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Pharmaceuticals, Volume 16, Issue 7

2023 July - 147 articles

Cover Story: Cyclic peptides are molecules that are already used as drugs in therapies approved for various pharmacological activities, for example, as antibiotics, antifungals, anticancer, and immunosuppressants. Interest in these molecules has been growing due to the improved pharmacokinetic and pharmacodynamic properties of the cyclic structure over linear peptides and by the evolution of chemical synthesis, computational, and in vitro methods. To date, 53 cyclic peptides have been approved by different regulatory authorities, and many others are in clinical trials for a wide diversity of conditions. In this review, the potential of cyclic peptides is presented, and general aspects of their synthesis and development are discussed. Furthermore, an overview of already approved cyclic peptides is also given, and the cyclic peptides in clinical trials are summarized. View this paper
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Articles (147)

  • Review
  • Open Access
8 Citations
9,670 Views
32 Pages

Peptide Vaccines as Therapeutic and Prophylactic Agents for Female-Specific Cancers: The Current Landscape

  • Manju Lekshmy,
  • Chandrasekharan Rajalekshmi Dhanya,
  • Jayashree SatheeshKumar Smrithi,
  • Janaki Anandavallyamma Sindhurani,
  • Jiji Joseph Vandanamthadathil,
  • Jayakrishnan Therthala Veettil,
  • Leelamma Anila,
  • Vishnu Sasidharan Lathakumari,
  • Adhira M. Nayar and
  • Maya Madhavan

24 July 2023

Breast and gynecologic cancers are significant global threats to women’s health and those living with the disease require lifelong physical, financial, and social support from their families, healthcare providers, and society as a whole. Cancer...

(This article belongs to the Topic Peptoids and Peptide Based Drugs)
  • Article
  • Open Access
7 Citations
4,324 Views
16 Pages

Anti-Obesity Effect of Chlorin e6-Mediated Photodynamic Therapy on Mice with High-Fat-Diet-Induced Obesity

  • Rajeev Shrestha,
  • Pallavi Gurung,
  • Junmo Lim,
  • Til Bahadur Thapa Magar,
  • Cheong-Wun Kim,
  • Hak Yong Lee and
  • Yong-Wan Kim

24 July 2023

This study aimed to evaluate the efficacy of Chlorin e6 (Ce6)-based photodynamic therapy (PDT) for anti-obesity activities in high-fat-diet (HFD)-induced obesity mouse models. We induced obesity in C57BL/6 mice by HFD and administered Ce6 (2.5 or 5 m...

(This article belongs to the Section Pharmaceutical Technology)
  • Review
  • Open Access
13 Citations
11,379 Views
31 Pages

Stable Gastric Pentadecapeptide BPC 157—Possible Novel Therapy of Glaucoma and Other Ocular Conditions

  • Predrag Sikiric,
  • Antonio Kokot,
  • Tamara Kralj,
  • Mirna Zlatar,
  • Sanja Masnec,
  • Ratimir Lazic,
  • Kristina Loncaric,
  • Katarina Oroz,
  • Marko Sablic and
  • Mario Staresinic
  • + 14 authors

24 July 2023

Recently, stable gastric pentadecapeptide BPC 157 therapy by activation of collateral pathways counteracted various occlusion/occlusion-like syndromes, vascular, and multiorgan failure, and blood pressure disturbances in rats with permanent major ves...

(This article belongs to the Section Biopharmaceuticals)
  • Article
  • Open Access
6 Citations
3,202 Views
19 Pages

On the Road towards Small-Molecule Programmed Cell Death 1 Ligand 1 Positron Emission Tomography Tracers: A Ligand-Based Drug Design Approach

  • Karsten Bamminger,
  • Verena Pichler,
  • Chrysoula Vraka,
  • Tina Nehring,
  • Katharina Pallitsch,
  • Barbara Lieder,
  • Marcus Hacker and
  • Wolfgang Wadsak

24 July 2023

PD-1/PD-L1 immune checkpoint blockade for cancer therapy showed promising results in clinical studies. Further endeavors are required to enhance patient stratification, as, at present, only a small portion of patients with PD-L1-positive tumors (as d...

(This article belongs to the Special Issue Tumor-Targeting Radioligands for Molecular Imaging and Therapy)
  • Review
  • Open Access
37 Citations
12,390 Views
18 Pages

Advances in the Applications of Bioinformatics and Chemoinformatics

  • Mohamed A. Raslan,
  • Sara A. Raslan,
  • Eslam M. Shehata,
  • Amr S. Mahmoud and
  • Nagwa A. Sabri

24 July 2023

Chemoinformatics involves integrating the principles of physical chemistry with computer-based and information science methodologies, commonly referred to as “in silico techniques”, in order to address a wide range of descriptive and pres...

(This article belongs to the Special Issue New Perspectives on Chemoinformatics and Drug Design)
  • Review
  • Open Access
38 Citations
18,117 Views
35 Pages

The Skin and Natural Cannabinoids–Topical and Transdermal Applications

  • Silviu-Iulian Filipiuc,
  • Anca-Narcisa Neagu,
  • Cristina Mariana Uritu,
  • Bogdan-Ionel Tamba,
  • Leontina-Elena Filipiuc,
  • Ivona Maria Tudorancea,
  • Andreea Nicoleta Boca,
  • Mădălina Florina Hâncu,
  • Vlad Porumb and
  • Walther Bild

24 July 2023

The chemical constituents of the Cannabis plant known as cannabinoids have been extensively researched for their potential therapeutic benefits. The use of cannabinoids applied to the skin as a potential method for both skin-related benefits and syst...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
10 Citations
3,729 Views
13 Pages

Renoprotective Effect of Chrysanthemum coronarium L. Extract on Adenine-Induced Chronic Kidney Disease in Mice

  • Yi-Seul Kim,
  • Ae-Sin Lee,
  • Haeng-Jeon Hur,
  • Sang-Hee Lee,
  • Hyun-Jin Na and
  • Mi-Jeong Sung

24 July 2023

Chronic kidney disease (CKD) gradually leads to loss of renal function and is associated with inflammation and fibrosis. Chrysanthemum coronarium L., a leafy vegetable, possesses various beneficial properties, including anti-oxidative, anti-inflammat...

(This article belongs to the Special Issue Pharmacological Studies of Medicinal Potential Phytochemicals in Plant Roots)
  • Article
  • Open Access
12 Citations
8,041 Views
34 Pages

Global Research Trends and Hotspots Analysis of the Scientific Production of Amitriptyline: A Bibliometric Approach

  • Cristian dos Santos Pereira,
  • Jorddy Neves Cruz,
  • Maria Karolina Martins Ferreira,
  • Daiane Claydes Baia-da-Silva,
  • Eneas Andrade Fontes-Junior and
  • Rafael Rodrigues Lima

24 July 2023

Amitriptyline was first introduced as a medication to treat depression. Over time, this substance has been used to treat other conditions, such as gastrointestinal disorders, fibromyalgia, neuropathic pain, and analgesia, among others. However, there...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
3 Citations
3,801 Views
39 Pages

Novel Lipophilic Hydroxamates Based on Spirocarbocyclic Hydantoin Scaffolds with Potent Antiviral and Trypanocidal Activity

  • Vasiliki Pardali,
  • Erofili Giannakopoulou,
  • George Mpekoulis,
  • Vassilina Tsopela,
  • Georgios Panos,
  • Martin C. Taylor,
  • John M. Kelly,
  • Niki Vassilaki and
  • Grigoris Zoidis

24 July 2023

Flaviviridae infections, such as those caused by hepatitis C (HCV) and dengue viruses (DENVs), represent global health risks. Infected people are in danger of developing chronic liver failure or hemorrhagic fever, both of which can be fatal if not tr...

(This article belongs to the Special Issue Antiviral Drugs 2021)
  • Article
  • Open Access
39 Citations
4,618 Views
19 Pages

Synthesis, Computational Studies, Antioxidant and Anti-Inflammatory Bio-Evaluation of 2,5-Disubstituted-1,3,4-Oxadiazole Derivatives

  • Sibghat Mansoor Rana,
  • Muhammad Islam,
  • Hamid Saeed,
  • Hummera Rafique,
  • Muhammad Majid,
  • Muhammad Tahir Aqeel,
  • Fariha Imtiaz and
  • Zaman Ashraf

24 July 2023

The 1,3,4-oxadiazole derivatives Ox-6a-f have been synthesized by incorporating flurbiprofen moiety with the aim to explore the potential of target molecules to decrease the oxidative stress. The title compounds Ox-6a-f were prepared by simple reacti...

(This article belongs to the Section Medicinal Chemistry)
  • Review
  • Open Access
38 Citations
6,370 Views
30 Pages

23 July 2023

Oxidative stress is an important, but elusive, therapeutic target for osteoarthritis (OA). Antioxidant strategies that target oxidative stress through the elimination of reactive oxygen species (ROS) have been widely evaluated for OA but are limited...

(This article belongs to the Special Issue Feature Reviews in Pharmaceutical Technology)
  • Review
  • Open Access
13 Citations
5,116 Views
24 Pages

Chemical Constituents and Their Biological Activities from Genus Styrax

  • Ding-Ding Xia,
  • Xin-Yu Han,
  • Yu Zhang and
  • Na Zhang

22 July 2023

Plants from the genus Styrax have been extensively used in folk medicines to treat diseases such as skin diseases and peptic ulcers and as an antiseptic and analgesic. Most Styrax species, especially Styrax tonkinensis, which is used as an expectoran...

(This article belongs to the Special Issue Discovery, Metabolism and Potential Bio-Activities of Natural Products in Traditional Medicine)
  • Review
  • Open Access
8 Citations
4,558 Views
29 Pages

Smart Sensors and Microtechnologies in the Precision Medicine Approach against Lung Cancer

  • Giulia Maria Stella,
  • Sara Lettieri,
  • Davide Piloni,
  • Ilaria Ferrarotti,
  • Fabio Perrotta,
  • Angelo Guido Corsico and
  • Chandra Bortolotto

22 July 2023

Background and rationale. The therapeutic interventions against lung cancer are currently based on a fully personalized approach to the disease with considerable improvement of patients’ outcome. Alongside continuous scientific progresses and r...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
15 Citations
10,212 Views
17 Pages

Probiotic Formulations Containing Fixed and Essential Oils Ameliorates SIBO-Induced Gut Dysbiosis in Rats

  • Ismail Aslan,
  • Leyla Tarhan Celebi,
  • Hulya Kayhan,
  • Emine Kizilay,
  • Mustafa Yavuz Gulbahar,
  • Halil Kurt and
  • Bekir Cakici

22 July 2023

Dysbiosis of the gut microbiota is associated with the pathogenesis of intestinal diseases such as inflammatory bowel disease, irritable bowel syndrome (IBS), small intestinal bacterial overgrowth (SIBO), and metabolic disease states such as allergie...

(This article belongs to the Special Issue Gut Microbiota Modulation: Probiotics, Postbiotics and other Bioactive Compounds)
  • Article
  • Open Access
12 Citations
3,309 Views
14 Pages

Small Molecules Incorporating Privileged Amidine Moiety as Potential Hits Combating Antibiotic-Resistant Bacteria

  • Selwan M. El-Sayed,
  • Samar A. Ahmed,
  • Kanika Gulia,
  • Justin R. Lenhard,
  • Ahmed H.E. Hassan and
  • Abdelbasset A. Farahat

22 July 2023

The continuing need for the discovery of potent antibacterial agents against antibiotic-resistant pathogens is the driving force for many researchers to design and develop such agents. Herein, we report the design, synthesis, and biological evaluatio...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
20 Citations
4,620 Views
23 Pages

Design, Synthesis, and Biological Evaluation of Indole-2-carboxamides as Potential Multi-Target Antiproliferative Agents

  • Lamya H. Al-Wahaibi,
  • Anber F. Mohammed,
  • Mostafa H. Abdelrahman,
  • Laurent Trembleau and
  • Bahaa G. M. Youssif

22 July 2023

A small set of indole-based derivatives, IV and Va–I, was designed and synthesized. Compounds Va–i demonstrated promising antiproliferative activity, with GI50 values ranging from 26 nM to 86 nM compared to erlotinib’s 33 nM. The mo...

(This article belongs to the Special Issue The 20th Anniversary of Pharmaceuticals—Advances in Medicinal Chemistry)
  • Article
  • Open Access
2 Citations
3,883 Views
14 Pages

21 July 2023

Background: There have been significant advancements in melanoma therapies. BET inhibitors (BETis) show promise in impairing melanoma growth. However, identifying BETi-sensitive melanoma subtypes is challenging. Methods and Results: We analyzed 48 me...

(This article belongs to the Special Issue Pharmacological Treatments for Melanoma)
  • Review
  • Open Access
17 Citations
4,541 Views
38 Pages

Innovative Delivery and Release Systems for Antioxidants and Other Active Substances in the Treatment of Cancer

  • Zerrin Sezgin-Bayindir,
  • Sonia Losada-Barreiro,
  • Sofía Fernández-Bravo and
  • Carlos Bravo-Díaz

21 July 2023

Cancer is one of the major diseases leading to death worldwide, and the fight against the disease is still challenging. Cancer diseases are usually associated with increased oxidative stress and the accumulation of reactive oxygen and nitrogen specie...

(This article belongs to the Special Issue Molecular and Cellular Studies of Natural Antioxidants as Potential Therapeutics for Cancer)
  • Review
  • Open Access
18 Citations
6,865 Views
17 Pages

Pomegranate: A Source of Multifunctional Bioactive Compounds Potentially Beneficial in Alzheimer’s Disease

  • Lidia Ciccone,
  • Susanna Nencetti,
  • Armando Rossello and
  • Elisabetta Orlandini

21 July 2023

Pomegranate fruit (PF) is a fruit rich in nutraceuticals. Nonedible parts of the fruit, especially peels, contain high amounts of bioactive components that have been largely used in traditional medicine, such as the Chinese, Unani, and Ayurvedic ones...

(This article belongs to the Special Issue Medicinal Plants and Natural Compounds for Potential Use in Aging-Related Disorders)
  • Article
  • Open Access
4 Citations
2,268 Views
11 Pages

21 July 2023

Bisphosphonate-related osteonecrosis of the jaw (BRONJ) is a rare but severe adverse effect that can occur as a result of bisphosphonate treatment. This study aimed to examine the relationship between PPARγ and PPARGC1A polymorphisms and the BR...

(This article belongs to the Special Issue Pharmacogenomics - A Genetic Approach to Drug Therapy and Development)
  • Article
  • Open Access
11 Citations
3,682 Views
12 Pages

Amlexanox: Readthrough Induction and Nonsense-Mediated mRNA Decay Inhibition in a Charcot–Marie–Tooth Model of hiPSCs-Derived Neuronal Cells Harboring a Nonsense Mutation in GDAP1 Gene

  • Nesrine Benslimane,
  • Federica Miressi,
  • Camille Loret,
  • Laurence Richard,
  • Angélique Nizou,
  • Ioanna Pyromali,
  • Pierre-Antoine Faye,
  • Frédéric Favreau,
  • Fabrice Lejeune and
  • Anne-Sophie Lia

21 July 2023

Nonsense mutations are involved in multiple peripheral neuropathies. These mutations induce the presence of a premature termination codon (PTC) at the mRNA level. As a result, a dysfunctional or truncated protein is synthesized, or even absent linked...

(This article belongs to the Special Issue Recent Advances in the Pharmacology of Peripheral Neuropathy)
  • Article
  • Open Access
4 Citations
2,823 Views
19 Pages

EYE-503: A Novel Retinoic Acid Drug for Treating Retinal Neurodegeneration

  • Sha Liu,
  • Yuke Ji,
  • Huan Li,
  • Ling Ren,
  • Junya Zhu,
  • Tianjing Yang,
  • Xiumiao Li,
  • Jin Yao,
  • Xin Cao and
  • Biao Yan

20 July 2023

Retinal neurodegeneration is a major cause of vision loss. Retinoic acid signaling is critical for the maintenance of retinal function, and its dysfunction can cause retinal neurodegeneration. However, the therapeutic effects of retinoic acid drugs o...

(This article belongs to the Section Biopharmaceuticals)
  • Article
  • Open Access
5 Citations
3,478 Views
16 Pages

Isolated Fraction of Gastric-Digested Camel Milk Yogurt with Carao (Cassia grandis) Pulp Fortification Enhances the Anti-Inflammatory Properties of HT-29 Human Intestinal Epithelial Cells

  • Jhunior Abrahan Marcia,
  • Ricardo S. Aleman,
  • Shirin Kazemzadeh,
  • Víctor Manrique Fernández,
  • Daniel Martín Vertedor,
  • Aryana Kayanush and
  • Ismael Montero Fernández

20 July 2023

Functional foods have recently generated a lot of attention among consumers looking for healthy options. Studies have examined yogurt with carao to increase health benefits and probiotic characteristics. It has been determined that carao fruit and ca...

(This article belongs to the Section Natural Products)
  • Article
  • Open Access
2 Citations
3,968 Views
17 Pages

Asthma and COPD: Comparison with International Guidelines and Medication Adherence in Belgium

  • Natacha Biset,
  • Mélanie Lelubre,
  • Stéphanie Pochet and
  • Carine De Vriese

20 July 2023

Asthma and chronic obstructive pulmonary disease (COPD) are major chronic conditions. It is possible to limit their impact by controlling symptoms, which limits exacerbations and worsening of the disease, by choosing the appropriate treatment and ens...

(This article belongs to the Section Pharmaceutical Technology)
  • Review
  • Open Access
32 Citations
25,983 Views
24 Pages

20 July 2023

A potential complication of pharmacotherapy for a given patient is the possibility of various side effects of drugs, which are manifested in many ways and constitute iatrogenic causes of diseases. Among the systemic side effects of drugs, there are a...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
20 Citations
3,609 Views
22 Pages

Gellan Gum/Alginate Microparticles as Drug Delivery Vehicles: DOE Production Optimization and Drug Delivery

  • Henrique Carrêlo,
  • Maria Teresa Cidade,
  • João Paulo Borges and
  • Paula Soares

19 July 2023

Gellan gum is a biocompatible and easily accessible polysaccharide with excellent properties to produce microparticles as drug delivery systems. However, the production methods often fail in reproducibility, compromising the translational potential o...

(This article belongs to the Special Issue Hydrogels for Pharmaceutical and Biomedical Applications)
  • Review
  • Open Access
9 Citations
3,932 Views
40 Pages

Covalent Inhibitors for Neglected Diseases: An Exploration of Novel Therapeutic Options

  • Erick Tavares Marcelino Alves,
  • Filipe Gomes Pernichelle,
  • Lucas Adriano Nascimento,
  • Glaucio Monteiro Ferreira and
  • Elizabeth Igne Ferreira

19 July 2023

Neglected diseases, primarily found in tropical regions of the world, present a significant challenge for impoverished populations. Currently, there are 20 diseases considered neglected, which greatly impact the health of affected populations and res...

(This article belongs to the Special Issue Targeted Covalent Inhibitors in Drug Discovery, Chemical Biology and Beyond)
  • Article
  • Open Access
3 Citations
3,575 Views
16 Pages

Quaternary Ammonium Palmitoyl Glycol Chitosan (GCPQ) Loaded with Platinum-Based Anticancer Agents—A Novel Polymer Formulation for Anticancer Therapy

  • Yvonne Lerchbammer-Kreith,
  • Michaela Hejl,
  • Nadine S. Sommerfeld,
  • Xian Weng-Jiang,
  • Uchechukwu Odunze,
  • Ryan D. Mellor,
  • David G. Workman,
  • Michael A. Jakupec,
  • Andreas G. Schätzlein and
  • Bernhard K. Keppler
  • + 2 authors

19 July 2023

Quaternary ammonium palmitoyl glycol chitosan (GCPQ) has already shown beneficial drug delivery properties and has been studied as a carrier for anticancer agents. Consequently, we synthesised cytotoxic platinum(IV) conjugates of cisplatin, carboplat...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
9 Citations
4,252 Views
16 Pages

Cryptolepine Suppresses Colorectal Cancer Cell Proliferation, Stemness, and Metastatic Processes by Inhibiting WNT/β-Catenin Signaling

  • Jude Tetteh Quarshie,
  • Kwadwo Fosu,
  • Nicholas Awuku Offei,
  • Augustine Kojo Sobo,
  • Osbourne Quaye and
  • Anastasia Rosebud Aikins

19 July 2023

Colorectal cancer (CRC) is the third most frequent cancer and the second leading cause of cancer-related deaths globally. Evidence shows that over 90% of CRC cases are initiated by a deregulated Wingless Integrated Type-1 (WNT)/β-catenin signali...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
27 Citations
4,131 Views
19 Pages

In Vitro and In Silico Evaluation of Antiproliferative Activity of New Isoxazolidine Derivatives Targeting EGFR: Design, Synthesis, Cell Cycle Analysis, and Apoptotic Inducers

  • Fahad Alminderej,
  • Siwar Ghannay,
  • Mohamed O. Elsamani,
  • Fahad Alhawday,
  • Abuzar E. A. E. Albadri,
  • Serag Eldin I. Elbehairi,
  • Mohammad Y. Alfaifi,
  • Adel Kadri and
  • Kaïss Aouadi

19 July 2023

A series of novel enantiopure isoxazolidine derivatives were synthesized and evaluated for their anticancer activities against three human cancer cell lines such as human breast carcinoma (MCF-7), human lung adenocarcinoma (A-549), and human ovarian...

(This article belongs to the Section Medicinal Chemistry)
  • Correction
  • Open Access
1,169 Views
1 Page

Correction: Pacelli et al. Fully Automated, High-Dose Radiosynthesis of [18F]PARPi. Pharmaceuticals 2022, 15, 865

  • Anna Pacelli,
  • Fadi Zarrad,
  • Corentin Warnier,
  • Thibault Gendron,
  • Muhammad Otabashi,
  • Charles Vriamont,
  • Alex Jackson,
  • Wolfgang P. Fendler,
  • Ken Herrmann and
  • Michael Nader

19 July 2023

Corentin Warnier, Thibault Gendron, Muhammad Otabashi, Charles Vriamont and Alex Jackson were not included as authors in the original publication [...]

(This article belongs to the Section Radiopharmaceutical Sciences)
  • Article
  • Open Access
12 Citations
3,922 Views
13 Pages

Mirogabalin Decreases Pain-like Behaviors by Inhibiting the Microglial/Macrophage Activation, p38MAPK Signaling, and Pronociceptive CCL2 and CCL5 Release in a Mouse Model of Neuropathic Pain

  • Renata Zajączkowska,
  • Katarzyna Pawlik,
  • Katarzyna Ciapała,
  • Anna Piotrowska,
  • Agata Ciechanowska,
  • Ewelina Rojewska,
  • Magdalena Kocot-Kępska,
  • Wioletta Makuch,
  • Jerzy Wordliczek and
  • Joanna Mika

19 July 2023

Neuropathic pain is a chronic condition that significantly reduces the quality of life of many patients as a result of ineffective pain relief therapy. For that reason, looking for new analgesics remains an important issue. Mirogabalin is a new gabap...

(This article belongs to the Special Issue Pharmacotherapy of Neuropathic Pain)
  • Article
  • Open Access
6 Citations
2,299 Views
16 Pages

19 July 2023

Cyclodextrin-based delivery systems have been intensively used to improve the bioavailability of drugs through the modification of their pharmaceutically relevant properties, such as solubility, distribution and membrane permeation. The present work...

(This article belongs to the Special Issue Cyclodextrin-Based Drug Delivery System and Its Pharmaceutical and Biomedical Application)
  • Review
  • Open Access
19 Citations
5,711 Views
23 Pages

The Effects of Green Tea Catechins in Hematological Malignancies

  • Fernanda Isabel Della Via,
  • Marisa Claudia Alvarez,
  • Rosanna Tarkany Basting and
  • Sara Teresinha Olalla Saad

18 July 2023

Green tea catechins are bioactive polyphenol compounds which have attracted significant attention for their diverse biological activities and potential health benefits. Notably, epigallocatechin-3-gallate (EGCG) has emerged as a potent apoptosis indu...

(This article belongs to the Section Natural Products)
  • Review
  • Open Access
638 Citations
84,073 Views
31 Pages

18 July 2023

Quercetin, a flavonoid found in fruits and vegetables, has been a part of human diets for centuries. Its numerous health benefits, including antioxidant, antimicrobial, anti-inflammatory, antiviral, and anticancer properties, have been extensively st...

(This article belongs to the Section Natural Products)
  • Article
  • Open Access
11 Citations
2,821 Views
18 Pages

In-Silico Mining of the Toxins Database (T3DB) towards Hunting Prospective Candidates as ABCB1 Inhibitors: Integrated Molecular Docking and Lipid Bilayer-Enhanced Molecular Dynamics Study

  • Mahmoud A. A. Ibrahim,
  • Khlood A. A. Abdeljawaad,
  • Alaa H. M. Abdelrahman,
  • Peter A. Sidhom,
  • Ahmed M. Tawfeek,
  • Gamal A. H. Mekhemer,
  • Mohamed K. Abd El-Rahman,
  • Eslam Dabbish and
  • Tamer Shoeib

18 July 2023

Multidrug resistance (MDR) is one of the most problematic issues in chemotherapeutic carcinoma therapy. The ABCB1 transporter, a drug efflux pump overexpressed in cancer cells, has been thoroughly investigated for its association with MDR. Thus, disc...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
8 Citations
12,086 Views
14 Pages

Efficacy of Pregabalin and Duloxetine in Patients with Painful Diabetic Peripheral Neuropathy (PDPN): A Multi-Centre Phase IV Clinical Trial—BLOSSOM

  • Martin Rakusa,
  • Iris Marolt,
  • Zorica Stevic,
  • Sandra Vuckovic Rebrina,
  • Tatjana Milenkovic and
  • Adam Stepien

18 July 2023

Introduction: Our trial (ClinicalTrials.gov Identifier: NCT04246619) evaluates the efficacy of two generic medications, pregabalin and duloxetine, for treating pain in PDPN patients. Methods: The patients were randomised either into the pregabalin (9...

(This article belongs to the Topic Research in Pharmacological Therapies)
  • Article
  • Open Access
8 Citations
2,674 Views
17 Pages

New Imadazopyrazines with CDK9 Inhibitory Activity as Anticancer and Antiviral: Synthesis, In Silico, and In Vitro Evaluation Approaches

  • Aisha A. Alsfouk,
  • Hanan M. Alshibl,
  • Najla A. Altwaijry,
  • Ashwag Alanazi,
  • Omkulthom AlKamaly,
  • Ahlam Sultan and
  • Bshra A. Alsfouk

18 July 2023

This study describes the synthesis and biological activity of new imadazopyrazines as first-in-class CDK9 inhibitors. The inhibition of CDK9 is a well-established therapeutic target in cancer therapy. The new compounds were assessed using an in vitro...

(This article belongs to the Special Issue Heterocyclic Compounds in Medicinal Chemistry)
  • Review
  • Open Access
24 Citations
7,128 Views
30 Pages

18 July 2023

The iron chelating orphan drug deferiprone (L1), discovered over 40 years ago, has been used daily by patients across the world at high doses (75–100 mg/kg) for more than 30 years with no serious toxicity. The level of safety and the simple, in...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
35 Citations
5,375 Views
17 Pages

LC/MS-MS Analysis of Phenolic Compounds in Hyoscyamus albus L. Extract: In Vitro Antidiabetic Activity, In Silico Molecular Docking, and In Vivo Investigation against STZ-Induced Diabetic Mice

  • Sabrina Lekmine,
  • Ouided Benslama,
  • Kenza Kadi,
  • Antonio Ignacio Martín-García,
  • Mustafa Abdullah Yilmaz,
  • Salah Akkal,
  • Ali Boumegoura,
  • Abdullah S. Alhomida,
  • Mohammad Shamsul Ola and
  • Ahmad Ali

18 July 2023

This study aimed to investigate the chemical composition and antidiabetic properties of cultivated Hyoscyamus albus L. The ethanol extract was analyzed using LC-MS/MS, and 18 distinct phenolic compounds were identified. Among these, p-coumaric acid (...

(This article belongs to the Special Issue Natural Products in Diabetes Mellitus)
  • Article
  • Open Access
22 Citations
3,719 Views
17 Pages

Synthesis and Structure Determination of Substituted Thiazole Derivatives as EGFR/BRAFV600E Dual Inhibitors Endowed with Antiproliferative Activity

  • Lamya H. Al-Wahaibi,
  • Essmat M. El-Sheref,
  • Alaa A. Hassan,
  • S. Bräse,
  • M. Nieger,
  • Bahaa G. M. Youssif,
  • Mahmoud A. A. Ibrahim and
  • Hendawy N. Tawfeek

17 July 2023

2,3,4-trisubstituted thiazoles 3a–i, having a methyl group in position four, were synthesized by the reaction of 1,4-disubstituted thiosemicarbazides with chloroacetone in ethyl acetate/Et3N at room temperature or in ethanol under reflux. The s...

(This article belongs to the Special Issue Novel Anti-proliferative Agents)
  • Article
  • Open Access
19 Citations
4,576 Views
21 Pages

17 July 2023

Ketamine, a racemic mixture of esketamine (S-ketamine) and arketamine (R-ketamine), has received particular attention for its rapid antidepressant and antisuicidal effects. NMDA receptor inhibition has been indicated as one of the main mechanisms of...

(This article belongs to the Special Issue Ketamine and Ketamine Metabolite Pharmacology)
  • Article
  • Open Access
7 Citations
4,318 Views
11 Pages

The Effect of Acetylsalicylic Acid, as a Representative Non-Steroidal Anti-Inflammatory Drug, on the Activity of Myeloperoxidase

  • Beata Gąsowska-Bajger,
  • Kinga Sosnowska,
  • Agnieszka Gąsowska-Bodnar and
  • Lubomir Bodnar

17 July 2023

Background: Acetylsalicylic acid (ASA or aspirin) is one of the world’s most widely used non-steroidal anti-inflammatory drug (NSAID). Numerous studies have shown that the long-term use of aspirin may contribute to longer survival among patient...

  • Review
  • Open Access
2,077 Views
13 Pages

How to Treat Today? Oral and Facial Cancer-Associated Venous Thromboembolism

  • Mária Janíčková,
  • Tomáš Bolek,
  • Lucia Stančiaková,
  • Norbert Nagy,
  • Marián Mokáň and
  • Matej Samoš

17 July 2023

The exact incidence of cancer-associated venous thromboembolism (CA-VTE) in patients with oral and facial cancer (OFC) is not exactly known, and this risk is empirically considered to be low. However, this suggestion may result in disease underdiagno...

(This article belongs to the Special Issue Pharmacotherapy of Thromboembolism)
  • Article
  • Open Access
7 Citations
2,037 Views
14 Pages

Marine Meroterpenoids Isolated from Gongolaria abies-marina Induce Programmed Cell Death in Naegleria fowleri

  • Iñigo Arberas-Jiménez,
  • Rubén L. Rodríguez-Expósito,
  • Desirée San Nicolás-Hernández,
  • Javier Chao-Pellicer,
  • Ines Sifaoui,
  • Ana R. Díaz-Marrero,
  • José J. Fernández,
  • José E. Piñero and
  • Jacob Lorenzo-Morales

17 July 2023

Naegleria fowleri is the causative agent of a central nervous system affecting disease called primary amoebic meningoencephalitis. It is a fulminant disease with a rapid progression that affects mainly children and young adults who report previous wa...

(This article belongs to the Section Natural Products)
  • Review
  • Open Access
10 Citations
4,316 Views
19 Pages

17 July 2023

Kinases play an important role in regulating various intracellular signaling pathways that control cell proliferation, differentiation, survival, and other cellular processes, and their deregulation causes more than 400 diseases. Consequently, macroc...

(This article belongs to the Special Issue Kinase Inhibitors in Targeted Cancer Therapy)
  • Article
  • Open Access
15 Citations
5,666 Views
21 Pages

D-Pinitol Content and Antioxidant and Antidiabetic Activities of Five Bougainvillea spectabilis Willd. Cultivars

  • Fatma Abo-Elghiet,
  • Amal H. Ahmed,
  • Hanan F. Aly,
  • Eman A. Younis,
  • Mohamed A. Rabeh,
  • Saad Ali Alshehri,
  • Khalid S. A. Alshahrani and
  • Shaza A. Mohamed

15 July 2023

Diabetes mellitus is a major challenge for global health, and Bougainvillea spectabilis Willd. (B. spectabilis) is a widely used herbal remedy with diverse cultivars traditionally used for diabetes treatment. However, the comparative efficacy of thes...

(This article belongs to the Special Issue Natural Products in Diabetes Mellitus)
  • Systematic Review
  • Open Access
32 Citations
8,322 Views
18 Pages

Dalbavancin in Bone and Joint Infections: A Systematic Review

  • Sofia Lovatti,
  • Giorgio Tiecco,
  • Alice Mulé,
  • Luca Rossi,
  • Anita Sforza,
  • Martina Salvi,
  • Liana Signorini,
  • Francesco Castelli and
  • Eugenia Quiros-Roldan

15 July 2023

Background: Approved for acute bacterial skin and skin structure infections, dalbavancin (DBV) has gradually acquired over the years a role as an off-label treatment for several infections caused by Gram-positive bacteria even in other anatomical sit...

(This article belongs to the Section Biopharmaceuticals)
  • Article
  • Open Access
24 Citations
4,025 Views
22 Pages

Stimulation of Autophagy by Dapagliflozin Mitigates Cadmium-Induced Testicular Dysfunction in Rats: The Role of AMPK/mTOR and SIRT1/Nrf2/HO-1 Pathways

  • Hany H. Arab,
  • Ebtehal Mohammad Fikry,
  • Shuruq E. Alsufyani,
  • Ahmed M. Ashour,
  • Azza A. K. El-Sheikh,
  • Hany W. Darwish,
  • Abdullah M. Al-Hossaini,
  • Muhammed A. Saad,
  • Muhammad Y. Al-Shorbagy and
  • Ahmed H. Eid

14 July 2023

Cadmium (Cd) is a widespread environmental pollutant that triggers testicular dysfunction. Dapagliflozin is a selective sodium-glucose co-transporter-2 inhibitor with notable antioxidant and anti-apoptotic features. It has shown marked cardio-, reno-...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
8 Citations
4,663 Views
30 Pages

Development and Characterization of Cationic Nanostructured Lipid Carriers as Drug Delivery Systems for miRNA-27a

  • Amina Tucak-Smajić,
  • Ivana Ruseska,
  • Ilse Letofsky-Papst,
  • Edina Vranić and
  • Andreas Zimmer

14 July 2023

Although miRNA-27a has been identified as a promising candidate for miRNA mimic therapy of obesity, its application is limited due to enzymatic degradation and low membrane permeation. To overcome these problems, we developed cationic nanostructured...

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Pharmaceuticals - ISSN 1424-8247