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Hyperlipidemia is a dyslipidemia caused by dyslipidemia of lipid metabolism， which can be divided into primary and secondary types. The current clinical diagnostic criteria are mainly changes in lipid levels， which are the inducers of high-risk cardiovascular diseases such as atherosclerosis， pancreatitis and coronary heart disease. As a key target in lipid metabolism， peroxisome proliferator-activated receptor α （PPARα） is involved in a variety of metabolic activities， including fatty acid degradation， synthesis， transport， storage， lipoprotein metabolism， etc. Activation of PPARα can maintain the balance of lipid metabolism through a variety of ways， which is an important way to treat hyperlipidemia. At present， chemical drugs such as statins and bettes are mainly used in the clinical treatment of hyperlipidemia. Although they can slow down the disease to a certain extent， there are many adverse reactions and drug resistance. By reviewing the literature in recent years， the author found that the activation of PPARα pathway by traditional Chinese medicine in the treatment of hyperlipidemia has significant effect and small adverse reactions. The lipid-lowering active ingredients include flavonoids， alkaloids， phenols， terpenoids and other compounds. These active components mainly affect the expression of downstream effectors through the activation of PPARα pathway， thereby inhibiting the synthesis of total cholesterol and promoting fatty acid oxidation， and play a role in the treatment of hyperlipidemia. In this paper， we systematically reviewed the structure types and mechanism of active components of traditional Chinese medicine that activate PPARα pathway， so as to provide guidance for the rational development and clinical application of lipid-lowering traditional Chinese medicine new drugs.
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Objective:To establish a method for the determination of four effective components in Paeoniae Radix Alba and evaluate its quality of Paeoniae Radix Alba by principal component analysis. Methods:The effective components of Paeoniae Radix Alba were extracted by ultrasonic extraction method with ethanol. Wondasil WR C18 chromatographic column (250 mm×4.6 mm,5 μm) was used, and the mobile phase was acetonitrile-water, the flow rate was set at 1 ml/min, the column temperature was set at 30 ℃, and the total operation time was 65 min. The mass score of active components was imported into SPSS for principal component analysis. Results:The linear ranges of Paeoniflorin, Paeoniflorin, Benzoyl Paeoniflorin and Pallyl Paeoniflorin were 0.020 1-3.820 0 μg ( r2=0.999 4), 0.015 9-2.850 0 μg ( r2=0.999 2), 0.008 2- 1.820 0 μg ( r2=0.999 1), 0.003 2-0.970 0 μg ( r2=0.999 5). The quality of the 10 batches of Paeoniae Radix Alba samples from Anhui province was the best, while that from Sichuan province was the worst. Conclusions:HPLC method was established for the determination of four effective components in Paeoniae Radix Alba, and principal component analysis and evaluation of 10 batches of Paeoniae Radix Alba. Bozhou, Anhui Province, was identified as the main production area of Paeoniae Radix Alba, which can provide reference for the quality control and preparation production of Paeoniae Radix Alba.
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Objective:To analyze the possible mechanism of Zuojin Pills on gastroesophageal reflux disease based on network pharmacology. Methods:By searching for the active constituent and protein targets of Zuojin Pills in TCMSP database,the protein names were converted into gene names in Uniprot database. Cytoscape 3.7.1 was used to draw the active constituent-target-medicine network diagram of Zuojin Pills and analyze the topological parameters. Then find the target of gastroesophageal reflux disease through OMIM,GeneCards,DRUGBANK database, find the intersection target of medicine and disease, perform PPI network analysis on the intersection target in STRING 11.0, and use the Metascape database to enrich the intersection target for further analysis. Cytoscape 3.7.1 was used to draw a network diagram of the active constituent- target-pathway of the medicine and to conduct a topology parameter analysis. Results:The main active constituent of Zuojin Pills in the treatment of gastroesophageal reflux disease are quercetin, Evodiamine, R-tetrahydroberberine, 1-methyl-2-nonyl-4-quinolone, berberine, etc. Targets include PTGS2, NOS3, MAPK1, EGFR, TNF, IL6, ERBB2, VEGFA, EGF, IL1B, etc., and these processes are mainly completed through inflammatory response, cancer, cell proliferation and apoptosis, cell connection, etc. Conclusions:The treatment of gastroesophageal reflux disease with Zuojin Pills is a complex process with multiple constituent, multiple targets, and multiple pathways. It is hoped that it which could provide reference for the future research on its mechanism of action.
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Objective:To predict the main active constituent, targets and signaling pathways of Huanglian-Jiedu Decoction against Helicobacter pylori infection by using network pharmacology, and to explore its potential mechanism, so as to provide objective foundation for the following experimental research. Methods:Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP) was used to screen the main active constituent and potential targets of Coptidis Rhizoma, Scutellaria baicalensis, Phellodendri Chinensis Cortex and Gardeniae Fructus in Huanglian-Jiedu Decoction. The targets related to Helicobacter pylori infection were screened by GeneCards suite database and human Mendelian genetic database (OMIM), and the intersection of Chinese herbs and disease targets was obtained. The Intersecting target were import into Cytoscape 3.7.2 to construct the network of active constituents and targets related to Helicobacter pylori infection. The protein protein interaction (PPI) network was constructed and analyzed by using string online analysis platform. Use R language to search Bioconductor platform online to enrich go function of targets. The enrichment of KEGG pathway was analyzed by David database. Results:total of 85 active constituent were screened from Huanglian-Jiedu Decoction, including quercetin, berberine, kaempferol, wogonin and baicalein. There are 112 corresponding targets, 1 960 disease-related targets and 71 common targets for herbal medicine and disease. Quercetin is the active constituent with the highest degree in the network diagram, and the target with the highest degree is cyclooxygenase-1 (PTGS1). In 69 nodes of PPI graph, the target proteins with the highest degree included CASP3, IL6, MAPK8, MYC, VEGFA and EGFR. A total of 89 items were obtained by GO functional enrichment analysis, and 12 signaling pathways with significant differences were screened by KEGG pathway enrichment analysis. Among them, pathways in cancer, ErbB Signal pathway, p53 signal pathway, apoptosis, and focal adhesion, which play a major role. Conclusions:Huanglian-Jiedu Decoction may treatm Helicobacter pylori with multi-component, multi-target and multi-pathway charateristics. At the same time, it may regulate the process of gastric cancer through anti-tumor mechanism, which could lay a foundation for the study of active components and anti-HP mechanism.
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Objective:This study aimed to determinate ten phenols (polydatin, resveratrol, rhein, emodin, chrysophanol, physcion, oxyresveratrol, 2,3,5,4'-tetera-hydroxystilbene-2-O-β-D-glucoside, (＋)-catechin and (-)-epicatechin) in Polygoni Cuspidati Rhizoma simultaneously based on the high-resolution multiple reaction monitoring (MRMHR) mode of ultra- performance liquid chromatography- quadrupole/time-of-flight mass spectrometry. Methods:The assay was performed on Waters ACQUITY UPLC BEH C18 (2.1 mm× 100 mm, 1.7 μm) column using acetonitrile-0.1% formic acid as the mobile phase. The flow rate was 0.2 ml/min. The MRMHR mode was adopted for quantification.Results:The analyzed compounds showed good linearity relationships ( r2>0.999). The intra- and inter-batch relative standard deviations were all <5% and the recovery rate was between 96.28%-103.23%. The content of polydatin was the highest, followed by resveratrol and emodin. However, the contents of chrysophanol and oxyresveratrol were relatively low and some batches were unqualified. The contents of analyzed compounds varied significantly among the ten batches. Conclusion:The proposed UPLC-Q/TOF-MS method was successfully established to determinate ten phenols in Polygoni Cuspidati Rhizoma simultaneously, which could provide technical support for the quality evaluation of Polygonum cuspidatum.
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Objective:To explore the potential mechanism of Jiajian Xuezheng Decotion in infiltrative gastric cancer by network pharmacology and proteomics.Methods:The Traditional Chinese Medicine Systems Pharmacology Database (TCMSP) database was used to find the compounds and their targets of Jiajianxuezhengtang, and the targets of invasive gastric cancer were determined by high performance liquid chromatography with tandem mass spectrometry (HPLC-MS/MS). The predicted target gene of Jiajian Xuezheng Decotion and the target protein data of infiltrative gastric cancer were analyzed by Venny to obtain the target gene. The target gene set was analyzed by Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment by the David. The protein interaction network diagram (PPI) was obtained by the String method, displaying the prescription-drug-compound-gene network in Cytoscape software.Results:69 active ingredients and 215 drug targets were screened from Jiajian Xuezheng Decotion; 660 proteins were significantly up-expressed in infiltrative gastric cancer, and 10 drug targets and gene targets were the common targets. There were 10 protein nodes in the PPI network, of which 3 core nodes were CASP3, BCL2L1 and STAT1. The 11 KEGG pathways were significantly enriched such as include PI3K-Akt signaling pathway, p53 signaling pathway, proteoglycan in cancer, apoptosis, Jak-STAT signaling pathway and other pathways.Conclusions:Jiajian Xuezheng Decotion plays an anti-infiltrative gastric cancer effect possibly regulated apoptosis through PI3K-Akt signaling pathway, p53 signaling pathway and Jak-STAT signaling pathway. This study provides a theoretical basis for further research on the mechanism of Jiajian Xuezheng Decotion in the treatment of invasive gastric cancer.
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Objective:To establish a method for quantitative analysis of the active ingredients including salidroside, rosarin and rosavin and content determination in Rhodiola rosea at different harvest months. Methods:HPLC was used on an X selectHSS T3 (250 mm×4.6 mm, 5 μm) column with mobile phase consisting of methol-acetonitrile-phosphoric acid (0.05%) aqueous solution for gradient elution at a flow rate of 1 ml/min. The wavelength was detected at 275 nm (salidroside) and 254 nm (rosarin, rosavin). The column temperature was set at 30 ℃ and the injection volume was 5 μl.Results:The peak areas of Salidroside, rosarin and rosavin showed good linear relationships ( r > 0.999) with the content in the ranges of 44-1 420, 10-307 and 18-573 μg, respectively. The method was precise, stable, repeatable and the sample recovery test all well satisfied the requirements of quantitative analysis. The highest accumulation of the active ingredients was observed in Rhodiola rosea in September and the content of salidroside, rosarin and rosavin were 0.66, 0.07 and 0.53 mg/g, respectively. Conclusion:This method is simple and rapid to evaluate the content of active ingredients in Rhodiola rosea.
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Objective:To establish the TLC identification method and content determination method of ferulic acid, ligustilide, hydroxysafflor yellow A and paeoniflorin in Shangke Huoxue Decoction for quality evaluation.Methods:Ferulic acid, ligustilide, hydroxysafflor yellow A and paeoniflorin were qualitatively identified by TLC method, and the content was determined by HPLC method. Waters Symmetry ShieldTM RP18 column (4.6 mm×250 mm, 5 μm) was set, the mobile phase consisted of acetonitrile-0.15% phosphoric acid water with gradient elution at a flow of 1.0 ml/min, and the column temperature was 30 ℃.The detection wavelength was 320 nm (33-50 min for ferulic acid, 55-70 min for ligustilide), 403 nm (7-31 min for hydroxysafflor yellow A) and 230 nm (7-31 min for paeoniflorin).Results:The TLC spots were clear. The linear relationships of ferulic acid, ligustilide, and hydroxysafflor yellow A were good in the range of 3.05-48.74 μg, 3.50-26.24 μg, 21.34-213.44 μg. The method was stable, repeatable with good recovery rate.Conclusion:The TLC and HPLC method for the simutanous determination of the four effective components in Shangke Huoxue Decoction were established, and the methods are suitable for the quality evaluation of Shangke Huoxue Decoction.
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Linarin, as a natural coumponent belongs to flavonoid glycoside, is widely existed in herbal plants such as chrysanthemum indicum and Mongolian flower, which has a variety of pharmacological effects, such as anti-inflammation, anti-cancer, liver protection, analgesia, antipyretic, anti-oxidation, anti-apoptosis, sedation and sleep, neuroprotection, preventing and treating hypertension, treatingdiabetes, preventing and treating osteoporosis, whitening, skin care and sunscreen. It is difficult to dissolve in water and has poor oral efficacy, but when combined with different substances or combined (forming phospholipid complex), its bioavailability can be improved, so as to improve its pharmacological efficacy.
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Objective:By using the network pharmacology method to predict the active constituents and action targets of Suzi-Jiangqi Decoction in the treatment of COPD, and to explore its potential molecular mechanism with multi-component, multi-target and multi-pathway characteristics. Methods:The active constituents and targets of Suzi-Jiangqi Decoction were collected, screened and predicted according to the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP) and UniProt software. Search for the gene targets related to COPD in GeneCards, online human Mendelian genetic database (OMIM) and TTD database. The intersection targets of component targets and disease targets were obtained by Veen map online software. The network model with the sequence of active constituents-target-disease was constructed and analyzed by Cytoscape software, and the protein-protein interaction network (PPI) was constructed by STRING database. The gene ontology function annotation (GO) and Tokyo genome encyclopedia (KEGG) pathway enrichment analysis of common targets with metascape online tool. Results:A total of 163 active constituents of Suzi-Jiangqi Decoction were screened, 283 targets were predicted, and 159 targets involved in the treatment of COPD. Quercetin, kaempferol, naringin and luteolin were the key active ingredients. IL6, TNF, MAPK3, JUN, CASP3, CXCL8, CXCL10, MMP9 and MAPK1 were important gene targets. GO analysis showed that the biological processes involved in the enrichment of key gene targets included the response to bacteria, the cytokine mediated signaling pathway, the cell's response to inorganic substances, the response to oxidative stress, the response to LPS, and so on. The enrichment analysis of KEGG pathway showed that the signaling pathway of Suzi-Jiangqi Decoction in the treatment of COPD included TNF signaling pathway, IL-17 signaling pathway, cell cycle, Influenza A, HTLV-I infection, AGE-RAGE signaling pathway, Tuberculosis, Epstein-Barr virus infection and so on. Conclusion:Suzi-Jiangqi Decoction can treat COPD through multi-target and multi-pathway mechanisms of anti-inflammatory, anti infection and immune regulation, which lays a foundation for further study of its molecular mechanism.
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Objective:With network pharmacology, this paper aims to explore the potential active constituents, related targets and signal pathways to elucidate the mechanism of Calyx seu Fructus Physalis in the treatment of lung cancer. Methods:By searching for Pharmacology Database of Traditional Chinese Medicine Systems and Analysis Platform (TCMSP) to obtain the active constituents of Calyx seu Fructus Physalis, and predict the target genes of active constituents by using SWISS and SEA. By collecting the corresponding targets approved by FDA and search for different database, including Therapeutic Target Database (TTD), Database of Gene-disease Associations (DisGeNET) and Online Mendelian Inheritance in OMIM to build a database of lung cancer related target genes; To get the target genes of herb-disease proteins by the intersection of the two databases and display the results through the network software of Cytoscape 3.7.2. Then to use the Database of Annotation, Visualization and Integrated Discovery (DAVID) to conduct key enrichment analysis of Kyoto Gene and Genome Encyclopedia (KEGG) pathway enrichment analysis. Combining related literature to analize the active ingredients and mechanism of Calyx seu Fructus Physalis in the prevention and treatment of lung cancer. Results:It was found that 11 active constituents of Calyx seu Fructus Physalis could play the role of anti-lung cancer by regulating 19 lung cancer related targets such as EGFR, ESR1, MDM2, MMP2 and MET. There were 15 signal pathways involved Proteoglycans in cancer, MicroRNAs in cancer, Pathways in cancer, Transcriptional misregulation in cancer, PI3K-Akt signaling pathway and other key signal pathways. Conclusion:The results show that the active constituents of anti-lung cancer effect of Calyx seu Fructus Physalis may be Oleic acid, Cycloartenol, Obturator, Graminesterol, β-sitosterol, etc. The mechanism of action may be related to multiple cancer-related signaling pathways such as Proteoglycans pathway, Transcriptional misregulation pathway, and PI3K-Akt signaling pathway.
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OBJECTIVE：To s tudy the intestinal absorption differences of 6 kinds of active constituents of Polygonum orientale （kaempferol，isokaempferol，vitexin，protocatechuic acid ，kaempferol-3-O-β-D-glucoside and quercetin ）in normal and myocardial ischemia（MI）model rats. METHODS ：UPLC-MS/MS method was adopted to determine the contents of 6 active components in the intestinal circulatory perfusion fluid. Totally male SD 80 rats were divided into normal group and model group ，with 40 rats in each group. Model group was given isoproterenol hydrochloride （50 mg/kg） subcutaneously to induce MI model；normal group was given constant volume of normalsaline， once a day ， for consecutive 2 days. 24 h after successful molding ，normal group and model group received in-situ intestinal circulatory perfusion experiment. The effects of different concentration s of P. orientale extract（5.0，10.0， 20.0 mg/mL），different intestinal segments （duodenum，jejunum，ileum，colon），P-glycoprotein（P-gp）inhibitors（verapamil） and bile on the intestinal absorption of each constituent were explored. RESULTS ：The linear ranges of concentrations of kaempferol， isokaempferol， vitexin， protocatechuic acid ， kaempferol-3-O-β-D-glucoside and quercetin were 3.15-50.40， 3.21-51.31，1.63-52.43，1.60-50.94，1.31-20.97，8.07-129.25 µg/mL（r＞0.999）. The lower limits of quantification were 7.86， 8.45，6.52，4.00，3.28，16.14 ng/mL，respectively. RSDs of precision ，matrix effect and stability tests were all lower than 11％； the accuracy were 85.64％-107.65％，which were in line with the requirements of biological sample quantification analysis. Except for there was no statistical significance in the absorption of kaempferol absorption in duodenum of model group at different concentrations，absorption of other five constituents in duodenum of normal and model rats increased with the increase of the concentration of active constituents ，and absorption of medium- and/or high- concentration active constituents （except quercetin ）in model group was significantly lower than normal group （P＜0.05）. In normal group ，the absorption of kaempferol was more in jejunum，ileum and colon ，isokaempferol was more in ileum ，vitexin and protocatechuic acid were more in jejunum and ileum ， kaempferin-3-O- β-D-glucoside was more in duodenum ，jejunum and colon ，quercetin was more in colon ；in the model group ，the absorption of Polygonum orientale in jejunum and colon was more ，the absorption of isokaempferol in 4 intestinal segments was little different ，vitexin was mainly absorbed in ileum ，protocatechuic acid and kaempferol- 3-O-β-D-glucoside was mainly absorbed in jejunum ，quercetin was mainly absorbed in duodenum and ileum ；in the same intestine ，the absorption of constituents in the model group was less than normal group. After adding verapamil ，absorption of all constituents in the normal group increased ，but the difference was not statistically significant （P＞0.05）；absorption of kaempferol ，isokaempferol，vitexin，protocatechuic acid and kaempferol- 3-O-β-D-glucoside were all increased significantly in model group （P＜0.05），while there was no statistical significance in the increase of quercetin （P＞0.05）. After the bile flowed into the duodenum ，absorption of protocatechuic acid was increased significantly in normal group （P＜0.05）；absorption of other active constituents were increased significantly in model group，except for isokaempferol and quercetin （P＜0.05）. CONCLUSIONS ：Six active constituents of P. orientale were absorbed in the whole intestine of normal and MI model rats ，and the absorption of above constituents may be enhanced more significantly by P-gp inhibitor and bile under pathological condition.
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OBJECTIVE：To evaluate the correlation between color difference values and active constituent contents of crude and processed Zingiber officinale . METHODS ：HPLC method was adopted to determint the content of 6 active constituents. The color difference values of crude and processed Z. officinale [lightness（L＊），red-green axis component （a＊），yellow-blue axis component（b＊）] were determined by chromatic aberration meter . SPSS 24.0 software was adopted for the correlation analysis between color difference values and active constituent contents. RESULTS ：The linear range of zingiberone ，6-gingerol， 8-gingerol， 6-shogaol， diacetoxy-6-gingerol and 10-gingerol were 2.65-105.90， 10.15-406.00， 4.87-194.80， 5.28-211.20， 6.14-245.70，7.02-280.80 μg/mL（r＞0.999）. The limits of quantification were 7.46，13.68，14.37，16.62，17.03，17.99 ng，and the limits of detection were 2.24，4.11，4.31，4.99，5.11，5.40 ng，respectively. RSDs of precision ，stability，and repeatability tests were all lower than 3％. The average recovery rates were 101.34％，102.14％，101.22％；103.12％，103.74％，103.54％；103.06％，properties critical for cell migration and invasion. induced EMT through downregulation of NF-κB-Snail sig- naling in breast cancer cells enchymal transition and activation of TLR 4/JNK signal - 98.55％，99.43％；99.36％，103.51％，101.21％；100.85％，99.42％，99.60％；100.39％，97.69％，103.84％（RSD were all lower than 3％，n＝3），respectively. The contents of them were 0-0.66，0.06-7.57，0.03-1.45，0.29-3.47，0.15-2.85，0.04-2.83 mg/g， respectively. L＊ and b＊ values were negative correlated with the processing degree of Z. officinale significantly（P＜0.01），a＊ showed a significantly positive correlation with the processing degree （P＜0.05）. L＊and b＊ values showed a significantly negative correlation with the content of zingiberone before and after processing ，but positively correlated with the other five components （P＜0.01）. a＊ showed a significantly positive correlation with the content of zingiberone ，but had no correlation with other five components（P＞0.05）. The crude and processed Z. officinale were positive correlated with the content of zingiberone ，negatively correlated with other five components （P＜0.01）. CONCLUSIONS ：There is a certain correlation between the color difference values of crude and processed Z. officinale and the contents of their active constituents. With the deepening of the processing ，a＊ values is increased ，L＊ values and b＊ values is decreased ；the content of zingiberone increases ，the contents of 6-gingerol， 8-gingerol，6-shogaol，diacetoxy-6-gingerol，10-gingerol reduce.
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OBJECTIVE： To study the anti-inflammatory and detumescent pharmacodynamic material basis of Jingyaokang capsule， and to provide reference for secondary development， the establishment of quality control method and technological upgrading of the preparations. METHODS： The constituents of Jingyaokang capsule were extracted and separated with different solvents and macroporous adsorption resin to obtain constituent A （overall enrichment part）， constituent B （chloroform extraction part）， constituent C （water-course part） and constituent D （elution part of 60％ ethanol）. Using dexamethasone acetate as positive control， the anti-inflammatory and detumescent effects of Jingyaokang capsule and different extraction parts （constituents A， B， C， D） were investigated by mice ear edema and rat paw edema tests to screen the active fraction. UPLC-Q-TOF-MS method was used to analyze active constituent， identify compounds and attribute medicinal material. RESULTS： Anti-inflammatory and detumescent effects of constituent B （chloroform extraction part）+constituent D （elution part of 60％ ethanol） were similar to those of Jingyaokang capsule in rats or mice， indicating both had synergistic anti-inflammatory and detumescent effects and were active constituents of Jingyaokang capsule. UPLC-Q-TOF-MS detection and identification showed that constituent B contained 13 compounds as strychnine， phellodendrine， periplogenin， tetraketone alcohol， 11-carbonyl-β-mastic acid， attributing to Strychnos nux-vomica， Stephania tetrandra， Periploca sepium， Lycopodium japonicum， Boswellia carterii， etc. Constituent D contained 7 compounds as adenine， hydroxysafflower yellow A， phellodendrine， neoeriocitrin， zingibroside R1， attributing to rainworm， Carthamus tinctorius， Stephania tetrandra， Davallia mariesii， Achyranthes bidentata， etc. CONCLUSIONS： Jingyaokang capsule shows the significant anti-inflammation and detumescent effects. The chloroform extraction part is synergistic with 60％ ethanol elution part， which are the active constituents of anti-inflammation and detumescence，mainly including alkaloids， flavonoids and boswellic acids.
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Herbal medicines, mainly of plant source, are invaluable source for the discovery of new therapeutic agents for all sorts of human ailments. The complex pathogenesis of stroke and multifactorial effect of herbal medicine and their active constituents may suggest the promising future of natural medicine for stroke treatment. Anti-oxidant, anti-inflammatory, anti-apoptotic, neuroprotective and vascular protective effect of herbal medicines are believed to be efficacious in stroke treatment. Herbs typically have fewer reported side effects than allopathic medicine, and may be safer to use over longer period of time. Herbal medicines are believed to be more effective for the longstanding health complaints, such as stroke. Several medicinal plants and their active constituents show the promising results in laboratory research. However failure in transformation of laboratory animal research to the clinical trials has created huge challenge for the use of herbal medicine in stroke. Until and unless scientifically comprehensive evidence of the efficacy and safety of herbal medicine in ischemic stroke patients is available, efforts should be made to continue implementing treatment strategies of proven effectiveness. More consideration should be paid to natural compounds that can have extensive therapeutic time windows, perfect pharmacological targets with few side effects. Herbal medicine has excellent prospective for the treatment of ischemic stroke, but a lot of effort should be invested to transform the success of animal research to human use.
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Animals , Humans , Brain Ischemia , Drug Therapy , Herbal Medicine , Neurons , Pathology , Neuroprotection , Phytotherapy , Stroke , Drug TherapyABSTRACT
The study aims to investigate the effective components of Semen Ziziphi Spinosae (SZR) in nourishing the heart and tranquilizing the mind. A method of ultra high liquid chromatography (UHPLC) coupled with Q Exactive high resolution mass spectrometry (HR-MS) was developed. Based on the UV spectra, retention time and MS spectra, 25 compounds of SZR extract were identified or tentatively characterized, including 12 flavonoids, 8 triterpenoids saponins, 2 fatty acid and 3 alakoids. The study illuminated the major chemical components. Twenty bioactive components were determined in rat urine after oral administration of SZR extract by "in vitro to in vivo" translation approach, including 16 prototype compounds and 4 metabolites. Spinosin, swertisin, jujuboside A and B were considered as the effective and active constituents in SZR of the sedative and hypnotic effects, which emodies characteristics of multiple components. It was beneficial exploration for searching the effective and active constituents of SZR in nourishing the heart and tranquilizing the mind.
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OBJECTIVE:To explore the effects and mechanism of extracts,active constituents and constituent combination of Sinopodophylli Fructus on cell proliferation of human breast cancer. METHODS:Acid phosphatase method was conducted to deter-mine the effects of 4 extracts [ethanol extract (Xc),petroleum ether extract from ethanol extract (Xp),ethyl acetate extract from ethanol extract (Xe),n-butanol extract from ethanol extract (Xz)],5 active constituents [podophyllotoxin (S1),deoxypodophyllo-toxin (S2),4-desmethyl deoxypodophyllotoxin (S3),8-isopentenyl kaempferol (S4),8,2′-diisoprenyl quercetin-3-methyl ether (S5)] and 3 active constituent combination [combination 1,S1-S2-S3-S4-S5 (2:4:1:4:32),Z1;combination 2,S2-S4 (1:1),Z2;combination 3,S3-S4(1:4),Z3] on the MDA-MB-231,MCF-7 cell proliferation;flow cytometry was adopted to detect the effects of above-mentioned samples on MDA-MB-231,MCF-7(T47D)cell cycle and mitochondrial membrane potential. RESULTS:The active constituent combination Z1 showed significant inhibitory effects on MDA-MB-231,MCF-7 cells,the half inhibitory concen-trations(IC50)were(0.27±0.2),(0.11±0.1)μg/mL;extracts Xc,Xp,Xe,active constituents S2,S4 and active constituent combi-nation Z2,Z3 showed relatively strong inhibitory effects on MDA-MB-231,MCF-7 (T47D) cell proliferation (IC50<15 μg/mL). Both extracts and active constituents can block MDA-MB-231,MCF-7 cell cycle in G2/M phase;all active constituents can block MDA-MB-231,T47D cell cycle in G0/G1 phase,and can reduce MDA-MB-231,T47D cell mitochondrial membrane potential. CONCLUSIONS:The active constituents and constituent combination of Sinopodophylli Fructus can inhibit cell proliferation of breast cancer by affecting cell cycle and mitochondrial mem-brane potential.
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In the present research, 674 wild medicinal material samples of Phellodendri amurensis Cortex were collected from 31 sampling sites in the whole distribution of its original plant Phellodendron amurense. The samples were collected under the premise that the stem diameter of sampling plant, sampling position and time were controlled. And the sampling sites were set at the interval of a latitude. The content of 6 kinds of active ingredients, palmatine chloride, berberine hydrochloride, phellodendrine chloride, jatrorrhizine hydrochloride, magnoflorine, chlorogenic acid, etc in the medicinal material samples were determined, and the results showed that the content of most active ingredients in the medicinal materials showed significant differences due to the difference of sampling sites. Among them, the medicinal materials from Liaoning region had the highest content of active ingredients, followed by Beijing and Jilin regions, and that from Heilongjiang region had the lowest content. The study has important directive significance to the exploration of environmental factors for the formation of active constituent and artificial planting regionalization of high quality Phellodendri amurensis Cortex.
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To point out the current problems on the water extraction process in the preparation of patent medicine or single medicine recorded in Chinese Pharmacopoeia 2010, and to provide the references for the next Chinese Pharmacopoeia and the water extraction technology of traditional Chinese patent medicine (CPM) industry. According to Chinese Pharmacopoeia 2010 and literature at home and abroad, the four basic stages of extraction were analyzed and the problems on the low transfer rate of active constituents by water extraction were discussed. In the four stages of water extraction process, any stage that was limited led to the low transfer rate of active constituents or even influenced the drug's efficacy directly. Not only the poor permeability of water, but also the high oil and macromolecular components in Chinese herbs could limit the infiltration with water as solvent. In desorption and dissolution stages, the poor solubility of nonpolar and medium polarity components with a low affinity for water was difficult to dissolve completely. In diffusion stage, the active constituents in Chinese materia medica were difficult to penetrate the cellular barrier and spread to the water due to the larger molecular weight. In substitution stage, coexisting macromolecular substances affect the other mass exchanges on both sides of cell biological membrane in the process of material mutual exchanges. It is the common problem that water extraction ratio of CPM is low. It is also the urgent problem of Chinese Pharmacopoeia to be solved, or it will definitely hinder the development of industrial CPM. Insiders should pay more attention to this problem and take new ideas to solve it.