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稳定的胃十五肽 BPC 157:胃肠道的新型治疗方法。

Stable gastric pentadecapeptide BPC 157: novel therapy in gastrointestinal tract.

机构信息

Department of Pharmacology and Pathology Medical Faculty University of Zagreb, Zagreb, Croatia.

出版信息

Curr Pharm Des. 2011;17(16):1612-32. doi: 10.2174/138161211796196954.

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.

摘要

稳定的胃十五肽 BPC 157 是一种抗溃疡肽类药物,在炎症性肠病临床试验(GEPPPGKPADDAGLV,MW1419,PL14736)和伤口愈合中是安全的,在人类胃液中稳定,且没有毒性报告。我们专注于 BPC 157 作为牙周炎、食管、胃、十二指肠、肠、肝和胰腺病变的治疗方法。特别是,它对酒精性病变(即急性、慢性)和 NSAIDs 性病变有显著的作用(有趣的是,BPC 157 既能预防又能逆转佐剂性关节炎)。在大鼠食管炎和下食管括约肌(LES)和幽门括约肌(PS)功能衰竭的情况下,BPC 157 增加了两个括约肌的压力,直至正常,并减轻了食管炎。然而,在健康的大鼠中,它可能会降低(PS)或增加(LES)括约肌的压力。它具有很强的血管生成潜力,对内皮起保护作用,预防和逆转腹主动脉吻合术后血栓形成,影响许多中枢干扰(即多巴胺和 5-HT 系统),一氧化氮系统(无论是 L-精氨酸和 L-NAME 效应),内皮素,作为自由基清除剂(对抗 CCl4-、扑热息痛、双氯芬酸损伤),并表现出神经保护特性。BPC 157 成功地治愈了大鼠的肠吻合、皮胃、十二指肠皮和结肠皮瘘,以及与一氧化氮系统的相互作用。有趣的是,即使 BPC 157 治疗推迟一个月,瘘管关闭也能实现。在短肠综合征在 4 周内逐渐加重的情况下,口服和肠外 BPC 157 治疗后,体重立即开始超过术前值增加,绒毛高度、隐窝深度和肌肉厚度(内(环形)肌层)也增加。因此,BPC 157 可能改善胃肠道治疗。

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