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https://read.qxmd.com/read/30878891/design-synthesis-and-dna-interaction-studies-of-furo-imidazo-3-3-3-propellane-derivatives-potential-anticancer-agents
#1
Alaa A Hassan, Ashraf A Aly, Nasr K Mohamed, Kamal M El Shaieb, Maysa M Makhlouf, El-Shimaa M N Abdelhafez, Stefan Bräse, Martin Nieger, Kevin N Dalby, Tamer S Kaoud
A large number of natural products containing the propellane scaffold have been reported to exhibit cytotoxicity against several cancers; however, their mechanism of action is still unknown. Anticancer drugs targeting DNA are mainly composed of small planar molecule/s that can interact with the DNA helix, causing DNA malfunction and cell death. The aim of this study was to design and synthesize propellane derivatives that can act as DNA intercalators and/or groove binders. The unique structure of the propellane derivatives and their ability to display planar ligands with numerous possible geometries, renders them potential starting points to design new drugs targeting DNA in cancer cells...
February 13, 2019: Bioorganic Chemistry
https://read.qxmd.com/read/30878874/the-in-vitro-and-in-vivo-anti-inflammatory-effect-of-osthole-the-major-natural-coumarin-from-cnidium-monnieri-l-cuss-via-the-blocking-of-the-activation-of-the-nf-%C3%AE%C2%BAb-and-mapk-p38-pathways
#2
Huaying Fan, Zhenfang Gao, Kai Ji, Xin Li, Jingbao Wu, Yue Liu, Xuekai Wang, Haiyue Liang, Yanan Liu, Xiaoting Li, Pan Liu, Daquan Chen, Feng Zhao
BACKGROUND: Ulcerative colitis (UC) is a chronic inflammatory condition of the intestines and is difficult to cure once diagnosed. The efficacy of the current clinical treatment for UC is limited. Common anti-inflammatory drugs are prone to adverse effects, while novel biological agents are expensive, although tolerated by patients. Therefore, an urgency exists to find more safe and effective drugs to treat UC. Osthole is an active constituent isolated from the fruit of Cnidium monnieri (L...
February 18, 2019: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://read.qxmd.com/read/30878827/evaluation-of-synthetic-substituted-1-2-dioxanes-as-novel-agents-against-human-leishmaniasis
#3
M Ortalli, S Varani, C Rosso, A Quintavalla, M Lombardo, C Trombini
The treatment of human leishmaniasis is currently based on few compounds that are highly toxic, expensive and have a high rate of treatment failure. A number of recent studies on new drugs focuses on natural or semi-synthetic compounds. Among them, the endoperoxide artemisinin, extracted from Artemisia annua, and some of its derivatives have shown leishmanicidal activity. In the present work, a series of structurally simple, fully synthetic 1,2-dioxanes were evaluated for in vitro antileishmanial activity against promastigotes of Leishmania donovani; the cytotoxicity for mammalian cells was also assessed...
March 3, 2019: European Journal of Medicinal Chemistry
https://read.qxmd.com/read/30878561/therapy-for-glioblastoma-is-it-working
#4
REVIEW
Edward D Zanders, Fredrik Svensson, David S Bailey
Glioblastoma (GBM) remains one of the most intransigent of cancers, with a median overall survival of only 15 months after diagnosis. Drug treatments have largely proven ineffective; it is thought that this is related to the heterogeneous nature and plasticity of GBM-initiating stem cell lineages. Although many combination drug therapies are being positioned to address tumour heterogeneity, the most promising therapeutic approaches for GBM to date appear to be those targeting GBM by vaccination or antibody- and cell-based immunotherapy...
March 13, 2019: Drug Discovery Today
https://read.qxmd.com/read/30878464/a-retrospective-analysis-of-data-from-forensic-toxicology-at-the-academy-of-forensic-science-in-2017
#5
Meiru Pan, Xin Wang, Yunli Zhao, Wei Liu, Ping Xiang
Knowing the specific pattern of forensic toxicology cases in a region is vital to help the local government establish an effective prevention and treatment system; currently, there have been no published reports investigating various types of forensic toxicology cases based on a large autopsy series and city size. The data in this study were obtained from records kept at the Academy of Forensic Science (AFS) between February 2017 and December 2017, and the cases were mainly from the Public Security Organs People's Police in Shanghai, China...
February 28, 2019: Forensic Science International
https://read.qxmd.com/read/30878091/flow-cytometry-evaluation-of-in-vitro-susceptibility-of-bovine-isolates-of-tritrichomonas-foetus-to-metronidazole
#6
María Belén Rivero, Melchor Emilio Luque, Maria Eugenia Abdala, Bruno Elías Luna, David Di Lullo, Pedro Gabriel Carranza, Fernando David Rivero
Bovine Trichomonosis, an endemic sexually transmitted disease in countries with extensive livestock and natural service, represents one of the most common causes of reproductive failure. 5-nitroimidazoles and their derivatives are used for its treatment, mainly metronidazole (Mz). The emergence of resistance mechanisms adopted by the parasites against the drug and failure of the treatments suggest the need to investigate susceptibility and obtain current values. The available information of in vitro susceptibility of these drugs comes from the use of a diversity of methodologies and criteria, especially observation of the mobility of the parasite under the optical microscope to evaluate its viability...
March 2019: Veterinary Parasitology
https://read.qxmd.com/read/30877973/therapeutic-potentials-of-plant-iridoids-in-alzheimer-s-and-parkinson-s-diseases-a-review
#7
REVIEW
Biswanath Dinda, Manikarna Dinda, Goutam Kulsi, Ankita Chakraborty, Subhajit Dinda
Alzheimer's disease (AD) and Parkinson's disease (PD) are the most common age-related neurodegenerative disorders, affecting several millions of aged people globally. Among these disorders, AD is more severe, affecting about 7% of individuals aged 65 and above. AD is primarily a dementia-related disorder from progressive cognitive deterioration and memory impairment, while PD is primarily a movement disorder illness having three major kinesia or movement disorder symptoms, bradykinesia (slowness of movements), hypokinesia (reduction of movement amplitude), and akinesia (absence of normal unconscious movements) along with muscle rigidity and tremor at rest...
March 8, 2019: European Journal of Medicinal Chemistry
https://read.qxmd.com/read/30877807/changes-in-mortality-involving-extended-release-and-long-acting-opioids-after-implementation-of-a-risk-evaluation-and-mitigation-strategy
#8
Joshua C Black, Gabrielle E Bau, Travis Rosen, M Soledad Cepeda, Gregory P Wedin, Jody L Green, Richard C Dart
OBJECTIVE: To assess changes in mortality rates in extended-release and long-acting (ER/LA) opioid analgesics after the implementation of the Risk Evaluation and Mitigation Strategy (REMS). SETTING: All drug poisoning deaths in three states: Florida, Oregon, and Washington. Data were obtained through state vital records offices and the Researched Abuse, Diversion and Addiction-Related Surveillance System Medical Examiner Program. METHODS: Using cause-of-death literal text from death certificates, individual opioid active pharmaceutical ingredients (APIs) involved in each death were identified using rules-based natural language processing...
March 16, 2019: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://read.qxmd.com/read/30877722/magnetic-chrysin-silica-nanomaterials-behavior-in-an-amyloidogenic-environment
#9
Christiane N Nday, Despoina Eleftheriadou, Graham Jackson
Alzheimer's disease (AD) is a progressive neurodegenerative disorder associated with brain damage induced by β-amyloid and tau accumulation. One of the hallmarks of amyloidogenesis, is the aggregation of amyloid proteins into a specific cross-β sheet structure, which alters their biological activity thereby affecting neuronal connectivity and function. Despite significant progress in the management of AD over the recent years, the early diagnostic and treatment options still remain limited. Recently, great attention has been focused on the advancement of therapeutic strategies exploiting the antioxidant properties of naturally occurring compounds...
January 2019: Hellenic Journal of Nuclear Medicine
https://read.qxmd.com/read/30877721/naringin-nanoparticles-against-neurodegenerative-processes-a-preliminary-work
#10
Christiane N Nday, Despoina Eleftheriadou, Graham Jackson
It is well established that during Alzheimer disease (AD), gradual loss of neuronal networks occurs in the brain, consequently, affecting cognition and memory tasks of the patients. Among other causative factors, oxidative stress induces changes that are eventually accompanied by an irreversible disruption of synaptic connectivity and death of neurons. Moreover, aging and oxidative stress cause alterations to the blood brain barrier, leading to increased permeability, which are thought to further aggravate the underlying pathology...
January 2019: Hellenic Journal of Nuclear Medicine
https://read.qxmd.com/read/30877660/effect-of-pterostilbene-a-natural-analog-of-resveratrol-on-the-activity-of-some-antiepileptic-drugs-in-the-acute-seizure-tests-in-mice
#11
Dorota Nieoczym, Katarzyna Socała, Piotr Jedziniak, Elżbieta Wyska, Piotr Wlaź
Pterostilbene (PTE), a natural analog of resveratrol, is available both as a diet ingredient and a dietary supplement. The present study was undertaken to assess the effect of PTE on the activity of antiepileptic drugs in the acute seizure tests in mice, i.e., the intravenous pentetrazole (iv PTZ) seizure threshold, maximal electroshock (MES), and 6 Hz-induced psychomotor seizure tests. Our study revealed that PTE enhanced the anticonvulsant effect of clonazepam but did not change the activity of tiagabine in the iv PTZ test...
March 15, 2019: Neurotoxicity Research
https://read.qxmd.com/read/30876845/machine-learning-on-adverse-drug-reactions-for-pharmacovigilance
#12
REVIEW
Chun Y Lee, Yi-Ping P Chen
Adverse drug reactions are an unresolved issue that can result in mortality, morbidity and substantial healthcare costs. Many conventional machine learning methods have been used for predicting post-marketing drug side-effects. However, owing to the complex chemical structures of certain drugs and the nonlinear and imbalanced nature of biological data, some side-effects might not be detected. Motivated by the drug discovery research studies that have shown that deep learning outperformed machine learning methods over prediction tasks, we proposed: (i) to exploit the unsupervised deep learning approaches to predict ADRs; (ii) to use a two-stage framework to predict personalized ADRs and repurpose the drugs...
March 12, 2019: Drug Discovery Today
https://read.qxmd.com/read/30875948/functional-magnetic-core-shell-system-based-iron-oxide-nanoparticle-coated-with-biocompatible-copolymer-for-anticancer-drug-delivery
#13
Thai Thanh Hoang Thi, Diem-Huong Nguyen Tran, Long Giang Bach, Hieu Vu-Quang, Duy Chinh Nguyen, Ki Dong Park, Dai Hai Nguyen
Polymer coating has drawn increasing attention as a leading strategy to overcome the drawbacks of superparamagnetic iron oxide nanoparticles (SPIONs) in targeted delivery of anticancer drugs. In this study, SPIONs were modified with heparin-Poloxamer (HP) shell to form a SPION@HP core-shell system for anticancer drug delivery. The obtained formulation was characterized by techniques including transmission electron microscopy (TEM), Fourier transform infrared spectra (FT-IR), vibration sample magnetometer (VSM), proton nuclear magnetic resonance (¹H-NMR), and powder X-ray diffraction (XRD)...
March 15, 2019: Pharmaceutics
https://read.qxmd.com/read/30875934/polymeric-co-delivery-systems-in-cancer-treatment-an-overview-on-component-drugs-dosage-ratio-effect
#14
REVIEW
Jiayi Pan, Kobra Rostamizadeh, Nina Filipczak, Vladimir P Torchilin
Multiple factors are involved in the development of cancers and their effects on survival rate. Many are related to chemo-resistance of tumor cells. Thus, treatment with a single therapeutic agent is often inadequate for successful cancer therapy. Ideally, combination therapy inhibits tumor growth through multiple pathways by enhancing the performance of each individual therapy, often resulting in a synergistic effect. Polymeric nanoparticles prepared from block co-polymers have been a popular platform for co-delivery of combinations of drugs associated with the multiple functional compartments within such nanoparticles...
March 15, 2019: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://read.qxmd.com/read/30875913/microbial-transformation-of-flavonoids-by-isaria-fumosorosea-accc-37814
#15
Fangmin Dou, Zhi Wang, Guiying Li, Baoqing Dun
Glycosylation is an efficient strategy to modulate the solubility, stability, bioavailability and bioactivity of drug-like natural products. Biological methods, such as whole-cell biocatalyst, promise a simple but highly effective approach to glycosylate biologically active small molecules with remarkable regio- and stereo-selectivity. Herein, we use the entomopathogenic filamentous fungus Isaria fumosorosea ACCC 37814 to biotransform a panel of phenolic natural products, including flavonoids and anthraquinone, into their glycosides...
March 15, 2019: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://read.qxmd.com/read/30875859/hybrid-cis-stilbene-molecules-novel-anticancer-agents
#16
REVIEW
Natalia Piekuś-Słomka, Renata Mikstacka, Joanna Ronowicz, Stanisław Sobiak
The growing interest in anticancer hybrids in the last few years has resulted in a great number of reports on hybrid design, synthesis and bioevaluation. Many novel multi-target-directed drug candidates were synthesized, and their biological activities were evaluated. For the design of anticancer hybrid compounds, the molecules of stilbenes, aromatic quinones, and heterocycles (benzimidazole, imidazole, pyrimidine, pyridine, pyrazole, quinoline, quinazoline) were applied. A distinct group of hybrids comprises the molecules built with natural compounds: Resveratrol, curcumin, coumarin, and oleanolic acid...
March 14, 2019: International Journal of Molecular Sciences
https://read.qxmd.com/read/30875854/phenolic-compounds-from-humulus-lupulus-as-natural-antimicrobial-products-new-weapons-in-the-fight-against-methicillin-resistant-staphylococcus-aureus-leishmania-mexicana-and-trypanosoma-brucei-strains
#17
Laetitia Bocquet, Sevser Sahpaz, Natacha Bonneau, Claire Beaufay, Séverine Mahieux, Jennifer Samaillie, Vincent Roumy, Justine Jacquin, Simon Bordage, Thierry Hennebelle, Feng Chai, Joëlle Quetin-Leclercq, Christel Neut, Céline Rivière
New anti-infective agents are urgently needed to fight microbial resistance. Methicillin-resistant Staphylococcus aureus (MRSA) strains are particularly responsible for complicated pathologies that are difficult to treat due to their virulence and the formation of persistent biofilms forming a complex protecting shell. Parasitic infections caused by Trypanosoma brucei and Leishmania mexicana are also of global concern, because of the mortality due to the low number of safe and effective treatments. Female inflorescences of hop produce specialized metabolites known for their antimicrobial effects but underexploited to fight against drug-resistant microorganisms...
March 14, 2019: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://read.qxmd.com/read/30875817/a-molecular-docking-approach-to-evaluate-the-pharmacological-properties-of-natural-and-synthetic-treatment-candidates-for-use-against-hypertension
#18
Syed Awais Attique, Muhammad Hassan, Muhammad Usman, Rana Muhammad Atif, Shahid Mahboob, Khalid A Al-Ghanim, Muhammad Bilal, Muhammad Zohaib Nawaz
Cardiovascular diseases (CVDs) have become the leading cause of disability and death worldwide, particularly in low- and middle-income countries. Hypertension, a major cause of CVD progression, is widely attributable to genetic, behavioral, and environmental risk factors. Among the genetic reasons, angiotensin II enzyme, produced as a result of abnormal functioning of the renin⁻angiotensin system, is reported as the foremost cause of hypertension. A cascade of genes, including those encoding for WNK kinases (WNK1 and WNK4), Bp1, Bp2, angiotensinogen, and other enzymes, is involved in the conversion of angiotensin I to angiotensin II...
March 14, 2019: International Journal of Environmental Research and Public Health
https://read.qxmd.com/read/30875780/analysis-of-flavonoids-bioactivity-for-cholestatic-liver-disease-systematic-literature-search-and-experimental-approaches
#19
Juan Carlos Sánchez-Salgado, Samuel Estrada-Soto, Sara García-Jiménez, Sergio Montes, Jaime Gómez-Zamudio, Rafael Villalobos-Molina
Flavonoids are naturally occurring compounds that show health benefits on the liver. However, there is little investigation about identification and evaluation of new flavonoid-containing drugs for cholestatic liver disease, one of the most common liver illnesses. We aimed to a systematic search regarding efficacy of flavonoids for treatment of cholestatic liver disease, and then evaluate naringenin (NG) as representative flavonoid in an obstructive cholestasis model. We searched for information of experimental and clinical studies in four major databases without time and language limits...
March 14, 2019: Biomolecules
https://read.qxmd.com/read/30875748/enhanced-autophagy-contributes-to-reduced-viral-infection-in-black-flying-fox-cells
#20
Eric D Laing, Spencer L Sterling, Dawn L Weir, Chelsi R Beauregard, Ina L Smith, Sasha E Larsen, Lin-Fa Wang, Andrew L Snow, Brian C Schaefer, Christopher C Broder
Bats are increasingly implicated as hosts of highly pathogenic viruses. The underlying virus⁻host interactions and cellular mechanisms that promote co-existence remain ill-defined, but physiological traits such as flight and longevity are proposed to drive these adaptations. Autophagy is a cellular homeostatic process that regulates ageing, metabolism, and intrinsic immune defense. We quantified basal and stimulated autophagic responses in black flying fox cells, and demonstrated that although black flying fox cells are susceptible to Australian bat lyssavirus (ABLV) infection, viral replication is dampened in these bat cells...
March 14, 2019: Viruses
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