Discovery of an Oxepine-Containing Diketopiperazine Derivative Active against Concanavalin A‑Induced Hepatitis

Varioxepine B (1), an oxepine-containing diketopiperazine derivative, was isolated from a marine-derived Aspergillus terreus strain. The structure of 1 was identified by spectroscopic experiments, single-crystal X-ray diffraction analysis, and electronic circular dichroism calculations. It is notewo...

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Bibliographic Details
Published in:Journal of natural products (Washington, D.C.) D.C.), 2020-09, Vol.83 (9), p.2672-2678
Main Authors: Qi, Changxing, Tan, Xiaosheng, Shi, Zhengyi, Feng, Hao, Sun, Lingjuan, Hu, Zhengxi, Chen, Gang, Zhang, Yonghui
Format: Article
Language:English
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Summary:Varioxepine B (1), an oxepine-containing diketopiperazine derivative, was isolated from a marine-derived Aspergillus terreus strain. The structure of 1 was identified by spectroscopic experiments, single-crystal X-ray diffraction analysis, and electronic circular dichroism calculations. It is noteworthy that 1 could suppressed murine splenocyte proliferation activated by concanavalin A (Con A) in vitro. More importantly, in Con A-challenged mice, pretreatment with 1 obviously decreased the generation of proinflammatory cytokines and ameliorated liver injury. Meanwhile, 1 also exhibited inhibitory activity in anti-CD3/anti-CD28 monoclonal antibodies (mAbs)-induced murine splenocytes and human T cell proliferation as well as both Th1 and Th2 cytokine production.
ISSN:0163-3864
1520-6025
DOI:10.1021/acs.jnatprod.0c00558