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For the first time, we determined the phytochemical profile of alkaloids from N. officinalis using ultraperformance liquid chromatography-quadrupole-time-of-flight-tandem mass spectrometry (UPLC-Q-TOF-MS/MS).

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Background: Scutebarbatine A is a new neo-Clerodane Diterpenoid Alkaloids from Scutellaria barbata, which has many pharmacological effects, such as anti-tumor, antibacterial and anti-inflammatory. However, there are no studies on the metabolism of Scutebarbatine A. Objective: To explore the metabolism of Scutebarbatine A in the body, the bile, plasma, urine and feces samples of rats after administration were investigated. Methods: The biological samples were investigated by using ultra-high-performance liquid chromatography coupled with Q Exactive hybrid quadrupole-orbitrap high-resolution mass spectrometry (UPLC-Q-Orbitrap-HRMS). Results: A total of 20 metabolites were identified: 16 phase I metabolites and 4 phase II metabolites. The main metabolic pathways were hydrolysis, oxidation, hydrogenation, dehydration and combination with sulfate. Conclusion: This study further elucidates the metabolism of Scutebarbatine A in rats, and provides a reference for the study of its pharmacodynamic material basis and pharmacological mechanism.

3,4-Difluorobenzyl(1-ethyl-5-(4-((4-hydroxypiperidin-1-yl)-methyl)thiazol-2-yl)-1Hindol-3-yl)carbamate (NAI59), a small molecule with outstanding therapeutic effectiveness to anti-pulmonary fibrosis, was developed as an autotaxin inhibitor candidate compound. To evaluate the pharmacokinetics and plasma protein binding of NAI59, a UPLC-MS/MS method was developed to quantify NAI59 in plasma and phosphate-buffered saline. The calibration curve linearity ranged from 9.95 to 1990.00 ng/mL in plasma. The accuracy was À6.8 to 5.9%, and the intra-and interday precision was within 15%. The matrix effect and recovery, as well as dilution integrity, were within the criteria. The chromatographic and mass spectrometric conditions were also feasible to determine phosphate-buffered saline samples, and it has been proved that this method exhibits good precision and accuracy in the range of 9.95-497.50 ng/mL in phosphate-buffered saline. This study is the first to determine the pharmacokinetics, absolute bioavailability, and plasma protein binding of NAI59 in rats using this established method. Therefore, the pharmacokinetic profiles of NAI59 showed a dose-dependent relationship after oral administration, and the absolute bioavailability in rats was 6.3%. In addition, the results of protein binding showed that the combining capacity of NAI59 with plasma protein attained 90% and increased with the increase in drug concentration.