Related Experiment Video

Updated: Aug 24, 2025

The Three-Dimensional Human Skin Reconstruct Model: a Tool to Study Normal Skin and Melanoma Progression
11:02

The Three-Dimensional Human Skin Reconstruct Model: a Tool to Study Normal Skin and Melanoma Progression

Published on: August 3, 2011

49.9K

Flavonoids from Ericameria nauseosa inhibiting PI3K/AKT pathway in human melanoma cells

Tanja Hell1, Maciej Dobrzyński2, Fabian Gröflin1

  • 1Division of Pharmaceutical Biology, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland.

Biomedicine & Pharmacotherapy = Biomedecine & Pharmacotherapie
|October 20, 2022
PubMed

Insights

Ericameria nauseosa extract inhibited oncogenic AKT activity in melanoma cells. Flavonoids, particularly flavones, showed the most potent activity, with compound 9 being the most effective.

Area of Science:

  • Natural Products Chemistry
  • Cancer Biology
  • Pharmacognosy

Background:

  • Metastatic melanoma frequently exhibits mutations in PI3K/AKT and MAPK/ERK pathways.
  • Targeting these pathways is crucial for melanoma treatment.

Purpose of the Study:

  • To identify natural compounds that inhibit oncogenic AKT activity in melanoma.
  • To isolate and characterize bioactive compounds from Ericameria nauseosa.

Main Methods:

  • Screening of over 2500 plant extracts for AKT inhibitory activity.
  • HPLC-based activity profiling for fractionation and isolation of active compounds.
  • Chemical characterization of isolated compounds, including ECD for absolute configuration.

Main Results:

  • Dichloromethane extract of Ericameria nauseosa significantly inhibited AKT activity.
  • Eleven flavones, four flavanones, two diterpenes, and a seco-caryophyllene were isolated.
  • Flavonoids, especially flavones, demonstrated significant AKT inhibitory activity.
  • Compound 9 (a flavone) exhibited the most potent activity with an IC50 of 14.7 ± 1.4 µM.
  • Two new diterpenes were identified, with compound 17 being the first clerodane type diterpene described in Ericameria.

Conclusions:

  • Ericameria nauseosa is a source of novel bioactive flavonoids with potential for melanoma therapy.
  • Flavones from this extract show promising AKT inhibitory activity, warranting further investigation.
  • The identified new diterpenes expand the chemical diversity known for the Ericameria genus.
Keywords:
Ericameria nauseosaFlavonoidsHPLC-based activity profilingMAPK/ERKMelanomaPI3K/AKT

More Related Videos

Author Spotlight: Exploring Salidroside's Molecular Mechanisms in Breast Cancer Treatment11:13

Author Spotlight: Exploring Salidroside's Molecular Mechanisms in Breast Cancer Treatment

Published on: June 9, 2023

1.7K
Y-27632 Enriches the Yield of Human Melanocytes from Adult Skin Tissues08:06

Y-27632 Enriches the Yield of Human Melanocytes from Adult Skin Tissues

Published on: July 8, 2020

5.6K

Related Concept Videos

PI3K/mTOR/AKT Signaling Pathway01:22

PI3K/mTOR/AKT Signaling Pathway

The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a...
3.8K
Cancer Prevention02:59

Cancer Prevention

Several factors can increase the risk of cancer in an individual. About 50% of cancer cases can be prevented by adopting a healthy lifestyle, regular exercise, eating healthy, and following a modest cancer prevention diet. Epidemiological studies have consistently shown that populations with vegetable and fruit-rich diets have reduced the incidence of cancer. On the other hand, populations who have a diet rich in animal fat, red meat, junk food, or high calories are predisposed to cancer.
Some...
6.3K
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...
4.9K
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...
6.7K
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...
6.6K
mTOR Signaling and Cancer Progression03:03

mTOR Signaling and Cancer Progression

The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
3.9K