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绿蟾蜍毒液中的蟾毒内酯通过诱导细胞凋亡和细胞周期停滞对癌细胞发挥细胞毒性作用。

Bufadienolides from the Bufo viridis toad venom exert cytotoxic effects on cancer cells by inducing cell apoptosis and cell cycle arrest.

机构信息

State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, and the Key Laboratory of Chemistry of Plant Resources in Arid Regions Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, South Beijing Road 40-1, Urumqi 830011, People's Republic of China; University of Chinese Academy of Sciences, No.19(A) Yuquan Road, Shijingshan District, Beijing, 100049, People's Republic of China.

State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, and the Key Laboratory of Chemistry of Plant Resources in Arid Regions Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, South Beijing Road 40-1, Urumqi 830011, People's Republic of China.

出版信息

Toxicol In Vitro. 2023 Jun;89:105566. doi: 10.1016/j.tiv.2023.105566. Epub 2023 Feb 3.

DOI:10.1016/j.tiv.2023.105566
PMID:36738868
Abstract

A series of bufadienolides were isolated from the Bufo viridis toad venom, and their cytotoxic activities against three human cancer cell lines (HeLa, HT-29, MCF7) and a non-cancer cell line (L-O2) were explored using the MTT assay in vitro. All of nine compounds exhibited cytotoxic activities against the three cancer cell lines, with compound D4 exhibiting potent cytotoxic activity against HeLa cells and was better than positive control. Herein, we further evaluated the effect of compound D4 on HeLa cells. The results revealed that compound D4 has excellent cytotoxic effect on HeLa cells by inhibiting cell colony formation and migration, promoting cell apoptosis, increasing reactive oxygen species (ROS) levels and arresting of HeLa cells in S and G2/M phases. These findings encourage further work on the chemistry and bioactivity of the Bufo viridis toad venom.

摘要

从绿蟾蜍毒液中分离得到一系列蟾毒内酯,并通过 MTT 法体外研究了它们对三种人癌细胞系(HeLa、HT-29、MCF7)和一种非癌细胞系(L-O2)的细胞毒性。这 9 种化合物均对三种癌细胞系表现出细胞毒性,化合物 D4 对 HeLa 细胞表现出较强的细胞毒性,优于阳性对照。在此,我们进一步评估了化合物 D4 对 HeLa 细胞的影响。结果表明,化合物 D4 通过抑制细胞集落形成和迁移、促进细胞凋亡、增加活性氧(ROS)水平以及将 HeLa 细胞阻滞在 S 和 G2/M 期,对 HeLa 细胞具有极好的细胞毒性作用。这些发现鼓励对绿蟾蜍毒液的化学和生物活性进行进一步研究。

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