Department of Pharmacology (State-Province Key Laboratories of Biomedicine-Pharmaceutics of China, Key Laboratory of Cardiovascular Medicine Research, Ministry of Education), College of Pharmacy, Harbin Medical University, Harbin, Heilongjiang, 150081, People's Republic of China.
Department of Michael Smith Building, Division of Cardiovascular Sciences, Faculty of Biology, Medicine and Health, The University of Manchester, Manchester, UK.
Eur J Pharmacol. 2023 Sep 5;954:175803. doi: 10.1016/j.ejphar.2023.175803. Epub 2023 Jun 8.
Peritoneal adhesion is a common abdominal surgical complication that induces abdominal haemorrhage, intestinal obstruction, infertility, and so forth. The high morbidity and recurrence rate of this disease indicate the need for novel therapeutic approaches. Here, we revealed the protective roles of tetrahydroberberrubine (THBru), a novel derivative of berberine (BBR), in preventing peritoneal adhesion and identified its underlying mechanism in vivo and in vitro. Abrasive surgery was used to create a peritoneal adhesion rat model. We found that THBru administration markedly ameliorated peritoneal adhesion, as indicated by a lowered adhesion score and ameliorated caecal tissue damage. By comparison, THBru exhibited more potent anti-adhesion effects than BBR at the same dose. Mechanistically, THBru inhibited inflammation and extracellular matrix (ECM) accumulation in the microenvironment of adhesion tissue. THBru suppressed the expression of inflammatory cytokines including interleukin-1β (IL-1β), IL-6, transforming growth factor β (TGF-β), tumor necrosis factor-α (TNF-α) and intercellular adhesion molecule-1 (ICAM-1), by regulating the transforming growth factor beta-activated kinase 1 (TAK1)/c-Jun N-terminal kinase (JNK) and TAK1/nuclear factor κB (NF-κB) signaling pathways. However, THBru promoted the activation of MMP-3 by directly blocking the TIMP-1 activation core and subsequently decreased collagen deposition. Taken together, this study identifies THBru as an effective anti-adhesion agent that regulates diverse mechanisms, thereby outlining its potential therapeutic implications for the treatment of peritoneal adhesion.
腹膜粘连是一种常见的腹部外科并发症,可导致腹腔出血、肠梗阻、不孕等。这种疾病的高发病率和复发率表明需要新的治疗方法。在这里,我们揭示了四氢小檗红碱(THBru),一种小檗碱(BBR)的新型衍生物,在预防腹膜粘连中的保护作用,并在体内和体外确定了其潜在机制。磨蚀手术用于创建腹膜粘连大鼠模型。我们发现,THBru 给药显著改善了腹膜粘连,粘连评分降低,盲肠组织损伤得到改善。相比之下,THBru 在相同剂量下表现出比 BBR 更强的抗粘连作用。在机制上,THBru 抑制了粘连组织微环境中的炎症和细胞外基质(ECM)积累。THBru 通过调节转化生长因子β激活激酶 1(TAK1)/c-Jun N 末端激酶(JNK)和 TAK1/核因子 κB(NF-κB)信号通路,抑制包括白细胞介素 1β(IL-1β)、IL-6、转化生长因子β(TGF-β)、肿瘤坏死因子-α(TNF-α)和细胞间黏附分子 1(ICAM-1)在内的炎症细胞因子的表达。然而,THBru 通过直接阻断 TIMP-1 激活核心促进 MMP-3 的激活,随后减少胶原蛋白沉积。总之,这项研究确定了 THBru 作为一种有效的抗粘连剂,它通过调节多种机制发挥作用,从而为治疗腹膜粘连提供了潜在的治疗意义。