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Abstract: Ethnopharmacological relevance: Hypericum perforatum (St. John''s wort) is an important anti-depressant herb used in clinic and commonly prescribed for mild depression. Hyperoside is one of the major components of H. perforatum and is also detected in many plant species such as Abelmoschus manihot, Black Currant, Rosa agrestis, Apocynum venetum and Nelumbo nucifera. Aim of the study: As the hyperoside showed CNS (central nervous system) protective activity (e.g. anti-depressant-like effect), the possibility of hyperoside or its metabolites to reach CNS should be investigated. Moreover, the pharmacokinetics profile of hyperoside or its metabolites in rat brain should be studied for further elucidating the mechanism of hyperoside action on CNS. Material and Methods: A simple method for simultaneous determination of unbound hyperoside and its metabolite 3′-O-methyl-hyperoside in rat brain was developed by using ultra-high performance liquid chromatography coupled with tandem mass spectrometry (UPLC–MS/MS) and microdialysis technique. This method was applied for pharmacokinetics study of hyperoside and 3′-O-methyl-hyperoside in rat brain after intragastric (i.g.) and intraperitoneally (i.p.) administration of hyperoside in vivo. Results: Results showed that neither hyperoside nor its metabolites were detected in rat brain after i.g. administration but both compounds could be detected after i.p. administration. Considering the activity of hyperoside through both i.g. and i.p. administration, our results imply that the active components of hyperoside in vivo might be different. Therefore, further studies are needed to identify the active components of hyperoside in vivo through these two different routes. Moreover, non-oral administration route (e.g., i.p.) should be further investigated and be explored to obtain higher bioavailability and better activity for hyperoside. Our results also showed that the real existing form of hyperoside in rat brain were hyperoside and its methylated metabolite with maximum concentration to be 63.78ng/mL and 24.66ng/mL after 20mg/kg i.p. administration, respectively. Therefore, a more reasonable concentration of hyperoside should be considered in in vitro assay to reflect the real situation of hyperoside concentration in vivo. Conclusion: Due to the wide use of herbal remedies containing hyperoside, our investigation will contribute to further clarifying the action of this substance. Moreover, this method will be applied for clinical pharmacokinetics study of hyperoside and its metabolite as well as herbs that contain hyperoside. [Copyright &y& Elsevier]

Abstract: Aim of the study: This present study was carried out to evaluate the anti-inflammatory and analgesic effects of 85% ethanol extract (EE) of Commiphora myrrha and its different fractions partitioned with petroleum ether extract (EPE), ethyl acetate extract (EEA), n-butanol extract (EBu), and the water extract (ECY). Moreover, the chemical constituents in EPE were analyzed and identified by UPLC–QTOF/MS/MS. Materials and methods: The anti-inflammatory activities were investigated by utilizing the paw edema mice induced by formalin. In addition, we determined the levels of PGE2 in the edema paw. While the analgesic activity was examined against thermally and chemically induced nociceptive pain in mice, using the acetic acid and hot-plate test methods. The effects of the administration of dolantin or indomethacin were also studied for references. The components in EPE were analyzed by the ultra-performance liquid chromatography coupled with mass spectrum. Results: In the anti-inflammatory test, EE inhibited the development of paw swelling induced by formalin significantly. The pharmacological activities of the petroleum ether fraction (EPE) were stronger than the EE extract and other fractions at the dose of 100mg/kg, and furthermore significantly decreased the levels of inflammatory factor PGE2 in the edema paw tissue at the fourth hour after formalin injection. It has been also shown that the ethanol extract (EE) significantly reduced acetic acid-induced writhing response in mice at the dose of 200mg/kg, and 100mg/kg. The petroleum ether fraction (EPE) showed significant analgesic activity in the model at the dose of 100mg/kg (p <0.01), and the ethyl acetate fraction (EEA) exhibited less analgesic activity (p <0.05). All test samples showed no significant analgesic activity on the hot plate pain threshold in mice. The UPLC–MS/MS chromatogram analysis of EPE stated that EPE contains the ingredients of sesquiterpenes, diterpenes, and diterpenic acids. Moreover, seven main compounds were identified. Conclusion: These data demonstrated that the EE and EPE posses analgesic and anti-inflammatory activities and may support the fact the traditional application of this herb in treating various diseases associated with inflammatory pain. [Copyright &y& Elsevier]