Pharmacokinetics of gallic acid and protocatechuic acid in humans after dosing with Relinqing (RLQ) and the potential for RLQ-perpetrated drug–drug interactions on organic anion transporter (OAT) 1/3

Abstract

2021) Pharmacokinetics of gallic acid and protocatechuic acid in humans after dosing with Relinqing (RLQ) and the potential for RLQperpetrated drug-drug interactions on organic anion transporter (OAT) 1

Pharmacokinetic herb-drug interactions: Altered systemic exposure and tissue distribution of ciprofloxacin, a substrate of multiple transporters, after combined treatment with Polygonum capitatum Buch.-Ham. ex D. Don extracts

“…Considering the relative exposure characteristics, GA and PCA were selected as PK-marker and Q-marker components of PCE in previous studies ( Ma et al, 2015 ; Ma et al, 2016 ; Li et al, 2021b ). In this study, we investigated the concentration-dependent inhibitions of GA and PCA on multiple transporters, including OAT1, OAT3, OCT2, MDR1, and BCRP.…”

“…Cells were cultured at 37°C in an atmosphere of 5% CO 2 . The inhibition experiments were adapted from previous methods with minor modifications ( Li et al, 2021a ; 2021b ).…”

“…Gallic acid (GA) and protocatechuic acid (PCA) were identified as appropriate pharmacokinetic markers (PK-markers) of P. capitatum because of their extensive pharmacological activities, high systemic exposures, and acceptable pharmacokinetic properties. Specifically, they are the two most abundant phenolic acids in P. capitatum ( Liao et al, 2013 ; Zhang et al, 2013a ; Zhang et al, 2013b ; Li et al, 2021b ), and their anti-microbial, anti-inflammatory, anti-oxidant, and analgesic activities associated with P. capitatum efficacy ( Liao et al, 2011 ; Khan et al, 2015 ; Choubey et al, 2018 ; Song et al, 2020 ; Bai et al, 2021 ). The qualitative and quantitative analysis of PCE systemic exposure showed that GA and PCA possess a relatively high exposure in rats ( Ma et al, 2015 , 2016 ; Huang et al, 2019 ; Guan et al, 2022 ) and humans ( Li et al, 2021b ).…”

“…Specifically, they are the two most abundant phenolic acids in P. capitatum ( Liao et al, 2013 ; Zhang et al, 2013a ; Zhang et al, 2013b ; Li et al, 2021b ), and their anti-microbial, anti-inflammatory, anti-oxidant, and analgesic activities associated with P. capitatum efficacy ( Liao et al, 2011 ; Khan et al, 2015 ; Choubey et al, 2018 ; Song et al, 2020 ; Bai et al, 2021 ). The qualitative and quantitative analysis of PCE systemic exposure showed that GA and PCA possess a relatively high exposure in rats ( Ma et al, 2015 , 2016 ; Huang et al, 2019 ; Guan et al, 2022 ) and humans ( Li et al, 2021b ). After oral administration of PCE, GA and PCA underwent a rapid absorption ( Ma et al, 2015 ; Li et al, 2021b ), a dose-dependent profile ( Ma et al, 2015 ), and a relatively targeted distribution in kidney tissue ( Ma et al, 2016 ).…”

“…The qualitative and quantitative analysis of PCE systemic exposure showed that GA and PCA possess a relatively high exposure in rats ( Ma et al, 2015 , 2016 ; Huang et al, 2019 ; Guan et al, 2022 ) and humans ( Li et al, 2021b ). After oral administration of PCE, GA and PCA underwent a rapid absorption ( Ma et al, 2015 ; Li et al, 2021b ), a dose-dependent profile ( Ma et al, 2015 ), and a relatively targeted distribution in kidney tissue ( Ma et al, 2016 ). Consequently, GA and PCA were chosen as PCE tracer components in the pharmacokinetic- and tissue distribution-based HDIs studies.…”