Discovery of an Oxepine-Containing Diketopiperazine Derivative Active against Concanavalin A-Induced Hepatitis.,Journal of Natural Products

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Discovery of an Oxepine-Containing Diketopiperazine Derivative Active against Concanavalin A-Induced Hepatitis.
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-09-08 , DOI: 10.1021/acs.jnatprod.0c00558
Changxing Qi ₁ , Xiaosheng Tan _{2,

3,

4,

5} , Zhengyi Shi ₁ , Hao Feng _{2,

3,

4,

5} , Lingjuan Sun _{2,

3,

4,

5} , Zhengxi Hu ₁ , Gang Chen _{2,

3,

4,

5} , Yonghui Zhang ₁

Affiliation

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.

中文翻译：

发现了一种抗伴刀豆球蛋白 A 诱发的肝炎的含氧西平二酮哌嗪衍生物活性物质。

Varioxepine B ( 1 )，一种含氧杂的二酮哌嗪衍生物，是从海洋来源的土曲霉菌株中分离出来的。通过光谱实验、单晶X射线衍射分析和电子圆二色性计算确定了1的结构。值得注意的是，1可以在体外抑制刀豆蛋白 A (Con A) 激活的鼠脾细胞增殖。更重要的是，在 Con A 攻击的小鼠中，用1预处理明显减少了促炎细胞因子的产生并减轻了肝损伤。同时，1 还在抗 CD3/抗 CD28 单克隆抗体 (mAb) 诱导的鼠脾细胞和人 T 细胞增殖以及 Th1 和 Th2 细胞因子产生中表现出抑制活性。

更新日期：2020-09-25

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