMO)/spermidine (Spd) experiments, is in accordance with its potent cell selectivity between human hepatoma HepG2 cells and normal QSG7701 hepatocyte. The antiproliferative effect is because of ANISpm-induced cell apoptosis, a common characteristic of both naphthalimide and polyamine analogs. Various apoptotic assessment assays have shown that ANISpm can induce apoptosis through the PI3K/Akt signal pathway. The apoptotic signaling cascade involves Akt inactivation, which results in a series of cellular events. The downstream pathway includes Bad dephosphorylation, dissociation of 14-3-3 and Bad, and binding to Bcl-xL, which triggers the disruption of the mitochondrial membrane, release of cytochrome c, and caspases' cascade activation. Furthermore, the Akt/mTOR signal pathway is also involved in ANISpm-mediated cell-cycle arrest. Additive DFMO or Spd, which only enhances or attenuates ANISpm-mediated cell apoptosis, respectively, does not alter the signal pathway. In addition, preliminary toxicology evaluation showed that ANISpm had no obvious system toxicity at a dose of 2.5 mg/kg, which exerted potent antitumor activity in vivo, especially hematotoxicity. Thus, ANISpm merits further investigation as a potential chemotherapeutic agent against hepatocellular carcinoma.

Conjugation of substituted naphthalimides to polyamines as cytotoxic agents targeting the Akt/mTOR signal pathway.

Though several naphthalimide derivatives have exhibited antitumor activity in clinical trials, some issues such as toxicity prompted further structural modifications on the naphthalimide backbone. A series of naphthalimides conjugated with polyamines were synthesized to harness the polyamine transporter (PAT) for drug delivery, which was beneficial for the tumor cell selectivity. Bioevaluation in human hepatoma HepG2 cells treated with alpha-difluoromethylornithine (DFMO) or spermidine (Spd), human hepatoma Bel-7402 and normal QSG-7701 hepatocyte confirmed the PAT recognition and cell selectivity. In addition, the novel naphthalimide polyamine conjugate kills cells via apoptosis, and the Akt/mTOR signal pathway was first identified as the upstream cellular target through the apoptotic mechanism research. The presence of DFMO or Spd only either elevated or attenuated the cell apoptosis, but did not change the signal pathway. Collectively, the proper polyamine recognition element (i.e., homospermidine) mediated effective drug delivery via the PAT, and helped the proper cytotoxic goods (i.e., diverse naphthalimides) exert antitumor properties.

[Synthesis and in vitro cytotoxicity of naphthalimide polyamine conjugates as antitumor agents].

Six naphthalimide polyamine conjugates were synthesized and their structures were confirmed by elemental analysis, 1H NMR, 13C NMR and MS. Antitumor activities were evaluated in vitro using MTT assay on Leukemia cells (K562), human breast cancer cells (MB-231) and prostate cancer cells (Ln cap cell). The results showed that most of the six compounds were superior to the control (amonafide), 6d, 6e, and 6f exhibited nice selectivity in a screen of hepatoma cells (BEL-7402) and human normal hepatocytes (QSG-7701).

[Research on CANON process for municipal sewage in room temperature].

In the room temperature 14.7-24.7 degrees C, simultaneous nitrification-ANAMMOX (CANON) process for municipal sewage was tested by SBR while the DO was controlled between 0.05 and 0.30 mg/L. As a result, the research shows that CANON process can be applied to the nitrogen treatment of municipal wastewater in room temperature by SBR. DO can be regarded as the indication parameter of reaction terminal, and 1 mg/L has been confirmed in the experiment. In the exploring SBR experiments, the consumption velocity of NH4(+) -N was 0.164-0.218 kg/(m3 x d), the production velocity of NO3(-) -N was 0.026-0.036 kg/(m3 x d), the removal velocity and efficiency of TN were 0.124-0.194 kg/(m3 x d) and 65%-75% respectively. Additionally, in the improving SBR experiments, there were three methods for avoiding nitrite accumulation and increasing the nitrogen removal efficiency. They were improving temperature, adding non-aeration period of time and increasing the quantity of ANAMMOX bacteria. Therefore, the removal efficiency of TN was increased to 77%-88% through the three ways above. However, in view of the nitrogen removal velocity and the fact of engineering application condition, the third approach was the best to advance the general ability of ANAMMOX.

[Relations of the substrate concentration to the COD and pH in the ANAMMOX process].

Analyzed the change rules of the concentration of nitrogen compounds, COD and pH in the upflow ANAMMOX biofilter, and the distribution rules of the ANAMMOX activity and biomass. And furthermore, the relations of the nitrogen compounds concentration to the COD and pH in the ANAMMOX process were studied with the statistical method. The results showed that the dissolved oxygen and nitrogen load together caused the uneven distribution of the ANAMMOX activity and biomass along the filter layer in a "ridge" shape; the existence of heterotrophic denitrification and the consumption of H+ made the COD decrease and the pH increase in the ANAMMOX process; the concentration of the organic matters below 100 mg/L has little influence on ANAMMOX bacteria, and the relations of the substrate NH4(+) -N concentration to the COD and pH showed a good linear correlation. The slopes of the fitting line of the COD-NH4(+) -N and pH-NH4(+) -N were 1.113 8 +/- 0.052 2 and - 0.111 3 +/- 0.001 2 respectively, with the confidence level being 95% and the average correlation coefficient R2 0.982 3 and 0.9850 respectively.

Synthesis, cytotoxicity and apoptosis of naphthalimide polyamine conjugates as antitumor agents.

Several naphthalimide polyamine conjugates were synthesized and evaluated for in vitro cytotoxicity against human leukemia K562, murine melanoma B16, Chinese hamster ovary CHO cell lines. Both triamine moieties and the length of spacers were crucial in elevating the potency of 1,8-naphthalimide. The typical compounds 5a and 5d exhibited excellent cell selectivity to cancer cells through the human hepatoma BEL-7402 and human normal hepatocyte QSG-7701 screens. In addition, 5d could disturb the cell cycle in B16 cells. The research on caspase activity and cytochrome c indicated that 5d could induce B16 cell apoptosis via both the mitochondrial and membrane death receptor pathways, and the Bcl-2 family numbers were involved in the control of apoptosis.

[Partial nitrification in SBR under normal temperature and limited oxygen condition].

Partial nitrification was researched in a SBR reactor under the limited oxygen condition (DO 0.3-0.4 mg/L) and the normal temperature of 14.1-24.2 degrees C to produce the correct influent for ANAMMOX process from secondary wastewater (NH4+ -N 30-100 mg/L). The influent for the ANAMMOX process must be composed of NH4+ and NO2- in a ratio of 1/1.31 and therefore only a partial nitrification of ammonium into nitrite was required. The control of alkalinity and the indication of monitoring profile of DO allowed to achieve this partial nitrification with a final effluent only composed of NH4+ -N and NO2(-) -N at the right stoichiometric ratio. The equal consumption of HCO3- /NH4+ in secondary wastewater resulted in a natural pH decrease when approximately 57% of NH4+ -N was oxidized. When the pH dropped to a certain level, the lowering of the metabolic rate of the ammonium oxidizer would lead to rapid decline of the oxygen uptake rate (OUR) in reactor, and the jump characteristic point (it was distinguished by the jump over 1.0 mg/L of DO value) in the DO profile would emerge, which signalled the end-point of the partial nitrifying. The optimum alkalinity of partial nitrification was studied under 4 concentrations in the range of NH4+ -N 30-100 mg/L of secondary wastewater. The result indicated that the bicarbonate/ammonium ratio was the key factor influencing the nitrification ratio (NO2-/NH4+), and it was absolutely possible to successfully achieve partial nitrification that provided right substrate for ANAMMOX reactor through the control of the alkalinity.

Synthesis and bioevaluation of 5-fluorouracil derivatives.

A series of six novel 5-fluorouracil derivatives 1-6 were synthesized and their structures confirmed by (1)H- and (13)C-NMR, MS and elemental analysis. The preliminary in vitro antitumor activities against B16, K562 and CHO cells and the in vivo inhibitions of liver cancer H(22) demonstrated that some of these compounds effectively inhibit the growth of tumor cells, but the in vivo trials in mice revealed that the compounds also exhibited serious liver and lung tissue toxicity. The hydrolysis experiments indicated that this type of compound did not readily liberate 5-fluorouracil, as expected.