Pharmacokinetics of tectorigenin, tectoridi, irigenin, and iridin in mouse blood after intravenous administration by UPLC-MS/MS

Abstract

Tectorigenin, tectoridin, irigenin, and iridin are the four most predominant compounds present in She Gan. She Gan has been used in traditional Chinese medicine because of its anti-inflammatory, hepatoprotective, anti-tumor, antioxidant, phytoestrogen-like properties. In this paper, a UPLC-MS/MS method was developed to measure the pharmacokinetics of tectorigenin, tectoridin, irigenin, iridin after intravenous administration in mice. A UPLC BEH C18 (50 mm × 2.1 mm, 1.7 μm particle size) chromatographic column was utilized for separation of the four target analytes and internal standard (IS), and the analysis of blood plasma samples; the mobile phase consisted of an acetonitrile-water (w/0.1% formic acid) gradient elution. Electron spray ionization (ESI) positive-ion mode and multiple reaction monitoring (MRM) mode was used for quantitative analysis of the analytes and internal standard. The four compounds were administered intravenously (sublingual) at doses of 5 mg/kg. After blood sampling, samples were processed and then analyzed by UPLC-MS/MS. The linearity of the method was robust over the concentration range of 2–5,000 ng/mL. The intra-day precision of the analysis was within 15%, the inter-day precision was within 12%, and the accuracy was between 92% and 110%. The recoveries were 65–68%, and the matrix effect was 93–109%. The established UPLC-MS/MS detection method was then successfully applied to study the pharmacokinetics of tectorigenin, tectoridin, irigenin, iridin in mice.

Tectorigenin: A Review of Its Sources, Pharmacology, Toxicity, and Pharmacokinetics

“…Another study indicated that oral administration of tectorigenin (80 mg/kg) resulted in a C max of 1.46 ± 0.30 µg/mL and AUC (0-t) of 7.31 ± 1.20 µg/mL × h [176]. Additionally, sublingual intravenous administration of tectorigenin (5 mg/kg) resulted in an AUC (0-t) of 219 ± 94 ng/mL × h [177]. Pharmacokinetic studies of some TCMs, such as Shejin-liyan Granule, extracts of Belamcandae Rhizoma and rhizome of Iris tectorum, also described the pharmacokinetic characteristics of tectorigenin as the main component [178][179][180].…”