, a widely used Chinese herbal medicine, was considered as central nervous system (CNS) drug for years. Both ethanol extracts (EES) and water extracts (WES) of it were applied clinically. Unfortunately, the difference of their efficacy and even effective material foundation of remains obscure. In this study, to explore the active constituents of , we compared pharmacodynamics and chemical profiles / of EES/WES for the first time using multiple chemical analysis, pharmacological and data processing approaches. It was proved that there was no significant difference in the anti-depressive effects between WES and EES. However, the contents of most components and in plasma were higher in EES than those in WES, which was unconvincing for their similar efficacy. Therefore, we further explored components of targeted onto brain and the results showed that 5 lignans were identified with definite absorptivity respectively both in EES and WES caused by the limitation of blood-brain barrier. Moreover, bioinformatic analysis predicted their anti-depressive action. Above all, the systematic strategy screened 5 brain-targeted effective substances of and it was suggested that exploring the components into nidi would promote the studies on herbs effective material basis.

Depression is a major mood disorder. Abnormal expression of glial glutamate transporter-1 (GLT-1) is associated with depression. Schisantherin B (STB) is one bioactive of lignans isolated from Schisandra chinensis (Turcz.) Baill which has been commonly used as a traditional herbal medicine for thousands of years. This paper was designed to investigate the effects of STB on depressive mice induced by forced swimming test (FST). Additionally, we also assessed the impairment of FST on cognitive function in mice with different ages. FST and open field test (OFT) were used for assessing depressive symptoms, and Y-maze was used for evaluating cognition processes. Our study showed that STB acting as an antidepressant, which increased GLT-1 levels by promoting PI3K/AKT/mTOR pathway. Although the damage is reversible, short-term learning and memory impairment caused by FST test is more serious in the aged mice, and STB also exerts cognition improvement ability in the meanwhile. Our findings suggested that STB might be a promising therapeutic agent of depression by regulating the GLT-1 restoration as well as activating PI3K/AKT/mTOR pathway.
Animals ; Cognition ; Cognition Disorders ; Depression ; Glutamic Acid ; Herbal Medicine ; Learning ; Lignans ; Memory ; Mice ; Mood Disorders ; Physical Exertion ; Schisandra

Related substances in pharmaceutical formulations are associated with their safety, efficacy and stability. However, there is no overall study already published on the assessment of related substances in the Compound Ketoconazole and Clobetasol Propionate Cream. In this work, a reliable HPLC-TOF-MS qua-litative method was developed for the analysis of related substances in this preparation with a quick and easy extraction procedure. Besides the active pharmaceutical ingredients, two compounds named ke-toconazole impurity B′ optical isomer and ketoconazole impurity E were identified. Furthermore, a new HPLC method for qualitative and quantitative assessment on related substances and degradation pro-ducts, which were found in the stability test, was established and validated. The single standard to determine multi-components method was applied in the quantitative analysis, which was an effective way for reducing cost and improving accuracy. This study can provide a creative idea for routine analysis of quality control of the Compound Ketoconazole and Clobetasol Propionate Cream.

A sensitive, fast and comprehensive method for the quality assessment of Semen Ziziphi Spinosae (SZS) standard decoction with characterization of its chemical components was developed and validated. UPLC-Q/TOF-MS/MS system was used to identify thirty-six chemical components of SZS standard de-coction which included nucleosides, phenolic acids, alkaloids, and flavonoids. Furthermore, a UPLC-PDA method was validated to simultaneously determine adenosine, protocatechuic acid, magnoflorine, ca-techin, protocatechin, vicenin II, spinosin, kaempferol-3-rutinoside, and 6'''-feruloylspinosin which re-present four species of characteristic compounds. The qualitative method had been validated according to Chinese Pharmacopoeia (2015 edition) in terms of lineary, repeatability, recovery and stability for all analytes, with the results showing good precision, accuracy and stability. In conclusion, the method using UPLC combined with MS and PDA provided a novel way for the standardization and identification of SZS standard decoction, and also offered a basis for qualitative analysis and quality assessment of the pre-parations for SZS standard decoction.

Previous studies have shown that spinosin was implicated in the modulation of sedation and hypnosis, while its effects on learning and memory deficits were rarely reported. The aim of this study is to investigate the effects of spinosin on the improvement of cognitive impairment in model mice with Alzheimer’s disease (AD) induced by Aβ1–42 and determine the underlying mechanism. Spontaneous locomotion assessment and Morris water maze test were performed to investigate the impact of spinosin on behavioral activities, and the pathological changes were assayed by biochemical analyses and histological assay. After 7 days of intracerebroventricular (ICV) administration of spinosin (100 µg/kg/day), the cognitive impairment of mice induced by Aβ1–42 was significantly attenuated. Moreover, spinosin treatment effectively decreased the level of malondialdehyde (MDA) and Aβ1–42 accumulation in hippocampus. Aβ1–42 induced alterations in the expression of brain derived neurotrophic factor (BDNF) and B-cell lymphoma-2 (Bcl-2), as well as inflammatory response in brain were also reversed by spinosin treatment. These results indicated that the ameliorating effect of spinosin on cognitive impairment might be mediated through the regulation of oxidative stress, inflammatory process, apoptotic program and neurotrophic factor expression, suggesting that spinosin might be beneficial to treat learning and memory deficits in patients with AD via multi-targets.
Alzheimer Disease* ; Animals ; B-Lymphocytes ; Brain ; Brain-Derived Neurotrophic Factor ; Cognition Disorders ; Hippocampus ; Humans ; Hypnosis ; Learning* ; Locomotion ; Malondialdehyde ; Memory Disorders ; Memory* ; Mice* ; Neuroprotection ; Neuroprotective Agents* ; Oxidative Stress ; Water

OBJECTIVE： To establish a method for simultaneous determination of rutin， isoquercitrin， kaempferol-3-O- rutinoside， daunorubicin， quercetin and kaempferol in the roots of Tetrastigma hemsleyanum.  METHODS： HPLC method was adopted. The determination was performed on Alliance SilGreen C18 column with mobile phase consisted of 0.2％ phosphoric acid solution-acetonitrile solution （gradient elution） at the flow rate of 1.0 mL/min. The detection wavelength was 360 nm and the column temperature was at 35 ℃. The sample size was 15 μL. RESULTS： The linear range of rutin， isoquercitrin， kaempferol-3- O-rutinoside， daunorubicin， quercetin and kaempferol were 21.77-217.77， 12.37-123.75， 13.23-132.31， 4.63-46.30， 5.75-57.50， 3.36-33.66 μg/mL （all r＝0.999 9）， respectively. limit of detection of them were 0.217 8， 0.123 8， 0.066 2， 0.046 3， 0.191 7， 0.112 3 μg/mL， respectively. limit of quantitation of them were 0.435 6， 0.247 5， 0.165 4， 0.154 3， 0.575 0， 0.421 2 μg/mL， respectively. RSDs of precision （n＝6）， stability （24 h， n＝7） and reproducibility tests （n＝6） were lower than 3.20％. The average recoveries of them were 96.23％， 86.88％， 97.51％， 97.67％， 97.50％， 87.46％， RSDs were 1.85％， 1.90％， 1.84％， 1.87％， 1.25％， 2.01％ （n＝9）， respectively. CONCLUSIONS： The method is fast and simple， and could be applied for simultaneous determination of rutin， isoquercitrin， kaempferol-3-O-rutinoside， daunorubicin， quercetin and kaempferol in the roots of T. hemsleyanum.  

Larotaxel, a new taxane compound prepared by partial synthesis from 10-deacetyl baccatin Ⅲ, is active against tumors. In this research, a selective LC–MS method was developed and validated for the study of degradation kinetics of larotaxel, which was carried out in aqueous solutions with different pH (1.5, 3.0, 5.0, 6.5, 7.4, 9.0, 10 and 11.0) and temperature (0, 25, 37 and 45 °C). The linear range was 0.5–25μg/mL, the intra-and inter-day precisions were less than 7.0%, and accuracy ranged from 97.4–104.5% for each analyte. The observed rate obtained by measuring the remaining intact larotaxel was shown to follow first-order kinetics. The activation energies for degradation were 126.7 and 87.01 kJ/mol at pH 1.5 and 11, respectively. Although larotaxel was stable in pH 5, 6.5 and 7.4 buffers at 37 °C for 24 h during our study, increasing or decreasing the pH of the solutions would decrease its stabilities. Moreover, three main degradation products in alkaline condition were separated by HPLC and identified by Q–TOF–MS. The three degradation products were confirmed as 10-deacetyl larotaxel, 7, 8-cyclopropyl baccatin Ⅲ and 10-deacetyl-7, 8-cyclopropyl baccatin Ⅲ.

A simple, rapid and sensitive method based on an ultra-performance liquid chromatography–tandem mass spectrometry(UPLC–MS/MS)has been developed and validated for the determination of pimavanserin in rat plasma.The analyte was extracted by protein precipitation with methanol and separated on an ACQUITY BEH C18column(100 mm×2.1 mm,1.7μm;Waters,USA),with an isocratic elution of acetonitrile-water containing 10 mM ammonium acetate (70:30, v/v), at a flow rate of 0.2 mL/min for 2.5 min. The analyte and clarithromycin (the internal standard) were detected and quantified in positive ion mode using multiple reaction monitoring transitions at m/z 428.2 → 223.0 for pimavanserin and m/z 748.5 → 589.5 for clarithromycin. Relative coefficient (r) for the calibration curve was more than 0.9980. The intra-day and inter-day precisions(relative standard deviation,RSD%)were less than 13.3% and 10.5%,respectively,and the accuracy(relative error,RE%)was within ± 11.5%.The analytical method was successfully applied to a routine pharmacokinetic study of pimavanserin in rats after oral administration at the dose of 10 mg/kg.

A rapid, simple and practical high-performance liquid chromatography method coupled with diode array detector (HPLC–DAD) was developed to evaluate the quality of Alisma orientale (Sam.) Juz. through a simultaneous determination of four major active triterpenes using a single standard to determine the multi-components (SSDMCs). Alisol B 23-acetate was selected as the reference compound for calculating the relative response factors. All calibration curves showed good linearity (R240.9998) within test ranges. RSDs for intra- and inter-day of four analytes were less than 3.6% and 2.3%; the overall recovery was 92.1–110.2%(SSDMC). The proposed method was successfully applied to quantify the four components in 20 samples from different localities in China. Moreover, significant variations were demonstrated in the content of these compounds. In addition, hierarchical clustering analysis (HCA) and principal components analysis (PCA) were performed to differentiate and classify the samples based on the contents of Alisol C 23-acetate, Alisol A, Alisol A 24-acetate and Alisol B 23-acetate. This simple, rapid, low-cost and reliable HPLC–DAD method using SSDMC is suitable for routine quantitative analysis and quality control of A. orientale (Sam.) Juz.

In order to analyze main influencing factors of exportation of Chinese traditional patent medicines to the EU and measure the potentialities, the panel data of the exportation of Chinese traditional patent medicines to 13 countries in the EU over the period from 2000 to 2011 were used to build a regression model. Then, this model was applied to estimate the export potentialities. The results showed that the GDPs of China and EU countries, the export prices of Chinese traditional patent medicines, the port capacities of EU countries and maritime distances between ports of two countries notably promote export trade. At the same time, unified standards of pesticide residue analysis are associated with reducing the volume of export trade. EU countries can be divided into two groups. One is the group with certain potentiality. The other is the group without ready potentiality. Suggestions were made on basis of research results in order to promote exportation of Chinese traditional patent medicines to the EU.