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Revitalizing Cancer Treatment: Exploring the Role of Drug Repurposing.

Cancer persists as a global challenge necessitating continual innovation in treatment strategies. Despite significant advancements in comprehending the disease, cancer remains a leading cause of mortality worldwide, exerting substantial economic burdens on healthcare systems and societies. The emergence of drug resistance further complicates therapeutic efficacy, underscoring the urgent need for alternative approaches. Drug repurposing, characterized by the utilization of existing drugs for novel clinical applications, emerges as a promising avenue for addressing these challenges. Repurposed d

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… Another study reported that micelles containing mebendazole (MBZ) reduced the expression of vascular endothelial growth factor (VEGF), akin to the established kinase inhibitor sorafenib [ 62 ]. … In Silico and In Vitro Studies for Benzimidazole Anthelmintics Repurposing as VEGFR-2 Antagonists: Novel Mebendazole-Loaded Mixed Micelles with Enhanced Dissolution and Anticancer Activity. ACS Omega. 2022;7:875–899. doi: 10.1021/acsomega.1c05519. 63. …

Положительный эффект эвобрютиниба в моделях ремиэлирования CNS и отсутствие синергизма с исследованием реакции на дозу клемастина-А.

Чтобы восстановить нормальные функции, крайне важно воспоминание в множестве склерозов. Несмотря на эндогенное восстановление, его часто недостаточно, и необходимо найти молекулы, способствующие восстановлению демиелинированных повреждений. БИДЖЕКЦЫ: Сравнение потенциала ремимилинации эвобротиниба, ингибитора тиросиновой кинеазы и клемастина Брютона, антагонистического рецептора M1 Muscarinic ацетилхолина. МЕТОДЫ: Ремиелинация была исследована в лизолицитинах, обезжиренных органотипными кусочками мыши, и трансгенной модели ксенопа инъецируемого демиелинирования.РЕЗУЛЬТАТЫ: Эвобрутиниб (Evobrut

Keyword Index for Volume 91

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From laboratory to clinic: opportunities and challenges of functional food active ingredients in cancer therapy.

This review provides a comprehensive analysis of the potential of functional food active ingredients in cancer prevention and therapy. It outlines the multifaceted anticancer mechanisms of bioactive compounds-such as polyphenols, carotenoids, omega-3 fatty acids, phytosterols, alkaloids, isothiocyanates, polysaccharides, phenolic acids, flavonols, and amide-bearing compounds-which include antioxidant and anti-inflammatory activities, induction of apoptosis and autophagy, modulation of the tumor microenvironment, interference with cell cycle regulation and signaling pathways, and regulation of

Emerging Target Discovery Strategies Drive the Decoding of Therapeutic Power of Natural Products and Further Drug Development: A Case Study of Celastrol.

Celastrol (CEL) is a natural pentacyclic triterpenoid demonstrating significant therapeutic properties against various diseases. However, the ambiguity of target information poses a significant challenge in transitioning CEL from a traditional remedy to a modern pharmaceutical agent. Recently, the emerging target discovery approaches of natural products have broadened extensive avenues for uncovering comprehensive target information of CEL and promoting its drug development. Herein, diverse target discovery strategies are overviewed for the pharmacological and toxicological studies of CEL, inc

Anti-Cancer Stem-like Cell Compounds in Clinical Development - An Overview and Critical Appraisal.

Cancer stem-like cells (CSC) represent a subpopulation of tumor cells with elevated tumor-initiating potential. Upon differentiation, they replenish the bulk of the tumor cell population. Enhanced tumor-forming capacity, resistance to antitumor drugs, and metastasis-forming potential are the hallmark traits of CSCs. Given these properties, it is not surprising that CSCs have become a therapeutic target of prime interest in drug discovery. In fact, over the last few years, an enormous number of articles describing compounds endowed with anti-CSC activities have been published. In the meanwhile,

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… Thus, PEGylated polymeric micelles were loaded with salinomycin to effectively target breast CSCs and shown to be more effective than salinomycin in vivo ( 204 ). …

Novel Investigations of Flavonoids as Chemopreventive Agents for Hepatocellular Carcinoma.

We would like to highlight the application of natural products to hepatocellular carcinoma (HCC). We will focus on the natural products known as flavonoids, which target this disease at different stages of hepatocarcinogenesis. In spite of the use of chemotherapy and radiotherapy in treating HCC, patients with HCC still face poor prognosis because of the nature of multidrug resistance and toxicity derived from chemotherapy and radiotherapy. Flavonoids can be found in many vegetables, fruits, and herbal medicines that exert their different anticancer effects via different intracellular signalin

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… Polymeric micelles have the ability to encapsulate a hydrophobic drug and deliver the drug to the desired site at a concentration exceeding the intrinsic solubility of the drug. … Duan et al. have developed mixed micelles loaded with a Silibinin-polyene phosphatidylcholine complex to improve its drug solubility and prolong its mean retention time in vivo [ 242 ]. …

Anticancer peptides as novel immunomodulatory therapeutic candidates for cancer treatment.

Cancer remains a concern after years of research in this field. Conventional therapies such as chemotherapy, radiation, and surgery are available for cancer treatment, but they are characterized by various side effects. There are several immunological challenges that make it difficult for the immune system and conventional therapies to treat cancer. Some of these challenges include heterogeneity, resistance to medicines, and cancer relapse. Even advanced treatments like immune checkpoint inhibitors (ICIs), which revolutionized cancer treatment, have associated toxicity and resistance further n

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… Yang et al. [ 109 ] (2014) used polydiacetylene micelles to deliver magainin-II and reported improved cytotoxicity both in in vitro and in vivo model systems (A549 cells and mice respectively). … Magainin II modified polydiacetylene micelles for cancer therapy. Nanoscale. 2014;6:14772–83. doi: 10.1039/c4nr04405c. 110. Chen PM, Yen ML, Liu KJ, Sytwu HK, Yen BL. Immunomodulatory properties of human adult and fetal multipotent mesenchymal stem cells. …

From bench to bedside: the application of cannabidiol in glioma.

Glioma is the most common malignant tumor in central nervous system, with significant health burdens to patients. Due to the intrinsic characteristics of glioma and the lack of breakthroughs in treatment modalities, the prognosis for most patients remains poor. This results in a heavy psychological and financial load worldwide. In recent years, cannabidiol (CBD) has garnered widespread attention and research due to its anti-tumoral, anti-inflammatory, and neuroprotective properties. This review comprehensively summarizes the preclinical and clinical research on the use of CBD in glioma therapy

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… Nanotechnological assemblies of CBD are primarily categorized into lipid-based nanocarriers (such as nanoliposomes, nanoemulsions, nanostructured lipid carriers (NLCs), and solid lipid nanoparticles (SLNs), vesicles [ 97 ], etc.), polymer carriers (including micelles [ 98 ], poly-lactic-co-glycolic acid … Nanocomposite cryogel carriers from 2-hydroxyethyl cellulose network and cannabidiol-loaded polymeric micelles for sustained topical delivery. Polymers (Basel) 2020;12(5):1172. doi: 10.3390/polym12051172. 99. Fraguas-Sánchez AI, Torres-Suárez AI, Cohen M, Delie F, Bastida-Ruiz D, Yart L, et al. …

Current Landscape and Future Directions in Cancer Immunotherapy: Therapies, Trials, and Challenges.

Cancer remains a leading global health challenge, placing immense burdens on individuals and healthcare systems. Despite advancements in traditional treatments, significant limitations persist, including treatment resistance, severe side effects, and disease recurrence. Immunotherapy has emerged as a promising alternative, leveraging the immune system to target and eliminate tumour cells. However, challenges such as immunotherapy resistance, patient response variability, and the need for improved biomarkers limit its widespread success. This review provides a comprehensive analysis of the curr

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… Similarly, Jiang et al. [ 111 ] investigated micelle-tailored vaccines that facilitate the cytosolic delivery of antigens, which is crucial for activating CD8+ T cells and generating a robust immune response against tumours. … Jin et al. [ 220 ] indicated that nanomaterials such as carbon nanotubes and polymeric micelles have shown considerable benefits in drug design, enhancing the delivery of therapeutic agents while minimising systemic toxicity. …

GD2: hopes and challenges for the treatment of pediatric patients with tumors of the central nervous system.

Pediatric Central Nervous System (CNS) tumors are the leading cause of cancer-related death in children, yet effective treatment options remain limited. The tumor-associated antigen GD2 is a promising target for immunotherapeutic approaches aimed at treating pediatric CNS cancers; however, its heterogeneous expression within and between tumors can complicate the development of effective strategies. Here we review different aspects of GD2 biology, including its structure, synthesis pathway, and cellular and tissue expression, focusing on pediatric CNS tumors. We provide a detailed overview of t

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… It has also to be noted that GD2 can be shed from the cytoplasmic membrane as micelles or extracellular vesicles, which can be incorporated into GD2-negative neighboring cells, influencing their behavior 12 . … As mentioned, GD2 can be released from the cytoplasmic membrane through extracellular vesicles or micelles, and, thus, it can be found in the serum or be incorporated in neighboring cells. …

NF-κB in Cell Deaths, Therapeutic Resistance and Nanotherapy of Tumors: Recent Advances.

The transcription factor nuclear factor-κB (NF-κB) plays a complicated role in multiple tumors. Mounting evidence demonstrates that NF-κB activation supports tumorigenesis and development by enhancing cell proliferation, invasion, and metastasis, preventing cell death, facilitating angiogenesis, regulating tumor immune microenvironment and metabolism, and inducing therapeutic resistance. Notably, NF-κB functions as a double-edged sword exerting positive or negative influences on cancers. In this review, we summarize and discuss recent research on the regulation of NF-κB in cancer cell deaths,

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… Furthermore, siNF-κB could also be encapsulated in polymeric micelle NPs and carried to tumor tissues or metastatic sites via intravenous administration, thereby inhibiting melanoma migration/invasion and pulmonary metastasis [ 161 ]. … Anti-Metastatic Effects on Melanoma via Intravenous Administration of Anti-NF-ΚB SiRNA Complexed with Functional Peptide-Modified Nano-Micelles Pharmaceutics 2020 12 64 10.3390/pharmaceutics12010064 31952106 PMC7022256 162. Gao X. Wu Y. Qiao L. Feng X. …

Involvement of Resveratrol against Brain Cancer: A Combination Strategy with a Pharmaceutical Approach.

A brain tumor (BT) is a condition in which there is growth or uncontrolled development of the brain cells, which usually goes unrecognized or is diagnosed at the later stages. Since the mechanism behind BT is not clear, and the various physiological conditions are difficult to diagnose, the success rate of BT is not very high. This is the central issue faced during drug development and clinical trials with almost all types of neurodegenerative disorders. In the first part of this review, we focus on the concept of brain tumors, their barriers, and the types of delivery possible to target the b

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… For example, liposomes, nanoparticles (NPs), and polymeric micelles are examples of novel DDSs that can be responsive tools for targeting the brain without causing toxicity in the nasal mucosa and CNS [ 109 ]. … Numerous nanoparticles, including liposomes, polymeric nanoparticles, micelles, dendrimers, and gold nanoparticles, have been studied for their anticancer drug delivery efficacy. …

Thiostrepton Suppresses the Progression of Rhabdomyosarcoma by Inhibiting the PI3K-AKT Signaling Pathway.

Rhabdomyosarcoma (RMS), the most common pediatric soft tissue sarcoma with 5-year survival below 30% in high-risk/metastatic cases, was investigated through integrated bioinformatics analysis (identifying 269 conserved differentially expressed genes in GEO datasets GSE28511/GSE141690) and experimentally validated thiostrepton (TST), a ribosomal-targeting antibiotic, as a potent therapeutic candidate via Connectivity Map analysis (p p AKT, JAK, CDKs). This was confirmed by PI3K activator 740 Y-P rescue experiments, which partially reversed the effects of TST (p < 0.05). These findings establish

Colorectal Cancer at the Crossroads: The Good, the Bad, and the Future of Platinum-Based Drugs.

Colorectal cancer (CRC) remains a significant global health challenge, ranking third in incidence and second in mortality among cancers worldwide. This review addresses the complex landscape of CRC, focusing on incidence, mortality trends, preventive strategies, and the evolving therapeutic approaches, particularly highlighting the role of platinum-based drugs like oxaliplatin (OXP). It also underscores the increasing burden of CRC, with factors such as westernized diets, aging populations, and genetic predispositions contributing to its prevalence. Therapeutically, early detection greatly enh

Reactive oxygen species (ROS) in cancer: from mechanism to therapeutic implications.

Reactive oxygen species (ROS) act as critical secondary messengers in various intracellular signaling pathways that regulate cellular proliferation, differentiation, and survival under normal physiological conditions. However, dysregulation of redox signaling-driven by genetic mutations, epigenetic alterations, and posttranscriptional or posttranslational modifications-plays a central role in malignant transformation and cancer progression. Cancer cells typically exhibit elevated basal ROS levels due to increased metabolic activity, mitochondrial dysfunction, and oncogene activation. This mode

Platycodon grandiflorum, as a medicinal and food homologous plant: a comprehensive review of anti-tumor components, mechanisms, modern applications, and preventive healthcare.

Platycodon grandiflorum (Jacq.) A. D C. (P. grandiflorum), as a medicinal and edible plant, is widely distributed in China. In terms of Chinese medical theories, Traditional Chinese Medicine (TCM) believes that the root of P. grandiflorum has the functions of relieving sore throat, eliminating phlegm, and draining pus, and is widely used in lung diseases and respiratory system disorders. Modern pharmacological studies have shown that Platycodon grandiflorum saponin, flavonoids, polysaccharides, and phenolic acids are the main active components of P. grandiflorum, which have significant antitus

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… In recently years, the widely studied nanoparticulate drug delivery systems mainly include solid lipid nanoparticles, liposomes, chitosan nanoparticles, polymeric micelles, hydrogels, etc. ( 112 ). … Diagram illustrating the application of liposomes, nanogels, polymer micelles, and inorganic nanoparticles in enhancing the bioavailability, solubility, and release of compounds like Platycodin D, Luteolin, and Apigenin. …

Targeted Delivery of Drugs and Genes Using Polymer Nanocarriers for Cancer Therapy.

Cancer is one of the primary causes of worldwide human deaths. Most cancer patients receive chemotherapy and radiotherapy, but these treatments are usually only partially efficacious and lead to a variety of serious side effects. Therefore, it is necessary to develop new therapeutic strategies. The emergence of nanotechnology has had a profound impact on general clinical treatment. The application of nanotechnology has facilitated the development of nano-drug delivery systems (NDDSs) that are highly tumor selective and allow for the slow release of active anticancer drugs. In recent years, veh

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… Polymer nanocarriers are generally divided into five types, namely micelles, nanogels, capsules, dendrimers, and mixed NPs with porous cores [ 134 ]. … Linoleic acid-grafted chitosan oligosaccharide micelles for intracellular drug delivery and reverse drug resistance of tumor cells. Int. J. Biol. Macromol. 2011;48:215–222. doi: 10.1016/j.ijbiomac.2010.11.005. 59. …

Mathematical modeling in cancer nanomedicine: a review.

Cancer continues to be among the leading healthcare problems worldwide, and efforts continue not just to find better drugs, but also better drug delivery methods. The need for delivering cytotoxic agents selectively to cancerous cells, for improved safety and efficacy, has triggered the application of nanotechnology in medicine. This effort has provided drug delivery systems that can potentially revolutionize cancer treatment. Nanocarriers, due to their capacity for targeted drug delivery, can shift the balance of cytotoxicity from healthy to cancerous cells. The field of cancer nanomedicine h

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… 2016 ) Iron oxide | SPION b | NanoTherm®/M-ag-Force AG | Glioblastoma | 12–20 | N/A | (Bellizzi and Bucci 2018 ) Mifamurtide | Liposome | Mepact®/Takeda Pharmaceutical | Osteocarcoma | 1–5 × 10 3 | 2.03–2.27 | (Ando et al. 2011 ; Venkatakrishnan et al. 2014 ; Yu and Li 2014 ) Paclitaxel | Polymeric micelles … Phase I and pharmacokinetic study of Genexol-PM, a cremophor-free, polymeric micelle-formulated paclitaxel, in patients with advanced malignancies. Clin. Cancer Res. 2004;10:3708–3716. doi: 10.1158/1078-0432.CCR-03-0655. …

Целевые стратегии лечения рака цвета кожи: изучение использования аптемеров и золотых нанопчастей.

Рак цвета кожи (КЗК) является второй ведущей причиной смертности от рака и является причиной ~10% из всех случаев рака. По оценкам, во всем мире случаи, связанные с КПР 1.9 million и 930,000 смертями в 2022. Несмотря на расширение доступа к обследованиям и лечению в рамках КПР, ожидается, что показатели смертности резко возрастут в районах с низким уровнем ресурсов, что подчеркивает настоятельную необходимость принятия новаторских мер по лечению в рамках КПР. Текущая химиотерапия создает проблемы, такие, как плохая биодоступность, резистентность к многочисленным лекарствам и негативные побочны

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… The organic NPs consist of liposomes, micelles, and polymers, while inorganic NPs are mostly metallic NPs (MNPs) include gold, silver, iron, zinc, and copper NPs [ 8 ]. … In cancer therapy, various nanomedicines that explore the exceptional properties of organic (polymer, micelle, protein, liposome) and inorganic (gold, silver, titanium and calcium) nanomaterials have received United States Food and Drug Agency (US FDA) approval, while some are currently undergoing clinical …