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https://www.readbyqxmd.com/read/28239924/cannabinoids-as-gastrointestinal-anti-inflammatory-drugs
#1
REVIEW
A Fabisiak, J Fichna
In this mini-review, we focus on the potential of the endocannabinoid system as a target for novel therapies to treat gastrointestinal (GI) inflammation. We discuss the organization of the endocannabinoid signaling and present possible pharmacological sites in the endocannabinoid system. We also refer to recent clinical findings in the field. Finally, we point at the potential use of cannabinoids at low, non-psychoactive doses to counteract non-inflammatory pathological events in the GI tract, like chemotherapy-induced diarrhea, as evidenced by Abalo et al...
March 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28239766/up-regulation-of-gbp2-is-associated-with-neuronal-apoptosis-in-rat-brain-cortex-following-traumatic-brain-injury
#2
Qi Miao, Meihong Ge, Lili Huang
Guanylate binding protein 2 (GBP2) is one member of GBP family. Recently, GBP2 has been proposed to be a novel target of anti-cancer drugs. However, the role of GBP2 in the traumatic brain injury (TBI) is very limited. In this study, we sought to define GBP2's role in brain injury. GBP2 protein levels were significantly increased in the brain 3 days after injury, suggesting a functional role for GBP2 in TBI. Neuronal cells overexpressing GBP2 exhibited up-regulation of co-location of GBP2 and NeuN following TBI, suggesting that GBP2 potentiates the neuron apoptosis...
February 27, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28239160/insights-into-the-molecular-mechanisms-of-polygonum-multiflorum-thunb-induced-liver-injury-a-computational-systems-toxicology-approach
#3
Yin-Yin Wang, Jie Li, Zeng-Rui Wu, Bo Zhang, Hong-Bin Yang, Qin Wang, Ying-Chun Cai, Gui-Xia Liu, Wei-Hua Li, Yun Tang
An increasing number of cases of herb-induced liver injury (HILI) have been reported, presenting new clinical challenges. In this study, taking Polygonum multiflorum Thunb (PmT) as an example, we proposed a computational systems toxicology approach to explore the molecular mechanisms of HILI. First, the chemical components of PmT were extracted from 3 main TCM databases as well as the literature related to natural products. Then, the known targets were collected through data integration, and the potential compound-target interactions (CTIs) were predicted using our substructure-drug-target network-based inference (SDTNBI) method...
February 27, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28238947/identification-of-novel-mrp3-inhibitors-based-on-computational-models-and-validation-using-an-in-vitro-membrane-vesicle-assay
#4
Izna Ali, Matthew A Welch, Yang Lu, Peter W Swaan, Kim L R Brouwer
INTRODUCTION: Multidrug resistance-associated protein 3 (MRP3), an efflux transporter on the hepatic basolateral membrane, may function as a compensatory mechanism to prevent the accumulation of anionic substrates (e.g., bile acids) in hepatocytes. Inhibition of MRP3 may disrupt bile acid homeostasis and is one hypothesized risk factor for the development of drug-induced liver injury (DILI). Therefore, identifying potential MRP3 inhibitors could help mitigate the occurrence of DILI. METHODS: Bayesian models were developed using MRP3 transporter inhibition data for 86 structurally diverse drugs...
February 23, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28238916/antiresorptive-and-anti-angiogenetic-octacalcium-phosphate-functionalized-with-bisphosphonates-an-in-vitro-tri-culture-study
#5
Lucia Forte, Paola Torricelli, Elisa Boanini, Massimo Gazzano, Milena Fini, Adriana Bigi
: Development of new materials for the local administration of bisphosphonates (BPs) is aimed to avoid the negative side effects of prolonged systemic use of these potent drugs. In this work, we synthesized octacalcium phosphate (OCP) in the presence of two potent BPs and obtained a single crystalline phase up to a zoledronate and alendronate content of 3.5 wt% and 5.2 wt%, respectively. Both BPs provoke minor structural modifications and a reduction of the crystal dimensions of OCP, which suggests a preferential interaction of the BPs with the structure of the calcium phosphate...
February 23, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28238876/ar-12-suppresses-dengue-virus-replication-by-down-regulation-of-pi3k-akt-and-grp78
#6
Hsin-Hsin Chen, Chien-Chin Chen, Yee-Shin Lin, Chiou-Feng Lin, Chia-Ling Chen, Chih-Peng Chang
Dengue virus (DENV) infection has become a public health issue of worldwide concern and is a serious health problem in Taiwan, yet there are no approved effective antiviral drugs to treat DENV. The replication of DENV requires both viral and cellular factors. Owing to the rapid mutation rate of viral factors, targeting host factors may serve as a more promising antiviral strategy. It has been known that up-regulation of PI3K/AKT signaling and GRP78 by DENV infection supports its replication. AR-12, a phase I trial completed anticancer drug, shows potent inhibitory activities on both PI3K/AKT signaling and GRP78 expression levels, and recently has been found to block the replication of several hemorrhagic fever viruses...
February 23, 2017: Antiviral Research
https://www.readbyqxmd.com/read/28238865/an-australian-nationwide-survey-on-medicinal-cannabis-use-for-epilepsy-history-of-antiepileptic-drug-treatment-predicts-medicinal-cannabis-use
#7
Anastasia S Suraev, Lisa Todd, Michael T Bowen, David J Allsop, Iain S McGregor, Carol Ireland, Nicholas Lintzeris
Epilepsy Action Australia conducted an Australian nationwide online survey seeking opinions on and experiences with the use of cannabis-based products for the treatment of epilepsy. The survey was promoted via the Epilepsy Action Australia's main website, on their Facebook page, and by word of mouth. The survey consisted of 39 questions assessing demographics, clinical factors, including diagnosis and seizure types, and experiences with and opinions towards cannabis use in epilepsy. A total of 976 responses met the inclusion criteria...
February 23, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28238742/molecular-signatures-order-the-potency-of-topically-applied-anti-inflammatory-drugs-in-atopic-dermatitis-patients
#8
Emma Guttman-Yassky, Benjamin Ungar, Kunal Malik, Daniel Dickstein, Maria Suprun, Yeriel D Estrada, Hui Xu, Xiangyu Peng, Margeaux Oliva, Dan Todd, Tord Labuda, Mayte Suarez-Farinas, Robert Bissonnette
BACKGROUND: Atopic Dermatitis (AD) presents a large unmet need for treatments with better safety and efficacy. To facilitate development of topical therapeutics, we need an efficient model for assessing different formulations and concentrations. The "plaque model" has been successfully implemented in psoriasis, another common inflammatory disease, to assess efficacy of topical treatments. This model has not been validated for AD, which has higher placebo responses and less stable lesions than psoriasis...
February 23, 2017: Journal of Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/28238718/towards-therapeutic-advances-in-melanoma-management-an-overview
#9
REVIEW
Swarnendra Singh, Atif Zafar, Saman Khan, Imrana Naseem
Melanoma is one of the most aggressive types of skin cancer with rapidly increasing incidence rate. The disease is largely considered incurable and the patients diagnosed with metastatic melanoma have a survival of not more than five years. Despite of the recent advances in anti-melanoma chemo- and immunotherapies, the available drugs are relatively toxic and responsive to only a limited subset of lesions. Currently, topical pharmacotherapy is demonstrated as an effective approach for the treatment of various skin cancers...
February 23, 2017: Life Sciences
https://www.readbyqxmd.com/read/28238511/comparison-of-the-anion-inhibition-profiles-of-the-%C3%AE-and-%C3%AE-carbonic-anhydrases-from-the-pathogenic-bacterium-burkholderia-pseudomallei
#10
Sonia Del Prete, Daniela Vullo, Pietro di Fonzo, Vincenzo Carginale, Claudiu T Supuran, Clemente Capasso
We report the cloning, purification and characterization of BpsβCA, a β-class carbonic anhydrase (CA, EC 4.2.1.1) from the pathogenic bacterium Burkholderia pseudomallei, the etiological agent of melioidosis, and compare its activity and inhibition with those of the γ-CA from the same organism, BpsγCA, recently investigated by our groups. BpsβCA showed a significant catalytic activity for the physiologic, CO2 hydration reaction, with the following kinetic parameters, kcat of 1.6×10(5)s(-1) and kcat/Km of 3...
February 16, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28238268/aryl-alkyl-lysines-membrane-active-fungicides-that-act-against-biofilms-of-candida-albicans
#11
Chandradhish Ghosh, Vikas Yadav, Waleed Younis, Haroon Mohammad, Youssef A Hegazy, Mohamed N Seleem, Kaustuv Sanyal, Jayanta Haldar
Mortality due to pathogenic fungi has been exacerbated by the rapid development of resistance to frontline antifungal drugs. Fungicidal compounds with novel mechanisms of action are urgently needed. Aryl-alkyl-lysines, which are membrane-active small molecules, were earlier shown to be broad-spectrum antibacterial agents with potency in vitro and in vivo. Herein, we report the antifungal properties of aryl-alkyl-lysines. After identifying the most active compound (NCK-10), we tested its activity against a panel of clinically relevant pathogenic fungi and examined NCK-10's effect against immature and mature biofilms of Candida albicans...
February 27, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28238095/adp-ribosylation-factor-1-arf1-takes-part-in-cell-proliferation-and-cell-adhesion-mediated-drug-resistance-cam-dr
#12
Xiaohong Xu, Qiru Wang, Yunhua He, Linlin Ding, Fei Zhong, Yangyu Ou, Yaodong Shen, Hong Liu, Song He
Cell adhesion-mediated drug resistance (CAM-DR) remains the primary obstacle in human multiple myeloma (MM) therapy. In this study, we aimed at investigating the expression and biologic function of ARF1 in MM. We determined that ARF1 expression was positively correlated with cell proliferation and knockdown of ARF1 contributed to CAM-DR. The enhancement in the adhesion of MM cells to fibronectin (FN) or the bone marrow stroma cell line HS-5 cells translated to an increased CAM-DR phenotype. Importantly, we showed that this CAM-DR phenotype was correlated with the phosphorylation of Akt and ERK in MM cells...
February 25, 2017: Annals of Hematology
https://www.readbyqxmd.com/read/28238078/phase-i-study-of-pazopanib-plus-th-302-in-advanced-solid-tumors
#13
Richard F Riedel, Kellen L Meadows, Paula H Lee, Michael A Morse, Hope E Uronis, Gerard C Blobe, Daniel J George, Jeffrey Crawford, Donna Niedzwiecki, Christel N Rushing, Christy C Arrowood, Herbert I Hurwitz
PURPOSE: To define the maximum tolerated dose (MTD), recommended phase II dose (RPTD), and assess safety and tolerability for the combination of pazopanib plus TH-302, an investigational hypoxia-activated prodrug (HAP), in adult patients with advanced solid tumors. METHODS: This was an open-label, non-randomized, single-center, phase I trial consisting 2 stages. Stage 1 was a standard "3 + 3" dose escalation design to determine safety and the RPTD for TH-302 plus pazopanib combination...
February 25, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28238060/novel-biotechnology-approaches-in-colorectal-cancer-diagnosis-and-therapy
#14
REVIEW
Soudabeh Kavousipour, Fathemeh Khademi, Mozhdeh Zamani, Bahareh Vakili, Pooneh Mokarram
With ever-increasing molecular information about colorectal cancer (CRC), there is an expectation to detect more sensitive and specific molecular markers for new advanced diagnostic methods that can surpass the limitations of current screening tests. Moreover, enhanced molecular pathology knowledge about cancer has led to the development of targeted therapies, designed to interfere with specific aberrant biological pathways in cancer. Furthermore, biotechnology has opened a new window in CRC diagnosis and treatment by introducing different application of antibodies, antibody fragments, non-Ig scaffold proteins, and aptamers in targeted therapy and drug delivery...
February 25, 2017: Biotechnology Letters
https://www.readbyqxmd.com/read/28238039/new-target-sites-for-treatment-of-osteoporosis
#15
Werner E G Müller, Xiaohong Wang, Heinz C Schröder
In the last few years, much progress has been achieved in the discovery of new drug target sites for treatment of osteoporotic disorders, one of the main challenging diseases with a large burden for the public health systems. Among these new agents promoting bone formation, shifting the impaired equilibrium between bone anabolism and bone catabolism in the direction of bone synthesis are inorganic polymers, in particular inorganic polyphosphates that show strong stimulatory effects on the expression of bone anabolic marker proteins and hydroxyapatite formation...
2017: Progress in Molecular and Subcellular Biology
https://www.readbyqxmd.com/read/28238036/discovery-and-development-of-novel-drugs
#16
Vesna Erakovic Haber, Radan Spaventi
Drug discovery and development process is nowadays conducted in relatively standardised sequence of phases, starting with Discovery and being followed by Preclinical, Clinical and Non-Clinical Development. Discovery phase is divided in Hit Finding, Lead generation, Lead Optimisation and Candidate Identification Phase. Main drivers of the whole process are regulatory requirements and the aim to eliminate the unnecessary spending by early elimination of unlikely drug candidates. Marine products, once purified, isolated and produced in required quantities, follow the same route as any other synthetic drug...
2017: Progress in Molecular and Subcellular Biology
https://www.readbyqxmd.com/read/28237943/kinome-profiling-identifies-druggable-targets-for-novel-hcmv-antivirals
#17
Kyle C Arend, Erik M Lenarcic, Heather A Vincent, Naim Rashid, Eric Lazear, Ian M MacDonald, Thomas S K Gilbert, Michael P East, Laura E Herring, Gary L Johnson, Lee Graves, Nathaniel J Moorman
Human cytomegalovirus (HCMV) is a significant cause of disease in immunecompromised adults and immune naive newborns. No vaccine exists to prevent HCMV infection, and current antiviral therapies have toxic side effects that limit the duration and intensity of their use. There is thus an urgent need for new strategies to treat HCMV infection. Repurposing existing drugs as antivirals is an attractive approach to limit the time and cost of new antiviral drug development. Virus-induced changes in infected cells are often driven by changes in cellular kinase activity, which led us to hypothesize that defining the complement of kinases (the kinome), whose abundance or expression is altered during infection would identify existing kinase inhibitors that could be repurposed as new antivirals...
February 25, 2017: Molecular & Cellular Proteomics: MCP
https://www.readbyqxmd.com/read/28237900/synthesis-of-novel-monomeric-graphene-quantum-dots-and-corresponding-nanocomposite-with-molecularly-imprinted-polymer-for-electrochemical-detection-of-an-anticancerous-ifosfamide-drug
#18
Bhim Bali Prasad, Anil Kumar, Ragini Singh
This paper reports a typical synthesis of a nanocomposite of functionalized graphene quantum dots and imprinted polymer at the surface of screen-printed carbon electrode using N-acryloyl-4-aminobenzamide, as a functional monomer, and an anticancerous drug, ifosfamide, as a print molecule (test analyte). Herein, graphene quantum dots in nanocomposite practically induced the electrocatalytic activity by lowering the oxidation overpotential of test analyte and thereby amplifying electronic transmission, without any interfacial barrier in between the film and the electrode surface...
February 20, 2017: Biosensors & Bioelectronics
https://www.readbyqxmd.com/read/28237794/combination-of-amino-acid-dipeptide-with-ligustrazine-betulinic-acid-as-antitumor-agents
#19
Bing Xu, Wen-Qiang Yan, Xin Xu, Gao-Rong Wu, Chen-Ze Zhang, Yao-Tian Han, Fu-Hao Chu, Rui Zhao, Peng-Long Wang, Hai-Min Lei
The lead compound TBA, 3β-Hydroxy-lup-20(29)-ene-28-oic acid-3, 5, 6-trimethylpyrazin-2-methyl ester, which exhibited promising antitumor activity and induced tumor cell apoptosis in various cancer cell lines, had previously been reported. Moreover, reports have revealed that the introduction of amino acid to betulinic acid could improve selective cytotoxicity as well as water solubility. Thus, a series of novel TBA amino acid and dipeptide derivatives were designed, synthesized and screened for selective cytotoxic activity against five cancer cell lines (HepG2, HT-29, Hela, BCG-823 and A549) and the not malignant cell line MDCK by standard MTT assay...
February 17, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28237749/redox-sensitive-self-assembled-nanoparticles-based-on-alpha-tocopherol-succinate-modified-heparin-for-intracellular-delivery-of-paclitaxel
#20
Xiaoye Yang, Xiaoqing Cai, Aihua Yu, Yanwei Xi, Guangxi Zhai
To remedy the problems riddled in cancer chemotherapy, such as poor solubility, low selectivity, and insufficient intra-cellular release of drugs, novel heparin-based redox-sensitive polymeric nanoparticles were developed. The amphiphilic polymer, heparin-alpha-tocopherol succinate (Hep-cys-TOS) was synthesized by grafting hydrophobic TOS to heparin using cystamine as the redox-sensitive linker, which could self-assemble into nanoparticles in phosphate buffer saline (PBS) with low critical aggregation concentration (CAC) values ranging from 0...
February 16, 2017: Journal of Colloid and Interface Science
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