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Pharmaceuticals, Volume 16, Issue 5

2023 May - 142 articles

Cover Story: G-protein-coupled receptors (GPCRs) represent valid molecular targets for directing peptide radioligands to malignant lesions. Diagnosis (γ-emitters: SPECT, β+-emitters: PET) and therapy (α, β-, Auger e- emitters: PRRT) are combined in a new promising “radiotheranostics” approach. Radiolabeled somatostatin analogs are widely used in neuroendocrine tumor patients, whereas peptide radioligands targeting other GPCRs in different tumors include bombesin, gastrin and exendin analogs. A recent switch from internalizing GPCR agonists to antagonists led to better pharmacokinetics and higher biosafety. GPCR antagonists do not activate their target receptor and do not elicit acute adverse effects when injected into patients. We herein discuss the challenges and opportunities of modern peptide radiotheranostics, focusing on GPCR antagonists. View this paper
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Articles (142)

  • Review
  • Open Access
17 Citations
4,598 Views
27 Pages

Carboxymethylated Gums and Derivatization: Strategies and Significance in Drug Delivery and Tissue Engineering

  • Madhuri Baghel,
  • Kalyani Sakure,
  • Tapan Kumar Giri,
  • Sabyasachi Maiti,
  • Kartik T. Nakhate,
  • Shreesh Ojha,
  • Charu Sharma,
  • Yogeeta Agrawal,
  • Sameer Goyal and
  • Hemant Badwaik

Natural polysaccharides have been widely exploited in drug delivery and tissue engineering research. They exhibit excellent biocompatibility and fewer adverse effects; however, it is challenging to assess their bioactivities to that of manufactured s...

  • Review
  • Open Access
7 Citations
5,514 Views
20 Pages

The Genus Dacryodes Vahl.: Ethnobotany, Phytochemistry and Biological Activities

  • Leseho Swana,
  • Bienvenu Tsakem,
  • Jacqueline V. Tembu,
  • Rémy B. Teponno,
  • Joy T. Folahan,
  • Jarmo-Charles Kalinski,
  • Alexandros Polyzois,
  • Guy Kamatou,
  • Louis P. Sandjo and
  • Xavier Siwe-Noundou
  • + 1 author

Dacryodes Vahl. species, belonging to the Burseraceae family, are widely used in traditional medicine in tropical regions to treat a range of ailments including malaria, wounds, tonsillitis, and ringworms. This review discusses the distribution, ethn...

  • Article
  • Open Access
5 Citations
2,933 Views
13 Pages

Rutin Gel with Bone Graft Accelerates Bone Formation in a Rabbit Model by Inhibiting MMPs and Enhancing Collagen Activities

  • Fahad F. Albaqami,
  • Hassan N. Althurwi,
  • Khalid M. Alharthy,
  • Abubaker M. Hamad and
  • Fatin A. Awartani

Bone graft techniques are used to compensate for bone loss in areas with deficient regeneration. However, matrix metalloproteases (MMPs) can limit bone formation by degrading extracellular matrices, which are required for bone regrowth. Noteworthily,...

  • Article
  • Open Access
29 Citations
6,406 Views
45 Pages

Brown seaweed is rich in phenolic compounds and has established health benefits. However, the phenolics present in Australian beach-cast seaweed are still unclear. This study investigated the effect of ultrasonication and conventional methodologies u...

  • Article
  • Open Access
5 Citations
3,471 Views
14 Pages

Prescribed Drugs and Self-Directed Violence: A Descriptive Study in the Spanish Pharmacovigilance Database

  • Ana Avedillo-Salas,
  • Javier Pueyo-Val,
  • Ana Fanlo-Villacampa,
  • Cristina Navarro-Pemán,
  • Francisco Javier Lanuza-Giménez,
  • Ignatios Ioakeim-Skoufa and
  • Jorge Vicente-Romero

Self-inflicted violence is a major and growing public health problem and its prediction and prevention is challenging for healthcare systems worldwide. Our aim was to identify prescribed drugs associated with self-directed violent behaviors in Spain....

  • Article
  • Open Access
9 Citations
4,187 Views
18 Pages

A Three-Step Process to Isolate Large Quantities of Bioactive Sesquiterpene Lactones from Cichorium intybus L. Roots and Semisynthesis of Chicory STLs Standards

  • Francesca Ruggieri,
  • Philippe Hance,
  • Bruna Gioia,
  • Alexandre Biela,
  • Pascal Roussel,
  • Jean-Louis Hilbert and
  • Nicolas Willand

Sesquiterpene lactones (STLs) are a large group of terpenoids most commonly found in plants of the Asteraceae family, e.g., in chicory plants, displaying a wide range of interesting biological activities. However, further studies on the biological po...

  • Review
  • Open Access
16 Citations
9,015 Views
13 Pages

The use of high-efficacy disease-modifying therapies (DMTs) early in the course of multiple sclerosis (MS) has been shown to improve clinical outcomes and is becoming an increasingly popular treatment strategy. As a result, monoclonal antibodies, inc...

  • Article
  • Open Access
19 Citations
3,615 Views
18 Pages

Based on their proven anti-inflammatory and antioxidant effects, recent studies have examined the therapeutic potential of the sodium-glucose cotransporter 2 (SGLT2) inhibitors in neurodevelopmental disorders such as autism spectrum disorder (ASD). T...

  • Article
  • Open Access
1 Citations
2,700 Views
13 Pages

Effect of the Composition of Leuzea and Cranberry Meal Extracts on Metabolic Processes in Norm and Pathology

  • Daria Khalikova,
  • Sergey An’kov,
  • Nataliya Zhukova,
  • Tatyana Tolstikova,
  • Sergey Popov and
  • Anastasia Saiko

This study was conducted to evaluate the effects of long-term administration of a new herbal composition of leuzea and cranberry meal extracts at a dose of 70:500 mg/kg in healthy and pathological mice. After 4 weeks of daily composition administrati...

  • Article
  • Open Access
12 Citations
3,644 Views
19 Pages

Drugs that cure COVID-19 have been marketed; however, this disease continues to ravage the world without becoming extinct, and thus, drug discoveries are still relevant. Since Mpro has known advantages as a drug target, such as the conserved nature o...

  • Review
  • Open Access
4 Citations
3,322 Views
19 Pages

Metal complexes feature a wide range of available geometries, diversified lability, controllable hydrolytic stability, and easily available rich redox activity. These characteristics, combined with the specific properties of coordinated organic molec...

  • Article
  • Open Access
26 Citations
3,599 Views
17 Pages

Alkaloid from Geissospermum sericeum Benth. & Hook.f. ex Miers (Apocynaceae) Induce Apoptosis by Caspase Pathway in Human Gastric Cancer Cells

  • Mirian Letícia Carmo Bastos,
  • João Victor Silva-Silva,
  • Jorddy Neves Cruz,
  • Amanda Roberta Palheta da Silva,
  • Alexandre Augusto Bentaberry-Rosa,
  • Gisele da Costa Ramos,
  • José Edson de Sousa Siqueira,
  • Márlia Regina Coelho-Ferreira,
  • Sandro Percário and
  • Maria Fâni Dolabela
  • + 3 authors

Gastric cancer is among the major causes of death from neoplasia leading causes of death worldwide, with high incidence rates and problems related to its treatment. Here, we outline how Geissospermum sericeum exerts antitumor activity on the ACP02 ce...

  • Article
  • Open Access
2 Citations
2,991 Views
16 Pages

Identification of the Hepatic Metabolites of Flumazenil and their Kinetic Application in Neuroimaging

  • Wei-Hsi Chen,
  • Chuang-Hsin Chiu,
  • Shiou-Shiow Farn,
  • Kai-Hung Cheng,
  • Yuan-Ruei Huang,
  • Shih-Ying Lee,
  • Yao-Ching Fang,
  • Yu-Hua Lin and
  • Kang-Wei Chang

Studies of the neurobiological causes of anxiety disorders have suggested that the γ-aminobutyric acid (GABA) system increases synaptic concentrations and enhances the affinity of GABAA (type A) receptors for benzodiazepine ligands. Flumazenil...

  • Article
  • Open Access
3 Citations
2,979 Views
12 Pages

Triple-Therapy of Peritoneal Metastasis—Partial-Dehydration under Hyperthermic Condition Combined with Chemotherapy: The First Preliminary In-Vitro Results

  • Carolina Khosrawipour,
  • Agata Diakun,
  • Shiri Li,
  • Hien Lau,
  • Joanna Kulas,
  • Veria Khosrawipour,
  • Wojciech Kielan and
  • Agata Mikolajczyk-Martinez

A newly introduced combination of intraperitoneal dehydration and hyperthermia has recently been shown to be feasible and cytotoxic for colon cancer cells in vivo. For the first time, our study now aims to evaluate dehydration under hyperthermic cond...

  • Article
  • Open Access
3 Citations
2,964 Views
12 Pages

SIRT1 Signaling Is Involved in the Vascular Improvement Induced by Moringa Oleifera Seeds during Aging

  • Valeria Conti,
  • Joseph Iharinjaka Randriamboavonjy,
  • Herintsoa Rafatro,
  • Valentina Manzo,
  • Jessica Dal Col,
  • Amelia Filippelli,
  • Graziamaria Corbi and
  • Angela Tesse

Vascular aging is linked to reduce NO bioavailability, endothelial dysfunction, oxidative stress, and inflammation. We previously showed that a 4-week treatment of middle-aged Wistar rats (MAWRs, 46 weeks old) with Moringa oleifera seed powder (MOI,...

  • Review
  • Open Access
8 Citations
7,865 Views
13 Pages

Honey-Related Treatment Strategies in Dry Eye Disease

  • Julia Prinz,
  • Nicola Maffulli,
  • Matthias Fuest,
  • Peter Walter,
  • Frank Hildebrand and
  • Filippo Migliorini

This systematic review and meta-analysis investigated whether honey-related treatment strategies improve the signs and symptoms of patients with dry eye disease (DED). In March 2023, the following databases were accessed for clinical trials investiga...

  • Review
  • Open Access
4 Citations
7,861 Views
10 Pages

Objective. The aim of this review is to explore the role of IGF-1 and IGF-1R inhibitors in pain-related conditions and assess the effectiveness of IGF-1-related drugs in pain management. Specifically, this paper investigates the potential involvement...

  • Article
  • Open Access
2 Citations
2,344 Views
13 Pages

To elucidate the potential roles of serotonergic activity in human character traits (i.e., self-directedness, cooperativeness, and self-transcendence), we investigated the relationship between these character traits and serotonin transporter (5-HTT)...

  • Article
  • Open Access
5 Citations
3,115 Views
26 Pages

Structure Optimization of 12β-O-γ-Glutamyl Oleanolic Acid Derivatives Resulting in Potent FXR Antagonist/Modulator for NASH Therapy

  • Hao Ma,
  • Yunyang Bao,
  • Shuaishuai Niu,
  • Shaorong Wang,
  • Yiming Li,
  • Hongwei He,
  • Na Zhang and
  • Weishuo Fang

The farnesoid X receptor (FXR) plays a crucial role in regulating the metabolism of bile acids, lipids, and sugars. Consequently, it is implicated in the treatment of various diseases, including cholestasis, diabetes, hyperlipidemia, and cancer. The...

  • Article
  • Open Access
2 Citations
3,066 Views
16 Pages

MKX-AS1 Gene Expression Associated with Variation in Drug Response to Oxaliplatin and Clinical Outcomes in Colorectal Cancer Patients

  • Ricardo D. Gonzalez,
  • George W. Small,
  • Adrian J. Green,
  • Farida S. Akhtari,
  • Alison A. Motsinger-Reif,
  • Julia C. F. Quintanilha,
  • Tammy M. Havener,
  • David M. Reif,
  • Howard L. McLeod and
  • Tim Wiltshire

Oxaliplatin (OXAL) is a commonly used chemotherapy for treating colorectal cancer (CRC). A recent genome wide association study (GWAS) showed that a genetic variant (rs11006706) in the lncRNA gene MKX-AS1 and partnered sense gene MKX could impact the...

  • Article
  • Open Access
7 Citations
2,902 Views
20 Pages

Screening and Elucidation of Chemical Structures of Novel Mammalian α-Glucosidase Inhibitors Targeting Anti-Diabetes Drug from Herbals Used by E De Ethnic Tribe in Vietnam

  • Van Bon Nguyen,
  • San-Lang Wang,
  • Tu Quy Phan,
  • Thi Huyen Thoa Pham,
  • Hung-Tse Huang,
  • Chia-Ching Liaw and
  • Anh Dzung Nguyen

Among ten extracts of indigenous medicinal plants, the MeOH extract of Terminalia triptera Stapf. (TTS) showed the most efficient mammalian α-glucosidase inhibition for the first time. The data of screening bioactive parts used indicated that t...

  • Article
  • Open Access
20 Citations
4,290 Views
18 Pages

Resveratrol Enhances Cytotoxic Effects of Cisplatin by Inducing Cell Cycle Arrest and Apoptosis in Ovarian Adenocarcinoma SKOV-3 Cells through Activating the p38 MAPK and Suppressing AKT

  • Phateep Hankittichai,
  • Phatarawat Thaklaewphan,
  • Nitwara Wikan,
  • Jirapak Ruttanapattanakul,
  • Saranyapin Potikanond,
  • Duncan R. Smith and
  • Wutigri Nimlamool

In the current study, we identified a mechanism of resveratrol (RES) underlying its anti-cancer properties against human ovarian adenocarcinoma SKOV-3 cells. We investigated its anti-proliferative and apoptosis-inducing effects in combination with ci...

  • Review
  • Open Access
7 Citations
3,565 Views
12 Pages

RadioLigand Therapy with [177Lu]Lu-PSMA-617 for Salivary Gland Cancers: Literature Review and First Compassionate Use in France

  • Marie Terroir,
  • Chloé Lamesa,
  • Mehdi Krim,
  • Lavinia Vija,
  • Jean-Sébastien Texier,
  • Thibaut Cassou-Mounat,
  • Jean-Pierre Delord,
  • Delphine Vallot and
  • Frédéric Courbon

Salivary gland cancers are rare tumors comprising a large group of heterogeneous tumors with variable prognosis. Their therapeutic management at a metastatic stage is challenging due to the lack of therapeutic lines and the toxicity of treatments. [1...

  • Article
  • Open Access
34 Citations
5,955 Views
21 Pages

Alzheimer’s disease (AD) is a progressive neurological illness characterized by memory loss and cognitive deterioration. Dapagliflozin was suggested to attenuate the memory impairment associated with AD; however, its mechanisms were not fully e...

  • Article
  • Open Access
4 Citations
3,836 Views
14 Pages

Network Biology-Inspired Machine Learning Features Predict Cancer Gene Targets and Reveal Target Coordinating Mechanisms

  • Taylor M. Weiskittel,
  • Andrew Cao,
  • Kevin Meng-Lin,
  • Zachary Lehmann,
  • Benjamin Feng,
  • Cristina Correia,
  • Cheng Zhang,
  • Philip Wisniewski,
  • Shizhen Zhu and
  • Hu Li
  • + 1 author

Anticipating and understanding cancers’ need for specific gene activities is key for novel therapeutic development. Here we utilized DepMap, a cancer gene dependency screen, to demonstrate that machine learning combined with network biology can...

  • Article
  • Open Access
7 Citations
3,691 Views
19 Pages

Assessment of Aptamer as a Potential Drug Targeted Delivery for Retinal Angiogenesis Inhibition

  • David Moreira,
  • Jéssica Lopes-Nunes,
  • Fátima Milhano Santos,
  • Maria Paula Cabral Campello,
  • Maria Cristina Oliveira,
  • António Paulo,
  • Cândida Tomaz and
  • Carla Cruz

AT11-L0 is an aptamer derivative of AS1411 composed of G-rich sequences that can adopt a G-quadruplex (G4) structure and target nucleolin (NCL), a protein that acts as a co-receptor for several growth factors. Hence, this study aimed to characterize...

  • Review
  • Open Access
21 Citations
9,846 Views
16 Pages

Effects of Lipid-Modifying and Other Drugs on Lipoprotein(a) Levels—Potent Clinical Implications

  • Amalia Despoina Koutsogianni,
  • George Liamis,
  • Evangelos Liberopoulos,
  • Petros Spyridonas Adamidis and
  • Matilda Florentin

The past few years have shown an ongoing interest in lipoprotein(a) (Lp(a)), a lipid molecule that has been proven to have atherogenic, thrombogenic, and inflammatory properties. Several lines of evidence, indeed, have demonstrated an increased risk...

  • Article
  • Open Access
6 Citations
3,907 Views
21 Pages

S-72, a Novel Orally Available Tubulin Inhibitor, Overcomes Paclitaxel Resistance via Inactivation of the STING Pathway in Breast Cancer

  • Zhenyan Hou,
  • Songwen Lin,
  • Tingting Du,
  • Mingjin Wang,
  • Weida Wang,
  • Shen You,
  • Nina Xue,
  • Yichen Liu,
  • Ming Ji and
  • Xiaoguang Chen
  • + 1 author

Microtubule-targeting agents are widely used as active anticancer drugs. However, drug resistance always emerges after their long-term use, especially in the case of paclitaxel, which is the cornerstone of all subtypes of breast cancer treatment. Hen...

  • Review
  • Open Access
23 Citations
5,294 Views
25 Pages

Neuropharmacological Potential of Diterpenoid Alkaloids

  • Arash Salehi,
  • Mustafa Ghanadian,
  • Behzad Zolfaghari,
  • Amir Reza Jassbi,
  • Maryam Fattahian,
  • Parham Reisi,
  • Dezső Csupor,
  • Ikhlas A. Khan and
  • Zulfiqar Ali

This study provides a narrative review of diterpenoid alkaloids (DAs), a family of extremely important natural products found predominantly in some species of Aconitum and Delphinium (Ranunculaceae). DAs have long been a focus of research attention d...

  • Article
  • Open Access
8 Citations
5,395 Views
14 Pages

The Potential of Epigallocatechin-3-gallate (EGCG) as Complementary Medicine for the Treatment of Inflammatory Bowel Disease

  • Sabrina Schnur,
  • Fabian Hans,
  • Annika Dehne,
  • Janina Osti,
  • Malte-Ole Schneemann,
  • Marc Schneider and
  • Marius Hittinger

Complementary and alternative medicine has the potential to enrich conventional therapy to improve the treatment of various diseases. Patients that suffer from inflammatory bowel disease, which requires a constant need for medication, have to deal wi...

  • Article
  • Open Access
10 Citations
3,234 Views
14 Pages

The Effect of Oleanolic Acid and Its Four New Semisynthetic Derivatives on Human MeWo and A375 Melanoma Cell Lines

  • Barbara Bednarczyk-Cwynar,
  • Anna Leśków,
  • Izabela Szczuka,
  • Lucjusz Zaprutko and
  • Dorota Diakowska

This study aimed to synthesize four new semisynthetic derivatives of natural oleanolic acid (OA) and, based on an analysis of their cytotoxic and anti-proliferative effects against human MeWo and A375 melanoma cell lines, select those with anti-cance...

  • Article
  • Open Access
4 Citations
3,078 Views
24 Pages

Polyglactin 910 Meshes Coated with Sustained-Release Cannabigerol Varnish Inhibit Staphylococcus aureus Biofilm Formation and Macrophage Cytokine Secretion: An In Vitro Study

  • Mustafa Abudalu,
  • Muna Aqawi,
  • Ronit Vogt Sionov,
  • Michael Friedman,
  • Irith Gati,
  • Yaron Munz,
  • Gil Ohana and
  • Doron Steinberg

Synthetic surgical meshes are commonly used in abdominal wall reconstruction surgeries to strengthen a weak abdominal wall. Common mesh-related complications include local infection and inflammatory processes. Because cannabigerol (CBG) has both anti...

  • Article
  • Open Access
5 Citations
2,742 Views
18 Pages

Combination of Bacteriophages and Antibiotics for Prevention of Vascular Graft Infections—An In Vitro Study

  • Stefan Ruemke,
  • Evgenii Rubalskii,
  • Christina Salmoukas,
  • Kristina Hermes,
  • Ruslan Natanov,
  • Tim Kaufeld,
  • Oleksandr Gryshkov,
  • Vitalii Mutsenko,
  • Maxim Rubalsky and
  • Christian Kuehn
  • + 4 authors

(1) Background: Implant-associated bacterial infections are usually hard to treat conservatively due to the resistance and tolerance of the pathogens to conventional antimicrobial therapy. Bacterial colonization of vascular grafts may lead to life-th...

  • Article
  • Open Access
2 Citations
2,658 Views
11 Pages

Use Pattern of Ophthalmic Antiglaucoma Agents with and without Preservatives: A Cross-Sectional Study

  • Luis Fernando Valladales-Restrepo,
  • María Camila Oyuela-Gutiérrez,
  • Ana Camila Delgado-Araujo and
  • Jorge Enrique Machado-Alba

Background: Different drugs have been approved to reduce the intraocular pressure. However, most of them contain preservatives to maintain sterility and these can be toxic to the ocular surface. The aim was to determine the patterns of use of antigla...

  • Review
  • Open Access
20 Citations
15,415 Views
19 Pages

Ketamine and the Disinhibition Hypothesis: Neurotrophic Factor-Mediated Treatment of Depression

  • Philip Borsellino,
  • Reese I. Krider,
  • Deanna Chea,
  • Ryan Grinnell and
  • Thomas A. Vida

Ketamine is a promising alternative to traditional pharmacotherapies for major depressive disorder, treatment-resistant depression, and other psychiatric conditions that heavily contribute to the global disease burden. In contrast to the current stan...

  • Article
  • Open Access
6 Citations
2,777 Views
15 Pages

Immunohistochemical Expression of Glutathione Peroxidase 1 (Gpx-1) as an Independent Prognostic Factor in Colon Adenocarcinoma Patients

  • Marlena Brzozowa-Zasada,
  • Adam Piecuch,
  • Karolina Bajdak-Rusinek,
  • Kamil Janelt,
  • Marek Michalski,
  • Olesya Klymenko and
  • Natalia Matysiak

Several studies revealed that expression levels of glutathione peroxidase 1 (Gpx-1) can be associated with cancer development, mainly through its role in hydroperoxide scavenging by regulating intracellular reactive oxygen species (ROS) levels. There...

  • Article
  • Open Access
5 Citations
4,435 Views
17 Pages

Effects of Piper betle Extracts against Biofilm Formation by Methicillin-Resistant Staphylococcus pseudintermedius Isolated from Dogs

  • Arpron Leesombun,
  • Sivapong Sungpradit,
  • Norasuthi Bangphoomi,
  • Orathai Thongjuy,
  • Jantraporn Wechusdorn,
  • Sunee Riengvirodkij,
  • Jakaphan Wannawong and
  • Sookruetai Boonmasawai

Emergence of methicillin-resistant Staphylococcus pseudintermedius (MRSP) isolated from dogs with cutaneous and wound infections has significantly impacted veterinary medicine. This study aimed to isolate S. pseudintermedius from canine pyoderma and...

  • Article
  • Open Access
5 Citations
3,124 Views
11 Pages

Angelica keiskei Impacts the Lifespan and Healthspan of Drosophila melanogaster in a Sex and Strain-Dependent Manner

  • Mahtab Jafari,
  • Samuel E. Schriner,
  • Yun-Seo Kil,
  • Sally T. Pham and
  • Eun Kyoung Seo

Angelica keiskei is a perennial plant, belonging to the Apiaceae family and originating from Japan. This plant has been reported to act as a diuretic, analeptic, antidiabetic, hypertensive, tumor, galactagogue, and laxative. The mechanism of action o...

  • Review
  • Open Access
15 Citations
4,259 Views
18 Pages

Natural Products Targeting PI3K/AKT in Myocardial Ischemic Reperfusion Injury: A Scoping Review

  • Syarifah Aisyah Syed Abd Halim,
  • Norhashima Abd Rashid,
  • Choy Ker Woon and
  • Nahdia Afiifah Abdul Jalil

This scoping review aimed to summarize the effects of natural products targeting phosphoinositide-3-kinases/serine/threonine kinase (PI3K/AKT) in myocardial ischemia-reperfusion injury (MIRI). The review details various types of natural compounds suc...

  • Article
  • Open Access
7 Citations
3,595 Views
16 Pages

Quorum sensing (QS) is a cell-to-cell communication mechanism that regulates bacterial pathogenicity, biofilm formation, and antibiotic sensitivity. Among the identified quorum sensing, AI-2 QS exists in both Gram-negative and Gram-positive bacteria...

  • Review
  • Open Access
7 Citations
3,826 Views
16 Pages

Diabetes mellitus (DM) is a metabolic disease characterized by abnormal blood glucose levels-hyperglycemia, caused by a lack of insulin secretion, impaired insulin action, or a combination of both. The incidence of DM is increasing, resulting in bill...

  • Article
  • Open Access
10 Citations
4,545 Views
17 Pages

Design, Synthesis, and Evaluation of Niclosamide Analogs as Therapeutic Agents for Enzalutamide-Resistant Prostate Cancer

  • Borui Kang,
  • Madhusoodanan Mottamal,
  • Qiu Zhong,
  • Melyssa Bratton,
  • Changde Zhang,
  • Shanchun Guo,
  • Ahamed Hossain,
  • Peng Ma,
  • Qiang Zhang and
  • Florastina Payton-Stewart
  • + 1 author

Niclosamide effectively downregulates androgen receptor variants (AR-Vs) for treating enzalutamide and abiraterone-resistant prostate cancer. However, the poor pharmaceutical properties of niclosamide due to its solubility and metabolic instability h...

  • Review
  • Open Access
15 Citations
14,531 Views
40 Pages

Function and Role of Histamine H1 Receptor in the Mammalian Heart

  • Joachim Neumann,
  • Britt Hofmann,
  • Uwe Kirchhefer,
  • Stefan Dhein and
  • Ulrich Gergs

Histamine can change the force of cardiac contraction and alter the beating rate in mammals, including humans. However, striking species and regional differences have been observed. Depending on the species and the cardiac region (atrium versus ventr...

  • Review
  • Open Access
24 Citations
10,444 Views
41 Pages

Characterization of Pharmaceutical Tablets by X-ray Tomography

  • Jaianth Vijayakumar,
  • Niloofar Moazami Goudarzi,
  • Guy Eeckhaut,
  • Koen Schrijnemakers,
  • Veerle Cnudde and
  • Matthieu N. Boone

Solid dosage forms such as tablets are extensively used in drug administration for their simplicity and large-scale manufacturing capabilities. High-resolution X-ray tomography is one of the most valuable non-destructive techniques to investigate the...

  • Article
  • Open Access
1 Citations
2,387 Views
22 Pages

Long-lasting hyperglycaemia may alter the role of adenosine-dependent receptors (P1R) in the control of kidney function. We investigated how P1R activity affects renal circulation and excretion in diabetic (DM) and normoglycaemic (NG) rats; the recep...

  • Review
  • Open Access
25 Citations
31,408 Views
23 Pages

Synergistic Effects of Caffeine in Combination with Conventional Drugs: Perspectives of a Drug That Never Ages

  • Davide Ialongo,
  • Valeria Tudino,
  • Merve Arpacioglu,
  • Antonella Messore,
  • Elisa Patacchini,
  • Roberta Costi,
  • Roberto Di Santo and
  • Valentina Noemi Madia

Plants have been known since ancient times for their healing properties, being used as preparations against human diseases of different etiologies. More recently, natural products have been studied and characterized, isolating the phytochemicals resp...

  • Article
  • Open Access
3 Citations
2,307 Views
18 Pages

Consensus Ensemble Multitarget Neural Network Model of Anxiolytic Activity of Chemical Compounds and Its Use for Multitarget Pharmacophore Design

  • Pavel M. Vassiliev,
  • Dmitriy V. Maltsev,
  • Alexander A. Spasov,
  • Maxim A. Perfilev,
  • Maria O. Skripka and
  • Andrey N. Kochetkov

A classification consensus ensemble multitarget neural network model of the dependence of the anxiolytic activity of chemical compounds on the energy of their docking in 17 biotargets was developed. The training set included compounds thathadalready...

  • Article
  • Open Access
7 Citations
3,565 Views
12 Pages

Preparation Strategies of the Anti-Mycobacterial Drug Bedaquiline for Intrapulmonary Routes of Administration

  • Sara E. Maloney,
  • Ian E. Stewart,
  • Brendan K. Podell,
  • Hadley E. Gary,
  • Jeffrey B. Mecham,
  • Bryan J. Berube,
  • Susan L. Baldwin,
  • Rhea N. Coler and
  • Anthony J. Hickey

Mycobacterium tuberculosis (M.tb) has infected one-quarter of the world’s population and led to the deaths of 1.6 million individuals in 2021 according to estimates from the World Health Organization. The rise in prevalence of multidrug-resista...

  • Article
  • Open Access
1 Citations
2,628 Views
16 Pages

Pharmacokinetic Study and Metabolite Identification of CAM106 in Rats by Validated UHPLC-MS/MS

  • Ruqi Xi,
  • Rahima Abdulla,
  • Jiangyu Zhao,
  • Haji Akber Aisa and
  • Yongqiang Liu

Given the limitations of existing antiviral drugs and vaccines, there is still an urgent need for new anti-influenza drugs. CAM106, a rupestonic acid derivative, was studied for its potent antiviral activity and showed a favorable inhibitory effect o...

  • Article
  • Open Access
8 Citations
2,931 Views
13 Pages

α-Viniferin-Induced Apoptosis through Downregulation of SIRT1 in Non-Small Cell Lung Cancer Cells

  • Cheng Huang,
  • Zi-Jun Lin,
  • Jui-Chieh Chen,
  • Hao-Jun Zheng,
  • Yu-Heng Lai and
  • Hsiu-Chen Huang

α-Viniferin, a natural stilbene compound found in plants and a polymer of resveratrol, had demonstrated potential anti-cancer and anti-inflammatory effects. However, the specific mechanisms underlying its anti-cancer activity were not yet fully...

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Pharmaceuticals - ISSN 1424-8247