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

Abstract

Acteoside, angoroside C, harpagoside, and cinnamic acid, which are the main bioactive ingredients of Scrophularia ningpoensis Hemsl., have wide clinical use with various biological effects. A new and sensitive ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was established with taxifolin as the internal standard (IS) in this study and was successfully used to study the pharmacokinetic profiles of four active components from S. ningpoensis Hemsl. in rats after sublingual intravenous administration. After protein precipitation with acetonitrile, the mobile phase (consisting of acetonitrile and 0.1% formic acid) was used to separate the analytes on an Acquity UPLC BEH C18 chromatography column (2.1 × 50 mm, 1.7 μm) under gradient elution. The precursor-to-product ion transitions of 623.4 → 161.3 m/z for acteoside, 783.5 → 175.0 m/z for angoroside C, 493.3 → 345.2 m/z for harpagoside and 147.2 → 103.4 m/z for cinnamic acid were monitored by mass spectrometry with negative electrospray ionization in the multiple reaction monitoring (MRM) mode. The concentration range of 10–1,000 ng/ml could be detected by this method with a lower limit of quantification (LLOQ) of 10 ng/ml for each analyte. The intra- and inter-day precision (RSD%) of the method ranged from 2.6 to 9.9% and 2.7–11.5%, respectively. Meanwhile, the accuracy (RE%) was −9.6–10.7% in this developed method. The mean recoveries of four active components from S. ningpoensis Hemsl. were more than 76.7% with negligible matrix effects. The four active components from S. ningpoensis Hemsl. were stable under multiple storage and process conditions. A new, sensitive and simple analytical method had been established and was successfully applied to the pharmacokinetic profiles of four active components from S. ningpoensis Hemsl. in rats after sublingual intravenous administration.

Pharmacokinetic Analysis of Diosgenin in Rat Plasma by a UPLC-MS/MS Approach

“…In contrast, the isocratic elution resulted in a more stable signal, although the peaks showed trailing without formic acid. In a previous study, formic acid enhanced the ion signal and achieved better resolution and sharper peaks [ 40 ]. Finally, we selected isocratic elution with acetonitrile-water (including 0.3% formic acid) at a ratio of 80 : 20 (v/v), with a separation time of only 5 min (including separation, column cleaning, and equilibration time) as the optimal conditions.…”

Molecular Insights into the Macrophage Immunomodulatory Effects of Scrophulariae Radix Polysaccharides

“…As shown in Figure 5, all SRPs fractions promoted the NO release from RAW264.7 macrophages, and the highest contents of NO were found in SRPs100 groups. 1Mannose, 2 Ribose, 3 Rhamnose, 4 Glucuronic acid, 5 Galacturonic acid, 6 Glucose, 7 Galactose, 8 Xylose, 9 Arabinose, 10 Fucose)…”

“…Modern pharmacological studies have isolated and identified numerous compounds from SR, including iridoids, phenolic glycosides, phenolic acids, alkaloids, flavonoids, triterpenes, volatile oils and other ingredients. [8,9] Recently, polysaccharides from SR (SRPs) were observed to have neuroprotective effects on cerebral ischemia/reperfusin injury (CIRI) rats. [10] The anti-oxidant and anti-inflammatory activities of SRPs were also evaluated and confirmed by radical scavenging assay and LPS-induced inflammation model.…”

Effect of Different Processing Methods on the Chemical Constituents of Scrophulariae Radix as Revealed by 2D NMR-Based Metabolomics

“…(Scrophulariaceae), was first recorded in the earliest Chinese medicinal classic, Shennong’s Materia Medica [ 1 , 2 , 3 ]. It has been used to treat rheumatism, pharyngalgia, arthritis, neuritis, constipation, conjunctival congestion, and diabetes [ 4 , 5 , 6 , 7 ] due to its excellent traditional therapeutic effects on “cooling blood”, “nourishing yin”, and “purging fire” for removing toxins [ 1 , 8 ]. In the last decades, SR has been extensively investigated and shown to contain iridoid glycosides, phenylpropanoid glycosides, organic acids, and triterpenes [ 1 , 8 , 9 ].…”