Objective This study aimed to investigate the effect and underlying mechanism of Fructus lycii in improving exercise fatigue.Methods A network pharmacological approach was used to explore potential mechanisms of actio...Objective This study aimed to investigate the effect and underlying mechanism of Fructus lycii in improving exercise fatigue.Methods A network pharmacological approach was used to explore potential mechanisms of action of Fructus lycii.Skeletal muscle C2C12 cells and immunofluorescence were employed to verify the effect and mechanism of the representative components in Fructus lycii predicted by network pharmacological analysis.Results Six potential active components,namely quercetin,β-sitosterol,stigmasterol,7-Omethylluteolin-6-C-beta-glucoside_qt,atropine,and glycitein,were identified to have potency in improving exercise fatigue via multiple pathways,such as the PI3K-Akt,neuroactive ligand-receptor interaction,IL-17,TNF,and MAPK signaling pathways.The immunofluorescence results indicated that quercetin,a significant active component in Fructus lycii,increased the mean staining area of 2-NBDG,TMRM,and MitoTracker,and decreased the area of CellRox compared to the control.Furthermore,the protein expression levels of p-38 MAPK,p-MAPK,p-JNK,p-PI3K,and p-AKT markedly increased after quercetin treatment.Conclusion Fructus lycii might alleviate exercise fatigue through multiple components and pathways.Among these,quercetin appears to improve exercise fatigue by enhancing energy metabolism and reducing oxidative stress.The PI3K-AKT and MAPK signaling pathways also appear to play a role in this process.展开更多
As a traditional Chinese herbal medicine,Schisandrae Chinensis Fructus(SC)has been used in medicine and food industry due to its health care and therapeutic effects.Over the past 20 years,the use of SC and its active ...As a traditional Chinese herbal medicine,Schisandrae Chinensis Fructus(SC)has been used in medicine and food industry due to its health care and therapeutic effects.Over the past 20 years,the use of SC and its active ingredient lignans in the prevention and treatment of liver diseases has been increasing,and their hepatoprotective effects has increased the interest of the public and academia.Therefore,in the present work,we first determined the effectiveness of SC in the treatment of liver diseases such as metabolic associated fatty liver disease,alcoholic liver disease,cholestatic liver disease and acute liver injury.Subsequently,the pharmacological effects and molecular mechanisms of lignans,the active components of SC,for liver disease treatment were comprehensively summarized for the first time.The results showed that the lignans in SC could achieve hepatoprotective effects by regulating lipid metabolism,anti-fibrosis,anti-inflammation,anti-oxidation,anti-tumor and regulating bile acid metabolism.The mechanism mainly involved adenosine 5’-monophosphate-activated protein kinase,endoplasmic reticulum stress,sterol regulatory element binding protein 1c,autophagy,transforming growth factor-β,mitogen-activated protein kinase,microRNA,nuclear factor kappa-B,nuclear factor erythroid-2-related factor 2,heat shock proteins and pregnane X receptor signaling pathways.These results can lay a scientific foundation for the development of hepatoprotective drugs or functional foods from SC/lignans.展开更多
Schisandrae chinensis Fructus (SF) is a commonly used herb in Traditional Chinese Medicine (TCM). According to TCM theory, SF can invigorate Qi in the liver and other visceral organs through the meridian system. Furth...Schisandrae chinensis Fructus (SF) is a commonly used herb in Traditional Chinese Medicine (TCM). According to TCM theory, SF can invigorate Qi in the liver and other visceral organs through the meridian system. Furthermore, the liver’s pivotal role in regulating the functions of various visceral organs helps explain how SF can promote holistic health benefits. The main active ingredient of SF, schisandrin B (Sch B), has been found to improve mitochondrial ATP production and enhance glutathione redox status in multiple organs. This could account for the overall protective effects of Sch B on organs. Due to its stronger impact on liver function, the positive influence of Sch B on different organs may be facilitated by signal molecules originating from the liver.展开更多
[Objectives]This study was conducted to explore the mechanism and pharmacological activity of Fructus Aurantii on human skin through network pharmacology.[Methods]The active components and targets of Fructus Aurantii ...[Objectives]This study was conducted to explore the mechanism and pharmacological activity of Fructus Aurantii on human skin through network pharmacology.[Methods]The active components and targets of Fructus Aurantii were screened byTCMSPand SymMap data-bases,and the targets were humanized after de-duplication by UniProt database.Relevant therapeutic targets were searched in Gencards data-base with"skin"as the key word,and those with higher weights were retained.An effective component-human skin action target network of Fructus Aurantii was established by Cytoscape software.Then,the topological analysis of protein-protein interaction(PPI)network was made by using String database and Cytoscape software.Gene Ontology(GO)funetional enrichment analysis and Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway enrichment analysis were carried out by david database,and the analysis results were visualized by Hiplot soft-ware.[Results]Thirteen active compounds of Fructus Aurantii were obtained by screening,and 99 gene targets of Fructus Aurantii which might have pharmacological activity on human skin were obtained by intersection analysis.PTGS2,PTGS1,HSP90AB1,HSP90AAI,NCOA2 and PIK3CG might be core action targets of Fructus Aurantii on human skin according to the topological analysis of the active component-target network.The analysis of PPI network showed that IL-1β,INS,TNF,TP53 and ESR1 might be core action proteins of Fructus Auranti.GO enrichment analysis showed that Fructus Aurantii might balance the imbalance of skin microenvironment caused by various in-vitro stimuli by participating in biological processes such as response to xenobiotic stimulus and regulation of small molecule metabolic process.KEGG pathway enrichment analysis showed that the targets of Fructus Aurantii acting on human skin were enriched in pathways in cancer,Kaposi sarcoma-associated herpesvirus infection,pathways in measles,AGE-RAGE signaling pathway in diabetic complications,IL.-17 signaling pathway,etc.[Conclusions]Fructus Aurantii may act on human skin targets through a variety of active components,and play a regulatory role in skin-related diseases.展开更多
[Objectives]This study was conducted to determine the contents of benzoylmesaconine,benzoylaconitine and benzoylhypacoitine in the decoctions of Heishun pieces,Trichosanthis Fructus and their combination.[Methods]Heis...[Objectives]This study was conducted to determine the contents of benzoylmesaconine,benzoylaconitine and benzoylhypacoitine in the decoctions of Heishun pieces,Trichosanthis Fructus and their combination.[Methods]Heishun pieces,Trichosanthis Fructus and their combination were extracted for different time periods,and then grouped.HPLC was performed using an Agilent ZORBAX SB-C 18 chromatographic column(4.6 mm×250 mm,5μm)and acetonitrile-0.02 mol/L sodium dihydrogen phosphate as the mobile phase at a flow rate of 1 mL/min and a column temperature of 30℃,and the sample volume was 20μL.The detection wavelength was 230 nm.[Results]The total amounts of benzoylmesaconine,benzoylaconitine and benzoylhypacoitine in the single decoction group of Heishun pieces were all significantly different from those in the combined decoction group at corresponding time.[Conclusions]The total content of the benzoylaconitine type increased significantly after the combined decoction of Heishun pieces and Fructus Trichosanthis,which proves the scientificity of"eighteen incompatible medicaments,19 counteraction"in traditional Chinese medicine to some extent.展开更多
The active components,targets,and pathways of Euphorbia fischeriana Steud.-Jujubae Fructus in treating hepatocirrhosis and the mechanism of action were explored by means of network pharmacology.Firstly,the active comp...The active components,targets,and pathways of Euphorbia fischeriana Steud.-Jujubae Fructus in treating hepatocirrhosis and the mechanism of action were explored by means of network pharmacology.Firstly,the active components and related targets of Jujubae Fructus were screened by TCMSP database and standardized by Uniprot database.The compounds of Euphorbia fischeriana Steud.were obtained by searching the literature and finally screened by PubChem database,Swiss ADME,and SwissTargetPrediction.Hepatocirrhosis targets were obtained through Genecards database,PPI network analysis was conducted on common targets of Euphorbia fischeriana Steud.-Jujubae Fructus and hepatocirrhosis by using String database,GO enrichment analysis and KEGG pathway enrichment analysis was conducted through Metascape database by using intersection targets of Euphorbia fischeriana Steud.-Jujubae Fructus and hepatocirrhosis,and the results were drawn by using Weishengxin online drawing platform.Then,the network of drug-compound-target-pathway was constructed by the software of Cytoscape3.8.0.Finally,the above results were verified by molecular docking.47 active compounds from Euphorbia fischeriana Steud.-Jujubae Fructus were screened out,which had 38 common targets,162 intersection targets,and 340 signal pathways with hepatocirrhosis,mainly involving hepatitis C,JAK-STAT signal pathway and AGE-RAGE signal pathway.Targets,such as MAPK1,AKT1,TNF,JUN,IL6 and PTGS2,play important roles in the treatment.The findings suggested that the main active ingredients of Euphorbia fischeriana Steud.-Jujubae Fructus in treating hepatocirrhosis are quercetin,scopolamine,physcion,7-deoxyrangduin,17-Hydroxyjolkinolide A,etc.Molecular docking results showed that the main active components and core targets might have a good binding capacity.This study preliminarily explored the potential mechanism of Euphorbia fischeriana Steud.-Jujubae Fructus in treating hepatocirrhosis and provided a theoretical basis for the clinical application of Euphorbia fischeriana Steud.-Jujubae Fructus.展开更多
Background Liver fibrosis and hepatocellular carcinogenesis secondary to liver fibrosis are serious liver diseases with no effective treatments.Mori fructus aqueous extracts(MFAEs)have served as successful treatments ...Background Liver fibrosis and hepatocellular carcinogenesis secondary to liver fibrosis are serious liver diseases with no effective treatments.Mori fructus aqueous extracts(MFAEs)have served as successful treatments for many types of liver injury including fibrosis although the molecular mechanisms are unknown at present.Purpose To investigate the effect of MFAEs in alleviating acute and chronic liver injury and tried to decipher the underlying mechanism.Methods and results Mice were divided into 5 groups(n ps:contro=8)for acute(groups:control,0.3%CCl_(4),bifendate(BD),100 and 200 mg/kg MFAEs,7 d)and chronic(groul,10%CCl_(4),BD,100 and 200 mg/kg MFAEs,4 weeks)liver injury study.Each mouse was injected intraperitoneally with 10μL/g corn oil containing CCl_(4)expect the control group.HepG2 cells were used in vitro study.Eighteen communal components were identified by UPLC-LTQOrbitrap-MS.We utilized a mouse model for acute and chronic liver injury using CCl_(4)and MFAEs administration effectively blocked fibrosis and significantly inhibited inflammation in the liver.MFAEs activated the nuclear factor erythroid derived 2 like 2/heme oxygenase 1(Nrf2/HO-1)pathway and promoted the synthesis of the antioxidants glutathione(GSH),superoxidedismutase(SOD)and glutathione peroxidase(GSH-Px)that resulted in reduced levels of CCl_(4)-induced oxidative stress molecules including reactive oxygen species.These extracts administered to mice also inhibited ferroptosis in the liver by regulating the expression of Acyl-CoA synthetase long chain family member 4(ACSL4),solute carrier family 7 member 11(SLC7A11)and glutathione peroxidase 4(GPX4),thus reducing the occurrence of liver fibrosis.Both in vivo and in vitro tests indicated that the mechanism of MFAEs protection against liver fibrosis was linked to activation of Nrf2 signaling.These effects were blocked in vitro by the addition of a specific Nrf2 inhibitor.Conclusion MFAEs inhibited oxidative stress,ferroptosis and inflammation of the liver by activating Nrf2 signal pathway and provided a significant protective effect against CCl_(4)-induced liver fibrosis.展开更多
Quzhou Aurantii Fructus(QAF)has a long history as a folk medicine and food for the treatment of liver diseases.While our earlier study provided evidence of hepatoprotective properties contained within the flavonoids a...Quzhou Aurantii Fructus(QAF)has a long history as a folk medicine and food for the treatment of liver diseases.While our earlier study provided evidence of hepatoprotective properties contained within the flavonoids and limonins constituents in QAF,the potential preventative effects afforded by essential oil components present within QAF remains enigmatic.In this study,we prepared Quzhou Aurantii Fructus essential oil(QAFEO)and confirmed its anti-inflammatory effects on liver inflammation through experimentation on lipopolysaccharide and D-galactosamine(LPS/D-GalN)induced acute liver failure(ALF)mouse models.Using RNA-sequence(RNA-seq)analysis,we found that QAFEO prevented ALF by systematically blunting the pathways involved in response to LPS and toll-like receptor signaling pathways.QAFEO effectively suppressed the phosphorylation of tank-binding kinase 1(TBK1),TGF-beta activated kinase 1(TAK1),interferon regulatory factor 3(IRF3),and the activation of mitogen activated kinase-like protein(MAPK)and nuclear factor-kappa B(NF-κB)pathways in vivo and in vitro.Importantly,QAFEO substantially reduced myeloid differentiation primary response gene 88(MyD88)-toll-like receptor 4(TLR4)interaction levels.Moreover,8 compounds from QAFEO could directly bind to REAL,TAK1,MyD88,TBK1,and IRF3.Taken together,the results of our study support the notion that QAFEO exerts a hepatoprotective effect through inhibiting LPS-mediated inflammatory response.展开更多
Euodiae Fructus,referred to as“Wuzhuyu”in Chinese,has been used as local and traditional herbal medicines in many regions,especially in China,Japan and Korea,for the treatment of gastrointestinal disorders,headache,...Euodiae Fructus,referred to as“Wuzhuyu”in Chinese,has been used as local and traditional herbal medicines in many regions,especially in China,Japan and Korea,for the treatment of gastrointestinal disorders,headache,emesis,aphtha,dermatophytosis,dysentery,etc.Substantial investigations into their chemical and pharmacological properties have been performed.Recently,interest in this plant has been focused on the different structural types of alkaloids like evodiamine,rutaecarpine,dehydroevodiamine and 1-methyl-2-undecyl-4(1H)-quinolone,which exhibit a wide range of pharmacological activities in preclinical models,such as anticancer,antibacterial,anti-inflammatory,anti-cardiovascular disease,etc.This review summarizes the up-to-date and comprehensive information concerning the botany,traditional uses,phytochemistry,pharmacology of Euodiae Fructus together with the toxicology and quality control,and discusses the possible direction and scope for future research on this plant.展开更多
Prohibited pesticide residues have become one of the main factors affecting the quality and safety of Lycii Fructus,However,rarely studies focus on the rapid determination of these residues.Here,a total of 30 kinds of...Prohibited pesticide residues have become one of the main factors affecting the quality and safety of Lycii Fructus,However,rarely studies focus on the rapid determination of these residues.Here,a total of 30 kinds of prohibited pesticide residues were determined by ultra-performance liquid chromatography tandem triple quadrupole mass spectrometry(UPLC-MS/MS)in five different process ways.Pretreatment methods,chromatographic separation and detection conditions in mass spectrometry were all optimized accordingly.Among the five different pretreatment methods,the first and third solid phase extraction failed to provide high recoveries of sulfosulfuron compounds(both lower than 60%).Recovery of chlorphenamidine by the Quick Easy Cheap Effective Rugged and Safe multiresidue method(QuEChERS)was lower than 60%,which did not meet the requirements of trace determination.The concentrations of 30 prohibited pesticides residues treated by straightforward and solid phase extraction showed good linearity in their corresponding ranges,with correlation coefficients over 0.99.The average recoveries of straightforward ranged from 78.13%to 110.9%,while RSD ranged from 1.3%to 16.9%,albeit poor purification was observed.The recovery yield from solid phase extraction was between 67.75%and 103.08%with RSD value from 0.8%to 14.0%,which met the requirements of trace determination,this method has good precision and stability.These results could be employed to other Traditional Chinese Medicines(TCMs)in detecting prohibited pesticide residues.展开更多
In this paper,the traditional identification and modern identification technology of Cnidii Fructus and its adulterant were reviewed,and their advantages,disadvantages and practicability were summarized,to provide a r...In this paper,the traditional identification and modern identification technology of Cnidii Fructus and its adulterant were reviewed,and their advantages,disadvantages and practicability were summarized,to provide a reference for the rapid and accurate identification and quality evaluation of Cnidii Fructus.展开更多
Forsythiae Fructus,a well-known traditional Chinese medicine preparation derived from the dried fruits of Forsythia suspensa(Thunb.)Vahl,has been historically utilized for its heat-clearing and detoxification properti...Forsythiae Fructus,a well-known traditional Chinese medicine preparation derived from the dried fruits of Forsythia suspensa(Thunb.)Vahl,has been historically utilized for its heat-clearing and detoxification properties.Forsythiae Fructus has been reported to exhibit antiviral activity such as against SARS-CoV-2 and influenza virus.This review highlights the recent updates on the effects and underlying action mechanisms of compounds in and active fractions from Forsythiae Fructus and Chinese formulae containing Forsythiae Fructus.展开更多
Background:In this study,we analyzed the potential active components,related crucial targets and possible signaling pathway mechanisms of Alpiniae Oxyphyllae Fructus and Saposhnikoviae Radix(AOF-SR)herb pairs in the t...Background:In this study,we analyzed the potential active components,related crucial targets and possible signaling pathway mechanisms of Alpiniae Oxyphyllae Fructus and Saposhnikoviae Radix(AOF-SR)herb pairs in the treatment of diabetic kidney disease(DKD)using network pharmacology and verification experiments.Methods:The active compounds and potential targets of AOF-SR were derived from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,The Encyclopedia of Traditional Chinese Medicine,and PubChem databases,and the potential therapeutic targets of DKD were derived from the OMIM,Drugbank,and DisGeNET databases.The“compounds-diseases-targets”network was constructed using Cytoscape 3.6.0.ClusterMaker functionality in Cytoscape is being used to screen important targets for AOF-SR treatment of DKD.Gene Ontology and Kyoto Encyclopedia of Genes and Genomes enrichment analysis of important targets were performed using DAVID database.In addition,according to the predicted results of network pharmacology,HK-2 cells were used to construct DKD model for verification experiment.HK-2 cells were divided into control group,high glucose(HG)group and AOF-SR(HG+AOF-SR)group to detect survival rate and expression of key proteins in NF-κB and PI3K/Akt signaling pathways.Results:A total of 38 compounds were selected from AOF-SR,of which 23 were Alpiniae Oxyphyllae Fructus and 15 were Saposhnikoviae Radix.Through enrichment analysis of 82 important targets,88 signaling pathways were identified;some of these pathways,such as the NF-κB,PI3K-Akt,IL-17,and JAK/STAT signaling pathways,regulate the pathological process of DKD.In verification experiment,the HK-2 cells survival rate was higher in the HG+AOF-SR group than in the HG group(P<0.05).Moreover,western blotting results showed that the expression levels of NF-κB,p-PI3K,and p-Akt in HG+AOF-SR group were significantly lower than those in HG group(P<0.05).Conclusion:Overall,this study revealed the active compounds,important targets and possible mechanisms of AOF-SR treatment for DKD,and conducted preliminary verification experiments on its correctness,provided novel insights into the treatment of DKD by AOF-SR.展开更多
[Objectives]Optimum extraction conditions of total flavonoids from Fructus Aurantii Immaturus(TFFAI)and its resistance activity to ultraviolet radiation were investigated in present research.[Methods]The optimal extra...[Objectives]Optimum extraction conditions of total flavonoids from Fructus Aurantii Immaturus(TFFAI)and its resistance activity to ultraviolet radiation were investigated in present research.[Methods]The optimal extraction conditions of TFFAI were determined by single factor and orthogonal experiments,and the survival rate of TFFAI on HaCaT cells irradiated with UVB rays was investigated.It s antioxidant capacity was determined by ABTS.[Results]The results showed that the highest yield of TFFAI was obtained with 70%ethanol at a solid-to-liquid ratio of 1:50(w/v)and 40℃for 1.5 h by single-factor and orthogonal experiments.Total flavonoids(0.25-1.00 mg/ml)could significantly improve the survival rate of HaCaT cell line.Meanwhile,the maximum absorption peak of TFFAI was found at 283 nm,and in-vitro antioxidant experiment identified that TFFAI had a good clearance rate to ABTS.It suggestes that TFFAI could protect the cells from UVB damage by absorption of UVB rays and anti-oxidation.[Conclusions]TFFAI played a protective role on UVB irradiated cells through UVB ultraviolet absorption and antioxidant pathways.展开更多
Background:The traditional Chinese medicine Toosendan Fructus has certain hepatotoxicity,which is used after being processed by stir-frying to attenuate toxicity.However,there are few studies on its attenuating toxici...Background:The traditional Chinese medicine Toosendan Fructus has certain hepatotoxicity,which is used after being processed by stir-frying to attenuate toxicity.However,there are few studies on its attenuating toxicity mechanism.The effects of Toosendan Fructus on the activities of CYP450P1A2,CYP2E1 and CYP3A4 were studied in vivo and in vitro and the dose-toxicity mechanism of hepatotoxicity before and after stir-frying was explored to provide the basis for safe,rational use of Toosendan Fructus.Methods:The rat liver microsomes in vitro incubation method and in vivo pharmacokinetics were used to detect the concentrations of phenacetin,chlorzoxazone and dapsone in the liver microsomes in vitro incubation system and the rat plasma to study the effect of stir-frying of Toosendan Fructus on the activity of CYP450P1A2,CYP2E1,CYP3A4.Results:The results of pharmacokinetics in vivo showed that the AUC of phenacetin and dapsone in different groups was lower,and CL value was higher than those of the normal group.At the same dose,the AUC of stir-fried Toosendan Fructus was higher than that of the raw,while CL value was lower.For the same processed product,AUC value was high-dose>low-dose>middle-dose group,CL value was high-dose<low-dose<middle-dose.AUC and CL values of chlorzoxazone showed no difference from those of the normal group.The results of pharmacokinetics in vivo showed that Toosendan Fructus can induce the activity of CYP3A4 in a dose-dependent manner and the induction effect will decrease after stir-frying in vitro.Conclusion:The toxicity attenuation of Toosendan Fructus may be related to the decrease of induction effect after stir-frying.These results would provide the basis for safe,rational use of Toosendan Fructus.展开更多
Objective It is imperative to provide some consistent experimental results for the extraction of flavonid from Fructus Gardeniae. Methods The key extraction parameters that influenced the yield of flavonid from Fructu...Objective It is imperative to provide some consistent experimental results for the extraction of flavonid from Fructus Gardeniae. Methods The key extraction parameters that influenced the yield of flavonid from Fructus Gardeniae were optimized by employing an orthogonal experiment [L9(3)4], including the ratio of buffer solution (Na2B4O7· 10H2O) to raw material, concentration of Fructus Gardeniae in extracting solution, extraction time and pH of buffer solution. An UV/Vis detector was used to perform the qualitative and quantitative analyses of the extracted flavonid with the using of the standard sample. Results The maximum extraction yield of the crude extract was 5.0533 (mg/g) after 20 min when the mass ratio of Na2B4O7 · 10H2O to raw material was 0.4%, the concentration of Fructus Gardeniae in the extraction solution was 1/12 (g/mL), and pH of buffer solution was 4.5. The positive reactions to the Molish and HCI-Mg tests suggested that the extracted compound was flavonoid, and FTIR measurements also identified the presence of flavonoid in the extracts. Conclusion This work is expected to provide a basis for further research, development, and utilization of Fructus gardenia in flavonid extraction.展开更多
AIM: To examine the effect of aqueous fructus aurantii immaturus(FAI) extracts on the intestinal plexus of cathartic colons.METHODS: Cathartic colons were induced in rats with dahuang,a laxative used in traditional Ch...AIM: To examine the effect of aqueous fructus aurantii immaturus(FAI) extracts on the intestinal plexus of cathartic colons.METHODS: Cathartic colons were induced in rats with dahuang,a laxative used in traditional Chinese medicine. Once the model was established(after approximately 12 wk),rats were administered mosapride(1.54 mg/kg) or various doses of aqueous FAI extracts(1-4 g/kg) for 14 d. Transit function was assessed using an ink propulsion test. Rats were then sacrificed,and the ultramicrostructure of colonic tissue was examined using transmission electron microscopy. The expression of the 5-hydroxytryptamine receptor 4(5-HTR4) and neurofilament-H was assessed in colon tissues using real-time PCR,Western blot,and immunohistochemistry.RESULTS: Mosapride and high dose(4 g/kg) of aqueous FAI extracts significantly improved the bowel movement in cathartic colons compared to untreated model colons as measured by the intestinal transit rate(70.06 ± 7.25 and 72.02 ± 8.74,respectively,vs 64.12 ± 5.19; P < 0.05 for both). Compared to controls,the ultramicrostructure of cathartic colons showed signsof neural degeneration. Treatment with mosapride and aqueous FAI extracts resulted in recovery of ultrastructural pathology. Treatment with mosapride alone upregulated the gene and protein expression of 5-HTR4 compared to untreated controls(P < 0.05 for both). Treatment with aqueous FAI extracts(≥ 2 g/kg) increased 5-HTR4 m RNA levels(P < 0.05),but no change in protein level was observed by Western blot or immunohistochemistry. The m RNA and protein levels of neurofilament-H were significantly increased with mosapride and ≥ 2 g/kg aqueous FAI extracts compared to controls(P < 0.05 for all).CONCLUSION: Aqueous FAI extracts and mosapride strengthen bowel movement in cathartic colons via increasing the expression of 5-HTR4 and neurofilament-H.展开更多
The qualitative and quantitative analysis of active constituents in Fructus Psoraleae is presented by high-performance liquid chromatography (HPLC) coupled with different detections.Extracts of Fructus Psoraleae were ...The qualitative and quantitative analysis of active constituents in Fructus Psoraleae is presented by high-performance liquid chromatography (HPLC) coupled with different detections.Extracts of Fructus Psoraleae were examined by HPLC with ion trap mass spectrometry (IT-MS) and 18 major compounds of coumarins,benzofuran glycosides,flavonoids,and meroterpene were identified.The determination of four major constituents including bavachin,isobavachalcone,bavachinin,and bakuchiol was accomplished by HPLC with UV,MS,and electrochemical detection (ECD).These methods were evaluated for a number of validation characteristics (repeatability,LOD,calibration range,and recovery).ECD obtained a high sensitivity for analysis of the four components;MS provided a high selectivity and sensitivity for determination of bavachin,isobavachalcone,and bavachinin in negative-ion mode.After optimization of the methods,separation,identification.and quantification of the four components in Fructus Psoraleae were comprehensively tested by HPLC with UV,MS,and ECD.展开更多
基金funded by China’s National Key R&D Programmers for“Hi-Tech Winter Olympics”Special Project[2020YFF0305001]。
文摘Objective This study aimed to investigate the effect and underlying mechanism of Fructus lycii in improving exercise fatigue.Methods A network pharmacological approach was used to explore potential mechanisms of action of Fructus lycii.Skeletal muscle C2C12 cells and immunofluorescence were employed to verify the effect and mechanism of the representative components in Fructus lycii predicted by network pharmacological analysis.Results Six potential active components,namely quercetin,β-sitosterol,stigmasterol,7-Omethylluteolin-6-C-beta-glucoside_qt,atropine,and glycitein,were identified to have potency in improving exercise fatigue via multiple pathways,such as the PI3K-Akt,neuroactive ligand-receptor interaction,IL-17,TNF,and MAPK signaling pathways.The immunofluorescence results indicated that quercetin,a significant active component in Fructus lycii,increased the mean staining area of 2-NBDG,TMRM,and MitoTracker,and decreased the area of CellRox compared to the control.Furthermore,the protein expression levels of p-38 MAPK,p-MAPK,p-JNK,p-PI3K,and p-AKT markedly increased after quercetin treatment.Conclusion Fructus lycii might alleviate exercise fatigue through multiple components and pathways.Among these,quercetin appears to improve exercise fatigue by enhancing energy metabolism and reducing oxidative stress.The PI3K-AKT and MAPK signaling pathways also appear to play a role in this process.
基金supported by National Natural Science Foundation of China(81891012,U19A2010,81630101)Sichuan Province Science and Technology Support Program(2021JDRC0041)Innovation Team and Talents Cultivation Program of National Administration of Traditional Chinese Medicine(ZYYCXTD-D-202209).
文摘As a traditional Chinese herbal medicine,Schisandrae Chinensis Fructus(SC)has been used in medicine and food industry due to its health care and therapeutic effects.Over the past 20 years,the use of SC and its active ingredient lignans in the prevention and treatment of liver diseases has been increasing,and their hepatoprotective effects has increased the interest of the public and academia.Therefore,in the present work,we first determined the effectiveness of SC in the treatment of liver diseases such as metabolic associated fatty liver disease,alcoholic liver disease,cholestatic liver disease and acute liver injury.Subsequently,the pharmacological effects and molecular mechanisms of lignans,the active components of SC,for liver disease treatment were comprehensively summarized for the first time.The results showed that the lignans in SC could achieve hepatoprotective effects by regulating lipid metabolism,anti-fibrosis,anti-inflammation,anti-oxidation,anti-tumor and regulating bile acid metabolism.The mechanism mainly involved adenosine 5’-monophosphate-activated protein kinase,endoplasmic reticulum stress,sterol regulatory element binding protein 1c,autophagy,transforming growth factor-β,mitogen-activated protein kinase,microRNA,nuclear factor kappa-B,nuclear factor erythroid-2-related factor 2,heat shock proteins and pregnane X receptor signaling pathways.These results can lay a scientific foundation for the development of hepatoprotective drugs or functional foods from SC/lignans.
文摘Schisandrae chinensis Fructus (SF) is a commonly used herb in Traditional Chinese Medicine (TCM). According to TCM theory, SF can invigorate Qi in the liver and other visceral organs through the meridian system. Furthermore, the liver’s pivotal role in regulating the functions of various visceral organs helps explain how SF can promote holistic health benefits. The main active ingredient of SF, schisandrin B (Sch B), has been found to improve mitochondrial ATP production and enhance glutathione redox status in multiple organs. This could account for the overall protective effects of Sch B on organs. Due to its stronger impact on liver function, the positive influence of Sch B on different organs may be facilitated by signal molecules originating from the liver.
文摘[Objectives]This study was conducted to explore the mechanism and pharmacological activity of Fructus Aurantii on human skin through network pharmacology.[Methods]The active components and targets of Fructus Aurantii were screened byTCMSPand SymMap data-bases,and the targets were humanized after de-duplication by UniProt database.Relevant therapeutic targets were searched in Gencards data-base with"skin"as the key word,and those with higher weights were retained.An effective component-human skin action target network of Fructus Aurantii was established by Cytoscape software.Then,the topological analysis of protein-protein interaction(PPI)network was made by using String database and Cytoscape software.Gene Ontology(GO)funetional enrichment analysis and Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway enrichment analysis were carried out by david database,and the analysis results were visualized by Hiplot soft-ware.[Results]Thirteen active compounds of Fructus Aurantii were obtained by screening,and 99 gene targets of Fructus Aurantii which might have pharmacological activity on human skin were obtained by intersection analysis.PTGS2,PTGS1,HSP90AB1,HSP90AAI,NCOA2 and PIK3CG might be core action targets of Fructus Aurantii on human skin according to the topological analysis of the active component-target network.The analysis of PPI network showed that IL-1β,INS,TNF,TP53 and ESR1 might be core action proteins of Fructus Auranti.GO enrichment analysis showed that Fructus Aurantii might balance the imbalance of skin microenvironment caused by various in-vitro stimuli by participating in biological processes such as response to xenobiotic stimulus and regulation of small molecule metabolic process.KEGG pathway enrichment analysis showed that the targets of Fructus Aurantii acting on human skin were enriched in pathways in cancer,Kaposi sarcoma-associated herpesvirus infection,pathways in measles,AGE-RAGE signaling pathway in diabetic complications,IL.-17 signaling pathway,etc.[Conclusions]Fructus Aurantii may act on human skin targets through a variety of active components,and play a regulatory role in skin-related diseases.
基金Supported by Project for Enhancing Young and Middle-aged Teacher's Scientific Research Basic Ability in Colleges and Universities of Guangxi in 2023 (2023KY0324).
文摘[Objectives]This study was conducted to determine the contents of benzoylmesaconine,benzoylaconitine and benzoylhypacoitine in the decoctions of Heishun pieces,Trichosanthis Fructus and their combination.[Methods]Heishun pieces,Trichosanthis Fructus and their combination were extracted for different time periods,and then grouped.HPLC was performed using an Agilent ZORBAX SB-C 18 chromatographic column(4.6 mm×250 mm,5μm)and acetonitrile-0.02 mol/L sodium dihydrogen phosphate as the mobile phase at a flow rate of 1 mL/min and a column temperature of 30℃,and the sample volume was 20μL.The detection wavelength was 230 nm.[Results]The total amounts of benzoylmesaconine,benzoylaconitine and benzoylhypacoitine in the single decoction group of Heishun pieces were all significantly different from those in the combined decoction group at corresponding time.[Conclusions]The total content of the benzoylaconitine type increased significantly after the combined decoction of Heishun pieces and Fructus Trichosanthis,which proves the scientificity of"eighteen incompatible medicaments,19 counteraction"in traditional Chinese medicine to some extent.
基金supported by Qiqihar Science and Technology Plan Joint Guidance Project (LSFGG-2022042).
文摘The active components,targets,and pathways of Euphorbia fischeriana Steud.-Jujubae Fructus in treating hepatocirrhosis and the mechanism of action were explored by means of network pharmacology.Firstly,the active components and related targets of Jujubae Fructus were screened by TCMSP database and standardized by Uniprot database.The compounds of Euphorbia fischeriana Steud.were obtained by searching the literature and finally screened by PubChem database,Swiss ADME,and SwissTargetPrediction.Hepatocirrhosis targets were obtained through Genecards database,PPI network analysis was conducted on common targets of Euphorbia fischeriana Steud.-Jujubae Fructus and hepatocirrhosis by using String database,GO enrichment analysis and KEGG pathway enrichment analysis was conducted through Metascape database by using intersection targets of Euphorbia fischeriana Steud.-Jujubae Fructus and hepatocirrhosis,and the results were drawn by using Weishengxin online drawing platform.Then,the network of drug-compound-target-pathway was constructed by the software of Cytoscape3.8.0.Finally,the above results were verified by molecular docking.47 active compounds from Euphorbia fischeriana Steud.-Jujubae Fructus were screened out,which had 38 common targets,162 intersection targets,and 340 signal pathways with hepatocirrhosis,mainly involving hepatitis C,JAK-STAT signal pathway and AGE-RAGE signal pathway.Targets,such as MAPK1,AKT1,TNF,JUN,IL6 and PTGS2,play important roles in the treatment.The findings suggested that the main active ingredients of Euphorbia fischeriana Steud.-Jujubae Fructus in treating hepatocirrhosis are quercetin,scopolamine,physcion,7-deoxyrangduin,17-Hydroxyjolkinolide A,etc.Molecular docking results showed that the main active components and core targets might have a good binding capacity.This study preliminarily explored the potential mechanism of Euphorbia fischeriana Steud.-Jujubae Fructus in treating hepatocirrhosis and provided a theoretical basis for the clinical application of Euphorbia fischeriana Steud.-Jujubae Fructus.
基金supported by the Key Project at Central Government Level(2060302)National Natural Science Foundation of China(No.32172897)。
文摘Background Liver fibrosis and hepatocellular carcinogenesis secondary to liver fibrosis are serious liver diseases with no effective treatments.Mori fructus aqueous extracts(MFAEs)have served as successful treatments for many types of liver injury including fibrosis although the molecular mechanisms are unknown at present.Purpose To investigate the effect of MFAEs in alleviating acute and chronic liver injury and tried to decipher the underlying mechanism.Methods and results Mice were divided into 5 groups(n ps:contro=8)for acute(groups:control,0.3%CCl_(4),bifendate(BD),100 and 200 mg/kg MFAEs,7 d)and chronic(groul,10%CCl_(4),BD,100 and 200 mg/kg MFAEs,4 weeks)liver injury study.Each mouse was injected intraperitoneally with 10μL/g corn oil containing CCl_(4)expect the control group.HepG2 cells were used in vitro study.Eighteen communal components were identified by UPLC-LTQOrbitrap-MS.We utilized a mouse model for acute and chronic liver injury using CCl_(4)and MFAEs administration effectively blocked fibrosis and significantly inhibited inflammation in the liver.MFAEs activated the nuclear factor erythroid derived 2 like 2/heme oxygenase 1(Nrf2/HO-1)pathway and promoted the synthesis of the antioxidants glutathione(GSH),superoxidedismutase(SOD)and glutathione peroxidase(GSH-Px)that resulted in reduced levels of CCl_(4)-induced oxidative stress molecules including reactive oxygen species.These extracts administered to mice also inhibited ferroptosis in the liver by regulating the expression of Acyl-CoA synthetase long chain family member 4(ACSL4),solute carrier family 7 member 11(SLC7A11)and glutathione peroxidase 4(GPX4),thus reducing the occurrence of liver fibrosis.Both in vivo and in vitro tests indicated that the mechanism of MFAEs protection against liver fibrosis was linked to activation of Nrf2 signaling.These effects were blocked in vitro by the addition of a specific Nrf2 inhibitor.Conclusion MFAEs inhibited oxidative stress,ferroptosis and inflammation of the liver by activating Nrf2 signal pathway and provided a significant protective effect against CCl_(4)-induced liver fibrosis.
基金Zhejiang Provincial Natural Science Foundation of China[LQ22H270014]the Chinese medicine science foundation of Zhejiang Province,China[2020ZA120]+1 种基金Quzhou technology projects,China[2022K53,2023K113,2023K120]Science and technology project of Zhejiang Provincial Drug Administration[2021013].
文摘Quzhou Aurantii Fructus(QAF)has a long history as a folk medicine and food for the treatment of liver diseases.While our earlier study provided evidence of hepatoprotective properties contained within the flavonoids and limonins constituents in QAF,the potential preventative effects afforded by essential oil components present within QAF remains enigmatic.In this study,we prepared Quzhou Aurantii Fructus essential oil(QAFEO)and confirmed its anti-inflammatory effects on liver inflammation through experimentation on lipopolysaccharide and D-galactosamine(LPS/D-GalN)induced acute liver failure(ALF)mouse models.Using RNA-sequence(RNA-seq)analysis,we found that QAFEO prevented ALF by systematically blunting the pathways involved in response to LPS and toll-like receptor signaling pathways.QAFEO effectively suppressed the phosphorylation of tank-binding kinase 1(TBK1),TGF-beta activated kinase 1(TAK1),interferon regulatory factor 3(IRF3),and the activation of mitogen activated kinase-like protein(MAPK)and nuclear factor-kappa B(NF-κB)pathways in vivo and in vitro.Importantly,QAFEO substantially reduced myeloid differentiation primary response gene 88(MyD88)-toll-like receptor 4(TLR4)interaction levels.Moreover,8 compounds from QAFEO could directly bind to REAL,TAK1,MyD88,TBK1,and IRF3.Taken together,the results of our study support the notion that QAFEO exerts a hepatoprotective effect through inhibiting LPS-mediated inflammatory response.
基金the National Natural Science Foundation of China(82004215,82173704,31870327,82003624,82004003)the Key Research and Development Program of China(2019YFC1711006,2017YFC1702002)+4 种基金the National Major Project of China(2018ZX09731016-005)Shanghai Engineering Research Center for the Preparation of Bioactive Natural Products(16DZ2280200)Shanghai Municipal Health Commission Project(20204Y0326)Science and Technology Commission of Shanghai Municipality(20YF1459000,20YF1458700)Sailing Program of Naval Medical University。
文摘Euodiae Fructus,referred to as“Wuzhuyu”in Chinese,has been used as local and traditional herbal medicines in many regions,especially in China,Japan and Korea,for the treatment of gastrointestinal disorders,headache,emesis,aphtha,dermatophytosis,dysentery,etc.Substantial investigations into their chemical and pharmacological properties have been performed.Recently,interest in this plant has been focused on the different structural types of alkaloids like evodiamine,rutaecarpine,dehydroevodiamine and 1-methyl-2-undecyl-4(1H)-quinolone,which exhibit a wide range of pharmacological activities in preclinical models,such as anticancer,antibacterial,anti-inflammatory,anti-cardiovascular disease,etc.This review summarizes the up-to-date and comprehensive information concerning the botany,traditional uses,phytochemistry,pharmacology of Euodiae Fructus together with the toxicology and quality control,and discusses the possible direction and scope for future research on this plant.
文摘Prohibited pesticide residues have become one of the main factors affecting the quality and safety of Lycii Fructus,However,rarely studies focus on the rapid determination of these residues.Here,a total of 30 kinds of prohibited pesticide residues were determined by ultra-performance liquid chromatography tandem triple quadrupole mass spectrometry(UPLC-MS/MS)in five different process ways.Pretreatment methods,chromatographic separation and detection conditions in mass spectrometry were all optimized accordingly.Among the five different pretreatment methods,the first and third solid phase extraction failed to provide high recoveries of sulfosulfuron compounds(both lower than 60%).Recovery of chlorphenamidine by the Quick Easy Cheap Effective Rugged and Safe multiresidue method(QuEChERS)was lower than 60%,which did not meet the requirements of trace determination.The concentrations of 30 prohibited pesticides residues treated by straightforward and solid phase extraction showed good linearity in their corresponding ranges,with correlation coefficients over 0.99.The average recoveries of straightforward ranged from 78.13%to 110.9%,while RSD ranged from 1.3%to 16.9%,albeit poor purification was observed.The recovery yield from solid phase extraction was between 67.75%and 103.08%with RSD value from 0.8%to 14.0%,which met the requirements of trace determination,this method has good precision and stability.These results could be employed to other Traditional Chinese Medicines(TCMs)in detecting prohibited pesticide residues.
文摘In this paper,the traditional identification and modern identification technology of Cnidii Fructus and its adulterant were reviewed,and their advantages,disadvantages and practicability were summarized,to provide a reference for the rapid and accurate identification and quality evaluation of Cnidii Fructus.
基金This work was supported by the Guangdong Basic and Applied Basic Research Foundation(2023A1515011106)General Project of Guangdong Provincial Enterprise Joint Fund(2022A1515220066)Project of Guangzhou Municipal Science and Technology Bureau(2023A04J1825).
文摘Forsythiae Fructus,a well-known traditional Chinese medicine preparation derived from the dried fruits of Forsythia suspensa(Thunb.)Vahl,has been historically utilized for its heat-clearing and detoxification properties.Forsythiae Fructus has been reported to exhibit antiviral activity such as against SARS-CoV-2 and influenza virus.This review highlights the recent updates on the effects and underlying action mechanisms of compounds in and active fractions from Forsythiae Fructus and Chinese formulae containing Forsythiae Fructus.
基金the National Natural Science Foundation of China(grant No.82160897,82205087)Hainan Provincial Natural Science Foundation of China(grant No.820RC635)+1 种基金Scientific Research Foundation of Hainan Medical University(grant No.HYPY201924,HYPY2020037)Hainan Medical University 2020 National Innovation and Entrepreneurship Program for College Students(grant No.202011810006).
文摘Background:In this study,we analyzed the potential active components,related crucial targets and possible signaling pathway mechanisms of Alpiniae Oxyphyllae Fructus and Saposhnikoviae Radix(AOF-SR)herb pairs in the treatment of diabetic kidney disease(DKD)using network pharmacology and verification experiments.Methods:The active compounds and potential targets of AOF-SR were derived from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,The Encyclopedia of Traditional Chinese Medicine,and PubChem databases,and the potential therapeutic targets of DKD were derived from the OMIM,Drugbank,and DisGeNET databases.The“compounds-diseases-targets”network was constructed using Cytoscape 3.6.0.ClusterMaker functionality in Cytoscape is being used to screen important targets for AOF-SR treatment of DKD.Gene Ontology and Kyoto Encyclopedia of Genes and Genomes enrichment analysis of important targets were performed using DAVID database.In addition,according to the predicted results of network pharmacology,HK-2 cells were used to construct DKD model for verification experiment.HK-2 cells were divided into control group,high glucose(HG)group and AOF-SR(HG+AOF-SR)group to detect survival rate and expression of key proteins in NF-κB and PI3K/Akt signaling pathways.Results:A total of 38 compounds were selected from AOF-SR,of which 23 were Alpiniae Oxyphyllae Fructus and 15 were Saposhnikoviae Radix.Through enrichment analysis of 82 important targets,88 signaling pathways were identified;some of these pathways,such as the NF-κB,PI3K-Akt,IL-17,and JAK/STAT signaling pathways,regulate the pathological process of DKD.In verification experiment,the HK-2 cells survival rate was higher in the HG+AOF-SR group than in the HG group(P<0.05).Moreover,western blotting results showed that the expression levels of NF-κB,p-PI3K,and p-Akt in HG+AOF-SR group were significantly lower than those in HG group(P<0.05).Conclusion:Overall,this study revealed the active compounds,important targets and possible mechanisms of AOF-SR treatment for DKD,and conducted preliminary verification experiments on its correctness,provided novel insights into the treatment of DKD by AOF-SR.
基金Supported by National Key Program of Innovation and Entrepreneurship Training for College Students (202211834021)Project Funds of Zhengzhou Science and Technology Bureau (ZZSZX202109).
文摘[Objectives]Optimum extraction conditions of total flavonoids from Fructus Aurantii Immaturus(TFFAI)and its resistance activity to ultraviolet radiation were investigated in present research.[Methods]The optimal extraction conditions of TFFAI were determined by single factor and orthogonal experiments,and the survival rate of TFFAI on HaCaT cells irradiated with UVB rays was investigated.It s antioxidant capacity was determined by ABTS.[Results]The results showed that the highest yield of TFFAI was obtained with 70%ethanol at a solid-to-liquid ratio of 1:50(w/v)and 40℃for 1.5 h by single-factor and orthogonal experiments.Total flavonoids(0.25-1.00 mg/ml)could significantly improve the survival rate of HaCaT cell line.Meanwhile,the maximum absorption peak of TFFAI was found at 283 nm,and in-vitro antioxidant experiment identified that TFFAI had a good clearance rate to ABTS.It suggestes that TFFAI could protect the cells from UVB damage by absorption of UVB rays and anti-oxidation.[Conclusions]TFFAI played a protective role on UVB irradiated cells through UVB ultraviolet absorption and antioxidant pathways.
基金supported by Natural Key R&D Program of China(No.2018YFC1707000).
文摘Background:The traditional Chinese medicine Toosendan Fructus has certain hepatotoxicity,which is used after being processed by stir-frying to attenuate toxicity.However,there are few studies on its attenuating toxicity mechanism.The effects of Toosendan Fructus on the activities of CYP450P1A2,CYP2E1 and CYP3A4 were studied in vivo and in vitro and the dose-toxicity mechanism of hepatotoxicity before and after stir-frying was explored to provide the basis for safe,rational use of Toosendan Fructus.Methods:The rat liver microsomes in vitro incubation method and in vivo pharmacokinetics were used to detect the concentrations of phenacetin,chlorzoxazone and dapsone in the liver microsomes in vitro incubation system and the rat plasma to study the effect of stir-frying of Toosendan Fructus on the activity of CYP450P1A2,CYP2E1,CYP3A4.Results:The results of pharmacokinetics in vivo showed that the AUC of phenacetin and dapsone in different groups was lower,and CL value was higher than those of the normal group.At the same dose,the AUC of stir-fried Toosendan Fructus was higher than that of the raw,while CL value was lower.For the same processed product,AUC value was high-dose>low-dose>middle-dose group,CL value was high-dose<low-dose<middle-dose.AUC and CL values of chlorzoxazone showed no difference from those of the normal group.The results of pharmacokinetics in vivo showed that Toosendan Fructus can induce the activity of CYP3A4 in a dose-dependent manner and the induction effect will decrease after stir-frying in vitro.Conclusion:The toxicity attenuation of Toosendan Fructus may be related to the decrease of induction effect after stir-frying.These results would provide the basis for safe,rational use of Toosendan Fructus.
基金supported by National Natural Science Foundation of China(No.21067004)Research Fund for the Doctoral Program of Jiangxi University of Science and Technology(22020)
文摘Objective It is imperative to provide some consistent experimental results for the extraction of flavonid from Fructus Gardeniae. Methods The key extraction parameters that influenced the yield of flavonid from Fructus Gardeniae were optimized by employing an orthogonal experiment [L9(3)4], including the ratio of buffer solution (Na2B4O7· 10H2O) to raw material, concentration of Fructus Gardeniae in extracting solution, extraction time and pH of buffer solution. An UV/Vis detector was used to perform the qualitative and quantitative analyses of the extracted flavonid with the using of the standard sample. Results The maximum extraction yield of the crude extract was 5.0533 (mg/g) after 20 min when the mass ratio of Na2B4O7 · 10H2O to raw material was 0.4%, the concentration of Fructus Gardeniae in the extraction solution was 1/12 (g/mL), and pH of buffer solution was 4.5. The positive reactions to the Molish and HCI-Mg tests suggested that the extracted compound was flavonoid, and FTIR measurements also identified the presence of flavonoid in the extracts. Conclusion This work is expected to provide a basis for further research, development, and utilization of Fructus gardenia in flavonid extraction.
基金Supported by National Natural Science Foundation of China,No.81473506Natural Science Foundation of Zhejiang Province,No.LY13H030011State Administration of Traditional Chinese Medicine of Zhejiang Province,No.2013ZB050
文摘AIM: To examine the effect of aqueous fructus aurantii immaturus(FAI) extracts on the intestinal plexus of cathartic colons.METHODS: Cathartic colons were induced in rats with dahuang,a laxative used in traditional Chinese medicine. Once the model was established(after approximately 12 wk),rats were administered mosapride(1.54 mg/kg) or various doses of aqueous FAI extracts(1-4 g/kg) for 14 d. Transit function was assessed using an ink propulsion test. Rats were then sacrificed,and the ultramicrostructure of colonic tissue was examined using transmission electron microscopy. The expression of the 5-hydroxytryptamine receptor 4(5-HTR4) and neurofilament-H was assessed in colon tissues using real-time PCR,Western blot,and immunohistochemistry.RESULTS: Mosapride and high dose(4 g/kg) of aqueous FAI extracts significantly improved the bowel movement in cathartic colons compared to untreated model colons as measured by the intestinal transit rate(70.06 ± 7.25 and 72.02 ± 8.74,respectively,vs 64.12 ± 5.19; P < 0.05 for both). Compared to controls,the ultramicrostructure of cathartic colons showed signsof neural degeneration. Treatment with mosapride and aqueous FAI extracts resulted in recovery of ultrastructural pathology. Treatment with mosapride alone upregulated the gene and protein expression of 5-HTR4 compared to untreated controls(P < 0.05 for both). Treatment with aqueous FAI extracts(≥ 2 g/kg) increased 5-HTR4 m RNA levels(P < 0.05),but no change in protein level was observed by Western blot or immunohistochemistry. The m RNA and protein levels of neurofilament-H were significantly increased with mosapride and ≥ 2 g/kg aqueous FAI extracts compared to controls(P < 0.05 for all).CONCLUSION: Aqueous FAI extracts and mosapride strengthen bowel movement in cathartic colons via increasing the expression of 5-HTR4 and neurofilament-H.
基金supported by the National Mega Project on Major Drug Development (No. 2009ZX09301-014-1)the National Scientific Foundation of China (Nos. 90817103,20775055,30973672)+1 种基金the start-up funds for ZC’s Luojia chair professorship of Wuhan University (Nos. 306276216,306271159)the Fundamental Research Funds for the Central Universities
文摘The qualitative and quantitative analysis of active constituents in Fructus Psoraleae is presented by high-performance liquid chromatography (HPLC) coupled with different detections.Extracts of Fructus Psoraleae were examined by HPLC with ion trap mass spectrometry (IT-MS) and 18 major compounds of coumarins,benzofuran glycosides,flavonoids,and meroterpene were identified.The determination of four major constituents including bavachin,isobavachalcone,bavachinin,and bakuchiol was accomplished by HPLC with UV,MS,and electrochemical detection (ECD).These methods were evaluated for a number of validation characteristics (repeatability,LOD,calibration range,and recovery).ECD obtained a high sensitivity for analysis of the four components;MS provided a high selectivity and sensitivity for determination of bavachin,isobavachalcone,and bavachinin in negative-ion mode.After optimization of the methods,separation,identification.and quantification of the four components in Fructus Psoraleae were comprehensively tested by HPLC with UV,MS,and ECD.