Cortagen 20mg

▎Cortagen Structure

▎Cortagen Research

What is the research background of Cortagen?

As a synthetic tetrapeptide, Cortagen originates from scientific research explorations in multiple fields. In the field of neuroscience, due to the intractability of neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease, researchers have been searching for substances that can protect neurons and promote nerve repair. Cortagen was born in this exploration and is expected to assist in neuron repair and slow down the disease progression. In immunological research, given that immune disorders lead to many diseases, scientists have been exploring small molecules for immune regulation. 

Cortagen can regulate the immune system, stimulate the expression of interleukin-2, and reduce autoimmune responses, bringing new ideas for the treatment of immune diseases. With the high incidence of cardiovascular and cerebrovascular diseases, the effects of Cortagen on relevant indicators and cardiac gene expression provide a new direction for the prevention and treatment of these diseases. Against the backdrop of the rising interest in anti-aging research due to the increasing aging of the population, Cortagen can regulate genes and make DNA closer to a younger state, contributing to the revelation of the aging mechanism and the achievement of healthy aging. In addition, since tissue repair and regeneration are a key focus in medicine, the characteristics of Cortagen in promoting cell regeneration and stimulating nerve regeneration have opened up a new path for research in this field.

What is the mechanism of action of Cortagen?

1. Effects on Heterochromatin

Inducing the Depolymerization of Total Heterochromatin: The peptide bioregulator Cortagen can induce the unwinding and deheterochromatization (depolymerization) of total heterochromatin. Through the use of molecular cytogenetic methods, such as differential scanning calorimetry, analyzing the activity of ribosomal genes in the satellite stalks of acrocentric chromosome NORs, studying the polymorphism of centromeric C-heterochromatin in the peripheral structure, and observing the variability of facultative heterochromatin (FH) in the lymphocytes cultured from individuals aged 80 and above, it has been found that Cortagen has a significant regulatory effect on heterochromatin^[1].

Activating Ribosomal Gene Synthesis: Due to the deheterochromatin activation of the satellite stalks of proximal chromosomes, Cortagen activates the synthesis process of ribosomal genes. At the same time, it does not induce the deheterochromatization of the constitutive heterochromatin around the centromere, and releases the inhibited genes due to the condensation of the autosomal regions that form FH ^[1].

2. Effects on Neurons

Regulating the Electrical Activity of Neurons: The drug cortexine and cortexine peptides have been proven to regulate the electrical activity of neurons in the same way, that is, moderately changing the resting potential, action potential, and impulse frequency, which is interpreted as an activation effect. Glycine can also activate neuron activity, but to a lesser extent. The tetrapeptide cortagen can also hyperpolarize neurons by 2-3 mV and reduce their spontaneous activity at a concentration of 0.1-100 μM, indicating its activation (neuroprotective) effect. At a concentration of 1000 μM, Cortagen moderately depolarizes neurons (2-4 mV), and an increase in impulse activity is recorded. At a concentration of 10 mM, it significantly and reversibly depolarizes neurons, increases the frequency, and inhibits the generation of action potentials ^[1].

Affecting Ion Currents: Cortagen can also increase the amplitude of the slow outward current by 3-5% at a concentration of 0.1 μM. After administering Cortagen, no increase in the amplitude (activation) of the inward sodium and calcium channels was observed. After administering Cortagen at a concentration of 100 μM and above, the amplitude of these currents began to show a dose-dependent and reversible inhibition. After the peptide concentration reaches 10 mM, the inhibition can reach 80-90%. Among them, the inhibition of sodium channels is more intense than that of calcium channels ^[1].

3. Effects on Cardiac Gene Expression

Changing the Cardiac Transcriptome: By analyzing 15,247 transcripts in the hearts of 6-month-old female CBA mice that received continuous injections of Cortagen for 5 days, it was found that compared with the control group, the cDNA microarray hybridization of the heart samples in the experimental group showed that the expression of 234 clones (accounting for 1.53% of the total number of clones) had significantly changed, and these clones matched 110 known genes belonging to various functional categories. The maximum up-regulation and down-regulation were +5.42 and -2.86 respectively^[2].

Comparison with Other Peptides and Hormones: Comparing the changes in the cardiac expression profiles caused by synthetic peptides (Cortagen, Vilon, Epitalon) and the pineal peptide hormone melatonin reveals the common and specific effects of Cortagen on cardiac gene expression^[2].

4. Roles in Other Aspects

Effects on Damaged Peripheral Nerve Tissues: In humans, Cortagen has an obvious therapeutic effect on the structural and functional recovery of damaged peripheral nerve tissues. It is a synthetic peptide obtained through directional synthesis based on the amino acid analysis of the natural cerebral cortex peptide preparation Cortexin ^[1].

Role in Hip Osteoarthritis: Some studies have shown that intra-articular corticosteroid injections have been used for decades. As a peptide bioregulator with a similar effect, Cortagen plays a role to a certain extent by regulating the inflammatory response and other pathways^[3].

What are the applications of Cortagen?

1. Anti-aging

Delaying the Aging Process: As an anti-aging peptide, Cortagen can regulate gene expression, restore DNA to a younger state, thereby reducing aging and reactivating specific genes. The aging process is usually accompanied by changes in gene expression. Cortagen can delay the aging process by regulating the expression of these genes. For example, it can achieve anti-aging effects by activating telomerase activity, reducing oxidative stress damage, or regulating epigenetic modifications.

Regulating Cellular Metabolism: It can normalize the metabolic disorders in the brain caused by chronic ischemia, which has potential benefits for maintaining brain health and function^[2]. Metabolic disorders in the brain are related to various neurodegenerative diseases and aging-related diseases. Cortagen can restore normal metabolic function by regulating metabolic pathways in the brain, thereby protecting brain health.

1. Neuroprotection and Brain Repair

Promoting Neuron Function: Cortagen can stimulate the operation and activity of neurons, playing a positive role in the recovery and maintenance of neuron function. Studies have shown that it can promote the growth and development of neurons by interacting with nerve growth factors^[4]. This mechanism of action may involve activating specific signaling pathways, thereby enhancing the metabolic activity and synaptic transmission efficiency of neurons.

Assisting in Nerve Tissue Recovery: Cortagen has shown potential in the structural and functional recovery of peripheral nerve tissues, which is helpful for the repair of nerve injuries. By regulating the composition and structure of the extracellular matrix, it provides a suitable environment for the growth of nerve cells. The extracellular matrix plays an important role in maintaining cell homeostasis and tissue development. Cortagen can promote the regeneration and repair of nerve tissues by influencing the components and functions of the extracellular matrix.

Research on Neurodegenerative Diseases: Cortagen is one of the hot topics in the research of neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. It helps to slow down or prevent the progression of these diseases. Neurodegenerative diseases are usually related to the death and dysfunction of neurons. Cortagen can reduce the damage and death of neurons through its neuroprotective effect, thereby delaying the development of the diseases. For example, it can play a role by regulating the levels of neurotransmitters, enhancing the antioxidant defense system, or promoting the proliferation and differentiation of neural stem cells.

2. Cognitive Enhancement

Improving Memory and Attention: Studies have shown that Cortagen can improve memory, attention, and intellectual ability, enhancing cognitive function. Its mechanism of action may involve regulating the neurotransmitter system in the brain, such as increasing the release of neurotransmitters like dopamine and norepinephrine ^[5]. These neurotransmitters play a key role in cognitive processes. For example, dopamine is related to the reward system and learning and memory, and norepinephrine is related to attention and alertness.

Reducing Anxious Behaviors: Cortagen has an anti-anxiety effect and can help reduce anxiety-related behaviors, thereby improving the emotional state. In mouse experiments, Cortagen has shown a regulatory effect on anxiety-related behaviors ^[4]. It can relieve anxiety symptoms by influencing the neural circuits in the brain, such as regulating the activities of regions like the amygdala and hippocampus.

3. Immunomodulation

Stimulating the Expression of Interleukin-2: Cortagen can stimulate the expression of interleukin-2, thereby regulating immune function and enhancing the body's immune response. Interleukin-2 is an important immunomodulatory factor that can promote the proliferation and activation of T cells and enhance the body's cellular immune function ^[1]. Cortagen can induce the expression of interleukin-2 by activating specific signaling pathways, thereby improving the body's immunity.

Reducing Autoimmune Responses: It helps regulate immune function by reducing autoimmune responses and can have a certain regulatory effect on autoimmune diseases. Autoimmune diseases are caused by the body's immune system mistakenly attacking its own tissues. Cortagen can reduce the occurrence of autoimmune responses by regulating the activity of the immune system, thereby playing a certain therapeutic role in autoimmune diseases.

4. Tissue Repair and Regeneration

Accelerating Injury Recovery: Cortagen can accelerate the recovery after injury, including tissue injury and post-surgical recovery, by promoting cell regeneration. The extracellular matrix has unique advantages in tissue regeneration and repair. Cortagen can promote the proliferation and differentiation of cells by influencing the components and functions of the extracellular matrix, accelerating tissue repair and regeneration.

Promoting Nerve Regeneration: Cortagen can stimulate nerve regeneration and has a positive impact on the repair and regeneration of peripheral nerve tissues. Nerve regeneration is a complex process involving the proliferation, differentiation, and migration of neural stem cells, as well as the growth of axons and the formation of synapses. Cortagen can promote nerve regeneration by regulating the key signaling pathways in these processes.

5. Cardiovascular and Cerebrovascular Health

Affecting Cardiovascular and Cerebrovascular Indicators: Some studies have found that Cortagen can affect certain indicators of the cardiovascular and cerebrovascular systems, although this area still requires further research. For example, it can affect indicators such as blood pressure, heart rate, and vascular elasticity (Anisimov S, 2004). Its mechanism of action may involve regulating neurotransmitters, hormones, and signaling pathways in the cardiovascular and cerebrovascular systems.

Regulating Cardiac Gene Expression: Cortagen can significantly up-regulate the expression of some genes in the heart, such as Pass1, Hsc70, Bmp2, Wnt4, Eps15, and Eps15-rs. These genes are related to the survival of cardiac cells, the formation of cardiac tissues, and the control of programmed cell death^[2]. By regulating the expression of cardiac genes, Cortagen can have a positive impact on the structure and function of the heart, thus helping to maintain cardiovascular health.

6. Mood Regulation

Improving the Emotional State: Cortagen can have an effect on regulating mood, improving the emotional state, and reducing symptoms of depression and anxiety. Its mechanism of action may be related to regulating the neurotransmitter system and neural circuits in the brain^[4]. For example, it can improve the emotional state by increasing the levels of neurotransmitters such as serotonin and dopamine; or it can reduce symptoms of anxiety and depression by regulating the activities of regions like the amygdala and hippocampus.

Adjuvant Treatment of Mood Disorders: It has potential application value in the treatment of emotional/depressive symptoms and can be used as an adjuvant treatment. Mood disorders are a common mental illness, and the current treatment methods mainly include drug treatment, psychotherapy, and physical therapy. Cortagen can be used as an adjuvant treatment, combined with traditional treatment methods to improve the treatment effect.

In conclusion, as a synthetic tetrapeptide, Cortagen has a non-negligible value in the biomedical field. In terms of anti-aging, it helps DNA return to a younger state by regulating gene expression, effectively delaying the aging process, and can also improve the metabolic disorders in the brain caused by chronic ischemia. In the field of neuroscience, it can promote neuron activity, which is of great significance for nerve injury repair and research on neurodegenerative diseases. At the same time, it can enhance cognition and relieve anxiety. In terms of immunity, it can stimulate the expression of interleukin-2 and regulate immune function. In the cardiovascular and cerebrovascular aspects, although further research is needed, it can already affect relevant indicators and regulate cardiac genes. Cortagen has opened up a new direction for human health and is expected to play a key role in the adjuvant treatment of diseases and the optimization of body functions.

About The Author

The above-mentioned materials are all researched, edited and compiled by Cocer Peptides.

Scientific Journal Author

Dr. Joseph I. Friedman is an accomplished researcher and medical professional affiliated with prestigious institutions such as the Mt. Sinai System of Hospitals, the Icahn School of Medicine at Mount Sinai, and the Pilgrim Psychiatric Center. His research spans across various fields including Psychiatry, Neurosciences & Neurology, Pharmacology & Pharmacy, Cardiovascular System & Cardiology, and General & Internal Medicine. He has made significant contributions to the understanding and treatment of psychiatric illnesses, cardiovascular diseases, and cognitive impairments, with numerous publications in peer-reviewed journals. His work has been instrumental in advancing the knowledge and treatment approaches in these areas. Dr. Joseph I. Friedman is listed in the reference of citation [5].

▎Relevant Citations

[1]    Lezhava T, Monaselidze J, Jokhadze T, et al. Epigenetic Regulation of “Aged” Heterochromatin by Peptide Bioregulator Cortagen[J]. International Journal of Peptide Research and Therapeutics, 2015,21(1):157-163.DOI:10.1007/s10989-014-9443-7.

[2]    Anisimov S, Khavinson V, Anisimov V. Elucidation of the effect of brain cortex tetrapeptide Cortagen on gene expression in mouse heart by microarray[J]. Neuro Endocrinology Letters, 2004,25:87-93. https://pubmed.ncbi.nlm.nih.gov/15159690/.

[3]    Choueiri M, Chevalier X, Eymard F. Mechanism of Action of Corticosteroids, 2021[C]. https://www.semanticscholar.org/paper/MechanismofActionofCorticosteroidsChoueiriChevalier/5042f7d966e01faaa7ab895b0f962ea7af829258.

[4]    Adriani W, Granstrem O K, Romano E, et al. Modulatory Effects of Cortexin and Cortagen on Locomotor Activity and Anxiety-Related Behavior in Mice[J]. The Open Neuropsychopharmacology Journal, 2009,2:22-29. DOI:10.2174/1876523800902010022.

[5]    Friedman J I, Stewart D G, Gorman J M. Potential Noradrenergic Targets for Cognitive Enhancement in Schizophrenia[J]. Cns Spectrums, 2004,9(5):350-356.DOI:DOI: 10.1017/S1092852900009330.

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