沉淀法制备的紫杉醇白蛋白微粒包封率测定

采用沉淀法制备紫杉醇白蛋白微粒,采用高效液相色谱法(HPLC)测定紫杉醇质量浓度,以二氯甲烷为有机相,采用萃取法分离白蛋白微粒与游离药物,测定其包封率。结果表明:紫杉醇在10~100 mg·L-1范围内线性良好,平均回收率可达到97.6%~101.0%;有机溶剂萃取法测定紫杉醇白蛋白微粒包封率的平均回收率,达94.80%~101.67%。这种方法测定紫杉醇白蛋白微粒回收率准确可靠,适用于沉淀法制备的白蛋白微粒的包封率测定。     

红豆杉观赏盆景的制作与管理

红豆杉是一种观赏效果极佳的树种。通过对红豆杉盆景的制作及管理方法的研究,探讨红豆杉在人工条件下的生长状况,以期对新兴的红豆杉盆景产业化经营提供依据。     

紫衫醇对小鼠不同组织巨噬细胞功能的影响

为了探讨紫杉醇(Paclitaxel,PA)对小鼠不同组织巨噬细胞增殖和功能的影响。无菌操作制备小鼠腹腔、骨髓和脾脏巨噬细胞,在体外细胞培养体系中分别加入不同浓度40、80、160 ng/mL的PA和脂多糖(LPS)共培养,采用MTT法检测细胞增殖,ELISA和Griess法分别检测细胞分泌TNF-α和NO量,瑞氏-吉姆萨染色法测定腹腔巨噬细胞吞噬能力。结果表明： PA促进腹腔巨噬细胞和LPS诱导的腹腔和骨髓巨噬细胞增殖,但抑制脾脏和骨髓巨噬细胞以及LPS诱导的脾脏巨噬细胞增殖;PA抑制不同组织巨噬细胞分泌TNF-α,但促进腹腔和脾脏巨噬细胞分泌NO;PA提高了腹腔巨噬细胞吞噬鸡红细胞的能力。PA对小鼠不同组织巨噬细胞的免疫功能均有影响,这为进一步阐明PA的免疫调节机理提供了新的理论依据。     

甲氨蝶呤和紫杉醇对棉铃虫繁育能力的影响

[目的]研究药剂对棉铃虫繁育能力的影响,为安全有效的控制棉铃虫危害奠定理论基础.[方法]采用饲喂法处理棉铃虫成虫,对其产卵量、卵孵化率、实验前后成虫体重差、成虫寿命进行测定.[结果]甲氨蝶呤抑制棉铃虫产卵量效果优于紫杉醇,0.02;甲氨蝶呤处理的棉铃虫单雌产卵量(104粒)最低,比对照降低了72.48;;紫杉醇抑制卵孵化效果好于甲氨蝶呤,0.5;紫杉醇处理的卵孵化率为11.43;,平均校正不育卵率(89.19;)达到最高.甲氨蝶呤处理对雌虫的寿命比对照缩短l～2d.紫杉醇对棉铃虫雄虫有增重作用,而甲氨蝶呤对棉铃虫雌虫有减重作用.[结论]甲氨蝶呤和紫杉醇对棉铃虫繁育能力均有弱化作用,0.02;甲氨蝶呤弱化棉铃虫单雌产卵量效果最好,0.5;紫杉醇抑制卵孵化效果最佳.     

试验用和临床用紫杉醇诱导肝癌细胞凋亡的比较

[目的]为了探讨试验用和临床用紫杉醇对肝癌HepG2细胞凋亡诱导作用的差异。[方法]用不同浓度的试验用和临床用紫杉醇处理肝癌HepG2培养细胞后,通过显微观察和流式细胞术检测其细胞凋亡。[结果]临床用紫杉醇在终浓度为0.5、1.0和2.0 mg/ml时,24 h非常显著性诱导细胞凋亡,48 h诱导细胞凋亡更剧烈。试验用紫杉醇24 h在终浓度为2.5、5.0和10.0 mg/ml时,非常显著诱导细胞凋亡;当试验用紫杉醇浓度为2.5 mg/ml时,48 h诱导细胞凋亡更剧烈。当试验用紫杉醇浓度为5和10 mg/ml细胞凋亡率逐步变低,可能走向死亡。[结论]在诱导肝癌细胞凋亡中,试验用紫杉醇要比临床所用紫杉醇的浓度要高。     

Effect of metformin combined with paclitaxel on apoptosis and AMPK signaling in human breast cancer cells

AIM:To investigate the effect of metformin combined with paclitaxel on the viability and apoptosis of breast cancer cell line MCF-7 and its possible mechanism. METHODS:MCF-7 cells were treated with metformin at different concentrations (2, 5, 10, 20, 40 and 80 mmol/L) and in vitro cultured. The viability of MCF-7 cells was measured by MTT assay. Metformin at 2 mmol/L or paclitaxel at 2.4 mg/L alone or in combination was used to treat the cells, and compound C, an inhibitor of adenosine monophosphate-activated protein kinase (AMPK) signaling transduction pathway, was also used. The cells were divided into control group, metformin group, paclitaxel group, combination group, and combination +compound C group. The apoptosis of the cells was analyzed by flow cytometry. The expression of Bax, Bcl-2 and caspase-3 at mRNA and protein levels was determined by RT-qPCR and Western blot. The protein levels of AMPK and P21 were examined by Western blot. RESULTS:Metformin at different concentrations (2, 5, 10, 20, 40 and 80 mmol/L) significantly inhibited the cell viability in a concentration-dependent manner (P<0.05). Compared with control group, treatment with metformin at 2 mmol/L or paclitaxel at 2.4 mg/L alone or in combination significantly inhibited the cell viability, induced apoptosis (P<0.05), decreased the level of Bcl-2 (P<0.05), increased the levels of Bax and caspase-3 (P<0.05), and promoted the protein expression of AMPK and P21 (P<0.05). The effects of metformin and paclitaxel in combination were better than those of single drug treatment, while AMPK inhibitor weaken these effects. CONCLUSION:Metformin combined with paclitaxel inhibits the viability and induces the apoptosis of breast cancer MCF-7 cells by activating AMPK signaling pathway and regulating apoptosis signaling pathway.     

几种辅料对紫杉醇脂质体粒径及Zeta电位的影响

[目的]探讨处方中几种辅料的加入对紫杉醇（Tax）脂质体粒径大小及Zeta电位的影响。[方法]采用薄膜分散-超声法制备Tax脂质体,利用正交设计筛选出Tax脂质体的最优处方,并测定Tax脂质体的粒径及Zeta电位。[结果]脂质体粒径及稳定性与处方中所加油酸钠等辅料有显著关系,且随着辅料量的增加,脂质体粒径变小,Zeta电位值降低,稳定性提高。[结论]油酸钠等辅料能显著降低Tax脂质体粒径及Zeta电位值。采用优选工艺制备的Tax脂质体包封率高,粒径均匀,稳定性好。     

Antifungal activities of compounds isolated from the leaves of Taxus cuspidata var. nana against plant pathogenic fungi

Antifungal activities of seven compounds, taxinine (1), paclitaxel (2), phenylisoserine methyl ester (3), sciadopitysin (4), ginkgetin (5), isorhamnetin (6), and quercetin (7), isolated from the leaves of kyaraboku, Taxus cuspidata var. nana, against five plant pathogenic fungi, Gibberella fujikuroi, Cladosporium cucumeninum, Fusarium oxysporum, Colletotrichum fragariae, and Corynespora cassiicola, were investigated for utilization of extractives from trees of the genus Taxus. Also, the amounts of compounds 2 and 3 on the leaf surface was measured in relation to the antifungal activities of compounds. Taxinine (1) showed antifungal activity against G. fujikuroi, C. cucumeninum, F. oxysporum, and C. cassiicola. The minimum inhibitory concentration of taxinine for the four fungi was 0.4mol. In addition, from the results of antifungal tests, it may be concluded that paclitaxel on the leaves and stem of T. cuspidata var. nana does not play an important role as an antifungicide in the resistance of trees to plant pathogenic fungal attack.     

RAD001 promotes chemotherapeutic sensitivity of human endometrial carcinoma cells to paclitaxel via inducing autophagy

AIM:To explore the effect of mammalian target of rapamycin (mTOR) inhibitor RAD001 on chemotherapeutic sensitivity of endometrial carcinoma cells to paclitaxel. METHODS:MTT assay and PI staining were used to assess the cell death. The protein expression of LC3-I, LC3-II, mTOR and ULK1 was detected by Western blotting. ULK1 siRNA was used to abolish the activation of ULK1. RESULTS:RAD001 significantly inhibited the growth of human endometrial carcinoma cell lines Ishikawa and HEC-1A. RAD001 enhanced the inhibitory effect of paclitaxel on the growth of Ishikawa cells and HEC-1A cells. RAD001 induced autophagy and autophagic cell death by the inhibition of mTOR/p70S6K pathway and up-regulation of ULK1 expression. CONCLUSION: RAD001 enhances the inhibitory effect of paclitaxel on endometrial carcinoma cell growth by inducing autophagy and autophagic cell death.