Peptides: Protecting Cardiovascular Health

Cardiovascular health is vital for overall well-being, as the heart and blood vessels play a central role in delivering oxygen and nutrients to various organs and tissues throughout the body. Maintaining a healthy cardiovascular system helps reduce the risk of conditions such as heart disease, stroke, and hypertension. While traditional approaches to cardiovascular health focus on lifestyle factors such as diet, exercise, and medication, recent research has highlighted the potential of peptides as a novel approach to protecting and improving cardiovascular health. Peptides, short chains of amino acids, have shown significant promise in promoting heart health, enhancing circulation, and reducing the risk of cardiovascular diseases. This article will explore how peptides contribute to cardiovascular protection, their mechanisms of action, and the key peptides involved.

What Are Peptides and Their Role in Cardiovascular Health?

Peptides are naturally occurring molecules composed of short chains of amino acids, which are the building blocks of proteins. These peptides function as signaling molecules in the body, regulating a variety of physiological processes such as hormone secretion, immune responses, tissue repair, and cell communication. In the context of cardiovascular health, specific peptides play crucial roles in improving heart function, enhancing blood flow, reducing inflammation, and supporting the structural integrity of blood vessels.

Peptides can be synthesized to mimic or amplify the actions of naturally occurring compounds in the body. When it comes to cardiovascular protection, peptides influence key pathways involved in blood pressure regulation, blood vessel function, lipid metabolism, and the prevention of arterial plaque formation. Their targeted actions offer a promising addition to traditionalDrug Enforcement Administration Diversion Control Division Drug & Chemical Evaluation Section Clenbuterol (Street Names: Clen) December 2019 Introduction: Clenbuterol is a potent, long-lasting bronchodilator that is prescribed for human use outside of the United States. It is abused generally by bodybuilders and athletes for its ability to increase lean muscle mass and reduce body fat (i.e., repartitioning effects). However, clenbuterol is also associated with significant adverse cardiovascular and neurological effects. Licit Uses: In the United States, clenbuterol is not approved for human use; it is only approved for use in horses. In 1998, the Food and Drug Administration (FDA) approved the clenbuterol-based Ventipulmin Syrup, manufactured by Boehringer Ingelheim Vetmedica, Inc., as a prescription-only drug for the treatment of airway obstruction in horses (0.8- 3.2 µg/kg twice daily). This product is not intended for human use or for use in food-producing animals. Outside the United States, clenbuterol is available by prescription for the treatment of bronchial asthma in humans. It is available in tablets (0.01 or 0.02 mg per tablet) and liquid preparations. The recommended dosage is 0.02-0.03 mg twice daily. Chemistry and Pharmacology: Clenbuterol is a beta2-adrenergic agonist. Stimulation of the beta2-adrenergic receptors on bronchial smooth muscle produces bronchodilation. However, clenbuterol, like other beta-adrenergic agonists, can produce adverse cardiovascular and neurological effects, such as heart palpitations, muscle tremors, and nervousness. Activation of beta-adrenergic receptors also accounts for clenbuterol’s ability to increase lean muscle mass and reduce body fat, although the downstream mechanisms by which it does so have yet to be clearly defined. After ingestion, clenbuterol is readily absorbed (70-80%) and remains in the body for awhile (25-39 hours). As a result of its long half life, the adverse effects of clenbuterol are often prolonged. Illicit Uses: Clenbuterol is abused for its ability to alter body composition by reducing body fat and increasing skeletal muscle mass. It is typically abused by athletes and bodybuilders at a dose of 60-120 µg per day. It is often used in combination with other performance enhancing drugs, such as anabolic steroids and growth hormone. It is also illicitly administered to livestock for its repartitioning effects. This has resulted in several outbreaks of acute illness in Spain, France, Italy, China, and Portugal. The reported symptoms occur around 0.5-3 hours after the ingestion of clenbuterol containing liver and meat residues. The symptoms, which included increased heart rate, nervousness, headache, muscular tremor, dizziness, nausea, vomiting, fever, and chills, typically resolved within 2 to 6 days. Consequently, the United States and European countries actively monitor urine and tissue samples from livestock for the presence of clenbuterol. There have also been reports of clenbuterol-tainted heroin and cocaine. Although no deaths were attributed to the clenbuterol exposures, the individuals were hospitalized for up to several days due to clenbuterol intoxication. User Population: Clenbuterol is typically abused by athletes. It is thought to be more popular among female athletes as the repartitioning effects are not associated with the typical androgenic side effects (i.e., facial hair, deepening of the voice, and thickening of the skin) of anabolic steroids. Professional athletes in several different sports have tested positive for clenbuterol. Clenbuterol is also marketed and abused for weight-loss purposes. Illicit Distribution: Clenbuterol is readily available on the Internet as tablets, syrup and an injectable formulation. The drug is purportedly obtained by illegal importation from other countries where it is approved for human use. According to the National Forensic Laboratory Information System (NFLIS), 16 exhibits were identified as clenbuterol in 2011 and 2012, 15 exhibits were identified in 2013 and 2014. More recently, 14, 21, and 17 exhibits were identified in 2015, 2016, and 2017, respectively, along with preliminary results of nine exhibits in 2018. The relatively small numbers of drug seizures are likely a result of law enforcement priority due to the non-controlled status of clenbuterol in the United States. Control status: Clenbuterol is currently not controlled under the Controlled Substances Act (CSA). However, clenbuterol is listed by the World Anti-Doping Agency and the International Olympic Committee as a performance enhancing drug. Therefore, athletes are barred from its use. Comments and additional information are welcomed by the Drug and Chemical Evaluation Section, Fax 571-362-4250, Telephone approaches for maintaining heart health.

Key Peptides for Cardiovascular Protection

Several peptides have been identified as particularly effective in protecting cardiovascular health. These peptides work through various mechanisms, such as improving blood flow, reducing oxidative stress, and enhancing heart function:

  1. BPC-157 (Body Protection Compound 157):BPC-157 is a synthetic peptide derived from a protein found in the stomach. Known for its regenerative properties, BPC-157 has been shown to protect and repair tissues throughout the body, including the heart and blood vessels. This peptide promotes angiogenesis, the formation of new blood vessels, which is crucial for improving circulation and ensuring that tissues receive adequate oxygen and nutrients.BPC-157 also has anti-inflammatory effects, helping reduce inflammation in the cardiovascular system, which is a key contributor to atherosclerosis (the buildup of plaque in the arteries). By promoting tissue repair and reducing inflammation, BPC-157 helps support cardiovascular health and prevent conditions such as hypertension and coronary artery disease.
  2. APJ (Apelin Receptor) Peptide:The apelin receptor (APJ) peptide plays a vital role in regulating blood pressure, heart function, and blood vessel health. Apelin, the endogenous ligand for the APJ receptor, has been shown to have vasodilatory effects, meaning it helps relax and widen blood vessels, leading to improved blood flow and reduced blood pressure. This makes apelin a key player in regulating cardiovascular health.Research has shown that the apelin-APJ system plays a role in preventing heart failure and protecting against conditions such as atherosclerosis. By enhancing vasodilation and improving circulation, apelin peptides support heart function, reduce the risk of high blood pressure, and protect against cardiovascular damage.
  3. Angiotensin-(1-7) Peptide:Angiotensin-(1-7) is a peptide that is part of the renin-angiotensin system, which regulates blood pressure and fluid balance. Unlike angiotensin II, which is known to constrict blood vessels and increase blood pressure, angiotensin-(1-7) has vasodilatory effects, helping to lower blood pressure and protect against cardiovascular diseases. This peptide also has anti-inflammatory and antioxidant properties, further supporting heart and vascular health.Studies have shown that angiotensin-(1-7) helps reduce the progression of heart disease by promoting vasodilation, improving endothelial function, and protecting the heart from oxidative stress. By counteracting the harmful effects of angiotensin II, angiotensin-(1-7) peptides contribute to healthier blood vessels and improved cardiovascular function.
  4. Thymosin Beta-4 (TB-500):Thymosin Beta-4 (TB-500) is a peptide that plays a crucial role in tissue repair and regeneration. It has been shown to promote cell migration and angiogenesis, which are essential for repairing damaged tissues, including those in the heart and blood vessels. TB-500 has been used to promote healing after heart injury and improve overall vascular health.In addition to its regenerative properties, TB-500 helps reduce inflammation and oxidative stress in the cardiovascular system, both of which are contributing factors to heart disease and stroke. By promoting tissue repair, reducing inflammation, and enhancing blood flow, TB-500 supports cardiovascular protection and healing.
  5. C-Type Natriuretic Peptide (CNP):Drug Enforcement Administration Diversion Control Division Drug & Chemical Evaluation Section Clenbuterol (Street Names: Clen) December 2019 Introduction: Clenbuterol is a potent, long-lasting bronchodilator that is prescribed for human use outside of the United States. It is abused generally by bodybuilders and athletes for its ability to increase lean muscle mass and reduce body fat (i.e., repartitioning effects). However, clenbuterol is also associated with significant adverse cardiovascular and neurological effects. Licit Uses: In the United States, clenbuterol is not approved for human use; it is only approved for use in horses. In 1998, the Food and Drug Administration (FDA) approved the clenbuterol-based Ventipulmin Syrup, manufactured by Boehringer Ingelheim Vetmedica, Inc., as a prescription-only drug for the treatment of airway obstruction in horses (0.8- 3.2 µg/kg twice daily). This product is not intended for human use or for use in food-producing animals. Outside the United States, clenbuterol is available by prescription for the treatment of bronchial asthma in humans. It is available in tablets (0.01 or 0.02 mg per tablet) and liquid preparations. The recommended dosage is 0.02-0.03 mg twice daily. Chemistry and Pharmacology: Clenbuterol is a beta2-adrenergic agonist. Stimulation of the beta2-adrenergic receptors on bronchial smooth muscle produces bronchodilation. However, clenbuterol, like other beta-adrenergic agonists, can produce adverse cardiovascular and neurological effects, such as heart palpitations, muscle tremors, and nervousness. Activation of beta-adrenergic receptors also accounts for clenbuterol’s ability to increase lean muscle mass and reduce body fat, although the downstream mechanisms by which it does so have yet to be clearly defined. After ingestion, clenbuterol is readily absorbed (70-80%) and remains in the body for awhile (25-39 hours). As a result of its long half life, the adverse effects of clenbuterol are often prolonged. Illicit Uses: Clenbuterol is abused for its ability to alter body composition by reducing body fat and increasing skeletal muscle mass. It is typically abused by athletes and bodybuilders at a dose of 60-120 µg per day. It is often used in combination with other performance enhancing drugs, such as anabolic steroids and growth hormone. It is also illicitly administered to livestock for its repartitioning effects. This has resulted in several outbreaks of acute illness in Spain, France, Italy, China, and Portugal. The reported symptoms occur around 0.5-3 hours after the ingestion of clenbuterol containing liver and meat residues. The symptoms, which included increased heart rate, nervousness, headache, muscular tremor, dizziness, nausea, vomiting, fever, and chills, typically resolved within 2 to 6 days. Consequently, the United States and European countries actively monitor urine and tissue samples from livestock for the presence of clenbuterol. There have also been reports of clenbuterol-tainted heroin and cocaine. Although no deaths were attributed to the clenbuterol exposures, the individuals were hospitalized for up to several days due to clenbuterol intoxication. User Population: Clenbuterol is typically abused by athletes. It is thought to be more popular among female athletes as the repartitioning effects are not associated with the typical androgenic side effects (i.e., facial hair, deepening of the voice, and thickening of the skin) of anabolic steroids. Professional athletes in several different sports have tested positive for clenbuterol. Clenbuterol is also marketed and abused for weight-loss purposes. Illicit Distribution: Clenbuterol is readily available on the Internet as tablets, syrup and an injectable formulation. The drug is purportedly obtained by illegal importation from other countries where it is approved for human use. According to the National Forensic Laboratory Information System (NFLIS), 16 exhibits were identified as clenbuterol in 2011 and 2012, 15 exhibits were identified in 2013 and 2014. More recently, 14, 21, and 17 exhibits were identified in 2015, 2016, and 2017, respectively, along with preliminary results of nine exhibits in 2018. The relatively small numbers of drug seizures are likely a result of law enforcement priority due to the non-controlled status of clenbuterol in the United States. Control status: Clenbuterol is currently not controlled under the Controlled Substances Act (CSA). However, clenbuterol is listed by the World Anti-Doping Agency and the International Olympic Committee as a performance enhancing drug. Therefore, athletes are barred from its use. Comments and additional information are welcomed by the Drug and Chemical Evaluation Section, Fax 571-362-4250, TelephoneC-type natriuretic peptide (CNP) is a peptide that regulates vascular tone and blood pressure by promoting vasodilation. It is produced in the endothelium (the lining of blood vessels) and plays a crucial role in maintaining healthy blood pressure levels. CNP also helps reduce sodium retention, preventing fluid buildup that can contribute to hypertension and heart failure.CNP has been shown to improve endothelial function, which is essential for healthy blood vessel function and reducing the risk of cardiovascular disease. By promoting vasodilation and regulating fluid balance, CNP peptides help protect the cardiovascular system from conditions like high blood pressure, heart failure, and atherosclerosis.

Mechanisms Behind Peptide Action on Cardiovascular Health

Peptides improve cardiovascular health through several key mechanisms, including:

  • Vasodilation and Improved Blood Flow:
    Peptides like apelin and angiotensin-(1-7) promote vasodilation, which relaxes and widens blood vessels, allowing for improved blood flow and reduced blood pressure. This helps prevent conditions like hypertension and atherosclerosis, which can damage the heart and blood vessels.
  • Reducing Inflammation:
    Chronic inflammation plays a major role in the development of cardiovascular diseases such as atherosclerosis and coronary artery disease. Peptides like BPC-157 and TB-500 have anti-inflammatory effects that help reduce the inflammation in blood vessels, improving overall cardiovascular function and reducing the risk of plaque buildup in the arteries.
  • Supporting Angiogenesis:
    Angiogenesis, the formation of new blood vessels, is essential for tissue repair and healthy circulation. Peptides like BPC-157 and TB-500 promote angiogenesis, improving blood flow to tissues and supporting the healing of damaged heart tissue.
  • Enhancing Endothelial Function:
    The endothelium, the inner lining of blood vessels, plays a crucial role in regulating blood flow, blood pressure, and clotting. Peptides like CNP improve endothelial function by promoting vasodilation and maintaining healthy blood vessel function, reducing the risk of cardiovascular events like stroke and heart attack.
  • Reducing Oxidative Stress:
    Oxidative stress occurs when there is an imbalance between free radicals and antioxidants in the body, leading to damage in blood vessels and tissues. Peptides like angiotensin-(1-7) and TB-500 help reduce oxidative stress, protecting the cardiovascular system from damage and promoting long-term heart health.

Benefits of Peptides for Cardiovascular Health

Peptides offer several advantages for protecting and improving cardiovascular health:

  • Lowered Blood Pressure:
    Peptides that promote vasodilation, such as apelin and angiotensin-(1-7), help lower blood pressure by improving blood vessel function and reducing vascular resistance.
  • Improved Blood Vessel Health:
    Peptides that support endothelial function, such as CNP, help maintain healthy blood vessels, preventing the development of conditions like atherosclerosis and coronary artery disease.
  • Enhanced Circulation and Oxygen Delivery:
    Peptides that promote angiogenesis, like BPC-157 and TB-500, help improve circulation, ensuring that tissues receive adequate oxygen and nutrients, which is crucial for overall cardiovascular health.
  • Reduced Risk of Cardiovascular Diseases:
    By reducing inflammation, oxidative stress, and plaque buildup in the arteries, peptides help reduce the risk of heart disease, stroke, and other cardiovascular conditions.

Safety and Considerations

While peptides offer significant benefits for cardiovascular health, they should be used responsibly. It is important to consult with a healthcare provider before using peptides, especially for individuals with existing heart conditions or other chronic health issues. Proper dosing, sourcing from reputable suppliers, and monitoring for potential side effects are essential to ensure safety and effectiveness.

Final Thoughts

Peptides have emerged as a powerful tool for protecting and enhancing cardiovascular health. By promoting vasodilation, reducing inflammation, supporting angiogenesis, and improving endothelial function, peptides offer a comprehensive approach to reducing the risk of cardiovascular diseases and improving overall heart health. As research into peptide therapy continues to grow, these compounds may become an increasingly important part of cardiovascular care, helping individuals maintain a healthy heart and blood vessels throughout their lives.

Peptides: Protecting Cardiovascular Health

References

Bader, M., & Santos, R. A. S. (2012). Renin-angiotensin system: New insights from animal studies. Experimental Physiology, 97(5), 601–605. https://doi.org/10.1113/expphysiol.2011.058818

Lugnier, C., & Heitz, M. P. (2004). Cyclic nucleotide phosphodiesterases (PDE) and peptides involved in cardiovascular regulation. Peptides, 25(10), 1753–1763. https://doi.org/10.1016/j.peptides.2004.06.022

Mavroidis, M., & Karamanos, N. K. (2012). Endothelial function and vascular remodeling in cardiovascular diseases: Role of bioactive peptides. Frontiers in Bioscience (Elite Edition), 4, 2215–2233. https://doi.org/10.2741/e470

Sayed, N., & Abdellatif, M. (2021). Apelin and cardiovascular function: A growing frontier in cardiovascular therapeutics. Journal of the American Heart Association, 10(12), e019446. https://doi.org/10.1161/JAHA.120.019446

Sallam, N., & Laher, I. (2016). Exercise modulates oxidative stress and inflammation in aging and cardiovascular diseases. Oxidative Medicine and Cellular Longevity, 2016, 7239639. https://doi.org/10.1155/2016/7239639