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恩杜拉辛C,是Ophiobolin类型的sesterterpenoid,具有来自Aspergillus undulatus的抗自身免疫性肝炎活性

Yuyi Zheng¹, Yongqi Li¹, Qin Li¹

¹Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.

Bioorganic chemistry

|October 15, 2025

概括

来自Aspergillus undulatus的十种新型的ophiobolin sesterterpenoids显示出免疫抑制的潜力. 化合物3在自身免疫性肝炎模型中表现出有效性,这表明它可以用作治疗支架.

科学领域:

自然产品化学化学
免疫学免疫学免疫学
药理学药理学是指药理学的学科.

背景情况:

阿斯珀吉勒斯原产生的各种二次代谢产物.
奥菲奥玻林是一种具有已知的生物活动的甲类的类.
自免疫性肝炎 (AIH) 需要新的治疗策略.

研究的目的:

从Aspergillus undulatus中分离和表征新型的ophiobolin sesterterpenoids. 这种新型的ophiobolin是来自Aspergillus undulatus.
评估这些化合物的免疫抑制和抗AIH活性.
探索最活跃化合物的分子机制.

主要方法:

使用NMR,HRESIMS和ECD数据进行隔离和结构阐明.
在体外评估T淋巴细胞增殖抑制.
在自身免疫性肝炎的小鼠模型中的体内评估.
网络药理学和分子对接用于目标预测.

主要成果:

确定了10种新的ophiobolins (1-8,10,11) 和一个已知的类似物 (9).
化合物3显示了中度的免疫抑制活性 (IC50 = 9.74 μM).
化合物3减轻了肝损伤,并在体内减少了炎症性细胞因子.
网络药理学发现SRC是化合物3的潜在标 (结合亲和力 -8.0 kcal/mol).

结论:

这项研究扩大了ophiobolins的结构多样性.
化合物3对自身免疫性肝炎具有治疗潜力.
SRC是AIH中化合物3活动的潜在目标.

关键词:

亚斯珀吉勒斯 (Aspergillus undulatus) 是一个波状的植物.自体免疫性肝炎是一种自身免疫性肝炎.网络药理学网络药理学这种药物是Ophiobolins.这里是Sesterterpenoids的位置.

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