Kopsileuconines A-D (1-4)，四种具有前所未有的骨架的单萜双吲哚生物碱，及其生物合成相关的前体 (5-8) 从海南 Kopsia 的根中分离出来。化合物 1 具有未描述的 aspidofractinine 型生物碱的 C-6-C-5' 二聚模式。化合物2-4分别是具有未描述骨架的Rhazinilam-kopsine (2)和Rhazinilam-aspidofractinine型(3和4)双吲哚生物碱。它们的绝对构型结构是通过广泛的光谱分析、量子化学计算和X射线晶体学完全完成的。提出了 1-4 的合理生物合成途径。化合物2对人肺癌细胞系PC9（EGFR突变体）具有显着的抑制作用，IC50值为15.07±1.19μM。版权所有©2024。Elsevier Ltd.出版。

Kopsileuconines A-D (1-4), four monoterpenoid bisindole alkaloids with unprecedented skeletons, along with their biosynthetically related precursors (5-8) were isolated from the roots of Kopsia hainanensis. Compound 1 possessed an undescribed C-6-C-5' dimerization pattern of aspidofractinine-type alkaloids. Compounds 2-4 were rhazinilam-kopsine (2) and rhazinilam-aspidofractinine type (3 and 4) bisindole alkaloids with undescribed skeletons, respectively. Their structures with absolute configurations were fully accomplished by extensive spectroscopic analysis, quantum-chemical calculations, and X-ray crystallography. A plausible biosynthetic pathway for 1-4 was proposed. Compound 2 exhibited a significant inhibitory effect against human lung cancer cell lines PC9 (EGFR mutant), with an IC50 value of 15.07 ± 1.19 μM.Copyright © 2024. Published by Elsevier Ltd.