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https://www.readbyqxmd.com/read/29149763/formulation-and-anti-neurotoxic-activity-of-baicalein-incorporating-neutral-nanoliposome
#1
Farhang Aliakbari, Ali Akbar Shabani, Hassan Bardania, Hossein Mohammad-Beigi, Amir Tayaranian Marvian, Faezeh Dehghani Esmatabad, Abbas Ali Vafaei, Seyed Abbas Shojaosadati, Ali Akbar Saboury, Gunna Christiansen, Daniel E Otzen, Dina Morshedi
Despite extensive studies of the effects of herbal-derived small molecules in the biopharmaceutical and biomedical sciences, their low solubility and stability remain a challenge. Here we focus on baicalein, a small molecule showing potential against neurodegenerative diseases such as Parkinson's and Alzheimer's. However, therapeutic usage in vivo is challenged by low solubility and stability. To address this we have applied neutrally-charged nanoliposome (NLP) as carrier for baicalein. Baicalein was incorporated into NLP to form NLP-Ba at molar baicalain:lipid ratios of up to 1:3, giving a drug entrapment efficiency of 96...
November 11, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29149728/tuning-magnetic-relaxation-properties-of-hard-cores-in-core-shell-colloids-by-modification-of-soft-shell
#2
Nataliya Shamsutdinova, Rustem Zairov, Irek Nizameev, Aidar Gubaidullin, Alsu Mukhametshina, Sergey Podyachev, Ildus Ismayev, Marsil Kadirov, Alexandra Voloshina, Timur Mukhametzyanov, Asiya Mustafina
The present work introduces an impact of polyelectrolyte-based hydrophilic shell on magnetic relaxivity and luminescence of hard cores built from isostructural complexes of Tb(III) and Gd(III) in the core-shell aqueous colloids. Microscopic and scattering techniques reveal "plum pudding" morphology of the colloids, where polyelectrolyte-coated ultrasmall (<5nm) hard cores form aggregates in aqueous solutions. Interaction of bovine serum albumin (BSA) with the colloids provides a tool to modify the polyelectrolyte-based shell, which is the reason for the improvement in both aggregation behavior of the colloids and their relaxivity...
November 11, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29149705/toll-like-receptor-4-deficiency-increases-resistance-in-sepsis-induced-immune-dysfunction
#3
Chao Cao, Yanfen Chai, Songtao Shou, Jun Wang, Ying Huang, Tao Ma
Sepsis constitutes a serious life-threatening syndrome associated with complications of deregulated inflammatory response against endotoxin/lipopolysaccharide (LPS)-mediated severe infection. Toll-like receptor 4 (TLR4) plays a critical role in the activation of innate immunity through recognition of LPS. However, the impact of TLR4 signaling on the development of sepsis-induced immune dysfunction remains unclear. The aim of this study was to investigate the effect of TLR4 on regulatory T cells (Tregs) and its potential mechanism...
November 14, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/29149694/a-high-brightness-probe-of-polymer-nanoparticles-for-biological-imaging
#4
Sirong Zhou, Jiarong Zhu, Yaping Li, Liheng Feng
Conjugated polymer nanoparticles (CPNs) with high brightness in long wavelength region were prepared by the nano-precipitation method. Based on fluorescence resonance energy transfer (FRET) mechanism, the high brightness property of the CPNs was realized by four different emission polymers. Dynamic light scattering (DLS) and scanning electron microscopy (SEM) displayed that the CPNs possessed a spherical structure and an average diameter of ~75nm. Analysis assays showed that the CPNs had excellent biocompatibility, good photostability and low cytotoxicity...
November 11, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/29149649/chk1-inhibitors-overcome-imatinib-resistance-in-chronic-myeloid-leukemia-cells
#5
Hu Lei, Jin Jin, Meng Liu, Xiangyun Li, Hao Luo, Li Yang, Hanzhang Xu, Yingli Wu
Drug resistance to tyrosine kinase inhibitors (TKIs) is currently a clinical problem of chronic myelogenous leukemia (CML). Bcr-Abl protein depletion is considered as a way to overcome drug resistance to TKIs. In our study, Chk1 inhibitors, AZD7762 and MK-8776, had strong antitumor effects on CML cell line KBM5 and imatinib-resistant form KBM5(T315I). Moreover, Chk1 inhibitors showed a strong cytotoxic effect on leukemia cells from primary CML and imatinib-resistance CML patients, but low cytotoxic effect on normal human mononuclear cells...
November 11, 2017: Leukemia Research
https://www.readbyqxmd.com/read/29149434/enhancement-of-therapeutic-dna-vaccine-potency-by-melatonin-through-inhibiting-vegf-expression-and-induction-of-antitumor-immunity-mediated-by-cd8-t-cells
#6
Sanaz Baghban Rahimi, Alireza Mohebbi, Gelareh Vakilzadeh, Peyvand Biglari, Soodeh Razeghi Jahromi, Seyed Reza Mohebi, Sadegh Shirian, Ali Gorji, Amir Ghaemi
To be effective, therapeutic cancer vaccines should stimulate both an effective cell-mediated and a robust cytotoxic CD8+ T-cell response against human papillomavirus (HPV)-infected cells to treat the pre-existing tumors and prevent potential future tumors. In this study, the therapeutic experiments were designed in order to evaluate antitumor effect against the syngeneic TC-1 tumor model. The anti-tumor efficacy of a HPV-16 E7 DNA vaccine adjuvanted with melatonin (MLT) was evaluated in a C57BL/6 mouse tumor model by measuring tumor growth post vaccination and the survival rate of tumor-bearing mice, analyzing the specific lymphocyte proliferation responses in control and vaccinated mice by MTT assay...
November 17, 2017: Archives of Virology
https://www.readbyqxmd.com/read/29149212/mycolactone-displays-anti-inflammatory-effects-on-the-nervous-system
#7
Caroline Isaac, Annie Mauborgne, Alfonso Grimaldi, Kemy Ade, Michel Pohl, Cristina Limatola, Yves Boucher, Caroline Demangel, Laure Guenin-Macé
BACKGROUND: Mycolactone is a macrolide produced by the skin pathogen Mycobacterium ulcerans, with cytotoxic, analgesic and immunomodulatory properties. The latter were recently shown to result from mycolactone blocking the Sec61-dependent production of pro-inflammatory mediators by immune cells. Here we investigated whether mycolactone similarly affects the inflammatory responses of the nervous cell subsets involved in pain perception, transmission and maintenance. We also investigated the effects of mycolactone on the neuroinflammation that is associated with chronic pain in vivo...
November 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/29149102/recombinant-immunotoxins-targeting-b-cell-maturation-antigen-are-cytotoxic-to-myeloma-cell-lines-and-myeloma-cells-from-patients
#8
T K Bera, Y Abe, T Ise, A Oberle, D Gallardo, X-F Liu, S Nagata, M Binder, I Pastan
No abstract text is available yet for this article.
November 17, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/29149089/mnsod-and-cyclin-b1-coordinate-a-mito-checkpoint-during-cell-cycle-response-to-oxidative-stress
#9
Amanda L Kalen, Iman M Ahmad, Maher Y Abdalla, Yunxia Q O'Malley, Prabhat C Goswami, Ehab H Sarsour
Communication between the nucleus and mitochondrion could coordinate many cellular processes. While the mechanisms regulating this communication are not completely understood, we hypothesize that cell cycle checkpoint proteins coordinate the cross-talk between nuclear and mitochondrial functions following oxidative stress. Human normal skin fibroblasts, representative of the G₂-phase, were irradiated with 6 Gy of ionizing radiation and assayed for cyclin B1 translocation, mitochondrial function, reactive oxygen species (ROS) levels, and cytotoxicity...
November 17, 2017: Antioxidants (Basel, Switzerland)
https://www.readbyqxmd.com/read/29148852/sildenafil-citrate-improves-the-delivery-and-anticancer-activity-of-doxorubicin-formulations-in-a-mouse-model-of-breast-cancer
#10
Khaled Greish, Maryam Fateel, Sara Abdelghany, Nanitha Rachel, Houman Alimoradi, Moiz Bakhiet, Ahmed Alsaie
Sildenafil is an approved drug for the treatment of erectile dysfunction. The drug exerts its action through the relaxation of smooth muscles and the modulation of vascular endothelial permeability. In this work, we tested whether the aforementioned effects of Sildenafil on tumor vasculatures could result in an improvement of anticancer drug concentration in tumor tissues, and hence improve its anticancer effect. Sildenafil when added to doxorubicin showed synergistic anticancer activity against 4T1 breast cancer cells in vitro...
November 17, 2017: Journal of Drug Targeting
https://www.readbyqxmd.com/read/29148846/preparation-and-evaluation-of-curcumin-loaded-self-assembled-micelles
#11
Lu-Lu Wang, Dan-Dan He, Shu-Xia Wang, Yun-Hao Dai, Jian-Ming Ju, Cheng-Lei Zhao
Objective Curcumin being used to treat various chronic diseases while its poor bioavailability issue limited its wide clinical application as a therapeutic agent. The aim of this work was to prepare curcumin-loaded self-assembled micelles using soluplus and solutol®HS15 (SSCMs) to enhance curcumin's solubility and thus oral bioavailability. Methods Optimum formulation was investigated and the optimized ratio of drugs and excipients was obtained and the SSCMs were prepared via ethanol solvent evaporation method...
November 17, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29148732/photocontrolled-release-of-doxorubicin-conjugated-through-a-thioacetal-photocage-in-folate-targeted-nanodelivery-systems
#12
Pamela T Wong, Shengzhuang Tang, Jayme Cannon, Dexin Chen, Rachel Sun, Jennifer Lee, James Phan, Ke Tao, Kang Sun, Biqiong Chen, James R Baker, Seok Ki Choi
Despite their proven ability for precise and targeted release, nanoplatform systems for photocontrolled delivery often face formidable synthetic challenges, in part, due to the paucity of advanced linker strategies. Here we report on a novel linker strategy using a thioacetal ortho-nitrobenzaldehyde (TNB) cage, demonstrating its application for delivery of doxorubicin (Dox) in two nanoscale systems. This photocleavable linker, TNB(OH), which presents two identical arms, each terminated with a hydroxyl functionality, was prepared in a single step from 6-nitroverataldehyde...
November 17, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29148584/metabolic-effects-of-p-p-dde-on-atlantic-salmon-hepatocytes
#13
Pål A Olsvik, Liv Søfteland
Decades after being banned in many countries, DDT and its metabolites are still considered major environmental hazards. The p,p'-DDE isomer, the DDT metabolite found in highest concentration in aquaculture feeds, is an endocrine disruptor with demonstrated ability to induce epigenetic effects. This study aimed at examining the impact of p,p'-DDE on Atlantic salmon. Primary hepatocytes were exposed to four concentrations of p,p'-DDE (0.1, 1, 10, 100 μm) for 48 hours, and endpoints included cytotoxicity, global DNA methylation, targeted transcription and metabolomics profiling (100 μm)...
November 17, 2017: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/29148294/synthesis-physiochemical-property-and-antimicrobial-activity-of-novel-quaternary-ammonium-salts
#14
Xianrui Xie, Wei Cong, Feng Zhao, Hongjuan Li, Wenyu Xin, Guige Hou, Chunhua Wang
Twenty-four novel 5-phenyl-1,3,4-oxadiazole-2-thiol (POT) analogues, benzo[d]oxazole-2-thiol, benzo[d]thiazole-2-thiol and 5-methyl-1,3,4-thiadiazole-2-thiol-substituted N,N-bis(2-hydroxyethyl) quaternary ammonium salts (QAS) (5a-d, 6a-d, 7a-d, 10a-d, 13a-d, 16a-d) were prepared and characterised by FTIR, NMR and elemental analysis. Part of target compounds (5d, 6d, 7d, 10d, 13d, 16d) displayed potent antimicrobial effect against ten common pathogens (S. aureus, α-H-tococcus, β-H-tococcus, E. coli, P. aeruginosa, Proteus vulgaris, Canidia Albicans, Cytospora mandshurica, Physalospora piricola, Aspergillus niger) and had relatively low cytotoxity against two human cell lines (HaCat and LO2)...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29147993/preparation-and-characterization-of-gelatin-sericin-carboxymethyl-chitosan-medical-tissue-glue
#15
Min Liang, Zhenzhu Li, Cengceng Gao, Fuping Wang, Zhongmin Chen
BACKGROUND: The development and application of medical glue has been continuously expanding and advancing. However, there are few glues that combine low-cost with excellent biocompatibility. METHODS: We have prepared a medical tissue glue using a gelatin (Gel), sericin (SS) and carboxymethyl chitosan (CMCS) blend solution, cross-linked with 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide (EDC). The combination's characteristics and microstructure morphology were observed by Fourier transform infrared spectroscopy (FT-IR) and scanning electron microscope (SEM)...
November 16, 2017: Journal of Applied Biomaterials & Functional Materials
https://www.readbyqxmd.com/read/29147952/gemigliptin-a-novel-dipeptidyl-peptidase-iv-inhibitor-exerts-a-synergistic-cytotoxicity-with-the-histone-deacetylase-inhibitor-pxd101-in-thyroid-carcinoma-cells
#16
S H Kim, J G Kang, C S Kim, S-H Ihm, M G Choi, H J Yoo, S J Lee
PURPOSE: The influence of the dipeptidyl peptidase-IV inhibitor gemigliptin alone or in combination with the histone deacetylase inhibitor PXD101 on survival of thyroid carcinoma cells was investigated. METHODS: SW1736, TPC-1, 8505C and BCPAP human thyroid carcinoma cells were used. To assess cell survival, cell viability, the percentage of viable cells and dead cells, cytotoxic activity, ATP levels and FACS analysis were measured. To validate the impact of gemigliptin combined with PXD101, the interactions were estimated by obtaining combination index in cells treated with two agents...
November 16, 2017: Journal of Endocrinological Investigation
https://www.readbyqxmd.com/read/29147891/long-term-presence-of-angiotensin-ii-type-1-receptor-autoantibody-reduces-aldosterone-production-by-triggering-ca-2-overload-in-h295r-cells
#17
Jinghui Lei, Suli Zhang, Pengli Wang, Yang Liao, Jingwei Bian, Xiaochen Yin, Ye Wu, Lina Bai, Feng Wang, Xiaoli Yang, Huirong Liu
Preeclamptic women are reported to have inadequate plasma volume expansion coupled with a suppressed secretion of aldosterone; however, the specific mechanism of preeclampsia remains unclear. We demonstrated that the presence of long-term angiotensin II type 1 receptor autoantibody (AT1-AA) reduces aldosterone production by triggering a Ca(2+) overload in H295R cells. AT1-AA was discovered in preeclamptic women and reported to activate AT1R, and consequently elevate intracellular Ca(2+). We found that AT1-AA significantly prolonged the time of intracellular Ca(2+) elevation...
November 16, 2017: Immunologic Research
https://www.readbyqxmd.com/read/29147875/evaluation-of-nfsa-like-nitroreductases-from-neisseria-meningitidis-and-bartonella-henselae-for-enzyme-prodrug-therapy-targeted-cellular-ablation-and-dinitrotoluene-bioremediation
#18
Michelle H Rich, Abigail V Sharrock, Kelsi R Hall, David F Ackerley, Joanna K MacKichan
OBJECTIVES: To characterize the activities of two candidate nitroreductases, Neisseria meningitidis NfsA (NfsA_Nm) and Bartonella henselae (PnbA_Bh), with the nitro-prodrugs, CB1954 and metronidazole, and the environmental pollutants 2,4- and 2,6-dinitrotoluene. RESULTS: NfsA_Nm and PnbA_Bh were evaluated in Escherichia coli over-expression assays and as His6-tagged proteins in vitro. With the anti-cancer prodrug CB1954, both enzymes were more effective than the canonical O2-insensitive nitroreductase E...
November 17, 2017: Biotechnology Letters
https://www.readbyqxmd.com/read/29147868/hydrogen-peroxide-h2o2-a%C3%A2-review-of-its-use-in-surgery
#19
REVIEW
Michael Vincent Urban, Thomas Rath, Christine Radtke
Hydrogen peroxide has been used in medicine for more than 100 years. It is known in surgery as a highly useful irrigation solution by virtue of both its hemostatic and its antimicrobial effects. Due to its possible negative effect on wound healing and its cytotoxic effect in higher concentrations, there are concerns about the safety of its use. The objective of this paper is to review the safety and beneficial effects of hydrogen peroxide.
November 16, 2017: Wiener Medizinische Wochenschrift
https://www.readbyqxmd.com/read/29147793/pharmacophoric-characteristics-of-dengue-virus-ns2b-ns3pro-inhibitors-a-systematic-review-of-the-most-promising-compounds
#20
REVIEW
Camyla Alves Leonel, William Gustavo Lima, Michelli Dos Santos, Ariane Coelho Ferraz, Alex Gutterres Taranto, José Carlos de Magalhães, Luciana Lara Dos Santos, Jaqueline Maria Siqueira Ferreira
Dengue virus (DENV) infection can lead to a wide range of clinical manifestations, including fatal hemorrhagic complications. There is a need to find effective pharmacotherapies to treat this disease due to the lack of specific immunotherapies and antiviral drugs. That said, the DENV NS2B/NS3pro protease complex is essential in both the viral multiplication cycle and in disease pathogenesis, and is considered a promising target for new antiviral therapies. Here, we performed a systematic review to evaluate the pharmacophoric characteristics of promising compounds against NS2B/NS3pro reported in the past 10 years...
November 16, 2017: Archives of Virology
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