Bioregulators

WHAT ARE PEPTIDE BIOREGULATORS?

Peptide bioregulators are short chains of amino acids that form proteins’ building blocks. Peptides perform many essential functions in the human body. They interact with different sections of DNA, transferring information encoded in amino acid sequences to control specific genes in a particular tissue.

Peptide bioregulators communicate with their specific section of the DNA, activating genes for cellular regeneration. Peptide bioregulators can function as cellular mediators to regulate gene expression and protein synthesis. These bioregulators are currently leading the research for anti-aging methods.

These proteins serve as the body’s natural signaling molecules similar to hormones. By mimicking the peptides found in the body or replacing them similar to hormone replacement therapy, you can affect disease and promote healthy lives.

BPC-157

BPC-157 composed of 15 amino acids, is a partial sequence of body protection compound (BPC) that is discovered in and isolated from the human gastric juice. Experimentally it has been demonstrated to accelerate the healing of many different wounds, including tendon-to-bone healing and superior healing of damaged ligaments. Also, BPC 157 seems to protect organs and to prevent ulcers of the stomach. This peptide is also shown to decrease pain in damaged areas. Those who suffer from discomfort due to muscle sprains, tears and damage may benefit from treatment with this peptide. It can also help aid skin burns to heal at a faster rate and increase blood flow to damaged tissues.

THE COMMON BENEFITS ARE:

• Tendon healing

• Reduction of pain

• Increase in collagen synthesis

• Quicker recovery times post-injury

• Wound and bone healing

• Decrease in inflammation

• Intestinal repair

THYMULIN

Thymulin is a thymic hormone produced by thymic epithelial cells (TEC) known to induce intra- and extrathymic T cell differentiation. Thymulin was isolated, sequenced, and characterized some 20 years ago and later identified as a thymic hormone involved in immunomodulation.  It has demonstrated that the neuro-endocrine system strongly influences the production and secretion of Thymulin.  Thymulin is an essential hormone for T lymphocyte differentiation and the normalization of T-helper cells to suppressor cells. Given its anti-inflammatory potential, Thymulin downregulates the release of inflammatory mediators, such as cytokines and chemokines, upregulates anti-inflammatory factors, such as interleukin (IL)-10, and exerts molecular control via the regulation of transcription factors and mediators.  The biological activity of Thymulin is dependent on equimolar interaction with zinc (Zn2+).

THE COMMON BENEFITS ARE:

• Immune strengthening
• Immune modulation
• Normalization of T-helper cells to suppressor cells
• Down-regulation of the inflammatory mediators, such as cytokines and chemokines.
• Up-regulation of anti-inflammatory factors, such as interleukin (IL)-10.

NAD (Nicotinamide Adenine Nucleotide)

NAD was first described in 1906 by Harden and Young as a cell component that enhanced alcohol fermentation (Harden and Young, 1906). Then in 1936, Warburg showed that NAD is required for redox reactions (Warburg and Christian, 1936) and solidified the nomenclature: “NAD” refers to the chemical backbone irrespective of charge, “NAD+” and “NADH” refer to the oxidized and reduced forms respectively. In 1963, a breakthrough came with the discovery that NAD+ is a co-substrate for the addition of poly-ADP-ribose to proteins (Chambon et al., 1963).

Nicotinamide adenine nucleotide (NAD+) has emerged as a key regulator of cellular processes that control the body’s response to stress. NAD boosters, small molecules that raise NAD+ levels, are now considered to be highly promising for the treatment of multiple diseases and the potential extension of the human lifespan.

Nicotinamide adenine dinucleotide (NAD) is one of the most important and interesting molecules in the body. It is required for over 500 enzymatic reactions and plays key roles in the regulation of almost all major biological processes (Ansari and Raghava, 2010). Above all, it may allow us to lead healthier and longer lives.

By modulating NAD+ sensing enzymes, it controls hundreds of critical processes from energy metabolism to cell survival, rising and falling depending on food intake, exercise, and the time of day.

NAD+ levels steadily fall as we age, leading to a decline in the function of cells and organs. By raising NAD+, NAD+ boosters can have profound effects on the health and survival of mammals. Increases in NAD+ promote cognitive and sensory function, gluconeogenesis in the liver, lipogenesis in adipose tissue, insulin secretion in the pancreas, and insulin sensitivity in muscle. NAD+ also promotes endothelial cell proliferation and protects against cardio- and cerebrovascular disease. NAD regulates immune function and inflammation and, protects against acute injury in the kidney.

BREMELANOTIDE PT-141 

Bremelanotide PT-141 is used to treat sexual dysfunction in men and women. Unlike other common medications such as Viagra and Cialis, this peptide works in the central nervous system to increase libido and arousal by stimulating certain parts of the brain.

Sexual function and performance is started in the brain. There are several neurochemical mediators which control the process, some increase libido and arousal while some decrease them. Bremelanotide PT-141 causes excitatory behavior in the paraventricular nucleus of the brain by stimulating Melanocortinin receptors. It is particularly helpful in women and has been FDA approved for women, however, it is also very effective in men at producing erections.

MELANOTAN

Melanotan I and Melanotan II are both analogs of the peptide hormone alpha-melanocyte-stimulating hormone (α-MSH) that induces skin tanning. Melanotan I plays a role in stimulating melanogenesis and thus provides a protective mechanism against UV rays since under its actions melanocytes are able to increase production and secretion of the hormone melanin. Melanotan I is an FDA approved drug under the brand name Scenesse. Scenesse is most commonly used to treat patients that have an intolerance to light.

PENTOSAN POLYSULFATE

Pentosan polysulfate is a semi-synthetic polysulfated xylan used for the relief of Osteoarthritis. The mechanism of PPS action in osteoarthritis is multi-factorial, with both stimulation of cartilage matrix synthesis and prevention of cartilage breakdown. There are also systemic effects on blood lipid and fibrinolysis that may help clear the subchondral circulation. In one study, after a series of four to six intra-articular PPS injections into knees of human volunteers, there was a significant increase in the size of the synovial fluid hyaluronan without causing any inflammation or bleeding into the joint cavity.
This a great option for those patients that are suffering from osteoarthritis and are wanting to prevent surgery or intra-articular injections.

SERMORELIN

Sermorelin is a synthetic hormone peptide composed of 29 amino acids. It’s similar in structure to a growth hormone releasing hormone (GHRH). It’s commonly utilized to optimize growth hormone levels in adults, while offering a variable IGF-1 increase. Sermorelin works to improve hormonal balance and enhance energy, burn
fat, increase lean muscle, improve sleep quality, enhance memory, sex drive and more by stimulating the production and release of hormones by the pituitary.

TIRZEPATIDE

Tirzepatide is GIP (glucose-dependent insulinotropic polypeptide) receptor and GLP-1 (glucagon-like peptide-1) receptor agonist, representing a new class of medicines studied for the treatment of obesity. Tirzepatide is a single peptide that triggers the body’s receptors for GIP and GLP-1, two natural incretin hormones.

GIP has shown to decrease food intake and increase energy expenditure, resulting in weight reductions. Combined with a GLP-1 receptor agonist, it has a more significant effect on glucose and body weight effects.

THE COMMON BENEFITS ARE:

• Substantial A1C reductions
• Boosted weight loss
• Improvement in cardiometabolic measures
• Reduced appetite and cravings

IGF-LR3

Insulin-like growth factor is a highly anabolic hormone that is released in the liver as well as in the peripheral tissues in response to the GH so that a new muscle could be built. The main work of IGF-1 is to build new muscle tissues by promoting nitrogen retention and protein synthesis. It differs from the original IGF-1 in that it possesses an arginine instead of a glutamic acid and also has an additional 13 amino acids. As a result, it is approximately three times more potent than IGF-1 and possesses a significantly longer half-life of about 20– 30 hours (comparative to IGF-1’s half-life of about 12–15 hours).

• Enhances muscle mass & strength
• Decreases inflammation & autoimmunity
• Improves gut health
• Boosts collagen production
• Helps balance insulin levels
• Stimulates weight loss

CJC/IPAMORELIN

CJC 1295 is a synthetically produced peptide that can increase your plasma growth hormone levels. Initially, CJC 1295 was developed to treat diseases and medical conditions for patients who had muscle disorders, diseases, and burn victims. CJC 1295 has drawn many individuals like athletes from around the globe for its incredible benefits and minimal side effects to enhance their performance on the field and in the gym. The primary purpose of CJC-1295 is to boost protein synthesis levels and help fuel the growth of muscle tissues in the body. Many benefits will be derived by users who are incorporating CJC-1295 to their regimen; among these are:

• Improve sleep quality
• Increase cognitive function
• Decrease body fat
• Quicker recovery times post-injury
• Increased muscle mass
• Increase in strength

SS-31

Mitochondria play a vital role in cellular metabolism. Because of their widespread effects on cellular functions, mitochondrial dysfunction is implicated in a wide range of diseases. SS-31 has been shown to reverse mitochondrial dysfunction by obliterating damaging inflammatory agents such as free radical oxygen species (ROS).

SS-31 is very unique in its ability to cross the blood-brain barrier and highly concentrate within the inner membrane of the mitochondria (IMM). SS-31 shows promise in the treatment of many neurodegenerative and cognitive disorders such as amyotrophic lateral sclerosis (ALS), Alzheimer’s, Friedreich ataxia, and glaucoma. Anti-aging research is investigating SS-31 for its ability to reverse mitochondrial dysfunction and premature cell death. The mitochondrial dysfunction theory of aging and the free radical theory of aging are intertwined and both would be addressed by the intracellular benefits of SS-31.

• Prevents Alzheimer’s Disease 
• Prevents Glaucoma, Diabetes & Kidney Fibrosis
• Regenerates Skeletal Muscle Weakness
• Helps with Traumatic Brain Injury (TBI)
• Prevents Atherosclerosis & Heart Failure

EPITALON

Epitalon is a tetrapeptide composed of four amino acids (alanine, glutamic acid, aspartic acid, and glycine). It is a synthetic version of Epihalamine, a peptide extract of the pineal gland developed in Russia in the 1980s. In the early 2000s, excitement about Epitalon increased, even more, when scientists found it could activate telomerase, leading to the regrowth of telomeres.

Recent studies indicate that telomere length, which can be affected by various lifestyle factors, can affect the pace of aging and the onset of age-associated diseases. Telomere length shortens with age. The progressive shortening of telomeres leads to senescence, apoptosis, or oncogenic transformation of somatic cells, affecting the health and lifespan of an individual. Shorter telomeres are associated with increased incidence of diseases and poor survival. The rate of telomere shortening can be either increased or decreased by specific lifestyle factors. Better choice of diet and activities has great potential to reduce the rate of telomere shortening or at least prevent excessive telomere attrition, leading to delayed onset of age-associated diseases and increased lifespan.

Epitalon has an important role, especially after 40 years, against aging not only by its action on the brain and pineal gland but also by increasing telomere length through its action as a telomerase activator.

Epitalon can provide you with better sleep and strengthen the immune system. Studies reveal increasing the cognitive capacities of your brain and bio-regulate your whole body through the action of the pineal gland and an increase in melatonin secretion. It has been intensively tested in Russia for more than 25 years and taken even by researchers for its anti-aging and enhancing properties. More people around the world increasingly use it.

• Increase in the life length by prolonging the telomeres in human cells
• Prevention of age-related declines & balance of melatonin production and circadian rhythm 
• Normalized carbohydrate and fat metabolism
• Decreased rates of hypertension and cardiovascular disease
• Better management of metabolism and body weight  & Improved endocrine health
• Reduced incidence of acute respiratory disease & Lower rates of osteoarthritis and osteoporosis 
• Rehabilitation of nervous system activity & Repairs damaged and weakened muscle cells
• Improve physiological functions, and reduce mortality by almost 50% after 15 years
• Works as an antioxidant by reducing Lipid oxidation and ROS and normalizes T cell function

MK 677/IBUTAMOREN

MK-677 is a hormone secretion compound that stimulates the pituitary gland to increase the production of human growth hormone. Ibutamoren is a long-acting, orally-active, selective, and non-peptide agonist of the ghrelin receptor and a growth hormone secretagogue, imitating the growth hormone (GH)-stimulating action of the endogenous hormone ghrelin. Increase IGF-1 Levels in as little as two weeks

• longer REM sleep and shorter sleep latency
• Increase fat-free muscle mass
• Decrease body fat percentage
• Stronger bones
• Improved endurance
• Increase nitrogen levels in the body
• Reversal of nitrogen wasting

MOTS-C

MOTS-c is a peptide encoded as an sORF in the mtDNA that is metabolically and developmentally regulated, which has endocrine-like effects on muscle metabolism, insulin sensitivity, and weight regulation establishes its role as a member of a new class of mitochondrial signals which can be called MDPs (Lee et al., 2013). The MDP humanin similarly acts in a systemic fashion to protect neuronal and vascular systems from disease processes and toxic insults (Cohen, 2014; Lee et al., 2013).  MOT-C is a short open reading frame (sORF) that encodes a signaling peptide inside the mitochondrial DNA (mtDNA). Mitochondrial 12S rRNA encoding a 16-amino-acid peptide named MOTS-c (mitochondrial open reading frame of the 12S rRNA-c) that regulates insulin sensitivity and metabolic homeostasis. Its primary target organ appears to be the skeletal muscle, and its cellular actions inhibit the folate cycle and its tethered de novo purine biosynthesis, leading to AMPK activation.

• Improves glucose regulation & decreases Insulin resistance
• Increases fatty acid oxidation & increases energy
• Promotes metabolic flexibility and homeostasis
• Protect against HFD-induced Obesity

THYMULIN DMAE/GHK-CU/HA CREAM

• Tightens loose skin, improves elasticity, reduces fine lines, and depth of wrinkles
• Reduces photodamage and hyperpigmentation
• Stimulates wound healing and reduces inflammation

DIHEXA

Neurodegenerative diseases are characterized by progressive neuron losses in specific brain regions that impact cognitive, sensory, and motor functioning. These disorders include Alzheimer’s disease (AD), Parkinson’s disease, amyotrophic lateral sclerosis, and Huntington’s disease. The destructive nature of the damage inflicted by these diseases results in a loss of patient dignity and self-worth and negatively impacts family members and friends.

The therapeutic value of this approach lies in its capacity to encourage the formation of new functional synaptic connections among existing neurons, encourage the replacement of damaged and lost neurons from available neural stem cell populations, and facilitate cerebral blood flow and neuroprotection. Such treatment outcomes would benefit patients afflicted with AD and possibly those suffering from other neurodegenerative diseases.

Dihexa (N-hexanoic-Tyr-Ile-(6) amino-hexanoic amide) is a potent cognitive-enhancing molecule that proved to be very stable, capable of inducing spinogenesis/synaptogenesis at picomolar concentrations, slowly cleared from the blood compartment, and sufficiently BBB-permeable.

Dihexa is a first-in-class compound that is orally active, penetrates the blood-brain barrier, and facilitates memory consolidation and retrieval. This angiotensin-based small molecule may be efficacious as a treatment for neurodegenerative diseases. Dihexa has documented procognitive/antidementia activity, is metabolically stable, blood-brain barrier–permeant, and orally active (McCoy et al., 2013).

THE COMMON BENEFITS ARE:

• The brain angiotensin system now includes learning, memory, and motor functions.
• Antidementia properties.
• Cognitive enhancement and increased mental stamina.
• Heighten creative thinking, social intuition, and conversational skills.
• The AngIV/AT4 receptor system coincides with the HGF/c-Met receptor system.
• Improve focus and learning.
• Dihexa binds at HGF and facilitates dimerization and availability at c-Met receptors.
• Activation of the c-Met receptor increases hippocampal synaptic connectivity.

• Reverses neurodegenerative diseases 
• Facilitates formation of new functional synapses
• Hightens creative thinking
• Improves focus and learning

SELANK

Selank is a synthetic regulatory peptide. It was designed and produced at the Institute of Molecular Genetics, Russian Academy of Sciences, in cooperation with the V.V. Zakusov Research Institute of Pharmacology, Russian Academy of Medical Sciences. Selank is a synthetic analog of the endogenous Tuftsin molecule, which was elongated at the C terminus via the addition of three amino acids (Pro-Gly-Pro) to increase its metabolic stability and allow a more extended duration. Selank has pronounced anxiolytic activity. It acts as a stable neuropsychotropic, antidepressant, and antistress drug that relieves aggression and fear reaction in different animal species. Selank has a nootropic action, which positively influences the formation of memory and learning processes. Selank has similar properties to the physiological effects of benzodiazepines. This suggests that there is a similar basis of their mechanism of action that is the allosteric modulation of GABA receptors. They enhance the GABA effect by allosteric modulation, which increases the frequency of opening of channels for chlorine ions. It does not have the unwanted side effects of Benzodiazepines such as withdrawal, dependence, and amnesia. Numerous clinical studies have shown that Selank has strong anti-anxiety and neuroprotective effects in the treatment of generalized anxiety disorders. It alsopositively influences memory and learning process and enhances GABA.

SEMAX

Semax is a heptapeptide and synthetic analogue of a fragment of adrenocorticotropic hormone (ACTH), ACTH (4-10). Semax is a neuroprotective peptide predominantly a nootropic, which has neurogenic/ neurorestorative properties. Semax rapidly elevates the levels and expression of the brain-derived neurotrophic factor (BDNF) and its signaling receptor TrkB in the hippocampus. The exact mechanism of Semax is unclear. During the past two decades, melanocortin peptides and receptors have received considerable attention regarding several CNS functions besides the regulation of energy control, and the multiple roles of the melanocortins represent an opportunity for therapeutic interventions. Molecular tools have allowed the identification of melanocortin receptors signaling in memory, reward, mood, nociception, and erectile function among others. A recent study investigated the effects of intranasally administered a selective MC4 receptor antagonist, and it resulted in marked resilience effects on the development of behavioral symptoms co-morbid with post-traumatic stress disorders. The melanocortin system has a well-established role in the regulation of energy homeostasis but there is growing evidence of its involvement in memory, nociception, mood disorders, and addiction. The involvement of the melanocortins in the regulation of behavioral and emotional states, neuroprotection, inflammation, and exocrine secretion are likely to spur the discovery of selective MC1 and MC5 receptor compounds. Semax is currently being used for numerous conditions like anxiety, positive mood enhancement, memory improvement, nerve regeneration, strokes, ADHD/Learning, Parkinson’s, ALS, and Alzheimer’s.