Complete Guide to Pinealon Peptide
In recent times, peptides have become increasingly popular due to their increased benefits, high stability in the body, and minimal side effects.
While most peptides bind with the receptors to exert their effects in the body, there are a handful of peptides that are capable of binding directly with the DNA to produce the biological reactions.
One of such bioregulator peptides is known as the Pinealon peptide, which possesses neuroprotective properties, and is one of the highly potential candidates to be used in the treatment and management of various neurological disorders (1).
What is Pinealon?
Pinealon is a short synthetic peptide composed of three amino acids Glu-Asp-Arg, also called the EDR peptide (2).
Pinealon is known to impact the central nervous system leading to behavior modification, while also protecting the neurons and various other cell types from oxidative stress.
The main advantage of this peptide is that it has the ability to penetrate through the blood brain barrier, cellular membrane, as well as the nuclear membrane. This is one of the reasons why it is able to interact directly with the DNA molecules.
Pinealon Synthesis and Isolation
Pinealon tripeptide is isolated from another chemical compound called Cortexin (2).
Cortexin is a polypeptide that is synthesized from the bovine brain and was first introduced in 1999. Owing to its low molecular weight, Cortexin also possesses the ability to cross the blood brain barrier and produce stimulatory effects on the neurotransmitters in the brain (3).
Pinealon has since been isolated and studied in elderly people to analyze its effects on the cerebral dysfunctions and ailments (2).
How Does Pinealon Work?
Neuroprotective and Anti-apoptotic Effects
The neuroprotective (protecting neurons and neurotransmitters) and anti-apoptotic (cell death inhibition) effects of the Pinealon peptide are via the MAPK / ERK signaling pathway (2).
ERK signaling cascade plays a vital role in the phosphorylation of the substrates leading to elevated neuron plasticity and increased cellular stress, leading to cellular apoptosis. Similarly, MAPK signaling leads to metabolic disorders and inflammatory reactions.
Upon administration, Pinealon reduces the synthesis of reaction oxygen species (ROS) at the cell granular level. ROS acts as a messenger to MAPK and ERK signaling pathways, and the reduced synthesis thereby leads to reduction in the signaling reactions. This event in turn prevents cellular stress and consequent cell death (2).
Direct Interaction With the Cell Genome
Studies on Pinealon have shown dose-dependent effects of the peptide. At lower doses, the peptide restricts the synthesis and subsequent accumulation of ROS and prevents cell death; while at higher doses, the peptide leads to a modulation of the cell cycle.
This depicts that the peptide exerts antioxidant effects at lower concentrations while possessing the ability to directly interact with the cell genome and alter the cell cycle (4).
What Are the Health Benefits of Pinealon?
The health benefits of the Pinealon peptide include the following:
- Anti-aging effects
- Potential therapeutic agent to treat depression
- Potential therapeutic agent to treat brain disorders including:
- Alzheimer’s disease
- Parkinson’s disease
- Memory enhancement
- Reduces fatigue
- Improves ability to concentrate
- Leads to behavioral modification
Research and Clinical Studies
The main purpose of this study was to analyze the cellular and metabolic aspect of the synthetic tripeptides including Pinealon and a similar peptide called Vesugen.
As part of this study (5), 32 volunteers (18 men and 12 women) between 41 and 83 years of age were enrolled in this study. All volunteers were suffering from poly-morbidity and organic brain syndrome.
Both peptides demonstrated anabolic effects, improving the functioning of the central nervous system and other vital organs, which in turn slowed down the rate of aging. The peptides do not affect the degree of chromatin condensation, which demonstrates that the peptides are safe to use and do not adversely affect at the cellular levels.
Another separate study (6) has demonstrated that the Pinealon peptide acts on the muscle cells where it modulates the levels of irisin. Irisin is central to muscle cell protection and is mainly secreted during exercise. Irisin leads to the burning of excessive fat and is assumed to induce an elongation of telomere (DNA cap) as well.
Hence, by increasing irisin levels, Pinealon boosts protection of DNA telomeres and thereby helps fight the effects of aging.
Role in Prenatal Hyperhomocysteinemia
Hyperhomocysteinemia is characterized by the excessive concentration of homocysteine (HC) amino acid in the blood, indicating extreme vitamin deficiency, which leads to increased risk of dementia (7).
The main goal of this study (8) was to determine the effects of Pinealon on experimentally induced hyperhomocysteinemic pregnant female rats. The female rats were administered with methionine from their second trimester onwards which led to increased HC levels. The rat offspring from the healthy mice and the experimental mice were then used for this study.
Upon analysis, it was determined that the peptide did not reduce or inhibit the development of homocysteine in the offspring, however, there were some beneficial effects seen in the peptide administered rats as the rats demonstrated increased cognitive functions. This suggested that the peptide did not induce metabolism of homocysteine but led to reduced toxic effects of the compound.
Role in Depression
Studies (9) were conducted on the isolated brain cell cultures where the Pinealon peptide was administered in vitro. Upon analysis, it was seen that the peptide stimulated the levels of serotonin expression in the cell cultures.
Through the molecular docking method, it was determined that the peptide regulated the synthesis of 5-typtophan hydroxylase enzyme that is involved in the synthesis of serotonin.
Serotonin is a key hormone that helps stabilize the mood and overall well-being of an individual. This research establishes that the peptide may play a promising role in the treatment of depression.
Studies (10) have shown that Pinealon peptide affects the levels of the caspase 3 enzyme. Caspase 3 enzyme is an initiator of cell apoptosis, or controlled cell death. When Pinealon peptide was administered in the experimental rat models suffering from an ischemic stroke, it modulated the levels of this enzyme, which thereby shut down the pathway of cellular death. This in turn reduced hypoxia effects during the stroke.
Additionally, a separate research study (11) showed that this effect of the peptide on the caspase 3 enzymes may also be beneficial in the treatment of the myocardial infarction.
Lastly, the benefits of suppressing the effects of caspase 3 enzyme were also seen in the skin cells. By reducing cellular apoptosis, the peptide stimulates cell proliferation in both young and aged people, hence leading to an increased regenerative process (12).
Role in Sleep Cycles Regulation and Other Effects on Pineal Gland
As the name suggests, Pinealon peptide acts on the pineal gland of the body which is known to regulate the sleep cycle.
The Pineal gland is located right at the center of the brain and is sensitive to light. Depending on the amount of light it is exposed to, it produces the melatonin hormone. In the dark environment, the pineal gland produces a higher amount of melatonin, which induces a greater amount of sleep.
Sleep cycle disturbances can either be natural due to increasing age or induced based on individual circumstances. Research (13) has shown that when used in the state of insomnia or disturbed sleep cycle, Pinealon resets the pineal gland back to its optimal state and helps improve sleep, elevates the mood, and maintains blood pressure levels.
Besides sleep regulation, pineal gland also regulates cognitive function, bone calcification, and drug metabolism. All these abilities decline due to the shrinkage of the pineal gland with the increasing age. Hence, by preserving the pineal gland, Pinealon peptide demonstrates its geroprotective properties as it aids in maintaining a healthy well being at all ages.
Are There Any Negative Effects of Pinealon?
The listed research studies have shown that the peptide possesses geroprotective properties and may potentially be used to treat ailments in aged people with no major side effects.
While research currently shows that the peptide can be deemed safe for use, it should be noted that there are some common side effects of peptides in general, which may also be applicable in this case:
- Pain, itchiness, and redness at the site of administration
- Flu-like symptoms and headaches
Pinealon is a small synthetic tripeptide, otherwise known as Glu-Asp-Arg or the EDR peptide. Owing to the lighter molecular weight, the peptide can easily cross the blood brain barrier and nuclear cell membrane. As a result, the peptide can easily bind with the DNA cell directly and cause cellular modifications.
Besides cellular modification, Pinealon also possesses neuroprotective, anti-apoptotic, and geroprotective properties.Research has shown extremely promising results on Pinealon administration, especially in treating disorders related to the brain and the nervous system. The peptide is useful in treating cerebral disorders such as Alzheimer’s and Parkinson’s, and helps improve the memory and cell cycle in humans. Since the peptide has been safely used in aged volunteers, it can be seen that there are negligible side effects associated with Pinealon.
Clinical trials are still in progress to fully explore the profile of this peptide and thereby potentially establish its use as a therapeutic agent in treating frequently occurring neuro disorders.
1. Khavinson, V., Linkova, N., Kozhevnikova, E., & Trofimova, S. (2020). EDR Peptide: Possible Mechanism of Gene Expression and Protein Synthesis Regulation Involved in the Pathogenesis of Alzheimer’s Disease. Molecules (Basel, Switzerland), 26(1), 159. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7795577/
2. National Center for Biotechnology Information. PubChem Compound Summary for CID 10273502, Glu-Asp-Arg. https://pubchem.ncbi.nlm.nih.gov/compound/Glu-Asp-Arg.
3. Eroğlu, O., Karlıdağ, T., Kuloğlu, T., Keleş, E., Kaygusuz, İ., & Yalçın, Ş. (2018). The Protective Effect of Cortexin on Cisplatin-Induced Ototoxicity. The journal of international advanced otology, 14(1), 27–33. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6354512/
4. Khavinson V, Ribakova Y, Kulebiakin K, Vladychenskaya E, Kozina L, Arutjunyan A, Boldyrev A. Pinealon increases cell viability by suppression of free radical levels and activating proliferative processes. Rejuvenation Res. 2011 Oct;14(5):535-41. https://pubmed.ncbi.nlm.nih.gov/21978084/
5. Meshchaninov VN, Tkachenko EL, Zharkov SV, Gavrilov IV, Katyreva Iue. EFFECT OF SYNTHETIC PEPTIDES ON AGING OF PATIENTS WITH CHRONIC POLYMORBIDITY AND ORGANIC BRAIN SYNDROME OF THE CENTRAL NERVOUS SYSTEM IN REMISSION. Adv Gerontol. 2015;28(1):62-7. Russian. PMID: 26390612. https://pubmed.ncbi.nlm.nih.gov/26390612/
6. Khavinson VKh, Kuznik BI, Tarnovskaya SI, Lin’kova NS. Short Peptides and Telomere Length Regulator Hormone Irisin. Bull Exp Biol Med. 2016 Jan;160(3):347-9. doi: 10.1007/s10517-016-3167-y. Epub 2016 Jan 8. PMID: 26742748. https://pubmed.ncbi.nlm.nih.gov/26742748/
7. Homocysteine. https://my.clevelandclinic.org/health/articles/21527-homocysteine
8. Arutjunyan, A., Kozina, L., Stvolinskiy, S., Bulygina, Y., Mashkina, A., & Khavinson, V. (2012). Pinealon protects the rat offspring from prenatal hyperhomocysteinemia. International journal of clinical and experimental medicine, 5(2), 179–185. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3342713/
9. Khavinson, V.K., Lin’kova, N.S., Tarnovskaya, S.I. et al. Short Peptides Stimulate Serotonin Expression in Cells of Brain Cortex. Bull Exp Biol Med 157, 77–80 (2014). https://link.springer.com/article/10.1007/s10517-014-2496-y#citeas
10. Mendzheritskiĭ AM, Karantysh GV, Ryzhak GA, Dem’ianenko SV. [Regulation of content of cytokines in blood serum and of caspase-3 activity in brains of old rats in model of sharp hypoxic hypoxia with Cortexin and Pinealon]. Adv Gerontol. 2014;27(1):94-7. Russian. PMID: 25051764. https://pubmed.ncbi.nlm.nih.gov/25051764/
11. Mariela Agosto, Michael Azrin, A Kanwar Singh, Allan S. Jaffe, Bruce T. Liang, T Serum Caspase-3 p17 Fragment Is Elevated in Patients With ST-Segment Elevation Myocardial Infarction, 2011, Journal of the American College of Cardiology, 220-221, V 57, https://www.jacc.org/doi/abs/10.1016/j.jacc.2010.08.628
12. Voicekhovskaya MA, Chalisova NI, Kontsevaya EA, Ryzhak GA. Effect of bioregulatory tripeptides on the culture of skin cells from young and old rats. Bull Exp Biol Med. 2012 Jan;152(3):357-9. doi: 10.1007/s10517-012-1527-9. PMID: 22803085. https://pubmed.ncbi.nlm.nih.gov/22803085/
13. Bashkireva AS, Artamonova VG. [The peptide correction of neurotic disorders among professional truck-drivers]. Adv Gerontol. 2012;25(4):718-28. Russian. PMID: 23734521. https://pubmed.ncbi.nlm.nih.gov/23734521/
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