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芒果茎皮提取物和芒果苷对 HepG2 细胞的细胞保护作用的多参数评价。

Multiparametric evaluation of the cytoprotective effect of the Mangifera indica L. stem bark extract and mangiferin in HepG2 cells.

机构信息

Unidad de Hepatología Experimental, Centro de Investigación, Hospital La Fe, Valencia, Spain.

出版信息

J Pharm Pharmacol. 2013 Jul;65(7):1073-82. doi: 10.1111/jphp.12071. Epub 2013 Apr 26.

Abstract

OBJECTIVE

Mango (Mangifera indica L.) stem bark extract (MSBE) is a natural product with biological properties and mangiferin is the major component. This paper reported the evaluation of the protective effects of MSBE and mangiferin against the toxicity induced in HepG2 cells by tert-butyl hydroperoxide or amiodarone.

METHOD

Nuclear morphology, cell viability, intracellular calcium concentration and reactive oxygen species (ROS) production were measured by using a high-content screening multiparametric assay.

KEY FINDINGS

MSBE and mangiferin produced no toxicity below 500 mg/ml doses. A marked recovery in cell viability, which was reduced by the toxicants, was observed in cells pre-exposed to MSBE or mangiferin at 5-100 mg/ml doses. We also explored the possible interaction of both products over P-glycoprotein (P-gp). MSBE and mangiferin above 100 mg/ml inhibited the activity of P-gp in HepG2 cells.

CONCLUSIONS

MSBE and mangiferin showed cytoprotective effects of against oxidative damage and mitochondrial toxicity induced by xenobiotics to human hepatic cells but it seemed that other constituents of the extract could contribute to MSBE protective properties. In addition, the drug efflux should be taken into account because of the inhibition of the P-gp function observed in those cells exposed to both natural products.

摘要

目的

芒果(Mangifera indica L.)茎皮提取物(MSBE)是一种具有生物特性的天然产物,其主要成分为芒果苷。本文报道了 MSBE 和芒果苷对 tert-butyl hydroperoxide 或胺碘酮诱导 HepG2 细胞毒性的保护作用评价。

方法

采用高通量筛选多参数分析方法测定细胞核形态、细胞活力、细胞内钙离子浓度和活性氧(ROS)的产生。

主要发现

MSBE 和芒果苷在低于 500mg/ml 剂量下不产生毒性。在有毒物质存在下,用 5-100mg/ml 剂量的 MSBE 或芒果苷预先处理细胞,可显著恢复因毒物而降低的细胞活力。我们还探索了两种产品对 P-糖蛋白(P-gp)的可能相互作用。MSBE 和芒果苷在 100mg/ml 以上剂量抑制 HepG2 细胞中 P-gp 的活性。

结论

MSBE 和芒果苷对人肝细胞的氧化损伤和线粒体毒性具有细胞保护作用,但提取物的其他成分可能有助于 MSBE 的保护作用。此外,由于观察到暴露于这两种天然产物的细胞中 P-gp 功能受到抑制,因此应考虑药物外排。

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