Ethnopharmacological Relevance: Quercetin is a ubiquitous flavonoid that is present in numerous plants that are utilized in many different cultures for their nervous system and anticancer effects. To better understand the neuroprotective and antiproliferative activities of quercetin, we present a comprehensive review of the divergent actions that contribute to the ethnopharmacological profile of these plants.
Results: The pharmacological activities of quercetin that modulate antioxidation/oxidation/kinase-signaling pathways might be differentially elicited in neurons compared with malignant cells, ultimately promoting cell survival or death in a cell type- and metabolism-specific manner. Whereas the broad antioxidation and anti-inflammatory activities of quercetin are important for neuronal survival, the oxidative, kinase- and cell cycle-inhibitory, apoptosis-inducing effects of quercetin are essential for its anticancer effects. The diverse mechanistic interactions and activities of quercetin that modulate the phosphorylation state of molecules as well as gene expression would alter the interconnected and concerted intracellular signaling equilibrium, either inhibiting or strengthening survival signals. These mechanisms, which have been mainly observed in in vitro studies, cannot be easily translated into an explanation of the divergent simultaneous neuroprotective and anticancer effects observed in vivo. This is in part due to low bioavailability in plasma and in the brain, as well as the nature of the actual active molecules.
Conclusions: Numerous studies have demonstrated the beneficial effects of chronic quercetin intake, which is ethnopharmacologically meaningful, as many plants that are chronically ingested by people contain quercetin. Although quercetin and quercetin-containing plants exhibit potential as therapeutic modalities in neuropathology and in cancer, the data collectively highlight the need to elucidate issues such as bioavailability as well as its correlation with effectiveness at biomarkers in vivo. There would be an increased potentential of these plants for chemoprevention and neuropathology prevention.
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http://dx.doi.org/10.1016/j.jep.2012.07.005 | DOI Listing |
Semin Oncol Nurs
January 2025
Nursing Department, Cyprus University of Technology, Limassol, Cyprus.
Objectives: Cancer-related cachexia affects approximately 50% to 80% of cancer patients and contributes significantly to cancer-related mortality, accounting for 20% of deaths. This multifactorial syndrome is characterized by systemic inflammation, anorexia, and elevated energy expenditure, leading to severe weight loss and muscle wasting. Understanding the underlying mechanisms is critical for developing effective interventions.
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December 2024
Department of Food Science and Biotechnology, Sejong University, Gwangjin-gu, Seoul, Republic of Korea. Electronic address:
For the first time, our study provides a comprehensive examination of the anti-cancer effects of structural isomers of carene in breast cancer cells, specifically focusing on cell cycle inhibition and the induction of apoptosis. We utilized the hydro-distillation method to extract Piper nigrum seed essential oil (PNS-EO) and identified its bioactive components through gas chromatography-mass spectrometry (GC-MS) analysis. A total of 46 bioactive compounds were isolated via hydro-distillation, identified through GC-MS analysis, and validated by co-injection using GC analysis.
View Article and Find Full Text PDFComput Biol Med
January 2025
Drug Design and Discovery Lab, Helmy Institute of Medical Sciences, Zewail City of Science, Technology and Innovation, Giza, 12578, Egypt; Biomedical Sciences Program, University of Science and Technology, Zewail City of Science, Technology and Innovation, Giza, 12578, Egypt. Electronic address:
Epidermal growth factor receptor (EGFR) is amongst the earliest targeted kinases by small-molecule inhibitors for the management of EGFR-positive cancer types. While a few inhibitors are granted FDA approval for clinical use, discovery of new inhibitors is still of merit to enhance ligand-binding stability and subsequent enzyme inhibition. Thus, a structure-based design approach was adopted to devise a new series of twenty-nine N3-substituted quinazolin-4-ones as type I ATP-competitive inhibitors targeting the deep hydrophobic pocket of EGFR.
View Article and Find Full Text PDFInt Immunopharmacol
January 2025
Department of Urology, Shanghai Children's Medical Center, School of Medicine, Shanghai Jiao Tong University, No. 1678 Dongfang Road, Pudong New Area, Shanghai 200127, China. Electronic address:
Hedyotis diffusa Willd. (HDW), a traditional Chinese medicinal plant, exhibits a variety of pharmacological effects and has anticancer potential for a wide range of cancer types; Ferroptosis is a non-apoptosis-regulated cell death induced by iron accumulation and subsequent lipid peroxidation; and there is currently an increasing interest in the therapeutic role of ferroptosis in cancer. However, the effects of HDW on bladder cancer and its underlying molecular mechanisms remain largely unknown.
View Article and Find Full Text PDFEur J Med Chem
December 2024
Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China. Electronic address:
Concurrent inhibition of HDAC and BRD4, two well-established epigenetic targets for anti-tumor therapy, demonstrates the potential to enhance anti-tumor effects synergistically. The present study involves the development of a series of novel HDAC3/BRD4 dual inhibitors, followed by evaluation of their antitumor efficacy against several tumor models. Guided by scaffold hopping strategy, key pharmacophore of BRD4 inhibitor I-BET-151 was incorporated into an in-house developed HDAC3-selective inhibitor 17h.
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