来自阳春砂的具有抑制一氧化氮生成活性的二芳基庚烷类化合物。

Diarylheptanoids with NO production inhibitory activity from Amomum kravanh.

机构信息

School of Biological Science and Technology, University of Jinan, Jinan, China.

出版信息

Bioorg Med Chem Lett. 2020 Apr 15;30(8):127026. doi: 10.1016/j.bmcl.2020.127026. Epub 2020 Feb 13.

DOI:10.1016/j.bmcl.2020.127026

PMID:32070636

Abstract

Seven new diarylheptanoids, kravanhols C-I (1-7), along with two known analogues (8 and 9), were isolated from the fruits of Amomum kravanh. The structures of compounds 1-7 were elucidated by analysis of spectroscopic data, and the absolute configurations of selective ones were determined by time-dependent density functional theory (TD-DFT) based electronic circular dichroism (ECD) calculations. All compounds were evaluated for their inhibitory effects on the nitric oxide (NO) production induced by lipopolysaccharide (LPS) in murine RAW264.7 macrophage cells. Compounds 2, 5, 6 and 9 exhibited moderate inhibitory activity with IC values in the range of 17.4-26.5 μM, being more potent than the positive control dexamethasone (IC = 32.5 μM).

摘要

从阳春砂果实中分离得到了 7 个新的二芳基庚烷类化合物，即 kravanhols C-I（1-7），以及 2 个已知类似物（8 和 9）。通过分析光谱数据阐明了化合物 1-7 的结构，并通过基于时间依赖密度泛函理论（TD-DFT）的电子圆二色性（ECD）计算确定了选择性化合物的绝对构型。所有化合物均评估了其对脂多糖（LPS）诱导的小鼠 RAW264.7 巨噬细胞中一氧化氮（NO）产生的抑制作用。化合物 2、5、6 和 9 表现出中等抑制活性，IC 值在 17.4-26.5 μM 范围内，比阳性对照地塞米松（IC = 32.5 μM）更有效。