Simultaneous determination of glaucocalyxin A and glaucocalyxin B in rat plasma by LC‐MS/MS and its application to a pharmacokinetic study after oral administration of Rabdosia japonica extract

Abstract

A specific and sensitive liquid chromatography tandem mass spectrometry (LC-MS/MS) method was developed and validated for the analysis of glaucocalyxin A and glaucocalyxin B in rat plasma using praeruptorin A as an internal standard. Separation was performed on a Hypurity C column (2.1 × 50 mm, 5 μm) with isocratic elution using 0.2% formic acid in water-acetonitrile (20:80, v/v). Mass spectrometric detection was conducted using selected reaction monitoring via an electrospray ionization source. Both analytes exhibited good linearity within their concentration ranges (r > 0.9932). The lower limit of quantitation of glaucocalyxin A and glaucocalyxin B was 1.10 ng/mL. Intra- and inter-day precision exhibited an RSD within 14.5%, and the accuracy (RE) ranged from -12.1 to 15.0% at the lower limit of quantitation and three quality control levels. The developed assay was successfully applied to a pharmacokinetic study of glaucocalyxin A and glaucocalyxin B in rats after oral administration of Rabdosia japonica extract.

A novel strategy for the characterization of glaucocalyxin A metabolites in vivo and in vitro by UHPLC-Q-TOF-MS based on DDA and DIA data acquisitions

“…14 The absorbance and elimination of GLA in rats were fast aer oral administration (T max ¼ 0.750 AE 0.224 h, t 1/2 ¼ 1.11 AE 0.17 h). 2 The excretion of GLA amounted to 23.8%, 12.8% and 35.68% in feces, urine, and bile within 12 h respectively. 15 These results indicated that GLA was fast metabolized and excreted mainly as metabolites.…”

“…Rats in groups 5 & 6 were collected blood samples from the orbital vein of the rats with heparinized tubes at 0.25, 0.5, 0.75, 1, 2, 4, 8, 12 and 24 h aer dosing. 2 Then all the blood samples were immediately centrifuged at 4500 rpm for 10 min under 4 C to obtain plasma. The same biological sample was mixed and then stored at À80 C.…”

“…1 For thousands of years, it has been used for the treatment of gastrointestinal oral infections. [2][3][4] Glaucocalyxin A (GLA), an ent-kauranoid diterpenoid, derives from the Rabdosia japonica plant. Diterpenoids, triterpenoids, and avonoids are the main components of the herb.…”

“…5 Moreover, GLA is the most active diterpenoid, acting as a quality index of this herb. 2 Nowadays, GLA has aroused widespread concern by scientists in various elds due to its multiple antitumor, [6][7][8][9][10] antibrotic, 11 anticoagulative, 12 antioxidant, 13 and anti-AD effects. 14 The absorbance and elimination of GLA in rats were fast aer oral administration (T max ¼ 0.750 AE 0.224 h, t 1/2 ¼ 1.11 AE 0.17 h).…”

Glycoproteins From Rabdosia japonica var. glaucocalyx Regulate Macrophage Polarization and Alleviate Lipopolysaccharide-Induced Acute Lung Injury in Mice via TLR4/NF-κB Pathway

“…Rabdosia genus is an important genus of the Labiatae family, with about 150 species worldwide ( Huang et al, 2018 ). Rabdosia japonica (Burm.…”