Apigenin induces apoptosis and impairs head and neck carcinomas EGFR/ErbB2 signaling

Laura Masuelli1, Laura Marzocchella, Alessandro Quaranta

  • 1Department of Experimental Medicine, University of Rome, Sapienza, Rome, Italy.

Insights

Apigenin, a plant flavonoid, effectively inhibits head and neck squamous cell carcinoma (HNSCC) growth and survival. It targets EGFR/ErbB2 signaling pathways, showing potential for HNSCC chemoprevention and therapy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Head and neck squamous cell carcinomas (HNSCCs) develop through a multistep process.
  • Epidermal Growth Factor Receptor (EGFR) family members, including EGFR and ErbB2, are critical in HNSCC development and progression.

Purpose of the Study:

  • To investigate the effects of apigenin on HNSCC cell growth, survival, and EGFR/ErbB2 signaling.
  • To evaluate apigenin's potential in HNSCC chemoprevention and therapy.

Main Methods:

  • Utilized sulforhodamine B assay, FACS analysis, and immunofluorescence for apoptosis detection.
  • Performed Western blotting to analyze EGFR, ErbB2, Erk1/2, and Akt phosphorylation.
  • Tested apigenin on tongue (CAL-27, SCC-15) and pharynx (FaDu) HNSCC cell lines.

Main Results:

  • Apigenin demonstrated dose-dependent inhibition of HNSCC cell survival and induction of apoptosis.
  • Apigenin reduced ligand-induced phosphorylation of EGFR and ErbB2.
  • Impaired downstream signaling pathways, including Erk1/2 and Akt, were observed.

Conclusions:

  • Apigenin exhibits significant anti-cancer properties against HNSCC cells.
  • Apigenin's ability to modulate EGFR/ErbB2 signaling suggests its therapeutic potential.
  • Further research into apigenin for HNSCC chemoprevention and treatment is warranted.

Related Concept Videos

Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
The Intrinsic Apoptotic Pathway01:31

The Intrinsic Apoptotic Pathway

Internal cellular stress, such as cellular injury or hypoxia, triggers intrinsic apoptosis. The B-cell lymphoma 2 (Bcl-2) family of proteins are the primary regulators of the intrinsic apoptotic pathway. For example, during DNA damage, checkpoint proteins, such as Ataxia Telangiectasia Mutated (ATM protein) and Checkpoints Factor-2 (Chk2) proteins, are activated. These proteins phosphorylate p53 which further activates pro-apoptotic proteins, such as Bax, Bak, PUMA, and Noxa, and inhibits...
Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists01:28

Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists

Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates these...
The Extrinsic Apoptotic Pathway01:17

The Extrinsic Apoptotic Pathway

The extrinsic apoptotic pathway is initiated when extracellular death-inducing signals, such as specific cytokines, activate the death receptors expressed on the cell surface. The immune cells involved in this pathway are natural killer cells (NK cells) and cytotoxic T-lymphocytes. NK cells are critical in innate immune response, while cytotoxic T-lymphocytes are associated with adaptive immune response. These cells recognize specific receptors expressed on the altered cells and activate...
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.
There are several types of targeted therapies against specific...