Objective To investigate in vitro anti-tumor activity and the related mechanism of four alkaloid monomers from Sophora alopecuroides,and to evaluate their toxicity on normal cells,thereby to screen the drugs with high efficiency and low toxicity anti-tumor effects.Methods Methyl thiazolyl tetrazolium (MTT) assay was employed to determine the effects of four alkaloid monomers on the proliferation activity of human lung cancer cells and hamster lung cells.Morphology of apoptotic lung cancer cell nucleus was observed by laser scanning confocal microscopy with Hochest33342 staining.Cell apoptosis and necrosis were measured by Annexin Ⅴ-FITC/PI double staining.Results The four alkaloid monomers showed different degree of proliferation inhibition on lung cancer cells with dose dependent manner.Oxysophoridine had the strongest inhibition effect on lung cancer cells and the minimun toxicity on normal lung cells.Hochest33342 staining and flow cytometry analysis demonstrated that oxysophoridine could induce the apoptosis and necrosis of A549 cells.Conclusions All four alkaloid monomers have certain anti-tumor effect on lung cancer cells.Oxysophoridine is the most active one with high efficiency and low toxicity characteristics,which is suitable for use as anti-tumor drug candidate for further development.

Objective To investigate susceptibility and antibacterial activity of cationic porphyfin derivative mediated photodynamic antimicrobial chemotherapy (CPD-PACT) against Pseudomonas aeruginosa,to provide experimental evidence for its high efficiency antibacterial activity.Methods The impacts of culture environments on minimum inhibitory concentration (MIC) were measured by double dilution method.The formation of inhibition zone was determined by diffusion plate method.The postantibiotic effect was analyzed by colony forming units.The viability and morphology of Pseudomonas aeruginosa were observed by confocal laser scanning microscopy (CLSM).Results The inoculum size of bacterial had a certain effect on the MIC.The MIC values increased as the pH of medium rose.When the calf serum content of culture medium increased,the MIC rose in light reaction and dropped in dark reaction.The diameter of inhibition zone mainly depended on the laser energy density,but not the concentration of photosensitizer.Though CPD possessed strong antimicrobial activity and persistent suppression on bacterial growth,the surviving Pseudomonas aeruginosa would soon continue to proliferate after PACT.The fluorescence images captured by CLSM showed that CPD-PACT could destroy the membrane integrity,leak the cytoplasmic component,decrease the bacterial activity and finally lead Pseudomonas aeruginosa to death.Conclusions CPD has strong inhibitory activity and obvious postantibiotic effect on Pseudomonas aeruginosa,which is suitable to be developed as an drug candidate for PACT.

Effect of organic acids on the synthesis of 1,3 propanediol was studied.The adsorption of organic acids from glycerol fermentation liquor by ion-exchange resins was investigated.The results showed that organic acid and 1,3 propanediol production was in negative relationship.The static adsorption showed that ion-exchange resin 005 had the best adsorption abilities of the organic acids in the glycerol fermentation liquor.It was showed that the yield of 1,3propanediol increased by 166% after the extraction of organic acids from glycerol fermentation liquor and the convertion rate increased by 34%.

Objective To study the radiation protection effect of sugar polyphenols A obtained by structured modification using mouse model of radiation injury induced by 137Cs γ-ray.Methods Total 42 male Kunming mice aged 4-6 weeks were randomly divided into six groups:negative control group (NCG),positive control group (PCG),irradiation control group (ICG) as well as three irradiation experimental groups.The radiation injury model was developed by once whole-body irradiation with 6.0 Gy 137Cs γ-ray.The mice in three experimental groups were fed sugar polyphenols A respectively with doses of 0.05,0.10 and 0.20 g/kg,for 14 d before irradiation,and continuously fed with the drug for 7 d after the irradiation.After that the mice were sacrificed,and the organ index,hematological parameters,spleen colony number,bone marrow DNA content and nucleated cells in bone-marrow were tested to evaluate the effect of sugar polyphenols A.Results Compared with the ICG,the irradiation experimental groups with the sugar polyphenols A doses of 0.05,0.10,0.20 g/kg showed reductions in irradiation injuries of immune system and hematopoietic system,which makes the significant increases of the spleen indexes (Z=-2.364,-3.003 and -2.747,P＜0.05) and the number of endogenous spleen colony (Z=-2.458,-2.141 and-2.206,P＜0.05).In the groups with the doses of 0.05 and 0.2 g/kg,the number of white blood cells were significantly increased (Z=-2.652 and-2.139,P＜0.05).Besides,in the group with the dose of 0.2 g/kg,the level of red blood cells (Z=-2.364,P＜0.05),bone marrow DNA content (Z=-2.492,P＜0.05) and nucleated cells in bone-marrow (Z=-2.492,P＜0.05) were also increased compared with the ICG.Conclusions Sugar polyphenols A has the positive effects on the recovery of immune and hematopoietic function of mice through improving the organ index,endogenous spleen colony number,peripheral white blood cell number,bone marrow DNA content and nucleated cells in bone-marrow,which can reduce the injury induced by ionizing radiation.

Objective To report the clinical effect of primary percutaneous coronary intervention(PCI)in patients with acute myocardial infarction(AMI).Methods A retrospective study was accomplished on the clinical data of 13 AMI patients who underwent PCI from March 2004 to April 2006.Results The infarct-related artery (IRA)was successfully recanalized by primary PCI for 12 AMI patients,without major complications occurred in these cases during hospitalization.Conclusion Primary PCI should be firstly chosen for treatment of AMI in the hospitals which could carry out PCI.

Objective To study the changes of plasma cystatin C level (PcyC),and evaluate the effects of the joint use of atorvastatin and probucol on PcyC and severity of coronary lesion in patients with borderline lesion of coronary artery.Methods One hundred and thirty consecutive patients with borderline coronary lesion assessed by quantitative coronary angiography were enrolled into borderline coronary lesion group (BCL),and another 136 subjects without coronary lesion were enrolled as controls (CTR).And in the meantime,the subjects in BCL group were randomized (closed envelope method) into routine treatment subgroup ( RTT,n =60),and combined treatment subgroup in which patients were treated with atorvastatin 20 mg plus probucol 1.0 g daily in addition to routine medication ( CBT,n =70) for 6 months.There were no statistical differences in basic clinical features between two subgroups.PcyC,high-sensitive C-reactive protein (hs-CRP),total cholesterol (TC),low-density lipoprotein cholesterol (LDL-C),high-density lipoprotein cholesterol ( HDL-C ) and triglycerides (TG) were determined.Of them,104 patients in BCL group rechecked by coronary angiography.Comparison of biomarkers carried out between two groups by using a number of independent-sample t-test and analysis of variance.For enumeration data,chi-square test was used to compare mean values of biomarkers between groups. P ＜ 0.05 was considered statistically significant.Results PcyC levels were significantly higher in BCL group than those in CTR group ( P ＜ 0.05 ).Compared with RTT subgroup,levels of PcyC,TC,LDL-C,TG and hs-CRP were more significantly decreased in CBT subgroup (P ＜ 0.05,P ＜ 0.01 ).Moreover,there was a trend of slight decrease in the mean percent of stenosis (MPS) of coronary artery with borderline lesion in RTT subgroup treated for 6 months,whereas more marked decrease in the MPS of coronary artery with borderline coronary lesion in CBT subgroup treated for 6 months ( P ＞ 0.05 ; P ＜ 0.05 ).Conclusions Cystatin C plays an important role in the pathogenesis of coronary artery,and PcyC is associated with severity of coronary lesion,the combination of atorvastatin and probucol decreases the PcyC level,and it may be the treatment of choice for borderline lesion of coronary artery.

AIMTo illustrate the non-equilibrium properties of drug permeation through stratum corneum (SC) to provide theory and method for transdermal drug delivery.

METHODSThe system of side-by-side permeation chambers in vitro was isolated, thus conditions for equilibrium state were decided. And a network thermodynamic model was established. Non-equilibrium and leakage experiments were completed with which tinidazole was pattern drug.

RESULTSThe properties of non-equilibrium including: long term to reach equilibrium state; delay-start of the permeation; uncertainty of initial drug permeable flux. The properties of leakage including: degression of drug permeable flux; changeability of permeation time constant.

CONCLUSIONThe permeation cell is believed to be a non-linear and time variable system.

Administration, Cutaneous ; Electroporation ; Epidermis ; metabolism ; Humans ; In Vitro Techniques ; Permeability ; Tinidazole ; administration & dosage ; pharmacokinetics

Antiphospholipid syndrome (APS) is a systemic autoimmune disease defined by thrombotic or obstetrical events and persistent antiphospholipid antibodies (aPLs). Chemokine-like factor-like MARVEL transmembrane domain-containing family (CMTM) is widely expressed in the immune system and may closely related to APS. This review aimed to systematically summarize the possible effects of CMTM on APS. Publications were collected from PubMed and Web of Science databases up to August 2020. CKLF, CKLFSF, CMTM, antiphospholipid syndrome, immune cells, and immune molecules were used as search criteria. Immune cells, including neutrophil, dendritic cells (DCs), T-cells, B-cells, and inflammatory cytokines, play an important role in the development of APS. Chemokine-like factor 1 (CKLF1) has a chemotactic effect on many cells and can affect the expression of inflammatory cytokines and adhesion molecules through the nuclear factor- kB (NF- kB) pathway or mitogen-activated protein kinase (MARK) pathway. CKLF1 can participate in the maturation of DCs, T lymphocyte activation, and the activation of neutrophils through the MAPK pathway. CMTM1 may act on Annexin A2 by regulating Ca 2+ signaling. CMTM2 and CMTM6 are up-regulated in neutrophils of APS patients. Some CMTM family members influence the activation and accumulation of platelets. CMTM3 and CMTM7 are binding partners of B-cell linker protein (BLNK), thereby linking B cell receptor (BCR) and activating BLNK-mediated signal transduction in B cells. Moreover, CMTM3 and CMTM7 can act on DCs and B-1a cell development, respectively. CMTM may have potential effects on the development of APS by acting on immune cells and immune molecules. Thus, CMTM may act as a novel prognostic factor or immunomodulatory treatment option of APS.

Objective To evaluate the relationship between plasma cystatin C concentration (PcyC) and coronary artery diseases (CAD). Method A total of 126 subjects with CAD evidenced by coronary angiography admitted from April 2007 to March 2009 were divided into three groups: stable angina pectoris (SAPs, n = 34),unstable angina pectoris (UAPs, n = 56) and acute myocardial infarction (AMIs, n = 36), according to the diag-nostic criteria of CAD set by WHO. Another 34 subjects without CAD were taken as controls. There were no statis-tical differences in demographics among four groups. Serum lipids profile, uric acid (UA), PcyC and high-sensi-tive C-reactive protein (hs-CRP) were determined. And in the meantime, all patients were followed up for six months and adverse cardiovascular events were recorded. Comparisons were made between groups with a number of independent-sample t -tests. Data were processed with analysis of variance to test the differences in means among four groups, and the means were compared with chi-square test. Statistical significance was established at a P val-ue of less than 0.05. Results Cystatin C levels were significantly higher in UAPs than that in SAPs and in controls (P < 0.05), but were much lower than that in AMIs (P < 0.05). And much higher concentration of hs-CRP was found in UAPs (P < 0.05) and in AMIs (P < 0.01). Cystatin C was positively and significantly corre-lated with age, hs-CRP, WBC, creatinine and UA (r > 0, P < 0.05), whereas a significantly negative correla-tion with high-density lipoprotein cholesterol was found (r = - 0.227, P < 0.05). These coefficients were obvi-ously high for creatinine (r = + 0. 612), and WBC (r = + 0.459). During the period of six-month follow-up, 26 patients with adverse cardiovascular events were found, and had significantly higher cystatin C levels than 22 con-trols at admission (P < 0.01). Conclusions Cystatin C plays a pivotal role in the course of CAD, and the PcyC is a strong predictor for the risk of cardiovascular events.

Objective To investigate the role of pharmacists participating in the drug therapy of glucocorticoid induced iatrogenic Cushing syndrome.Methods Clinical pharmacists provided recommendations and pharmaceutical care for a patient with iatrogenic Cushing syndrome and secondary diabetes,which was attributed to his oral intake of dexamethasone tablets for up to 10 years.Result and conclusion The patient gradually reduced the dosage of dexamethasone tablets and withdrew it finally,replaced with hydrocortisone acetate 20 mg bid.Withdrawal symptom and bounce phenomenon didn't appear during the process.Complications were treated respectively and the patient discharged then.The pharmacist plays an important role in improving the accuracy of patient medication,and could be helpful in avoiding drug-induced adverse reactions and unnecessary economic burden for patients.