181 results match your criteria: "University of Hertfordshire Hosted by Global Academic Foundation[Affiliation]"

Ethnopharmacological Relevance: Mangifera indica (family Anacardiaceae), often acknowledged as mango and renowned for being a plant of diverse ethnopharmacological background since ancient times, harbors the polyphenolic bioactive constituent, mangiferin (MNG). MNG is a major phytochemical of Mangifera indica and other plants with a wide range of reported pharmacological activities, including antioxidant, anti-inflammatory, neuroprotective and hepatoprotective effects. MNG has also been utilized in traditional medicine; it is reportedly a major bioactive element in over 40 polyherbal products in traditional Chinese medicine (TCM), and two prominent anti-inflammatory, immunomodulatory and antiviral Cuban formulations.

View Article and Find Full Text PDF

Targeting the ubiquitin proteasome system in cancer stem cells.

Trends Cell Biol

December 2024

Biochemistry Department, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt. Electronic address:

Over the past few years there has been an alarming burst of cancer burden worldwide. Cancer stem cells (CSCs) act as hidden devils within tumors, rendering cancer therapy a strenuous goal. Recently, the ubiquitin proteasome system (UPS) was proved to be an essential contributor to the CSC phenotype.

View Article and Find Full Text PDF

Many plants are reported to enhance cognition in amnesic-animal models. The metabolite profile of fruit methanolic extract (CDFME) was characterized by LC-QTOF-MS/MS, and its total phenolics content (TPC) and total flavonoids content (TFC) were determined. In parallel, its cognitive-enhancing effect on scopolamine (SCOP)-induced AD in rats was evaluated.

View Article and Find Full Text PDF

Chemoresistance encountered using conventional chemotherapy demands novel treatment approaches. Asplatin (Asp), a novel platinum (IV) prodrug designed to release cisplatin and aspirin in a reductive environment, has demonstrated high cytotoxicity at reduced drug resistance. Herein, we investigated the ability of green-synthesized nanocarriers to enhance Asp's efficacy.

View Article and Find Full Text PDF

Introduction: Atopic dermatitis (AD) is a type of chronic inflammatory disorder that affects all age groups including children. AD is characterized by elevated inflammatory marker levels.

Aim: To assess the safety and effectiveness of topical tacrolimus ointment versus topical hydrocortisone cream in the treatment of pediatric AD by comparing the two treatments' ability to reduce serum cytokines.

View Article and Find Full Text PDF

Discovery of a novel, selective CK2 inhibitor class with an unusual basic scaffold.

Eur J Med Chem

January 2025

Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C2.3, 66123, Saarbrücken, Germany. Electronic address:

Article Synopsis
  • CK2 is an important enzyme involved in cell growth and survival, making it a potential target for cancer treatments, but many existing inhibitors are not selective enough.
  • Researchers discovered a new compound, a dihydropyrido-thieno[2,3-d]pyrimidine derivative, which showed strong inhibitory activity against CK2α and was notable for its unique chemical structure.
  • The most effective compound, 10b, had an IC value of 36.7 nM and demonstrated good selectivity and cellular activity against certain cancer cell lines, outperforming existing inhibitors in terms of inducing cell death.
View Article and Find Full Text PDF

A series of novel molecules with pyrazolopyrimidine-4-amine core were designed and synthesized as potential cytotoxic agents over Renal Cell Carcinoma cells (UO-31). Results of cytotoxic activity against UO-31 cells showed that pyrazolopyrimidines 19 and 31 were found to be more cytotoxic than sorafenib (SOR). The cytotoxic activity of these compounds appeared to correlate with their ability to inhibit p38α MAPK which are 2.

View Article and Find Full Text PDF

DZH2, a dual inhibitor of the chemokine receptors CCR5 and CXCR4, was discovered from virtual screening for CCR5 antagonists. In specific Ca chemokine signaling assays, DZH2 displayed low micromolar IC values at both chemokine receptors. Its binding to intracellular allosteric binding sites of CCR5 and CXCR4 was confirmed by MD simulations and binding free-energy calculations.

View Article and Find Full Text PDF

, has been widely recognized for its medical applications. LC-ESI-TOF-MS identified 22 secondary metabolites including phenolics, flavonoids, and anthocyanidin glycosides among its total extract (LCTE). The study aimed to apply LCTE as a biogenic material for reducing and capping the silver nanoparticles (LC-AgNPs).

View Article and Find Full Text PDF
Article Synopsis
  • Carboplatin is effective against cancer but has significant side effects, prompting researchers to explore the use of nanoparticle formulations with frankincense extract to enhance its effectiveness.
  • The study developed nanoparticles (Cp@CS/BME NPs) that increased the uptake and cancer cell-killing ability of carboplatin, particularly in acidic tumor environments.
  • In vitro results showed these nanoparticles improve apoptosis in colorectal cancer cell lines by lowering anti-apoptotic genes and promoting pro-apoptotic gene expression, suggesting a more effective and safer chemotherapy approach.
View Article and Find Full Text PDF

This study explores the impact of γ-irradiation on ethanolic extracts of Solanum aculeastrum Dunal. The anti-cancer and antimicrobial properties were investigated. The obtained results revealed that total phenol (TP) and total flavonoid (TF) of total ethanol extract (100%) (FTE) were higher than 70% ethanol extract (SE), and these contents increased after gamma radiation with 5 kGy.

View Article and Find Full Text PDF

Design, synthesis, and structure-activity relationship studies of 6-benzo[]indeno[1,2-]thiophen-6-one derivatives as DYRK1A/CLK1/CLK4/haspin inhibitors.

RSC Med Chem

October 2024

Universite Claude Bernard Lyon 1, CNRS UMR 5246, Institut de Chimie et Biochimie Moléculaires et Supramoléculaires (ICBMS), COSSBA Team, Faculté de Pharmacie, ISPB 8, avenue Rockefeller F-69373 Lyon Cedex 08 France

A series of sulfur-containing tetracycles was designed and evaluated for their ability to inhibit protein kinase DYRK1A, a target known to have several potential therapeutic applications including cancers, Down syndrome or Alzheimer's disease. Our medicinal chemistry strategy relied on the design of new compounds using ring contraction/isosteric replacement and constrained analogy of known DYRK1A inhibitors, thus resulting in their DYRK1A inhibitory activity enhancement. Whereas a good inhibitory effect of targeted DYRK1A protein was observed for 5-hydroxy compounds 4i-k (IC = 35-116 nM) and the 5-methoxy derivative 4e (IC = 52 nM), a fairly good selectivity towards its known DYRK1B off-target was observed for 4k.

View Article and Find Full Text PDF

Background: Over the past decades, a substantial portion of the population worldwide has been infected with varicella zoster and most cases developed shingles. Unfortunately, shingles is usually accompanied by postherpetic neuralgia, which may persist for months to years after the resolution of the viral infection.

Objectives: Gabapentin is an orally gamma-aminobutyric acid analogue approved by the Food and Drug Administration to manage shingles postherpetic neuralgia.

View Article and Find Full Text PDF

The development of anticancer drugs targeting both PI3K and mTOR pathways is recognized as a promising cancer therapeutic approach. In the current study, we designed and synthesized seventeen new thiazole compounds to investigate their effect on both PI3K and mTOR as well as their anti-apoptotic activity. All the synthesized thiazoles were investigated for their antiproliferative activity on a panel of 60 different cancer cell lines at the National Cancer Institute.

View Article and Find Full Text PDF

Gastric cancer (GC) remains a major public health challenge worldwide. Long non-coding RNAs (lncRNAs) play important roles in the development, progression, and resistance to the treatment of GC, as shown by recent developments in molecular characterization. Still, an in-depth investigation of the lncRNA landscape in GC is absent.

View Article and Find Full Text PDF

Despite recent advancements in cancer therapies, challenges such as severe toxic effects, non-selective targeting, resistance to chemotherapy and radiotherapy, and recurrence of metastatic tumors persist. Consequently, there has been considerable effort to explore innovative anticancer compounds, particularly in immunotherapy, which offer the potential for enhanced biosafety and efficacy in cancer prevention and treatment. One such avenue of exploration involves the miRNA-34 (miR-34) family, known for its ability to inhibit tumorigenesis across various cancers.

View Article and Find Full Text PDF

Targeting neutrophil function has gained attention as a propitious therapeutic strategy for diverse inflammatory diseases. Accordingly, a series of enone-based derivatives were developed to inhibit neutrophil-mediated inflammation, showing promise for treating inflammatory diseases. These compounds fall into two clusters with distinct effects: one inhibits neutrophilic superoxide (SO) anion production and elastase release triggered by N-formyl-Met-Leu-Phe (fMLF), with compound being most effective (IC values of 1.

View Article and Find Full Text PDF

Colorectal cancer (CRC) is recognized as one of the most prevalent malignancies, both in terms of incidence and mortality rates. Current research into CRC has shed light on the molecular mechanisms driving its development. Several factors, including lifestyle, environmental influences, genetics, and diet, play significant roles in its pathogenesis.

View Article and Find Full Text PDF

Objectives: The aim of the current study was to assess the natural course of partial remission (PR) phase of type 1 diabetes (T1D) and to highlight the putative association between vitamin D receptor (VDR) (Fok1) gene polymorphism and PR phase.

Methods: Ninety participants with newly diagnosed T1D were followed up for a total of 12 months. The VDR (Fok1) rs2228570 gene polymorphism was genotyped using allelic discrimination (AD) assay.

View Article and Find Full Text PDF

This study uses the aerial parts of total extract (PMTE) to synthesize silver nanoparticles (AgNPs) in an environmentally friendly manner. TEM, SEM, FTIR, X-ray powder diffraction (XRD), Zeta potential, UV, and FTIR were used to characterize the green silver nanoparticles (PM-AgNPs). PM-AgNPs were evaluated as anticancer agents compared to (PMTE) against breast (MCF-7), lung (A549), and ovary adenocarcinoma (SKOV3) human tumour cells.

View Article and Find Full Text PDF
Article Synopsis
  • Fungal infections are a major health issue in developing countries, prompting the need for better treatment methods.
  • Oral antifungal medications have severe side effects, making topical delivery systems a safer option.
  • Ultra-deformable penetration enhancer vesicles (PEVs) were created using Labrasol and Transcutol to improve the delivery of Fluconazole, showing promising antifungal effectiveness and stable performance over six months.
View Article and Find Full Text PDF

Gastric cancers (GCs) are among the most common and fatal malignancies in the world. Despite our increasing understanding of the molecular mechanisms underlying GC, further biomarkers are still needed for more in-depth examination, focused prognosis, and treatment. GC is one among the long non-coding RNAs, or lncRNAs, that have emerged as key regulators of the pathophysiology of cancer.

View Article and Find Full Text PDF

Management of rheumatoid arthritis (RA) requires long-term administration of different medications since there has been no cure until now. Etodolac (ETD) is a nonsteroidal anti-inflammatory drug commonly used for RA management. However, its long-term administration resulted in severe side effects.

View Article and Find Full Text PDF

Dysregulation of the CXCL12/CXCR4 axis is implicated in autoimmune, inflammatory, and oncogenic diseases, positioning CXCR4 as a pivotal therapeutic target. We evaluated optimized variants of the specific endogenous CXCR4 antagonist, EPI-X4, addressing existing challenges in stability and potency. Our structure-activity relationship study investigates the conjugation of EPI-X4 derivatives with long-chain fatty acids, enhancing serum albumin interaction and receptor affinity.

View Article and Find Full Text PDF
Article Synopsis
  • Gallbladder cancer (GBC) is a highly aggressive cancer with a low survival rate, influenced significantly by long noncoding RNAs (lncRNAs) and natural products that affect cancer behaviors such as proliferation and metastasis.
  • Natural compounds like curcumin and baicalein have shown potential in fighting GBC by targeting crucial signaling pathways.
  • Specific lncRNAs can serve as biomarkers for diagnosing and predicting GBC, and targeting these lncRNAs holds promise for improving treatment outcomes and reducing resistance to therapies.
View Article and Find Full Text PDF