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https://www.readbyqxmd.com/read/29353335/leveraging-model-informed-approaches-for-drug-discovery-and-development-in-the-cardiovascular-space
#1
REVIEW
Marissa F Dockendorf, Ryan C Vargo, Ferdous Gheyas, Anne S Y Chain, Manash S Chatterjee, Larissa A Wenning
Cardiovascular disease remains a significant global health burden, and development of cardiovascular drugs in the current regulatory environment often demands large and expensive cardiovascular outcome trials. Thus, the use of quantitative pharmacometric approaches which can help enable early Go/No Go decision making, ensure appropriate dose selection, and increase the likelihood of successful clinical trials, have become increasingly important to help reduce the risk of failed cardiovascular outcomes studies...
January 20, 2018: Journal of Pharmacokinetics and Pharmacodynamics
https://www.readbyqxmd.com/read/29353300/empirical-validation-of-the-crafft-abuse-screening-test-in-a-spanish-sample
#2
Antonio Rial, Sion Kim-Harris, John R Knight, Manuel Araujo, Patricia Gómez, Teresa Braña, Jesús Varela, Sandra Golpe
The CRAFFT Substance Abuse Screening Instrument, developed by the Center for Adolescents Substance Abuse Research (CeASAR) (Knight et al., 1999), is a screening tool for high-risk alcohol and drug risk consumption designed for use with adolescents. Since its publication it has been the subject of translations and validations in different countries, populations and contexts that have demonstrated its enormous potential. However, there is still no empirical validation study that would ensure its good psychometric performance in Spain...
January 15, 2018: Adicciones
https://www.readbyqxmd.com/read/29353047/clinical-profile-of-nonresponders-to-surgical-myectomy-with-obstructive-hypertrophic-cardiomyopathy
#3
Sophie Wells, Ethan J Rowin, Griffin Boll, Hassan Rastegar, Wendy Wang, Martin S Maron, Barry J Maron
BACKGROUND: In the vast majority of patients with obstructive hypertrophic cardiomyopathy and drug-refractory heart failure, surgical myectomy results in reversal of heart failure symptoms. However, a small patient subgroup fails to experience sustained postoperative improvement despite relief of left ventricular outflow obstruction. Clinical profile of such patients has not been well defined. METHODS: Consecutive obstructive hypertrophic cardiomyopathy patients undergoing myectomy at Tufts Medical Center for drug refractory NYHA III/IV heart failure symptoms, 2004 to 2017, were followed postoperatively for 2...
January 15, 2018: American Journal of Medicine
https://www.readbyqxmd.com/read/29353042/ginkgolic-acid-induces-interplay-between-apoptosis-and-autophagy-regulated-by-ros-generation-in-colon-cancer
#4
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/29353039/cetylpyridinium-chloride-as-a-novel-inhibitor-of-hepatitis-b-viral-capsid-assembly
#5
Hyun Wook Seo, Joon Pyung Seo, Yoon Jun Kim, Guhung Jung
Hepatitis B virus (HBV) infection is a major risk factor for chronic liver disease, cirrhosis, and hepatocellular carcinoma (HCC) worldwide. While multiple hepatitis B drugs have been developed, development of drug resistance during treatment or weak efficacies observed in some cases have limited their application. Therefore, there is an urgent need to develop better pharmacological agents for HBV-infected individuals. Here, we identified cetylpyridinium chloride (CPC) as a novel inhibitor of HBV. Using computational analysis of CPC-nucleocapsid proteins, microscale thermophoresis analysis of CPC binding to viral nucleocapsids, and in vitro nucleocapsid formation assays, we found that CPC interacts with dimeric viral nucleocapsid protein (known as core protein or HBcAg)...
January 15, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29353017/ph-triggered-surface-charge-reversal-nanoparticles-alleviate-experimental-murine-colitis-via-selective-accumulation-in-inflamed-colon-regions
#6
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/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/29352991/molecular-monitoring-of-dihydrofolatereductase-dhfr-and-dihydropteroatesynthetase-dhps-associated-with-sulfadoxine-pyrimethamine-resistance-in-plasmodium-vivax-isolates-of-palawan-philippines
#8
Alison Paolo Bareng, Fe Esperanza Espino, Wanna Chaijaroenkul, Kesara Na-Bangchang
The emergence of drug-resistant Plasmodium vivax poses problems for malaria control and elimination in some parts of the world, especially in developing countries where individuals are routinely exposed to the infection. The aim of this study was to determine the single nucleotide polymorphisms (SNPs) in dihydropteroate synthase (pvdhps) and dihydrofolate reductase (pvdhfr) genes associated with sulfadoxine-pyrimethamine (SP) drug resistance among P. vivax isolates collected in Palawan, Philippines. Genetic polymorphisms of pvdhps and pvdhfr were analysed by nested PCR...
January 15, 2018: Acta Tropica
https://www.readbyqxmd.com/read/29352935/development-of-ph-responsive-chitosan-based-hydrogel-modified-with-bone-ash-for-controlled-release-of-amoxicillin
#9
Didem Aycan, Neslihan Alemdar
In present study, bone ash-reinforced chitosan-based hydrogels were obtained by encapsulation of bone ash into the hydrogel structure which was fabricated by photopolymerization of chitosan-grafted-glycidyl methacrylate (CTS-g-GMA) and poly(ethylene glycol)diacrylate (PEGDA) under the UV light. Hydrogels were characterized by ATR-FTIR, SEM and XRD analyses. Mechanical performance of the hydrogels was determined by universal mechanical tester. Cytotoxicity tests for hydrogels were conducted with L929 cell lines to determine cellular compatibility...
March 15, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29352934/%C3%AE-cyclodextrin-phenylacetic-acid-mesh-as-a-drug-trap
#10
Hyeong Sup Yu, Jae Min Lee, Yu Seok Youn, Kyung Taek Oh, Kun Na, Eun Seong Lee
In this study, we developed a nanoporous biodegradable mesh, bioinspired by the spider web, which is prepared via electrospinning using γ-cyclodextrin (γ-CD) conjugated with phenylacetic acid (PA), named γ-CDP. The resulting γ-CDP has a microfibrous or microspherical shape and contains drug trap meshlike γ-CD pores. These γ-CDP micromeshes (microspheres or microfibers) enable efficient drug capture and drug transport into deep γ-CDP nanocompartments or out of the γ-CDP web, resulting in a driving domain for a 4-week drug release...
March 15, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29352929/structural-characterization-antioxidant-and-hepatoprotective-activities-of-polysaccharides-from-sophorae-tonkinensis-radix
#11
Liangliang Cai, Shanshan Zou, Dengpan Liang, Libiao Luan
In current study we present two polysaccharides, STRP1 and STRP2, purified from Sophorae tonkinensis Radix via column chromatography. Structural analyses indicated that STRP1 and STRP2 were consisted of mannose, rhamnose, glucuronic acid, glucose, galactose and arabinose in a similar molar ratio with main backbones of (1 → 3)-linked-α-d-Gal and (1 → 4)-linked-α-d-Glc, while average molecular weights were 1.30 × 104 and 1.98 × 105 Da, respectively. We observed a strong chelating ability on ferrous ions; substantial radical scavenging activities on DPPH, hydroxyl and superoxide anion radicals in vitro; and significant attenuation on acetaminophen-induced hepatic oxidative damage in mice for STRP1 and STRP2...
March 15, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29352911/hpmcas-as-an-effective-precipitation-inhibitor-in-amorphous-solid-dispersions-of-the-poorly-soluble-drug-candesartan-cilexetil
#12
Juliana Munari Oliveira Pinto, Aline Franciane Leão, Manoela Klüppel Riekes, Maria Terezinha França, Hellen Karine Stulzer
Among the strategies to improve the biopharmaceutic properties of poorly soluble drugs, Supersaturating Drug Delivery Systems like polymer-based amorphous solid dispersions (SD) have been successfully applied. The screening of appropriate polymeric carriers to compose SD is a crucial point on their development. In this study, hydroxypropylmethylcellulose (HPMC), hydroxypropylmethylcellulose acetate succinate (HPMCAS) types L, M and H and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (SOL) were evaluated by in vitro supersaturation studies regarding their anti-precipitant ability on the poorly soluble drug candesartan cilexetil (CC) under two different media, including biorelevant conditions...
March 15, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29352895/sequencing-the-oligosaccharide-pool-in-the-low-molecular-weight-heparin-dalteparin-with-offline-hplc-and-esi-ms-ms
#13
Zhangjie Wang, Tianji Zhang, Shaoshuai Xie, Xinyue Liu, Hongmei Li, Robert J Linhardt, Lianli Chi
Low molecular weight heparins (LMWHs) are widely used anticoagulant drugs. The composition and sequence of LMWH oligosaccharides determine their safety and efficacy. The short oligosaccharide pool in LMWHs undergoes more depolymerization reactions than the longer chains and is the most sensitive indicator of the manufacturing process. Electrospray ionization tandem mass spectrometry (ESI-MS/MS) has been demonstrated as a powerful tool to sequence synthetic heparin oligosaccharide but never been applied to analyze complicated mixture like LMWHs...
March 1, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29352859/is-selective-5-ht1f-receptor-agonism-an-entity-apart-from-that-of-the-triptans-in-antimigraine-therapy
#14
REVIEW
Eloísa Rubio-Beltrán, Alejandro Labastida-Ramírez, Carlos M Villalón, Antoinette MaassenVanDenBrink
Migraine is a neurovascular disorder that involves activation of the trigeminovascular system and cranial vasodilation mediated by release of calcitonin gene-related peptide (CGRP). The gold standard for acute migraine treatment are the triptans, 5-HT1B/1D/(1F) receptor agonists. Their actions are thought to be mediated through activation of: (i) 5-HT1B receptors in cranial blood vessels with subsequent cranial vasoconstriction; (ii) prejunctional 5-HT1D receptors on trigeminal fibers that inhibit trigeminal CGRP release; and (iii) 5-HT1B/1D/1F receptors in central nervous system involved in (anti)nociceptive modulation...
January 17, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29352826/the-in-vitro-antileishmanial-activity-of-essential-oil-from-aloysia-gratissima-and-guaiol-its-major-sesquiterpene-against-leishmania-amazonensis
#15
Maria Carolina Freitas Garcia, Deivid Costa Soares, Raissa Couto Santana, Elvira Maria Saraiva, Antonio Carlos Siani, Mônica Freiman S Ramos, Maria das Graças Miranda Danelli, Thaïs Cristina Souto-Padron, Lucia H Pinto-da-Silva
Leishmaniases is a tropical disease caused by protozoa of the genus Leishmania for which the current treatment is expensive, besides increasing reports of parasite resistance. This study investigated the anti-Leishmania amazonensis activity of the essential oil from Aloysia gratissima (AgEO) and guaiol, the major sesquiterpene constituent in the oil. Our results showed that AgEO killed promastigotes and intracellular amastigotes at an IC50 of 25 and 0·16 µg mL-1, respectively, while guaiol killed amastigotes at an IC50 of 0·01 µg mL-1...
January 21, 2018: Parasitology
https://www.readbyqxmd.com/read/29352734/resistance-to-tyrosine-kinase-inhibitors-in-non-small-cell-lung-cancer-the-role-of-cancer-stem-cells
#16
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/29352704/treatment-of-adult-chronic-indeterminate-chagas-disease-with-benznidazole-and-three-e1224-dosing-regimens-a-proof-of-concept-randomised-placebo-controlled-trial
#17
Faustino Torrico, Joaquim Gascon, Lourdes Ortiz, Cristina Alonso-Vega, María-Jesús Pinazo, Alejandro Schijman, Igor C Almeida, Fabiana Alves, Nathalie Strub-Wourgaft, Isabela Ribeiro
BACKGROUND: Chagas disease is a major neglected vector-borne disease. In this study, we investigated the safety and efficacy of three oral E1224 (a water-soluble ravuconazole prodrug) regimens and benznidazole versus placebo in adult chronic indeterminate Chagas disease. METHOD: In this proof-of-concept, double-blind, randomised phase 2 clinical trial, we recruited adults (18-50 years) with confirmed diagnosis of Trypanosoma cruzi infection from two outpatient units in Bolivia...
January 15, 2018: Lancet Infectious Diseases
https://www.readbyqxmd.com/read/29352526/ectrims-ean-guideline-on-the-pharmacological-treatment-of-people-with-multiple-sclerosis
#18
X Montalban, R Gold, A J Thompson, S Otero-Romero, M P Amato, D Chandraratna, M Clanet, G Comi, T Derfuss, F Fazekas, H P Hartung, E Havrdova, B Hemmer, L Kappos, R Liblau, C Lubetzki, E Marcus, D H Miller, T Olsson, S Pilling, K Selmaj, A Siva, P S Sorensen, M P Sormani, C Thalheim, H Wiendl, F Zipp
BACKGROUND AND PURPOSE: Multiple sclerosis (MS) is a complex disease of the central nervous system. As new drugs are becoming available, knowledge on diagnosis and treatment must continuously evolve. There is therefore a need for a reference tool compiling current data on benefit and safety, to aid professionals in treatment decisions and use of resources across Europe. The European Committee of Treatment and Research in Multiple Sclerosis (ECTRIMS) and the European Academy of Neurology (EAN) have joined forces to meet this need...
January 19, 2018: European Journal of Neurology: the Official Journal of the European Federation of Neurological Societies
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
#19
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/29352503/in-vivo-effects-of-%C3%AE-opioid-receptor-agonist-%C3%AE-opioid-receptor-antagonist-peptidomimetics-following-acute-and-repeated-administration
#20
Jessica P Anand, Kelsey E Kochan, Anthony F Nastase, Deanna Montgomery, Nicholas W Griggs, John R Traynor, Henry I Mosberg, Emily M Jutkiewicz
BACKGROUND AND PURPOSE: Mu opioid receptor (μ-receptor) agonists are used for pain management, but produce adverse effects including tolerance, dependence, and euphoria. The co-administration of a μ-receptor agonist with a delta opioid receptor (δ-receptor) antagonist has been shown to produce antinociception with reduced development of some side effects. We characterized the effects of three μ-receptor agonist/δ-receptor antagonist peptidomimetics in vivo after acute and repeated administration to determine if this profile provides a viable alternative to traditional opioid analgesics...
January 19, 2018: British Journal of Pharmacology
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