AI Article Synopsis
- NAD(P)H: quinone oxidoreductase1 (NQO1) is crucial for detoxifying toxic quinones, helping reduce cancer risks.
- The study found that three main compounds from Danshen (salvianolic acid B, lithospermic acid, and rosmarinic acid) could not induce NQO1 activity in liver cells due to poor absorption, despite effectively conjugating with glutathione.
- A methylation method improved the absorption and NQO1-inducing activities of these phenolic acids, maintaining their glutathione-conjugating abilities, with specific activity concentration values showing significant enhancement.
Article Abstract
NAD(P)H: quinone oxidoreductase1 (NQO1) is an important detoxification enzyme that can protect mammalian cells against toxic quinones and reduce the risk of tumorigenesis. In this study, it was found that salvianolic acid B (SaB), lithospermic acid (LA), and rosmarinic acid (RA), three main hydrophilic constituents in Danshen, conjugated with glutathione (GSH) easily in vitro but exhibited no NQO1-inducing activities in Hepa 1c1c7 cells, which might attribute to their poor absorptions. After a simple methylation strategy that aimed at improving the liposolubility, both the NQO1-inducing activities and the absorptions in cells of the phenolic acids improved obviously, without losing the GSH-conjugating abilities. The concentration to double the specific activity of NQ01 values of methylated products of lithospermic acid and rosmarinic acid were 17.86 ± 2.34 μg/mL and 11.97 ± 0.60 μg/mL, respectively. The findings indicated that methylation is an effective strategy to improve the NQO1-inducing activities of phenolic acids in Danshen.
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| http://dx.doi.org/10.1111/j.1747-0285.2011.01171.x | DOI Listing |
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