Objective To observe the efficacy and safety of albumin bound paclitaxel in the treatment of retreatment advanced non-small-cell lung cancer (NSCLC).Methods Retreatment NSCLC patients failed from first line regimen or beyond were treated with albumin bound paclitaxel weekly by intravenous dose of 130 mg/m2 on day 1 and day 8,with a 21-day cycle.Efficacy was evaluated every two cycles and side effects were observed during each cycle.Results None of 69 patients achieved complete remission (CR),15 patients (21.7 ％) achieved partial remission (PR),and 23 patients (33.4 ％) achieved stable disease (SD).Objective response rate (ORR) was 21.7 ％,disease control rate (DCR) was 55.1％,and progress free survival (PFS) time was 3.8 months.Efficacy was not correlated with gender,age,histology and lines of previous treatment (all P ＞ 0.05).Main adverse reactions included neutropenia,alopccia and neurotoxicity,which were all tolerable.Conclusion Weekly albumin bound paclitaxel is effective and well tolerated in the treatment of retreatment advanced NSCLC,which can be considered as the second line or beyond regimen.

This study was aimed to establish a HPLC method for the determination of isogarcinol. Daojin Inertsil WP300 C18 (4.6 mm× 150 mm, 5μm) was employed with methanol and water (75?25) as the mobile phase. The flow rate was 1.0 mL·min-1. The column temperature was set at 40°C. The detection wavelengthγ was set at 277 nm. The results showed that the linear range of isogarcinol was 0.005 7-0.039 9μg. The average recovery rate was 99.58%. The relative standard deviation (RSD) was 1.25%. The contents of isogarcinol inGarcinia mangostana,Garcinia oblongifolia,Garcinia oligantha,Cratoxylum cochinchinense andCalophyllum membranaceum were 0.285%, 0.199%, 0.857%, 0.161% and 0.006%, respectively. Isogarcinol was not detected inCratoxylum formosum orCalophyllum inophyllum. It was concluded that the method was convenient, accurate with high sensitivity, good stability and repeatability. It can be used for determination of isogarcinol content in Chinese herbal medicine.

Aim Toinvestigatingtheinductionof CYPs in hepatocytes or HepG2 cells by triptolide(TP) andthepossiblemechanism.Methods AfterTPtreat-ment,the expression of CYPs in rat primary hepato-cytes or human HepG2 cells was detected by real-time PCR and Western blot assays.Specific inhibitors or gene knockdown method were employed to analyze the possiblemechanism.Results Theexpressionof CYP1A2,2C7,2C11,2C12,2D2,2E1 and 3A1 in rat primary hepatocytes was induced by TP.The fold was 19,2,31,3,21,88 and 34 at 50 nmol·L-1, respectively while at 100 nmol·L-1 it was 20,5,30,23,61,83 and 38,respectively.In HepG2 cells,the expression of human CYP1A1,2B6,2C9,2C19, 2D6,2E1 and 3A4 was also induced by TP.The ac-tivities of nuclear receptor PXR and CAR were inhibi-ted.TP upregulated p53 expression,and the induction of several CYPs caused by TP was blocked when p53 wasinhibited.Conclusions TPinducesCYPsexpres-sion in rat hepatocytes and HepG2 cells.Nuclear re-ceptors may not be involved in TP induced CYPs, while the mechanism may partly attribute to p53.

BACKGROUND:In recent years, some studies have demonstrated that ganglioside can promote survival and differentiation of umbilical blood cord mesenchymal stem cel s in vitro. OBJECTIVE:To observe the effect of injection of human umbilical blood cord mesenchymal stem cel s and ganglioside into rat lateral ventricles on neurological functional recovery from cerebral palsy. METHODS:Total y 60 cerebral palsy neonatal rats were delivered from pregnant rats which were modes were given intraperitoneal injection of lipopolysaccharide for 2 successive days on day 17 of gestation. Then those neonatal rats were randomly divided into five groups, including model group (n=10), sham transplantation group (n=10), stem cel transplantation group (n=18), ganglioside group (n=10) and combination group (n=12). Under stereotaxic instrument, umbilical blood cord mesenchymal stem cel s or ganglioside were injected into left lateral ventricles of the rat brain, respectively, and the sham transplantation group was given the same volume of phosphate buffered saline. Two rats from the stem cel transplantation group were put to death for immunofluorescence staining at 7, 14, 21 and 28 days after transplantation, respectively, and two rats in the combination group were kil ed for immunofluorescence staining at 14 days. Besides, al rats were underwent neurologic evaluation at 28 days after transplantation. RESULTS AND CONCLUSION:The umbilical blood cord mesenchymal stem cel s could survive, migrate and differentiate, which mainly distributed in the lateral ventricle, hippocampus and cortex. At 14 days after transplantation, positive expressions of BrdU and glial fibril ary acidic protein in the combination group were significantly higher than those in the stem cel transplantation group (P<0.05). In addition, compared with the model group, the holding time significantly prolonged and foot error times significantly decreased in the latter three groups (P<0.05), as wel as in the combination group compared with the stem cel transplantation and ganglioside groups (P<0.05). These results indicate that umbilical blood cord mesenchymal stem cel s and ganglioside can both improve neurological function of rats with cerebral palsy. Given that ganglioside can promote survival and differentiation of umbilical blood cord mesenchymal stem cel s in vivo, the combined transplantation is preferred.

Objective To construct lentiviral expression plasmids of CYP2C9,CYP2C9 * 8 and CYP2C9 * 27,and to express CYP2C9,CYP2C9 * 8 and CYP2C9 * 27 stably in HEK2C9T cells.Methods CYP2C9 coding region was obtained by reverse transcription PCR from the human liver total RNA,and then cloned into the mammalian expression vector MigR1.CYP2C9 * 8 or CYP2C9 * 27 coding sequences were obtained from MigR1-CYP2C9 by overlapping PCR and then cloned into MigR1.The coding sequences were introduced to HEK293 cells by lentivirus,and 293T-2C9,293T-2C9 * 8 and 293T-2C9 * 27 were screened by flow cytometry and monoclonal picking.Cellular fluorescence,qRT-PCR,Western blot and the metabolic activity assays were used to identify the cells.Results MigR1-CYP2C9,MigR1-CYP2C9 * 8 and MigR1-CYP2C9 * 2293T-2C9 * 8 plasmids were constructed.All monoclonal cells 293T-2C9,293T-2C9 * 8 and 293T-2C9 * 27 cell lines expressed GFP after 30 passages.Both qRT-PCR and Western blot assay showed CYP2C9 expression in the cells.Microsomes of the three cell lines were capable of catalyzing diclofenac to 4-OH diclofenac.Conclusion 293T-2C9,293T-2C9 * 8 and293T-2C9 * 27 celllines stably expresse CYP2 C9,CYP2C9 * 8 and CYP2C9 * 27,respectively.The cell lines provide useful tools for the function investigation of CYP2C9 * 8 and CYP2C9 * 27.

Objective To construct lentiviral expression plasmids of CYP2C9,CYP2C9 * 8 and CYP2C9 * 27,and to express CYP2C9,CYP2C9 * 8 and CYP2C9 * 27 stably in HEK2C9T cells.Methods CYP2C9 coding region was obtained by reverse transcription PCR from the human liver total RNA,and then cloned into the mammalian expression vector MigR1.CYP2C9 * 8 or CYP2C9 * 27 coding sequences were obtained from MigR1-CYP2C9 by overlapping PCR and then cloned into MigR1.The coding sequences were introduced to HEK293 cells by lentivirus,and 293T-2C9,293T-2C9 * 8 and 293T-2C9 * 27 were screened by flow cytometry and monoclonal picking.Cellular fluorescence,qRT-PCR,Western blot and the metabolic activity assays were used to identify the cells.Results MigR1-CYP2C9,MigR1-CYP2C9 * 8 and MigR1-CYP2C9 * 2293T-2C9 * 8 plasmids were constructed.All monoclonal cells 293T-2C9,293T-2C9 * 8 and 293T-2C9 * 27 cell lines expressed GFP after 30 passages.Both qRT-PCR and Western blot assay showed CYP2C9 expression in the cells.Microsomes of the three cell lines were capable of catalyzing diclofenac to 4-OH diclofenac.Conclusion 293T-2C9,293T-2C9 * 8 and293T-2C9 * 27 celllines stably expresse CYP2 C9,CYP2C9 * 8 and CYP2C9 * 27,respectively.The cell lines provide useful tools for the function investigation of CYP2C9 * 8 and CYP2C9 * 27.

Objective To explore the incidence and associated factors of aortic artery calcification (AAC) by lateral lumbar X-ray score in maintenance hemodialysis (MHD) patients.Mehtods A total of 155 MHD patients with complete clinical data in our hospital were enrolled in the study.Lateral lumbar X-ray score of the abdominal aorta was used to determine AAC in MHD patients.Results Aortic calcification was most severe in front of the fourth lumbar segment and ameliorated in higher lumbar levels.63.63％ of MHD patients presented visible calcification in the abdominal aorta,and 28.39％ had severe calcification with more than three segments.Age (OR=1.094,P＜0.01),dialysis vintage (OR=1.013,P=0.022),triglyceride (OR=1.261,P=0.030) and phosphate level (OR=1.324,P=0.023) were risk factors of abdominal aorta calcification,however serum albumin level (OR =0.239,P=0.013) was protect factor of aortic calcification.Conclusions Incidence of AAC is quite high in MHD patients and associated with increasing of age,duration of hemodialysis,serum triglyceride,phosphate level and plasma albumin.The semi-quantitative X-ray method of determining vascular calcification is less expensive and may be widely available clinically.

In order to improve the yield and simplify the operation, the synthesizing process of JAK3 inhibitor tofacitinib citrate was improved based on the analysis of the methods previously published.Using 2, 4-dichloro-7H-pyrrolo [2, 3-d] pyrimidine and (3R, 4R)-1-benzyl-N, 4-dimethylpiperidin-3-amine dihydrochloride as starting materials, tofacitinib citrate was obtained through four steps of nucleophilic substitution, catalytic transfer hydrogenation, cyanide acetylation and citrate salt, and its crystal form was consistent with the original research.After optimization, the yield was better than those reported in literature, and the mild reaction conditions were suitable for industrial production.

OBJECTIVETo develop a method for detecting the topical concentration of hydrocortisone (HC) in the subcutaneous adipose of rats using microdialysis sampling technique and liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS).

METHODSTopical samples were collected by applying the probe into the subcutaneous adipose of rats, with alcohol (5%)-ringers solution as the perfusion solution. A LC-MS/MS method was established for detecting the HC concentration in the dialysates.

RESULTSThe protonated precursor to produce ion transitions monitored for HC was m/z 363.2→121.1. The calibration curve was linear over the range of 0.5-1000 ng/ml, with the intra- and inter-day precision and accuracy within ∓15%, and no significant matrix effect was noted. The in vivo recovery of the probe was about 59%.

CONCLUSIONA selective and sensitive method has been successfully established for the on-line HC detection in the subcutaneous adipose of rats.

Administration, Cutaneous ; Animals ; Chromatography, Liquid ; methods ; Hydrocortisone ; administration & dosage ; pharmacokinetics ; Male ; Microdialysis ; methods ; Rats ; Rats, Wistar ; Subcutaneous Fat ; chemistry ; metabolism ; Tandem Mass Spectrometry ; methods

Objective To explore and analyze the relationship between the peripheral blood changes in BNP and NT-proBNP levels and the complication of chronic obstructive pulmonary disease(COPD)and heart failure(CHF)in the elderly.Methods A total of 210 elderly COPD patients admitted to our hospital from April 2021 to August 2023 were enrolled,and according to compli-cation with HF or not,they were divided into COPD+HF group(61 cases)and COPD group(149 cases).Immunofluorescence assay was used to detect the expression levels of BNP and NT-proBNP in the peripheral blood samples of all patients.Routine echocardiography was applied to detect left ventricular ejection fraction(LVEF),left ventricular end-systolic diameter(LVESD),and left ventricular end-diastolic diameter(LVEDD).Pearson correlation analysis was used to evaluate the correlation between peripheral blood BNP and NT-proBNP expression and cardiac function.Multi-variate regression analysis was conducted to analyze the independent influencing factors of COPD complicated with HF,and ROC curves were drawn to evaluate the predictive value of peripheral blood BNP and NT-proBNP levels for COPD complicated by HF.Results The BNP,NT-proBNP,LVESD and LVEDD were significantly higher and the LVEF was obviously lower in COPD+HF group than the COPD group(P＜0.01).BNP,NT-proBNP,LVEF,and LVEDD were risk factors for COPD complicated with HF(P＜0.05,P＜0.01).The sensitivity,specificity,and AUC value of BNP in predicting the complication were 82.0％,94.6％,and 0.802(95％CI:0.712-0.892),and those of NT-proBNP in the prediction were 88.5％,92.6％,and 0.823(95％CI:0.767-0.879),respectively.In the COPD patients complicated with HF,the NT-proBNP and BNP levels in the peripheral blood were negatively correlated with LVEF(r=-0.413,P=0.013;r=-0.521,P=0.000),and positively with LVESD(r=0.356,P=0.010;r=0.565,P=0.000),LVEDD(r=0.335,P=0.014;r=0.501,P=0.000)and NYHA cardiac function grades(r=0.687,P=0.000;r=0.752,P=0.000).Conclusion The high levels of BNP and NT-proBNP in peripheral blood are closely associated with COPD complication with HF,and are related to cardi-ac function grade,which is of great value for the evaluation of HF severity in COPD patients.