Abstract: The peptide BPC-157 acts directly on the nervous system, exhibiting both neuroprotective and antidepressant effects. Its broad spectrum of action is applied, among others, in neurotransmission.

Keywords: · BPC-157, · nervous system, · cuprizone, · toxin, · reserpine, · GABA, · serotonergic transmission, · depression

List of abbreviations: BPC - Body Protection Compound; GABA - gamma-aminobutyric acid; MPTP - prodrug of the neurotoxin MPP

Materials and methods: The studies were conducted on laboratory animals, in this case rats.

Effects of BPC-157 on the nervous system in the experimental aspect

Study 1

Material

The study was conducted on rats using the toxin cuprizone, which allows the induction of disease symptoms similar to those occurring in multiple sclerosis or schizophrenia.

Study procedure

The peptide BPC-157 was administered to rats in drinking water or by injection, in combination with the toxin cuprizone.

Results

Oral administration of BPC-157, approximately 10 µg/kg (0.16 µg/ml in water), shows effective action similar to injection administration at doses of 10 ng/kg and 10 µg/kg. It demonstrates such effects in the presence of the toxin cuprizone, which may cause neuronal damage, including demyelination leading to the breakdown of myelin sheaths in the central or peripheral nervous system, without the need to reach the brain.

Conclusions

BPC-157, both in the form of a stable oral salt and in injectable form, exhibits protective effects on brain tissue.

Study 2

Material

The study was conducted on rats using the neurotoxin MPTP and reserpine, which are used to induce a Parkinson’s disease model.

Study procedure

The rats were administered the peptide BPC-157 subcutaneously in the presence of the neurotoxin MPTP and reserpine. Results The effects of the toxins MPTP and reserpine were significantly reduced in the presence of the peptide BPC-157. The range is presented in the graphs below.

Figure 2. The level of the toxins MPTP and reserpine is within the range of 0–140, presented as high in Parkinson’s disease. When the peptide BPC-157 is included in the action of the toxins, their level is reduced and falls within the range of 0–60.

Conclusions

As a result of the above study, BPC-157 demonstrates effects minimizing the symptoms of Parkinson’s disease, a neurodegenerative disorder that significantly impairs proper functioning of the body.

Effects of BPC-157 on the nervous system in the theoretical aspect

Characteristics of nootropic drugs

Nootropic drugs belong to a group of medications that are intended to exhibit therapeutic effects by improving cognitive functions such as memory, concentration, and attention. Medicinal substances belonging to this group may increase motivation or improve motor functions. Both synthetic and natural preparations are classified as nootropics. The list of substances recognized as nootropics is constantly changing, with some preparations being removed and others added. The peptide BPC-157 exhibits nootropic properties as a neuroprotective preparation.

Neuroprotective effects of BPC-157

The studies presented above allow the classification of the peptide BPC-157, both in oral and injectable form, as a neuroprotective preparation. The studies demonstrated the action of BPC-157 as an agent protecting brain tissue and reducing symptoms of nervous system diseases. Moreover, other laboratory experiments allow conclusions to be drawn regarding additional therapeutic effects of the peptide, such as regeneration of nerve cells, protective action in drug withdrawal syndrome, and even in the case of seizures occurring due to excessive intake.

Effect of BPC-157 on the GABA system

Characteristics of GABA

GABA, or γ-aminobutyric acid, is one of the main neurotransmitters. Due to its chemical structure, it is classified as an amino acid. Proper functioning of GABA is associated with the activity of two main receptors: ionotropic GABA-A and metabotropic GABA-B. In the human body, the neurotransmitter GABA is responsible for proper nervous system function by inhibiting excessive excitation. The conclusion from such a broad spectrum of action is that both deficiency and excess lead to nervous system disorders, which is why maintaining its proper level is so important. Other functions of the neurotransmitter GABA include proper functioning during the body’s resting phase during sleep, helping maintain concentration while preventing distraction. It allows the body to calm down, thereby reducing stress, and stimulates the production and secretion of growth hormone from the pituitary gland. BPC-157 and its effect on GABA The peptide BPC-157 has a direct effect on the regeneration of the GABA system while simultaneously accelerating the return to homeostasis after addiction or abuse of drugs and stimulants that directly damage the GABA system. Using benzodiazepines, specifically diazepam, as an example, it was observed that simultaneous administration with the peptide BPC-157 resulted in, among others, reduced development of drug tolerance, improved drug efficacy, and maintenance of GABA receptor complex homeostasis. The GABA receptor is presented in the diagram.

Serotonergic transmission in the experimental aspect

Material

The study was conducted on rats with regard to involvement in the serotonergic system, in relation to the possible brain-gut axis, due to the action of BPC-157 in both areas.

Study procedure

The peptide BPC-157 was administered to rats by subcutaneous injection at a dose of 10 µg/kg while serotonin was simultaneously administered. The study was conducted for 40 minutes daily over a period of one week. Results Results were observed in several brain regions, including the substantia nigra of the midbrain and the medial anterior olfactory nucleus, with simultaneous reduction in the hypothalamus, ventral and dorsal hippocampus, and dorsal thalamus. Serotonin synthesis was increased, and the increase in serotonin synthesis in the substantia nigra persisted in both the reticular and compact parts during week-long administration. After a single administration, the reduction in serotonin synthesis was not maintained.

Conclusions

BPC-157 exhibits antidepressant effects resulting from interaction with the serotonin system. Neuroprotective and antidepressant effects of BPC-157. The influence of BPC-157 on brain function.

Serotonergic transmission in the theoretical aspect

The concept of serotonin syndrome

Serotonin syndrome is a condition directly threatening proper functioning and life. It is an adverse effect of pharmacotherapy characterized by symptoms such as changes in mental state, autonomic disturbances, and neuromuscular disorders. The occurrence of this syndrome is most commonly associated with pain therapy that may intensify serotonergic transmission.

Serotonergic transmission with BPC-157

According to the above studies, it can be observed that peripherally administered BPC-157 has the ability to cross the blood-brain barrier. The peptide administered together with serotonin allows bypassing the stage of serotonin syndrome, which directly affects the nervous system and depressive states.

Depression and BPC-157 in the experimental aspect

Material

The study was conducted on rats during the forced swim test (Porsolt test).

Study procedure

The rat was placed in a cylindrical container filled with water for a period of 15 minutes. After 24 hours from the first trial, a second trial was performed consisting of placing the animal in the same container, but for 5 minutes. During this time, observation was made of how long the animal remained immobile. Animal immobility corresponds to depressive states in humans. Simultaneously during the forced swim test, the rat was administered BPC-157 intraperitoneally. Neuroprotective and antidepressant effects of BPC-157. The influence of BPC-157 on brain function.

Results

At both doses of 10 ng/kg and 10 µg/kg, BPC-157 acted statistically to a similar extent as the active controls of both groups, with imipramine (15 mg and 30 mg) and nialamide (20 mg and 40 mg), performing better than the control group. The action of BPC-157 together with different doses of imipramine and nialamide.

Conclusions

BPC-157 exhibits protective effects in the case of stress and demonstrates antidepressant effects in relation to the conducted studies.

Depression and BPC-157 in the theoretical aspect

Pathomechanism of depressive disorders

Depressive disorders belong to a group of heterogeneous diseases caused by biological, psychological, genetic, or social factors. A number of neurotransmitter and metabolic pathways contribute to the nervous system disorder known as depression. Theories of depressive disorders include the monoaminergic, neurotrophic, glucocorticosteroid, glutamatergic, inflammatory, and cytokine theories.

Antidepressant effects of BPC-157

Taking into account the above studies, it can be concluded that the peptide BPC-157 acts in a manner similar to antidepressant drugs, helping maintain proper body functioning during low mood, emotional disturbances, or moments of hesitation.

References

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  7. Clic A, Zemba M, Belenowic I, Pentadecapeptide BPC 157 counteracts L-NAME-induced catalepsy. BPC 157, L-NAME, L-arginine, NO-relation, in the suited rat acute and chronic models resembling ‘positive-like’ symptoms of schizophrenia. Behavioural Brain Research 2016; 423: 56-132. DOI: 10.1016/j.bbr.2020.112919.
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