Attiq Ali, Jalil Juriyati, Afzal Sheryar, Ahmad Waqas
Discipline of Pharmacology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800, Gelugor, Penang, Malaysia.
Centre for Drug and Herbal Development, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300, Kuala Lumpur, Malaysia.
Inflammopharmacology. 2025 Jul 12. doi: 10.1007/s10787-025-01843-6.
In our previous findings, the methanol extract of A. elliptica (MEL) exhibited platelet-activating factor inhibition, indicating possible anti-inflammatory properties. Despite its ethnopharmacological significance, no studies have thoroughly investigated its anti-inflammatory potential. Based on our preliminary findings, we hypothesised that MEL might exert anti-inflammatory effects by modulating key inflammatory mediators, such as prostaglandin E2 (PGE2), cyclooxygenase-2 (COX-2), and pro-inflammatory cytokines (IL-1β and IL-6). The cytotoxicity of MEL was assessed on peripheral blood mononuclear cells (PBMCs) using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. In vitro, anti-inflammatory activity was investigated in lipopolysaccharide (LPS)-induced human plasma through an enzyme-linked immunosorbent assay (ELISA) and a radioimmunoassay. In addition, the phytochemical profile of MEL was characterised using LC-ESI-MS/MS spectrometry. The extract demonstrated no cytotoxic effects at 20 μg/mL concentrations. MEL exhibited significant anti-inflammatory activity, with notable inhibition of PGE2 (76.18%) and COX-2 (80.12%), as well as pronounced reductions in IL-1β and IL-6 levels, corresponding to 11.6-fold and ninefold decreases at 10 μg/mL, respectively. Concentration-dependent effects were observed, with IC₅₀ values of 4.09, 5.81, 2.12, and 1.97 μg/mL for PGE2, COX-2, IL-1β, and IL-6, respectively. LC-ESI-MS/MS analysis revealed the presence of 30 bioactive compounds, including Gramine, Eruberin B, and Grossamide, which likely contributed to the extract's anti-inflammatory effects. In conclusion, MEL abrogated LPS-induced inflammatory responses in human plasma at non-cytotoxic concentrations, demonstrating its potential as a natural anti-inflammatory agent. Furthermore, this study is the first to report the phytochemical composition of A. elliptica leaves, providing insights into its bioactive constituents and therapeutic potential.
在我们之前的研究结果中，椭圆叶滨藜甲醇提取物（MEL）表现出对血小板活化因子的抑制作用，表明其可能具有抗炎特性。尽管其具有民族药理学意义，但尚未有研究全面探究其抗炎潜力。基于我们的初步研究结果，我们推测MEL可能通过调节关键炎症介质，如前列腺素E2（PGE2）、环氧化酶-2（COX-2）和促炎细胞因子（IL-1β和IL-6）来发挥抗炎作用。使用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐法评估MEL对外周血单个核细胞（PBMCs）的细胞毒性。在体外，通过酶联免疫吸附测定（ELISA）和放射免疫测定法研究了MEL在脂多糖（LPS）诱导的人血浆中的抗炎活性。此外，使用液相色谱-电喷雾串联质谱（LC-ESI-MS/MS）光谱法对MEL的植物化学特征进行了表征。该提取物在20μg/mL浓度下未显示出细胞毒性作用。MEL表现出显著的抗炎活性，对PGE2（76.18%）和COX-2（80.12%）有明显抑制作用，同时IL-1β和IL-6水平也显著降低，在10μg/mL时分别下降了11.6倍和9倍。观察到浓度依赖性效应，PGE2、COX-2、IL-1β和IL-6的IC₅₀值分别为4.09、5.81、2.12和1.97μg/mL。LC-ESI-MS/MS分析揭示了30种生物活性化合物的存在，包括禾本科碱、埃鲁贝林B和格罗斯酰胺，这些可能是该提取物抗炎作用的原因。总之，MEL在非细胞毒性浓度下消除了LPS诱导的人血浆中的炎症反应，证明了其作为天然抗炎剂的潜力。此外，本研究首次报道了椭圆叶滨藜叶的植物化学成分，为其生物活性成分和治疗潜力提供了见解。
