Department of Pharmacy, Zhongnan Hospital of Wuhan University, School of Pharmaceutical Sciences, Wuhan University, Wuhan, 430071, China; Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Wuhan University), Ministry of Education, and Wuhan University, Wuhan, 430071, China.
Renmin Hospital of Wuhan University, Wuhan, 430060, China.
Phytochemistry. 2024 Nov;227:114232. doi: 10.1016/j.phytochem.2024.114232. Epub 2024 Aug 2.
A bioassay-guided isolation from Atractylodes lancea (Thunb.) DC. obtained 22 compounds, including eight previously undescribed sesquiterpenoids and polyacetylenes (1, 3 and 12-17), as well as fourteen known analogues, and their structures were confirmed by extensive spectroscopic methods. This study evaluated their antibacterial activity against methicillin resistant Staphylococcus aureus (MRSA) for the first time, as well as anti-inflammatory activity. Most of them, including new compounds, showed varying degrees of antibacterial activity against S. aureus and MRSA. Notably, compound 21 exhibited significant antibacterial activity against four different bacteria (MIC 6.25-20.00 μg/mL). This suggested that 21 may have the potential to be developed into a broad-spectrum antibacterial agent. Moreover, except for 9 and 11, most compounds exhibited great anti-inflammatory activity (IC 1.92-37.91 μM), and iNOS might be a potential target of these compounds according to the molecular docking analysis.
从白术（白术）（DC。）中分离得到的生物测定指导获得了 22 种化合物，包括 8 种以前未描述的倍半萜烯和炔（1、3 和 12-17），以及 14 种已知类似物，其结构通过广泛的光谱方法证实。本研究首次评估了它们对耐甲氧西林金黄色葡萄球菌（MRSA）的抗菌活性，以及抗炎活性。它们中的大多数，包括新化合物，对金黄色葡萄球菌和 MRSA 均显示出不同程度的抗菌活性。值得注意的是，化合物 21 对四种不同的细菌（MIC 6.25-20.00μg/mL）显示出显著的抗菌活性。这表明 21 可能有潜力开发成一种广谱抗菌剂。此外，除了 9 和 11，大多数化合物均表现出很强的抗炎活性（IC 1.92-37.91μM），并且根据分子对接分析，iNOS 可能是这些化合物的潜在靶标。
