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Related Concept Videos

Cancer02:18

Cancer

Cancers arise due to mutations in genes involved in the regulation of cell division, which leads to unrestricted cell proliferation. Modern science and medicine have made great strides in the understanding and treatment of cancer, including eradicating cancer in some patients. However, there is still no cure for cancer. This is largely due to the fact that cancer is a large group of many diseases.
Cancer Stem Cells and Tumor Maintenance02:40

Cancer Stem Cells and Tumor Maintenance

Early diagnosis and treatment can often cure cancer. However, even with treatment, residual cells called cancer stem cells (CSC) might remain, often causing tumor recurrence. These cancer stem cells possess the potential for self-renewal and multi-lineage differentiation and are often responsible for the therapeutic resistance displayed in most cancers.
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Mouse Models of Cancer Study

Mice have long served as models for studying human biology and pathology because of their phylogenetic and physiological similarity with humans. They are also easy to maintain and breed in the laboratory, and hence, many inbred strains are now available for research. Studies on mice have contributed immeasurably to our understanding of cancer biology.
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Cancer Therapies02:49

Cancer Therapies

Cancer therapies are various modes of treatment, such as surgery, radiation therapy, and chemotherapy that are administered to cancer patients.
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Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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Tumor Immunotherapy01:27

Tumor Immunotherapy

Immunotherapy is a treatment that boosts or manipulates the immune system to fight diseases, including cancer. For instance, by stimulating an immune response through vaccinations against viruses that cause cancers, like hepatitis B virus and human papillomavirus, these diseases can be prevented. Nonetheless, some cancer cells can avoid the immune system due to their rapid mutation and division. The immune response to many cancers involves three phases: elimination, equilibrium, and escape.

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Click on Click: Click-Flavone Glycosides Encapsulated in Click-Functionalised Polymersomes for Glioblastoma Therapy.

Nuno M Saraiva1,2, Ana Alves3,4, Ana Isabel Barbosa5

  • 1LQOF-Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge de Viterbo Ferreira 228, 4050-313 Porto, Portugal.

Pharmaceutics
|June 27, 2025
PubMed
Summary

Three new flavone glycosides were synthesized using click chemistry and showed potential against glioblastoma cells. Encapsulation in targeted polymersomes enhanced their efficacy and delivery for glioblastoma treatment.

Keywords:
click chemistrydrug deliveryflavonesglioblastomapolymersome

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Area of Science:

  • Medicinal Chemistry
  • Materials Science
  • Nanotechnology

Background:

  • Flavonoids possess diverse biological activities, but their therapeutic application is often limited by poor solubility and bioavailability.
  • Glioblastoma multiforme (GBM) is an aggressive brain tumor with limited treatment options.
  • Click chemistry offers a versatile platform for the efficient synthesis of complex molecules and functionalized nanomaterials.

Purpose of the Study:

  • To design and synthesize novel 3,7-dihydroxyflavone glycoside derivatives using click chemistry.
  • To evaluate the cytocompatibility and anti-cancer activity of these derivatives against GBM cell lines.
  • To develop and characterize targeted polymersomes for enhanced delivery and therapeutic efficacy of flavone glycosides in GBM treatment.

Main Methods:

  • Synthesis of 3,7-dihydroxyflavone derivatives via copper-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry.
  • In vitro biological assays using L929 fibroblast and U-251 GBM cell lines.
  • Preparation and characterization of polylactic acid-polyethylene glycol (PEG-PLA) based polymersomes functionalized with a transferrin mimetic peptide (T7-HRPYIAH) via click chemistry.
  • Encapsulation efficiency, particle size, and stability studies of the polymersomes.

Main Results:

  • Three novel flavone glycosides (5a-5c) were successfully synthesized and characterized.
  • Compounds 5b and 5c exhibited reduced metabolic activity in U-251 GBM cells, while showing cytocompatibility with fibroblasts.
  • Polymersomes demonstrated good stability, encapsulation efficiency (39-93%), and size (120-180 nm), with T7-HRPYIAH functionalization enhancing targeting potential.
  • Flavone 5c-loaded polymersomes showed the highest efficacy against U-251 cells, indicating significant potential for GBM therapy.

Conclusions:

  • Novel flavone glycosides synthesized via click chemistry show promising anti-GBM activity.
  • Targeted polymersomes serve as an effective delivery system, improving the therapeutic potential of flavone glycosides for glioblastoma.
  • The developed drug delivery system offers a potential strategy to overcome challenges in GBM treatment, including drug solubility and targeted delivery.