Bioactive prenylated coumarins as potential anti-inflammatory and anti-HIV agents from Clausena lenis
Bioactive prenylated coumarins as potential anti-inflammatory and anti-HIV agents from Clausena lenis
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黄皮中具有生物活性的异戊二烯化香豆素作为潜在的抗炎和抗 HIV 药物
DOI：
10.1016/j.bioorg.2020.103699
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发表时间：
2020-04-01
影响因子：
5.1
通讯作者：
Fu, Yan-Hui
中科院分区：
文献类型：
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作者：
Liu, Yan-Ping;Yan, Gui;Fu, Yan-Hui
对黄皮茎的植物化学研究导致分离出三种新的异戊烯化香豆素，黄皮素A-C（1-3），以及九种已知的异戊烯化香豆素（4-12）。通过全面的光谱分析，阐明了新的异戊烯基香豆素（1-3）的化学结构，并通过将其实验光谱数据与文献中描述的数据进行比较，确定了已知化合物（4-12）。所有分离的异戊烯化香豆素进行了评估，他们的抗炎作用，以及在体外抗艾滋病毒的活动。异戊烯化香豆素1-12在体外对脂多糖诱导的小鼠巨噬细胞RAW 264.7产生一氧化氮（NO）有明显的抑制作用，其IC 50值与氢化可的松相当。同时，异戊烯化香豆素1-12表现出相当大的抗HIV-1逆转录酶（RT）活性，其EC 50值在0.17-9.08 μ M的范围内。这些发现表明，从C. lenis对开发新的抗炎和抗HIV药物及其在制药工业中的潜在应用具有重要意义。
The phytochemical study on the stems of Clausena lenis resulted in the isolation of three new prenylated coumarins, clauselenins A-C (1-3), together with nine known prenylated coumarins (4-12). The chemical structures of new prenylated coumarins (1-3) were elucidated by means of comprehensive spectral analyses and the known compounds (4-12) were determined by means of comparing their experimental spectral data with those described data in the literatures. All isolated prenylated coumarins were assessed for their anti-inflammatory effects together with anti-HIV activities in vitro. Prenylated coumarins 1-12 displayed remarkable inhibitory effects against nitric oxide (NO) production induced by lipopolysaccharide in mouse macrophage RAW 264.7 cells in vitro with the IC50 values which are comparable to hydrocortisone. Meanwhile, prenylated coumarins 1-12 exhibited considerable anti-HIV-1 reverse transcriptase (RT) activities possessing EC50 values in the range of 0.17-9.08 mu M. These findings indicate that the isolation and identification of these prenylated coumarins with pronounced anti-inflammatory effects as well as anti-HIV activities separated from the stems of C. lenis could be of great significance to the development of new anti-inflammatory and anti-HIV agents and their potential applications in the pharmaceutical industry.