Tetrahydropalmatine sulfate

Tissue pharmacokinetics is crucial for druggability assessment and plays a vital role in identifying the core bioactive components of traditional Chinese medicines (TCMs). This study aims to develop an integrated analytical approach combining ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) and desorption electrospray ionization-mass spectrometry imaging (DESI-MSI) to systematically characterize the temporal and spatial brain exposure profiles of Corydalis Decumbentis Rhizoma (CDR) in rats. Using UPLC-quadrupole time of flight mass spectrometry (UPLC-QTOF), a total of 35 drug-derived constituents were identified from rat brain after oral administration of CDR. Then, a rapid and sensitive UPLC-triple-stage quadrupole mass spectrometry (UPLC-TSQ) method was developed and validated for the quantification of 15 major alkaloids in rat brain tissue. The pharmacokinetic results indicated that most compounds reached peak concentrations within 4 h and were rapidly eliminated within 12 h. Tetrahydropalmatine and protopine exhibited notably high brain exposure levels (AUC_0-t > 100 ng·h·g⁻¹), suggesting their potential as key active constituents responsible for the anti-ischemic effects of CDR. DESI-MSI further revealed the spatial distribution of these compounds, with most alkaloids predominantly localized in the telencephalon. The spatial distribution of CDR constituents furnished a scientific basis for its traditional application against cerebral ischemic injury. This study provides a scientific basis for the anti-stroke effects of CDR and a reference for investigating the material basis of other TCMs.

Biling Weitong Granules (BLWTG) is a clinical formula employed for treating epigastric pain, yet its pharmacodynamic components and mechanisms against chronic gastric ulcers (GU) remain inadequately understood. The objective of this study was to investigate the targets and mechanisms of BLWTG and its bioactive components in chronic GU. Chronic GU model was induced in SD rats through acetic acid injection, and administered BLWTG post-induction. The macroscopic ulcer appearance, microscopic histology, mucosal growth, vascular promoting factors, myeloperoxidase, and inflammatory factors in gastric tissue were assessed. Network analysis was used to predict the potential core targets and pathways. Further, bioactive components were screened based on cell model, identified by HPLC-QTOF-MS and validated in vivo. The results showed that BLWTG effectively mitigated pathological damage, achieving a 63.32% ulcer healing rate. Network analysis and experimental verification showed that the effectiveness of BLWTG stemmed from its capacity lower oxidative stress and inflammation, boost antioxidant levels, and promote the synthesis of gastric mucosal protective factors and repair. Further, the primary active fraction of BLWTG was ethyl acetate fraction, which increased the ulcer healing rate to 75.04%. Among the 55 compounds identified in the ethyl acetate fraction of BLWTG, evodiamine, dehydroevodiamine, berberine and tetrahydropalmatine may represent the active components responsible for facilitating the regeneration and repair of GU. In conclusion, BLWTG and its bioactive components significantly promote healing in rat models of chronic GU, providing a scientific basis for further applications of BLWTG in treating chronic GU.