科研成果 by Year: 2011

2011
Guiqiu Y, Chunrui YU, Xiulan YU, Xinghua QIU. Synthesis and bioactivity Baylis-Hillman adducts. Chemical Reagents. 2011;33:803-806.Abstract
Nineteen Baylis-Hillman adducts(BH)were synthesized at room temperature using trimethylamine or 1,4-diaza-bicyclo[2.2.2]octane(DABCO)as catalyst.Biological activity evaluations showed that methyl 2-((2,4-dichlorophenyl)(hydroxy)methyl)acrylate(BH-7)exhibited broadspectrum herbicidal activity,with 100%control of broadleaved weeds Zinnia elegans Jacq.(YOA)and Abutilon theophrasti Medic(VEL),80%and 75%control of grass weeds Echinochloa crusgalli(L.)Baeuv(BYG)and Digitaria sanguinalis(L.)Scop(CRG)at 2000 g ai/ha respectively.3-(hydroxy(4-nitrophenyl)methyl)but-3-en-2-one(BH-18)exhibi ted efficient fungicidal activity,with 100%control of Phytophthora infestans,50%and 50%control of Sclerophthoramacrospora thirumctal(RB)and bocrytis Cinerea Pers(CGM)at 25 g a.i./ha.以三甲胺、1,4-重氮二环[2,2,2]辛烷(DABCO)为催化剂,室温合成了19个Baylis-Hillman加成物(BH),生物活性测试发现 :在2 000 g a.i./ha的剂量下,2-((2,4-二氯苯基)(羟基)甲基)丙烯酸甲酯(BH-7)具有较为广谱的除草活性,对阔叶杂草百日草和苘麻的防效达到1 00%;对禾本科杂草稗草和马唐的防效分别为80%和75%;在25 g a.i./ha的剂量下3-(羟基(4-硝基苯基)甲基)丁-3-烯-2-酮(BH-18)对番茄晚疫病的防效为100%,对稻瘟病及蔬菜灰霉病的防效均 为50%。
Ma J, Qiu X, Zhou Y, Zhu T. PAHs Pollution and Spatial Distribution in Agricultural Soils of Dongguan. Acta Scientiarum Naturalium Universitatis Pekinensis. 2011;47:149-58.Abstract
Investigation on PAHs in agricultural soils in Dongguan, South China were conducted. A total of 59 agricultural soil samples were collected from sites representative of the region for analysis of contents of 16 PAHs. Results show that 13 PAHs were detected with detectable ratios above 90%, Fie, Phe, Chr and Bbf were detected in all 59 samples, the detectable ratio of Ant was the lowest (13.56%). Sigma PAHs in soil samples is ranged from 29 to 2184 mug/kg, and 44.07%, 8.47% and 3.39% soil samples were slightly, moderately and heavily polluted by PAHs, respectively. Compared with other regions, Dongguan city is higher in soil PAHs contents, which can be confirmed that the increase of PAHs in agricultural soils is connected with human activities closely. Principal component analvsis demonstrate that the above-said 16 PAHs in agricultural soils may have three major contributors, corresponding to biomass burning, volatilization of oil production, and coal burning respectively. It is found that environmental factors (temperature, humidity), soil characters (pH, organic materials) and other pollutants (heavy metals) can affect environmental behaviors of PAHs. By means of ordinary Kriging interpolation, spatial distribution of 16 PAHs were studied. The results indicate that 16 PAHs vary greatly in spatial distribution between types, PAHs contents in west-north soils are much higher than that in south-east soils, and the highest PAHs contents area is in Wangniudun town, which hint that there are some pollutant sources connected with poisonous wastes combustion.
Meng Y, Yan Z, Xia Y, Qiu X. Resent study and prospect of ursolic acid and derivatives. Chemical Reagents. 2011;33:39-43.Abstract
Ursolic acid(UA,3beta-hydroxy-urs-12-en-28-oic acid),a pentacyclic triterpene compound, exists abundantly in the plant kingdom as the major constituent of medicinal herbs. UA has been reported to display a remarkable spectrum of biochemical activities to influence processes capable of controlling cancer development. The pleuripotent anti-tumor activities of UA have stimulated the experts to research actively in this field. This paper summarizes the modification and pharmacological activity of ursolic acid derivatives according to literature and reports both at home and abroad熊果酸(UA,3beta-羟基-乌苏烷型-12-烯-28-羧酸),五环三萜化合物,作为药草的主要成分,存在于丰富的植物王国中.据报道,UA具有广 谱的生物活性,调控和控制肿瘤细胞形成.UA多效性的抗肿瘤活性激发了专家们在这方面的积极研究,现综合国内外文献报道,对熊果酸结构修饰物及其药理活性 进行综述
Ren A, Qiu X, Jin L, Ma J, Li Z, Zhang L, Zhu H, Finnell RH, Zhu T. Association of selected persistent organic pollutants in the placenta with the risk of neural tube defects. Proceedings of the National Academy of Sciences of the United States of America. 2011;108:12770-12775.Abstract
Persistent organic pollutants (POPs) have been associated with a wide range of adverse health effects. Our case-control study was performed to explore the association between placental levels of selected POPs and risks for neural tube defects (NTDs) in a Chinese population with a high prevalence of NTDs. Cases included 80 fetuses or newborns with NTDs, whereas the controls were 50 healthy, nonmalformed newborn infants. Placental concentrations of polycyclic aromatic hydrocarbons (PAHs), organochlorine pesticides, polychlorinated biphenyls, and polybrominated diphenyl ethers were analyzed by gas chromatography-mass spectrometry. The medians of PAHs, o,p'-isomers of dichlorodiphenyltrichloroethane (DDT) and metabolites, alpha- and gamma-hexachlorocyclohexane (HCH), and alpha-endosulfan were significantly higher in case placentas than in controls. PAH concentrations above the median were associated with a 4.52-fold (95% confidence interval (CI), 2.10-9.74) increased risk for any NTDs, and 5.84-(95% CI, 2.28-14.96) and 3.71-fold (95% CI, 1.57-8.79) increased risks for anencephaly and spina bifida, respectively. A dose-response relationship was observed between PAH levels and the risk of NTDs, with odds ratios for the second, third, and fourth quartiles, compared with the first, of 1.77-(95% CI, 0.66-4.76), 3.83-(95% CI, 1.37-10.75), and 11.67-fold (95% CI, 3.28-41.49), respectively. A dose-response relationship was observed for anencephaly and spina bifida subtypes. Similar results were observed for o,p'-DDT and metabolites, alpha-HCH, gamma-HCH, and alpha-endosulfan, whereas no dose-response relationship was observed for the last two pollutants. Elevated placental concentrations of PAHs, o,p'-DDT and metabolites, and alpha-HCH were associated with increased risks of NTDs in this population.
Xia Y, Meng Y, Qiu X, Yan Z. Process routing design on structure modifier of A-ring cleavage of ursolic acid. Chinese Traditional and Herbal Drugs. 2011;42:34-37.Abstract
目的设计一条原辅材料易得、低毒, 操作条件简单可控的熊果酸A环开环结构修饰的工艺路线, 从而得到更多具有广泛生物活性的熊果酸衍生物. 方法对类似的化合物进行国内外文献资料的调查与研究工作, 根据活性拼接原理提出设计路线. 结果提出自行设计的熊果酸A环开环结构修饰路线成本较低, 试剂低毒. 结论熊果酸A环结构修饰路线设计合理, 为熊果酸结构修饰物的深入研究提供基础