OBJECTIVETo study the in vitro antibacterial activity of cefdinir against clinical isolates of respiratory tract pathogens in Children.

METHODSMIC values of cefdinir against 380 strains were determined with E-test method and compared with those of cefaclor.

RESULTSAll penicillin-susceptible Streptococcus pneumoniae (PSSP) strains were also susceptible to cefdinir and cefaclor. Both cefdinir and cefaclor were not active against penicillin-resistant SP (PRSP). Against penicillin-intermediate SP (PISP) the susceptibility rates of cefdinir and cefaclor were 70.1% and 57.4%, respectively. The activity of cefdinir and cefaclor against beta-lactamases negative Hemophilus influenzae (HI) was excellent, but the susceptibility rates of cefdinir and cefaclor against beta-lactamases positive HI were 85.0% and 70.0%, respectively with MIC(90) of 1.5 mg/L vs. 256.0 mg/L. Cefdinir presented higher activities and lower MIC values than cefaclor against Moraxella catarrhalis (MC), Group A streptococcus (GAS), methicillin susceptible staphylococcus aureus (MSSA), and extended spectrum beta-lactamases (ESBLs) negative Escherichia coli (E. coli) or Klebsiella pneumoniae (K. pn). Both cefdinir and cefaclor were not susceptible to ESBLs positive E. coli and K. pn.

CONCLUSIONSCefdinir exhibits excellent activity against PSSP, PISP, HI, as well as MC, GAS, MSSA and ESBLs negative E. coli or K. pn.

Anti-Bacterial Agents ; pharmacology ; Bacteria ; drug effects ; Cephalosporins ; pharmacology ; Child ; Humans ; Microbial Sensitivity Tests ; Respiratory System ; microbiology

According to the super-position principle of the reinforcement of biological activities, a series of novel E-substituted 2, 3-diaryl propenoic acyloxy phosphonate derivatives were designed and synthesized. And the structures of the target compounds were confirmed by IR, 1H NMR, 13C NMR and elemental analysis. Furthermore, the cytotoxicities of all compounds on A-549, SGC-7901 and EC-109 in vitro were evaluated by MTT assay, and some of them showed good antitumor activity. Among the active compounds, especially, the IC50 value of compound 3e was (12.7 ± 1.9) μmol x L(-1) against A-549 cells, similar to cisplatin [IC50 = (8.0 ± 1.5) μmol x L(-1)], compounds 3g and 3k had better inhibition effect on EC-109 cells growth, with the IC50 values of (9.5 ± 1.8) μmol x L(-1) and (11.5 ± 0.9) μmol x L(-1) respectively, and compounds 3i and 3k exhibited good cytotoxic property on A-549, SGC-7901 and EC-109, which were worth further investigation.
Antineoplastic Agents ; chemical synthesis ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; Drug Design ; Humans ; Organophosphonates ; chemical synthesis ; pharmacology

Objective: To assess the clinical significance of changes in levels of serum β2 microglobulin (β2-MG), vascular endothelial growth factor (VEGF), and lactate dehydrogenase (LDH) in patients with diffuse large B-cell lymphoma (DLBCL) after treatment. Methods: A total of 89 patients with DLBCL who were admitted to the hospital between February 2015 an July 2017 were included in the DLBCL group and 40 normal, healthy persons admitted during the same period were selected as the control group. All DLBCL patients underwent standard chemotherapy after admission. Peripheral venous blood was collected before and after chemotherapy to determine any changes in serum β2-MG, VEGF, and LDH levels. Biomarker levels were also compared with those from normal, healthy subjects. The clinical and pathological data of all DLBCL patients were collected and the relationships between changes in biomarker levels, clinical and pathological parameters of DLBCL, and curative effects were analyzed. Results: The levels of serum β2-MG, VEGF, and LDH in the DLBCL group were higher than those in the control group (P<0.05) and all levels in DLBCL group decreased after chemotherapy (P<0.05). The effective rate of the R-CHOP group was higher than that of the CHOP group (P<0.05). Serum LDH levels were higher in patients with typical B symptoms than in those without such symptoms (P<0.05). Serum levels of β2-MG, VEGF, and LDH were higher in patients with Ann Arbor stageⅢ-Ⅳlymphoma, with bone marrow involvement, whose international prognostic index (IPI) was high-risk, and with treatment failure than in those with stageⅠ-Ⅱlymphoma, without bone marrow involvement, with low-risk IPI, and with treatment response (P<0.05). The levels of serum VEGF, β2-MG, and LDH were positively correlated with each other, and all three biomarkers were negatively correlated with treatment response (P<0.05). Conclusions: Levels of serum β2-MG, VEGF, and LDH are elevated in patients with DLBCL but are significantly decreased after treatment. Changes in expression levels of these three biomarkers are related to clinical stage, bone marrow involvement, IPI, and treatment response. These biomarkers can be used as a basis for monitoring DLBCL and evaluating curative effect and prognosis.

Bacteria ; drug effects ; isolation & purification ; Drug Resistance ; Escherichia coli ; drug effects ; Female ; Haemophilus influenzae ; drug effects ; Humans ; Klebsiella pneumoniae ; drug effects ; Male ; Microbial Sensitivity Tests ; Respiratory Tract Infections ; microbiology ; Staphylococcus aureus ; drug effects ; Streptococcus pneumoniae ; drug effects

OBJECTIVETo explore permeability of artificial blood-brain barrier (aBBB) by oxygen-glucose deprivation combined (OGD)-induced using tetramethylpyrazine combined with puerarin in vitro.

METHODRats were divided into normal control group, model group, tetramethylpyrazine group, puerarin group, tetramethylpyrazine-puerarin group and nimodipine group. Culture rat brain microvascular endothelial cells and astrocytes in vitro and build the OGD-induced aBBB damage model. Evaluate aBBB damage characteristics by TEER, gamma-GT, AKP and LDH. Determine contents of tetramethylpyrazine, puerarin, nimodipine and calculate drug permeating concentration of OGD-induced aBBB model by HPLC.

RESULTCompared with the model, the level of TEER was lower than the control group with significant difference (P < 0.01). The levels of gamma-GT, AKP in tetramethylpyrazine group, tetramethylpyrazine-puerarin group and nimodipine group were higher than the model group, the differences were significant (P < 0.01). Compared with tetramethylpyrazine group or puerarin group, the level of AKP of tetramethylpyrazine-puerarin group increased significantly (P < 0.01). The differences of levels of TEER, gamma-GT, AKP and LDH between tetramethylpyrazine-puerarin group and nimodipinthe group were significant (P < 0.05). Tetramethylpyrazine-puerarin group has a synergistic effect of increasing TEER, gamma-GT, AKP and reducing LDH. The permeating rate in tetramethylpyrazine-puerarin group was higher than tetramethylpyrazine group and puerarin group.

CONCLUSIONTetramethylpyrazine-puerarin can permeate aBBB more easily and protect aBBB. The cause may relate to reducing the permeability of the OGD-induced aBBB.

Animals ; Blood-Brain Barrier ; drug effects ; Drug Combinations ; Glucose ; physiology ; Isoflavones ; administration & dosage ; pharmacology ; Male ; Oxygen ; physiology ; Permeability ; Pyrazines ; administration & dosage ; pharmacology ; Rats ; Rats, Sprague-Dawley

This study aimed to investigate the underlying mechanism of Zhenwu Decoction in the treatment of heart failure by regulating electrical remodeling through the transient outward potassium current(I_(to))/voltage-gated potassium(Kv) channels. Five normal SD rats were intragastrically administered with Zhenwu Decoction granules to prepare drug-containing serum, and another seven normal SD rats received an equal amount of distilled water to prepare blank serum. H9c2 cardiomyocytes underwent conventional passage and were treated with angiotensin Ⅱ(AngⅡ) for 24 h. Subsequently, 2%, 4%, and 8% drug-containing serum, simvastatin(SIM), and BaCl_2 were used to interfere in H9c2 cardiomyocytes for 24 h. The cells were divided into a control group [N, 10% blank serum + 90% high-glucose DMEM(DMEM-H)], a model group(M, AngⅡ + 10% blank serum + 90% DMEM-H), a low-dose Zhenwu Decoction-containing serum group(Z1, AngⅡ + 2% drug-containing serum of Zhenwu Decoction + 8% blank serum + 90% DMEM-H), a medium-dose Zhenwu Decoction-containing serum group(Z2, AngⅡ + 4% drug-containing serum of Zhenwu Decoc-tion + 6% blank serum + 90% DMEM-H), a high-dose Zhenwu Decoction-containing serum group(Z3, AngⅡ + 8% drug-containing serum of Zhenwu Decoction + 2% blank serum + 90% DMEM-H), an inducer group(YD, AngⅡ + SIM + 10% blank serum + 90% DMEM-H), and an inhibitor group(YZ, AngⅡ + BaCl_2 + 10% blank serum + 90% DMEM-H). The content of ANP in cell extracts of each group was detected by ELISA. The relative mRNA expression levels of ANP, Kv1.4, Kv4.2, Kv4.3, DPP6, and KChIP2 were detected by real-time quantitative PCR. The protein expression of Kv1.4, Kv4.2, Kv4.3, DPP6, and KChIP2 was detected by Western blot. I_(to) was detected by the whole cell patch-clamp technique. The results showed that Zhenwu Decoction at low, medium, and high doses could effectively reduce the surface area of cardiomyocytes. Compared with the M group, the Z1, Z2, Z3, and YD groups showed decreased ANP content and mRNA level, increased protein and mRNA expression of Kv4.2, Kv4.3, DPP6, and KChIP2, and decreased protein and mRNA expression of Kv1.4, and the aforementioned changes were the most notable in the Z3 group. Compared with the N group, the Z1, Z2, and Z3 groups showed significantly increased peak current and current density of I_(to). The results indicate that Zhenwu Decoction can regulate myocardial remodeling and electrical remodeling by improving the expression trend of Kv1.4, Kv4.2, Kv4.3, KChIP2, and DPP6 proteins and inducing I_(to) to regulate Kv channels, which may be one of the mechanisms of Zhenwu Decoction in treating heart failure and related arrhythmias.
Rats ; Animals ; Myocytes, Cardiac ; Atrial Remodeling ; Rats, Sprague-Dawley ; Heart Failure/metabolism* ; RNA, Messenger/metabolism* ; Potassium

Objective To investigate the difference in the prognosis of hepatitis B virus-related acute-on-chronic liver failure (HBV-ACLF) caused by hepatitis recurrence after withdrawal of nucleos(t)ide analogues (NUC) and possible causes in HBeAg-positive versus HBeAg-negative chronic hepatitis B (CHB) patients. Methods A total of 108 CHB patients with HBV-ACLF caused by withdrawal of NUC who were admitted to The First Affiliated Hospital of Nanchang University from January 2017 to December 2018 were enrolled, and according to HBeAg status, these patients were divided into HBeAg-positive group with 57 patients and HBeAg-negative group with 51 patients. The two groups were compared in terms of sex, age, clinical manifestation, signs, levels of total bilirubin, direct bilirubin, alanine aminotransferase, aspartate aminotransferase, prothrombin time, activated partial thromboplastin time, prothrombin time/international normalized ratio, and HBV DNA quantification on admission, complications (including hepatic encephalopathy, hepatorenal syndrome, and spontaneous bacterial peritonitis), and prognosis of HBV-ACLF. In addition, 48 CHB patients with continuous NUC antiviral therapy for > 2 years and HBV DNA < 20 IU/mL were enrolled, and the serum level of HBV pgRNA was measured to investigate the possible causes of the difference in the prognosis of HBV-ACLF between the patients with different HBeAg statuses. The two-independent-samples t test was used for comparison of normally distributed continuous data between two groups, and the Kruskal-Wallis H test was used for comparison of non-normally distributed continuous data between two groups; the chi-square test was used for comparison of categorical data. Results For the 108 patients with HBV-ACLF caused by drug withdrawal and recurrence, the HBeAg-positive group had an improvement rate of 49.1% and the HBeAg-negative group had an improvement rate of 74.5%. The HBeAg-negative group had a significantly higher improvement rate than the HBeAg-positive group ( χ 2 =2.811, P =0.006). The HBeAg-positive group had a significantly higher level of HBV DNA than the HBeAg-negative group on admission ( t =-3.138, P =0.002). For the 48 CHB patients who achieved virologic response after long-term antiviral therapy, the HBeAg-positive group had a significantly higher HBV pgRNA load than the HBeAg-negative group ( H =2.814, P =0.049). Conclusion Compared with the HBeAg-positive CHB patients, HBeAg-negative CHB patients have a significantly better improvement rate of HBV-ACLF caused by hepatitis recurrence after withdrawal of NUC antiviral therapy. The difference in baseline HBV pgRNA level may be associated with the difference in the prognosis of HBV-ACLF in patients with different HBeAg statuses.