Microsomal pre‐receptor cortisol production is inhibited by resveratrol and epigallocatechin gallate through different mechanisms

Abstract

Local activation of cortisol in hormone target tissues is a major determinant of glucocorticoid effect. Disorders in this peripheral cortisol metabolism play an important role in the development of metabolic diseases, such as obesity or type 2 diabetes mellitus. Hence, dietary factors influencing the activity of the involved enzymes can have major impacts on the risk of the above diseases. Resveratrol and epigallocatechin gallate (EGCG), two natural polyphenols found in several nutriments and in green tea, respectively, are well‐known for their antiobesity and antidiabetic activities. EGCG has been shown to interfere with microsomal cortisol production through decreasing the luminal NADPH:NADP+ ratio. The aim of this study was to clarify if resveratrol also induces such a redox shift or causes any direct enzyme inhibition that influences local cortisol production. Cortisone–cortisol conversions and changes in NADPH levels were monitored in rat liver microsomal vesicles. Cortisol production was inhibited by resveratrol in a concentration dependent manner while the intrinsic reducing and oxidizing capacity as well as the NADPH level inside the ER‐derived vesicles remained unaffected. Activity measurements performed in permeabilized microsomes confirmed that resveratrol, unlike EGCG, inhibits 11β‐hydroxysteroid dehydrogenase type 1 directly. Long‐term moderation of pre‐receptor cortisol production likely contributes to the beneficial health effects of both polyphenols. © 2018 BioFactors, 45(2):236–243, 2019

The Bioprotective Effects of Polyphenols on Metabolic Syndrome against Oxidative Stress: Evidences and Perspectives

“…RSV was shown to suppress NOX activity, including an O-methylation group, a 4′-OH group, and an extra -OH group. RSV was confirmed to inhibit 11 β -hydroxysteroid dehydrogenase type 1 directly by decreasing cortisol production [95]. With supplementation of anthocyanins, both mRNA and protein level of XOD as well as XOD activity in the serum and liver were inhibited significantly in a dose-dependent manner [64].…”

The Mechanism of Kelulut Honey in Reversing Metabolic Changes in Rats Fed with High-Carbohydrate High-Fat Diet

“…Naringin has been found to suppress metabolic features and improve the number of functional β cells in rats [ 30 , 31 ]. Epigallocatechin gallate (EGCG) could inhibit 11βHSD1 activity and reduce cortisol levels [ 32 , 33 ], improve metabolic features and insulin sensitivity in animals [ 34 ], and renal histology [ 35 , 36 , 37 ]. p -coumaric acid could inhibit insulin resistance and increase adiponectin levels [ 38 , 39 ] Therefore, it is likely that phenolic compounds contained within KH contribute to the inhibition of MetS risk demonstrated in this study.…”

Resveratrol, novel application by preconditioning to attenuate myocardial ischemia/reperfusion injury in mice through regulate AMPK pathway and autophagy level

“…With the in‐depth study of RSV, research's shown that RSV has a wide range of pharmacological actions. Such as, anti‐oxidation, 6 anti‐cardiovascular disease, 7 liver protection, 8 anti‐cancer, 9 antibacterial, 10 anti‐inflammatory 11 and anti‐aging. 12 …”

“…With the in-depth study of RSV, research's shown that RSV has a wide range of pharmacological actions. Such as, anti-oxidation, 6 anti-cardiovascular disease, 7 liver protection, 8 anti-cancer, 9 antibacterial, 10 anti-inflammatory 11 and anti-aging. 12 Recent studies have pointed out that silent information regulator of transcription 1 (SIRT1) acts as pre-sensor of body energy metabolism, targeting histones, co-regulatory molecules, and metabolic enzymes to regulate gene expression and metabolic activity, thus reflecting the energy state of the cells.…”