^(125)I-眼镜蛇神经毒素透鼻黏膜吸收及冰片的促进作用研究

目的:考察125I-(a-cobratoxin,Nt)透鼻黏膜吸收的情况及冰片的促进作用。方法:以大鼠、家兔、狗和羊为研究对象,以放射性活性(每分钟计数,count per minute,cpm)为指标,采用离体渗透鼻黏膜实验、在体渗透鼻黏膜重循环实验等方法,研究125I-Nt对不同动物透鼻黏膜吸收的情况及冰片的促进作用。结果:研究发现,Nt很难透过鼻黏膜吸收,但在冰片作用下吸收显著增加。结论:冰片对Nt透鼻黏膜吸收有显著促进作用。

Using a non-radioisotopic, quantitative TRAP-based method detecting telomerase activities in human hepatoma cells

A non-radioisotopic, quantitative TRAP-based telomerase activity assay was established mainly by using SYBR Green-I staining instead of radioisotope. Comparing with conventional radioisotope based method, it was better in reproducibility and accuracy. Using this method, we found telomerase activities were absent in normal human liver cells, while detected in ail of four human hepatoma cell lines (BEL-7404, SMMC-7721, QGY-7903 and HCCM) without significant differences.

Synthesis and antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(4-substituted acyl piperazin-1-yl)-2-propanols

Objective: To study the effect of fluconzole derivatives from a side chain containing 4-substituted acyl piperazin-1-yl on antifungal activity. Methods: Fourteen title compounds were synthesized and confirmed by the elementary analysis, 1HNMR and IR spectra. Five deep fungal strains and 3 shallow fungal strains were chosen as the experimental strains.Minimum inhibitory concentrations(MICs) of all title compounds were determined by the method recommended by the National Committee for Clinical Laboratory Standards (NCCLS) using RPMI 1640 test medium. Results: Among the 14 title compounds, 12 were first reported. The results of preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities to a certain extent. The activity of 4 compounds were more than 4 times as high as that of fluconazole and equal to that of ketoconazole against Candida albicans in vitro(MIC 80 value≤0.125 μg/ml). Conclusion: Introduction of a side chain containing 4-substituted acyl piperazin-1-yl into the main part of fluconazole has important influence on antifungal activities of title compounds.

Nanosecond Pulse Treatment on Water and Water Solutions

The experiment results of the nanosecond electromagnetic pulses action on water and water solutions containing radionuclides are described. An activity decrease of radionuclides solution is observed in many experiments. The results may be useful to create water purification devices from heavy metals and radionuclides.

^(99m)Tc-MIBI检测肺癌耐药性的作用研究

目的拟探讨99mTcMIBI能否检测肺腺癌A549DDP细胞的耐药性及人参单体Rh2作用后A549DDP细胞对顺铂耐药性的变化。方法用MTT法检测顺铂对敏感A549细胞和耐药A549DDP细胞的IC50、对A549DDP细胞的低效浓度(≤IC20),Rh2对A549DDP细胞的无毒浓度(≤IC5)。以无毒浓度Rh2和低效浓度的顺铂联合作用于A549DDP细胞,检测Rh2对顺铂抑制A549DDP细胞的影响。以无毒浓度的Rh2单独作用于A549DDP细胞作为Rh2组,以低效浓度的顺铂单独作用于A549DDP细胞作为DDP组,以无毒浓度的Rh2和低效浓度的顺铂联合作用于A549DDP细胞作为Rh2+DDP组,以不加药物干预作为对照组,Hoechst33258染色荧光显微镜下观察细胞形态的变化,流式细胞仪检测细胞凋亡峰。γ计数器检测以上4组细胞及A549细胞的放射性活性。将以上细胞注入裸鼠皮下建模后,用99mTcMIBI进行SPECT显像。结果順铂对A549细胞、A549DDP细胞的IC50分别为24、325μmol/L,耐药指数为13.54。Rh2≤10μmol/L时,对A549DDP细胞无明显毒性作用;100μmol/L顺铂对A549DDP细胞的抑制率为12%。10μmol/LRh2与100μmol/L顺铂联合作用,顺铂对A549DDP细胞的IC50降为94μmol/L,与100μmol/L顺铂单独作用于A549DDP细胞的IC50比,逆转3.5倍。荧光显微镜下,Rh2组和DDP组的大部分细胞核和对照组的一样,荧光分布均匀;Rh2+DDP组的荧光成团块分布,有凋亡小体形成。对照组、Rh2组和DDP组的细胞无明显凋亡峰,而Rh2+DDP组则出现了显著的凋亡峰。各组A549DDP细胞和A549细胞均能摄取99mTcMIBI,Rh2组和DDP组与对照组之间细胞的放射性活性差异无统计学意义,而Rh2+DDP组则较对照组细胞的放射性活性显著性降低,P<0.05。A549细胞的放射性活性显著性高于A549DDP细胞的对照组,P<0.01。99mTcMIBI显像,A549组裸鼠可见瘤块的放射性浓聚影。A549DDP对照组和DDP组裸鼠亦可见瘤块的放射性浓聚影,其放射性浓度较A549组淡,这两组间的R或R′差异无统计学意义,但与A549组比较,P<0.05。DDP+Rh2组裸鼠无肿瘤生长,局部未见明显放射性浓聚影。结论99mTc-MIBI能检测肺腺癌耐药的A549DDP细胞的耐药性;无毒浓度的Rh2能有效逆转A549DDP细胞对顺铂的耐药性,这种耐药性的变化亦能被99mTc-MIBI有效检测。