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OBJECTIVE To analyze the main components of Chelidonii Herba-Corydalis Rhizoma （CHCR）， and to predict pharmacodynamic substances against estrogen receptor （ER） -positive breast cancer and their potential targets and signaling pathways， followed by verifying experiments. METHODS The ethanol extract of CHCR was analyzed by ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry （UPLC-Q-TOF-MS/MS）. The network pharmacology analysis was performed for the screened components. The network diagram of CHCR “active components-target-pathway” was constructed， and the enrichment pathway in vitro was validated. RESULTS A total of 58 chemical components were identified， including 57 alkaloids and 1 organic acid. A total of 38 active ingredients were screened from the network pharmacology， and 38 core targets were found in the protein-protein interaction network of “component-disease” intersection targets； 258 gene ontology entries and 137 Kyoto encyclopedia of genes and genomics pathways were obtained， mainly including estrogen signal pathway， phosphatidylinositol-3-kinase/protein kinase B （PI3K/Akt） signal pathway， etc. The results of validation test showed that the median inhibitory concentration of CHCR to MCF-7 cells was 693 μg/mL； 150， 300， 600 μg/mL CHCR could significantly reduce the expressions of phosphorylated PI3K， phosphorylated Akt， ERα protein and ESR1 mRNA （P＜0.01）. CONCLUSIONS The anti-ER-positive breast cancer effect of CHCR may be related to the regulation of ER and PI3K/Akt pathways， which has the characteristics of multi-component and multi-target effects.
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OBJECTIVE To study the pharmacological basis of Schisandra chinensis in the treatment of allergic asthma. METHODS The common components of 10 batches of S. chinensis from different habitats were analyzed by UPLC-Q-TOF-MS/MS. Furthermore， the allergic asthma model was established by intraperitoneal injection of ovalbumin （OVA） and aluminum hydroxide for stimulation combined with atomization exitation； general behavioral observation and the contents of interferon γ （IFN-γ）， interleukin-4 （IL-4） and immunoglobulin E （IgE） in serum were taken as criteria for evaluating the therapeutic effect of S. chinensis from different habitats in the treatment of allergic asthma. Correlation coefficients between common peak area and efficacy evaluation index of each batch of medicinal material were analyzed through grey correlation degree and Pearson correlation analysis. RESULTS A total of 21 common components were identified in 10 batches of S. chinensis from different habitats. After administration of S. chinensis， symptoms such as shortness of breath， sneezing and curling of rats were alleviated. In addition， the content of IFN-γ was significantly increased while the contents of IL-4 and IgE in serum were distinctly decreased （P＜0.01）. Grey correlation analysis showed that 11 common components had high correlation coefficients with IFN-γ， IL-4 and IgE （rˉ＞0.8）. Pearson correlation analysis showed that 8 components were significantly positively correlated with the content of IFN-γ （P＜ 0.05）， and 9， 8 components were significantly negatively correlated with the content of IL-4 and IgE （P＜0.05）. Based on the results of grey correlation degree and Pearson correlation analysis， 7 components such as peak 3， 4， 6， 7， 9， 19 and 20， were highly related to S. chinensis in the treatment of allergic asthma. CONCLUSIONS Schisandrol A， schisandrin B， schisandrin C， gomisin M2， gomisin J， pregomisin and angeloylgomisin H are the potential pharmacodynamic substance basis of S. chinensis in the treatment of allergic asthma.
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OBJECTIVE：To study the prepar ation technology of gastric floating tablets of Schisandra chinensis total lignans （SCTL），and evaluate the quality of prepared tablets. METHODS ：Based on single factor test ，the orthogonal experiment was conducted to optimize the formulation of SCTL gastric floating tablets with the contents of hydroxypropylmethylcellulose （HPMC） K15M，NaHCO3 and microcrystalline cellulose as the factors ，using starting time ，holding time and cumulative release rate of gastric floating tablets as evaluation indexes. The properties ，weight difference ，floatability and accumulative release rate of the prepared SCTL gastric floating tablets were determined. The gastric floating tablets were qualitatively identified by TLC ，and the contents of schisandrin A and total lignans were determined by HPLC and UV spectrophotometry. RESULTS ：The optimal formulation of SCTL gastric floating tablets was made up of 23％ SCTL extract ，20％ HPMC K 15M，40％ microcrystalline cellulose，15％ sodium bicarbonate ，1％ octadecyl alcohol and 1％ polyvinylpyrrolidone. The results of detection of this preparation were in line with the related provisions of “0101 tablet”stated in 2015 edition of Chinese Pharmacopoeia （part Ⅳ）. TLC indicated that the chromatogram of the test sample showed the main spots of same color as the corresponding positions of the chromatogram of schizandrol A control ，Schisandra chinensis reference substance and raw material ，while the negative control has no interference. Content determination results shows that the average content of schizandrol A and total lignans in SCTL gastric floating tablets is 3.187，19.617 mg. It was preliminarily formulated that the content limitation of schizandrol A in one tablet should not be less than 2.50 mg，and the content of total lignans （calculated by schizandrol A ）should not be less than 15.50 mg. CONCLUSIONS：The preparation technology of SCTL gastric floating tablets is stable ，feasible and controllable in quality.
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Microtubule inhibitor has been a hot area of anticancer drugs research.Microtubule inhibitor exert an anti-tumor effect by promoting or inhibiting the microtubule aggregation to break the dynamic balance of microtubule,hindering the spindle forma-tion of tumor cells,and then blocking the process of cell divi-sion.Mitotic catastrophe is a cell death phenomenon that is caused by abnormal cell division and damage of spindle structure in cell mitosis phase.In recent years more and more attention has been paid to mitotic catastrophe cell death because it has been confirmed clinically that microtubule inhibitors can induce mitotic catastrophe death of tumor cells.This paper reviews the latest research progress of microtubule inhibitors,and discusses the molecular mechanisms of mitotic catastrophe cell death tumor cells induced by microtubule inhibitors.
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Objective To explore the effects of humulon on kinetic parameters of N-acetyltransferase-1(NAT1) of human gastric cancer SGC-7901.Methods Employing HPLC,using para-aminobenzoic acid(PABA) as substrate,in intact SGC-7901 cells and their cytoplasm,taking the speed of PABA being acetylated to Ac-PABA by NAT1 as the rate of NAT1,using double reciprocal plot,taking the reciprocal of concentration of PABA and reaction rate of NAT1 as coordinates,regression equation was obtainied and the Michaelis constant(Km) and maximum reaction velocity(Vmax) were calculated.Results Study on enzyme kinetics demonstrated,as for intact SGC-7901 cells,Km and Vmax of control group were(3.910?0.087) ?mol/L and(0.306 0?0.006 7) pmol/L(1?106 cells),respectively,Km and Vmax of the humulon group were(3.830?0.123) ?mol/L and(0.275 0?0.005 8) pmol(1?106 cells),respectively.As for the cytoplasm of SGC-7901 cells,Km and Vmax of control group were(760.2?210.2) ?mol/L and(0.191 0?0.043 7) pmol/(mg?min),Km and Vmax of the humulon group were(449.0?72.9) ?mol/L and(0.094 0?0.010 4) pmol/(mg?min).Statistically,as for intact SGC-7901 cells or their cytoplasm,there was no difference of the Km between control group and humulon group,but there was remarkable difference of Vmax between control group and humulon group,P
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Objective To study the anti-tumor effects of humulon on arylamine N-acetyltransferase-1(NAT1)activity.Methods Employing HPLC,using PABA as substrate,in intact SGC-7901 cells and their cytoplasm,making PABA being acetylated to Ac-PABA by NAT1 as the activity of NAT1.Reverse transcriptase polymerase chain reaction(RT-PCR)assay was used to study the expression of the NAT1 mRNA.Results The results show that humulon could inhibit the production of Ac-PABA in intact SGC-7901 cell and the cytoplasm,the production of Ac-PABA was gradually increased with the interaction time increasing.But comparing with corresponding negative control group's,the production of Ac-PABA was decreased evidently and the humulone could inhibit the expression of NAT1 mRNA.Conclusion Humulon could prevent the occurrence and deterioration of cancer.Its mechanisms can be attributed to its effect on decreasing the production of acetylation of carcinogenic aromatic amines,which is acetylated from aromatic amines,and inhibiting the NAT1 activity and expression of NAT1 mRNA.