Discover the science behind ACTIVITIS⢠and its groundbreaking approach to anti-aging by targeting PP2A demethylation.
Imagine if your skin had a master switch capable of turning back the clock on agingâa single protein that coordinates your skin's response to environmental damage, regulates hydration, and maintains firmness and elasticity. Recent scientific research has uncovered that such a switch actually exists within our skin cells, and it's called Protein Phosphatase 2A (PP2A). Even more remarkably, researchers have discovered how a novel ingredient derived from grape seeds can influence this switch to provide remarkable anti-aging benefits 1 .
The journey to this discovery began with a challenge: traditional grape seed extract, while beneficial, has limitations in cosmetic formulations due to its dark purple color and limited solubility. Scientists addressed this through an ingenious encapsulation technology, creating what's known as Encapsulated Activated Grape Seed Extract (E-AGSE), commercially referred to as ACTIVITIS⢠1 . This innovation not only improved the ingredient's usability but unexpectedly enhanced its biological activity, opening new frontiers in skincare science that directly targets the molecular mechanisms of skin aging.
Protein Phosphatase 2A (PP2A) is not just another cellular componentâit's considered a master regulatory protein that plays a critical role in cellular response to oxidative stress 1 . Think of PP2A as the conductor of a cellular orchestra, coordinating various responses to environmental threats like UV radiation and pollution. It achieves this through a complex structure consisting of three subunits that work together to regulate essential cellular processes 1 .
When PP2A is functioning optimally, it helps maintain skin youthfulness by:
However, when PP2A activity declines, the consequences become visible on our skin in the form of wrinkles, sagging, and dullness.
The activity of PP2A is precisely controlled through a process called methylationâthe addition of a small chemical group (a methyl group) to the protein. This methylation "activates" PP2A, enabling it to perform its protective functions. The problem arises when an enzyme called PME-1 (Protein Phosphatase Methylesterase-1) removes this crucial methyl group through a process called demethylation, effectively "switching off" PP2A's activity 1 6 .
Research has shown that reactive oxygen species (ROS), which are generated by UV exposure and environmental stressors, can trigger PP2A demethylation 1 . This creates a vicious cycle: environmental stress inactivates PP2A, which then reduces the skin's ability to combat further stress. As we age, this cycle accelerates, leading to more pronounced signs of skin aging.
The researchers faced a significant hurdle: while they had identified Activated Grape Seed Extract (AGSE) as a potent activator of PP2A, its physical properties made it difficult to incorporate into cosmetic products. The extract was a dark purple powder with limited solubility, restricting its use in transparent or light-colored formulations that consumers prefer 1 .
To overcome these challenges, scientists developed an innovative encapsulation system that packages AGSE into microscopic delivery vehicles using:
This combination created what we now know as Encapsulated Activated Grape Seed Extract (E-AGSE), which completely transformed the ingredient's properties while enhancing its biological activity.
Activated Grape Seed Extract
Liposomes + HPCD
Enhanced Bioavailability
The encapsulation process created a novel formulation with reduced color and increased solubility 1 . More importantly, this nanotechnology-based approach offered several scientific advantages:
Improved dissolution in aqueous formulations
Enhanced resistance to degradation
Sustained delivery of active compounds
This final pointâenhanced absorptionâproved critical. The encapsulation allowed the active flavonoids to penetrate more effectively into the skin layers where they could exert their effects on PP2A, meaning lower concentrations could achieve greater efficacy.
To validate the anti-aging benefits of their newly developed E-AGSE, researchers conducted a comprehensive series of experiments combining laboratory models and human clinical trials 1 . The multi-faceted approach included:
Using human dermal fibroblasts and epidermal keratinocytes to measure expression of aging and dermal-epidermal junction markers
Using EpiDerm⢠models to measure protection against cytokine release, DNA damage, apoptosis, and skin barrier compromise
Using human melanocytes and mushroom tyrosinase to measure reduction in melanin production
4-week, 31-subject study on sensitive skin using a 2% E-AGSE Essence
The PP2A demethylation assay specifically measured the extract's ability to prevent PME-1 from removing the crucial methyl group from PP2A. This was done using a radioactive filter binding assay format where PME-1 was incubated with the extract before adding radioactive-labeled methylated PP2A 1 .
The 4-week clinical trial on human subjects demonstrated significant improvements across multiple skin parameters. The results below show the percentage improvement for key anti-aging indicators:
At the molecular level, E-AGSE works primarily by inhibiting the demethylation of PP2A 1 . The encapsulated grape seed extract contains specialized flavonoids that interfere with PME-1, the enzyme responsible for removing the activating methyl group from PP2A. This mechanism ensures that PP2A remains in its active, methylated state where it can perform its protective functions.
The significance of this mechanism is profoundâby maintaining PP2A in its active form, E-AGSE helps preserve the skin's natural defense systems against environmental stressors that would otherwise accelerate aging.
Beyond PP2A protection, E-AGSE delivers multiple verified anti-aging benefits through various pathways:
Significantly increases production of both Collagen I and IIIâthe key structural proteins that maintain skin firmness and prevent sagging 1 .
Enhances production of filaggrin, a crucial protein for proper skin barrier function 1 . This strengthens the skin's defense against environmental aggressors and reduces moisture loss.
Inhibits tyrosinase activity and reduces melanin production, leading to a more even skin tone and reduced appearance of age spots 1 .
The groundbreaking research on ACTIVITIS relied on several crucial laboratory reagents and materials that enabled the encapsulation and testing processes:
Research Reagent | Function in E-AGSE Development | Scientific Role |
---|---|---|
Hydroxypropyl-β-cyclodextrin (HPCD) | Formation of inclusion complexes with AGSE | Enhances solubility and stability of active compounds |
Soybean Lecithin | Primary component of liposomal encapsulation | Creates biodegradable nanoparticle delivery system |
Butylene Glycol | Solvent for AGSE dissolution | Facilitates integration of extract into formulation |
Cholesterol | Component of liposomal membrane | Improves stability and fluidity of delivery vesicles |
Dynamic Light Scattering (DLS) | Particle size analysis | Verifies nanoscale encapsulation success |
Human Dermal Fibroblasts | Cellular model for anti-aging testing | Measures collagen and elastin production |
EpiDerm⢠Model | UVB protection assays | Evaluates DNA protection and anti-inflammatory effects |
The development of Encapsulated Activated Grape Seed Extract represents a significant advancement in cosmetic scienceâone that moves beyond superficial treatments to target the fundamental molecular mechanisms of skin aging. By specifically addressing PP2A demethylation, ACTIVITIS⢠offers a sophisticated approach to maintaining skin health and youthfulness.
The implications of this research extend beyond cosmetic applications. Since PP2A plays crucial roles throughout the body, understanding how to regulate its activity through natural compounds like grape seed flavonoids could inform approaches to other age-related conditions. Future research may explore how these encapsulated extracts could benefit wound healing, inflammatory skin conditions, and even broader applications in healthy aging.
What makes this discovery particularly exciting is that it demonstrates how ancient natural ingredientsâlike grape seeds that would otherwise be agricultural wasteâcan be transformed through cutting-edge science into powerful solutions for modern health and wellness challenges. The marriage of traditional botanical knowledge with advanced nanotechnology has created a skincare ingredient that truly works with your skin's biology to combat the signs of aging at their source.
As research in this field continues to evolve, we can anticipate even more targeted approaches to controlling the molecular switches that govern how our skin ages. For now, ACTIVITIS⢠stands as a remarkable example of how understanding basic cellular mechanisms can lead to transformative innovations in skincare and beyond.