Nasal resorption of prim-O-glucosylcimifugin and 5-O-methylvisammioside in rats / 中国中药杂志

In this experiment, rat nasal mucosa absorption characteristics of prim-O-glucosylcimifugin and 5-O-methylvisammioside were studied to provide a basis for drug delivery of Toutongning nasal spray. The nasal mucosa absorption test in rats was conducted with in situ nasal perfusion method after pH 6 buffer solution was used to prepare high, medium and low concentrations of prim-O-glucosylcimifugin, 5-O-methylvisammioside mixed solution as liquid circulation in nasal cavity. Then the concentrations of the circulating liquid compositions to be measured were determined by HPLC, and the absorption rates of prim-O-glucosylcimifugin and 5-O-methylvisammioside under different pH conditions were also investigated. According to the results, the absorption rate constant was (0.588±0.041)×10⁻³, (0.547±0.023)×10⁻³, (0.592±0.063)×10⁻³ min⁻¹ for prim-O-glucosylcimifugin high, middle and low concentrations, and (0.438±0.041)×10⁻³, (0.407±0.023)×10⁻³, and (0.412±0.063)×10⁻³ min⁻¹ for 5-O-methylvisammioside high, middle and low concentrations. There was no significant difference among high, middle and low concentration groups, and the absorption under pH 6 was better than that under other pH conditions. Therefore, we can get the conclusion that the main active ingredient of Toutongning nasal sprays can be absorbed through the nasal mucosa, and it is feasible to make nasal spray; in addition, pH 6 of nasal spray is scientific and reasonable.

Anti-tumor effect of brucine-loaded chitosan nanoparticles in vitro / 药学学报

We designed two novel polymer materials N-glycyrrhetinic acid-polyethylene glycol-chitosan derivatives (NGPC) and N-quaternary ammonium-chitosan derivatives (NQC). We prepared three kinds of drug loaded chitosan nanoparticles (brucine/NGPC-NPs, brucine/NQC-NPs, brucine/MNPs) by ionic crosslinking method with brucine as a model drug and chitosan nanoparticles (brucine/NGPC-NPs, brucine/NQC-NPs) as the reference formulation. Using high content analysis, flow cytometry, immunofluorescence, transmission electron microscopy and other advanced technology, we tested the effect of 20 μg·mL-1 concentration of brucine solution and brucine/chitosan nanoparticles (brucine/CTS-NPs) in hepatocarcinoma (HepG2) cells and evaluated the apoptosis induced by the treatment. The results suggested that brucine-CTS/NPs had a strongest activity in killing tumor cells, and increased the total cell apoptosis rate with a significant formation of "crescent-shaped" body, swelling mitochondria, mitochondria cristae missing, decreased mitochondrial membrane potential and release of cytochrome C. The activity was enhanced by multifunctional nanocomposite particles that increased the cumulative amount of drug in the mitochondria for the anti-tumor effect.

Effects of carvedilol and metoprolol on expression of autoantibodies against cardiac adrenergic receptors in aged patients with chronic heart failure and ventricular arrhythmia / 中华心血管病杂志

<p><b>OBJECTIVE</b>To investigate the effects of carvedilol and metoprolol on the expression of autoantibodies against cardiac β(1), β(2) and α(1) adrenergic receptors in aged patients with chronic heart failure (CHF) and ventricular arrhythmia (VA).</p><p><b>METHODS</b>Sixty-eight patients with CHF and VA were randomly divided metoprolol treatment group or carvedilol treatment group on the basis of digoxin and diuretic treatment. All patients were followed up for six months cardiac function was monitored by echocardiography, VA by Holter and the three autoantibodies by enzyme-linked immunosorbent assay (ELISA).</p><p><b>RESULTS</b>(1) Systolic blood pressure and brain natriuretic peptide (BNP) were significantly lower in carvedilol group than that in metoprolol group (P < 0.05). (2) The positive ratio of autoantibodies against the cardiac β(1) adrenergic receptor was significantly decreased compared with that of pre-treatment (P < 0.05) in metoprolol group. The positive ratios of autoantibodies against cardiac β(1), β(2) and α(1)-adrenergic receptors were all significantly decreased compared with that of pre-treatment (P < 0.01) in carvedilol group. Moreover, the incidence of VA was significantly decreased in carvedilol group (P < 0.05) but not in metoprolol group.</p><p><b>CONCLUSION</b>Carvedilol is superior to metoprolol on decreasing the incidence of VA in aged patients with chronic heart failure and ventricular arrhythmia.</p>

Myocardial expression and distribution of calcineurin in normal and failing human ventricular myocardium / 中华心血管病杂志

<p><b>OBJECTIVE</b>To explore the expression and distribution of calcineurin (CaN) in normal and failing human myocardium.</p><p><b>METHODS</b>Left and right ventricles were obtained from end-staged heart failure patients (n = 12) undergoing heart transplantation and donor hearts (n = 5) taken from victims of vehicle accidents. Immunohistochemistry and SDS-PAGE technique were used to demonstrate expression and distribution of CaN.</p><p><b>RESULTS</b>Positive immunoreactive staining for CaN was detected in human cardiomyocytes, cardiac fibroblasts and epicardial mesothelial cells, but not detected in cardiac vascular endothelial cells and smooth muscle cells. There was no difference in CaN protein levels between failing hearts and donor hearts (Band intensity of right ventricle in failing hearts and donor hearts was 130.20 +/- 8.66 and 139.87 +/- 6.21, P = 0.33. Band intensity of left ventricle in failing hearts and donor hearts was 106.45 and 126.34 +/- 12.09) and between left ventricular and right ventricular myocardium (Band intensity of left and right ventricles in failing hearts was 96.99 +/- 10.67 and 104.58 +/- 13.18, P = 0.63. Band intensity of left and right ventricles in failing hearts was 132.12 and 120.74).</p><p><b>CONCLUSIONS</b>CaN is expressed in human cardiomyocytes, fibroblasts and epicardial mesothelial cells and the protein level and distribution of CaN are similar in failing and donor hearts.</p>

Treatment by Slow-released salbuterol for patients with asthma / 第三军医大学学报

Objective　In a RCT study, the safety and efficacy of sabot (a slow-release salbuteral) and volmax (controlled-release salbuterol) were compared in bronchial asthma. Methods　40 patients with moderate to severe asthma were randomly divided into two groups and treated by sabot or volmax for 2 weeks. The FEV1%, peak expiratory flow (PEF), symptom score and use of rescue ventolin were measured to evaluate the effect of treatment. Results　After treatment FEV1%, PEF and symptom score improved and the need for inhaling short-acting beta 2-agonis in both groups reduced significantly. There was no difference of these improvement between two groups. Conclusion　The safety and efficacy of sabot for treatment of asthma was similar to volmax.

Treatment by Slow-released salbuterol for patients with asthma / 第三军医大学学报

Objective　In a RCT study, the safety and efficacy of sabot (a slow-release salbuteral) and volmax (controlled-release salbuterol) were compared in bronchial asthma. Methods　40 patients with moderate to severe asthma were randomly divided into two groups and treated by sabot or volmax for 2 weeks. The FEV1%, peak expiratory flow (PEF), symptom score and use of rescue ventolin were measured to evaluate the effect of treatment. Results　After treatment FEV1%, PEF and symptom score improved and the need for inhaling short-acting beta 2-agonis in both groups reduced significantly. There was no difference of these improvement between two groups. Conclusion　The safety and efficacy of sabot for treatment of asthma was similar to volmax.