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女贞子(Roxb.)中分离得到的化合物对 HepG2 肝癌细胞的抑制活性:异贝壳杉烯和 4-(2-乙酰氧基乙基)苯酚作为潜在的候选药物。

Inhibitory Activity of Compounds Isolated from Ligustrum robustum (Roxb.) Against HepG2 Liver Cancer Cells: Isocubein and 4-(2-Acetoxyethyl)phenol as Potential Candidates.

机构信息

Thai Nguyen University of Medicine and Pharmacy, Thai Nguyen University, Thai Nguyen, Vietnam.

Thai Nguyen University of Sciences, Thai Nguyen University, Thai Nguyen, Vietnam.

出版信息

Chem Biodivers. 2024 Oct;21(10):e202401065. doi: 10.1002/cbdv.202401065. Epub 2024 Sep 6.

DOI:10.1002/cbdv.202401065
PMID:39004876
Abstract

Many herbal species in the genus Ligustrum have been shown to contain compounds with anti-cancer biological activity. This study aimed to isolate some compounds from the leaves of Ligustrum robustum (Roxb.) Blume (L. robustum) and evaluate their effects against liver cancer cells. As a result, seven previously reported compounds (1-7) were isolated, including four lignans (1-4) and three phenolic derivatives (5-7). The structures of these compounds were determined using spectroscopic methods and comparison with reported data. All isolates were assessed for their inhibitory effects on HepG2 liver cancer cells. Screening results revealed that two compounds, isocubein (3) and 4-(2-acetoxyethyl)phenol (7), exhibited strong inhibitory activity against cell proliferation, with IC values of 3.1±0.9 and 4.5±14 μM, respectively. Further analyses demonstrated that both compounds could suppress the formation and development of 3D tumorspheres in terms of quantity and size. Additionally, isocubein (3) and 4-(2-acetoxyethyl)phenol (7) exhibited the ability to inhibit the migration of HepG2 cells. This study represents the first report on the inhibitory activity against HepG2 liver cancer cells of extracts and isolated compounds from L. robustum, providing valuable information for future research aiming to develop products for liver cancer treatment.

摘要

许多女贞属植物已被证明含有具有抗癌生物活性的化合物。本研究旨在从粗壮女贞(Ligustrum robustum (Roxb.) Blume)的叶子中分离一些化合物,并评估它们对肝癌细胞的作用。结果,从该植物中共分离到 7 种先前报道的化合物(1-7),包括 4 种木脂素(1-4)和 3 种酚类衍生物(5-7)。这些化合物的结构通过光谱方法确定,并与报道的数据进行比较。所有分离物均评估了对 HepG2 肝癌细胞的抑制作用。筛选结果表明,两种化合物,异松柏脂素(3)和 4-(2-乙酰氧基乙基)苯酚(7)对细胞增殖具有很强的抑制活性,IC 值分别为 3.1±0.9 和 4.5±14 μM。进一步的分析表明,这两种化合物都可以在数量和大小方面抑制 3D 肿瘤球的形成和发展。此外,异松柏脂素(3)和 4-(2-乙酰氧基乙基)苯酚(7)还具有抑制 HepG2 细胞迁移的能力。本研究首次报道了粗壮女贞提取物和分离化合物对 HepG2 肝癌细胞的抑制活性,为未来开发肝癌治疗产品的研究提供了有价值的信息。

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