JPET #172338 1 Human Pregnane X Receptor Agonism by Ginkgo biloba Extract: Assessment of the Role of Individual Ginkgolides
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Human pregnane X receptor agonism by Ginkgo biloba extract: assessment of the role of individual ginkgolides.
Ginkgo biloba extract activates pregnane X receptor (PXR), but how this occurs is not known. Therefore, we investigated the mechanism of PXR activation by the extract and the role of five individual terpene trilactones in the activation. In a cell-based reporter gene assay, G. biloba extract activated human PXR (hPXR), and at a concentration present in the extract, ginkgolide A, but not ginkgol...
متن کاملSelective agonism of human pregnane X receptor by individual ginkgolides.
Ginkgolide A, ginkgolide B, ginkgolide C, and ginkgolide J are structurally related terpene trilactones present in Ginkgo biloba extract. Pregnane X receptor (PXR), glucocorticoid receptor (GR), and constitutive androstane receptor (CAR) regulate the expression of genes involved in diverse biological functions. In the present study, we investigated the effects of individual ginkgolides as singl...
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Naturally occurring splice variants of human constitutive androstane receptor (hCAR) exist, including hCAR-SV23 (insertion of amino acids SPTV), hCAR-SV24 (APYLT), and hCAR-SV25 (SPTV and APYLT). An extract of Ginkgo biloba was reported to activate hCAR-SV24 and the wild type (hCAR-WT). However, it is not known whether it selectively affects hCAR splice variants, how it activates hCAR isoforms,...
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Introduction: Many people with amnesia would like to try herbal therapies. Ginkgo biloba is one of the most popular herbs which is used to treat amnesia. The beneficial effects of this plant, however, has not been scientifically assessed yet. Although, there have been some reports on the memory enhancement effect of Ginkgo biloba, the mechanism of its action is not yet explained well. Consi...
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Pregnane X receptor (PXR; NR1I2) is a ligand-activated transcription factor that plays a role not only in drug metabolism and transport but also in various other biological processes. Ginkgo biloba is a herbal medicine commonly used to manage memory impairment. Treatment of primary cultures of rat hepatocytes with G. biloba extract increases the mRNA expression of CYP3A23, which is a target gen...
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