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https://www.readbyqxmd.com/read/29353288/quercetin-inhibits-breast-cancer-stem-cells-via-downregulation-of-aldehyde-dehydrogenase-1a1-aldh1a1-chemokine-receptor-type-4-cxcr4-mucin-1-muc1-and-epithelial-cell-adhesion-molecule-epcam
#1
Rong Wang, Laixiu Yang, Shen Li, Dongmei Ye, Lihong Yang, Qingyan Liu, Zibo Zhao, Qing Cai, Junzhen Tan, Xiuli Li
BACKGROUND Quercetin, nature's most common flavonoid, possesses anticarcinogenic properties against various forms of cancer. The aim of this study was to investigate the effect of quercetin on breast cancer stem cells in the MDA-MB-231 cell line, and to elucidate the possible mechanisms for those effects. MATERIAL AND METHODS We evaluated breast cancer stem cell proliferation, clone generation, and mammosphere formation to determine the effect of quercetin treatment on breast cancer stem cells. RESULTS In our study, quercetin suppressed breast cancer stem cell proliferation, self-renewal, and invasiveness...
January 21, 2018: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/29353209/mir-182-promotes-prostate-cancer-progression-through-activating-wnt-%C3%AE-catenin-signal-pathway
#2
Dawei Wang, Guoliang Lu, Yuan Shao, Da Xu
Although prostate cancer can be surgical excised and effectively treated by androgen-deprivation therapy, radiotherapy, or chemotherapy, management of patients with advanced or drug-resistance prostate cancer stills remains a big trouble. Accumulated evidence indicated that miR-182 and Wnt/β-catenin function as tumor oncogene in the progression of a variety of tumors. However, little is known about how miR-182 regulates β-catenin signal molecular and impacts on the tumorigenesis of human prostate cancer. In this study, employing the analyses of qRT-PCR, we found that prostate cancer tissues expressed much more miR-182 than non-cancer tissues did...
January 17, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29353042/ginkgolic-acid-induces-interplay-between-apoptosis-and-autophagy-regulated-by-ros-generation-in-colon-cancer
#3
Yuxia Liu, Bin Yang, Lirong Zhang, Xianling Cong, Zhen Liu, Yu Hu, Jing Zhang, Haixia Hu
Presently, developing effective anti-colon cancer drugs still remains to be important. Ginkgolic acids (GA), as a botanical drug extracted from the seed coat of Ginkgo biloba L., possess various bioactive properties. Our findings, for the first time, indicated that GA suppressed colon cancer cell proliferation, migration and invasion. GA led to cell death through G0/G1 phase arrest. In addition, apoptosis was significantly induced by GA treatment. The intrinsic apoptosis pathway was included, proved by the release of cytochrome c (Cyto-c) from the mitochondria into the cytosol...
January 15, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29353022/using-medical-examiner-case-narratives-to-improve-opioid-overdose-surveillance
#4
Emily Hurstak, Christopher Rowe, Caitlin Turner, Emily Behar, Rachel Cabugao, Nikolas P Lemos, Phillip Coffin
BACKGROUND: Current opioid overdose mortality surveillance methods do not capture the complexity of the overdose epidemic. Most rely on death certificates, which may underestimate both opioid analgesic and heroin deaths. Categorizing deaths using other characteristics from the death record including route of drug administration may provide useful information to design and evaluate overdose prevention interventions. METHODS: We reviewed California Electronic Death Reporting System records and San Francisco Office of the Chief Medical Examiner (OCME) toxicology reports and investigative case narratives for all unintentional opioid overdose deaths in San Francisco County from 2006 to 2012...
January 17, 2018: International Journal on Drug Policy
https://www.readbyqxmd.com/read/29353017/ph-triggered-surface-charge-reversal-nanoparticles-alleviate-experimental-murine-colitis-via-selective-accumulation-in-inflamed-colon-regions
#5
Muhammad Naeem, Murtada A Oshi, Jihyun Kim, Juho Lee, Jiafu Cao, Hasan Nurhasni, Eunok Im, Yunjin Jung, Jin-Wook Yoo
In this study, we developed pH-triggered surface charge-reversal lipid nanoparticles (LNPs), loaded with budesonide, which could precisely deliver the drug to inflamed colon segments for the treatment of ulcerative colitis. Polyethyleneimine (PEI) was used to render LNPs cationic (PEI-LNPs), and Eudragit® S100 (ES) was coated on PEI-LNPs to obtain pH-triggered charge-reversal LNPs (ES-PEI-LNPs). ES coating avoided a burst drug release under acidic conditions mimicking the stomach and early small intestine environments and showed a sustained release in the colon...
January 15, 2018: Nanomedicine: Nanotechnology, Biology, and Medicine
https://www.readbyqxmd.com/read/29353012/fabrication-of-poly-ethylene-glycol-coated-mesoporous-nanocomposite-zno-fe2o3-for-methotrexate-delivery-an-integrated-nanoplatform-for-dual-mode-cancer-therapy
#6
Azam S Alavi, Azadeh Meshkini
Although chemotherapy is an effective strategy for treatment of tumor cells, the non-specific distribution of chemotherapy drugs and their poor aqueous solubility result in impaired treatment and cause serious side effects in patients. In this study, mesoporous ZnO@Fe2O3 nanocomposite was fabricated and used as a platform for drug delivery. ZnO@Fe2O3 nanocomposite showed a high capacity for the adsorption of chemotherapy drug, methotrexate (MTX). Drug-loaded nanoparticle was coated with poly(ethylene glycol) (PEG), leading to the enhanced colloidal stability and good cytocompatibility...
January 15, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29352994/topical-drug-delivery-devices-a-review
#7
REVIEW
C J F Bertens, M Gijs, R M M A Nuijts, F J H M van den Biggelaar
For the treatment and prevention of ocular diseases, most patients are treated with conventional drug delivery formulations such as eye drops or ointments. However, eye drops and ointments suffer from low patient compliance and low effective drug concentration at the target site. Therefore, new medical devices are being explored to improve drug delivery to the eye. Over the years, various delivery devices have been developed including resorbable devices, oval- and ring-shaped devices, rod-shaped devices, punctum plugs, contact lenses and corneal shields...
January 15, 2018: Experimental Eye Research
https://www.readbyqxmd.com/read/29352964/c24-hydroxylated-stigmastane-derivatives-as-liver-x-receptor-agonists
#8
Francisco Fermin Castro Navas, Gianluca Giorgi, Daniela Maggioni, Manuela Pacciarini, Vincenzo Russo, Maura Marinozzi
Phytosterols are stucturally correlated to the endogenous ligands of Liver X Receptor (LXR), a ligand-activated nuclear receptor that has emerged as an attractive drug target due to its ability to integrate metabolic and inflammatory signaling. Natural and semi-synthetic phytosterol derivatives characterized by the presence of side-chain oxygenated functions have shown to be able to modulate LXR activity. Here, we describe the efficient synthesis of four stigmastane derivatives, endowed with a hydroxyl group at C24 position, namely (24R)- and (24S)-stigmasta-5,28-diene-3β,24-ols (also referred to as saringosterols, 10a and 10b) and (24R)- and (24S)-stigmasta-5-ene-3β,24-ols (11a and 11b), starting from the readily available stigmasterol...
January 15, 2018: Chemistry and Physics of Lipids
https://www.readbyqxmd.com/read/29352920/biomass-based-magnetic-fluorescent-nanoparticles-one-step-scalable-synthesis-application-as-drug-carriers-and-mechanism-study
#9
Lei Li, Feijun Wang, Ziqiang Shao
A biomass-based magnetic fluorescent nanoparticle (MFNPs) was successively in situ synthesized via a one-step high-gravity approach, which constructed by a magnetic core of Fe3O4 nanoparticles, the fluorescent marker of carbon dots (CDs), and shells of chitosan (CS). The obtained MFNPs had a 10 nm average diameter and narrow particle size distribution, low cytotoxicity, superior fluorescent emission and superparamagnetic properties. The encapsulating and release 5-fluorouracil experiments confirmed that the introduction of CS/CDs effectively improved the drug loading capacity...
March 15, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29352885/synthesis-of-stimuli-responsive-chitosan-based-hydrogels-by-diels-alder-cross-linking-click%C3%A2-reaction-as-potential-carriers-for-drug-administration
#10
O Guaresti, C García-Astrain, R H Aguirresarobe, A Eceiza, N Gabilondo
Stimuli-responsive chitosan-based hydrogels for biomedical applications using the Diels-Alder reaction were prepared. Furan modified chitosan (Cs-Fu) was cross-linked with polyetheramine derived bismaleimide at different equivalent ratios in order to determine the effect in the swelling and release properties on the final CsFu:BMI hydrogels. The Diels Alder cross-linking reaction was monitored by UV-vis spectroscopy and rheological measurements. Both the sol-gel transition value and the final storage modulus for the different formulations were similar and close to 40 min and 400 Pa, respectively...
March 1, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29352755/a-mos1-transposase-in-vivo-assay-to-screen-new-hiv-1-integrase-inhibitors
#11
Mariana Cancian, Elgion L S Loreto
The integrase and transposase enzymes of retrovirus and transposons, respectively, share the catalytic DDE domain. In vitro assays showed that inhibitors of HIV-1 integrase generally inhibit the mariner Mos1 transposase. Using a Drosophila strain in which the mobilisation of the mariner element can be quantified by mosaic eyes, we showed that flies maintained in medium containing 210 µM to 4 mM of raltegravir, or 1 or 2 mM of dolutegravir, which are HIV-1 integrase inhibitor used in AIDS treatment, have 23-33% less somatic mobilisation in mosaic eyes when treated with raltegravir and 28-32% when treated with dolutegravir...
January 19, 2018: Genetica
https://www.readbyqxmd.com/read/29352734/resistance-to-tyrosine-kinase-inhibitors-in-non-small-cell-lung-cancer-the-role-of-cancer-stem-cells
#12
REVIEW
Marzia Del Re, Elena Arrigoni, Giuliana Restante, Antonio Passaro, Eleonora Rofi, Stefania Crucitta, Filippo De Marinis, Antonello Di Paolo, Romano Danesi
Among the potential mechanisms involved in resistance to tyrosine kinase inhibitors (TKIs) in non-small cell lung cancer (NSCLC), the manifestation of stem-like properties in cancer cells seems to have a crucial role. Alterations involved in the development of TKI resistance may be acquired in a very early phase of tumorigenesis, supporting the hypothesis that these aberrations may be present in cancer stem cells (CSCs). In this regard, the characterization of tumor subclones in the initial phase and the identification of the CSCs may be helpful in planning a specific treatment to target selected biomarkers, suppress tumor growth, and prevent drug resistance...
January 20, 2018: Stem Cells
https://www.readbyqxmd.com/read/29352597/potential-drug-targets-in-the-mycobacterium-tuberculosis-cytochrome-p450-system
#13
REVIEW
Paul R Ortiz de Montellano
The Mycobacterium tuberculosis genome encodes twenty cytochrome P450 enzymes, most or all of which appear to have specific physiological functions rather than being devoted to the removal of xenobiotics. However, in many cases their specific functions remain obscure. Considerable spectroscopic, biophysical, crystallographic, and catalytic information is available on nine of these cytochrome P450 enzymes, although gaps exist in our knowledge of even these enzymes. The available evidence indicates that at least three of the better-characterized enzymes are promising targets for antituberculosis drug discovery...
January 12, 2018: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/29352515/principles-of-alemtuzumab-immunoablation-in-hematopoietic-cell-transplantation-for-non-malignant-diseases-in-children-a-review
#14
REVIEW
Gregory M T Guilcher, Ravi Shah, Shalini Shenoy
Alemtuzumab is a humanized mAb targeted to CD52. Alemtuzumab is highly immunosuppressive with the ability to deplete T and B cells (in addition to other immune cell lines). A growing understanding of the PKs, dosing, and timing of administration of alemtuzumab has allowed for the study of its use as a conditioning agent for allogeneic HCT. The highly immunosuppressive properties of the drug are particularly appealing in the setting of non-malignant HCT, where GVHD provides no clinical benefit and relapse of malignancy is not applicable...
January 19, 2018: Pediatric Transplantation
https://www.readbyqxmd.com/read/29352512/trpv1-antagonists-that-cause-hypothermia-instead-of-hyperthermia-in-rodents-compounds-pharmacological-profiles-in-vivo-targets-thermoeffectors-recruited-and-implications-for-drug-development
#15
Andras Garami, Eszter Pakai, Heath A McDonald, Regina M Reilly, Arthur Gomtsyan, Joshua J Corrigan, Erika Pinter, Dawn X D Zhu, Sonya G Lehto, Narender R Gavva, Philip R Kym, Andrej A Romanovsky
AIM: Thermoregulatory side effects hinder the development of transient receptor potential vanilloid-1 (TRPV1) antagonists as new painkillers. While many antagonists cause hyperthermia, a well-studied effect, some cause hypothermia. The mechanisms of this hypothermia are unknown and were studied herein. METHODS: Two hypothermia-inducing TRPV1 antagonists, the newly synthesized A-1165901 and the known AMG7905, were used in physiological experiments in rats and mice...
January 20, 2018: Acta Physiologica
https://www.readbyqxmd.com/read/29352409/recent-perspectives-on-the-molecular-basis-of-biofilm-formation-by-pseudomonas-aeruginosa-and-approaches-for-treatment-and-biofilm-dispersal
#16
REVIEW
Sinosh Skariyachan, Vaishnavi Sneha Sridhar, Swathi Packirisamy, Supreetha Toplar Kumargowda, Sneha Basavaraj Challapilli
Pseudomonas aeruginosa, a Gram-negative, rod-shaped bacterium causes widespread diseases in humans. This bacterium is frequently related to nosocomial infections such as pneumonia, urinary tract infections (UTIs) and bacteriaemia especially in immunocompromised patients. The current review focuses on the recent perspectives on biofilms formation by these bacteria. Biofilms are communities of microorganisms in which cells stick to each other and often adhere to a surface. These adherent cells are usually embedded within a self-produced matrix of extracellular polymeric substance (EPS)...
January 19, 2018: Folia Microbiologica
https://www.readbyqxmd.com/read/29352320/high-level-production-and-purification-in-a-functional-state-of-an-extrasynaptic-gamma-aminobutyric-acid-type-a-receptor-containing-%C3%AE-4%C3%AE-3%C3%AE-subunits
#17
Xiaojuan Zhou, Rooma Desai, Yinghui Zhang, Wojciech J Stec, Keith W Miller, Youssef Jounaidi
The inhibitory γ-aminobutyric acid type A receptors are implicated in numerous physiological processes, including cognition and inhibition of neurotransmission, rendering them important molecular targets for many classes of drugs. Functionally, the entire GABAAR family of receptors can be subdivided into phasic, fast acting synaptic receptors, composed of α-, β- and γ-subunits, and tonic extrasynaptic receptors, many of which contain the δ-subunit in addition to α- and β-subunits. Whereas the subunit arrangement of the former group is agreed upon, that of the αβδ GABAARs remains unresolved by electrophysiological and pharmacological research...
2018: PloS One
https://www.readbyqxmd.com/read/29352318/temozolomide-induced-increase-of-tumorigenicity-can-be-diminished-by-targeting-of-mitochondria-in-in-vitro-models-of-patient-individual-glioblastoma
#18
Doreen William, Madlin Walther, Björn Schneider, Michael Linnebacher, Carl Friedrich Classen
Glioblastoma multiforme (GBM) is a highly heterogeneous and aggressive brain tumor with a dismal prognosis. Development of resistance towards cytostatic drugs like the GBM standard drug temozolomide is a severe problem in GBM treatment. One potential source of GBM relapse could be so called cancer stem like cells (CSCs). These represent an undifferentiated subpopulation of cells with high potential for tumor initiation. Furthermore, it has been shown that differentiated GBM cells can regain CSC properties when exposed to continuous temozolomide treatment in vitro...
2018: PloS One
https://www.readbyqxmd.com/read/29352187/reduction-in-hepatic-secondary-bile-acids-caused-by-short-term-antibiotic-induced-dysbiosis-decreases-mouse-serum-glucose-and-triglyceride-levels
#19
Takuya Kuno, Mio Hirayama-Kurogi, Shingo Ito, Sumio Ohtsuki
Antibiotic-caused changes in intestinal flora (dysbiosis) can have various effects on the host. Secondary bile acids produced by intestinal bacteria are ligands for specific nuclear receptors, which regulate glucose, lipid, and drug metabolism in the liver. The present study aimed to clarify the effect of changes in secondary bile acids caused by antibiotic-induced dysbiosis on the host physiology, especially glucose, lipid, and drug metabolism. After oral administration of non-absorbable antibiotics for 5 days, decreased amounts of secondary bile acid-producing bacteria in faeces and a reduction in secondary bile acid [lithocholic acid (LCA) and deoxycholic acid (DCA)] levels in the liver were observed...
January 19, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29352121/efficient-differentiation-of-human-pluripotent-stem-cells-into-skeletal-muscle-cells-by-combining-rna-based-myod1-expression-and-pou5f1-silencing
#20
Tomohiko Akiyama, Saeko Sato, Nana Chikazawa-Nohtomi, Atsumi Soma, Hiromi Kimura, Shunichi Wakabayashi, Shigeru B H Ko, Minoru S H Ko
Direct generation of skeletal muscle cells from human pluripotent stem cells (hPSCs) would be beneficial for drug testing, drug discovery, and disease modelling in vitro. Here we show a rapid and robust method to induce myogenic differentiation of hPSCs by introducing mRNA encoding MYOD1 together with siRNA-mediated knockdown of POU5F1 (also known as OCT4 or OCT3/4). This integration-free approach generates functional skeletal myotubes with sarcomere-like structure and a fusion capacity in several days. The POU5F1 silencing facilitates MYOD1 recruitment to the target promoters, which results in the significant activation of myogenic genes in hPSCs...
January 19, 2018: Scientific Reports
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