Abstract

Ginkgo leaf extract (GLE) is a popular herbal medicine and dietary supplement for the treatment of various diseases, including cardiovascular disease. GLE contains a variety of secondary plant metabolites, such as flavonoids and terpenoids, as active components. Some of these phytochemicals have been known to be metabolized by gut microbial enzymes. The aim of this study was to investigate the effects of the gut microbiota on the pharmacokinetics of the main constituents of GLE using antibacterial-treated mice. The bilobalide, ginkgolide A, ginkgolide B, ginkgolide C, isorhamnetin, kaempferol, and quercetin pharmacokinetic profiles of orally administered GLE (600 mg/kg), with or without ciprofloxacin pretreatment (150 mg/kg/day for 3 days), were determined. In the antibacterial-treated mice, the maximum plasma concentration (Cmax) and area under the curve (AUC) of isorhamnetin were significantly (p < 0.05) increased when compared with the control group. The Cmax and AUC of kaempferol and quercetin (other flavonol glycosides) were slightly higher than those of the control group, but the difference was not statistically significant, while both parameters for terpenoids of GLE showed no significant difference between the antibacterial-treated and control groups. These results showed that antibacterial consumption may increase the bioavailability of isorhamnetin by suppressing gut microbial metabolic activities.

Highlights

  • Herbal products contain a range of bioactive phytochemicals [1,2,3].The use of herbal products as dietary supplements has increased dramatically in recent years, and most are taken daily for the prevention and treatment of lifestyle-related chronic diseases [4,5,6,7,8,9]

  • That the gut microbiota may not influence the intestinal statistically. These results suggest that the gut microbiota maymetabolism not influenceand theabsorption intestinal of major terpene lactones in Ginkgo leaf extract (GLE)

  • The present study investigated the influence of the gut microbiota on the pharmacokinetics of

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Summary

Introduction

Herbal products contain a range of bioactive phytochemicals (e.g., polyphenols and terpenes) [1,2,3].The use of herbal products as dietary supplements has increased dramatically in recent years, and most are taken daily for the prevention and treatment of lifestyle-related chronic diseases [4,5,6,7,8,9]. Herbal products contain a range of bioactive phytochemicals (e.g., polyphenols and terpenes) [1,2,3]. Many research papers have demonstrated that the gut microbiota is involved in the biotransformation of natural active components such as flavonoids, saponins, phenylethanoid glycosides, and alkaloids, both in vitro and in vivo [12,13,14,15,16]. Such metabolic reactions by the gut microbiota may contribute to the activation or detoxification of phytochemicals. Orally administered Rb1 and baicalin are metabolized into ginsenoside Rd/compound K and baicalein, respectively, by gut microbiota [17,18,19,20]

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