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1.
Huan Jing Ke Xue ; 41(7): 3315-3325, 2020 Jul 08.
Article in Chinese | MEDLINE | ID: mdl-32608905

ABSTRACT

Wheat straw biochar (BC) was modified by KOH and magnetics to generate composited modified biochar (FKC). Based on characterization by scanning electron microscopy-energy dispersive spectrometry (SEM-EDS), Brunauer-Emmett-Teller (BET), Fourier transform infrared (FT-IR), X-ray diffraction (XRD), and magnetic (VSM) techniques, the adsorption characteristics and mechanisms of Cd2+ in water and the effects of temperature, pH value, and dosage on the adsorption characteristics of FKC were studied. The results showed that the modified biochar was loose and porous. The specific surface area of FKC increased by 19.11 times, the number of aromatic and oxygen-containing functional groups such as O-H, C=O, and C=C increased, and a new functional group Fe-O formed compared to the BC. FKC is magnetic, and its magnetization is 8.43 emu·g-1, which can be recycled and reused. The adsorption of Cd2+ by FKC fitted well with the pseudo-second-order kinetic model and the Langmuir model, indicating that chemical adsorption is the main adsorption mechanism. The theoretical maximum equilibrium adsorption capacity of FKC is 23.44 mg·g-1, which is 1.47 times that of BC. The thermodynamic parameters suggested the adsorption of Cd2+ by FKC was a spontaneous and endothermic process. The adsorption capacity increased with an increase of pH in the region 2-8, and a biochar dosage of 10 g·L-1 was used. After three cycles of adsorption-desorption-adsorption, the adsorption capacity of Cd2+ by FKC still reached 17.71 mg·g-1, indicating that FKC has good reusability. These results can provide a theoretical basis for the application of KOH and magnet-modified biochar from wheat straw to remove heavy metals from contaminated wastewater.

2.
J Zhejiang Univ Sci B ; 20(2): 180-192, 2019.
Article in English | MEDLINE | ID: mdl-30666850

ABSTRACT

To understand the effects of Lactobacillus rhamnosus GG (ATCC 53103) on intestinal barrier function in pre-weaning piglets under normal conditions, twenty-four newborn littermate piglets were randomly divided into two groups. Piglets in the control group were orally administered with 2 mL 0.1 g/mL sterilized skim milk while the treatment group was administered the same volume of sterilized skim milk with the addition of viable L. rhamnosus at the 1st, 3rd, and 5th days after birth. The feeding trial was conducted for 25 d. Results showed that piglets in the L. rhamnosus group exhibited increased weaning weight and average daily weight gain, whereas diarrhea incidence was decreased. The bacterial abundance and composition of cecal contents, especially Firmicutes, Bacteroidetes, and Fusobacteria, were altered by probiotic treatment. In addition, L. rhamnosus increased the jejunal permeability and promoted the immunologic barrier through regulating antimicrobial peptides, cytokines, and chemokines via Toll-like receptors. Our findings indicate that oral administration of L. rhamnosus GG to newborn piglets is beneficial for intestinal health of pre-weaning piglets by improving the biological, physical, and immunologic barriers of intestinal mucosa.


Subject(s)
Intestinal Mucosa/immunology , Lacticaseibacillus rhamnosus , Probiotics/administration & dosage , Administration, Oral , Animals , Animals, Newborn , Cytokines/genetics , Female , Gastrointestinal Microbiome , Immunity, Innate , Male , Signal Transduction , Swine , Weaning
3.
J Enzyme Inhib Med Chem ; 34(1): 150-162, 2019 Dec.
Article in English | MEDLINE | ID: mdl-30427217

ABSTRACT

A series of new Olaparib derivatives was designed and synthesized, and their inhibitory activities against poly (ADP-ribose) polymerases-1 (PARP-1) enzyme and cancer cell line MDA-MB-436 in vitro were evaluated. The results showed that compound 5l exhibited the most potent inhibitory effects on PARP-1 enzyme (16.10 ± 1.25 nM) and MDA-MB-436 cancer cell (11.62 ± 2.15 µM), which was close to that of Olaparib. As a PARP-1 inhibitor had been reported to be viable to neuroprotection, in order to search for new multitarget-directed ligands (MTDLs) for the treatment of Alzheimer's disease (AD), the inhibitory activities of the synthesized compounds against the enzymes AChE (from electric eel) and BChE (from equine serum) were also tested. Compound 5l displayed moderate BChE inhibitory activity (9.16 ± 0.91 µM) which was stronger than neostigmine (12.01 ± 0.45 µM) and exhibited selectivity for BChE over AChE to some degree. Molecular docking studies indicated that 5l could bind simultaneously to the catalytic active of PARP-1, but it could not interact well with huBChE. For pursuit of PARP-1 and BChE dual-targeted inhibitors against AD, small and flexible non-polar groups introduced to the compound seemed to be conducive to improving its inhibitory potency on huBChE, while keeping phthalazine-1-one moiety unchanged which was mainly responsible for PARP-1 inhibitory activity. Our research gave a clue to search for new agents based on AChE and PARP-1 dual-inhibited activities to treat Alzheimer's disease.


Subject(s)
Acetylcholinesterase/metabolism , Antineoplastic Agents/pharmacology , Cholinesterase Inhibitors/pharmacology , Molecular Docking Simulation , Phthalazines/chemistry , Phthalazines/pharmacology , Piperazines/chemistry , Piperazines/pharmacology , Poly (ADP-Ribose) Polymerase-1/antagonists & inhibitors , Animals , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Butyrylcholinesterase/metabolism , Cell Line, Tumor , Cell Proliferation/drug effects , Cholinesterase Inhibitors/chemical synthesis , Cholinesterase Inhibitors/chemistry , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Electrophorus , Horses , Humans , Molecular Structure , Phthalazines/chemical synthesis , Piperazines/chemical synthesis , Poly (ADP-Ribose) Polymerase-1/metabolism , Structure-Activity Relationship
4.
J Mol Model ; 24(7): 151, 2018 Jun 05.
Article in English | MEDLINE | ID: mdl-29869722

ABSTRACT

Alzheimer's disease (AD) is a chronic neurodegenerative disease of the elderly that seriously affects the quality of life and the life expectancy of those affected. There is, as yet, no effective drug treatment of AD, although several acetylcholinesterase (AChE) inhibitors and a glutamate antagonist can provide relief from its symptoms. Recent studies have indicated that the overactivation of poly(ADP-ribose) polymerase-1 (PARP-1) may promote nerve cell death in the brains of AD patients, implying that PARP-1 inhibition may have therapeutic value for the treatment of AD. Therefore, it is important to investigate novel agents with both AChE- and PARP-1-inhibitory bioactivities. In this study, the structure-based virtual screening of PARP-1 inhibitors was performed to search for potential agents with high affinities for AChE. The dynamic stability of the selected AChE-ligand complexes was investigated by molecular dynamics (MD) simulation. Two compounds, CID57390505 and CID71605390, showed high affinities for and stability in complex with AChE in docking and MD simulations. Thus, our in silico research identified two compounds with AChE and PARP-1 dual-targeted activities, indicating that this technique could aid attempts to develop more potent agents against AD.


Subject(s)
Acetylcholinesterase/chemistry , Cholinesterase Inhibitors/chemistry , Enzyme Inhibitors/chemistry , Molecular Docking Simulation , Molecular Dynamics Simulation , Poly (ADP-Ribose) Polymerase-1/chemistry , Alzheimer Disease/drug therapy , Cholinesterase Inhibitors/pharmacology , Drug Discovery , Enzyme Inhibitors/pharmacology , Humans , Inhibitory Concentration 50 , Ligands , Molecular Structure , Poly (ADP-Ribose) Polymerase-1/antagonists & inhibitors , Quantitative Structure-Activity Relationship
5.
Arch Microbiol ; 195(5): 349-56, 2013 May.
Article in English | MEDLINE | ID: mdl-23455449

ABSTRACT

Depending on the microenvironment, macrophages can acquire distinct functional phenotypes, referred to as classically activated M1 and M2. M1 macrophages are considered potent effector cells that kill intracellular pathogens, and M2 macrophages promote the resolution of wound healing. In this study, we are interested to know whether probiotic Bacillus amyloliquefaciens (Ba) can induce macrophages polarization. Real-time fluorescence PCR analysis demonstrated that the expression of IL-1ß, iNOS, TNF-α and IL-6 genes for M1 macrophages was significantly increased at 1.5 h after probiotic Ba treatment compared to the probiotic Ba-free treatment (P < 0.01), whereas the expression of M2 macrophage marker genes (Arg1, Fizz1, MR, Ym1) was decreased (P < 0.05). Furthermore, the phagocytic activity was dramatically increased in the Ba-treated BMDMs using a FITC-dextran endocytosis assay. Together, these findings indicated that probiotic Ba facilitated polarization of M1 macrophages and enhanced its phagocytic capacity. The results expanded our knowledge about probiotic function-involved macrophage polarization.


Subject(s)
Bacillus , Macrophage Activation , Macrophages/immunology , Probiotics/administration & dosage , Transcriptome , Animals , Bacillus/classification , Bacillus/metabolism , Macrophages/cytology , Macrophages/metabolism , Mice , Mice, Inbred C57BL , Nitric Oxide/metabolism
6.
Asian Pac J Cancer Prev ; 13(7): 3403-8, 2012.
Article in English | MEDLINE | ID: mdl-22994768

ABSTRACT

The molecular mechanisms involved in the progression of clear cell renal cell carcinomas (ccRCCs) are still unclear. The aim of this study was to analyse the relationships between expression of RALYL and clinical characteristics. In 41 paired samples of ccRCCs and adjacent normal tissues, we used real-time qPCR to evaluate the expression of RALYL mRNA. RALYL protein levels were determined in 146 samples of ccRCC and 37 adjacent normal tissues by immunohistochemistry. Statistical analysis was used to explore the relationships between expression of RALYL and the clinical characteristics (gender, age, tumor size, T stage, N stage, M stage, survival times and survival outcome) in ccRCC. In addition, these patients were follow-up period 64 months (range: 4~116 months) to investigate the influence on prognosis. We found significantly differences between ccRCC tissues and normal tissues (p<0.001, paired-sample t test) in mRNA levels of RALYL. Immunohistochemistry analyses in 146 ccRCC samples and 37 adjacent normal tissues showed significantly lower RALYL protein levels in ccRCC samples (χ2-test, p<0.001), inversely correlating with tumour size (p=0.024), T stage (0.005), N stage (p<0.001) as well as M stage (p=0.019), but not age (p=0.357) and gender (p=0.348). Kaplan-Meier survival analysis demonstrated that people with lower level of RALYL expression had a poorer survival rate than those with a higher level of RALYL expression, significantly different by the log-rank test (p=0.011). Cox regression analysis indicated that RALYL expression (p=0.039), N stage (p=0.008) and distant metastasis (p<0.001) were independent prognosis factors for the overall survival of ccRCC patients. We demonstrated that the expression of RALYL was significantly low in ccRCC and correlated with a poor prognosis in a large number of clinical samples. Our findings showed that RALYL may be a potential therapeutic target as well as a poor prognostic factor.


Subject(s)
Carcinoma, Renal Cell/metabolism , Carcinoma, Renal Cell/pathology , Heterogeneous-Nuclear Ribonucleoprotein Group C/biosynthesis , Kidney Neoplasms/metabolism , Kidney Neoplasms/pathology , Carcinoma, Renal Cell/genetics , Female , Follow-Up Studies , Heterogeneous-Nuclear Ribonucleoprotein Group C/genetics , Heterogeneous-Nuclear Ribonucleoprotein Group C/metabolism , Humans , Immunohistochemistry/methods , Kaplan-Meier Estimate , Kidney Neoplasms/genetics , Male , Middle Aged , Prognosis , Proportional Hazards Models , RNA, Messenger/biosynthesis , RNA, Messenger/genetics , Survival Rate
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