茴香脑衍生物的合成工艺研究

以茴香脑为原料经H2O:氧化合成茴香脑环氧化物2-(4-甲氧基苯基)-3-甲基环氧乙烷,产率91%,并研究了溶剂配比、物料配比、催化剂用量、反应温度、反应时间等因素对产物产率的影响.实验结果表明:乙腈与甲醇体积比为1:5、茴香脑与H2O2的物质的量之比为1:2.5、原料与无水碳酸钠的物质的量之比为1:0.8、反应时间为...     

In vitro suppression of quercetin on hypertrophy and extracellular matrix accumulation in rat glomerular mesangial cells cultured by high glucose

Quercetin's protective effects on the glomerulosclerosis of diabetic nephropathy (DN) in rat mesangial cells were investigated. The cell cycles, type IV collagen and laminin, TGF-β₁ mRNA, Smad 2/3 and Smad 7, and activities of cell antioxidases were measured. Compared with the high glucose group, quercetin may decrease the cell percentages of G₀/G₁ phase, Smad 2/3 expression, laminin and type IV collagen, and TGF-β₁ mRNA level significantly. The antioxidant capacity, the cell percentages of S phase and Smad 7 expression was significantly increased by quercetin. These results suggest that quercetin is a protective agent against glomerulosclerosis in DN.     

Ginsenoside Rh1 inhibits the invasion and migration of THP-1 acute monocytic leukemia cells via inactivation of the MAPK signaling pathway

Ginsenoside Rh1 has been reported to possess antiallergic and anti-inflammatory activities, but its effects on monocytes remain to be determined. Herein, we investigated the effects of Rh1 on the expression of MCP-1 and CCR2, activation of MAPK signaling, and chemotaxis of monocytes. Treatment of Rh1 decreased the levels of MCP-1 and CCR2 and the expression of VLA5 and activated β1 integrin on the cell surface, and attenuated the phosphorylation of MAPKs. Based on these results, the inhibitory effects of Rh1 on monocyte function should be regarded as a promising new anti-inflammatory response with a potential therapeutic role against inflammation-dependent diseases.     

Kaurane-type diterpenoids from Chromoleana odorata, their X-ray diffraction studies and potent α-glucosidase inhibition of 16-kauren-19-oic acid

A new diterpenoid, 15-angeloyloxy-16,17-epoxy-19-kauronic acid (1), along with five known metabolites, 16-kauren-19-oic acid (2), 6′-hydroxy-2′,3′,4,4′-tetramethoxychalcone (3), isosakuranetin (4), acacetin (5), and kaempferide (6) was isolated from the organic extracts of the roots of Chromoleana odorata. Their structures were determined by spectroscopic evidences. The structures of 1 and 2 were further confirmed by single-crystal X-ray diffraction studies. Compound 2 exhibited significant α-glucosidase inhibitory and antibacterial activities against Escherichia coli and Bacillus subtilis.     

Semisynthesis and pharmacological investigation of lipo-alkaloids prepared from aconitine

Processed aconite drugs are widely used in Eastern medicine as painkillers and antirheumatic agents. It is known that the traditional processing of aconite drugs increases the amount of lipo-alkaloids. In order to obtain information about the pharmacological potential of these compounds, semisynthesis of 9 aconitine-derived lipo-alkaloids was carried out and their COX-1, COX-2 and LTB₄ formation inhibitory activities were investigated. It was found that compounds esterified with unsaturated fatty acids demonstrated significant COX-2 inhibitory effects, while in the COX-1 assay only 14-benzoylaconine-8-O-eicosapentaenoate exerted remarkable activity. The inhibition of LTB₄ formation was pronounced in cases of long chain fatty acid derivatives.     

Berberine attenuates lipopolysaccharide-induced impairments of intestinal glutamine transport and glutaminase activity in rat

Berberine was reported to protect against the intestinal injury and improve the survival rate in sepsis, and glutamine deficiency was considered to be correlated with mortality in sepsis. We found that berberine pretreatment ameliorated lipopolysaccharide-induced direct intestinal injury and mucosal hypoplasia and attenuated impairments of intestinal glutamine transport and glutaminase activity, B⁰AT1 mRNA and protein expressions, and glutaminase protein expression. These findings showed the first time that berberine pretreatment could improve intestinal recovery and attenuate the impairment of glutamine transport and glutaminase activity in rat sepsis. This might be one of the mechanisms for the beneficial effect of berberine on sepsis.     

Intestinal absorption of forsythoside A in different compositions of Shuang-Huang-Lian

Shuang-Huang-Lian (SHL), a traditional Chinese formula containing Lonicerae japonicae flos (LJF), Scutellariae radix (SR) and Forsythiae fructus (FF), is commonly used to treat acute upper respiratory tract infection, acute bronchitis and light pneumonia. Forsythoside A is one of the main active ingredients in Forsythiae fructus, a key herb in SHL. In the present study, effects of different compositions in SHL on the intestinal absorption of forsythoside A were investigated. The observations from in situ intestinal circulation model showed that A/%(h^− 1) of forsythoside A in FF + LSF, FF + SR and SHL were all reduced greatly compared with that in FF. However, in pharmacokinetics study, C_max and AUC_0 → 1440 of forsythoside A all increased and T_1/2 prolonged in SHL, FF + LJF and FF + SR compared with FF. The results indicated that the different compositions of SHL decreased absorption but increased bioavailability of forsythoside A, which may be related to its metabolism inhibited in intestine or liver.     

优质抗裂金丝小枣新品种‘沧金1号’选育研究

‘沧金1号’由沧州市农林科学院选育。果实圆形,个大,纵横径平均为2.61 cm×2.58 cm,成熟果实紫红色,平均单果重8.3 g,最大单果重12.7 g,制干率60%,鲜果含可溶性固形物32.08%,Vc451 mg/100 g,干枣含糖量73.5%;味甘甜微酸,品质上等,可食率97%,肉厚核小,制干率60%,适于鲜食和制干。株行距3 m×5m,嫁接后连续3 a开甲,株产鲜枣20.5 kg,产量13.84 t/hm2;较普通金丝小枣增产10%;连续4 a开甲,株产鲜枣21.5 kg,产量14.51 t/hm2,较普通金丝小枣增产13%;连续5 a开甲,株产鲜枣23.5 kg,产量15.86 t/hm2,较普通金丝小枣增产12%;耐瘠薄,抗盐碱,抗病能力强,抗裂果,裂果率低于3%;2010年12月通过河北省林木品种审定委员会审定。     

基于1:5万数据库研究土壤空间分异及其影响因素——以江苏省无锡和常州市为例

土壤数据库在土壤学研究工作中作为一种存储、分析工具的重要性是不言而喻的.本研究利用ArcGIS和Visual FoxPro建立了包括8 830个图斑、269个土壤剖面数据的无锡和常州市1：5万土壤数据库,根据“土壤质量演变规律与持续利用‘973＇项目”的土壤肥力质量指标（pH、速效磷和速效钾）和全国养分分级标准（全氮）编制出土壤表层（0～15 cm）pH、全氮、速效磷和速效钾的空间分异图,从中表明pH 1～2级的土壤占整个研究区面积90%左右;土壤养分全氮、速效磷和速效钾的空间分布有明显共同特征-太滆平田区养分含量要显著高于其他地区.对不同母质和不同土壤类型（亚类级别）间的土壤表层容重、粘粒、pH、有机质、全氮、全磷、全钾、速效磷和速效钾进行了方差分析,结果显示,除全氮之外,其他属性均有显著差异.在1：5万尺度范围内,成土母质对pH、容重、全磷、有机质和速效钾起到主导作用,土壤类型对pH起到主导作用,成土母质对土壤属性的影响程度要大于土壤类型.     

Speciation in the parthenogenetic oribatid mite genus Tectocepheus (Acari, Oribatida) as indicated by molecular phylogeny

Despite the lack of universal concepts for species and speciation, both sexual and asexual organisms are expected to diversify into discrete genotypic and morphological clusters. Species-rich clusters of parthenogenetic oribatid mites likely evolved in the absence of sexual reproduction. We used nucleotide sequences of the large and small rDNA genes (18S and 28S) and the coding genes for heat shock protein 82 (hsp82) and elongation factor-1 alpha (ef-1α) for phylogenetic analyses of three morphotypes of the parthenogenetic oribatid mite genus Tectocepheus. DNA sequence divergences of the different morphotypes were similar to those of sexual species in other organisms. Maximum likelihood analyses of single genes and combined data sets were largely congruent in reconstructing the phylogeny of the Tectocepheus species. The results suggest that the different morphotypes of Tectocepheus indeed evolved in the absence of sexual reproduction, and that Tectocepheus minor, Tectocepheus velatus and Tectocepheus sarekensis are best considered distinct species. Further, the results suggest that 18S rDNA, hsp82 and ef-1α are powerful markers for resolving phylogenetic relationships of oribatid mites. Saturation plots indicated that the D3-region of 28S is much more saturated than all other examined genes. This indicates that the D3-region is unsuitable for resolving ancient splits in oribatid mites.