Focus on Ulcerative Colitis: Stable Gastric Pentadecapeptide BPC 157

Abstract

Stable gastric pentadecapeptide BPC 157 (GEPPPGKPADDAGLV, M.W. 1419) may be the new drug stable in human gastric juice, effective both in the upper and lower GI tract, and free of side effects. BPC 157, in addition to an antiulcer effect efficient in therapy of inflammatory bowel disease (IBD) (PL 14736) so far only tested in clinical phase II, has a very safe profile, and exhibited a particular wound healing effect. It also has shown to interact with the NO-system, providing endothelium protection and angiogenic effect, even in severely impaired conditions (i.e., it stimulated expression of early growth response 1 gene responsible for cytokine and growth factor generation and early extracellular matrix (collagen) formation (but also its repressor nerve growth factor 1-A binding protein-2)), important to counteract severe complications of advanced and poorly controlled IBD. Hopefully, the lessons from animal studies, particularly advanced intestinal anastomosis healing, reversed short bowel syndrome and fistula healing indicate BPC 157's high significance in further IBD therapy. Also, this supportive evidence (i.e., no toxic effect, limit test negative, LD1 not achieved, no side effect in trials) may counteract the problems commonly exercised in the use of peptidergic agents, particularly those used on a long-term basis.

Pentadecapeptide BPC157 reduces bleeding and thrombocytopenia after amputation in rats treated with heparin, warfarin, L-NAME and L-arginine

“…BPC 157 has been shown to exert beneficial effects against different pathological conditions [1,2,10-26], it induced gastroprotective, analgesic and anti-inflammatory wound healing effects [1,2,10-17], also effective against experimental colitis [10][11][12][13][14][15][16] and showing a particular interaction with the NO-system [14,15,[18][19][20][21][22][23][24][25][26]. Recently, we demonstrated the effect of BPC 157 against bleeding/thrombocytopenia after amputation, with or without anticoagulant and aspirin administration and abdominal aorta anastomotic site-thrombosis [1,2].…”

“…To counteract the consequences of L-NAME and/or L-arginine administration with the disturbed hemostasis, we administered the stable gastric pentadecapeptide BPC 157 [1,2,[10][11][12][13][14][15][16][17][18][19][20][21][22][23][24][25][26] not only due to its special effect on hemostasis [1,2], but also owing to a particular beneficial combining [1,2,[10][11][12][13][14], wound healing capacity [1,2,[10][11][12][13][14][15][16][17] and particular interaction with NO-system [14,15,[18][19][20][21][22][23][24][25][26]. Previously, BPC 157 as an originally anti-...…”

“…Previously, BPC 157 as an originally anti-ulcer peptide was implemented in inflammatory bowel disease trials [10][11][12][13][14][15], and now multiple sclerosis [16], lethal dose (LD1) could be not achieved [10][11][12][13][14][15][16]. As mentioned, this unusual combining effect in hemostasis was recently evidenced with bleeding/thrombocytopenia after amputation, with or without anticoagulant and aspirin administration, abdominal aorta anastomotic site-thrombosis, both being counteracted [1,2].…”

“…Wound healing capacity in different tissues [1,2,[10][11][12][13][14][15][16][17] (including blood vessels) (i.e., stimulation of the early growth response 1 (egr-1) gene and its co-repressor nerve growth factor 1-A binding protein-2 (naB2) [17] also responsible for cytokine and growth factor generation and thereby, early extracellular matrix (collagen) and blood vessel formation [17]) and endothelium protection [1,2,14,15] were implicated in these counteracting effects.…”

“…Also, interactions with NO-system are shown in different models and various species [12,13,[18][19][20][21][22][23][24][25][26]. As an illustrative analogy for counteraction of the opposite effects of L-NAME and L-arginine in haemorrhage, we should emphasize that the particular effects of BPC 157 on blood pressure [18,20,25] and the anti-arrhythmic effect [18][19][20][21] include antagonization of both L-NAME (hypertension) and L-arginine (hypotension) [25] and counteraction of endothelin serum increase [20].…”