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Full name: Body Protection Compound-157, a pentadecapeptide (15-amino acid peptide) originally isolated from human gastric juice.
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Amino acid sequence: Gly-Glu-Pro-Pro-Pro-Gly-Lys-Pro-Ala-Asp-Asp-Ala-Gly-Leu-Val, molecular weight ≈ 1419.55 Da.
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Compared with many other peptides, BPC-157 is relatively stable in water and gastric juice, which makes oral or gastric administration more feasible.
Mechanisms of Action
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Angiogenesis / Circulatory Recovery
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Upregulates VEGFR-2 expression, promoting new blood vessel formation.
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Activates the Src–Caveolin-1–eNOS pathway, leading to nitric oxide (NO) release, vasodilation, and improved vascular function.
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Anti-inflammatory & Antioxidant
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Downregulates pro-inflammatory cytokines such as IL-6 and TNF-α.
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Reduces reactive oxygen species (ROS) production, protecting cells from oxidative stress.
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Tissue Repair
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Promotes structural and functional recovery in tendon, ligament, and muscle injury models.
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Provides neuroprotection in central nervous system injury models (spinal cord compression, cerebral ischemia-reperfusion), reducing neuronal death and improving motor/sensory recovery.
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Regulation of Vascular Tone
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Ex vivo vascular studies show BPC-157 induces vasorelaxation, dependent on intact endothelium and NO pathways.
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Animal & In Vitro Comparative Data
| Experiment Type | Model / Intervention | Dose / Administration | Control | Key Results | Comparison Data |
|---|---|---|---|---|---|
| Vasodilation (rat aorta, ex vivo) | Phenylephrine-precontracted aortic rings | BPC-157 up to 100 μg/ml | No BPC-157 | Vasorelaxation ~ 37.6 ± 5.7% | Reduced to 10.0 ± 5.1% / 12.3 ± 2.3% with NOS inhibitor (L-NAME) or NO scavenger (Hb) |
| Endothelial cell assay (HUVEC) | HUVEC culture | 1 μg/ml | Untreated control | ↑ NO production (1.35-fold); ↑ cell migration | Migration abolished with Hb |
| Ischemic limb model (rat) | Hindlimb ischemia | 10 μg/kg/day (i.p.) | No treatment | Faster blood flow recovery, ↑ angiogenesis | Treatment > Control |
| Spinal cord compression (rat) | Sacrococcygeal spinal cord compression | Single i.p. injection 10 min post-injury | Untreated group | Significant neurological and structural recovery | Control group remained paraplegic |
| Hepatotoxicity model (CCl₄ / alcohol) | Chemically induced liver injury | 1 µg or 10 ng/kg (i.p. / oral) | Untreated | ↓ AST/ALT, reduced necrosis | Control group showed severe liver injury |
| Toxicity studies | Mice, rabbits, dogs | Multiple doses / routes | Placebo controls | No significant toxicity, no LD₅₀ observed | Well tolerated even at high doses |
Human Studies
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Case series: Intra-articular injection of BPC-157 in 12 patients with knee pain → 11 reported significant pain relief. Limitations: no control group, no blinding, subjective outcomes.
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Clinical trial: A Phase I safety and pharmacokinetic study (NCT02637284) in 42 healthy volunteers was conducted, but results have not been published.
Currently, no high-quality randomized controlled trials (RCTs) are available to confirm clinical efficacy and safety.
Safety & Potential Risks
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Angiogenesis: Beneficial for healing, but could theoretically promote tumor vascularization, accelerating growth or metastasis in cancer patients.
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Dose & Administration: Effective in animals at very low doses (ng–µg/kg), but optimal human dose and route remain undefined.
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Long-term use: No comprehensive long-term toxicity data; most studies are short-term.
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Regulatory status: Not approved as a drug in most countries; classified as a prohibited substance by WADA (World Anti-Doping Agency).
Comparative Insights & Limitations
| Comparison | Strengths | Limitations |
|---|---|---|
| Animal vs Human | Consistent beneficial effects in animals (tendon, nerve, liver repair, angiogenesis) | Human evidence is minimal, uncontrolled, and lacks long-term follow-up |
| Dose range | Effective at very low doses in animals (ng–µg/kg; µg/ml in vitro) | Safe/effective human dosing unknown |
| Onset of action | Early post-injury administration (e.g., 10 min after spinal injury) yields strong recovery | Clinical feasibility of such timing is unclear |
| Toxicity | No lethal dose or severe adverse effects observed in multiple animal species | Long-term toxicity, carcinogenicity, and reproductive safety remain untested |
Conclusion
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BPC-157 shows strong regenerative and protective effects in animal and cell models: angiogenesis, anti-inflammation, tissue repair, neuroprotection, and hepatoprotection.
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Human evidence is extremely limited, with no robust clinical trial data available.
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Further well-designed randomized controlled trials are required to establish efficacy, safety, optimal dosing, and administration routes in humans.
Post time: Sep-23-2025