Simultaneous Quantification of Four Phenylethanoid Glycosides in Rat Plasma by UPLC-MS/MS and Its Application to a Pharmacokinetic Study of Acanthus Ilicifolius Herb

Abstract

Acanthus ilicifolius herb (AIH), the dry plant of Acanthus ilicifolius L., has long been used as a folk medicine for treating acute and chronic hepatitis. Phenylethanoid glycosides (PhGs) are one family of the main components in AIH with hepatoprotective, antioxidant, and anti-inflammatory activities. In this study, the pharmacokinetics of AIH was investigated preliminarily by ultra-performance liquid chromatography coupled with triple quadrupole mass spectrometry (UPLC-MS/MS). A simultaneously quantitative determination method for four PhGs (acteoside, isoacteoside, martynoside, and crenatoside) in rat plasma was first established by UPLC-MS/MS. These four PhGs were separated with an ACQUITY UPLC BEH C18 column (2.1 × 50 mm, 1.7 μm) by gradient elution (mobile phase: MeCN and 0.1% formic acid in water, 0.4 mL/min). The mass spectrometry detection was performed using negative electrospray ionization (ESI−) in multiple reaction monitoring (MRM) mode. By the established method, the preliminary pharmacokinetics of AIH was elucidated using the kinetic parameters of the four PhGs in rat plasma after intragastric administration of AIH ethanol extract. All four PhGs showed double peaks on concentration-time curves, approximately at 0.5 h and 6 h, respectively. Their elimination half-lives (t1/2) were different, ranging from 3.42 h to 8.99 h, although they shared similar molecular structures. This work may provide a basis for the elucidation of the pharmacokinetic characteristics of bioactive components from AIH.

Therapeutic potential of phenylethanoid glycosides: A systematic review

“…Although the four PhGs share similar molecular structures, they displayed different elimination half-lives (T 1/2 ), and different areas under the curves (AUC 0-t ), ranging from 3.4 to 9.0 h, and 1826.3 to 23.6 μg/L•h, respectively. 77 Different dosages and administrative patterns might affect the bioavailability of PhGs. However, there is one exception.…”

“…Zhang et al investigated the pharmacokinetic of four PhGs (verbascoside, isoverbascoside, martynoside, and crenatoside) after orally administrated 10.0 g crude Acanthus ilicifolius herb per kg to rats. Although the four PhGs share similar molecular structures, they displayed different elimination half‐lives ( T 1/2 ), and different areas under the curves (AUC 0–t ), ranging from 3.4 to 9.0 h, and 1826.3 to 23.6 μg/L·h, respectively 77 . Different dosages and administrative patterns might affect the bioavailability of PhGs.…”

Assessment of a developed HPLC-MS/MS approach for determining plasma eupatorin in rats and its application in pharmacokinetics analysis

“…The absorbed drug superimposed in the blood, and the double peak phenomenon of the drug-time curve appeared. 38,39 In Fig. 3 The concentration-time curve of plasma eupatorin in rats after single oral medication (50 mg kg À1 ).…”

Determination and Pharmacokinetic Profiles of Four Active Components From Scrophularia ningpoensis Hemsl. in Rats

“…Recently, an increasing number of analytical methods have been used to characterize and determine acteoside, angoroside C, harpagoside, and cinnamic acid in biological fluids ( Zhao et al, 2016 ; Feng et al, 2018 ; Zhang et al, 2018 ; Axmann et al, 2019 ; Guan et al, 2019 ; Zhang et al, 2019 ). These detection methods only determined one or two of the main bioactive ingredients of S. ningpoensis Hemsl.…”