Alherz Fatemah A, Abdallah Mahmoud S, Mosalam Esraa M, Bahaa Mostafa M, Elmasry Thanaa A, El-Gammal Mohamad A, Negm Walaa A, Elberri AyaIbrahim, Elshorbagi Nora, Abo Mansour Hend E, Hamouda Amir O, Salahuddin Muhammed M, Yasser Mohamed, Eldesoqui Mamdouh, Alrubia Sarah, Alsegiani Amsha S, El-Khateeb Eman, ElMahdy Mohamed Kh, Wahsh Eman
Department of Pharmaceutical Sciences, College of Pharmacy, Princess Nourah Bint Abdulrahman University, Riyadh, Saudi Arabia.
Department of PharmD, Faculty of Pharmacy, Jadara University, Irbid, Jordan.
Pharmacol Res Perspect. 2025 Jun;13(3):e70115. doi: 10.1002/prp2.70115.
Multiple signaling pathways have been implicated in the pathogenesis of ulcerative colitis (UC), including Sphingosine Kinase 1 (SPHK)/Sphingosine-1-Phosphate (S1P), AMP-activated protein kinase (AMPK)/mammalian target of rapamycin (mTOR)/NLR family pyrin domain-containing 3 (NLRP3), zonula occludens-1 (ZO-1), and signal transducer and activator of transcription 3 (STAT3). We aimed to investigate the Colo protective and anti-ulcerative effects of pentoxifylline (PTX) in a rat model of UC. Colitis was induced by intracolonic administration of 2 mL of 3% (v/v) acetic acid (AA). Thirty-five rats were randomly assigned to five groups (n = 7 each): normal control, colitis, mesalamine, PTX, and a combination of PTX plus mesalamine. Disease activity was assessed using the disease activity index, colon weight and length measurements, histological examination, and immunohistochemical detection of caspase-3. Colonic tissue homogenates were analyzed for interleukin-6 (IL-6), S1P, SPHK, mTOR, heme oxygenase-1 (HO-1), nuclear factor erythroid 2-related factor 2 (Nrf2), AMPK, and STAT3 levels. Gene expression of ZO-1 and NLRP3 was also evaluated. Intracolonic AA induced marked functional, biochemical, and inflammatory damage to colonic tissue. Treatment with PTX, mesalamine, or their combination significantly attenuated these effects. Specifically, all treatments reduced levels of IL-6, S1P, SPHK, mTOR, STAT3, NLRP3, and caspase-3, while increasing levels of ZO-1, HO-1, Nrf2, and AMPK. The combination treatment group exhibited near-complete restoration of normal colonic architecture, characterized by intact crypt morphology and minimal fibrosis in the lamina propria. PTX attenuated inflammation, apoptosis, and oxidative stress in colitis, supporting its potential as an adjuvant therapy in UC management.
多种信号通路与溃疡性结肠炎(UC)的发病机制有关,包括鞘氨醇激酶1(SPHK)/1-磷酸鞘氨醇(S1P)、AMP激活的蛋白激酶(AMPK)/雷帕霉素哺乳动物靶蛋白(mTOR)/含NLR家族pyrin结构域3(NLRP3)、紧密连接蛋白1(ZO-1)以及信号转导和转录激活因子3(STAT3)。我们旨在研究己酮可可碱(PTX)在UC大鼠模型中的结肠保护和抗溃疡作用。通过向结肠内注射2 mL 3%(v/v)乙酸(AA)诱导结肠炎。将35只大鼠随机分为五组(每组n = 7):正常对照组、结肠炎组、美沙拉嗪组、PTX组以及PTX加美沙拉嗪联合组。使用疾病活动指数、结肠重量和长度测量、组织学检查以及caspase-3的免疫组织化学检测来评估疾病活动度。分析结肠组织匀浆中白细胞介素-6(IL-6)、S1P、SPHK、mTOR、血红素加氧酶-1(HO-1)、核因子红细胞2相关因子2(Nrf2)、AMPK和STAT3的水平。还评估了ZO-1和NLRP3的基因表达。结肠内注射AA对结肠组织造成了明显的功能、生化和炎症损伤。PTX、美沙拉嗪或它们的联合治疗显著减轻了这些影响。具体而言,所有治疗均降低了IL-6、S1P、SPHK、mTOR、STAT3、NLRP3和caspase-3的水平,同时提高了ZO-1、HO-1、Nrf2和AMPK的水平。联合治疗组表现出结肠正常结构近乎完全恢复,其特征为隐窝形态完整且固有层纤维化轻微。PTX减轻了结肠炎中的炎症、细胞凋亡和氧化应激,支持其作为UC治疗辅助药物的潜力。