Determination of swertianolin in rat plasma by LC‐MS/MS and its application to a pharmacokinetic study

Abstract

A sensitive and rapid LC-MS/MS method has been developed and validated for quantifying swertianolin in rat plasma using rutin as an internal standard (IS). Following liquid-liquid extraction with ethyl acetate, chromatographic separation for swertianolin was achieved on a C18 column with a gradient elution using 0.1% formic acid as mobile phase A and acetonitrile as mobile phase B at a flow rate of 0.3 mL/min. The detection was performed on a tandem mass spectrometer using multiple reaction monitoring via an electrospray ionization source and operating in the negative ionization mode. The optimized mass transition ion pairs (m/z) for quantitation were 435.1/272.0 for swertianolin and 609.2/300.1 for IS. The lower limit of quantitation was 0.5 ng/mL within a linear range of 0.5-500 ng/mL. Intra-day and inter-day precision was less than 6.8%. The accuracy was in the range of -13.9 to 12.0%. The mean recovery of swertianolin was >66.7%. The proposed method was successfully applied in evaluating the pharmacokinetics of swertianolin after an oral dose of 50 mg/kg Swertia mussotii extract in rats.

Determination and pharmacokinetic study of four xanthones in rat plasma after oral administration of Gentianella acuta extract by UHPLC–ESI–MS/MS

“…With T max at 0.27 h, norswertianolin was absorbed more rapidly than DMB (T max at 0.94 h), where T max of the former was roughly in conformity with the previous reference (He et al, 2014). As shown in Fig.…”

“…An appropriate internal standard will control for the variability in extraction, HPLC injection and ionization. Among several compounds being tested as the I.S., rutin (He et al 2014), bergamottin , butylparaben exhibited good response negative ionization mode of ESI. However, the polarity of the four xanthones, swertianolin, norswertianolin, bellidifolin and DMB, was too low for them to be eluted under the selected LC condition.…”

“…Wei et al (Wei et al, 2014) established a HPLC method to simultaneously determine three xanthone glycosides from G. acuta, and norswertianolin was also determined by HPLC (Wu et al, 2011). Furthermore, Han et al (Han et al, 2008) established a HPLC method to study pharmacokinetics of DMB in mice and He et al (He et al, 2014) determined swertianolin in rat plasma by LC-MS/MS and applicated to a pharmacokinetic study. However, there is no report on the method for the pharmacokinetic study of bellidifolin and norswertianolin.…”

Swertianolin ameliorates immune dysfunction in sepsis <em>via</em> blocking the immunosuppressive function of myeloid- derived suppressor cells

“…[40][41][42] Swertianolin, a natural product, showed to be a strong anticancer and antioxidant activities in both tumor and chronic infection experimental systems. [18][19][20][21][22][23] Therefore, we tested the hypothesis that swertianolin may affect MDSCs. In in vitro experiments, swertianolin reduced significantly the secretion of immunosuppressor factors (IL-10, NO, ROS, argininase).…”

“…19,20 Swertianolin, a xanthone glucoside isolated from the Swertia species, is one of the representative constituents of many Swertia species, and has been reported to possess antiinflammatory, hepatoprotective, antioxidant activity while improving the immune function. [21][22][23] CD34 + MDSCs were firstly described in cancer patients in 1995 as the main cause of immune escape and metastasis progression. Subsequently, MDSCs have been reported in the areas of inflammation, infectious diseases, especially chronic infections, and sepsis.…”