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Pharmaceutical Sciences and Drug Design

Volume 4, Issue 2 (2024)

Targeting ADRB2 Signaling with 10-Gingerol Enhances the Chemotherapeutic Response to Paclitaxel in Triple-Negative Breast Cancer
Downloads: 33
Views: 414
Written by Amelie Dubois   Published on Vol 4 Issue 2, 2024
Paclitaxel is a key drug in cancer therapy, yet its clinical benefit is often constrained by pronounced toxicity and the development of resistance. 10-Gingerol (10-G), a naturally occurring ginger-derived molecule with known anti-inflammatory and antiproliferative actions, has been proposed as a potential chemosensitizer. However, its influence on the response of triple-negative breast cancer (TNBC) to paclitaxel has not been clearly defined. This work investigates whether 10-G can improve pacli
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Mechanistic Insights Into Vancomycin-Induced Renal Injury: The Role of Ferroptosis and GPX4 Suppression
Downloads: 30
Views: 361
Written by Gabriel Johansen   Published on Vol 4 Issue 2, 2024
Vancomycin (VCM) is commonly used to treat infections caused by Gram-positive bacteria. However, over the past decades, VCM overdose has increasingly been linked to kidney damage. The mechanisms driving this nephrotoxicity remain incompletely understood. This study aimed to investigate how VCM induces renal injury.Kidney tissues from mice were analyzed for the expression of Ki67, DDX5, PTGS2, GPX4, and SLC7A11 using immunohistochemistry, RT-qPCR, and Western blot. In parallel, HK-2 cells were as
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Mechanistic Insights into Zuogui Jiangtang Shuxin Formula for Diabetic Cardiomyopathy: An Integrated Serum Pharmacochemistry and Network Pharmacology Study
Downloads: 37
Views: 383
Written by Hiroshi Tanaka   Published on Vol 4 Issue 2, 2024
This research aimed to elucidate the mechanisms through which the Zuogui Jiangtang Shuxin formula (ZGJTSXF) alleviates diabetic cardiomyopathy (DCM) using a combined approach of serum pharmacochemistry, network pharmacology, and experimental validation.Following oral administration of ZGJTSXF in rats, serum compounds were analyzed using UPLC-Q-Exactive-Orbitrap-MS. A network linking bioactive components of ZGJTSXF to DCM-associated targets was established with Cytoscape. Functional enrichment an
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Protective Effects of Sichen Formula on LPS-Induced Acute Lung Injury via Modulation of TLR4 Signaling Pathways
Downloads: 32
Views: 315
Written by Xiao Li   Published on Vol 4 Issue 2, 2024
Sichen (SC) formula, a well-known Tibetan medicinal preparation, has been traditionally applied to treat respiratory ailments in Tibet due to its anti-inflammatory potential. This study aimed to systematically investigate its anti-inflammatory effects and the molecular mechanisms involved.The chemical profile of SC was analyzed using HPLC. An acute lung injury (ALI) model in mice was established by intratracheal administration of lipopolysaccharide (LPS), with subsequent collection of bronchoalv
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Enhanced Therapeutic Efficacy of Dexamethasone in Experimental Ulcerative Colitis via Mucoadhesive Nanoparticle-Based Enema Delivery
Downloads: 38
Views: 466
Written by Caroline Fischer   Published on Vol 4 Issue 2, 2024
Glucocorticoids (GCs) are the primary treatment for ulcerative colitis (UC), but their long-term use is associated with severe systemic toxicity and side effects. Local delivery via enema can enhance GC concentrations at the site of inflammation in the distal colon while minimizing systemic exposure. However, frequent diarrhea in UC patients often shortens colonic residence time, limiting the therapeutic efficacy of GCs.This study aimed to develop mucoadhesive nanoparticles (NPs) carrying differ
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Indirect ^18F-Labeling of Estradiol via Automated Click Chemistry: Radiochemical Development and In Vitro Evaluation
Downloads: 32
Views: 512
Written by Ayesha Khan   Published on Vol 4 Issue 2, 2024
Click chemistry provides a powerful method for selectively linking diverse molecular building blocks to create sophisticated molecules efficiently. Here, we report the use of copper(I)-catalyzed biorthogonal cycloaddition between alkynes and azides for the indirect incorporation of fluorine-18 into an estradiol-based compound, aimed at imaging estrogen receptors. The synthesis protocol was entirely established and refined using an automated module, with parameters adjusted to deliver the target
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Comprehensive Structure-Based In Silico Identification of IRESSA as a Multitarget Inhibitor of Key Breast Cancer Signaling Proteins
Downloads: 34
Views: 266
Written by Thomas Berger   Published on Vol 4 Issue 2, 2024
Breast cancer originates in breast tissue cells and primarily affects women. It typically begins in the cells lining the milk ducts or the lobules that produce milk, with the potential to invade surrounding tissues and metastasize to distant parts of the body. In 2020, approximately 2.3 million women worldwide were diagnosed with the disease, resulting in an estimated 685,000 deaths. Furthermore, 7.8 million women were alive with a breast cancer diagnosis, establishing it as the fifth leading ca
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QSAR-Guided Identification of Novel Triazole Derivatives as Potent α-Glucosidase Inhibitors with Favorable ADMET Profiles
Downloads: 29
Views: 444
Written by Maria Gonzalez   Published on Vol 4 Issue 2, 2024
Due to the rising incidence of diabetes mellitus and the drawbacks of existing therapies, there is an urgent demand for new therapeutic agents targeting this condition. This research concentrates on developing novel compounds with potent alpha-glucosidase inhibitory activity, a key enzyme in managing diabetes. A series of 33 triazole derivatives was subjected to comprehensive QSAR analysis to determine the critical factors affecting their α-glucosidase inhibitory potency. Based on the multiple l
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Aptamer- and Transferrin-Codecorated Nanoparticles for Synergistic Delivery of Daunorubicin and Luteolin in Leukemia
Downloads: 28
Views: 324
Written by Anders Nilsson   Published on Vol 4 Issue 2, 2024
The purpose of this research was to create a binary nanodrug-delivery platform functionalized with aptamers (APs) and transferrin (Tf), and encapsulating daunorubicin (Drn) and luteolin (Lut) for leukemia therapy. Oligonucleotide ligands containing APs and Tf were designed and synthesized independently. AP-functionalized nanoparticles loaded with Drn (AP-Drn NPs) and Tf-functionalized nanoparticles loaded with Lut (Tf-Lut NPs) were fabricated through self-assembly. A binary nanodrug-delivery sys
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Antiproliferative Activity of Novel Isosteviol-Derived 1,3-Aminoalcohols: Synthesis and Structure–Activity Relationships
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Views: 395
Written by Marco Rossi   Published on Vol 4 Issue 2, 2024
A series of diterpenoid 1,3-aminoalcohol derivatives was synthesised from isosteviol through stereoselective transformations. Isosteviol was obtained via acid-catalysed hydrolysis and rearrangement of natural stevioside and subsequently converted to the key methyl ester intermediate. A 1,3-aminoalcohol library was then constructed by reductive amination of the 3-hydroxyaldehyde intermediate derived from isosteviol in a two-step process. To evaluate the influence of the carboxylate ester at posit
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