Antifatigue Activity of Glycoprotein from Schisandra chinensis Functions by Reducing Oxidative Stress.

The glycoprotein from Schisandra chinensis was obtained with alkali extraction and acid precipitation, purified with DEAE Sepharose Fast Flow and Superdex G-75 column. The molecular composition structure and antifatigue activities of glycoprotein were studied. SCGP's molecular weight was approximately 10 KDa, and it consisted of a carbohydrate component (52.94%) and protein component (47.06%). SCGP comprised mannose, galactoside, rhamnose, glucose, galactose, xylose, arabinose, and fucose, its molar ratio was 2.14 : 1.43 : 1.59 : 8.17 : 8.99 : 3.18 : 18.51 : 1, and it contained 16 kinds of amino acids. SCGP could obviously extend the swimming time in mice by increasing LDH, SOD level, GSH-Px activity, and liver glycogen and decreasing the contents of BUN and MDA. The antioxidant activity of SCGP is a potential mechanism of its antifatigue effect. In vitro antioxidant test showed that SCGP scavenged DPPH and OH radicals in a dose-dependent manner (IC50 was 0.91 mg/ml and 0.72 mg/ml).

Safety assessment of concurrent statin treatment and evaluation of drug interactions in China.

OBJECTIVES: Acute muscle injury and potentially fatal rhabdomyolysis may occur with the use of statins and certain enzyme inhibitors, but data on this topic from China are quite limited. This study aimed to measure the concomitant exposure of patients to different statins and their enzyme inhibitors or interacting medications in 76 hospitals in six Chinese cities. METHODS: Prescription database was retrieved from Hospital Prescription Analysis Cooperation Project from January 2015 to December 2015, covering 76 tertiary facilities in six cities in China. Every evidence-based enzyme inhibitor was included, and labeled enzyme inhibitors and other relevant information were identified and obtained using the Drug Safety Update from the UK Medicines and Healthcare Products Regulatory Agency. The proportions of different statin types among all patients and those co-medicated with their inhibitors were examined. RESULTS: A total of 296,765 patients exposed to statins were included in this study. 80% of patients (n = 144,863, 80.5%) were concomitantly prescribed a CYP3A4-metabolized statin with an interacting drug during the study period. Among those prescribed a non-CYP3A4-metabolized statin, 40.0% of patients were concomitantly given an interacting drug, and approximately 20% of patients were concomitantly given a labeled inhibitor, predominantly calcium channel blockers, other statins, and fibrates. Rates of co-prescription were higher in patients aged over 65 years and in patients taking high-dose statins. CONCLUSION: Statins were frequently co-prescribed with metabolic inhibitors in China, where drug safety strategy on highlighting warnings and contraindications of statins are still lacking. For high-dose statins patients who are over 65 years and co-administered with any metabolic inhibitors, prescribers and pharmacists should be more concerned in order to prevent adverse drug reactions.

Preparative enrichment and separation of astragalosides from Radix Astragali extracts using macroporous resins.

The enrichment and separation of astragalosides I-IV (AGs I-IV) were studied on eight macroporous resins in the present study. SA-3 resin offered the best adsorption and desorption capacities for AGs I-IV than other resins. The models of adsorption kinetics were investigated in order to elucidate the mechanism of adsorption. The pseudo-second-order model was the better choice than the pseudo-first-order model to describe the adsorption behavior of AGs I-IV onto SA-3 resin. The equilibrium experimental data were well fitted to Langmuir and Freundlich isotherms. SA-3 resin adsorption chromatography tests were carried out to optimize the separation process of AGs I-IV from Radix Astragali extracts. With the optimum parameters for adsorption and desorption, the contents of AGs I-IV were 8.78-, 11.60-, 10.52- and 11.28-fold increased with the recovery yields being 65.88, 90.92, 84.25 and 94.17%, respectively. The preparative enrichment and separation of AGs I-IV from Radix Astragali extracts can be easily and effectively achieved by SA-3 resin adsorption chromatography. The developed methodology can also be referenced for the separation of other active constituents from herbal materials and manufacture of Radix Astragali products.

Enhanced extraction of astragalosides from Radix Astragali by negative pressure cavitation-accelerated enzyme pretreatment.

The optimal conditions for extraction of astragalosides III and IV (AGs III and IV) in Radix Astragali by negative pressure cavitation-accelerated enzyme pretreatment were studied on the basis of a Box-Behnken design and response surface methodology. Experimental results showed that negative pressure, amount of enzyme and incubation temperature were the main factors governing the enzyme pretreatment of Radix Astragali. The optimum parameters were obtained as follows: negative pressure -0.08 Mpa, amount of enzyme 1.48% (w/w of materials) and incubation temperature 45 degrees C. Under the optimal conditions, the maximal extraction yields of AGs III and IV were 0.103 and 0.325 mg/g, which were 41.67% and 65.31% increased as compared to those without enzyme pretreatment, respectively. The effect of negative pressure cavitation and enzyme pretreatment on the structural changes of plant cells was observed by scanning electron microscopy. In conclusion, negative pressure cavitation-accelerated enzyme pretreatment was proved to be environment-friendly and economical, and could be used in secondary metabolites production.

D(1)/D(2) receptor-targeting L-stepholidine, an active ingredient of the Chinese herb Stephonia, induces non-rapid eye movement sleep in mice.

L-stepholidine, an active ingredient of the Chinese herb Stephonia, is the first compound known to have mixed dopamine D(1) receptor agonist/D(2) antagonist properties and to be a potential treatment medication for schizophrenia. In schizophrenic patients insomnia is a common symptom and could be partly related to the presumed over-activity of the dopaminergic system. To elucidate whether stepholidine modulates sleep behaviors, we observed its effects on sleep-wake profiles in mice. The results showed that stepholidine administered i.p. at doses of 20, 40 or 80 mg/kg significantly shortened the sleep latency to non-rapid eye movement (non-REM, NREM) sleep, increased the amount of NREM sleep, and prolonged the duration of NREM sleep episodes, with a concomitant reduction in the amount of wakefulness. Stepholidine at doses of 40 and 80 mg/kg increased the number of state transitions from wakefulness to NREM sleep and subsequently from NREM sleep to wakefulness. However, stepholidine had no effect on either the amount of REM sleep or electroencephalogram power density of either NREM or REM sleep. Immunohistochemistry study showed that stepholidine dose-dependently increased c-Fos expression in neurons of the ventrolateral preoptic area, a sleep center in the anterior hypothalamus, as compared with the vehicle control. These results indicate that stepholidine initiates and maintains NREM sleep with activation of the sleep center in mice, suggesting its potential application for the treatment of insomnia.

[Studies on the constituents from the herba of Erigeron acer].

OBJECTIVE: To investigate the chemical constituents of the aerial part of Erigeron acer. METHODS: The chemical constituents were isolated by various columns and thin layer chromatographic methods. The structures were identified by spectral data. RESULTS: Five compounds were isolated and identified as alpha-amyrin (1), beta-amyrin (2), caffeic acid (3), quercetin (4), 4'-hydroxywogonin-7-O-beta-D-glucuronic acid glycoside (5). CONCLUSION: The five compounds are obtained from this plant for the first time. The signals of 13C-NMR of the compound(5) are reassigned by means of DEPT, HMQC, HMBC, the signals of 1H-NMR of 2" - 5"-H of the glucuronic acid moiety are assigned by means of HMBC, HMQC, 1H-1H COSY for the first time.

[Isolation and structure identification of flavonol glycoside from Lysimachia christinae Hance].

AIM: To isolate and prepare chemical standards. METHODS: Flavonol glycoside and rhamnonic acid gamma-lactone were isolated from whole plants of Lysimachia christinae Hance. with 95% ethanol and purified by silica gel column chromatography. UV, IR, MS, 1HNMR, 13CNMR, DEPT, HMQC, HMBC were used for the structural identification. RESULTS: Two compounds were obtained. They were identified as rhamnonic acid gamma-lactone (I) and kaempferol-3-O-alpha-L-rhamnosyl (1-->2)-beta-D-xyloside (II). CONCLUSION: Compound I was isolated from this genus for the first time. Compound II is a new compound named as lysimachiin.