Abstract

To determine the effect of Rooibos (Aspalathus linearis) on glucocorticoid biosynthesis and inactivation in vivo and in vitro. Ultra-performance liquid chromatography/tandem mass spectrometry (UPLC-MS/MS) analyses of in vivo studies showed that human Rooibos consumption increased cortisone plasma levels in males (p = 0.0465) and reduced cortisol:cortisone ratios in males and females (p = 0.0486) at risk for cardiovascular disease. In rats, corticosterone (CORT) (p = 0.0275) and deoxycorticosterone (p = 0.0298) levels as well as the CORT:testosterone ratio (p = 0.0009) decreased following Rooibos consumption. The inactivation of cortisol was investigated in vitro by expressing 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and type 2 (11βHSD2) in CHO-K1 cells. Rooibos inhibited 11βHSD1, which resulted in a significant reduction in the cortisol:cortisone ratio (p < 0.01). No significant effect was detected on 11βHSD2. In vitro studies in adrenal H295R cells showed that Rooibos and rutin, one of the more stable flavonoid compounds present in Rooibos, significantly reduced the levels of cortisol and CORT in cells stimulated with forskolin to mimic a stress response. In vivo studies demonstrate that Rooibos significantly decreased glucocorticoid levels in rats and steroid metabolite ratios linked to metabolic disorders--cortisol:cortisone in humans and CORT:testosterone in rats. Results obtained at cellular level elucidate possible mechanisms by which these effects were achieved.

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