轻稀土与联吡啶和菲罗啉三元配合物的合成与表征

合成了稀土（Ｌｎ）与２，２－联吡啶（Ｌ１）、１，１０－菲罗啉（Ｌ２）的三元固态配合物。通过元素分析、ＩＲ谱、ＴＧＡ谱和摩尔电导等对该系列配合物进行了表征，实测结果与通式ＬｎＬ１Ｌ２Ｃｌ３·３Ｈ２Ｏ符合较好。抗菌试验表明，该系列配合物有较强的广谱抗菌作用。     

菲啰啉对不同氧化剂和多柔比星所致CHL细胞DNA链断裂的影响

目的 为了研究菲啰啉对2种氧化剂和抗癌药多柔比星诱发细胞DNA损伤的影响, 并初步探讨其损伤机制。方法 用不同浓度菲啰啉预处理CHL细胞30 min, 再分别加入3种不同染毒受试物,共同培养一定时间(0.3 mmol·L^-1重铬酸钾：105 min； 0.5 μmol·L^-1多柔比星：5 min； 0.4 mmol·L^-1过氧化氢(H₂O₂)：25 min)后, 用碱性单细胞凝胶电泳方法(ASCGE)测定DNA链断裂情况, 并同时以菲啰啉与二甲亚砜(DMSO，0.33 mol·L^-1)比较对H₂O₂致DNA损伤中·OH的产生和清除。结果 3种染毒受试物均可明显引起CHL细胞DNA链断裂；而当3 μmol·L^-1菲啰啉预处理后, 可使重铬酸钾、H₂O₂所致DNA迁移长度和细胞拖尾率明显降低, 并超过DMSO降低H₂O₂的损伤作用, 当菲啰林浓度升至12 μmol·L^-1时, 可完全消除这两种因素所致的DNA链断裂损伤；10 μmol·L^-1菲啰啉可抑制多柔比星所致DNA损伤, 但浓度直至60 μmol·L^-1仍不能完全消除多柔比星的损伤作用。结论 菲啰啉对2种氧化剂和多柔比星所致DNA损伤均有不同程度的防护作用,同时提示重铬酸钾和H₂O₂所致的DNA损伤主要与需过渡金属离子参与的·OH产生有关, 而多柔比星所致损伤仅部分与此有关。     

新型氮杂大环化合物的合成与表征

目的与方法以邻菲罗啉5,6-二酮和乙二胺为原料,合成了两个新型大环化合物2,3,8,9-二邻菲罗啉-1,4,7,10-四氮杂十二环-1,3,7,9-四烯(化合物1)和2,3,8,9-二邻菲罗啉并-1,4,7,10-四氮杂十二环-1,3,5,7,9,11-六烯(化合物2)。采用元素分析,电喷雾质谱,核磁共振以及电子吸收光谱和荧光发射光谱对化合物进行表征。结果与结论确定了目标产物的结构,并且推断出在过量的乙二胺存在下,化合物2的脱氢机理。     

Modulation of streptonigrin's clastogenic effects in CHO cells by the metal-chelating agent 1,10-phenanthroline.

The effect of the metal-chelating agent 1,10-phenanthroline (PNT) on the clastogenesis induced by streptonigrin (SN) in CHO cells was investigated. When CHO cells were exposed to SN, chromosomal aberrations (CAs) and sister-chromatid exchanges (SCEs) were formed in a dose-dependent manner (P < 0.05). When PNT was present in the culture medium, the production of CAs by SN was strongly inhibited (inhibition range = 54.9-80.8%). Similarly, the induction of SCEs by SN was significantly decreased by the addition of PNT to CHO cultures (P < 0.05), although the effect was minor. This finding suggests that intracellular transition metals are implicated in the clastogenesis by SN, and that the Fenton reaction (Fe(2+) + H2O2 --> OH* + OH(-) + Fe(3+)) may be responsible for the production of CAs by this compound. Moreover, the fact that PNT did not completely inhibit the induction of SCEs by SN suggests that this phenomenon might be attributable to a different mechanism, in which transition metals and free radicals play a minor role.     

响应面法优化鹰嘴豆铁蛋白提取工艺

目的： 优选鹰嘴豆铁蛋白的提取工艺。 方法： 在单因素试验基础上,选择缓冲液pH、料液比、盐析盐摩尔浓度为自变量,干膏量及铁蛋白、总蛋白得率为响应值,根据Box-Behnken原理采用三因素三水平响应面分析法优选鹰嘴豆铁蛋白的提取工艺参数。 结果： 最佳提取工艺条件为缓冲液pH 7.46,料液比1：4,盐析盐摩尔浓度50 mmol·L^-1;铁蛋白得率0.002 556%,与理论预测值0.002 633%偏差较小。 结论： 采用响应面法优选的鹰嘴豆铁蛋白提取工艺稳定合理,为提高铁蛋白得率和植物补铁制剂的开发利用提供参考。     

Spermine-Induced Alteration of Small Intestine in Suckling Rat: Involvement of Apoptosis or Zn2+ Enzymes?

Polyamines are of great importance in several physiological processes, such as cell proliferation and differentiation. The ingestion of spermine by suckling rats induces precocious maturation of their small intestine. Shortly after ingestion, spermine produces cell elimination at the villous top. The origin of this exfoliation was investigated to determine whether it was due to apoptosis. Wistar rats were orally treated with spermine. Apoptosis was analyzed in their small intestine by Tdt-mediated dUTP-fluorescein nick-end labeling reaction, caspase-3-like analysis, and DNA laddering. Polyamine content was measured by HPLC. The intestinal transitory alteration appeared as soon as 2 hr after spermine administration. Apoptosis events increased strongly at the same moment in the small intestine. They were evidenced by Tdt-mediated dUTP-fluorescein nick-end labeling analysis, DNA laddering, and caspase-3-like activity. Changes observed are consistent with apoptosis, but caspase inhibitor did not reduce intestinal alteration, as did Zn²⁺ chelator.     

Interactions of phospholipase D and cytochrome P450 protein stability

Previous studies have suggested a relationship between cytochrome P450 (P450) 3A (CYP3A) conformation and the phospholipid composition of the associated membrane. In this study, we utilized a novel microsomal incubation system that mimics many of the characteristics of CYP3A degradation pathway that have been observed in vivo and in cultured cells to study the effects of phospholipid composition on protein stability. We found that addition of phosphatidylcholine-specific phospholipase D (PLD) stabilized CYP3A in this system, but that phosphatidylinositol-specific phospholipase C (PLC) was without effect. Addition of phosphatidic acid also stabilized CYP3A protein in the microsomes. The use of 1,10-phenanthroline (phenanthroline), an inhibitor of PLD activity, decreased CYP3A stability in incubated microsomes. Similarly, 6-h treatment of primary cultures of rat hepatocytes with phenanthroline resulted in nearly complete loss of CYP3A protein. Treatment of rats with nicardipine or dimethylsulfoxide (DMSO), which have been shown to affect CYP3A stability, altered the phospholipid composition of hepatic microsomes. It did not appear, though, that the changes in phospholipid composition that resulted from these in vivo treatments accounted for the change in CYP3A stability observed in hepatic microsomes from these animals.     

Design,synthesis, and antiprotozoal evaluation of new 2,9‐bis[(substituted‐aminomethyl)phenyl]‐1,10‐phenanthroline derivatives

A series of new 2,9‐bis[(substituted‐aminomethyl)phenyl]‐1,10‐phenanthroline derivatives was synthesized, and the compounds were screened in vitro against three protozoan parasites (Plasmodium falciparum, Leishmania donovani, and Trypanosoma brucei brucei). Biological results showed antiparasitic activity with IC₅₀ values in the μm range. The in vitro cytotoxicity of these molecules was assessed by incubation with human HepG2 cells; for some derivatives, cytotoxicity was observed at significantly higher concentrations than antiparasitic activity. The 2,9‐bis[(substituted‐aminomethyl)phenyl]‐1,10‐phenanthroline 1h was identified as the most potent antimalarial candidate with ratios of cytotoxic‐to‐antiparasitic activities of 107 and 39 against a chloroquine‐sensitive and a chloroquine‐resistant strain of P. falciparum, respectively. As the telomeres of the parasite P. falciparum are the likely target of this compound, we investigated stabilization of the Plasmodium telomeric G‐quadruplexes by our phenanthroline derivatives through a FRET melting assay. The ligands 1f and 1m were noticed to be more specific for FPf8T with higher stabilization for FPf8T than for the human F21T sequence.     

A sensitive flow injection chemiluminescence method for the determination of progesterone

A sensitive flow injection (FI) chemiluminescence (CL) method was developed for the determination of trace amounts of progesterone. This method was based on the luminescent properties of the tris(1,10‐phenanthroline) ruthenium(II) ‐ potassium permanganate (KMnO₄) ‐ progesterone in acidic medium sensitized by Na₂SO₃. With the peak height as a quantitative parameter applying optimum conditions, the relative CL intensity was linear with progesterone concentration in the range of 1.0 × 10^?10 ～ 6.0 × 10^?9 g·ml^?1 and 6.0 × 10^?9 ～ 4.0 × 10^?8 g·ml^?1 with a detection limit of 7.1 × 10^?11 g·ml^?1. The relative standard deviation (RSD) was 2.79% for 1.0 × 10^?8 g·ml^?1 progesterone (n = 11). The proposed method held low detection limit and was successfully applied to determination of progesterone in pharmaceutical preparations. The possible CL reaction mechanism was also discussed. Copyright © 2011 John Wiley & Sons, Ltd.     

人参皂苷Re体外抗氧化能力及其对血清剥夺神经细胞作用的研究

目的:探讨三七中人参皂苷Re体外抗氧化能力和对血清剥夺损伤神经细胞的作用.方法:通过体外清除二苯代苦味酰肼(1,1-Diphenyl-2-picrylhydrazyl radical 2,2-Diphenyi-1-(2,4,6-trinitrophenyl)hydrazyl,DPPH)自由基法、还原能力测定法测定人参皂苷Re体外抗氧化能力;通过细胞计数试剂盒(cell counting kit-8,CCK-8)测定人参皂苷Re对神经细胞血清剥夺损伤的保护作用.结果:人参皂苷Re体外自由基清除率不足10％,还原能力不足12％,低于阳性对照维生素E,但对血清剥夺损伤的神经细胞保护作用非常显著(细胞存活率最高78％),活性高于同浓度下的维生素E.结论:人参皂苷Re体外抗氧化能力微弱,不是通过提供电子来达到抗氧化作用,但可保护血清剥夺损伤的神经细胞,提高神经细胞成活率,抑制其损伤、凋亡的作用.