Muhtar Eldar, Ylham Gulfira, Tiemuer Atawulla, Edirs Salamet
Institute of Agro-products Storage and Processing, Xinjiang Key Laboratory of Processing and Preservation of Agricultural Products, Xinjiang Academy of Agricultural Science, Urumqi, Xinjiang, 830091, China.
Chem Biodivers. 2025 Feb;22(2):e202401564. doi: 10.1002/cbdv.202401564. Epub 2024 Nov 7.
Acteoside (ACT) is one of the primary bioactive ingredients in Cistanche tubulosa (Schenk). Its remarkable efficacy in treating immune-related and inflammatory disorders has garnered significant interest among scientific circles. However, the anti-inflammatory and antioxidant effects of ACT and its underlying molecular mechanisms require further investigation. In this study, pharmacophore-based reverse docking and molecular dynamics simulations identified potential anti-inflammatory targets in silico. Studies conducted in vitro with lipopolysaccharide (LPS)-induced RAW264.7 cells validated the anti-inflammatory properties of ACT. Methyl thiazolyl tetrazolium (MTT) and lactate dehydrogenase (LDH) assays indicated ACT's non-toxic and growth-promoting effects on cells. ACT significantly reduced nitric oxide (NO) and reactive oxygen species (ROS) production and restored levels of antioxidant enzymes. It also decreased pro-inflammatory cytokines. Western blotting assays indicated that ACT inhibited p38, TNF-α, PI3 K/AKT, and NF-κB signaling pathways. These findings underscore ACT's ability to mitigate acute inflammation in RAW264.7 cells by modulating key signaling pathways and provide the scientific basis for enhancing the medicinal value of ACT and future drug development.
松果菊苷（ACT）是管花肉苁蓉中的主要生物活性成分之一。其在治疗免疫相关和炎症性疾病方面的显著疗效已引起科学界的广泛关注。然而，ACT的抗炎和抗氧化作用及其潜在的分子机制仍需进一步研究。在本研究中，基于药效团的反向对接和分子动力学模拟在计算机上确定了潜在的抗炎靶点。用脂多糖（LPS）诱导RAW264.7细胞进行的体外研究验证了ACT的抗炎特性。甲基噻唑基四氮唑（MTT）和乳酸脱氢酶（LDH）测定表明ACT对细胞无毒且具有促生长作用。ACT显著降低了一氧化氮（NO）和活性氧（ROS）的产生，并恢复了抗氧化酶的水平。它还降低了促炎细胞因子。蛋白质印迹分析表明，ACT抑制了p38、TNF-α、PI3 K/AKT和NF-κB信号通路。这些发现强调了ACT通过调节关键信号通路减轻RAW264.7细胞急性炎症的能力，并为提高ACT的药用价值和未来药物开发提供了科学依据。
