Overcoming multidrug resistance in 2D and 3D culture models by controlled drug chitosan-graft poly(caprolactone)-based nanoparticles.

The principal limitations of chemotherapy are dose-limiting systemic toxicity and the development of multidrug-resistant phenotypes. The aim of this study was to investigate the efficiency of a new sustained drug delivery system based on chitosan and ε-caprolactone to overcome multidrug resistance in monolayer and drug resistance associated with the three-dimensional (3D) tumor microenvironment in our established 3D models. The 5-fluorouracil (5-FU)-loaded nanoparticles (NPs) were characterized by transmission electron microscope and dynamic light scattering, and its released property was determined at different pH values. 5-FU/NPs exhibited well-sustained release properties and markedly enhanced the cytotoxicity of 5-FU against HCT116/L-OHP or HCT8/VCR MDR cells in two-dimensional (2D) and its parental cells in 3D collagen gel culture with twofold to threefold decrease in the IC50 values, as demonstrated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, Hoechst/propidium iodide staining and flow cytometry analysis. Furthermore, the possible mechanism was explored by high-performance liquid chromatography and rhodamine 123 accumulation experiment. Overall, the results demonstrated that 5-FU/NPs increase intracellular concentration of 5-FU and enhance its anticancer efficiency by inducing apoptosis. It was suggested that this novel NPs are a promising carrier to decrease toxic of 5-FU and has the potential to reverse the forms of both intrinsic and acquired drug resistance in 2D and 3D cultures.

[Clinical study of super crush-run Tongxinluo capsule on treatment of stroke].

OBJECTIVE: To evaluate the clinical efficacy and security of super crush-run tong xinluo capsule (SCTXLC) for apoplexy due to energy-deficiency and blood-stasis. METHOD: The randomised controlled double blind non-inferiority trial versus paroxetine, parallel contrast, different Kinds of Techniques and dosage, the clinical trial design was adopted, 144 patients with stroke of convalescent stage were selected by 2 group, which course of diseases was in 2 weekens to 3 months, neurological deficit scores was 8 to 30, grade of acaties of daily living scores was 2 to 5. the treatment group (n = 72) received SCTXLC 0.26 g (a capsule), 4 capsules at a time, three times a day, while that of the control group (n = 72) received common crush-run tong xinluo capsule (CCTXLC) 0.38 g (a capsule), 4 capsules at a time, three times a day, the therapeutic course for both groups was 28 d. RESULT: The synthesis total effective rates of the stroke in treatment group and control group were 91.3% and 87.3% respectively, showing no significant difference. The Lower Bound Upper Bound of Asymptotic 95% Confidence Interval of the total effective rates difference is -4.57%, over the beforehand Lower Bound of 15%, non-inferiority trial versus paroxetine was eligible. The adverse reactions occurred was 1 patient in the treatment group and 2 patients in control group in clinical trial. CONCLUSION: SCTXLC has definite effect for apoplexy due to energy-deficiency and blood-stasis, the efficacy in the treated group was equal to that in the control group, and favourable satety for usage.

[Extraction, combination and distribution regularity of syndrome elements in patients with variant angina pectoris].

OBJECTIVE: To explore the pathogenesis characteristics of variant angina pectoris (VAP) by extracting its syndrome elements and analyzing the combination and distribution regularity of the syndrome elements. METHODS: One hundred and seventy-five case files of VAP patients were collected. The extraction of syndrome elements and symptom contribution to syndrome was completed by the partition method of complex system based on entropy theory. Diagnostic threshold was established by receiver operator characteristic curve. According to the results diagnosed by diagnostic criteria for syndrome element with quantitation, the combination and distribution regularity of the syndrome elements in patients with VAP was analyzed. RESULTS: The basic syndrome elements in the patients with VAP were qi deficiency, qi stagnation, blood stasis, phlegm turbidity, phlegm-heat, stagnation-heat, yin deficiency and yang deficiency syndromes. It showed that the combination types of syndrome elements could be made up of one syndrome, two, three, four or more than four syndromes. Qi deficiency, yin deficiency, qi stagnation, blood stasis and phlegm turbidity syndromes had the higher frequency than other syndrome elements in the patients with VAP. CONCLUSION: The partition method of complex system based on entropy theory can be used in extracting the syndrome elements of the patients with VAP. It is found that VAP has complicated pathogenesis according to the combination and distribution regularity of syndrome elements. Qi deficiency, qi stagnation, blood stasis, phlegm turbidity and yin deficiency syndromes are the main syndrome elements.

[Effect of shensong yangxin capsule on ventricular premature beat and cardiovascular autonomic nervous function in patients with coronary heart disease].

OBJECTIVE: To observe the clinical efficacy of shensong yangxin capsule (SYC) on ventricular premature beat (VPB) differentiated in TCM as palpitation of Qi-yin deficiency syndrome or Xin collateral stagnation syndrome, and cardiovascular autonomic nervous function in patients with coronary heart disease (CHD). METHODS: The randomized, double-blind, parallel contrast method was adopted, patients were randomly assigned by 3:1 ratio into two groups. One hundred and sixty-five patients in SYC treated group and 56 in the control group (treated with Xinlvning tablet), and the therapeutic course for both groups was 4 weeks. RESULTS: The clinical efficacy on VPB and in improving TCM syndromes was better in SYC group than that in the control group (P < 0.01). After treatment, the heart rate variability (HRV) and QT dispersion in the two groups were improved in a certain degree. The changes of SDNN, SDANN, SDNN Index and PNN50 in the two groups were significantly different (P < 0.05, P < 0.01), the efficacy in the treated group was superior to that in the control group. CONCLUSION: SYC has definite effect on VPB and TCM Syndromes, it can obviously meliorate the activity of cardiovascular autonomic nervous system in the patients with CHD.