Anti-inflammatory octahydroindolizine alkaloid enantiomers from Dendrobium crepidatum.,Bioorganic Chemistry

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Anti-inflammatory octahydroindolizine alkaloid enantiomers from Dendrobium crepidatum.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2020-04-02 , DOI: 10.1016/j.bioorg.2020.103809
Yang Hu ₁ , Hua Yang ₂ , Xiaoqian Ding ₂ , Jian Liu ₂ , Xiachang Wang ₂ , Lihong Hu ₂ , Minyan Liu ₃ , Chaofeng Zhang ₄

Affiliation

Six pairs of octahydroindolizine-type alkaloid enantiomers (1-6) including three new compounds [(-)-1/(+)-1, 2] were isolated from the stems of Dendrobium crepidatum. Their structures including the absolute configurations were elucidated by extensive spectroscopic analyses and comparison between the experimental and calculated electronic circular dichroism (ECD). All compounds were examined for their inhibitory effects on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW264.7 cells. It was found that compounds (+)-1, 2 and (+)-6 exhibited pronounced inhibition on NO production with IC50 values in the range of 3.62-16.11 µM, being more active than the positive control, dexamethasone (IC50 = 47.04 µM). In vivo, compound 6 (100, 50 and 10 mg/kg) showed protective effects against LPS-induced acute lung injury (ALI) in mice.

中文翻译：

石cre石end的抗炎八氢吲哚嗪生物碱对映体。

从铁皮石end的茎中分离出六对八氢吲哚嗪类生物碱对映体（1-6），包括三个新化合物[（-）-1 /（+）-1，2]。通过广泛的光谱分析以及实验和计算的电子圆二色性（ECD）之间的比较，阐明了它们的结构，包括绝对构型。检查所有化合物对RAW264.7细胞中脂多糖（LPS）诱导的一氧化氮（NO）产生的抑制作用。发现化合物（+）-1、2和（+）-6对NO的产生具有明显的抑制作用，IC50值在3.62-16.11 µM范围内，比阳性对照地塞米松（IC50 = 47.04 µM）更具活性。）。在体内，化合物6（100、50和10 mg / kg）在小鼠中显示出对LPS诱导的急性肺损伤（ALI）的保护作用。

更新日期：2020-04-02

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