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Pharmaceuticals, Volume 12, Issue 1

2019 March - 45 articles

Cover Story: Tolterodine is a chiral drug with muscarinic receptor antagonist activity, patented and marketed as L-tartrate salt of (R)-enantiomer. The absolute configuration of tolterodine was ambiguously defined in the original patents, and only later established by X-ray analysis. We report the first chiroptical investigation of tolterodine by electronic and vibrational circular dichroism (ECD and VCD), including solvent effects and temperature dependence. The CD-based combined experimental/computational approach allows a safe assignment of the absolute configuration of a chiral drug, independent of chemical correlations with other chiral compounds. The existing literature does not ultimately prove the enantioselective calcium antagonist and anticholinergic mode of action of tolterodine, posing a question on the necessity of using this drug in its enantiomerically pure form rather than as a racemate. View this paper.
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Articles (45)

  • Article
  • Open Access
22 Citations
5,388 Views
11 Pages

APELA Expression in Glioma, and Its Association with Patient Survival and Tumor Grade

  • Debolina Ganguly,
  • Chun Cai,
  • Michelle M. Sims,
  • Chuan He Yang,
  • Matthew Thomas,
  • Jinjun Cheng,
  • Ali G. Saad and
  • Lawrence M. Pfeffer

Glioblastoma (GBM) is the most common and deadliest primary adult brain tumor. Invasion, resistance to therapy, and tumor recurrence in GBM can be attributed in part to brain tumor-initiating cells (BTICs). BTICs isolated from various patient-derived...

  • Article
  • Open Access
7 Citations
4,342 Views
11 Pages

Raman Microspectroscopy as a Tool to Elucidate the Efficacy of Topical Formulations Containing Curcumin

  • Ievgeniia Iermak,
  • Ana Paula da Silva,
  • Cristina Kurachi,
  • Vanderlei Salvador Bagnato and
  • Natalia Mayumi Inada

The success of the onychomycosis treatment is directly associated with factors such as the choice of the medication, the administration route, and the pharmaceutical formulation. Photodynamic therapy (PDT) is an emerging and promising technique indic...

  • Article
  • Open Access
55 Citations
9,882 Views
14 Pages

The treatment of enteric bacterial infections using oral bacteriophage therapy can be challenging since the harsh acidic stomach environment renders phages inactive during transit through the gastrointestinal tract. Solid oral dosage forms allowing s...

  • Article
  • Open Access
9 Citations
5,419 Views
14 Pages

Localization of 99mTc-GRP Analogs in GRPR-Expressing Tumors: Effects of Peptide Length and Neprilysin Inhibition on Biological Responses

  • Aikaterini Kaloudi,
  • Emmanouil Lymperis,
  • Panagiotis Kanellopoulos,
  • Beatrice Waser,
  • Marion de Jong,
  • Eric P. Krenning,
  • Jean Claude Reubi,
  • Berthold A. Nock and
  • Theodosia Maina

The overexpression of gastrin-releasing peptide receptors (GRPRs) in frequently occurring human tumors has provided the opportunity to use bombesin (BBN) analogs as radionuclide carriers to cancer sites for diagnostic and therapeutic purposes. We hav...

  • Article
  • Open Access
20 Citations
6,124 Views
15 Pages

Physical Stability and Viscoelastic Properties of Co-Amorphous Ezetimibe/Simvastatin System

  • Justyna Knapik-Kowalczuk,
  • Krzysztof Chmiel,
  • Karolina Jurkiewicz,
  • Natália T. Correia,
  • Wiesław Sawicki and
  • Marian Paluch

The purpose of this paper is to examine the physical stability as well as viscoelastic properties of the binary amorphous ezetimibe–simvastatin system. According to our knowledge, this is the first time that such an amorphous composition is pre...

  • Review
  • Open Access
120 Citations
12,908 Views
31 Pages

Alzheimer’s disease (AD) is a growing global health concern with a massive impact on affected individuals and society. Despite the considerable advances achieved in the understanding of AD pathogenesis, researchers have not been successful in f...

  • Communication
  • Open Access
5 Citations
4,827 Views
14 Pages

A rapid, high-yielding microwave-mediated synthetic procedure was developed and optimized using a model system of monovalent sugar linkers, with the ultimate goal of using this method for the synthesis of multivalent glycoclusters. The reaction occur...

  • Review
  • Open Access
4 Citations
4,691 Views
14 Pages

Potential of the Other Genetic Information Coded by the Viral RNA Genomes as Antiviral Target

  • Alfredo Berzal-Herranz,
  • Cristina Romero-López,
  • Beatriz Berzal-Herranz and
  • Sara Ramos-Lorente

In addition to the protein coding information, viral RNA genomes code functional information in structurally conserved units termed functional RNA domains. These RNA domains play essential roles in the viral cycle (e.g., replication and translation)....

  • Article
  • Open Access
59 Citations
8,608 Views
19 Pages

In Silico Study to Identify New Antituberculosis Molecules from Natural Sources by Hierarchical Virtual Screening and Molecular Dynamics Simulations

  • Vinícius de S. Pinto,
  • Janay S. C. Araújo,
  • Rai C. Silva,
  • Glauber V. da Costa,
  • Jorddy N. Cruz,
  • Moysés F. De A. Neto,
  • Joaquín M. Campos,
  • Cleydson B. R. Santos,
  • Franco H. A. Leite and
  • Manoelito C. S. Junior

Tuberculosis (TB) is an infection caused by Mycobacterium tuberculosis, responsible for 1.5 million documented deaths in 2016. The increase in reported cases of M. tuberculosis resistance to the main drugs show the need for the development of new and...

  • Brief Report
  • Open Access
45 Citations
11,603 Views
7 Pages

In 2018, Baricitinib was approved by the Food and Drig Administration (FDA) for the treatment of rheumatoid arthritis. Baricitinib exerts its action by targeting Janus kinases (JAK). In this study, we describe the necessary steps for preparing the dr...

  • Review
  • Open Access
411 Citations
35,397 Views
23 Pages

For a bacteriophage to be useful for phage therapy it must be both isolated from the environment and shown to have certain characteristics beyond just killing strains of the target bacterial pathogen. These include desirable characteristics such as a...

  • Article
  • Open Access
23 Citations
8,247 Views
14 Pages

Chemical Characterization, Antioxidant, Cytotoxic and Microbiological Activities of the Essential Oil of Leaf of Tithonia Diversifolia (Hemsl) A. Gray (Asteraceae)

  • Ana Luzia Ferreira Farias,
  • Alex Bruno Lobato Rodrigues,
  • Rosany Lopes Martins,
  • Érica de Menezes Rabelo,
  • Carlos Wagner Ferreira Farias and
  • Sheylla Susan Moreira da Silva de Almeida

The present study aimed to evaluate the chemical composition, antioxidant potential, and the cytotoxic and antimicrobial activity of the essential oil of the plant species Tithonia diversifolia (Hemsl) A. Gray. The essential oil obtained was used to...

  • Article
  • Open Access
67 Citations
6,572 Views
15 Pages

Development and Characterization of Chitosan Microparticles-in-Films for Buccal Delivery of Bioactive Peptides

  • Patrícia Batista,
  • Pedro Castro,
  • Ana Raquel Madureira,
  • Bruno Sarmento and
  • Manuela Pintado

20 February 2019

Nowadays, bioactive peptides are used for therapeutic applications and the selection of a carrier to deliver them is very important to increase the efficiency, absorption, release, bioavailability and consumer acceptance. The aim of this study was to...

  • Article
  • Open Access
10 Citations
6,009 Views
20 Pages

Characterisation of an Isogenic Model of Cisplatin Resistance in Oesophageal Adenocarcinoma Cells

  • Amy M. Buckley,
  • Becky AS. Bibby,
  • Margaret R. Dunne,
  • Susan A. Kennedy,
  • Maria B. Davern,
  • Breandán N. Kennedy,
  • Stephen G. Maher and
  • Jacintha O’Sullivan

20 February 2019

Cisplatin (cis-diamminedichloroplatinum) is widely used for the treatment of solid malignancies; however, the development of chemoresistance hinders the success of this chemotherapeutic in the clinic. This study provides novel insights into the molec...

  • Review
  • Open Access
39 Citations
8,048 Views
11 Pages

Iron in Lung Pathology

  • Vida Zhang,
  • Elizabeta Nemeth and
  • Airie Kim

15 February 2019

The lung presents a unique challenge for iron homeostasis. The entire airway is in direct contact with the environment and its iron particulate matter and iron-utilizing microbes. However, the homeostatic and adaptive mechanisms of pulmonary iron reg...

  • Article
  • Open Access
5 Citations
5,121 Views
15 Pages

2-Nitroimidazole-Furanoside Derivatives for Hypoxia Imaging—Investigation of Nucleoside Transporter Interaction, 18F-Labeling and Preclinical PET Imaging

  • Florian C. Maier,
  • Anna Schweifer,
  • Vijaya L. Damaraju,
  • Carol E. Cass,
  • Gregory D. Bowden,
  • Walter Ehrlichmann,
  • Manfred Kneilling,
  • Bernd J. Pichler,
  • Friedrich Hammerschmidt and
  • Gerald Reischl

15 February 2019

The benefits of PET imaging of tumor hypoxia in patient management has been demonstrated in many examples and with various tracers over the last years. Although, the optimal hypoxia imaging agent has yet to be found, 2-nitroimidazole (azomycin) sugar...

  • Review
  • Open Access
24 Citations
7,762 Views
18 Pages

14 February 2019

The possibility that inflammation plays a causal role in major depression is an important claim in the emerging field of immunopsychiatry and has generated hope for new treatments. The aims of the present review are first to provide some historical b...

  • Article
  • Open Access
13 Citations
5,998 Views
17 Pages

13 February 2019

Although the branched capsular polysaccharides of Streptococcus agalactiae serotype III (GBSIII PS) and Streptococcus pneumoniae serotype 14 (Pn14 PS) differ only in the addition of a terminal sialic acid on the GBSIII PS side chains, these very simi...

  • Review
  • Open Access
73 Citations
11,385 Views
22 Pages

9 February 2019

Neurodegeneration with brain iron accumulation (NBIA) is a set of neurodegenerative disorders, which includes very rare monogenetic diseases. They are heterogeneous in regard to the onset and the clinical symptoms, while the have in common a specific...

  • Article
  • Open Access
110 Citations
11,357 Views
11 Pages

6 February 2019

Ferroptosis is a form of programmed cell death that is characterized by lipid peroxidation and is inducible by iron and the accumulation of reactive oxygen species (ROS). It is triggered by erastin but inhibited by antioxidants such as α-tocoph...

  • Article
  • Open Access
22 Citations
4,819 Views
8 Pages

Comparative Study of Two Oxidizing Agents, Chloramine T and Iodo-Gen®, for the Radiolabeling of β-CIT with Iodine-131: Relevance for Parkinson’s Disease

  • Ana Claudia R. Durante,
  • Danielle V. Sobral,
  • Ana Claudia C. Miranda,
  • Érika V. de Almeida,
  • Leonardo L. Fuscaldi,
  • Marycel R. F. F. de Barboza and
  • Luciana Malavolta

5 February 2019

Parkinson’s disease (PD) is a neurodegenerative disease characterized by the loss of dopaminergic neurons in the substantia nigra pars compacta, leading to alteration of the integrity of dopaminergic transporters (DATs). In recent years, some r...

  • Article
  • Open Access
5 Citations
4,755 Views
11 Pages

Camphor, Applied Epidermally to the Back, Causes Snout- and Chest-Grooming in Rats: A Response Mediated by Cutaneous TRP Channels

  • Débora T. Ishikawa,
  • Robson Cristiano Lillo Vizin,
  • Cristiane Oliveira de Souza,
  • Daniel Carneiro Carrettiero,
  • Andrej A. Romanovsky and
  • Maria Camila Almeida

2 February 2019

Thermoregulatory grooming, a behavioral defense against heat, is known to be driven by skin-temperature signals. Because at least some thermal cutaneous signals that drive heat defenses are likely to be generated by transient receptor potential (TRP)...

  • Review
  • Open Access
49 Citations
9,309 Views
23 Pages

1 February 2019

The lungs are essential for gas exchange and serve as the gateways of our body to the external environment. They are easily accessible for drugs from both sides, the airways and the vasculature. Recent literature provides evidence for a role of Trans...

  • Correction
  • Open Access
3 Citations
3,537 Views
1 Page

Correction: Mateusz, S., et al. Iron Supplementation in Suckling Piglets: An Ostensibly Easy Therapy of Neonatal Iron Deficiency Anemia. Pharmaceuticals 2018, 11, 128

  • Mateusz Szudzik,
  • Rafał R. Starzyński,
  • Aneta Jończy,
  • Rafał Mazgaj,
  • Małgorzata Lenartowicz and
  • Paweł Lipiński

29 January 2019

The authors wish to make the following corrections to this paper [1]: the term “liposomal” should be replaced with the term “sucrosomial” in the following places [...]

  • Article
  • Open Access
11 Citations
5,487 Views
12 Pages

On the Absolute Stereochemistry of Tolterodine: A Circular Dichroism Study

  • Marcin Górecki,
  • Valerio Zullo,
  • Anna Iuliano and
  • Gennaro Pescitelli

26 January 2019

Tolterodine (1) is a potent muscarinic receptor antagonist used in the treatment of overactive urinary bladder (OAB) syndrome. Tolterodine is chiral and it was patented, and is currently marketed, as the l-tartrate salt of the (R)-enantiomer. However...

  • Article
  • Open Access
45 Citations
8,623 Views
22 Pages

Identification of Potential Inhibitors from Pyriproxyfen with Insecticidal Activity by Virtual Screening

  • Ryan da Silva Ramos,
  • Josivan da Silva Costa,
  • Rai Campos Silva,
  • Glauber Vilhena da Costa,
  • Alex Bruno Lobato Rodrigues,
  • Érica de Menezes Rabelo,
  • Raimundo Nonato Picanço Souto,
  • Carlton Anthony Taft,
  • Carlos Henrique Tomich de Paula da Silva and
  • Williams Jorge da Cruz Macêdo
  • + 2 authors

25 January 2019

Aedes aegypti is the main vector of dengue fever transmission, yellow fever, Zika, and chikungunya in tropical and subtropical regions and it is considered to cause health risks to millions of people in the world. In this study, we search to obtain n...

  • Article
  • Open Access
56 Citations
11,081 Views
9 Pages

[177Lu]Lu-PSMA-617 Salivary Gland Uptake Characterized by Quantitative In Vitro Autoradiography

  • Roswitha Tönnesmann,
  • Philipp T. Meyer,
  • Matthias Eder and
  • Ann-Christin Baranski

24 January 2019

Irradiation of salivary glands remains the main dose-limiting side effect of therapeutic PSMA-inhibitors, especially when using alpha emitters. Thus, further advances in radiopharmaceutical design and therapy strategies are needed to reduce salivary...

  • Article
  • Open Access
3 Citations
4,538 Views
20 Pages

TRPV1 Inhibits the Ventilatory Response to Hypoxia in Adult Rats, but Not the CO2-Drive to Breathe

  • Luis Gustavo A. Patrone,
  • Jaime B. Duarte,
  • Kênia Cardoso Bícego,
  • Alexandre A. Steiner,
  • Andrej A. Romanovsky and
  • Luciane H. Gargaglioni

24 January 2019

Receptors of the transient receptor potential (TRP) channels superfamily are expressed in many tissues and have different physiological functions. However, there are few studies investigating the role of these channels in cardiorespiratory control in...

  • Review
  • Open Access
18 Citations
11,237 Views
15 Pages

Can the Efficacy of [18F]FDG-PET/CT in Clinical Oncology Be Enhanced by Screening Biomolecular Profiles?

  • Hazel O’Neill,
  • Vinod Malik,
  • Ciaran Johnston,
  • John V Reynolds and
  • Jacintha O’Sullivan

23 January 2019

Positron Emission Tomography (PET) is a functional imaging modality widely used in clinical oncology. Over the years the sensitivity and specificity of PET has improved with the advent of specific radiotracers, increased technical accuracy of PET sca...

  • Article
  • Open Access
24 Citations
12,352 Views
15 Pages

L-Ferritin: One Gene, Five Diseases; from Hereditary Hyperferritinemia to Hypoferritinemia—Report of New Cases

  • Beatriz Cadenas,
  • Josep Fita-Torró,
  • Mar Bermúdez-Cortés,
  • Inés Hernandez-Rodriguez,
  • José Luis Fuster,
  • María Esther Llinares,
  • Ana María Galera,
  • Julia Lee Romero,
  • Santiago Pérez-Montero and
  • Mayka Sanchez
  • + 1 author

23 January 2019

Ferritin is a multimeric protein composed of light (L-ferritin) and heavy (H-ferritin) subunits that binds and stores iron inside the cell. A variety of mutations have been reported in the L-ferritin subunit gene (FTL gene) that cause the following f...

  • Article
  • Open Access
83 Citations
8,195 Views
23 Pages

19 January 2019

In this study, self-assembling Soluplus® micelles were examined for inherent properties. Through calorimetric analysis, the critical micelle concentration (CMC) could be determined at 25 and 37 °C, and the influence of three media (Milli-Q wa...

  • Article
  • Open Access
13 Citations
7,683 Views
16 Pages

Structural and In Vitro Functional Comparability Analysis of Altebrel™, a Proposed Etanercept Biosimilar: Focus on Primary Sequence and Glycosylation

  • Ramin Fazel,
  • Yudong Guan,
  • Behrouz Vaziri,
  • Christoph Krisp,
  • Laura Heikaus,
  • Amirhossein Saadati,
  • Siti Nurul Hidayah,
  • Manasi Gaikwad and
  • Hartmut Schlüter

17 January 2019

The demand for reliable comparability studies of biosimilars grows with their increased market share. These studies focus on physicochemical, structural, functional and clinical properties to ensure that a biosimilar has no significant differences to...

  • Article
  • Open Access
14 Citations
4,795 Views
15 Pages

Cholecystokinin-2 Receptor Targeting with Novel C-terminally Stabilized HYNIC-Minigastrin Analogs Radiolabeled with Technetium-99m

  • Maximilian Klingler,
  • Christine Rangger,
  • Dominik Summer,
  • Piriya Kaeopookum,
  • Clemens Decristoforo and
  • Elisabeth von Guggenberg

15 January 2019

The high overexpression of cholecystokinin-2 receptors (CCK2R) in tumors, such as medullary thyroid carcinoma, allows for highly specific diagnostic and therapeutic targeting with radiolabeled peptide probes derived from natural ligands for the recep...

  • Article
  • Open Access
3 Citations
4,539 Views
14 Pages

Optimization of the Automated Synthesis of [11C]mHED—Administered and Apparent Molar Activities

  • Chrysoula Vraka,
  • Verena Pichler,
  • Neydher Berroterán-Infante,
  • Tim Wollenweber,
  • Anna Pillinger,
  • Maximilian Hohensinner,
  • Lukas Fetty,
  • Dietrich Beitzke,
  • Xiang Li and
  • Wolfgang Wadsak
  • + 4 authors

14 January 2019

The tracer [11C]meta-Hydroxyephedrine ([11C]mHED) is one of the most applied PET tracers for cardiac imaging, whose radiosynthesis was already reported in 1990. While not stated in the literature, separation difficulties and an adequate formulation o...

  • Review
  • Open Access
691 Citations
33,250 Views
18 Pages

The Therapeutic Potential of Naringenin: A Review of Clinical Trials

  • Bahare Salehi,
  • Patrick Valere Tsouh Fokou,
  • Mehdi Sharifi-Rad,
  • Paolo Zucca,
  • Raffaele Pezzani,
  • Natália Martins and
  • Javad Sharifi-Rad

10 January 2019

Naringenin is a flavonoid belonging to flavanones subclass. It is widely distributed in several Citrus fruits, bergamot, tomatoes and other fruits, being also found in its glycosides form (mainly naringin). Several biological activities have been asc...

  • Article
  • Open Access
29 Citations
7,394 Views
17 Pages

Juvenile Arthritis Patients Suffering from Chronic Inflammation Have Increased Activity of Both IDO and GTP-CH1 Pathways But Decreased BH4 Efficacy: Implications for Well-Being, Including Fatigue, Cognitive Impairment, Anxiety, and Depression

  • Gerdien A. H. Korte-Bouws,
  • Eline Albers,
  • Marije Voskamp,
  • Hendrikus Hendriksen,
  • Lidewij R. De Leeuw,
  • Onur Güntürkün,
  • Sytze De Roock,
  • Sebastiaan J. Vastert and
  • S. Mechiel Korte

Juvenile idiopathic arthritis (JIA) represents joint inflammation with an unknown cause that starts before the age of 16, resulting in stiff and painful joints. In addition, JIA patients often report symptoms of sickness behavior. Recent animal studi...

  • Review
  • Open Access
68 Citations
10,263 Views
29 Pages

The importance of Ca2+ signalling in key events of cancer cell function and tumour progression, such as proliferation, migration, invasion and survival, has recently begun to be appreciated. Many cellular Ca2+-stimulated signalling cascades utilise t...

  • Review
  • Open Access
11 Citations
7,330 Views
14 Pages

Radioligands for Tropomyosin Receptor Kinase (Trk) Positron Emission Tomography Imaging

  • Ralf Schirrmacher,
  • Justin J. Bailey,
  • Andrew V. Mossine,
  • Peter J. H. Scott,
  • Lena Kaiser,
  • Peter Bartenstein,
  • Simon Lindner,
  • David R. Kaplan,
  • Alexey Kostikov and
  • Vadim Bernard-Gauthier
  • + 8 authors

The tropomyosin receptor kinases family (TrkA, TrkB, and TrkC) supports neuronal growth, survival, and differentiation during development, adult life, and aging. TrkA/B/C downregulation is a prominent hallmark of various neurological disorders includ...

  • Article
  • Open Access
4 Citations
4,557 Views
9 Pages

Introduction: Benzotriazine-1,4-dioxides (BTDOs) such as tirapazamine (TPZ) and its derivatives act as radiosensitizers of hypoxic tissues. The benzotriazine-1-monoxide (BTMO) metabolite (SR 4317, TPZMO) of TPZ also has radiosensitizing properties, a...

  • Review
  • Open Access
85 Citations
14,945 Views
28 Pages

Iron Homeostasis in the Lungs—A Balance between Health and Disease

  • Joana Neves,
  • Thomas Haider,
  • Max Gassmann and
  • Martina U. Muckenthaler

A strong mechanistic link between the regulation of iron homeostasis and oxygen sensing is evident in the lung, where both systems must be properly controlled to maintain lung function. Imbalances in pulmonary iron homeostasis are frequently associat...

  • Review
  • Open Access
28 Citations
8,728 Views
21 Pages

The need for new drugs is compelling, irrespective of the disease. Focusing on medical problems in the Western countries, heart disease and cancer are at the moment predominant illnesses. Owing to the fact that ~90% of all 21,000 cellular proteins in...

  • Review
  • Open Access
19 Citations
7,100 Views
20 Pages

Radiolabelled Aptamers for Theranostic Treatment of Cancer

  • Umair Khalid,
  • Chris Vi,
  • Justin Henri,
  • Joanna Macdonald,
  • Peter Eu,
  • Giovanni Mandarano and
  • Sarah Shigdar

24 December 2018

Cancer has a high incidence and mortality rate worldwide, which continues to grow as millions of people are diagnosed annually. Metastatic disease caused by cancer is largely responsible for the mortality rates, thus early detection of metastatic tum...

  • Article
  • Open Access
20 Citations
5,319 Views
11 Pages

Decrease of Antimicrobial Resistance through Polyelectrolyte-Coated Nanoliposomes Loaded with β-Lactam Drug

  • Lina M. Arévalo,
  • Cristhian J. Yarce,
  • José Oñate-Garzón and
  • Constain H. Salamanca

23 December 2018

Currently, one of the greatest health challenges worldwide is the resistance to antibiotic drugs, which has led to the pursuit of new alternatives for the recovery of biological activity, where the use of different types of nano-systems has shown an...

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Pharmaceuticals - ISSN 1424-8247