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一种来自栀子属的细胞毒天然产物

A Cytotoxic Natural Product from Juss.

机构信息

School of Pharmaceutical Science, Liaoning University, Shenyang, China.

Department of Head and Neck Surgery, Cancer Hospital of China Medical University, Shenyang, Liaoning 110042, China.

出版信息

Anticancer Agents Med Chem. 2019;19(11):1399-1404. doi: 10.2174/1871520619666190416101014.

Abstract

BACKGROUND AND PURPOSE

Juss is an important Chinese herbal medicine widely used for thousands of years, but few reports on the ingredients of the herb have been presented. In this study, we aim to isolate the bioactive compound from the plant.

MATERIAL AND METHODS

The air-dried leaves of (15kg) were extracted three times with 70% EtOH under reflux. The condensed extract was suspended in HO and partitioned with light petroleum, dichloromethane and -BuOH. The dichloromethane portion was then subjected to normal-phase silica gel column chromatography, ODS silica gel column chromatography and semi-preparative HPLC to yield compound 1. Cytotoxicities of 1 were assayed on HepG2, A549 and A2780 cell lines. The mechanism of apoptosis and cell cycle on A549 was confirmed subsequently.

RESULTS

A new impecylone (Impecylone A) was isolated from the leaves of Juss, and its structures were established using 1D, 2D-NMR spectra and HR-ESI-MS. Impecylone A could selectivity inhibit HepG2 and A549 cell lines. The compound could induce apoptosis of A549 and arrest the cell cycle at G/M phase in a dose-dependent manner.

CONCLUSION

Impecylone A is a novel compound from Juss and could be a potential antitumor agent especially in the cell lines of A549.

摘要

背景与目的

鸡血藤是一种重要的中药,已有数千年的应用历史,但目前关于其成分的报道较少。本研究旨在从该植物中分离出生物活性化合物。

材料与方法

将 (15kg)的干燥叶片用 70% EtOH 在回流下提取三次。浓缩提取物混悬于 HO 中,用轻石油、二氯甲烷和 -BuOH 进行分配。二氯甲烷部分随后经正相硅胶柱层析、ODS 硅胶柱层析和半制备 HPLC 分离,得到化合物 1。测定了 1 对 HepG2、A549 和 A2780 细胞系的细胞毒性。随后证实了 1 在 A549 上的细胞凋亡和细胞周期的机制。

结果

从鸡血藤的叶片中分离得到一种新的异皮醇(Impecylone A),并通过 1D、2D-NMR 谱和 HR-ESI-MS 确定了其结构。Impecylone A 可以选择性地抑制 HepG2 和 A549 细胞系。该化合物可以剂量依赖性地诱导 A549 细胞凋亡,并将细胞周期阻滞在 G/M 期。

结论

Impecylone A 是从鸡血藤中分离得到的一种新型化合物,可能是一种潜在的抗肿瘤药物,尤其是在 A549 细胞系中。

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