Jeong So Yeong, Kang Dong-Min, Kim Hyun-Jun, Yeon Sang Won, Lee Hak Hyun, Kim Min Hee, Hwang Bang Yeon, Ahn Mi-Jeong, Lee Mi Kyeong
College of Pharmacy, Chungbuk National University, Cheongju 28160, Republic of Korea.
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju 52828, Republic of Korea.
Molecules. 2025 Jul 26;30(15):3142. doi: 10.3390/molecules30153142.
, a spiral-shaped bacterium found in the stomach, is associated with various gastrointestinal and systemic health conditions. Effective suppression of is therefore critical for managing gastrointestinal diseases. In a search for natural products with anti- activity, the extract of rhizoma showed significant inhibitory effects. Chromatographic purification of extract yielded thirteen compounds, which were identified as ten sesquiterpenes and three polyacetylenes by spectroscopic analysis. The sesquiterpene compounds belong to the eudesmane or eudesmane lactone types and exhibited structure-dependent efficacy. The major eudesmane lactone sesquiterpene, atractylenolide I (), showed strong inhibitory activity comparable to metronidazole, a positive control, and atractylenolide III () also showed good efficacy. However, structural modification such as hydroxylation, methylation, or acetylation of the sesquiterpenes led to reduced activity. In contrast, polyacetylene derivatives displayed only mild inhibitory effects. Further evaluation of the active compounds against three strains such as 51, 43504, and 26695 showed that atractylenolide I () had potent inhibitory effects against all three strains, with MIC values of ranging from 27.3 to 48.6 μM and MIC values from 45.4 to 87.2 μM. Atractylenolide III () exhibited selective activity against strain 51 with MIC value of 89.9 μM. Both compounds also exhibited anti-inflammatory activity with IC values of 23.3 and 31.1 μM, respectively, although they showed little effect on urease. This is the first report on the anti- efficacy of various constituents of and comparative analysis of inhibitory effects against several strains, which will provide scientific evidence supporting its potential as therapeutic agent for -related infection.
幽门螺杆菌是一种在胃中发现的螺旋形细菌，与各种胃肠道和全身健康状况有关。因此，有效抑制幽门螺杆菌对于管理胃肠道疾病至关重要。在寻找具有抗幽门螺杆菌活性的天然产物时，白术根茎提取物显示出显著的抑制作用。白术提取物的色谱纯化产生了13种化合物，通过光谱分析鉴定为10种倍半萜和3种聚乙炔。倍半萜化合物属于桉烷型或桉烷内酯型，并表现出结构依赖性功效。主要的桉烷内酯倍半萜白术内酯I对幽门螺杆菌显示出与阳性对照甲硝唑相当的强抑制活性，白术内酯III也显示出良好的功效。然而，倍半萜的羟基化、甲基化或乙酰化等结构修饰导致活性降低。相比之下，聚乙炔衍生物仅显示出轻微的抑制作用。对51、43504和26695等三种幽门螺杆菌菌株的活性化合物的进一步评估表明，白术内酯I对所有三种菌株都有强效抑制作用，MIC值范围为27.3至48.6μM，MBC值为45.4至87.2μM。白术内酯III对51菌株表现出选择性活性，MIC值为89.9μM。这两种化合物还表现出抗炎活性，IC50值分别为23.3和31.1μM，尽管它们对脲酶几乎没有影响。这是关于白术各种成分的抗幽门螺杆菌功效以及对几种菌株抑制作用的比较分析的首次报告，这将为支持其作为幽门螺杆菌相关感染治疗剂的潜力提供科学证据。
