The effect of BPC157, with or without growth hormone (GH), on proliferating cell nuclear antigen (PCNA) gene expression (dRn) in rat tendon fibroblasts. Asterisks indicate significant effects. From Chang et al., Pentadecapeptide BPC 157 enhances the growth hormone receptor expression in tendon fibroblasts, Molecules (Basel, Switzerland). 2014;19(11):19066-19077.

The effect of BPC157, with or without growth hormone (GH), on proliferating cell nuclear antigen (PCNA) gene expression (dRn) in rat tendon fibroblasts. Asterisks indicate significant effects. From Chang et al., Pentadecapeptide BPC 157 enhances the growth hormone receptor expression in tendon fibroblasts, Molecules (Basel, Switzerland). 2014;19(11):19066-19077.

 

BPC157 is a 15-amino acid peptide compound linked to a number of medical and scientific applications1. It is associated with protective effects against stomach ulcers, as assessed by clinical models of this disorder (i.e. 96% ethanol-induced lesions)2. BPC157 is also associated with beneficial effects on blood pressure. The mechanisms of action of BPC157 are not completely understood, but may be indirectly linked to endothelial (cells in the linings of many organs and systems, including the gut) nitric oxide (NO) production. BPC157 has demonstrated an ability to generate NO comparable to that of similar doses of L-arginine in in vitro studies using samples of rat gastric mucosa. Studies using stomach ulcer models have found that the anti-ulcer effects of the NO precursor, L-arginine, are reversed by N(G)-nitro-L-arginine methylester (L-NAME), which inhibits NO production2. However, L-NAME may only attenuate (slow down or partially reverse) the effects of BPC157 on lesions2.

Another study investigated the effect of BPC157, alone or combined with L-arginine (200 mg/kg), L-NAME (5 mg/kg), or both, on experimental colonic fistulas (severe gastrointestinal lesions that may connect the colon to other surfaces, including skin) in rats. 10 μg/kg doses of this peptide, intraperitoneally or in drinking water, resulted in rapid healing of these lesions, leading to their closure3. Groups receiving BPC157 with L-NAME, L-arginine or both also exhibited fistula healing, despite the detrimental effect of L-NAME administration (without BPC157 or L-arginine) on the same3. BPC157 may also have a role in the healing of other tissue types, including muscle, ligaments and tendons4. Intraperitoneal or cutaneous (i.e. as a cream) administrations of this peptide improved markers of healing (e.g. reduced edema or hematoma and enzymes such as alanine aminotransferase or creatine kinase) in a rat model of muscle injury5.

BPC157 may also affect the central nervous system. A single 10 μg/kg intraperitoneal dose of this peptide resulted in reductions in the synthesis of serotonin in several rat brain regions, including the thalamus, hypothalamus and hippocampus compared to control rats1. However, this also resulted in increased synthesis of the same neurotransmitter in other brain regions, such as the substantia nigra1. A seven-day regimen of subcutaneous BPC157 (10 μg/kg per dose) resulted in significant increases of serotonin synthesis in the substantia nigra, nucleus accumbens and lateral caudate. This indicates that BPC157 may have the potential to affect memory, emotional responses and/or processing and homeostatis1.

BPC157 may also be applied to the treatment of alcohol withdrawal and toxicity. A study used a mouse model of toxicity (i.e. acute intoxication with ethanol) to investigate this possibility. A 10 μg/kg intraperitoneal dose of BPC157 quickly reversed the symptoms of acute intoxication (e.g. anesthesia, hypothermia, absence of self-righting reflex and increased risk of mortality)6. This study also assessed the effect of BPC157 on withdrawal after access to 20% ethanol for thirteen days. The same dose of the peptide also resulted in reduced symptoms of this (e.g. seizure). Rats and mice treated with BPC157 showed decreases in clinical biomarkers following experimentally-induced congestive heart failure7. BPC157 (at the doses as above) has also demonstrated beneficial effects on increased portal pressure and liver damage in animal models of chronic alcohol intake7.

1. Tohyama Y, Sikiric P, Diksic M. Effects of pentadecapeptide BPC157 on regional serotonin synthesis in the rat brain: alpha-methyl-L-tryptophan autoradiographic measurements. Life sciences. 2004;76(3):345-357.

2. Sikiric P, Seiwerth S, Grabarevic Z, et al. The influence of a novel pentadecapeptide, BPC 157, on N(G)-nitro-L-arginine methylester and L-arginine effects on stomach mucosa integrity and blood pressure. European journal of pharmacology. 1997;332(1):23-33.

3. Klicek R, Sever M, Radic B, et al. Pentadecapeptide BPC 157, in clinical trials as a therapy for inflammatory bowel disease (PL14736), is effective in the healing of colocutaneous fistulas in rats: role of the nitric oxide-system. Journal of pharmacological sciences. 2008;108(1):7-17.

4. Chang CH, Tsai WC, Hsu YH, Pang JH. Pentadecapeptide BPC 157 enhances the growth hormone receptor expression in tendon fibroblasts. Molecules (Basel, Switzerland). 2014;19(11):19066-19077.

5. Novinscak T, Brcic L, Staresinic M, et al. Gastric pentadecapeptide BPC 157 as an effective therapy for muscle crush injury in the rat. Surgery today. 2008;38(8):716-725.

6. Boban-Blagaic A, Blagaic V, Romic Z, et al. The influence of gastric pentadecapeptide BPC 157 on acute and chronic ethanol administration in mice. The effect of N(G)-nitro-L-arginine methyl ester and L-arginine. Medical science monitor : international medical journal of experimental and clinical research. 2006;12(1):Br36-45.

7. Lovric-Bencic M, Sikiric P, Hanzevacki JS, et al. Doxorubicine-congestive heart failure-increased big endothelin-1 plasma concentration: reversal by amlodipine, losartan, and gastric pentadecapeptide BPC157 in rat and mouse. Journal of pharmacological sciences. 2004;95(1):19-26.