Stable Gastric Pentadecapeptide BPC 157: Novel Therapy in Gastrointestinal Tract

Abstract

Stable gastric pentadecapeptide BPC 157 is an anti-ulcer peptidergic agent, safe in inflammatory bowel disease clinical trials (GEPPPGKPADDAGLV, M.W. 1419, PL 14736) and wound healing, stable in human gastric juice and has no reported toxicity. We focused on BPC 157 as a therapy in peridontitis, esophagus, stomach, duodenum, intestine, liver and pancreas lesions. Particularly, it has a prominent effect on alcohol-lesions (i.e., acute, chronic) and NSAIDs-lesions (interestingly, BPC 157 both prevents and reverses adjuvant arthritis). In rat esophagitis and failed function of both lower esophageal sphincter (LES) and pyloric sphincters (PS), BPC 157 increased pressure in both sphincters till normal and reduced esophagitis. However, in healthy rats, it may decrease (PS) or increase (LES) the pressure in sphincters. It has strong angiogenic potential, it acts protectively on endothelium, prevents and reverses thrombus formation after abdominal aorta anastomosis, affects many central disturbances (i.e., dopamine and 5-HT system), the NO-system (either L-arginine and L-NAME effects), endothelin, acts as a free radical scavenger (counteracting CCl4-, paracetamol-, diclofenac-injuries) and exhibits neuroprotective properties. BPC 157 successfully heals the intestinal anastomosis, gastrocutaneous, duodenocutaneous and colocutaneous fistulas in rats, as well as interacting with the NO-system. Interestingly, the fistula closure was achieved even when the BPC 157 therapy was postponed for one month. In short-bowel syndrome escalating throughout 4 weeks, the constant weight gain above preoperative values started immediately with peroral and parental BPC 157 therapy and the villus height, crypth depth and muscle thickness (inner (circular) muscular layer) additionally increased. Thus, BPC 157 may improve gastrointestinal tract therapy.

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].…”

“…Possibly, the consistent endothelium protection during advanced healing processes in different wounds of various tissues, including blood vessels [1,2,[10][11][12][13][14][15][16][17], associated with the counteraction of the L-NAME-induced disturbances as well as the counteraction of the L-arginineinduced disturbances, obtained with the same BPC 157 dose range [14,15,[18][19][20][21][22][23][24][25][26], should likely compete with the prominent endothelium effect of the heparin-impaired endothelial nitric oxide (NO) synthesis [36] as well as warfarin endothelium damage [37]. Finally, as emphasized, BPC 157 beneficial effects include stimulation of egr-1 gene and its co-repressor gene naB2 [17], also responsible for cytokine and growth factor generation and thereby, early extracellular matrix (collagen) and blood vessel formation [17].…”

“…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.…”