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研究蝙蝠葛诺林碱和呋甾醇呋哺烷醇酮的细胞毒性作用及其在 Caco-2 细胞中的体外生物利用度。

Study of the cytotoxic activity of beauvericin and fusaproliferin and bioavailability in vitro on Caco-2 cells.

机构信息

Laboratory of Food Chemistry and Toxicology, Faculty of Pharmacy, University of Valencia, Av Vicent Andrés Estellés s/n, 46100 Burjassot, Spain.

出版信息

Food Chem Toxicol. 2012 Jul;50(7):2356-61. doi: 10.1016/j.fct.2012.04.030. Epub 2012 Apr 25.

Abstract

Beauvericin (BEA) is a cyclohexadepsipeptide mycotoxin which has insecticidal properties and produces cytotoxic effects in mammalian cells. Fusaproliferin (FUS) is a mycotoxin that has toxic activity against brine shrimp, insect cells, and teratogenic effects on chicken embryos. The aim of this study was to determine the cytotoxicity of BEA and FUS in human epithelial colorectal adenocarcinoma HT-29 and Caco-2 cells, the transepithelial transport and the bioavailability using Caco-2 cells as a simulated in vitro gastrointestinal model of the human intestinal epithelium. The inhibitory concentration (IC(50)) evidenced by BEA in the Caco-2 cells was 24.6 and 12.7 μM at 24 and 48 h exposure, respectively, whereas the IC(50) values evidenced in HT-29 cells were 15.0 and 9.7 μM, respectively. FUS was cytotoxic, but no IC(50) data were observed in the range of concentration tested. BEA bioavailability was variable from 50.1% to 54.3%, whereas FUS presented a bioavailability variable from 80.2% to 83.2%. Results obtained demonstrated a potential risk for human health.

摘要

beauvericin (BEA) 是一种具有杀虫特性的环六肽真菌毒素,对哺乳动物细胞具有细胞毒性作用。 fusaproliferin (FUS) 是一种真菌毒素,对盐水虾、昆虫细胞具有毒性活性,并对鸡胚具有致畸作用。本研究旨在确定 BEA 和 FUS 在人上皮结肠直肠腺癌 HT-29 和 Caco-2 细胞中的细胞毒性,利用 Caco-2 细胞作为人肠道上皮的体外胃肠道模型,研究其跨上皮转运和生物利用度。在 24 和 48 h 暴露时,BEA 在 Caco-2 细胞中的抑制浓度 (IC50) 分别为 24.6 和 12.7 μM,而在 HT-29 细胞中的 IC50 值分别为 15.0 和 9.7 μM。FUS 具有细胞毒性,但在所测试的浓度范围内未观察到 IC50 数据。BEA 的生物利用度在 50.1%至 54.3%之间变化,而 FUS 的生物利用度在 80.2%至 83.2%之间变化。研究结果表明,这对人类健康存在潜在风险。

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