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Pharmaceuticals, Volume 15, Issue 7

2022 July - 138 articles

Cover Story: Commonly in lung cancer, EGFR mutations increase PI3K activity through PKB/AKT activation; in addition, these kinases simultaneously participate in cell metabolism through stimulation of HIF1a expression and mTOR activation. This effect promotes translocation and increased expression of GLUTs and HKs, increasing glycolytic potential. Metformin treatment blocks mTOR activity through AMPK activation, increasing the function of TSC2/RHEB, which inhibits protein synthesis promoted by mTOR and its effectors. In addition, metformin modulates protein and enzymes that regulate key metabolic pathways, such as glycolysis and lipid metabolism, leading to the down-regulation of cell proliferation, migration and protein synthesis. View this paper
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Articles (138)

  • Review
  • Open Access
11 Citations
6,694 Views
26 Pages

Traditional Uses, Phytochemistry, and Pharmacological Properties of the Genus Blechnum—A Narrative Review

  • Emmanuel Nyongesa Waswa,
  • Felix Wambua Muema,
  • Wyclif Ochieng Odago,
  • Elizabeth Syowai Mutinda,
  • Consolata Nanjala,
  • Elijah Mbandi Mkala,
  • Sarah Getachew Amenu,
  • Shi-Xiong Ding,
  • Jing Li and
  • Guang-Wan Hu

Blechnum L. is a genus belonging to the Blechnaceae family with 236 accepted species that grow in intertropical, subtropical, and southern temperate regions. Several species of the genus have long been used in folk medicines to treat a broad spectrum...

(This article belongs to the Special Issue Natural Pharmacons: Biologically Active Plant-Based Pharmaceuticals 2022)
  • Article
  • Open Access
19 Citations
6,985 Views
16 Pages

Siccanin Is a Dual-Target Inhibitor of Plasmodium falciparum Mitochondrial Complex II and Complex III

  • Keisuke Komatsuya,
  • Takaya Sakura,
  • Kazuro Shiomi,
  • Satoshi Ōmura,
  • Kenji Hikosaka,
  • Tomoyoshi Nozaki,
  • Kiyoshi Kita and
  • Daniel Ken Inaoka

Plasmodium falciparum contains several mitochondrial electron transport chain (ETC) dehydrogenases shuttling electrons from the respective substrates to the ubiquinone pool, from which electrons are consecutively transferred to complex III, complex I...

(This article belongs to the Special Issue Drug Candidates for the Treatment of Infectious Diseases)
  • Article
  • Open Access
5 Citations
3,464 Views
10 Pages

Diabetes is commonly treated with glucagon-like peptide-1 receptor (GLP-1R) agonists including liraglutide and others. However, liraglutide was found to raise plasma glucose levels in normal rats. The current study aims to determine how liraglutide c...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
4 Citations
3,985 Views
13 Pages

Sensitive Detection of Pharmaceutical Drugs and Metabolites in Serum Using Data-Independent Acquisition Mass Spectrometry and Open-Access Data Acquisition Tools

  • Syed Muhammad Zaki Shah,
  • Arslan Ali,
  • Muhammad Noman Khan,
  • Adeeba Khadim,
  • Mufarreh Asmari,
  • Jalal Uddin and
  • Syed Ghulam Musharraf

Data-independent acquisition (DIA) based strategies have been explored in recent years for improving quantitative analysis of metabolites. However, the data analysis is challenging for DIA methods as the resulting spectra are highly multiplexed. Thus...

(This article belongs to the Section Pharmaceutical Technology)
  • Article
  • Open Access
21 Citations
3,646 Views
17 Pages

Naturally Occurring 8ß,13ß-kaur-15-en-17-al and Anti-Malarial Activity from Podocarpus polystachyus Leaves

  • Mira Syahfriena Amir Rawa,
  • Mohammad G. Al-Thiabat,
  • Toshihiko Nogawa,
  • Yushi Futamura,
  • Akiko Okano and
  • Habibah A. Wahab

Despite much interest and studies toward the genus Podocarpus, the anti-malarial evaluation of Podocarpus polystachyus’s phytoconstituents remains lacking. Herein, the phytoconstituents of P. polystachyus leaves and their anti-malarial effect a...

(This article belongs to the Special Issue Botanicals: Bioactive Molecules and Therapeutic Properties for Human Health 2021)
  • Article
  • Open Access
8 Citations
4,132 Views
16 Pages

Novel p38 Mitogen-Activated Protein Kinase Inhibitor Reverses Hypoxia-Induced Pulmonary Arterial Hypertension in Rats

  • Grazielle Fernandes Silva,
  • Jaqueline Soares da Silva,
  • Allan Kardec Nogueira de Alencar,
  • Marina de Moraes Carvalho da Silva,
  • Tadeu Lima Montagnoli,
  • Bruna de Souza Rocha,
  • Rosana Helena Coimbra Nogueira de Freitas,
  • Roberto Takashi Sudo,
  • Carlos Alberto Manssour Fraga and
  • Gisele Zapata-Sudo

Mitogen-activated protein kinase (MAPK) signaling is strongly implicated in cardiovascular remodeling in pulmonary hypertension (PH) and right ventricle (RV) failure. The effects of a newly designed p38 inhibitor, LASSBio-1824, were investigated in e...

(This article belongs to the Section Pharmacology)
  • Review
  • Open Access
13 Citations
4,613 Views
12 Pages

Phosphodiesterase-4 Inhibitor Roflumilast-Mediated Protective Effect in Sepsis-Induced Late-Phase Event of Acute Kidney Injury: A Narrative Review

  • Imran Kazmi,
  • Fahad A. Al-Abbasi,
  • Muhammad Afzal,
  • Muhammad Shahid Nadeem,
  • Hisham N. Altayb and
  • Gaurav Gupta

Severe infections such as viral, bacterial, or fungal sepsis can cause an inflammatory response in the host, leading to organ failure and septic shock—phosphodiesterase-4 (PDE-4) inhibiting related agents from suppressing cyclic adenosine monop...

(This article belongs to the Special Issue Phosphodiesterases as Drug Targets: Development and Challenges)
  • Review
  • Open Access
13 Citations
9,681 Views
16 Pages

Post-traumatic stress disorder (PTSD) occurs after exposure to traumatic events and is characterized by overwhelming fear and anxiety. Disturbances in the hypothalamic–pituitary–adrenal (HPA) axis are involved in the pathogenesis of mood...

(This article belongs to the Special Issue Therapeutic Agents for Neurological Disorders 2022)
  • Review
  • Open Access
104 Citations
30,415 Views
17 Pages

The Future of Tissue-Targeted Lipid Nanoparticle-Mediated Nucleic Acid Delivery

  • Ruvanthi N. Kularatne,
  • Rachael M. Crist and
  • Stephan T. Stern

The earliest example of in vivo expression of exogenous mRNA is by direct intramuscular injection in mice without the aid of a delivery vehicle. The current state of the art for therapeutic nucleic acid delivery is lipid nanoparticles (LNP), which ar...

(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems)
  • Article
  • Open Access
16 Citations
3,896 Views
12 Pages

Phloridzin Reveals New Treatment Strategies for Liver Fibrosis

  • Yahong Shi,
  • Tun Yan,
  • Xi Lu,
  • Kai Li,
  • Yifeng Nie,
  • Chuqiao Jiao,
  • Huizhen Sun,
  • Tingting Li,
  • Xiang Li and
  • Dong Han

Liver fibrosis is an urgent public health problem which is difficult to resolve. However, various drugs for the treatment of liver fibrosis in clinical practice have their own problems during use. In this study, we used phloridzin to treat hepatic fi...

(This article belongs to the Section Natural Products)
  • Review
  • Open Access
2 Citations
5,440 Views
21 Pages

Druggable Targets and Compounds with Both Antinociceptive and Antipruritic Effects

  • Hao-Jui Weng,
  • Quoc Thao Trang Pham,
  • Chia-Wei Chang and
  • Tsen-Fang Tsai

Pain and itch are both important manifestations of various disorders, such as herpes zoster, atopic dermatitis, and psoriasis. Growing evidence suggests that both sensations have shared mediators, overlapping neural circuitry, and similarities in sen...

(This article belongs to the Special Issue Novel Target for the Treatment of Itch (Pruritus) and Pruritus-Related Pain of Different Origin)
  • Article
  • Open Access
6 Citations
4,036 Views
11 Pages

Analgesic and Anesthetic Efficacy of Rocuronium/Sugammadex in Otorhinolaryngologic Surgery: A Propensity Score-Matched Analysis

  • En-Bo Wu,
  • Chao-Ting Hung,
  • Sheng-Dean Luo,
  • Shao-Chun Wu,
  • Tsung-Yang Lee,
  • Jo-Chi Chin,
  • Peng-Neng Tsai and
  • Johnson Chia-Shen Yang

The use of rocuronium/sugammadex in otorhinolaryngologic surgery improves intubation conditions and surgical rating scales. This study primarily aimed to evaluate the effect of the combination of rocuronium and sugammadex on intraoperative anesthetic...

(This article belongs to the Special Issue Drug Candidates for Anesthesia and Analgesia)
  • Article
  • Open Access
30 Citations
4,877 Views
16 Pages

Investigation of Patient-Centric 3D-Printed Orodispersible Films Containing Amorphous Aripiprazole

  • Ju-Hyun Lee,
  • Chulhun Park,
  • In-OK Song,
  • Beom-Jin Lee,
  • Chin-Yang Kang and
  • Jun-Bom Park

The objective of this study was to design and evaluate an orodispersible film (ODF) composed of aripiprazole (ARP), prepared using a conventional solvent casting technique, and to fuse a three-dimensional (3D) printing technique with a hot-melt extru...

(This article belongs to the Special Issue 3D Printing of Drug Formulations)
  • Article
  • Open Access
8 Citations
3,354 Views
13 Pages

In our previous study, we reported the isolation of pennogenin-3-O-α-L-rhamnopyranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→3)]-β-D-glucopyranoside (spiroconazol A), a steroidal saponin, from the flowers of Dioscorea bulbifera L....

(This article belongs to the Section Natural Products)
  • Article
  • Open Access
32 Citations
5,580 Views
39 Pages

Synthesis and Evaluation of Some New 4H-Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

  • Nahed N. E. El-Sayed,
  • Magdi E. A. Zaki,
  • Sami A. Al-Hussain,
  • Abir Ben Bacha,
  • Malika Berredjem,
  • Vijay H. Masand,
  • Zainab M. Almarhoon and
  • Hanaa S. Omar

Colorectal cancer oncogenesis is linked to dysbiosis, oxidative stress and overexpression of CDK2. The 4H-pyran scaffold is considered an antitumoral, antibacterial and antioxidant lead as well as a CDK2 inhibitor. Herein, certain 4H-pyran derivative...

(This article belongs to the Topic Compounds with Medicinal Value)
  • Case Report
  • Open Access
6 Citations
3,779 Views
8 Pages

Good Response of Advanced Thymic Carcinoma with Low PD-L1 Expression to Chemotherapy plus Pembrolizumab as First-Line Therapy and to Pembrolizumab as Maintenance Therapy: A Case Report

  • Yoichi Nishii,
  • Kazuki Furuhashi,
  • Kentaro Ito,
  • Tadashi Sakaguchi,
  • Yuta Suzuki,
  • Kentaro Fujiwara,
  • Taro Yasuma,
  • Tetsu Kobayashi,
  • Corina N. D’Alessandro-Gabazza and
  • Osamu Hataji
  • + 2 authors

Thymic carcinoma is a rare malignant tumor with a poor prognosis. No standard treatment is currently available. The present case was a 64-year-old male smoker with no symptoms referred to our hospital because of abnormal chest radiological findings....

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
34 Citations
4,096 Views
14 Pages

C-Myc Expression in Oral Squamous Cell Carcinoma: Molecular Mechanisms in Cell Survival and Cancer Progression

  • Guya Diletta Marconi,
  • Ylenia Della Rocca,
  • Luigia Fonticoli,
  • Francesco Melfi,
  • Thangavelu Soundara Rajan,
  • Simone Carradori,
  • Jacopo Pizzicannella,
  • Oriana Trubiani and
  • Francesca Diomede

Oral squamous cell carcinoma (OSCC) represents 90% of malignant epithelial cancer that occurs in the oral cavity. The c-Myc factor is expressed in multiple types of cancer, comprising head and neck squamous cell carcinoma (HNSCC), where it plays a fu...

(This article belongs to the Special Issue Novel Anti-proliferative Agents)
  • Article
  • Open Access
8 Citations
3,469 Views
18 Pages

Tigecycline (TIGC) reacts with 7,7,8,8-tetracyanoquinodimethane (TCNQ) to form a bright green charge transfer complex (CTC). The spectrum of the CTC showed multiple charge transfer bands with a major peak at 843 nm. The Plackett–Burman design (...

(This article belongs to the Special Issue Perspectives and Challenges in the Synthesis and Analysis of Drugs—49th Conference “Synthesis and Analysis of Drugs” (SAD 2021))
  • Article
  • Open Access
2 Citations
4,280 Views
18 Pages

Assessing the Immunomodulatory Effect of Size on the Uptake and Immunogenicity of Influenza- and Hepatitis B Subunit Vaccines In Vitro

  • Rick Heida,
  • Philip A. Born,
  • Gabriela Tapia-Calle,
  • Henderik W. Frijlink,
  • Anna Salvati,
  • Anke L. W. Huckriede and
  • Wouter L. J. Hinrichs

Viral subunit vaccines are a safer and more tolerable alternative to whole inactivated virus vaccines. However, they often come with limited efficacy, necessitating the use of adjuvants. Using free and particle-bound viral antigens, we assessed wheth...

(This article belongs to the Section Biopharmaceuticals)
  • Article
  • Open Access
27 Citations
4,472 Views
40 Pages

Palladium(II) Complexes of Substituted Salicylaldehydes: Synthesis, Characterization and Investigation of Their Biological Profile

  • Ariadni Zianna,
  • George Geromichalos,
  • Augusta-Maria Fiotaki,
  • Antonios G. Hatzidimitriou,
  • Stavros Kalogiannis and
  • George Psomas

Five palladium(II) complexes of substituted salicylaldehydes (X-saloH, X = 4-Et2N (for 1), 3,5-diBr (for 2), 3,5-diCl (for 3), 5-F (for 4) or 4-OMe (for 5)) bearing the general formula [Pd(X-salo)2] were synthesized and structurally characterized. Th...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
19 Citations
3,501 Views
16 Pages

The objective of this study was to prepare hydroxyapatite (HA) with potential antibacterial activity against gram-negative and gram-positive bacteria by incorporating different atomic ratios of Cu2+ (0.1–1.0%), Mg2+ (1.0–7.0%), and Zn2+ (...

(This article belongs to the Special Issue Synthesis of Metal Nanoparticles and Their Pharmaceutical Applications)
  • Article
  • Open Access
12 Citations
3,427 Views
19 Pages

Hybrid Nanosystems Based on Nicotinate-Functionalized Mesoporous Silica and Silver Chloride Nanoparticles Loaded with Phenytoin for Preventing Pseudomonas aeruginosa Biofilm Development

  • Maider Ugalde-Arbizu,
  • John Jairo Aguilera-Correa,
  • Aranzazu Mediero,
  • Jaime Esteban,
  • Paulina L. Páez,
  • Eider San Sebastian and
  • Santiago Gómez-Ruiz

Pseudomonas aeruginosa (PA) is one of the most common bacteria isolated from chronic wounds and burns. Its treatment is a challenge due to antimicrobial drug resistance and biofilm formation. In this context, this study aimed to perform the synthesis...

(This article belongs to the Special Issue Novel Antibacterial Agents 2022)
  • Article
  • Open Access
34 Citations
5,151 Views
18 Pages

In this research, KLA-modified liposomes co-loaded with 5-fluorouracil and paclitaxel (KLA-5-FU/PTX Lps) were developed, and their antitumor activity against triple-negative breast cancer (TNBC) was evaluated. KLA-5-FU/PTX Lps were prepared using the...

(This article belongs to the Special Issue Synergistic Effects of Plant Derivatives with Other Drugs)
  • Technical Note
  • Open Access
25 Citations
3,468 Views
9 Pages

Chronic Pruritus in Atopic Patients Treated with Dupilumab: Real Life Response and Related Parameters in 354 Patients

  • Luca Mastorino,
  • François Rosset,
  • Federica Gelato,
  • Michela Ortoncelli,
  • Giovanni Cavaliere,
  • Pietro Quaglino and
  • Simone Ribero

Chronic pruritus is a major symptom of atopic dermatitis (AD). Its etiopathogenesis is complex, and an understanding of the driving factors of its pathogenesis allows for the development of new molecule-targeted therapies. Dupilumab, targeting and bl...

(This article belongs to the Special Issue Novel Target for the Treatment of Itch (Pruritus) and Pruritus-Related Pain of Different Origin)
  • Article
  • Open Access
14 Citations
4,863 Views
17 Pages

The N-Methyl-D-Aspartate Receptor Blocker REL-1017 (Esmethadone) Reduces Calcium Influx Induced by Glutamate, Quinolinic Acid, and Gentamicin

  • Ezio Bettini,
  • Sara De Martin,
  • Andrea Mattarei,
  • Marco Pappagallo,
  • Stephen M. Stahl,
  • Francesco Bifari,
  • Charles E. Inturrisi,
  • Franco Folli,
  • Sergio Traversa and
  • Paolo L. Manfredi

REL-1017 (esmethadone) is a novel N-methyl-D-aspartate receptor (NMDAR) antagonist and promising rapid antidepressant candidate. Using fluorometric imaging plate reader (FLIPR) assays, we studied the effects of quinolinic acid (QA) and gentamicin, wi...

(This article belongs to the Special Issue NMDA Receptor-Based Therapeutics)
  • Review
  • Open Access
77 Citations
7,183 Views
23 Pages

The Pivotal Role of Quantum Dots-Based Biomarkers Integrated with Ultra-Sensitive Probes for Multiplex Detection of Human Viral Infections

  • Seyyed Mojtaba Mousavi,
  • Seyyed Alireza Hashemi,
  • Masoomeh Yari Kalashgrani,
  • Navid Omidifar,
  • Chin Wei Lai,
  • Neralla Vijayakameswara Rao,
  • Ahmad Gholami and
  • Wei-Hung Chiang

The spread of viral diseases has caused global concern in recent years. Detecting viral infections has become challenging in medical research due to their high infectivity and mutation. A rapid and accurate detection method in biomedical and healthca...

(This article belongs to the Section Pharmaceutical Technology)
  • Review
  • Open Access
428 Citations
20,163 Views
24 Pages

Bone Tissue Engineering in the Treatment of Bone Defects

  • Nannan Xue,
  • Xiaofeng Ding,
  • Rizhong Huang,
  • Ruihan Jiang,
  • Heyan Huang,
  • Xin Pan,
  • Wen Min,
  • Jun Chen,
  • Jin-Ao Duan and
  • Yiwei Wang
  • + 1 author

Bones play an important role in maintaining exercise and protecting organs. Bone defect, as a common orthopedic disease in clinics, can cause tremendous damage with long treatment cycles. Therefore, the treatment of bone defect remains as one of the...

(This article belongs to the Section Pharmaceutical Technology)
  • Systematic Review
  • Open Access
6 Citations
5,602 Views
14 Pages

Dexamethasone Increases the Anesthetic Success in Patients with Symptomatic Irreversible Pulpitis: A Meta-Analysis

  • Lorenzo Franco-de la Torre,
  • Eduardo Gómez-Sánchez,
  • Nicolás Addiel Serafín-Higuera,
  • Ángel Josabad Alonso-Castro,
  • Sandra López-Verdín,
  • Nelly Molina-Frechero,
  • Vinicio Granados-Soto and
  • Mario Alberto Isiordia-Espinoza

Inferior alveolar nerve block (IANB) has a high failure rate in subjects with symptomatic irreversible pulpitis (SIP). It has been suggested that drugs with anti-inflammatory activity could improve the efficacy of the anesthetic used for IANB. The ai...

(This article belongs to the Special Issue Drug Candidates for Anesthesia and Analgesia)
  • Review
  • Open Access
15 Citations
5,654 Views
27 Pages

Tumor-derived membrane vesicles (TDMVs) are non-invasive, chemotactic, easily obtained characteristics and contain various tumor-borne substances, such as nucleic acid and proteins. The unique properties of tumor cells and membranes make them widely...

(This article belongs to the Special Issue Recent Progress of Nanomedicine and Targeted Drug Delivery for Cancer Treatment)
  • Review
  • Open Access
36 Citations
11,088 Views
22 Pages

Novel Pharmaceutical Strategies for Enhancing Skin Penetration of Biomacromolecules

  • Luyu Zhang,
  • Zirong Dong,
  • Wenjuan Liu,
  • Xiying Wu,
  • Haisheng He,
  • Yi Lu,
  • Wei Wu and
  • Jianping Qi

Skin delivery of biomacromolecules holds great advantages in the systemic and local treatment of multiple diseases. However, the densely packed stratum corneum and the tight junctions between keratinocytes stand as formidable skin barriers against th...

(This article belongs to the Special Issue Delivery Systems of Peptides and Proteins: Challenges, Status Quo and Future Perspectives)
  • Review
  • Open Access
13 Citations
7,022 Views
15 Pages

The delta opioid receptor is a Gi-protein-coupled receptor (GPCR) with a broad expression pattern both in the central nervous system and the body. The receptor has been investigated as a potential target for a multitude of significant diseases includ...

(This article belongs to the Special Issue In Silico Approaches in Drug Design)
  • Article
  • Open Access
2 Citations
2,986 Views
15 Pages

ZLM-7 Blocks Breast Cancer Progression by Inhibiting MDM2 via Upregulation of 14-3-3 Sigma

  • Min Wen,
  • Zi-Zheng Zou,
  • Tiao Luo,
  • Xuan Li,
  • Su-You Liu,
  • Ji-Jia Li and
  • Zhi-Yong Luo

Breast cancer is one of the most prevalent malignancies with poor prognosis. Inhibition of angiogenesis is becoming a valid and evident therapeutic strategy to treat cancer. Recent studies uncovered the antiangiogenic activity of ZLM-7 (a combretasta...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
29 Citations
6,729 Views
17 Pages

New Life of an Old Drug: Caffeine as a Modulator of Antibacterial Activity of Commonly Used Antibiotics

  • Anna Woziwodzka,
  • Marta Krychowiak-Maśnicka,
  • Grzegorz Gołuński,
  • Anna Łosiewska,
  • Agnieszka Borowik,
  • Dariusz Wyrzykowski and
  • Jacek Piosik

With the rapid and continuous emergence of antimicrobial resistance, bacterial infections became a significant global healthcare concern. One of the proposed strategies to combat multidrug-resistant pathogens is to use additional compounds, such as n...

(This article belongs to the Special Issue Synergistic Effects of Plant Derivatives with Other Drugs)
  • Review
  • Open Access
25 Citations
5,505 Views
16 Pages

Na+/H+ Exchanger 1, a Potential Therapeutic Drug Target for Cardiac Hypertrophy and Heart Failure

  • Huiting Xia,
  • Aqeela Zahra,
  • Meng Jia,
  • Qun Wang,
  • Yunfu Wang,
  • Susan L. Campbell and
  • Jianping Wu

Cardiac hypertrophy is defined as increased heart mass in response to increased hemodynamic requirements. Long-term cardiac hypertrophy, if not counteracted, will ultimately lead to heart failure. The incidence of heart failure is related to myocardi...

(This article belongs to the Special Issue Effects of Drugs on Ion Channels)
  • Article
  • Open Access
10 Citations
3,901 Views
15 Pages

Reversing Cardiac Hypertrophy at the Source Using a Cardiac Targeting Peptide Linked to miRNA106a: Targeting Genes That Cause Cardiac Hypertrophy

  • G. Ian Gallicano,
  • Jiayu Fu,
  • Samiksha Mahapatra,
  • Michael V. R. Sharma,
  • Conor Dillon,
  • Claire Deng and
  • Maliha Zahid

Causes and treatments for heart failure (HF) have been investigated for over a century culminating in data that have led to numerous pharmacological and surgical therapies. Unfortunately, to date, even with the most current treatments, HF remains a p...

(This article belongs to the Section Pharmaceutical Technology)
  • Article
  • Open Access
23 Citations
10,035 Views
16 Pages

Clinical Impact of Functional CYP2C19 and CYP2D6 Gene Variants on Treatment with Antidepressants in Young People with Depression: A Danish Cohort Study

  • Liv S. Thiele,
  • Kazi Ishtiak-Ahmed,
  • Janne P. Thirstrup,
  • Esben Agerbo,
  • Carin A. T. C. Lunenburg,
  • Daniel J. Müller and
  • Christiane Gasse

Background: The clinical impact of the functional CYP2C19 and CYP2D6 gene variants on antidepressant treatment in people with depression is not well studied. Here, we evaluate the utility of pharmacogenetic (PGx) testing in psychiatry by investigatin...

(This article belongs to the Special Issue Clinical Utility of Applying PGx and Deprescribing-Based Decision Support in Polypharmacy: Future Perspectives)
  • Article
  • Open Access
10 Citations
3,368 Views
18 Pages

Safety and Pharmaceutical Evaluation of a Novel Natural Polymer, Ocicum, as Solubility and Dissolution Enhancer in Solid Dispersion

  • Mobina Manzoor,
  • Syed Atif Raza,
  • Mulazim Hussain Asim,
  • Nadeem Irfan Bukhari,
  • Shumaila Arshad and
  • Uzma Zafar

Plant mucilages are commonly employed as excipients in pharmaceutical manufacturing. Ocimum basilicum (Lamiaceae family), a source of hydrophilic mucilage referred herein as Ocicum, was evaluated for the solubility enhancer of a model drug, aceclofen...

(This article belongs to the Section Pharmaceutical Technology)
  • Review
  • Open Access
28 Citations
11,089 Views
56 Pages

Traditional herbal medicine (THM) is a “core” from which modern medicine has evolved over time. Besides this, one third of people worldwide have no access to modern medicine and rely only on traditional medicine. To date, drugs of plant o...

(This article belongs to the Special Issue Novel Anti-proliferative Agents)
  • Opinion
  • Open Access
13 Citations
4,565 Views
11 Pages

Complexed Polymer Film-Forming Spray: An Optimal Delivery System for Secretome of Mesenchymal Stem Cell as Diabetic Wound Dressing?

  • Abd. Kakhar Umar,
  • Jittima Amie Luckanagul,
  • James H. Zothantluanga and
  • Sriwidodo Sriwidodo

Diabetes-related wounds have physiological factors that make healing more complicated. High sugar levels can increase microbial infection risk while limiting nutrition and oxygen transfer to the wound area. The secretome of mesenchymal stem cells has...

(This article belongs to the Section Pharmaceutical Technology)
  • Article
  • Open Access
4 Citations
2,601 Views
11 Pages

Fully Automated, High-Dose Radiosynthesis of [18F]PARPi

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

[18F]PARPi is currently undergoing clinical trials as a PET tracer for many applications. However, only manual radiosynthesis was reported; this has several drawbacks, including an increased risk of contamination from the operator, and the need to li...

(This article belongs to the Section Radiopharmaceutical Sciences)
  • Review
  • Open Access
25 Citations
4,882 Views
22 Pages

Computational Methods in Cooperation with Experimental Approaches to Design Protein Tyrosine Phosphatase 1B Inhibitors in Type 2 Diabetes Drug Design: A Review of the Achievements of This Century

  • Mara Ibeth Campos-Almazán,
  • Alicia Hernández-Campos,
  • Rafael Castillo,
  • Erick Sierra-Campos,
  • Mónica Valdez-Solana,
  • Claudia Avitia-Domínguez and
  • Alfredo Téllez-Valencia

Protein tyrosine phosphatase 1B (PTP1B) dephosphorylates phosphotyrosine residues and is an important regulator of several signaling pathways, such as insulin, leptin, and the ErbB signaling network, among others. Therefore, this enzyme is considered...

(This article belongs to the Special Issue Design of Enzyme Inhibitors as Potential Drugs 2022)
  • Article
  • Open Access
25 Citations
5,352 Views
20 Pages

Formulation and Characterization of O/W Nanoemulsions of Hemp Seed Oil for Protection from Steatohepatitis: Analysis of Hepatic Free Fatty Acids and Oxidation Markers

  • Mona Qushawy,
  • Yasmin Mortagi,
  • Reem Alshaman,
  • Hatem I. Mokhtar,
  • Fatma Azzahraa Hisham,
  • Abdullah Alattar,
  • Dong Liang,
  • Eman T. Enan,
  • Amira H. Eltrawy and
  • Sawsan A. Zaitone
  • + 2 authors

Non-alcoholic steatohepatitis (NASH) is a common type of metabolic liver disease which is characterized by fatty changes associated with hepatocyte injury, lobular inflammation, and/or liver fibrosis. Nanoemulsions are kinetically stable colloidal sy...

(This article belongs to the Special Issue Recent Advances in Natural Products Discoveries for Antioxidants: Pharmacology and Mechanisms)
  • Article
  • Open Access
9 Citations
3,898 Views
13 Pages

The Role of Interventional Irisin on Heart Molecular Physiology

  • Foad Alzoughool,
  • Mohammad Borhan Al-Zghoul,
  • Bayan Y. Ghanim,
  • Michael Gollob,
  • Nasir Idkaidek and
  • Nidal A. Qinna

Irisin, encoded by the FNDC5 (fibronectin type III domain containing 5) gene, is a novel myokine that has been implicated as an essential mediator of exercise benefits. Effects of irisin on heart physiology is still ambiguous. This study aimed to eva...

(This article belongs to the Special Issue Drug Candidates for the Prevention and Treatment of Cardiovascular Diseases)
  • Article
  • Open Access
12 Citations
3,964 Views
19 Pages

Design and Anticancer Properties of New Water-Soluble Ruthenium–Cyclopentadienyl Complexes

  • Tânia S. Morais,
  • Fernanda Marques,
  • Paulo J. Amorim Madeira,
  • Maria Paula Robalo and
  • Maria Helena Garcia

Ruthenium complexes are emerging as one of the most promising classes of complexes for cancer therapy. However, their limited aqueous solubility may be the major limitation to their potential clinical application. In view and to contribute to the pro...

(This article belongs to the Special Issue Metal-Based Agents in Drug Discovery)
  • Article
  • Open Access
22 Citations
3,789 Views
28 Pages

Plant Alkylbenzenes and Terpenoids in the Form of Cyclodextrin Inclusion Complexes as Antibacterial Agents and Levofloxacin Synergists

  • Igor D. Zlotnikov,
  • Natalya G. Belogurova,
  • Sergey S. Krylov,
  • Marina N. Semenova,
  • Victor V. Semenov and
  • Elena V. Kudryashova

Allylpolyalkoxybenzenes (APABs) and terpenoids from plant essential oils exhibit a range of remarkable biological effects, including analgesic, antibacterial, anti-inflammatory, antioxidant, and others. Synergistic activity with antibiotics of differ...

(This article belongs to the Special Issue Synergistic Effects of Plant Derivatives with Other Drugs)
  • Article
  • Open Access
5 Citations
3,598 Views
14 Pages

Predictiveness of the Human-CYP3A4-Transgenic Mouse Model (Cyp3aXAV) for Human Drug Exposure of CYP3A4-Metabolized Drugs

  • David Damoiseaux,
  • Wenlong Li,
  • Alejandra Martínez-Chávez,
  • Jos H. Beijnen,
  • Alfred H. Schinkel,
  • Alwin D. R. Huitema and
  • Thomas P. C. Dorlo

The extrapolation of drug exposure between species remains a challenging step in drug development, contributing to the low success rate of drug approval. As a consequence, extrapolation of toxicology from animal models to humans to evaluate safe, fir...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
11 Citations
3,578 Views
18 Pages

Synthesis and Biological Evaluation of Imadazo[1,2-a]pyrazines as Anticancer and Antiviral Agents through Inhibition of CDK9 and Human Coronavirus

  • Aisha A. Alsfouk,
  • Hanan M. Alshibl,
  • Bshra A. Alsfouk,
  • Najla A. Altwaijry and
  • Ebtehal S. Al-Abdullah

In this work, novel imadazo[1,2-a]pyrazine derivatives were synthesized and evaluated as CDK9 inhibitors. The results of CDK9 assay showed that the derivatives with pyridin-4-yl in position 2 and benzyl in position 3 of imadazo[1,2-a]pyrazine 3c disp...

(This article belongs to the Section Medicinal Chemistry)
  • Review
  • Open Access
10 Citations
7,702 Views
19 Pages

Aspects of Antiviral Strategies Based on Different Phototherapy Approaches: Hit by the Light

  • Hannah Kunstek,
  • Fanny Vreken,
  • Aminata Keita,
  • Michael R. Hamblin,
  • Florence Dumarçay and
  • Mihayl Varbanov

The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) which caused the COVID-19 pandemic spreading around the world from late 2019, served as a ruthless reminder of the threat viruses pose to global public health. The synthesis of new anti...

(This article belongs to the Special Issue Photodynamic Therapy 2022)
  • Article
  • Open Access
13 Citations
4,688 Views
15 Pages

Structure-Based Identification and Biological Characterization of New NAPRT Inhibitors

  • Jorge Franco,
  • Francesco Piacente,
  • Melanie Walter,
  • Simone Fratta,
  • Moustafa Ghanem,
  • Andrea Benzi,
  • Irene Caffa,
  • Alexander V. Kurkin,
  • Andrea Altieri and
  • Alberto Del Rio
  • + 5 authors

NAPRT, the rate-limiting enzyme of the Preiss–Handler NAD biosynthetic pathway, has emerged as a key biomarker for the clinical success of NAMPT inhibitors in cancer treatment. Previous studies found that high protein levels of NAPRT conferred...

(This article belongs to the Special Issue Computational Methods in the Design of Anticancer Drugs)
  • Article
  • Open Access
10 Citations
4,678 Views
17 Pages

Design and Synthesis of New Hydantoin Acetanilide Derivatives as Anti-NSCLC Targeting EGFRL858R/T790M Mutations

  • Moamen A. Hassanin,
  • Muhamad Mustafa,
  • Mohammed A. S. Abourehab,
  • Heba A. Hassan,
  • Omar M. Aly and
  • Eman A. M. Beshr

Epidermal Growth Factor Receptor (EGFR), its wild type and mutations L858R/T790M, is overexpressed in non-small cell lung cancer (NSCLC) patients and is considered an inevitable oncology target. However, while the potential EGFR inhibitors have been...

(This article belongs to the Special Issue Novel Anti-proliferative Agents)

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