A549细胞对壳寡糖及其纳米粒的摄取作用

目的 研究壳寡糖及其纳米粒的A5 4 9肺上皮细胞摄取作用 ,探讨壳寡糖纳米粒作为药物载体的可能性。方法 溶剂扩散法制备壳寡糖纳米粒 ,以A5 4 9肺上皮细胞评价壳寡糖及其纳米粒的细胞毒性 ,由荧光倒置显微镜、流式细胞仪研究A5 4 9细胞对壳寡糖及其纳米粒的摄取作用。结果 壳寡糖及其纳米粒的细胞毒性均较低 ,IC50 分别为 94 4 36和 6 4 3 16mg·L- 1 。壳寡糖及其纳米粒的细胞摄取作用与其浓度及细胞孵育时间相关 ;在同一孵育时间壳寡糖纳米粒的摄取量比等浓度的壳寡糖增加 0 4 9～ 13 9倍。结论 壳寡糖及其纳米粒的细胞毒性较低。壳寡糖形成纳米粒后 ,可显著增加A5 4

肺泡巨噬细胞摄取微粒作用影响因素的研究进展

近几年来肺部给药传递系统已成为人们研究的新焦点,但将微粒转运到肺组织后微粒与肺泡巨噬细胞间的作用却很少被人关注。根据不同的疾病通过调控微粒与肺泡巨噬细胞的摄取作用能够提高药物的治疗作用。文章参考大量的文献,综述了一些常见疾病与巨噬细胞间的关系并总结了肺部给药传递系统中肺泡巨噬细胞对微粒摄取作用的影响因素,为肺部给药制剂的发展与临床应用奠定基础。

TLR7刺激对Balb/c小鼠树突状细胞免疫功能影响的体外研究

树突状细胞是迄今所知的功能最强的抗原提呈细胞,是连接固有免疫和适应性免疫的桥梁。未成熟的DC主要发挥抗原摄取作用,摄取抗原后DC成熟并由非淋巴器官到归巢到淋巴结,活化机体初始性淋巴细胞,介导了细胞免疫和体液免疫。

N Mineralization as Affected by Long-Term N Fertilization and Its Relationship with Crop N Uptake

A field experiment established in 1997 was conducted to study the effect of long-term N fertilizer application on N mineralization in a paddy soil determined using a laboratory anaerobic incubation followed with a field incubation and to measure the relationship between in situ N mineralization and crop N uptake. To estimate N mineralization in the laboratory, soil samples were collected from plots with N application at different rates for six years and were incubated. Soils treated with fertilizer N mineralized more N than unfertilized soils and mineralization increased with N application rates. Also, the fraction of total N mineralized increased with increasing N fertilizer application. These findings meant that a substantial portion of previously applied N could be recovered slowly over time in subsequent crops. The field incubation of the plot receiving no fertilizer N showed that the NH4^＋-N concentration varied greatly during the rice-growing season and seasonal changes of N mineralization were due more to accumulation of NH4^＋-N than NO3^-N. Hice N uptake increased up to a maximum of 82 kg N ha^-1 during the season. The close agreement found between in situ N mineralization and rice N uptake suggested that the measurement of in situ N mineralization could provide useful recommendations for adequate fertilizer N application.

Difference in Selenium Accumulation in Shoots of Two Rice Cultivars

Two japonica rice （Oryza sativa L.） cultivars, Xiushui 48 and S. Andrea, differing in their ability to accumulate Se in the grain （as high as a three-fold difference）, were compared for selenium （Se） accumulation in their shoots when their growth media was supplied with different forms of Se. Results indicated that when treated with 0.25μmol L^-1 Na2SeO3, Xiushui 48 accumulation of Se in the shoots was significantly more rapid （P〈0.05） than S. Andrea, probably because of greater Se uptake and transport in Xiushui 48. Xiushui 48 rice seedlings had a higher shoot-Se accumulation rate and absorbed selenocysteine （Se-Cys） more rapidly than S. Andrea seedlings. However, when treated with Se as 0.25μmol L^-1 selenomethionine （Se-Met）, the S. Andrea seedlings＇ accumulation rate was significantly greater （P〈0.05） than that of Xiushui 48. Possibly, the high Se accumulation rate of Xiushui 48 seedling shoots compared to S. Andrea shoots was the result of a higher capacity of Xiushui 48 to transform selenite to organic Se compounds and a higher selenite uptake rate.

抗抑郁候选新药SIPI6116手性异构体的合成及大鼠体内药动学研究

目的设计合成对5-HT/NE/DA再摄取有抑制作用的抗抑郁候选化合物SIPI6116的两个手性异构体,并对SIPI6116、(+)-SIPI6116和(-)-SIPI6116在大鼠体内的药动学特征进行研究。方法以邻二氯苯(1)和3-氯丙酰氯(2)为原料,经Friedel-Crafts酰基化反应得到3-氯-1-(3,4-二氯苯基)-1-丙酮(3),3与二甲胺盐酸盐经取代反应得到1-(3,4-二氯苯基)-3-二甲氨基-1-丙酮(4),4经硼氢化钠还原得到1-(3,4-二氯苯基)-3-二甲氨基-1-丙醇(5),5经手性拆分后与对甲苯磺酰氯、吗啉采用“一锅法”制得(+)-SIPI6116和(-)-SIPI6116。采用高效液相-串联质谱(LC-MS/MS)测定大鼠血浆和脑组织中SIPI6116消旋体及其两个手性异构体的浓度,并考察其在大鼠体内的药动学特征以及在体内是否发生构型转化。结果与结论合成并考察了SIPI6116及其两个手性异构体在大鼠体内的药动学特征,结果显示(-)-SIPI6116的药动学数据更理想,且两个光学异构体在体内未发生构型转化,研究结果为(-)-SIPI6116的后续开发提供了依据。

In vitro and in vivo antitumor efficacy of CLA-PTX on B16-F10 melanoma cells

The purpose of this study was to investigate the potential antitumor efficacy of conjugated linoleic acid-paclitaxel （CLA-PTX） on B16-F10 melanoma cell line in vitro and in vivo. The in vitro cytotoxicity, apoptosis and cell cycle of CLA-PTX were investigated. The in vitro cellular uptake of CLA-PTX in B16-F10 cells was also analyzed. The antitumor activity of CLA-PTX was also evaluated in B16-F10 tumor-bearing C57BL6/N mice in vivo. The in vitro cytotoxicity results showed that the IC50 of the CLA-PTX is （4.25±0.43） μM, compared with that of （6.70±0.80） μM in PTX treatment group （P〈0.01）. CLA-PTX increased the percentage of total apoptotic cells compared with that of control and PTX treatment groups （P〈0.01）. Compared with untreated cells, CLA-PTX arrested cell cycle progression at the S phase, whereas PTX caused accumulation of cell at GE-M phase both along with the reduction of the cellular fraction arrested at the G1 phase. The amount of cellular uptake of CLA-PTX was significantly higher than that of PTX （P〈0.01）. The in vivo antitumor activity of CLA-PTX was significantly higher than that of control and PTX treatment groups （P〈0.01 or P〈0.05）. In conclusion, our study demonstrated that CLA-PTX has significant antitumor activity in B 16-F 10 cell line.

The anti-tumor efficacy of c9,t11-CLA-PTX and t10,c12-CLA-PTX on MCF-7 breast cancer cells:in vitro and in vivo

Considering the results of our previous research that conjugated linoleic acid mixture-paclitaxel （CLA-mixture-PTX） possesses anti-tumor activity against melanoma and brain glioma, the purpose of this study was to investigate the potential anti-tumor efficacy of cis-9, trans- 1 1-conjugated linoleic acid-paclitaxel （c9, tl 1-CLA-PTX） and trans- 1 O, cis- 12-conjugated linoleic acid-paclitaxel （tl0, c12-CLA-PTX） on MCF-7 breast cancer cell line in vitro and in vivo. The in vitro cytotoxicity, apoptosis induction effect and cell cycle arresting effect of c9, t1 1-CLA-PTX and t10, c12-CLA-PTX were investigated. The in vitro cellular uptake of c9, tl 1-CLA-PTX and tl0, cl2-CLA-PTX in MCF-7 cells were also analyzed. Besides, the anti-tumor activity of c9, tl 1-CLA-PTX and tl0, cl2-CLA-PTX was evaluated in MCF-7 tumor bearing nude mice in vivo. The in vitro cytotoxicity results showed that the value of ICs0 of the tl 0, c l2-CLA-PTX is （0.17±0.02） μM, compared with that of （1.08±0.15） μM in CLA-mixture-PTX and （6.50±1.20） μM in c9, tl 1-CLA-PTX treatment group （P〈0.01）. Both tl0, cl2-CLA-PTX and c9, t l 1-CLA-PTX increased the percentage of total apoptotic cells compared with that of control （P〈0.01）. And the rank of apoptosis induction efficacy was t 10, c 12-CLA-PTX〉CLA-mixture-PTX〉c9, t 11-CLA-PTX （P〈0.01）. Compared with untreated cells, the tl0, c12-CLA-PTX and c9, tl 1-CLA-PTX arrested cell cycle progression at the S and G2-M phase. The amount of cellular uptake of t 10, c 12-CLA-PTX was significantly higher than that of CLA-mixture-PTX （P〈0.01）, which was significantly higher than that of c9, t1 1-CLA-PTX （P〈0.01）. The rank of in vivo anti-tumor activity was tl0, c12-CLA-PTX〉CLA-mixture-PTX〉 c9, t1 1-CLA-PTX （P〈0.01）. In conclusion, our study demonstrated that both tl0, cl2-CLA-PTX and c9, tl 1-CLA-PTX has significant anti-tumor activity in MCF-7 cell line. And while c9, tl 1-CLA-PTX showed weaker inhibitory effect than CLA-mixture-PTX, stronger inhibitory effect was presented by t10, c12-CLA-PTX, which could be a promising alternative for CLA-mixture-PTX.