熊果酸的生物转化及其抗神经炎症衍生物的发现。
Biotransformation of Ursonic Acid by and to Discover Anti-Neuroinflammatory Derivatives.
机构信息
School of Pharmacy, Nantong University, 19 Qixiu Road, Nantong 226001, China.
Department of Pharmacy, The Fourth Affiliated Hospital of Nantong University, The First People's Hospital of Yancheng, 166 Yulongxi Road, Yancheng 224005, China.
出版信息
Molecules. 2023 Dec 5;28(24):7943. doi: 10.3390/molecules28247943.
Biotransformation of ursonic acid () by two fungal strains CGMCC 3.5324 and CGMCC 3.407 yielded thirteen new compounds (, , -, and -), along with five recognized ones. The structural details of new compounds were determined through spectroscopic examination (NMR, IR, and HR-MS) and X-ray crystallography. Various modifications, including hydroxylation, epoxidation, lactonization, oxygen introduction, and transmethylation, were identified on the ursane core. Additionally, the anti-neuroinflammatory efficacy of these derivatives was assessed on BV-2 cells affected by lipopolysaccharides. It was observed that certain methoxylated and epoxylated derivatives (, , and ) showcased enhanced suppressive capabilities, boasting IC values of 8.2, 6.9, and 5.3 μM. Such ursonic acid derivatives might emerge as potential primary molecules in addressing neurodegenerative diseases.
两株真菌 CGMCC 3.5324 和 CGMCC 3.407 对熊果酸（）进行生物转化，生成了 13 种新化合物（、、-、-），以及 5 种已知化合物。新化合物的结构细节通过光谱分析（NMR、IR 和 HR-MS）和 X 射线晶体学确定。在ursane 核上鉴定了各种修饰，包括羟基化、环氧化、内酯化、氧引入和甲基化。此外，还评估了这些衍生物在脂多糖作用下对 BV-2 细胞的抗神经炎症活性。结果表明，某些甲氧基化和环氧化衍生物（、、和）具有增强的抑制能力，IC 值分别为 8.2、6.9 和 5.3 μM。这些熊果酸衍生物可能成为治疗神经退行性疾病的潜在主要分子。
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