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AIM: To explore the mechanism of action of alkaloid components of compound kushen Injection (CKI) in the treatment of lung cancer based on serum metabolomics, network pharmacology, and molecular docking techniques. METHODS: A lung cancer model was established in C57 mice by inoculation of Lewis mouse lung cancer tumor strain. Thirty male mice were randomly divided into normal group, model group and CKI group. The drug was administered by tail vein injection once daily for 17 consecutive days. Mouse serum was examined by ultrahigh performance liquid chromatography tandem mass spectrometry (LC-MS) metabolomics, and several multivariate statistical analyses including principal component analysis (PCA) and orthogonal partial least squares discriminant analysis (OPLS-DA), combined with databases such as the human metabolic database (HMDB) and related literature to identify and identify differential metabolites, the relevant metabolic pathways were searched for by the metaboanalyst online tool. Using network pharmacology, construct the“component-target-disease”network of CKI in the treatment of lung cancer. Molecular docking method was used to verify the interaction between potential active ingredients and core targets. Serum metabolomics was jointly analyzed with network pharmacology to construct a“metabolite-germinal-enzyme-gene” network. RESULTS: Through metabolomics technology, 16 differential metabolites associated with lung cancer were screened from serum, and CKI addback these differential metabolite levels compared with the model group. Metabolic pathways mainly involve retinol metabolism, tryptophan metabolism, glycerophospholipid metabolism and other metabolic pathways. Network pharmacology analysis indicated that CKI treatment of lung cancer mainly targets STAT3, MAPK3, and MAPK1, which are closely related to proteoglycans, cellular senescence, and HIF − 1 signaling pathways in cancer. CONCLUSION: This article explains the mechanism of CKI in treating lung cancer from the perspective of metabonomics and network pharmacology, and provides basis for further study of CKI.
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AIM: To study the effect of Qingdaipowder Gel (QDPG) on mice specific dermatitis (AD) model and the antibacterial effect of the ethanol extract of Qingdaipowder. METHODS: AD model of mice was established by repeated skin induction with 2,4-dinitrochlorobenzene (DNCB). Fifty-six mice were randomly divided into blank group, model group, Hydrocortisone Butyrate Cream group (Hyd, 1.5 mg/cm
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AIM: To investigate the effect of an effective component total sterone (TSR) of Echinops latifolius Tausch, the main component of a Chinese patent medicine Cuiru Keli (national drug standard WS3-413 (Z-085)-2003 (Z), on lactation and its possible mechanism. METHODS: After mating between male and female SD rats, 60 female rats were randomly divided into normal control group, model group, TSR low-dose and high-dose groups and prolactin granule positive control group, with 12 female rats in each group and 8 newborn rats in each nest. In addition to the normal control group, the rats in each group were intraperitoneally injected with levodopa 2 mg/kg once a day for 7 days from the second day of delivery. The rats in the normal control group were given normal saline by gavage once a day for 14 days. From the beginning of self-sufficiency, the single lactation of the female rats was measured every day until the 14th day, and then the female rats in each group were killed. Pathological HE staining was used to observe the morphological changes of mammary gland tissue in each group. ELISA was used to detect the levels of serum prolactin (PRL) and 5-hydroxytryptamine (5-HT). Immunohistochemistry was used to detect the distribution of PRL in mammary gland tissue of each group. Furthermore, Real-time qPCR was used to detect the expression of milk protein, milk fat related genes β-casein, FAS, ACC and the expression of canonical Wnt signaling pathway related genes β-catenin, c-Myc, CCND1, SFRP4, DNMT1, MeCP2 in mammary gland of each group. RESULTS: Both low and high dose TSR could significantly increase the single lactation volume, improve the pathological morphology of mammary gland, and increase the serum levels of PRL and 5-HT. TSR increased the distribution of PRL and up-regulated the expression of milk protein, milk fat related genes β-casein, FAS, ACC and canonical Wnt signaling pathway related genes β-catenin, c-Myc, CCND1, SFRP4, DNMT1, MeCP2.CONCLUSION: TSR can significantly promote lactation in lactation deficient rats, and its mechanism may be related to promoting the release of PRL and 5-HT in serum, increasing the distribution of PRL in mammary gland, up-regulating the milk protein and milk fat related genes and activating the canonical Wnt signal.
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Deoxyglycychloxazol (TY501) is a glycyrrhetinic acid derivative which exhibits high anti-inflammatory activity and reduced pseudoaldosteronism compared to glycyrrhetinic acid. In this study, a sensitive and rapid liquid chromatography–tandem mass spectrometry (LC–MS/MS) method was established for the quantitation of TY501 in rat plasma. Plasma samples were treated by precipitating protein with methanol and supernatants were separated by a Symmetry C8 column with the mobile phase consisting of me-thanol and 10 mM ammonium formate (containing 0.1%of formic acid) (90:10, v/v). The selected reaction monitoring (SRM) transitions were performed at m/z 647.4-191.2 for TY501 and m/z 473.3-143.3 for astragaloside aglycone (IS) in the positive ion mode with atmospheric pressure chemical ionization (APCI) source. Calibration curve was linear over the concentration range of 5–5000 ng/mL. The lower limit of quantification was 5 ng/mL. The mean recovery was over 88%. The intra-and inter-day precisions were lower than 6.0% and 12.8%, respectively, and the accuracy was within 71.3%. TY501 was stable under usual storage conditions and handling procedure. The validated method has been successfully applied to a pharmacokinetic study after oral administration of TY501 to rats at a dosage of 10 mg/kg.
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Aim To develop a simple,rapid and ac-curate analysis method for determination of chiral ibu-profen in Beagle dog plasma.Method The plasma sample was submitted to liquid - liquid extraction u-sing hexane /isopropanol (95 ∶5,V/V),with ketopro-fen as the internal standard (IS).The separation was accomplished in a Lux 5u Cellulose-3 (250 mm·4.6 mm,5 μm)column,and the mobile phase consisted of methanol and a mixture of 1 mmol·L -1 ammonium acetate-methanol-formic acid (90 ∶1 0 ∶0.2,V/V/V) with the volume ratio of 82 ∶1 8 at a flow rate of 0.8 mL· min -1 .The mass spectrometer consisted of an ESI interface operating at negative ionization mode and the detection was performed using multiple reaction monitoring at the transitions of m /z 205.2 /1 61 .2 for ibuprofen and m /z 253.1 /209.2 for ketoprofen (IS). Method validation included the evaluation of the matrix effect, extraction recovery, linearity, lower LOQ, within-run and between-run precision,stability and di-lution effect.Results The calibration curve was line-ar across the concentration range of 0.2 ~50 mg·L -1 for each ibuprofen enantiomer with a lower LOQ of 0.2 mg·L -1 .The within-run and between-run precision (RSD%)was in the range 1 .01 % ~1 3.1 % for each ibuprofen.The pharmacokinetic parameters for orally single dose of (S +)and racemic ibuprofen in Beagle dogs were as follows: Cmax , T1 /2 , AUC(0-t) were (82.98 ±1 4.83 )mg·L -1 ,(3.21 7 ±0.7298)h, (362.0 ±58.67)h·mg·L -1 for (S +)ibuprofen and 70.62 /74.48 mg·L -1 ,1 .520 /5.432 h ,1 77.8 /649.6 h·mg·L -1 for (R -)/(S +)ibuprofen,re-spectively.Conclusions A simple,rapid,accurate, high sensitivity and repeatability method has been suc-cessfully developed,which can analyze the concentra-tions of (R -)/(S +)ibuprofen in Beagle dog plasma simultaneously.The method could be applied for the investigation of pharmacokinetics of ibuprofen enanti-omers in Beagle dogs.
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Objeetive To investigate the retired elderly patients who had traditional Chinese medicine for preventing cardio-vascular disease and their complications for providing the best possible care.Methods Forty-eight retired elderly patients who had been given the infusion of traditional Chinese medicine for preventing the cardio-vascular disease over two years were analyzed.Results The finance,individual choice and social influences were the three major factors for the retired elderly people to choose traditional Chinese medicine for preventing cardiovascular diseases.In forty-eight patients of the study,100％ of them had secure medical insurance and they did not have any worries with the finance.93.75％ of them positively agreed with the treatment.91.67％ of them supported the idea use of the traditional Chinese medicine to promote the health and had the positive influence on the society.Conclusion Financial reasons,individual preference and social influences are the main factors to affect the retired elderly patient's choice of having traditional Chinese medicine to prevent cardiovascular disease.Our health care system for the retired elderly people has ensured the compliance of the treatment.With the increased awareness of the importance of the health,the traditional Chinese medicine has been widely used to prevent the occurrence of the cardio-vascular disease.
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Objective To explore the diagnostic value of impulse oscillometry(IOS) in the patients with COPD. Methods The IOS parameters of 142 cases of COPD (COPD group) were measured and compared with those of 160 normal eases (control group). Linear correlation analysis was done between the IOS parameters and the conventional pulmonary function indexes such as FEV1 / Pred and FEV1/FVC, and the diagnostic value of the IOS parameters in COPD was discussed. Results Compared with those of the control group, respiratory impedance (Zrs),resistance at 5 Hz and 20 Hz (R5,R<<20>) and their difference (R5-R20), central resistance (Re) and peripheral resistance (Rp), resonance frequency (Fres)in the COPD group increased significantly, while reactance at 5 Hz (X5) decreased obviously (P< 0.01 ). In the COPD group, Zrs, Fres, R5, R20, R5-R20 and Rp were all correlated negatively with FEV1 / Pred, but X5 was correlated positively with FEV1/Pred. And the most strong correlation was found between Fres and FEV1/Pred. Fres, R5, R5-R20, Rp were correlated negatively with FEV1/FVC( P all < 0.05). Conclusions IOS is suitable for the diagnosis of COPD,and can be used to evaluate the severity of COPD. The application perspective is very extensive.
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OBJECTIVE To prevent the infection at intravenous injection site with peripherally inserted central catheter(PICC). METHODS The relationship between infection with sites,methods,and times of PICC placement in 160 patients was observed. RESULTS There was no correlated infection in all the patients,but family nursing might lead to infection. CONCLUSIONS Regular management and standard operation can prevent infection.Instructions of family nursing and follow-up are necessary for infection control.
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brain and fatty. The accumulation excretion ratios within 96 h were 70.16% in urine and only 1.35% in feces after iv administration in rats, while within 24 h was 3.46% in bile. Conclusion The results of pharmacokinetics of novel r-hirudin in rats given by iv determined by RA are different from those determined by TCA-RA, but the trends indicated by the two methods are the same; urine excretion is the major excretion pathway.