摘要/Abstract
应用多种色谱和波谱学方法，从云南蕊木（Kopsia officinalis）茎中分离鉴定了27个单萜吲哚生物碱，包括7个新化合物kopsiofficines A～G和20个已知化合物.此外，建立脂多糖（LPS）诱导的小鼠巨噬细胞RAW 264.7炎症模型，通过测定IL-1β，PGE2和TNF-α炎症因子释放评价生物碱的抗炎活性.结果表明，kopsiofficines A（1），kopsiofficines B（2），kopsiofficines D（4），kopsiofficines F（6），kopsiofficines G（7），12-methoxykopsine（11），kopsinoline（15），（－）-N-methoxy-carbonyl-11，12-methylenedioxykopsinaline（16），kopsinine（18）和kopsinic acid（20）表现出显著的抗炎活性，与阳性对照（地塞米松）基本相当.研究发现C-5位丙酮基取代的单萜吲哚生物碱的抗炎活性明显强于原型生物碱，推测丙酮基可能是抗炎活性的药效促进基团，研究结果为进一步的结构修饰和药理学研究提供了线索.
关键词: 云南蕊木, kopsiofficines A～G, 抗炎, 单萜吲哚生物碱
Seven new monoterpenoid indole alkaloids, kopsiofficines A~G, together with twenty known alkaloids, were isolated from the stems of Kopsia officinalis. Their structures were elucidated on the basis of extensive spectroscopic methods. The anti-inflammatory activities of all alkaloids were evaluated on lipopolysaccharide (LPS)-stimulated RAW 264.7 cells by the inhibiting the production of IL-1β, PGE2 and TNF-α. Among them, kopsiofficines A (1), kopsiofficines B (2), kopsiofficines D (4), kopsiofficines F (6), kopsiofficines G (7), 12-methoxykopsine (11), kopsinoline (15), (-)-N-methoxycarbonyl-11,12-methylenedioxykopsinaline (16), kopsinine (18) and kopsinic acid (20) exhibited significant anti-inflammatory activity, which were comparable to that of dexamethasone. The results supposed that the acetonyl group at C-5 of monoterpenoid indole alkaloids play an important role in their anti-inflammatory activity.
Key words: Kopsia officinalis, kopsiofficines A～G, anti-inflammatory, monoterpenoid indole alkaloids
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