Differential activity of lipoic acid enantiorners in cell culture

Differential activity of lipoic acid enantiorners in cell culture
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DOI:
10.1080/j157v05n03_05
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发表时间:
2005-01-01
期刊:
Journal of Herbal Pharmacotherapy
影响因子:
--
通讯作者:
Parker, Keith K.
Parker, Keith K.
中科院分区:
其他
文献类型:
--
作者:
Smith, Jerry Robert;Thiagaraj, Harish V.;Parker, Keith K.

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目前尚不清楚硫辛酸 (LA) 的两种对映体形式 (R & S) 是否具有相似的药理活性,并且 LA 的确切细胞靶点尚未明确。我们对代表不同细胞类型的 3 个细胞培养系统进行氧化应激。线粒体代谢是主要终点。当 C6 神经胶质瘤被过氧化氢 (H2O2) 损伤时,所有形式的 LA 都会受到保护。外消旋和 S-LA 的效果不如 R 异构体,而 R 异构体对叔丁基过氧化氢 (TBHP) 损伤的 C6 神经胶质瘤也具有保护作用。 TBHP 对 PC12 细胞几乎没有造成损伤; R-LA 使线粒体代谢增加至未受损对照水平之上。在 H2O2 损伤的 PC 12 细胞中,R-LA 和外消旋 LA(但不是 S-LA)不仅可以防止损伤,而且可以使线粒体代谢增加到高于未损伤的对照水平。当BAE细胞被H2O2损伤时,R-和外消旋LA受到保护,而S-LA则无效。
It is Unclear whether the two enantiomeric forms (R & S) of lipoic acid (LA) share similar pharmacological activity and the exact cellular targets of LA are not well identified. We oxidatively stressed 3 cell Culture systems representing different cell types. Mitochondrial metabolism was the primary endpoint. When C6 glioma was damaged by hydrogen peroxide (H2O2), all forms of LA protected. Racemic and S-LA were less effective than the R-isomer that was also protective in tertiary butyl hydroperoxide (TBHP)-damaged C6 glioma. In PC12 cells, little damage was produced by TBHP; R-LA increased mitochondrial metabolism above the level of non-damaged control. In H2O2 damaged PC 12 cells, R-LA and racemic LA (but not S-LA) not only protected against damage, but increased mitochondrial metabolism above the non-damaged control level. When BAE cells were damaged with H2O2, R- and racemic LA protected while S-LA was ineffective.