Exploring the key anti-fatigue components of American ginseng based on metabolomics and zebrafish models / 药学学报

The aim of this paper is to explore the key anti-fatigue active components in the saponin-like composition of American ginseng. The anti-fatigue activity of western ginseng samples was evaluated using a zebrafish model; metabolomics techniques were used to identify the main saponins in western ginseng from different origins; the active substances and relevant targets of the anti-fatigue effect of western ginseng were initially screened by constructing a PPI protein interaction network between western ginseng saponins and disease targets, and the key active ingredients were screened using a molecular docking method; finally, the anti-fatigue activity of the key active ingredients was evaluated using a zebrafish, animal experiment was approved by the Ethics Committee of Shandong Academy of Medical Sciences (SYXK20220005). The anti-fatigue activity of the key active ingredients was evaluated using a zebrafish model. The results of the zebrafish activity evaluation showed that there were significant differences in the activities of the western ginseng samples from the two origins, and a total of 10 different saponins were identified as possibly related to the anti-fatigue activity after further metabolomic testing and pattern discrimination. The core anti-fatigue targets were screened with the help of component-disease target PPI, combined with pharmacophore-like parameters and molecular docking techniques, and pseudoginsenoside F11 was found to have good binding activity to five of the targets. Finally, the zebrafish model revealed that pseudoginsenoside F11 exhibited significant anti-fatigue activity. This study used metabolomics and zebrafish model to screen the key active substances of pseudoginsenoside F11 for its anti-fatigue activity, which will provide a reference for further research on the anti-fatigue of pseudoginsenosides.

Characterization of the anti-fatigue effect of Astragali Radix from the Shanxi Hengshan area and its association with taurine metabolism based on 1H NMR metabolomic technology combined with network pharmacology / 药学学报

The objective of this work was to evaluate the anti-fatigue efficacy of Astragali Radix (AR) from the Shanxi Hengshan area and to reveal possible mechanisms by which it relieves fatigue. Efficacy differences between Guangling (GL) and Hunyuan (HY) AR preparations were compared and evaluated, and an 1H NMR metabolomic technique combined with statistical methods was used to identify the metabolites in different groups of mouse gastrocnemius muscle tissues. The differential metabolites after AR treatments were identified according to VIP and P values and the upstream targets were predicted with the help of Metscape. Cytoscape software was utilized to construct a network map of AR potential anti-fatigue targets. Key differential metabolites were identified based on shared targets and entered into the Metaboanalyst website for pathway enrichment analysis, which led to the preliminary elucidation of the molecular mechanisms. The results showed that intervention with AR can significantly improve the swimming-to-exhaustion time, increase liver glycogen, and reduce urea-nitrogen levels in mice. The difference between GL and HY ARs was relatively small, indicating that the quality of AR produced in the Hengshan area is consistent and stable. The metabolic fingerprints of mouse gastrocnemius muscle tissue extracts were composed of 34 metabolites, and the statistical results showed that 19 differential metabolites were significantly reversed after the Hengshan AR intervention. We found that the anti-fatigue effects of AR in the Shanxi Hengshan area were mainly associated with taurine and hypotaurine metabolism through regulation of GAD1, based on network pharmacological analysis. In conclusion, 1H NMR metabolomic techniques were combined with network pharmacology to compare and evaluate the quality of Hengshan ARs, and further associate the fatigue relieve with the regulation of taurine metabolism. This provides a theoretical basis for the resource utilization of Hengshan ARs and the development of anti-fatigue-related products. The animal experiments in this study followed the regulations of the Animal Ethics Committee of Shanxi University and passed the ethical review of animal experiments (Approval No. SXULL2021028).

Anti-fatigue effect of Lubian on kidney Yin deficiency and kidney Yang deficiency mice and mechanism based on PI3K-Akt pathway / 中国中药杂志

This study aimed to investigate the anti-fatigue effect and mechanism of Lubian(Cervi Penis et Testis) on kidney Yin deficiency and kidney Yang deficiency mice. After one week of adaptive feeding, 88 healthy male Kunming mice were randomly divided into a blank group, a kidney Yin deficiency model group, a kidney Yin deficiency-Panacis Quinquefolii Radix(PQR) group, kidney Yin deficiency-Lubian treatment groups, a kidney Yang deficiency model group, a kidney Yang deficiency-Ginseng Radix et Rhizoma(GR) group, and kidney Yang deficiency-Lubian treatment groups, with eight mice in each group. The kidney Yin deficiency model and kidney Yang deficiency model were prepared by daily regular oral administration of dexamethasone acetate and hydrocortisone, respectively, and meanwhile, corresponding drugs were provided. The mice in the blank group received blank reagent. The treatment lasted 14 days. The exhaustive swimming time was measured 30 min after drug administration on the 14th day. On the 15th day, blood was collected from eyeballs and the serum was separated to determine the content of lactic acid(LD), blood urea nitrogen(BUN), lactate dehydrogenase(LDH), cyclic adenosine monophosphate(cAMP), and cyclic guanosine monophosphate(cGMP). The liver was dissected to determine the content of liver glycogen and the protein expression of phosphoinositide 3-kinase(PI3K) and protein kinase B(Akt). Compared with the kidney Yang deficiency model group, the kidney Yang deficiency-Lubian treatment groups showed increased body weight(P<0.05), relieved symptoms of Yang deficiency, decreased cGMP content(P<0.01), increased cAMP/cGMP(P<0.01), prolonged exhausted swimming time(P<0.01), reduced LD(P<0.01), elevated BUN content(P<0.01), increased liver glycogen content(P<0.01), and increased protein expression of PI3K and Akt in the liver(P<0.05). Compared with the kidney Yin deficiency model group, the kidney Yin deficiency-Lubian treatment groups showed increased body weight(P<0.01), relieved symptoms of Yin deficiency, increased content of cGMP(P<0.01), decreased cAMP/cGMP(P<0.01), prolonged exhausted swimming time(P<0.01), decreased LD(P<0.01), decreased BUN content(P<0.01), increased liver glycogen content(P<0.01), and increased protein expression of PI3K(P<0.05) and Akt in the liver(P<0.05). To sum up, Lubian can regulate Yin deficiency and Yang deficiency and increase glycogen synthesis by affecting the PI3K-Akt pathway, thereby exerting an anti-fatigue role.

Preparation of Baoyuan Chewable Tablets and Evaluation of Its Anti-fatigue Effect / 中国实验方剂学杂志

ObjectiveTo screen the preparation technology of Baoyuan chewable tablets and to preliminarily elucidate its anti-fatigue effect and mechanism. MethodTaking encapsulation rate of volatile oil， extract rate and extraction rate of active ingredients as indexes， single factor test and orthogonal test were used to optimize the volatile oil inclusion， aqueous decoction and formulation molding processes of Baoyuan chewable tablets. ICR rats were randomly divided into the blank group， model group， Gaoshan Hongjingtian oral liquids group（6.01 mL·kg-1） and and Baoyuan chewable tablets low， medium， and high dose groups（2.1， 4.2， 8.4 g·kg-1）， 8 mice in each group， and were administered by gastric gavage at the corresponding dose once a day， the blank and model groups were given equal volume of saline for 15 d. After the last administration for 30 min， the mice were loaded with 5% of the body mass of lead at the tail and swam until exhaustion to establish the fatigue model， and the weighted swimming time of the mice in each group was recorded， meanwhile， the muscle tissues of the mice were sliced， stained by hematoxylin-eosin（HE） and subjected to pathological observation， and the levels of blood urea nitrogen（BUN）， lactic acid（LA）， liver glycogen（LG）， activities of lactate dehydrogenase（LDH） and creatine kinase（CK） in the serum were determined. ResultThe optimal inclusion process of cinnamon oil in Baoyuan chewable tablets was 10∶1 for β-cyclodextrin-volatile oil， and inclusion at 50 ℃ for 2 h with saturated aqueous solution method. The optimal water extraction process was to extract twice， adding 10 times of water to extract for 50 min for the first time， and adding 9 times of water to extract for 40 min for the second time. The ratio of the extract of Baoyuan chewable tablets with microcrystalline cellulose， maltodextrin， mannitol， citric acid， magnesium stearate was 63∶13∶8∶17∶17∶1∶1， the tablets were pressed by wet granulation， the each tablet weight was 1.2 g， and the hardness was 60-80 N. Compared with the model group， Baoyuan chewable tablets low， medium， and high dose groups could significantly prolong the exhaustion time of mice in weight bearing swimming（P<0.05， P<0.01）， and improve the exercise endurance of the body， and the results of HE staining showed that all dose groups of Baoyuan chewable tablets could significantly improve the muscle tissue damage caused by exercise， significantly reduce the levels of BUN， LA and the activities of LDH and CK in serum（P<0.01）， and significantly increase the content of LG（P<0.05， P<0.01）. ConclusionThe optimized preparation process of Baoyuan chewable tablets is stable and feasible， and the preparation can improve exercise endurance by increasing the LG level in liver tissue， and relieve muscle soreness by accelerating the removal of LA from the body， and reduce CK and LDH activities to exert anti-fatigue effects.

Effect of Polysaccharides from Root， Stem， Leaf and Fruit of Schisandra chinensis on Exercise Endurance in D-galactose-induced Aging Mice / 中国实验方剂学杂志

ObjectiveTo observe the effect of polysaccharides from root， stem， leaf and fruit of Schisandra chinensis on exercise endurance in the aging mice induced by D-galactose. MethodMale ICR mice were randomly assigned into six groups： blank control group， model group， root polysaccharide group， stem polysaccharide group， leaf polysaccharide group and fruit polysaccharide group. The mice were administrated with distilled water or root， stem， leaf and fruit polysaccharide （total sugar content of 35 mg·kg-1） by gavage. Thirty minutes after the administration， the blank control group was subcutaneously injected with normal saline， and the other groups with D-galactose （300 mg·kg-1）， once daily for 6 weeks. The anti-fatigue effects were evaluated by rotarod test， forelimb grip strength test， and weight-loaded swimming test. The fatigue and oxidation indicators such as blood urea nitrogen （BUN）， serum lactic acid （LD）， lactic dehydrogenase （LDH）， creatine kinase （CK）， superoxide dismutase （SOD）， malondialdehyde （MDA）， glutathione peroxidase （GSH-Px）， and reactive oxygen species （ROS） were measured by chemical colorimetry. The protein levels of pro-apoptotic protein B cell lymphoma-2 （Bcl-2）-associated X protein （Bax）， anti-apoptotic Bcl-2 and cleaved cysteinyl aspartate-specific protease-3 （cleaved Caspase-3） in mouse skeletal muscle were detected by Western blot. ResultIn the rotarod test， the time on rod was shorter in the model group than in the blank control group （P<0.01） and the root， stem and fruit polysaccharide groups （P<0.01）. In the forelimb grip strength test， the forelimb grip strength in the model group was lower than that in the blank control group （P<0.01） and the root， stem， leaf and fruit polysaccharide groups （P<0.01）. In the weight-loaded swimming test， the weight-loaded swimming time in the model group was shorter than that in the blank control group （P<0.01） and the root， stem， leaf and fruit polysaccharide groups （P<0.01）. Compared with those in the blank control group， the BUN， LD， LDH and CK levels significantly increased in the model group （P<0.05， P<0.01）. The increases in BUN and LDH levels were decreased by the root， stem and fruit polysaccharides （P<0.05， P<0.01） and those in LD and CK by the root， stem， leaf and fruit polysaccharides （P<0.05， P<0.01）. Compared with the blank control group， the model group showed decreased SOD and GSH-Px activities （P<0.01） and increased MDA and ROS content （P<0.01）. Compared with the model group， the root， stem， and fruit polysaccharide increased the SOD activity （P<0.05， P<0.01） and decreased ROS content （P<0.01）. The root and stem polysaccharides decreased the MDA content （P<0.01） and increased the GSH-Px activity （P<0.05， P<0.01）. Compared with the blank control group， the model group showed up-regulated protein levels of Bax and cleaved Caspase-3 and down-regulated protein level of Bcl-2 （P<0.01）. Compared with the model group， the root， and stem polysaccharides down-regulated the protein levels of cleaved Caspase-3 （P<0.05） and up-regulated protein level of Bcl-2 （P<0.01）. ConclusionThe polysaccharides from the root， stem， leaf， and fruit of S. chinensis have anti-fatigue effect in D-galactose-induced aging mice. The polysaccharides may exert such effect by improving the antioxidant capacity and inhibiting the apoptosis of skeletal muscle cells.

Protective effects of 7-hydroxyethyl chrysin on rats with exercise-induced fatigue in hypobaric hypoxia environment / 浙江大学学报·医学版

: To investigate the protective effect of 7-hydroxyethyl chrysin (7-HEC) on rats with exercise-induced fatigue in hypobaric hypoxic condition.Forty healthy male Wistar rats were randomly divided into four groups with 10 rats in each group: control group, model group, chrysin group and 7-HEC group. The rats in control group were raised at local altitude but other three groups were raised in a simulating altitude of for hypobaric hypoxia treatment. The chrysin group and 7-HEC group were given chrysin or 7-HEC by gavage for respectively; while the control group and model group were given the same amount of sterilized water. The weight-bearing swimming tests were performed 3 d later, and the weight-bearing swimming time was documented. After rats were sacrificed, the liver and skeletal muscle tissue samples were taken for pathological examination and determination of lactate, malondialdehyde (MDA), total superoxide dismutase (T-SOD) and glycogen levels. Blood urea nitrogen was also determined. Compared with the model group, weight-bearing swimming times were significantly prolonged in 7-HEC group [ vs. (4.04±1.30) min, <0.01]; pathological changes in liver and skeletal muscle tissue were attenuated; generation rate of blood urea nitrogen vs. 0.60) mmol·L·min, <0.05], lactate [liver: (0.14±0.05) vs. (0.10±0.03) mg·g·min, skeletal muscle: vs. (0.18±] and MDA [liver: (0.48) vs. (0.78±0.28) nmol·mg·min, skeletal muscle: (0.87±0.19) vs. (0.63±0.11) nmol·mg·min] were significantly reduced (all < 0.05); glycogen content [liver: (15.16±2.69) vs. skeletal muscle: (1.46±0.49) vs.0.48) mg/g] and T-SOD [liver: (1.87±0.01) vs. (2.68±0.12) U/mL, skeletal muscle: 0.42) vs. 0.96) U/mL] were significantly improved (all <0.05). 7-HEC has significant protective effect on the rats with exercise-induced fatigue in hypobaric hypoxia condition.

Mechanism of anti-fatigue of Epimedii Folium based on network pharmacology / 中草药

Objective: To study the anti-fatigue mechanism of Epimedii Folium by network pharmacology. Methods: The main active ingredients of Epimedii Folium and the targets of active ingredients were obtained by TCMSP. The GeneCards was used to predict and screen the anti-fatigue targets. The Cytoscape 3.6.1 software was used to construct the active ingredient-disease-target network. The protein interactions network was constructed using the String database. The GO enrichment and KEGG pathways of the targets were analyzed by using DAVID database. Results: Nine active ingredients were screened from Epimedii Folium, including chrysoeriol, kaempferol, anhydroicaritin, C-homoerythrinan,1,6-didehydro-3,15,16-trimethoxy-,(3.beta.)-, 8-(3-methylbut-2-enyl)-2-phenyl- chromone, luteolin, magnograndiolide, quercetin, 8-isopentenyl-kaempferol, which acted on 31 fatigue targets such as PPARG, GABRA1, CASP3, ICAM1, etc. Biological function analysis showed that the targets of Epimedii Folium included cellular response to hypoxia, regulation of apoptotic, positive regulation of nitric oxide biosynthetic, cellular response to hydrogen peroxide, cellular response to hyperoxia, and negative regulation of lipid storage. Signaling pathway analysis showed that Epimedii Folium exerted the anti-fatigue effect by regulating PI3K-Akt, P53, HIF-1, TNF, FoxO, ErbB, MAPK, and other pathways. Conclusion: This study reflects the characteristics of multi-component, multi-target, and multi-pathway of Epimedii Folium, which provides reference for further research on the mechanism of anti-fatigue effects of Epimedii Folium.

Accurate positioning and analysis on health function of high frequency anti-fatigue herbal medicines / 中国中药杂志

Fatigue is a widespread and complex physiological phenomenon. Chronic fatigue can lead to cardiovascular dysfunction, mental disorders and other serious pathological reactions. Therefore, how to relieve fatigue accurately and effectively is an important proposition to implement the concept of "Healthy China" in the new era. As an important part of Chinese medicine health industry, Chinese medicine health food has been developing rapidly in recent years. At present, there are 1 157 kinds of anti-fatigue health food on the market in China, most of which are single Chinese medicine and its compound. However, their functions are generally labeled as "anti-fatigue", and their function positioning is too extensive and unclear. With the deepened understanding of fatigue classification and its physiological and pathological basis, it is urgent to be combined with the progress of modern chemical and pharmacological stu-dies to differentiate and precisely position the anti-fatigue health effects of traditional Chinese medicine. For this purpose, the classifications of fatigue were summarized in this paper, and the mechanism of fatigue was explained from the aspects of energy metabolism, accumulation of metabolites, oxidative stress, inflammation, hypothalamus pituitary adrenal axis and so on. We selected 10 traditional Chinese medicines which are most frequently used in health food, analyzed their anti-fatigue effect mechanisms, and summarized the best types of anti-fatigue food, so as to promote the scientific development of anti-fatigue health food industry, expand the market application scope of anti-fatigue health food, better respond to the construction of a healthy China and serve for people's health.

Changes in Effective Compounds and Anti-fatigue Activity Before and After Compatibility of Ginseng Radix et Rhizoma Rubra and Rhodiolae Crenulate Radix et Rhizoma / 中国实验方剂学杂志

Objective:To preliminarily interpret the compatibility of Ginseng Radix et Rhizoma Rubra and Rhodiolae Crenulate Radix et Rhizoma in chemical and pharmacodynamic levels，and provide theoretical basis for its clinical application.Method:Rapid resolution liquid chromatography coupled with quadrupole-time-of-flight tandem mass spectrometry（RRLC-Q-TOF-MS） was applied to identify and analyze the changes in chemical components of the Ginseng Radix et Rhizoma Rubra and Rhodiolae Crenulate Radix et Rhizoma before and after compatibility. The anti-fatigue activity before and after compatibility of Ginseng Radix et Rhizoma Rubra and Rhodiolae Crenulate Radix et Rhizoma was detected by weight-loading swimming experiment and determination of levels of serum urea，blood lactic acid and hepatic glycogen.Result:A total of 51 compounds were identified in mixture decoction of Ginseng Radix et Rhizoma Rubra and Rhodiolae Crenulate Radix et Rhizoma. Malonyl ginsenoside mRg1，mRb1，mRb2，mRb3 and mRd contents were significantly decreased，while ginsenoside Rb1，Rb2，Rb3，Rd，F2 and Rg3 contents were significantly increased in the compatibility mixture. According to pharmacodynamics study，as compared with those in the blank control group，swimming time of mice was significantly prolonged in all other groups （P<0.01），serum urea nitrogen（P<0.05，P<0.01） and lactic acid（P<0.05，P<0.001） levels of mice in the combined decoction and the single decoction groups were significantly lowered，while liver glycogen levels were significantly elevated（P<0.05，P<0.01）. The anti-fatigue ability of the combined decoction of Ginseng Radix et Rhizoma Rubra and Rhodiolae Crenulate Radix et Rhizoma was higher than that of the single decoctions.Conclusion:In this article, the effect enhancing mechanism of compatibility of Ginseng Radix et Rhizoma Rubra with Rhodiolae Crenulate Radix et Rhizoma was revealed based on the chemical changes, providing theoretical reference for the clinical application and development of products.

Examination of the correlation between grades, chemicalcharacteristics and anti-fatigue effect of Astragali Radix / 药学学报

To provide a basis for the establishment of the commodity grade of Astragali Radix (AR), we compared the chemical components and the anti-fatigue effect of different grades of AR. The components of primary metabolites were analyzed by 1H NMR and the contents of five flavonoids were determined by HPLC-UV with different grades of AR. Fatigue efficacy of different grades of AR was compared. All the procedures were approved by the Laboratory Animal Ethics Committee of the Shanxi University. The results showed that the content of water soluble extracts (WSE) of the Grade Ⅱ AR was the lowest, and 21 compounds were identified through 1H NMR spectrum. There are 3 components showing a higher content in the Grade-top AR, and 7 components were higher in the Grade-Ⅳ, and 7 other components were higher in the Grade-Ⅱ AR. Total flavonoid content was the highest in Grade-Ⅱ but it was the lowest in the Grade-Ⅳ. Pharmacodynamic results showed that AR could significantly enhance the exhaustion time of rats and improve the biochemical indexes of serum and gastrocnemius muscle, and the best anti-fatigue effect was observed with Grade -Ⅱ AR. Therefore, chemical composition and efficacy index were used to evaluate the quality of different grades of AR, and the quality evaluation approach was established based on chemical and pharmacological effects to provide a scientific basis for the development of AR. The study may provide useful information for construction of the quality grade standard of AR.

The Interaction of Cognitive Interference, Standing Surface, and Fatigue on Lower Extremity Muscle Activity

BACKGROUND: Performing cognitive tasks and muscular fatigue have been shown to increase muscle activity of the lower extremity during quiet standing. A common intervention to reduce muscular fatigue is to provide a softer shoe-surface interface. However, little is known regarding how muscle activity is affected by softer shoe-surface interfaces during static standing. The purpose of this study was to assess lower extremity muscular activity during erect standing on three different standing surfaces, before and after an acute workload and during cognitive tasks. METHODS: Surface electromyography was collected on ankle dorsiflexors and plantarflexors, and knee flexors and extensors of fifteen male participants. Dependent electromyography variables of mean, peak, root mean square, and cocontraction index were calculated and analyzed with a 2 × 2 × 3 within-subject repeated measures analysis of variance. RESULTS: Pre-workload muscle activity did not differ between surfaces and cognitive task conditions. However, greater muscle activity during post-workload balance assessment was found, specifically during the cognitive task. Cognitive task errors did not differ between surface and workload. CONCLUSIONS: The cognitive task after workload increased lower extremity muscular activity compared to quite standing, irrespective of the surface condition, suggesting an increased demand was placed on the postural control system as the result of both fatigue and cognitive task.

Effects of Raphani Semen on anti-fatigue and pharmacokinetics of Panax ginseng / 中草药·英文版

Objective: To explain the phenomenon that Panax ginseng is not compatible with Raphani Semen based on pharmacodynamics and pharmacokinetics. Methods: The forced swimming time and biochemical parameters such as blood lactate (BLA), serum urea nitrogen (SUN), and hepatic glycogen (GLU) were determined for anti-fatigue experiment. The UPLC-MS/MS was used to analyze the pharmacokinetics of Rg1, Re, Rb1, and Rd after orally administration of P. ginseng and P. ginseng combined with Raphani Semen to rats. Pharmacokinetic differences of four ginsenosides between single uses of P. ginseng and combined with Raphani Semen were investigated. Results: The results showed that Raphani Semen tended to significantly reduce the anti-fatigue activity of P. ginseng. Co-administration of P. ginseng and Raphani Semen had significant effects on the pharmacokinetics of the four ginsenosides in rats compared to that observed with P. ginseng extract alone. The AUC0–12 h values of the four ginsenosides in PG group were higher than the corresponding values in the PR group. It can be inferred that Raphani Semen decreased the blood exposure of the four ginsenosides in rats when it combined with P. ginseng. Conclusion: The anti-fatigue activity and pharmacokinetic results showed that Raphani Semen may reduce the pharmacological actions of P. ginseng.

Mechanism of anti-fatigue of Astragali Radix based on network pharmacology / 中草药

Objective: To explore the anti-fatigue mechanism of Astragali Radix based on network pharmacology. Methods: The main active ingredients of Astragali Radix were obtained by TCMSP and the results of our previous work. GeneCards and OMIM were used to predict and screen the therapeutic targets of Astragali Radix. The Cytoscape 3.6.0 software was used to construct the active components-targets network of Astragali Radix. The protein interactions network was constructed using the String database and Cytoscape software. The GO and KEGG pathways involved in the targets were analyzed by using DAVID database. Results: The results showed that 11 active components including six flavonoids (calycosin-7-O-β-D-glucoside, calycosin, ononin, formononetin,7,2’-dihydroxy-3,4-dimethoxyisoflavan, 3-hydroxy-9,10-dimethoxypterocarpan), four saponins (astragaloside I, II, III, IV) and sucrose and 76 targets of Astragali Radix were involved. The network analysis results showed that the process of nitric oxide biosynthesis, hydrogen peroxide reaction, positive regulation on brown adipocyte differentiation, and active oxygen metabolism were mainly involved by adjusting the cancer, FoxO, PI3K-Akt, HIF-1, VEGF, MAPK and other signaling pathways to exert its antifatigue effect. Conclusion: This study reflects the characteristics of multi-components, multi-targets, and multi-pathways of Astragali Radix, which provides new ideas and clues for further research on the mechanism of anti-fatigue effects of Astragali Radix.

Progress toward the clinical application of Rhodiolae Crenulatae Radix et Rhizoma / 国际中医中药杂志

Rhodiolae Crenulatae Radix et Rhizoma is a precious traditional Chinese medicine and has extensive pharmacological effects, such as anti-hypoxic, anti-fatigue, anti-aging, anti-inflammatory, anti-tumor, lowing blood sugar, heart and brain protection. It has been applied to the treatment of cardiovascular diseases, nervous diseases, respiratory diseases, endocrine diseases, fracture problems, emotional stress, and skin diseases. The present review summarized the literature about its clinical use, which would provide a reference for further utilization.

Study on anti-fatigue, anti-oxidative and hemostatic effects of small molecule Asini Corii Colla / 中国药理学通报

Aim: To study the anti-fatigue,anti-oxidative and hemostatic effects of small molecule Asini Corii Colla (SMACC). Methods: Rat model of complex blood deficiency was established to detect the exhausted time of swimming, hematology, superoxide dismutase (SOD), serum maleic dialdehyde (MDA), and lipid peroxide (LPO) levels, aiming to explore the anti-fatigue and anti-oxidative effects of SMACC. ICR mice were used to measure the blood clotting time (CT) and bleeding time (BT). Fevered and bleeding model and the heparinized bleeding model in rats were established to investigate the effect of SMACC in hemostasis and its possible mechanism. Results: Compared with model group, SMACC significantly prolonged the swimming time of model rats (P < 0. 05, P < 0. 01) and decreased the content of serum MDA, LPO (P < 0.05,P<0.01) at doses of 1. 500,0. 750,0. 375 g. kg-1,and increased the number of lymphocytes in the blood at doses of 1. 500,0. 375 g. kg-1 (P <0. 05). SMACC of 3. 00,1.50 g kg-1 significantly reduced the BT and CT (P < 0. 05). SMACC markedly reversed the prolonged prothrombin time (P < 0. 05) and the adverse changes of the hematological indicators. Conclusions: SMACC has the pharmacological effects of anti-fatigue, anti-oxidation and enhancing endurance, and also the effects of hemostasis and convergence.

1H NMR-based metabolomics analysis of the anti-fatigue effects of Astragali Radix based on muscle tissue Pubescentis / 药学学报

This study was designed to explore the intervention of muscle fatigue in rats with Astragali Radix using 1H NMR metabolomics methods. The fatigue model was induced in rats by forced swimming plus food restriction, and the effects of Astragali Radix (3, 6 and 12 g·kg-1) were investigated using the exhaustive time of rat swimming. After 3 weeks, the gastrocnemius was collected for 1H NMR detection, and the anti-fatigue effects of Astragali Radix were explored using multivariate statistical analysis. Astragali Radix significantly improved the exhaustive swimming time of rats. Compared with control group, the levels of isoleucine, leucine, creatine, phosphatidylcholine, trimethylamine oxide, taurine, guanidinoacetate, AMP, inosine, histidine, hypoxanthine, anserine in rat gastrocnemius of model group were increased. While the levels of lactate, acetone, choline, glycerophosphocholine, glycine were decreased. These 6, 11, 5 potential biomarkers could be reversely regulated by treatment with Astragali Radix (high dose, middle dose, low dose), respectively. Metabolomics analysis revealed that Astragali Radix has a certain anti-fatigue effects and the mechanism may be related to regulation of amino metabolism.

Batch Inspection of Sildenafil and its Analogues in Anti-fatigue Health Foods by HPLC-MS/MS / 中国药师

Objective:To detect 11 kinds of illegally added chemicals in anti-fatigue health foods including sildenafil ,tadalafil, vardenafil , acetildenafil , homosildenafil , hydorxyhomosildenafil , norneosildenafil , aminotadalafil , pseudovardenafil , thioaildenafil and noracetildenafil.Methods:An HPLC-MS/MS method was used with LUNA C18(250 mm ×4.6 mm, 5μm)as the analysis column and triethylamine phosphate , acetonitrile and methanol as the mobile phase with gradient elution at the flow rate of 1ml.min-1 .An ESI+scan and an MS/MS mode were applied .The qualitative and quantitative analysis were carried out by HPLC-MS/MS.Results:Through the detection of 100 batches of samples , 85 batches were only found illegally added chemical substance sildenafil mainly at the concentration of 5-15 mg per granule .Conclusion:The method of HPLC-MS/MS can be used as a powerful screening tool for the rapid drug screening in basic level drug control laboratories to reduce chemical substances illegally added in anti -fatigue health foods .

Experimental studies on anti-fatigue effects and spectra-effect relationship of different extracts from black Lepidium meyenii (Maca) / 中草药

Objective To investigate the anti-fatigue effects and the relationship between UPLC and anti-fatigue effects of different extracts of black Maca, and to provide a basis for clarifying the material basis of anti-fatigue effects of black Maca. Methods Anti- fatigue effects of eight different extracts of black Maca were evaluated through exhaustive swimming time, contents of liver glycogen, and lactic acid in serum; UPLC-Q-TOF/MS was applied to establish the fingerprints for black Maca from eight extracts; Using the anti-fatigue effects of exhaustive swimming experiment as pharmacodynamic indicators, spectra-effect relationship was analyzed by using PLSR. Results 60%, 80%, and 95% ethanol extracts of black Maca could significantly prolong the exhaustive swimming time of mice, with the effects of 95% ethanol extract of black Maca was the strongest; The treatment of 80% ethanol extract of black Maca significantly increased the level of depressed hepatic glycogen due to excessive exercise; Moreover, 95% ethanol extract of black Maca substantially decreased the serum lactic acid accumulation after loaded-swimming. A total of 23 characteristic peaks were characterized by HPLC fingerprints of eight different extracts of black Maca. N-benzylhexadecanamide, N-benzyl-5-oxo-6E,8E-octadecadienamide, 1,3-dibenzyl-2-phenyl-4,5-dimethylimidazilium, and N-octadecanamide were found to be positively related to the anti-fatigue effects with VIP > 1 in extracts of black Maca from PLSR analysis by using anti-fatigue effects of exhaustive swimming time as pharmacodynamic indicators. Conclusion 95% and 80% ethanol extracts of black Maca showed the obvious anti-fatigue function. It is clear that four components N-benzylhexadecanamide, N-benzyl-5-oxo-6E,8E-octadecadienamide, 1,3-dibenzyl-2-phenyl-4,5-dimethylimidazilium, and N-octadecanamide are the principal anti-fatigue substances in black Maca. The study has the contribution to to explore the material basis of anti-fatigue effects and provides new ideas for the omprehensive and reliable quality control of black Maca.

A new antifatigue eudesmane sesquiterpenoid from Acanthopanax senticosus / 中草药

Objective To study the antifatigue bioactive constituents from Acanthopanax senticosus. Methods The compounds were isolated by means of various chromatographic techniques (Silica gel, Sephadex LH-20, MCI GEL CHP-20P, and HPLC), and its structures were elucidated by extensive spectroscopic analysis (IR, HR-MS, 1D- and 2D-NMR). The free radical scavenging activity in vitro was assessed by an ABTS assay. Results One new eudesmane sesquiterpenoid was isolated and identified as 7α(H)-eudesm-4α,5β,11,12- tetraol-3-one, and its scavenging activities towards ABTS free radical with half scavenging concentration of (43.1 ± 1.2) μg/mL. Conclusion Compound 1 is a new eudesmane sesquiterpenoid named senticosol A. Meanwhile, this compound with eudesmane skeleton is also obtained from the Araliaceae for the first time.

Studies on the synthesis and anti-fatigue activity of the salidroside derivatives / 药学实践杂志

Objective A series of 4 substituted salidroside derivatives were designed and synthesized .Their anti-fatigue effects were investigated .Methods With five-acetyl glucose and different 4-substituted benzyl tyrosols as the starting materi-als ,salidroside derivatives were synthesized through glycosidation and deacetylation reactions .The exercise exhaustive mice model was used to study the anti-fatigue effects of those synthesized derivatives by comparing the loading swimming time of mice .Results 10 novel salidroside derivatives were synthesized .The loading swimming tests showed that the swimming time of the mice in the positive group (salidroside) and 3a-1 group (phenethyl-β-D-glucoside) was longer than that in the control group with statistically significant difference(P<0 .05) .The swimming times for other groups were similar to control group with no statistically significant difference .Conclusion This synthetic method for salidroside derivatives was convenient and feasible for large production .The 4-hydroxyl groups on the benzene ring of salidroside and its derivatives may be the active site responsible for their anti-fatigue activity .