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ETHNOPHARMACOLOGICAL RELEVANCE: 'Ershiwuwei Shanhu' pill (ESP), a classical and famous prescription of traditional Tibetan medicine, has a long history of empirical clinical use for the treatment of cerebrovascular and neurological diseases, but the absence of scientific evidence for its effect restricted its clinical application and further development.MATERIALS AND METHODS: The methodology of plasma pharmacochemistry was adopted to analyze the potentially bioactive components in ESP extracts. A method based on UPLC-DAD/Q-TOF-MS was established to identify herb components in ESP extracts and analyze the absorbed components of ESP and their metabolites in rat plasma, brain, heart, liver and kidney samples after oral administration of ESP extracts. RESULTS: A total of 61 herb components were detected and identified in ESP extracts, while 35 absorbed components-including 19 prototype compounds and 16 metabolites-were discovered as potentially bioactive components in rat plasma and tissues by comparative analysis of the UV and MS chromatograms of ESP extracts, blank biosamples and dosed biosamples. CONCLUSIONS: The potentially bioactive components of ESP extracts identified from rat plasma and tissues provide useful information for further study of the pharmacology and mechanism of action of ESP.

‘Ershiwuwei Shanhu’ pill (ESP), a classical and famous prescription of traditional Tibetan medicine, has a long history of empirical clinical use for the treatment of cerebrovascular and neurological diseases, but the absence of scientific evidence for its effect restricted its clinical application and further development. The methodology of plasma pharmacochemistry was adopted to analyze the potentially bioactive components in ESP extracts. A method based on UPLC-DAD/Q-TOF-MS was established to identify herb components in ESP extracts and analyze the absorbed components of ESP and their metabolites in rat plasma, brain, heart, liver and kidney samples after oral administration of ESP extracts. A total of 61 herb components were detected and identified in ESP extracts, while 35 absorbed components—including 19 prototype compounds and 16 metabolites—were discovered as potentially bioactive components in rat plasma and tissues by comparative analysis of the UV and MS chromatograms of ESP extracts, blank biosamples and dosed biosamples. The potentially bioactive components of ESP extracts identified from rat plasma and tissues provide useful information for further study of the pharmacology and mechanism of action of ESP.

Rannasangpei (RSNP) is used as a therapeutic agent in the treatment of cardiovascular diseases, neurological disorders, and neurodegeneration in China; however, its potential use in the treatment of vascular dementia (VD) was unclear. In this study, our aim was to examine the neuroprotective effect of RSNP in a VD rat model, which was induced by permanent bilateral common carotid artery occlusion (2VO). Four-week administration with two doses of RSNP was investigated in our study. Severe cognitive deficit in the VD model, which was confirmed in Morris water maze (MWM) test, was significantly restored by the administration of RSNP. ELISA revealed that the treatments with both doses of RSNP could reinstate the cholinergic activity in the VD animals by elevating the production of choline acetyltransferase (ChAT) and reducing the acetylcholinesterase (AChE); the treatment of RSNP could also reboot the level of superoxide dismutase (SOD) and decrease malondialdehyde (MDA). Moreover, Western blot and quantitative PCR (Q-PCR) results indicated that the RSNP could suppress the apoptosis in the hippocampus of the VD animals by increasing the expression ratio of B-cell lymphoma-2 (Bcl-2) to Bcl-2-associated X protein (Bax). These results suggested that RSNP might be a therapeutic agent in the treatment of vascular dementia in the future.