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Diarylheptanoids with NO production inhibitory activity from Amomum kravanh.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-02-13 , DOI: 10.1016/j.bmcl.2020.127026 Jun-Sheng Zhang 1 , Xin-Xin Cao 1 , Jin-Hai Yu 1 , Zhi-Pu Yu 1 , Hua Zhang 1
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-02-13 , DOI: 10.1016/j.bmcl.2020.127026 Jun-Sheng Zhang 1 , Xin-Xin Cao 1 , Jin-Hai Yu 1 , Zhi-Pu Yu 1 , Hua Zhang 1
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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 IC50 values in the range of 17.4-26.5 μM, being more potent than the positive control dexamethasone (IC50 = 32.5 μM).
中文翻译：
砂仁中不产生抑制活性的二芳基庚烷。
从砂仁砂仁的果实中分离出了七个新的二芳基庚烷类化合物，香芹酚CI（1-7），以及两个已知的类似物（8和9）。通过光谱数据分析阐明了化合物1-7的结构，并通过基于时间依赖性密度泛函理论（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。评价了所有化合物对鼠RAW264.7巨噬细胞中脂多糖（LPS）诱导的一氧化氮（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，IC50值在17.4-26.5μM范围内，比阳性对照地塞米松（IC50 = 32.5μM）更有效。
更新日期：2020-02-20
中文翻译：
砂仁中不产生抑制活性的二芳基庚烷。
从砂仁砂仁的果实中分离出了七个新的二芳基庚烷类化合物，香芹酚CI（1-7），以及两个已知的类似物（8和9）。通过光谱数据分析阐明了化合物1-7的结构，并通过基于时间依赖性密度泛函理论（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。评价了所有化合物对鼠RAW264.7巨噬细胞中脂多糖（LPS）诱导的一氧化氮（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，IC50值在17.4-26.5μM范围内，比阳性对照地塞米松（IC50 = 32.5μM）更有效。
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