Synthesis and biological evaluation of noscapine analogues as microtubule-interfering agents / 药学学报

A series of noscapine analogues have been synthesized via 13-step reaction starting from 2-hydroxy-3-methoxybenzaldehyde. Anti-tumor activities of these compounds were evaluated against HL-60 cell lines in vitro by the standard MTT assay. It was found that most of these derivatives showed appreciable inhibitory activity against HL-60 and tubulin polymerization. The results also indicated that the potency of compound 31 is about three times more than that ofnoscapine against HL-60 cell line and tubulin polymerization. Moreover, it induced a massive accumulation of cells in G2/M phase. These results showed noscapine and its derivatives were worth to be intensively studied further.

An ionic liquid supported CeO2 nanoparticles-carbon nanotubes composite-enhanced electrochemical DNA-based sensor for the detection of Pb2+ / 药物分析学报

An electrochemical sensor incorporating a signal enhancement for the determination of lead (Ⅱ) ions (Pb2+) was designed on the basis of the thrombin-binding aptamer (TBA) as a molecular recognition element and ionic liquid supported cerium oxide (CeO2) nanoparticles-carbon nanotubes composite modification. The composite comprises nanoparticles CeO2, multi-wall carbon nanotubes (MWNTs)and hydrophobic room temperature ionic liquid (RTIL) l-ethyl-3-methylimidazolium tetrafluoroborate (EM1MBF4). The electrochemical sensors were fabricated by immersing the CeO2-MWNTs-EMIMBF4 modified glassy carbon electrode (GCE) into the solution of TBA probe. In the presence of Pb2+, the TBA probe could form stable G-quartet structure by the specific binding interactions between Pb2+ and TBA. The TBA-bound Pb2+ can be electrochemically reduced, which provides a readout signal for quantitative detection of Pb2+. The reduction peak current is linearly related to the concentration of Pb2+ from 1.0 × 10 8 M to 1.0 × 10-5 M with a detection limit of 5 × 109 M. This work demonstrates that the CeO2-MWNTs-EMIMBF4 nanocomposite modified GCE provides a promising platform for immobilizing the TBA probe and enhancing the sensitivity of the DNA-based sensors.

Electrocatalytic oxidation and determination of dopamine at a carbon ionic liquid electrode modified with nafion-L-aspartic acid composite film / 药物分析学报

The electrocatalytic oxidation of dopamine (DA) was studied by electrochemical approaches at a carbon ionic liquid electrode (CILE) modified with the composite film of nafion and L-aspartic acid (NL-CILE). The CILE was fabricated by replacing non-conductive organic binders with a room-temperature hydrophobic ionic liquid, 1-butyl-3-methyl-imidazolium hexafluorophosphate. The composite film of NL was used as matrix to adsorb DA and catalyze the oxidation of DA in phosphate buffer solution (PBS). The electrochemical response of DA was investigated at the NL-CILE, the traditional carbon paste electrode (TCPE), CILE and the nafion modified CILE (N-CILE) in 0.1M PBS (pH 7.4), respectively. The results showed the superiority of NL-CILE to N-CILE, CILE and TCPE in terms of provision of higher sensitivity, faster electron transfer and better reversibility. Under optimum condition, the oxidation peak current was rectilinear with DA concentration range from 0.1μM to 0.1mM, with a detection limit of 0.03μM (S/N=3) by differential pulse voltammetry. The proposed method was applied to determine DA in samples successfully.

Metabolic fingerprint and profile analysis of compound Danshen dripping pills by CS-HPLC-ESI-MSn / 中国药科大学学报

Aim: To establish the metabolic fingerprint and profile of bioactive components in human plasma after sublingual administration of compound Danshen dripping pills. Methods: Human plasma samples were collected at different time intervals. Powerlab tension system was used to measure their ability of expanding blood vessel and column switching system was employed to purify and enrich the components of interest. Results: The plasma sample of 1.5h had the strongest ability for expanding blood vessel, and had five new peaks in the chromatogram. Conclusion: After being identified, the intensity ratio of these 5 peaks was calculated. The diagram called metabolic profile was established to link bioactive compounds with pharmacodynamic action.

MODIFIED METHOD TO EVALUATE THE PROTECTION OF THE ANTIOXIDANTS AGAINST HYDROXYL RADICAL-MEDIATED DNA DAMAGE / 营养学报

Objective To establish a modified method to evaluate the protection of the antioxidant of DNA damage induced by hydroxyl radical. Method Reaction mixture at a final volume of 1.0 ml contained 0.8mg/ml DNA,0.2 mmol/L H2O2,1.0 mmol/L ascorbic acid,in 50 mmol/L NaH2PO4-Na2HPO4 buffer (pH 7.4). EDTA(1.0 mmol/L) and FeCl2 (1.0 mmol/L)were premixed and then dispensed into the reaction mixture to trigger the Fenton reaction,and the mixture was incubated at 37℃ for 30 min. The reaction was stopped by dispensing 1ml of 10% (w/v) trichloroacetic acid ,and reaction mixture was mixed with 1ml of 1% (w/v) 2-thiobarbituric acid,then further heated at 80 ℃ for 30 min. The chromogen formed was extracted into n-1-butanol and absorbance was measured at 532 nm. Results Addition of hydroxyl radical scavenger can compete with DNA for the hydroxyl radicals and diminished TBARS formation at a defined time of reaction with dose-dependent effect. The result showed that hydroxyl radical scavenger exerted inhibition effects on hydroxyl radical-mediated DNA damage. Conclusion This method can be used to evaluate the protection of the antioxidant of DNA damage induced by hydroxyl radical.