Prospective observation of breakthrough cases and analysis of antibody dynamic changes after two doses of varicella / 中华预防医学杂志

Objective: To investigate the breakthrough rate and antibody level of children vaccinated two doses varicella vaccine in Tianjin city, and to compare them with those vaccinated one dose. Methods: A total of 1 112 children who were vaccinated two doses varicella vaccine were selected as the experimental group. According to the same street and township, children who had received only one dose within one year of age difference, and whose first injection time was less than one month from the first dose of varicella vaccine in the experimental group were selected as the control group. A three-year prospective observation was conducted on the incidence of varicella in the two groups. 108 pairs of children in the two groups were selected to collect antivaricella serum in the first to third year. The rate of breakthrough cases, antibody level and antibody positive rate were compared by χ2 test, t-test and variance analysis between and within the two groups in three years. Results: The cumulative breakthrough rate of the experimental group was 0.54%(6/1 112), which was lower than that of the control group 3.96% (44/1 112, χ²=29.544, P<0.001). The GMC level of antibody in the experimental group decreased year by year (F=18.291, P<0.001), and the GMC level in the control group also decreased year by year (F=91.383, P<0.001). There was significant difference in GMC level between the two groups (P<0.001). The difference of antibody positive rate in the experimental group was statistically significant in three years (χ²=11.107, P<0.01), there was significant difference in the positive rate between the first year and third year (P<0.01), there was no significant difference in the positive rate of the control group in three years (χ²=3.351, P>0.05). The positive rate of the experimental group was higher than that of the control group (P<0.001). Conclusion: Two doses varicella vaccine can significantly improve the antibody level and positive rate, but it still shows a downward trend with the extension of time. It is necessary to consider strengthening immunization according to the actual situation.

In vivo fate study of drug nanocarriers: the applications of environment-responsive fluorescent dyes / 药学学报

The in vivo fate is a crucial factor that governs the successful translation of nanoformulations. However, one of the current biggest challenges is with the real-time monitoring of the body of the nanoparticles themselves. Conventional radioactive or fluorescent probes give signals even after they are disassociated from the particle matrix, generating interference to bioimaging and leading to misjudgment of results. Environment-responsive fluorescent dyes are regarded as promising tools due to signal switching in response to the changes in the environment. Currently, there are three categories of dyes in bioimaging of nanoparticles based on Förster resonance energy transfer (FRET), aggregation-induced emission (AIE) and aggregation-caused quenching (ACQ). They have similar characteristics that strong fluorescence is emitted when they are embedded in the matrix of nanocarriers, whereas the fluorescence quenches upon release from the matrix due to dissociation of nanocarriers. The fluorescence switching reflects the existing status of the nanocarriers and therefore helps to interpret the in vivo behaviors. FRET and AIE probes have been widely used in elucidating the interactions between nanoparticles and cell models. However, they show intrinsic defects in studying in vivo fate of nanoparticles. ACQ-based dyes are sensitive to water, a universal factor in the biological environment. Therefore, with the help of bioimaging equipment, the in vivo trafficking process of nanoparticles can be unraveled. This review article tends to provide an overview on the rationale, pros and cons and applications of the three categories of environment-responsive fluorescent dyes in the investigation of the in vivo fate of nanocarriers.

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.

Synthesis of 1-furfuryl-indolin-2-one derivatives and preliminary evaluation of their antitumor activities / 药学学报

In order to find new indolin-2-one derivatives as antitumor agents, a series of 3-pyrrole substituted 1-(5-formyl-2-furanylmethyl) indolin-2-one derivatives were designed and synthesized. 5-Formyl-2 ,4-dimethyl-lH-pyrrole-3-carboxylic acid ethyl ester was condensed with 5-substituted indolin-2-one 2a-2d to afford 3-[(pyrrol-2-yl) -methylidenyl] indolin-2-ones 3a-3d. Through N-alkylation, 1-(5-formyl-furfuryl) -indolin-2-one 4a-4d were prepared. Compounds 4a-4d were then condensed with indolin-2-one to afford bis-indolin-2-one derivatives 5a-5d. The structures of the synthesized compounds were determined by 1H NMR, MS and element analysis. Antitumor activities of all the synthesized compounds in vitro were tested. All the 12 synthesized compounds possess antitumor activities against SPC-A1 strain. Especially the compounds 5a-5d possess potent antitumor activities better than sunitinib. Their IC50 are all below 5 micromol x L(-1).

Synthesis of 1-indole substituted beta-carboline alkaloid and its derivatives and evaluation of their preliminary antitumor activities / 药学学报

<p><b>AIM</b>To synthesize eudistomin U and its 6-OCH3/Br derivatives and 5'-Br derivatives as antitumor agents.</p><p><b>METHODS</b>Using tryptamine and indole-3-aldehyde as starting materials, through condensation, Pictet-Spengler cyclization and dehydrogenation three steps, the alkaloids and its derivatives were prepared.</p><p><b>RESULTS</b>The structures of the compounds were determined by 1HNMR, MS and HRMS. Antitumor activity in vitro was tested.</p><p><b>CONCLUSION</b>Eudistomin U and its derivatives were synthesized. The results showed that they all showed antitumor activities against mouse P388 strain.</p>