3-chloromethylene-6-fluorothiochroman-4-one, A novel DNA Topoisomerase poison

3-Chloromethylene-6-fluorothiochroman-4-one [CMFT] is a novel thiochromanones derivative that has better anti-tumor activity. In this paper, we will compare the antitumor activity of the cis-trans isomers, and explore their inhibiting effects on human topoisomerase I and topoisomerase II in cell free reaction system. The MTT method was used to study inhibition rates; the AO/EB double staining and TUNEL assay was used to assess proportion of apoptotic cells. The inhibition of CMFT to Topo I and II could be identified by adding CMFT solutions to Topo-DNA reaction mixtures and observing the relative quantities of relaxed strands and supercoils in electrophoresis assay. Results showed that CMFT had dramatic anti-tumor activities at low concentrations and the activity of CMFT trans-isomer is more significant. Use of AO/EB double staining and TUNEL indicated that CMFT induces apoptosis. DNA relaxation assays and DNA cleavage and relegation assays were performed and showed a higher potential to interact with topoisomerase I [Topo I] and topoisomerase II [Topo II] and it was verified that CMFT is a Topo poison which could be one of the mechanisms that induce cell apoptosis. Our results provide preliminary data for further investigation for the mechanism of CMFT of the apoptotic mechanism

Design, synthesis and evaluation of 5-aminobenzimidazolone derivatives as acetylcholinesterase inhibitors / 药学学报

The target compounds were prepared from 5-aminobenzimidazolone by two steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The AChE inhibitory activity of compound 4d is the best of them, and its IC50 value is equal to 7.2 μmol·L(-1), which is better than that of rivastigmine; moreover the 4d had no inhibitory activities to BuChE. Therefore, the inhibitory activities of 5-aminobenzimidazolone derivatives to acetylcholinesterase are worth further researching.

Design, synthesis and evaluation of new L-proline derivatives as acetylcholinesterase inhibitors / 药学学报

In this paper, fourteen new L-proline derivatives were designed and synthesized, and their acetlcholinesterase (AChE) inhibitory activities were also investigated in vitro. New L-proline derivatives were prepared from substituted 2-bromo-1-acetophenones through four-step reaction; and their bioactivities as AChE inhibitors were measured by Ellman spectrophotometry. The results showed that the target compounds had a certain AChE inhibitory activity to in vitro. The bioactivity of compound 8b was the best of them, and its IC50 value was 5.45 µmol.L-1, which was better than that of rivastigmine. So the acetylcholinesterase inhibitory activities of new L-proline derivatives were worth to be further studied.

To investigate the effect of the mild conjunctivitis complication on the tear break-up time in patients with dry eye / 重庆医学

Objective To investigate the effect of the mild conjunctivitis complication on the tear break-up time(BUT) in pa-tients with dry eye .Methods 93 patients with dry eye from Sep .2007 to Sep .2011 were selected .For all of them the BUT was 5 seconds or less than 5 seconds after corneal fluorescein staining .They were divided into experimental group (with mild conjunctivi-tis) and control group (without mild conjunctivitis) .We checked the BUT and compared the difference of BUT between experimen-tal group and control group .Results The average BUT of the 54 patients with complicated mild conjunctivitis ,of which conjuncti-val papillae was found in 40 cases ,was (3 .54 ± 1 .02)s ,the average BUT of the 39 patients without conjunctivitis was(3 .41 ± 1 .04) s .There was no significant difference between two groups .Conclusion Dry eyes complicated mild conjunctivitis had no effect on BU T .

The effect of minimally invasive lock pressurized titanium plate plus bone graft on distal tibial fracture / 中国基层医药

Objective To study the effectiveness of minimally invasive lock pressurized titanium plate plus bone graft on distal tibial fracture.Methods 63 patients with distal tibial fracture were enrolled.They were operated through minimally invasive lock pressurized titanium plate plus bone graft.The Iowa was compared after follow-up.Results The fractures were all healed with three pin tract infection and nonunion.Iowa was(67.2±24.5)before operation and(93.7±29.1)after twelve months(P＜0.01).The excellent cases were 30 paeitnts,the good 28 cases,the suit 5 cases and the poor 0 cases.The excellent rate was 92.1％.Conclusion Minimally invasive lock pressurized titanium plate plus bone graft was an effe(ct)ive operation for distal tibial fracture.