Multifunctionality and Possible Medical Application of the BPC 157 Peptide-Literature and Patent Review

Abstract

BPC 157, known as the "Body Protection Compound", is a pentadecapeptide isolated from human gastric juice that demonstrated its pleiotropic beneficial effects in various preclinical models mimicking medical conditions, such as tissue injury, inflammatory bowel disease, or even CNS disorders. Unlike many other drugs, BPC 157 has a desirable safety profile, since only a few side effects have been reported following its administration. Nevertheless, this compound was temporarily banned by the World Anti-Doping Agency (WADA) in 2022 (it is not currently listed as banned by the WADA). However, it has not been approved for use in standard medicine by the FDA and other global regulatory authorities due to the absence of sufficient and comprehensive clinical studies confirming its health benefits in humans. In this review, we summarize information on the biological activities of BPC 157, with particular reference to its mechanism of action and probable toxicity. This generated the attention of experts, as BPC 157 has been offered for sale on many websites. We also present recent interest in BPC 157 as reflected in a number of patent applications and granted patents.

Keywords: BCP 157-based patents; BPC 157; efficacy and application; molecular pathways; safety.

Figure 1

Proposed targets for BPC 157 biological effects. The BPC 157 pentadecapeptide positively interacts with nitric oxide synthase to increase expression of several antioxidants, including heme oxygenase (HO-1). However, on the other hand, NO generated from NOS, apart from its cytotoxic activity, is used in immune responses as well as being crucial in maintaining activity in developing neurons. It can bind directly to the heme iron of NOS to trigger various chemical and biochemical reactions (e.g., NO deoxygenation associated with scavenging of NO and vasoconstriction, as observed for hemolytic diseases [52], or S-nitrosylation of HbA hemoglobin responsible mainly for lung injury associated with an increased formation of red blood cells [53]). It was found to have a modulatory effect on dopamine level, as it antagonizes catalepsy induced by dopamine antagonist haloperidol [54], while mitigating harmful effects caused by amphetamine [55]. Also, the peptide may stimulate VEGF receptors, while VEGF, particularly VEGF-C, has been reported to induce expression of cyclooxygenase COX-2 and vice versa. In turn, PGF2alpha is known for its increasing activity in raising intracellular calcium levels, and therefore it is an important marker of myocardial stress and heart failure. VEGF is also a well-known agent that causes NO release [56]. Abbreviations: COX (1, 2), cyclooxygenase; HbA, hemoglobin; HO-1, heme oxygenase; NO, nitric oxide; NOS, nitric oxide synthase; NSAIDs, non-steroidal anti-inflammatory drugs; PGF, prostaglandin F2alpha; PGH2, prostaglandin H2; TNF-α, tumor necrosis factor; VEGFR, vascular endothelial growth factor receptor; 5HT2A, serotonin receptor type 2A; ↑, increase; ↓, decrease.

Figure 2

Chemical structures of BPC 157 metabolites as presented by He et al. [61]. Sequences in a colored background represent metabolites.