Poupartia borbonica is an endemic tree from the Mascarene Islands that belongs to the Anacardiaceae family. The leaves of this plant were phytochemically studied previously, and isolated alkyl cyclohexenone derivatives, poupartones A – C, demonstrated antiplasmodial and antimalarial activities. In addition to their high potency against the Plasmodium sp., high toxicity on human cells was also displayed. The present study aims to investigate in more detail the cytotoxicity and pharmacological interest of poupartone B, one of the most abundant derivatives in the leaves of P. borbonica. For that purpose, real-time live-cell imaging of different human cancer cell lines and normal fibroblasts, treated or not treated with poupartone B, was performed. A potent inhibition of cell proliferation associated with the induction of cell death was observed. A detailed morphological analysis of different adherent cell lines exposed to high concentrations of poupartone B (1 – 2 µg/mL) demonstrated that this compound induced an array of cellular alterations, including a rapid retraction of cellular protrusions associated with cell rounding, massive cytoplasmic vacuolization, loss of plasma membrane integrity, and plasma membrane bubbling, ultimately leading to paraptosis-like cell death. The structure-activity relation of this class of compounds, their selective toxicity, and pharmacological potential are discussed.

中文翻译：

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Poupartone B（一种来自 Poupartia borbonica 的烷基环己烯酮衍生物）对人类癌细胞系的细胞毒性

Poupartia borbonica 是马斯卡林群岛的特有树种，属于漆树科。先前对这种植物的叶子进行了植物化学研究，分离出的烷基环己烯酮衍生物 poupartones A – C 表现出抗疟原虫和抗疟活性。除了它们对疟原虫的高效力外，还显示出对人体细胞的高毒性。本研究旨在更详细地研究 poupartone B 的细胞毒性和药理学意义，它是 P. borbonica 叶子中最丰富的衍生物之一。为此目的，对不同的人类癌细胞系和正常成纤维细胞进行了实时活细胞成像，用 poupartone B 处理或未处理。观察到与诱导细胞死亡相关的细胞增殖的有效抑制。对暴露于高浓度 poupartone B (1 – 2 µg/mL) 的不同贴壁细胞系进行详细的形态学分析表明，该化合物诱导了一系列细胞改变，包括与细胞变圆、大量细胞质空泡化相关的细胞突起快速收缩，质膜完整性丧失和质膜起泡，最终导致细胞凋亡样死亡。讨论了这类化合物的构效关系、选择性毒性和药理潜力。大量细胞质空泡化、质膜完整性丧失和质膜起泡，最终导致细胞凋亡样细胞死亡。讨论了这类化合物的构效关系、选择性毒性和药理潜力。大量细胞质空泡化、质膜完整性丧失和质膜起泡，最终导致细胞凋亡样细胞死亡。讨论了这类化合物的构效关系、选择性毒性和药理潜力。