Preparation of MoFs-Derived Cobalt Oxide/Carbon Nanotubes Composites for High-Performance Asymmetric Supercapacitor.

Metal-organic frameworks (MOFs)-derived metallic oxide compounds exhibit a tunable structure and intriguing activity and have received intensive investigation in recent years. Herein, this work reports metal-organic frameworks (MOFs)-derived cobalt oxide/carbon nanotubes (MWCNTx@Co3O4) composites by calcining the MWCNTx@ZIF-67 precursor in one step. The morphology and structure of the composite were investigated by scanning electron microscope (SEM) and transmission electron microscope (TEM) characterization. The compositions and valence states of the compounds were characterized by X-ray diffraction (XRD) and X-ray photoelectron spectroscopy (XPS). Benefiting from the structurally stable MOFs-derived porous cobalt oxide frameworks and the homogeneous conductive carbon nanotubes, the synthesized MWCNTx@Co3O4 composites display a maximum specific capacitance of 206.89 F·g-1 at 1.0 A·g-1. In addition, the specific capacitance of the MWCNT3@Co3O4//activated carbon (AC) asymmetric capacitor reaches 50 F·g-1, and has an excellent electrochemical performance. These results suggest that the MWCNTx@Co3O4 composites can be a potential candidate for electrochemical energy storage devices.

Comprehensive identification and characterization of the HERV-K (HML-9) group in the human genome.

BACKGROUND: Human endogenous retroviruses (HERVs) result from ancestral infections caused by exogenous retroviruses that became incorporated into the germline DNA and evolutionarily fixed in the human genome. HERVs can be transmitted vertically in a Mendelian fashion and be stably maintained in the human genome, of which they are estimated to comprise approximately 8%. HERV-K (HML1-10) transcription has been confirmed to be associated with a variety of diseases, such as breast cancer, lung cancer, prostate cancer, melanoma, rheumatoid arthritis, and amyotrophic lateral sclerosis. However, the poor characterization of HML-9 prevents a detailed understanding of the regulation of the expression of this family in humans and its impact on the host genome. In light of this, a precise and updated HERV-K HML-9 genomic map is urgently needed to better evaluate the role of these elements in human health. RESULTS: We report a comprehensive analysis of the presence and distribution of HERV-K HML-9 elements within the human genome, with a detailed characterization of the structural and phylogenetic properties of the group. A total of 23 proviruses and 47 solo LTR elements were characterized, with a detailed description of the provirus structure, integration time, potential regulated genes, transcription factor binding sites (TFBS), and primer binding site (PBS) features. The integration time results showed that the HML-9 elements found in the human genome integrated into the primate lineage between 17.5 and 48.5 million years ago (mya). CONCLUSION: The results provide a clear characterization of HML-9 and a comprehensive background for subsequent functional studies.

Spectroscopic Methodology and Molecular Docking Studies on Changes in Binding Interaction of Felodipine with Bovine Serum Albumin Induced by Cocrystallization with ß-Resorcylic Acid.

In the present study, a novel cocrystal of felodipine (FEL) and ß-resorcylic acid (ßRA) was developed. We specially focused on the change of binding pattern with bovine serum albumin (BSA) induced by cocrystallization of FEL with ßRA. The solid characterizations and density functional theory (DFT) simulation verified that FEL-ßRA cocrystal formed in equimolar ratio (1 : 1 M ratio) through C=O…H-O hydrogen bond between C=O group in FEL and O-H group in ßRA. The binding interactions between FEL-ßRA system and BSA were studied using fluorescence spectral and molecular docking methods. Two guest molecule systems, including a physical mixture of FEL and ßRA and FEL-ßRA cocrystal were performed binding to BSA in molecular docking. According to the Kb and binding energy, the supramolecular form of FEL-ßRA system was retained during binding to BSA. Molecular docking simulation suggested that FEL and its cocrystal inserted into the subdomain IIIA (site II') of BSA. The interactions between FEL and BSA including hydrogen bonding with ASN390 residue and intermolecular hydrophobic interactions with LEU429 and LEU452 residues. However, the size of supramolecular FEL-ßRA better matched that of active cavity of BSA; the cocrystal is closely bound to BSA through hydrogen bonding with ASN390 residue and intermolecular hydrophobic interactions with LEU429, VAL432, LEU452 and ILE387 residues. This change on binding affinity of FEL to BSA induced by cocrystallization with ßRA provided theoretical basis to evaluate the transportation, distribution and metabolism of cocrystal drug.

Characterizations and Assays of α-Glucosidase Inhibition Activity on Gallic Acid Cocrystals: Can the Cocrystals be Defined as a New Chemical Entity During Binding with the α-Glucosidase?

Cocrystallization with co-former (CCF) has proved to be a powerful approach to improve the solubility and even bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). However, it is still uncertain whether a cocrystal would exert the pharmacological activity in the form of a new chemical entity, an API-CCF supramolecule. In the present study, gallic acid (GA)-glutaric acid and GA-succinimide cocrystals were screened. The solubility, dissolution rate and oral bioavailability of the two cocrystals were evaluated. As expected, AUCs of GA-glutaric acid and GA-succinimide cocrystals were 1.86-fold and 2.60-fold higher than that of single GA, respectively. Moreover, experimental evaluations on α-glucosidase inhibition activity in vitro and theoretical simulations were used to detect whether the two cocrystals would be recognized as a new chemical entity during binding with α-glucosidase, a target protein in hypoglycemic mechanisms. The enzyme activity evaluation results showed that both GA and glutaric acid displayed α-glucosidase inhibition activity, and GA-glutaric acid cocrystals showed strengthened α-glucosidase inhibition activity at a moderate concentration, which is attributed to synergism of the two components. Molecular docking displayed that the GA-glutaric acid complex deeply entered the active cavity of the α-glucosidase in the form of a supramolecule, which made the guest-enzyme binding configuration more stable. For the GA and succinimide system, succinimide showed no enzyme inhibition activity, however, the GA-succinimide complex presented slightly higher α-glucosidase inhibition activity than that of GA. Molecular docking simulation indicated that the guest molecules entering the active cavity of the α-glucosidase were free GA and succinimide, not the GA-succinimide supramolecule.

Metal ion-assisted drug-loading model for novel delivery system of cisplatin solid lipid nanoparticles with improving loading efficiency and sustained release.

Metal ion-assisted drug loading model, in which metal ion was used to modify the microstructure of lipid layer, has been developed to improve drug loading efficiency of solid lipid nanoparticles (SLNs). The microstructure and properties of metal ion-assisted cisplatin-loading SLNs were investigated by infra-red spectroscopy, fluorescence spectroscopy and zetasizer. The reactions of hydrogenated soybean lecithin with Zn(2+), Cu(2+), Mn(2+ )and Mg(2+ )have been detected; the mechanism for higher drug encapsulation efficiency (EE) has been investigated. In metal ion introduction SLNs, the compact degree of the lipid molecules was increased due to the electrostatic interaction between metal ions and phospholipid acyl and choline polarity groups, which result in increasing of drug EE. Meanwhile, these electrostatic interactions slowed the releasing rate of encapsulated drug. The study of cytotoxic activity in vitro indicated that the cell cytotoxicity of metal ions introduction SLNs depended on both cell uptake of SLNs and drug releasing from SLNs.

Preparation, characterization, and evaluation of dipfluzine-benzoic acid co-crystals with improved physicochemical properties.

PURPOSE: To prepare and characterize the co-crystal of dipfluzine and benzoic acid. To investigate the feasibility of the co-crystal for improving solubility and a faster dissolution rate in vitro and evaluate the bioavailability and tissue distribution of co-crystal in vivo. METHODS: A novel dipfluzine-benzoic acid co-crystal prepared using the solvent-assisted co-grinding and the solvent ultrasonic methods were identified and characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA), as well as Raman, solid-state nuclear magnetic resonance (ssNMR), and terahertz (THz) spectroscopy. Pharmacokinetics and tissue distribution were tested in vivo using murine models. Statistics analysis for dissolution data of co-crystal in vitro and animal experiment data in vivo were evaluated using t-test. RESULTS: Results of PXRD and DSC identified the dipfluzine-benzoic acid co-crystals were formed with a molar ratio of 1:2. The IR, Raman, and ssNMR spectra verified the formation of O-H · · · O and O-H · · · F hydrogen bonds. The complex constant, K, was evaluated to be 10(9) orders of magnitude with Δ r G < 0. The co-crystal solubility, the rate of drug dissolution and the relative bioavailability were approximately 500 times, five times and double that of dipfluzine, respectively. Increased solubility of co-crystal did not reduce distribution in the brain; the mean concentrations in the brain increased, but the differences had no statistic significance (p > 0.05). CONCLUSIONS: The co-crystal of dipfluzine-benzoic acid improved the physicochemical properties of dipfluzine, such as solubility and dissolution rate. Furthermore, the increased relative bioavailability of co-crystal indicated the potential use in further clinical study.

Decolorization of methyl orange by green rusts with hydrogen peroxide at neutral pH.

Heterogeneous Fenton-like processes using green rusts (GRs) with hydrogen peroxide (H2O2) were studied to decolorize methyl orange (MO) in aqueous solution at an initial pH of 7.0. In this study, two types of crystal structure for GRs, the hydroxycarbonate GR(CO3(2-)) (GR1) and the hydroxysulphate GR(SO4(2-)) (GR2), were synthesized by partial oxidation of Fe(OH)2 suspension under light irradiation and distinguished by X-ray diffraction (XRD) due to different characteristic peaks. In oxidation reactions, decolorization rate of MO, bubbling air through the solution, was about 65% (experiment B), whereas, it was up to 95% in the presence of H2O2 (experiment C) within 60 min. The comparative tests of GR1 and GR2 show that the reduction capability of GR2 is stronger than GR1, which may be due to Fe(II) content and interlayer anions. XRD analysis and Fourier transform infrared spectroscopy revealed that the oxidation end products of GR2 were mainly a poorly crystallized mixture of magnetite (Fe3O4) and hydroxy ferric oxide (FeOOH). However, when GR was immediately oxidized, the weakly crystallized goethite (α-FeOOH) and lepidocrocite (γ-FeOOH) were formed for O2 and H2O2, respectively. Based on the intermediates obtained, a probable decolorization mechanism has been proposed.

Comprehensive Identification and Characterization of HML-9 Group in Chimpanzee Genome.

Endogenous retroviruses (ERVs) are related to long terminal repeat (LTR) retrotransposons, comprising gene sequences of exogenous retroviruses integrated into the host genome and inherited according to Mendelian law. They are considered to have contributed greatly to the evolution of host genome structure and function. We previously characterized HERV-K HML-9 in the human genome. However, the biological function of this type of element in the genome of the chimpanzee, which is the closest living relative of humans, largely remains elusive. Therefore, the current study aims to characterize HML-9 in the chimpanzee genome and to compare the results with those in the human genome. Firstly, we report the distribution and genetic structural characterization of the 26 proviral elements and 38 solo LTR elements of HML-9 in the chimpanzee genome. The results showed that the distribution of these elements displayed a non-random integration pattern, and only six elements maintained a relatively complete structure. Then, we analyze their phylogeny and reveal that the identified elements all cluster together with HML-9 references and with those identified in the human genome. The HML-9 integration time was estimated based on the 2-LTR approach, and the results showed that HML-9 elements were integrated into the chimpanzee genome between 14 and 36 million years ago and into the human genome between 18 and 49 mya. In addition, conserved motifs, cis-regulatory regions, and enriched PBS sequence features in the chimpanzee genome were predicted based on bioinformatics. The results show that pathways significantly enriched for ERV LTR-regulated genes found in the chimpanzee genome are closely associated with disease development, including neurological and neurodevelopmental psychiatric disorders. In summary, the identification, characterization, and genomics of HML-9 presented here not only contribute to our understanding of the role of ERVs in primate evolution but also to our understanding of their biofunctional significance.

Comprehensive characterization of ERV-K (HML-8) in the chimpanzee genome revealed less genomic activity than humans.

Endogenous retroviruses (ERVs) originate from ancestral germline infections caused by exogenous retroviruses. Throughout evolution, they have become fixed within the genome of the animals into which they were integrated. As ERV elements coevolve with the host, they are normally epigenetically silenced and can become upregulated in a series of physiological and pathological processes. Generally, a detailed ERV profile in the host genome is critical for understanding the evolutionary history and functional performance of the host genome. We previously characterized and cataloged all the ERV-K subtype HML-8 loci in the human genome; however, this has not been done for the chimpanzee, the nearest living relative of humans. In this study, we aimed to catalog and characterize the integration of HML-8 in the chimpanzee genome and compare it with the integration of HML-8 in the human genome. We analyzed the integration of HML-8 and found that HML-8 pervasively invaded the chimpanzee genome. A total of 76 proviral elements were characterized on 23/24 chromosomes, including detailed elements distribution, structure, phylogeny, integration time, and their potential to regulate adjacent genes. The incomplete structure of HML-8 proviral LTRs will undoubtedly affect their activity. Moreover, the results indicated that HML-8 integration occurred before the divergence between humans and chimpanzees. Furthermore, chimpanzees include more HML-8 proviral elements (76 vs. 40) and fewer solo long terminal repeats (LTR) (0 vs. 5) than humans. These results suggested that chimpanzee genome activity is less than the human genome and that humans may have a better ability to shape and screen integrated proviral elements. Our work is informative in both an evolutionary and a functional context for ERVs.

Cocrystallization of 5-fluorouracil with gallic acid: A novel 5-fluorouracil cocrystal displaying synergistic anti-tumor activity both in oral and intraperitoneal injection administration.

Gallic acid (GA) is a naturally occurring polyphenolic compound exhibiting anti-tumor activity. To clarify the capability of GA in optimizing the in vitro/in vivo properties of the first line anti-tumor drug 5-fluorouracil (5-FU) and achieve synergistically enhanced anti-tumor activity, a novel cocrystal hydrate of 5-FU-GA-H2O was successfully screened and characterized based on various spectroscopic and experimental analysis including Fourier transform infrared spectroscopy (FT-IR), Raman spectra (Raman), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric (TG) and scanning electric microscope (SEM) techniques. The results suggested the existence of hydrogen bonding interactions between C=O group of 5-FU and O-H group of GA. Although the dissolution rate and solubility of 5-FU-GA-H2O cocrystal were slowed and lowered compared with that of 5-FU, respectively, the membrane permeability was enhanced for cocrystal compared with that of intact 5-FU and physical mixture (PM) of 5-FU and GA. For the cocrystal, the cumulative amount per unit area of permeated 5-FU in the first 10 h was 2.56 and 9.97 times of that of pure 5-FU and PM, respectively, in the case that transmembrane behavior of 5-FU depended on the type of solution from which the powder was dissolved. Meanwhile, improvement on oral bioavailability by co-crystallization was observed; AUC0-t of cocrystal was 2.78-fold higher than that of 5-FU. Furthermore, the cocrystal displayed a superior cytotoxic activity on 4T1 mouse breast cancer cells compared with pure 5-FU and even the PM. It was confirmed that the cocrystal solution induced higher autophagic flux than those of 5-FU and PM in 4T1 cell, suggesting that autophagy rather than apoptosis mainly mediated cell death. The obvious difference of tumor inhibition activity between PM and cocrystal in intraperitoneal injection administration indicated that some of the interactions formed in the solid cocrystal could retain in solution in some way. Benefiting from synergistic cytotoxicity, drug efficacy in vivo was enhanced through injection administration of solution from which cocrystal was dissolved.

Co-amorphous formulation of dipyridamole with p-hydroxybenzoic acid: Underlying molecular mechanisms, physical stability, dissolution behavior and pharmacokinetic study.

Coamorphization has been proven to be an effective approach to improve bioavailability of poorly soluble active pharmaceutical ingredients (APIs) by virtue of solubilization, and also contributes to overcome limitation of physical stability associated with amorphous drug alone. In current work, a co-amorphous formulation of dipyridamole (DPM), a poor solubility drug, with p-hydroxybenzoic acid (HBA) was prepared and investigated. At a molar ratio of 1:2, DPM and HBA were melted result in the formation of a binary co-amorphous system. The DPM-HBA co-amorphous was structurally characterized by powder X-ray diffraction (PXRD), temperature modulated differential scanning calorimetry (mDSC), high performance liquid chromatography (HPLC) and solution state 1H nuclear magnetic resonance (1H NMR). The molecular mechanisms in the co-amorphous were further analysed via Fourier-transform infrared (FTIR) and Raman spectroscopies, as well as density functional theory (DFT) calculation. All the results consistently revealed the presence of hydrogen bonding interactions between -OH of DPM and -COOH on HBA. Accelerated test and glass transition kinetics showed excellent physical stability of DPM-HBA co-amorphous compared with amorphous DPM along with glass transition temperatures (Tg). The phase-solubility study indicated that complexation occurred between DPM and HBA in solution, which contributed to the solubility and dissolution enhancement of DPM in co-amorphous system. Pharmacokinetic study of co-amorphous DPM-HBA in mouse plasma revealed that the DPM exhibited 1.78-fold and 2.64-fold improvement in AUC0­∞ value compared with crystalline and amorphous DPM, respectively. This current study revealed coamorphization is an effective approach for DPM to improve the solubility and biopharmaceutical performance.

Identification of differentially expressed HERV-K(HML-2) loci in colorectal cancer.

Colorectal cancer is one of the malignant tumors with the highest mortality rate in the world. Survival rates vary significantly among patients at various stages of the disease. A biomarker capable of early diagnosis is required to facilitate the early detection and treatment of colorectal cancer. Human endogenous retroviruses (HERVs) are abnormally expressed in various diseases, including cancer, and have been involved in cancer development. Real-time quantitative PCR was used to detect the transcript levels of HERV-K(HML-2) gag, pol, and env in colorectal cancer to systematically investigate the connection between HERV-K(HML-2) and colorectal cancer. The results showed that HERV-K(HML-2) transcript expression was significantly higher than healthy controls and was consistent at the population and cell levels. We also used next-generation sequencing to identify and characterize HERV-K(HML-2) loci that were differentially expressed between colorectal cancer patients and healthy individuals. The analysis revealed that these loci were concentrated in immune response signaling pathways, implying that HERV-K impacts the tumor-associated immune response. Our results indicated that HERV-K might serve as a screening tumor marker and a target for tumor immunotherapy in colorectal cancer.

Use of the co-grinding method to enhance the dissolution behavior of a poorly water-soluble drug: generation of solvent-free drug-polymer solid dispersions.

The solid dispersion (SD) technique is the most effective method for improving the dissolution rate of poorly water-soluble drugs. In the present work, SDs of the Ca2+ channel blocker dipfluzine (DF) with polyvinylpyrrolidone K30 (PVP) and poloxamer 188 (PLXM) were prepared by the powder solid co-grinding method under a solvent-free condition. The properties of all SDs and physical mixtures were investigated by X-ray diffraction, Fourier-transform infrared, differential scanning calorimetry, scanning electron microscopy, dissolution test, and particles size determination. Eutectic compounds were produced between the DF and PLXM matrix during the co-grinding process, whereas glass suspension formed in the SDs with PVP carrier. Hydrogen bond formation was not observed between DF and carriers and DF was microcrystalline state in the PVP and PLXM matrices. The solubility of DF in different concentration of carriers at 25, 31, and 37°C was investigated; the values obtained were used to calculate the thermodynamic parameters of interaction between DF and carriers. The Gibbs free energy (ΔrGθ) values were negative, indicating the spontaneous nature of dispersing DF into the carriers. Moreover, entropy is the drive force when DF disperses into the matrix of PVP, while, enthalpy-driven dispersing encounters in the PLXM carrier. All the SDs of DF/carriers showed a considerably higher dissolution rate than pure DF and the corresponding physical mixtures. The cumulative dissolution rate at 10 min of the SD with a 1 : 3 DF/carrier ratio increased 5.1-fold for PVP and 5.5-fold for PLXM.

Solid state characterizations and analysis of stability in azelnidipine polymorphs.

Azelnidipine, a new dihydropyridine calcium ion antagonist, was protected by patent in Japan. In present study, identifications of the crystal phases, including two polymorphic and a pseudopolymorphic crystal forms of azelnidipine, were attempted using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), IR-, Raman-, THz-, and ss-NMR-spectroscopy. PXRD identified three different crystal forms, while, spectroscopy analysis provided the information of crystal structure involving intermolecular interactions. The transition thermodynamics of the azelnidipine polymorphs were extensively investigated by solubility method. The solubility of the two polymorphs of α and ß in 50% ethanol at 25, 31, 37, 42, and 49°C was investigated; the values obtained were used to calculate the thermodynamic parameters of the transition reaction. The temperature of polymorphic phase transition in 50% ethanol was 50.78°C, and the values of ΔG(α,ß)(θ), ΔH(α,ß)(θ), and ΔS(α,ß)(θ) at 25°C were -1.18 kJ·mol(-1), -14.81 kJ·mol(-1), and -45.73 J·mol(-1)·K(-1), respectively. Form ß was proved to be thermodynamic stable form at room temperature and enantiotropically related with form α. The kinetics of the solid-state decomposition, studied using DSC analysis, showed that the activation energies of decomposition of the polymorphs α and ß at high temperatures were 148.67 and 151.93 kJ·mol(-1).

Effects of loading procedures of magnetic nanoparticles on the structure and physicochemical properties of cisplatin magnetic liposomes.

The effects of different loading procedures of magnetic nanoparticles (MNs) on the structure and physicochemical properties of cisplatin magnetic liposomes were investigated by X-ray diffraction, infrared spectroscopy, transmission electron microscopy, and fluorescence spectroscopy. 1, 2-Dipalmitoyl-sn-glycero-3-Phosphocholine based cisplatin magnetic liposomes were prepared using two different procedures. In procedure I, MNs were combined with phospholipids during film formation; MNs were embedded in a phospholipid bilayer. In procedure II, MNs were mixed with drugs during hydration and MNs were contained in an interior aqueous compartment. The encapsulation efficiency of cisplain and the content of MN in procedure I liposomes were 33.5% ± 3.3% and 2.34 ± 0.09 mg mL(-1), respectively. It indicated that the deliberate MN loading into the liposome structure was not only successful using procedure I, but also superior over procedure II both in cisplatin encapsulation efficiency and MN content, which can promote the magnetic targeting effect of magnetic liposomes during delivering cisplatin.

High Expression of HERV-K (HML-2) Might Stimulate Interferon in COVID-19 Patients.

Background. Interferon is a marker of host antiviral immunity, which is disordered in COVID-19 patients. ERV can affect the secretion of interferon through the cGAS-STING pathway. In this study, we explored whether IFN-I and HERV-K (HML-2) were activated in COVID-19 patients and whether there was an interaction between them. Methods. We collected blood samples from COVID-19 patients and healthy controls. We first detected the expression of HERV-K (HML-2) gag, env, and pol genes and IFN-I-related genes between patients and healthy people by qPCR, synchronously detected VERO cells infected with SARS-CoV-2. Then, the chromosome distributions of highly expressed HERV-K (HML-2) gag, env, and pol genes were mapped by the next-generation sequencing results, and GO analysis was performed on the related genes. Results. We found that the HERV-K (HML-2) gag, env, and pol genes were highly expressed in COVID-19 patients and VERO cells infected with SARS-CoV-2. The interferon-related genes IFNB1, ISG15, and IFIT1 were also activated in COVID-19 patients, and GO analysis showed that HERV-K (HML-2) can regulate the secretion of interferon. Conclusions. The high expression of HERV-K (HML-2) might activate the increase of interferon in COVID-19 patients, proving that HERV-K does not only play a negative role in the human body.

Significant Upregulation of HERV-K (HML-2) Transcription Levels in Human Lung Cancer and Cancer Cells.

Lung cancer is the second most common cancer worldwide and the leading cause of cancer death in the world. Therefore, there is an urgent need to develop new and effective biomarkers for diagnosis and treatment. Under this circumstance, human endogenous retroviruses (HERVs) were recently introduced as novel biomarkers for cancer diagnosis. This study focused on the correlation between lung cancer and HERV-K (HML-2) transcription levels. At the cellular level, different types of lung cancer cells and human normal lung epithelial cells were used to analyze the transcription levels of the HERV-K (HML-2) gag, pol, and env genes by RT-qPCR. At the level of lung cancer patients, blood samples with background information from 734 lung cancer patients and 96 healthy persons were collected to analyze the transcription levels of HERV-K (HML-2) gag, pol, and env genes. The results showed that the transcriptional levels of the HERV-K (HML-2) gag, pol, and env genes in lung cancer cells and lung cancer patient blood samples were significantly higher than those in the healthy controls, which was also verified by RNAScope ISH technology. In addition, we also found that there was a correlation between the abnormal transcription levels of HERV-K (HML-2) genes in lung cancer patients and the clinicopathological parameters of lung cancer. We also identified the distribution locations of the gag, pol, and env primer sequences on each chromosome and analyzed the function of these loci. In conclusion, HERV-K (HML-2) genes may be a potential biomarker for the diagnosis of lung cancer.

[Assemble of magnetic nanoparticles into the structure of cisplatin liposome].

Effects of different procedures of magnetic nanoparticles into the liposome structure on the distribution of magnetic particles in the liposome were investigated. Magnetic liposomes with high-encapsulating rate of cisplatin (CDDP) were obtained. Fe3O4 magnetic nanoparticles which was modified by organic functional group on surface was synthesized by an one-step modified hydrothermal method. The CDDP magnetic liposomes were prepared by a film scattering-ultrasonic technique and the concentrations of CDDP in the liposomes were measured by graphite furnace atomic absorbance spectroscopy. Magnetic liposomes with different microstructure were prepared by the two different procedures, where the magnetic particles were combined with phospholipid before the film preparation to form liposome in procedure I, and drug solution and the magnetic particles were mixed before hydrating the lipids film to form liposome in procedure II. The liposome structure was observed by transmission electron microscope (TEM). The CDDP magnetic liposomes were prepared by the optimized method which was selected by orthogonal test. Encapsulation rate of the magnetic particles distributed in the phospholipid bilayer through the procedure I was 34.90%. While liposome, produced by the procedure II technique, contained magnetic particles in the interior aqueous compartment, which encapsulation rate was 28.34%. Encapsulation rates of both I and II were higher than that of conventional liposome. The release profile of all the three different liposomes in vitro fitted with a first-order equation. Because of distribution of magnetic particles in the phospholipid bilayer, the skeleton of phospholipid bilayer was changed. The releasing tl/2 of magnetic liposomes produced by the procedure I technique is 9 h, which is shorter than that of the other two liposomes. Assemble of magnetic nanoparticles into the structure of liposome was succeeded by the procedure I, which showed superiority than by procedure II whatever in CDDP liposome encapsulation efficiency and content of the magnetic particles and would ensure sustained-release character.

1-Diphenyl-methyl-4-[3-(4-fluoro-benzo-yl)prop-yl]piperazine-1,4-diium dichloride monohydrate.

In the title compound, C(27)H(31)FN(2)O(2+)·2Cl(-)·H(2)O, the piperazine ring adopts a chair conformation and both N atoms are protonated. The Cl(-) anions form strong hydrogen bonds to these protons. O/N-H⋯Cl and C-H⋯O hydrogen bonds link the anions, cations and water of hydration into a three-dimensional network.

[Synthesis and spectral characteristic of pharmaceutical dipfluzine hydrochloride-benzoic acid co-crystal].

Pharmaceutical co-crystals can improve the chemical and physical properties of active pharmaceutical ingredient (API), which is new idea and expected to provide new stable structures. Pharmaceutical co-crystals have the potential to be much more useful in pharmaceutical products than salts, solvates or hydrates, polymorphs and stoichiometric solvates (pseudo-polymorphs). In our study, dipfluzine hydrochloride-benzoic acid co-crystal was synthesized by solid co-grinding. The samples were subjected to IR, DSC, XRD, Raman and THz spectral analysis. The results indicated that dipfluzine hydrochloride-benzoic acid complex was new phase compared with the single API and CCF. THz-TDS characterization indicated that hydrogen bond formed between API and CCF, which confirmed the formation of co-crystal.