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Pharmaceuticals, Volume 14, Issue 9

2021 September - 113 articles

Cover Story: An indole alkaloid, isolated from the African medicinal plant Tabernaemontana elegans, was derivatized yielding nineteen azines and eleven semicarbazones. Through a functional assay, in a human ABCB1-transfected mouse T-lymphoma cell model overexpressing P-glycoprotein, a significant increase in P-gp inhibitory activity was observed for most derivatives, those with trimethoxyphenyl or naphthyl motifs being among the most active. In chemosensitivity assays, they interacted synergistically with doxorubicin. Most of them showed MDR-selective activity toward resistant cells, having a collateral sensitivity effect. In the ATPase assay, selected compounds behaved as inhibitors. A QSAR model allowed us to deduce that compounds bearing bulky and lipophilic substituents were stronger P-gp inhibitors. View this paper.
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Articles (113)

  • Article
  • Open Access
11 Citations
4,360 Views
11 Pages

The Synthetic Curcumin Analog HO-3867 Rescues Suppression of PLAC1 Expression in Ovarian Cancer Cells

  • Eric J. Devor,
  • Brandon M. Schickling,
  • Jace R. Lapierre,
  • David P. Bender and ,
  • Jesus Gonzalez-Bosquet and
  • Kimberly K. Leslie
  • + 1 author+ 0 author

21 September 2021

Elevated expression of placenta-specific protein 1 (PLAC1) is associated with the increased proliferation and invasiveness of a variety of human cancers, including ovarian cancer. Recent studies have shown that the tumor suppressor p53 directly suppr...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
7 Citations
6,500 Views
20 Pages

Development and Validation of a New Storage Procedure to Extend the In-Use Stability of Azacitidine in Pharmaceutical Formulations

  • Antonella Iudicello,
  • Filippo Genovese,
  • Valentina Strusi,
  • Massimo Dominici and
  • Barbara Ruozi

21 September 2021

Stability studies performed by the pharmaceutical industry are principally designed to fulfill licensing requirements. Thus, post-dilution or post-reconstitution stability data are frequently limited to 24 h only for bacteriological reasons, regardle...

(This article belongs to the Section Pharmaceutical Technology)
  • Article
  • Open Access
18 Citations
3,806 Views
23 Pages

Less Polar Compounds and Targeted Antioxidant Potential (In Vitro and In Vivo) of Codium adhaerens C. Agardh 1822

  • Sanja Radman,
  • Ana-Marija Cikoš,
  • Ivana Flanjak,
  • Sanja Babić and ,
  • Lara Čižmek,
  • Drago Šubarić,
  • Rozelindra Čož-Rakovac,
  • Stela Jokić and
  • Igor Jerković
  • + 4 authors+ 0 author

21 September 2021

Codium adhaerens from the Adriatic Sea (Croatia) was comprehensively investigated regarding less polar compounds for the first time. Although there are several phytochemical studies on C. adhaerens from other regions, this is the first report on vola...

(This article belongs to the Special Issue Chemistry and Biomedical Potential of Marine Natural Products)
  • Article
  • Open Access
27 Citations
4,080 Views
15 Pages

A Comparative Survey of Anti-Melanoma and Anti-Inflammatory Potential of Usnic Acid Enantiomers—A Comprehensive In Vitro Approach

  • Agnieszka Galanty,
  • Paweł Zagrodzki,
  • Joanna Gdula-Argasińska,
  • Karolina Grabowska and ,
  • Paulina Koczurkiewicz-Adamczyk,
  • Dagmara Wróbel-Biedrawa,
  • Irma Podolak,
  • Elżbieta Pękala and
  • Paweł Paśko
  • + 4 authors+ 0 author

21 September 2021

Usnic acid (UA) is a chiral lichen metabolite with an interesting pharmacological profile. The aim of this study was to compare the anti-melanoma effect of (+)-UA and (−)-UA in an in vitro model by studying their impact on the cells as well as the pr...

(This article belongs to the Special Issue Antiradical, Chemopreventive and Antimicrobial Analysis of Bioactive Substances)
  • Article
  • Open Access
80 Citations
5,894 Views
16 Pages

Antioxidant and Anti-Inflammatory Potential of Thymoquinone and Lycopene Mitigate the Chlorpyrifos-Induced Toxic Neuropathy

  • Mohamed Aboubakr,
  • Said M. Elshafae,
  • Ehab Y. Abdelhiee,
  • Sabreen E. Fadl and ,
  • Ahmed Soliman,
  • Afaf Abdelkader,
  • Mohamed M. Abdel-Daim,
  • Khaled A. Bayoumi,
  • Roua S. Baty and
  • Ahmed Abdeen
  • + 9 authors+ 4 authors

20 September 2021

CPF (chlorpyrifos) is an organophosphate pesticide used in agricultural and veterinary applications. Our experiment aimed to explore the effects of thymoquinone (TQ) and/or lycopene (LP) against CPF-induced neurotoxicity. Wistar rats were categorized...

(This article belongs to the Special Issue Natural Bioactive Compounds and Neurological Disorders: Exploiting Resources from Nature)
  • Article
  • Open Access
48 Citations
8,513 Views
20 Pages

Chicory Extracts and Sesquiterpene Lactones Show Potent Activity against Bacterial and Fungal Pathogens

  • Suvi T. Häkkinen,
  • Marina Soković,
  • Liisa Nohynek,
  • Ana Ćirić and ,
  • Marija Ivanov,
  • Dejan Stojković,
  • Irina Tsitko,
  • Melanie Matos,
  • João P. Baixinho and
  • Kirsi-Marja Oksman-Caldentey
  • + 8 authors+ 3 authors

20 September 2021

Chicory (Cichorium intybus L.) is an important industrial crop cultivated mainly to extract the dietary fiber inulin. However, chicory also contains bioactive compounds such as sesquiterpene lactones and certain polyphenols, which are currently disca...

(This article belongs to the Special Issue Natural Pharmacons: Biologically Active Plant Based Pharmaceuticals)
  • Article
  • Open Access
23 Citations
3,979 Views
20 Pages

Preparation of Soluble Complex of Curcumin for the Potential Antagonistic Effects on Human Colorectal Adenocarcinoma Cells

  • Jamal Moideen Muthu Mohamed,
  • Ali Alqahtani,
  • Barkat A. Khan,
  • Adel Al Fatease and ,
  • Taha Alqahtani,
  • Krishnaraju Venkatesan,
  • Fazil Ahmad,
  • Bashar I. Alzghoul and
  • Ali Alamri
  • + 4 authors+ 0 author

19 September 2021

This study was designed to investigate the effects of curcumin (CMN) soluble complex (SC) prepared by melt casting (HM) and hot-melt extrusion (HME) technology. Phase solubility (PS) study, in silico molecular modeling, aqueous solubility, drug relea...

(This article belongs to the Topic Compounds with Medicinal Value)
  • Article
  • Open Access
3 Citations
3,628 Views
14 Pages

19 September 2021

Chiral total syntheses of both enantiomers of the anti-MRSA active plymuthipyranone B and all of the both enantiomers of three unnatural and synthetic analogues were performed. These two pairs of four chiral compounds are composed of the same 3-acyl-...

(This article belongs to the Special Issue Chirality in Drug Discovery)
  • Article
  • Open Access
62 Citations
6,355 Views
19 Pages

High-Throughput Screening and Molecular Dynamics Simulation of Natural Product-like Compounds against Alzheimer’s Disease through Multitarget Approach

  • Danish Iqbal,
  • Md Tabish Rehman,
  • Abdulaziz Bin Dukhyil,
  • Syed Mohd Danish Rizvi and ,
  • Mohamed F. Al Ajmi,
  • Bader Mohammed Alshehri,
  • Saeed Banawas,
  • M. Salman Khan,
  • Wael Alturaiki and
  • Mohammed Alsaweed
  • + 5 authors+ 0 author

18 September 2021

Alzheimer’s disease (AD) is a progressive neurological disorder that affects 50 million people. Despite this, only two classes of medication have been approved by the FDA. Therefore, we have planned to develop therapeutics by multitarget approach. We...

(This article belongs to the Special Issue In Silico Approaches in Drug Design)
  • Review
  • Open Access
18 Citations
5,673 Views
18 Pages

Neuropsychiatric Disorders and COVID-19: What We Know So Far

  • Fernanda Majolo,
  • Guilherme Liberato da Silva,
  • Lucas Vieira,
  • Cetin Anli and ,
  • Luís Fernando Saraiva Macedo Timmers,
  • Stefan Laufer and
  • Márcia Inês Goettert
  • + 2 authors+ 0 author

17 September 2021

SARS-CoV-2 (Severe Acute Respiratory Syndrome Coronavirus-2) affects the central nervous system (CNS), which is shown in a significant number of patients with neurological events. In this study, an updated literature review was carried out regarding...

(This article belongs to the Special Issue COVID-19 in Pharmaceuticals)
  • Review
  • Open Access
22 Citations
8,336 Views
16 Pages

Manufacturing Bacteriophages (Part 1 of 2): Cell Line Development, Upstream, and Downstream Considerations

  • Tayfun Tanir,
  • Marvin Orellana,
  • Aster Escalante,
  • Carolina Moraes de Souza and
  • Michael S. Koeris

17 September 2021

Within this first part of the two-part series on phage manufacturing, we will give an overview of the process leading to bacteriophages as a drug substance, before covering the formulation into a drug product in the second part. The principal goal is...

(This article belongs to the Special Issue Bacteriophages as Therapeutic Delivery Vehicles)
  • Feature Paper
  • Article
  • Open Access
31 Citations
5,585 Views
18 Pages

The Metabolomic Approach Reveals the Alteration in Human Serum and Cerebrospinal Fluid Composition in Parkinson’s Disease Patients

  • Szymon Plewa,
  • Karolina Poplawska-Domaszewicz,
  • Jolanta Florczak-Wyspianska,
  • Agnieszka Klupczynska-Gabryszak and ,
  • Bartosz Sokol,
  • Wojciech Miltyk,
  • Roman Jankowski,
  • Wojciech Kozubski,
  • Zenon J. Kokot and
  • Jan Matysiak
  • + 5 authors+ 0 author

17 September 2021

Parkinson’s disease (PD) is a major public health problem. Since currently there are no reliable diagnostic tools to reveal the early steps of PD, new methods should be developed, including those searching the variations in human metabolome. Alterati...

(This article belongs to the Section Pharmacology)
  • Review
  • Open Access
21 Citations
9,758 Views
26 Pages

The Endocannabinoid System and Cannabidiol: Past, Present, and Prospective for Cardiovascular Diseases

  • Martina Rabino,
  • Sara Mallia,
  • Elisa Castiglioni,
  • Davide Rovina and ,
  • Giulio Pompilio and
  • Aoife Gowran
  • + 1 author+ 0 author

17 September 2021

In the past, cannabis was commonly associated with mysticism and illegality. Fortunately, in recent years perspectives and discourses have changed. More prominence has been given to the rigorous scientific effort that led to the discovery of cannabis...

(This article belongs to the Special Issue Cannabidiol: Advances in Therapeutic Applications and Future Perspectives)
  • Article
  • Open Access
20 Citations
6,926 Views
15 Pages

In Vitro and In Vivo Evaluation of Oral Controlled Release Formulation of BCS Class I Drug Using Polymer Matrix System

  • Mosab Arafat,
  • Muhammad Sarfraz,
  • Mohammad F. Bostanudin,
  • Anna Esmaeil and ,
  • Aisha Salam and
  • Salahdein AbuRuz
  • + 1 author+ 0 author

16 September 2021

Diltiazem hydrochloride is a calcium channel blocker, which belongs to the family of benzothiazepines. It is commonly used to treat hypertension and atrial fibrillation. Even though the drug has high solubility, its high permeability and rapid metabo...

(This article belongs to the Section Pharmaceutical Technology)
  • Review
  • Open Access
38 Citations
16,467 Views
15 Pages

16 September 2021

Mirtazapine belongs to the category of antidepressants clinically used mainly in major depressive disorder but also used in obsessive-compulsive disorders, generalized anxiety, and sleep disturbances. This drug acts mainly by antagonizing the adrener...

(This article belongs to the Special Issue Treatment of Alzheimer Disease)
  • Article
  • Open Access
7 Citations
3,264 Views
11 Pages

Pilot Sub-Study of the Effect of Hepatitis C Cure by Glecaprevir/Pibrentasvir on the Gut Microbiome of Patients with Chronic Hepatitis C Genotypes 1 to 6 in the Mythen Study

  • Bahtiyar Yilmaz,
  • Lisa Ruckstuhl,
  • Beat Müllhaupt,
  • Lorenzo Magenta and ,
  • Melanie Harrer Kuster,
  • Olivier Clerc,
  • Ralph Torgler and
  • Nasser Semmo
  • + 3 authors+ 0 author

16 September 2021

In this small pilot sub-study, longitudinal gut microbiota composition changes, after successful treatment of hepatitis C virus (HCV) with the co-formulated glecaprevir/pibrentasvir (GLE/PIB), were analyzed before treatment (baseline) and 12 weeks po...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
28 Citations
5,405 Views
25 Pages

Engineering Mitochondriotropic Carbon Dots for Targeting Cancer Cells

  • Archontia Kaminari,
  • Eleni Nikoli,
  • Alexandros Athanasopoulos,
  • Elias Sakellis and ,
  • Zili Sideratou and
  • Dimitris Tsiourvas
  • + 1 author+ 0 author

16 September 2021

Aiming to understand and enhance the capacity of carbon dots (CDs) to transport through cell membranes and target subcellular organelles—in particular, mitochondria—a series of nitrogen-doped CDs were prepared by the one-step microwave-assisted pyrol...

(This article belongs to the Special Issue Nano Drug Carriers 2021)
  • Review
  • Open Access
11 Citations
8,254 Views
27 Pages

New Strategies for the Treatment of Atrial Fibrillation

  • Norbert Jost,
  • Torsten Christ and
  • János Magyar

15 September 2021

Atrial fibrillation (AF) is the most prevalent cardiac arrhythmia in the clinical practice. It significantly contributes to the morbidity and mortality of the elderly population. Over the past 25–30 years intense effort in basic research has advanced...

(This article belongs to the Special Issue Ion Channels: Current Pharmacological Challenges)
  • Article
  • Open Access
16 Citations
4,704 Views
14 Pages

Population Pharmacokinetic Analysis of Pazopanib in Patients and Determination of Target AUC

  • Agustos Cetin Ozbey,
  • David Combarel,
  • Vianney Poinsignon,
  • Christine Lovera and ,
  • Esma Saada,
  • Olivier Mir and
  • Angelo Paci
  • + 2 authors+ 0 author

15 September 2021

Pazopanib is a potent multi-targeted kinase inhibitor approved for the treatment of advanced renal cell carcinoma and soft tissue sarcoma. The pharmacokinetics of pazopanib is characterized by a significant inter- and intra-patient variability and a...

(This article belongs to the Special Issue Precision Medicine in Oncology: Controlling the Pharmacokinetics Variability)
  • Review
  • Open Access
28 Citations
8,355 Views
22 Pages

State of the Art on Approved Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Modulators and Triple-Combination Therapy

  • Aniello Meoli,
  • Valentina Fainardi,
  • Michela Deolmi,
  • Giulia Chiopris and ,
  • Francesca Marinelli,
  • Caterina Caminiti,
  • Susanna Esposito and
  • Giovanna Pisi
  • + 3 authors+ 0 author

15 September 2021

Cystic fibrosis (CF) is the most common life-limiting inherited disease in Caucasian populations, affecting approximately 80,000 people worldwide. CF is a complex multi-organ monogenic autosomal recessive disorder caused by a mutation in cystic fibro...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
12 Citations
3,891 Views
12 Pages

14 September 2021

Accumulating evidence indicates a link between diabetes and cancer. Selective estrogen receptor modulators (SERMs) may increase diabetes risk via antiestrogen effects. This study investigated incident diabetes risk of SERM treatment and its effects o...

(This article belongs to the Special Issue Adverse Drug Reactions and Gender Differences)
  • Article
  • Open Access
9 Citations
4,253 Views
17 Pages

Development and Characterisation of Antibody-Based Optical Imaging Probes for Inflammatory Bowel Disease

  • Matthijs David Linssen,
  • Wouter Tjerk Rudolph Hooghiemstra,
  • Annelies Jorritsma-Smit,
  • Derk Pieter Allersma and ,
  • Gerard Dijkstra and
  • Wouter Bastiaan Nagengast
  • + 1 author+ 0 author

13 September 2021

Monoclonal antibodies are an important addition to the medicinal treatment paradigm for IBD patients. While effective, these agents show a high degree of primary and secondary non-response, and methods to predict response are highly desired. Informat...

(This article belongs to the Special Issue Hybrid Agents for Multimodal Imaging)
  • Review
  • Open Access
43 Citations
6,145 Views
19 Pages

Osteosarcoma in Children: Not Only Chemotherapy

  • Maura Argenziano,
  • Chiara Tortora,
  • Elvira Pota,
  • Alessandra Di Paola and ,
  • Martina Di Martino,
  • Caterina Di Leva,
  • Daniela Di Pinto and
  • Francesca Rossi
  • + 3 authors+ 0 author

13 September 2021

Osteosarcoma (OS) is the most severe bone malignant tumor, responsible for altered osteoid deposition and with a high rate of metastasis. It is characterized by heterogeneity, chemoresistance and its interaction with bone microenvironment. The 5-year...

(This article belongs to the Special Issue Osteosarcomas: Treatment Strategies)
  • Perspective
  • Open Access
9 Citations
4,215 Views
10 Pages

13 September 2021

Migraine is the second cause of disability and of lost years of healthy life worldwide. Migraine is characterized by recurrent headache attacks and accompanying disabling symptoms lasting 4–48 h. In episodic migraine, attacks occur in less than 15 da...

(This article belongs to the Section Biopharmaceuticals)
  • Communication
  • Open Access
1 Citations
3,498 Views
9 Pages

Testing the Stability of Drug Resistance on Cryopreserved, Gene-Engineered Human Induced Pluripotent Stem Cells

  • Dilaware Khan,
  • Ann-Christin Nickel,
  • Sebastian Jeising,
  • Constanze Uhlmann and ,
  • Sajjad Muhammad,
  • Daniel Hänggi,
  • Igor Fischer and
  • Ulf Dietrich Kahlert
  • + 3 authors+ 0 author

11 September 2021

Human induced pluripotent stem cells (hiPSCs) have emerged as a powerful tool for in vitro modelling of diseases with broad application in drug development or toxicology testing. These assays usually require large quantities of hiPSC, which can entai...

(This article belongs to the Special Issue Drug Screening or Drug Designing Based on Stem Cell Models)
  • Opinion
  • Open Access
26 Citations
5,357 Views
6 Pages

11 September 2021

The Mediterranean diet (MD), characterized by a high intake of fruits, vegetables, legumes, nuts and grains, a moderate intake of red wine and a reduced consumption of meat, has been considered one of the healthiest dietary patterns worldwide. Growin...

(This article belongs to the Special Issue Anticancer Compounds in Medicinal Plants)
  • Article
  • Open Access
52 Citations
6,429 Views
15 Pages

Use of 3D Printing for the Development of Biodegradable Antiplatelet Materials for Cardiovascular Applications

  • Juan Domínguez-Robles,
  • Luis Diaz-Gomez,
  • Emilia Utomo,
  • Tingjun Shen and ,
  • Camila J. Picco,
  • Carmen Alvarez-Lorenzo,
  • Angel Concheiro,
  • Ryan F. Donnelly and
  • Eneko Larrañeta
  • + 4 authors+ 0 author

11 September 2021

Small-diameter synthetic vascular grafts are required for surgical bypass grafting when there is a lack of suitable autologous vessels due to different reasons, such as previous operations. Thrombosis is the main cause of failure of small-diameter sy...

(This article belongs to the Special Issue Recent Advances in Polymers as Matrices for Drug Delivery Applications)
  • Article
  • Open Access
71 Citations
7,269 Views
14 Pages

Chemical Composition and Antimicrobial Activity of a New Olive Pomace Functional Ingredient

  • Maria Antónia Nunes,
  • Josman Dantas Palmeira,
  • Diana Melo,
  • Susana Machado and ,
  • Joana Correia Lobo,
  • Anabela Sílvia Guedes Costa,
  • Rita Carneiro Alves,
  • Helena Ferreira and
  • Maria Beatriz Prior Pinto Oliveira
  • + 4 authors+ 0 author

10 September 2021

Olive pomace, an olive oil processing byproduct, can be upcycled and meet the current demand for natural and sustainable food ingredients. In this work, a patented process was used to obtain a functional ingredient from different olive pomaces. The n...

(This article belongs to the Special Issue Antiradical, Chemopreventive and Antimicrobial Analysis of Bioactive Substances)
  • Article
  • Open Access
7 Citations
6,895 Views
18 Pages

In Silico-Based Design and In Vivo Evaluation of an Anthranilic Acid Derivative as a Multitarget Drug in a Diet-Induced Metabolic Syndrome Model

  • Héctor González-Álvarez,
  • Astrid Bravo-Jiménez,
  • Matilda Martínez-Arellanes,
  • Gabriela Odette Gamboa-Osorio and ,
  • Edwin Chávez-Gutiérrez,
  • Lino A. González-Hernández,
  • Karina Gallardo-Ignacio,
  • Osvaldo J. Quintana-Romero,
  • Armando Ariza-Castolo and
  • Marco A. Loza-Mejía
  • + 9 authors+ 4 authors

10 September 2021

Metabolic syndrome (MetS) is a complex disease that affects almost a quarter of the world’s adult population. In MetS, diabetes, obesity, hyperglycemia, high cholesterol, and high blood pressure are the most common disorders. Polypharmacy is the most...

(This article belongs to the Special Issue Multitarget Drug Discovery and Pharmacology)
  • Review
  • Open Access
49 Citations
10,472 Views
16 Pages

10 September 2021

The spreading of antibiotic resistance is responsible annually for over 700,000 deaths worldwide, and the prevision is that this number will increase exponentially. The identification of new antimicrobial treatments is a challenge that requires scien...

(This article belongs to the Collection Old Pharmaceuticals with New Applications)
  • Article
  • Open Access
2 Citations
2,761 Views
16 Pages

Chemoreversal Agents from Taiwanofungus Genus and Their More Potent Methyl Derivatives Targeting Signal Transducer and Activator of Transcription 3 (STAT3) Phosphorylation

  • Ko-Hua Yu,
  • Chin-Chuan Hung,
  • Tian-Shung Wu,
  • Chin-Fu Chen and ,
  • I-Ting Wu,
  • Ping-Chung Kuo,
  • Sio-Hong Lam and
  • Hsin-Yi Hung
  • + 3 authors+ 0 author

10 September 2021

Multidrug resistance (MDR), for which the mechanisms are not yet fully clear, is one of the major obstacles to cancer treatment. In recent years, signal transducer and activator of transcription 3 (STAT3) were found to be one of the important MDR mec...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
8 Citations
4,625 Views
17 Pages

Antifungal Activity of Extracts, Fractions, and Constituents from Coccoloba cowellii Leaves

  • Daniel Méndez,
  • Julio C. Escalona-Arranz,
  • Enrique Molina Pérez,
  • Kenn Foubert and ,
  • An Matheeussen,
  • Emmy Tuenter,
  • Ann Cuypers,
  • Paul Cos and
  • Luc Pieters
  • + 4 authors+ 0 author

10 September 2021

Coccoloba cowellii Britton (Polygonaceae, order Caryophyllales) is an endemic and critically endangered plant species that only grows in the municipality of Camagüey, a province of Cuba. A preliminary investigation of its total methanolic extract led...

(This article belongs to the Special Issue Natural Pharmacons: Biologically Active Plant Based Pharmaceuticals)
  • Article
  • Open Access
3 Citations
3,586 Views
14 Pages

10 September 2021

Many recent efforts have been put into the association between expression heterogeneity and different cell types and states using single-cell RNA transcriptome analysis. There is only limited understanding of gene dosage effects for the genetic heter...

(This article belongs to the Special Issue Potential Molecular Targets and Therapeutics in Triple-Negative Breast Cancer)
  • Article
  • Open Access
15 Citations
3,377 Views
15 Pages

Gemcitabine Direct Electrochemical Detection from Pharmaceutical Formulations Using a Boron-Doped Diamond Electrode

  • Iulia Rus,
  • Alexandra Pusta,
  • Mihaela Tertiș,
  • Cristina Barbălată and ,
  • Ioan Tomuță,
  • Robert Săndulescu and
  • Cecilia Cristea
  • + 2 authors+ 0 author

10 September 2021

The development of fast and easy-to-use methods for gemcitabine detection is of great interest for pharmaceutical formulation control in both research laboratories and hospitals. In this study, we report a simple, fast and direct electrochemical meth...

(This article belongs to the Section Pharmaceutical Technology)
  • Article
  • Open Access
8 Citations
5,175 Views
13 Pages

Transient Receptor Potential Ankyrin-1 (TRPA1) Block Protects against Loss of White Matter Function during Ischaemia in the Mouse Optic Nerve

  • Wendy Lajoso,
  • Grace Flower,
  • Vincenzo Giacco,
  • Anjuli Kaul and ,
  • Circe La Mache,
  • Andra Brăban,
  • Angela Roxas and
  • Nicola B. Hamilton
  • + 3 authors+ 0 author

9 September 2021

Oligodendrocytes produce myelin, which provides insulation to axons and speeds up neuronal transmission. In ischaemic conditions, myelin is damaged, resulting in mental and physical disabilities. Recent evidence suggests that oligodendrocyte damage d...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
5 Citations
4,233 Views
16 Pages

If It Works, Don’t Touch It? A Cell-Based Approach to Studying 2-[18F]FDG Metabolism

  • Eva-Maria Klebermass,
  • Mahshid Mahmudi,
  • Barbara Katharina Geist,
  • Verena Pichler and ,
  • Chrysoula Vraka,
  • Theresa Balber,
  • Anne Miller,
  • Arvand Haschemi,
  • Helmut Viernstein and
  • Markus Mitterhauser
  • + 7 authors+ 2 authors

9 September 2021

The glucose derivative 2-[18F]fluoro-2-deoxy-D-glucose (2-[18F]FDG) is still the most used radiotracer for positron emission tomography, as it visualizes glucose utilization and energy demand. In general, 2-[18F]FDG is said to be trapped intracellula...

(This article belongs to the Section Radiopharmaceutical Sciences)
  • Article
  • Open Access
4 Citations
3,835 Views
15 Pages

Flavanonol Glycosides from the Stems of Myrsine seguinii and Their Neuroprotective Activities

  • Hee-Ju Lee,
  • Eun-Jin Park,
  • Ba-Wool Lee,
  • Hyo-Moon Cho and ,
  • Thi-Linh-Giang Pham,
  • Quynh-Hoa Hoang,
  • Cheol-Ho Pan and
  • Won-Keun Oh
  • + 3 authors+ 0 author

9 September 2021

The accumulation of amyloid beta (Aβ) peptides is common in the brains of patients with Alzheimer’s disease, who are characterized by neurological cognitive impairment. In the search for materials with inhibitory activity against the accumulation of...

(This article belongs to the Section Natural Products)
  • Article
  • Open Access
10 Citations
5,214 Views
25 Pages

Semaphorin 3A—Glycosaminoglycans Interaction as Therapeutic Target for Axonal Regeneration

  • Yolanda Pérez,
  • Roman Bonet,
  • Miriam Corredor,
  • Cecilia Domingo and ,
  • Alejandra Moure,
  • Àngel Messeguer,
  • Jordi Bujons and
  • Ignacio Alfonso
  • + 3 authors+ 0 author

7 September 2021

Semaphorin 3A (Sema3A) is a cell-secreted protein that participates in the axonal guidance pathways. Sema3A acts as a canonical repulsive axon guidance molecule, inhibiting CNS regenerative axonal growth and propagation. Therefore, interfering with S...

(This article belongs to the Special Issue High Field NMR and Ultra-High Field NMR in Medicinal Chemistry)
  • Article
  • Open Access
20 Citations
4,159 Views
14 Pages

Benzydamine Reverses TMexCD-TOprJ-Mediated High-Level Tigecycline Resistance in Gram-Negative Bacteria

  • Ziwen Tong,
  • Tianqi Xu,
  • Tian Deng,
  • Jingru Shi and ,
  • Zhiqiang Wang and
  • Yuan Liu
  • + 1 author+ 0 author

7 September 2021

Recently, a novel efflux pump gene cluster called tmexCD1-toprJ1 and its variants have been identified, which undermine the antibacterial activity of tigecycline, one of the last remaining options effective against multidrug-resistant (MDR) Gram-nega...

(This article belongs to the Special Issue Mechanisms of Antibiotic Action and Resistance)
  • Article
  • Open Access
19 Citations
5,027 Views
20 Pages

Potential and Limits of Kidney Cells for Evaluation of Renal Excretion

  • Christian Lechner,
  • Ursula Mönning,
  • Andreas Reichel and
  • Gert Fricker

7 September 2021

A large number of therapeutic drugs, herbal components and their metabolites are excreted by the kidneys. Therefore, generally applied models for estimating renal excretion, including freshly isolated rat proximal tubule cells, cultured tubule cells...

(This article belongs to the Special Issue Promising Anti-inflammatory Medicinal Plants—An Assessment of Bioavailability, Pharmacokinetics, Clinical Efficacy and Overview of New Methodological Approaches)
  • Review
  • Open Access
23 Citations
5,525 Views
21 Pages

Population Pharmacokinetics of Colistin Methanesulfonate Sodium and Colistin in Critically Ill Patients: A Systematic Review

  • Mohd Shafie Zabidi,
  • Ruzilawati Abu Bakar,
  • Nurfadhlina Musa,
  • Suzana Mustafa and
  • Wan Nazirah Wan Yusuf

6 September 2021

Understanding the pharmacokinetics parameter of colistin methanesulfonate sodium (CMS) and colistin is needed to optimize the dosage regimen in critically ill patients. However, there is a scarcity of pharmacokinetics parameters in this population. T...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
18 Citations
4,857 Views
14 Pages

Targeting the Bromodomain of BRG-1/BRM Subunit of the SWI/SNF Complex Increases the Anticancer Activity of Temozolomide in Glioblastoma

  • Chuanhe Yang,
  • Yinan Wang,
  • Michelle M. Sims,
  • Yali He and ,
  • Duane D. Miller and
  • Lawrence M. Pfeffer
  • + 1 author+ 0 author

6 September 2021

Glioblastoma (GBM) is a deadly and incurable brain cancer with limited therapeutic options. PFI-3 is a small-molecule bromodomain (BRD) inhibitor of the BRM/BRG1 subunits of the SWI/SNF chromatin remodeling complex. The objective of this study is to...

(This article belongs to the Section Medicinal Chemistry)
  • Review
  • Open Access
8 Citations
5,213 Views
19 Pages

Clinical Application of Pharmacogenetic Markers in the Treatment of Dermatologic Pathologies

  • Cristina Membrive Jiménez,
  • Cristina Pérez Ramírez,
  • Almudena Sánchez Martín,
  • Sayleth Vieira Maroun and ,
  • Salvador Arias Santiago,
  • María Carmen Ramírez Tortosa and
  • Alberto Jiménez Morales
  • + 2 authors+ 0 author

6 September 2021

Dermatologic pathologies are the fourth most common cause of non-fatal disease worldwide; however, they produce a psychosocial, economic, and occupational impact equal to or greater than other chronic conditions. The most prevalent are actinic kerato...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
23 Citations
4,111 Views
14 Pages

5 September 2021

Although various methods, such as surgery and chemotherapy, are applied to the treatment of OSCC, there are problems, such as functional and aesthetic limitations of the mouth and face, drug side effects, and lymph node metastasis. Many researchers a...

(This article belongs to the Section Natural Products)
  • Article
  • Open Access
2 Citations
3,053 Views
10 Pages

Subchronic Toxicity Study of Oral Anthrafuran on Rabbits

  • Michael I. Treshchalin,
  • Helen M. Treshalina,
  • Vasilisa A. Golibrodo,
  • Andrey E. Shchekotikhin and
  • Eleonora R. Pereverzeva

4 September 2021

A new antitumor multi-target drug anthrafuran, with cellular targets such as topoisomerase I/II and some protein kinases, was obtained in Gause Institute of New Antibiotics and was demonstrated to have a reliable specific effect on different murine a...

(This article belongs to the Special Issue Recent Advance in Oral Drug Delivery Development)
  • Article
  • Open Access
14 Citations
5,408 Views
24 Pages

Caesalpinia mimosoides Leaf Extract Promotes Neurite Outgrowth and Inhibits BACE1 Activity in Mutant APP-Overexpressing Neuronal Neuro2a Cells

  • Panthakarn Rangsinth,
  • Chatrawee Duangjan,
  • Chanin Sillapachaiyaporn,
  • Ciro Isidoro and ,
  • Anchalee Prasansuklab and
  • Tewin Tencomnao
  • + 1 author+ 0 author

4 September 2021

Alzheimer’s disease (AD) is implicated in the imbalance of several proteins, including Amyloid-β (Aβ), amyloid precursor protein (APP), and BACE1. APP overexpression interferes with neurite outgrowth, while BACE1 plays a role in Aβ generation. Medici...

(This article belongs to the Special Issue Natural Bioactive Compounds and Neurological Disorders: Exploiting Resources from Nature)
  • Article
  • Open Access
30 Citations
5,848 Views
24 Pages

3 September 2021

The unprecedented pandemic of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is threatening global health. SARS-CoV-2 has caused severe disease with significant mortality since December 2019. The enzyme chymotrypsin-like protease (3CLpr...

(This article belongs to the Special Issue In Silico Approaches in Drug Design)
  • Article
  • Open Access
10 Citations
4,707 Views
13 Pages

Covalent 18F-Radiotracers for SNAPTag: A New Toolbox for Reporter Gene Imaging

  • Sophie Stotz,
  • Gregory D. Bowden,
  • Jonathan M. Cotton,
  • Bernd J. Pichler and
  • Andreas Maurer

3 September 2021

There is a need for versatile in vivo nuclear imaging reporter systems to foster preclinical and clinical research. We explore the applicability of the SNAPTag and novel radiolabeled small-molecule ligands as a versatile reporter gene system for in v...

(This article belongs to the Special Issue Targets, Tracers and Translation, Part 2 - New Horizons in Radiopharmaceutical Development)
  • Article
  • Open Access
7 Citations
4,264 Views
16 Pages

RTK25: A Comprehensive Molecular Profiling Strategy in Cholangiocarcinoma Using an Integrated Bioinformatics Approach

  • Brinda Balasubramanian,
  • Simran Venkatraman,
  • Tavan Janvilisri,
  • Tuangporn Suthiphongchai and ,
  • Siriporn Jitkaew,
  • Jittiyawadee Sripa and
  • Rutaiwan Tohtong
  • + 2 authors+ 0 author

3 September 2021

Cholangiocarcinoma (CCA) is a heterogeneous group of malignancies that primarily originate from the bile duct. Tumor heterogeneity is a prime characteristic of CCA and considering the scarcity of approved targeted therapy drugs, this makes precision...

(This article belongs to the Special Issue Cancer Translational Biomarkers and Targeted Therapies)
  • Article
  • Open Access
3 Citations
3,808 Views
14 Pages

3 September 2021

Background: This study measures the use of drugs within the therapeutic areas of antithrombotic agents (B01), the cardiovascular system (C), analgesics (N02), psycholeptics (N05), and psychoanaleptics (N06) among the general population (GP) in compar...

(This article belongs to the Special Issue Clinical Utility of Applying PGx and Deprescribing-Based Decision Support in Polypharmacy: Future Perspectives)

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Pharmaceuticals - ISSN 1424-8247