Isolation and Insecticidal Activity of Essential Oil from Artemisia lavandulaefolia DC. against Plutella xylostella

Many plants show significant biological activity against pests due to their unique chemical constituents. It is important to identify effective constituents for their development and utilization as botanical pesticides. Our previous study showed that Artemisia lavandulaefolia essential oil had biological activity against Plutella xylostella. Here, we isolated and identified the constituents of essential oil from A. lavandulaefolia by silica gel column chromatography. The main constituents identified were eucalyptol and caryophyllene oxide, and they were confirmed by gas chromatography–mass spectrometry (GC–MS). Eucalyptol and caryophyllene oxide showed strong contact toxicity against P. xylostella larvae after 24 h of application (Median lethal dose, LD₅₀ = 76.97 μL/mL and 20.71 mg/mL. Furthermore, the two active constituents against P. xylostella adults showed significant fumigant activity (Mmedian lethal concentration, LC₅₀ = 3.25 μL/L and 1.06 mg/L, respectively. Finally, we measured the detoxification enzymes and acetylcholinesterase of the larvae treated with active constituents. The eucalyptol-treated larvae displayed enhanced carboxylesterase (CarE) and glutathione-S-transferase (GST) activities in an in vivo experiment, but it was lower for acetylcholinesterase (AchE) activity. The activities of the CarE and GST significantly decreased when exposed to caryophyllene oxide. In general, the two active constituents, eucalyptol and caryophyllene oxide, showed high insecticidal activity, which demonstrates their potential to be used as natural insecticides.     

(E)-4-芳酰氧基苯基丙烯酸类衍生物的合成及抑癌活性(英文)

本文报道了 18个 (E) 4 芳酰氧基苯基丙烯酸类衍生物的设计与合成。其中 17个化合物未见文献报道。所有目标物的化学结构经元素分析、红外光谱和核磁共振氢谱确证。初步体外抑癌试验结果表明 ,在 0 3μmol·L- 1 浓度下化合物 3e、3f、3g、3h、3k、4h和 4j对小鼠艾氏腹水癌 (EAC)呈现显著抑制作用。     

(E)-4-酰氧基苯基丙烯酸类衍生物的合成及抑癌活性

报道了18个(E)-4-酰氧基苯基丙烯酸类衍生物的设计与合成。其中17个化合物未见文献报道。所有目标物的化学结构经元素分析、红外光谱和核磁共振氢谱确证。初步体外抑癌试验结果表明,化合物3e、3f、3g、3h、3k、4h和4j在0.3μmol·L-1浓度下对小鼠艾氏腹水癌(EAC)呈现显著抑制作用。     

Synthesis and Pharmacological Activity of S(-)-2-Amino-2-Methyl-3-Phenylpropanoic Acid

Pharmaceutical Chemistry Journal - Taking into account the high efficacy of 2-arylpropionic acid derivatives among NSAIDs and based on their SARs, we have evaluated the anti-inflammatory,...     

(R)-(-)-扁桃酸的不对称生物合成

研究了生物不对称催化苯乙酮酸合成（R）-（-）-扁桃酸的方法。通过对38株菌进行初筛,获得对底物苯乙酮酸具有较高转化活性的出发菌株假丝酵母Ca.3。进一步紫外与微波诱变,得到具有高转化率与高对映体选择性的突变菌株Ca.3.37.48。在转化培养中,选择初始底物浓度30mmol/L、pH7.0、温度32℃的条件,（R）-（-）-扁桃酸得率86.5%,对映体过量值为99.5%。     

N-〔3-(1H-1,2,4-三唑-1-基)-2-(2,4-二氟苯基)-2-羟基-丙基〕-氨基乙酸及其衍生物的合成和抗真菌活性

设计合成了Ｎ〔３（１Ｈ１，２，４三唑１基）２（２，４二氟苯基）２羟基丙基〕氨基乙酸及其９个衍生物，均为未见文献报道的新化合物，初步药理试验表明：部分化合物对浅部真菌有一定的活性，除卡氏枝孢霉菌外，对其它深部真菌活性较弱，其中化合物（５ｅ），（５ｈ）对某些真菌的体外活性较强，明显优于氟康唑，但稍弱于酮康唑     

Isolation of (-)-Epicatechin from Pterocarpus marsupium and its Pharmacological Actions

(-)-Epicatechin has been isolated from the bark of PTEROCARPUS MARSUPIUM Roxb (Leguminosae). This flavonoid compound was tested for its activity on central nervous system, isolated frog heart preparations and blood sugar levels of rats. Preliminary acute toxicity studies were also carried out. It was observed that (-)-epicatechin did not have any effect on central nervous system of rats and mice, (-)-epicatechin had shown both positive chronotropic and inotropic effects on frog hearts, the effect of which is blocked by propranolol. The compound in higher doses caused hyperglycemia in rats and this effect is also blocked by propranolol, showing adrenergic type of activity. (-)-Epicatechin was found to have no untoward effect even in higher doses.     

汉麻果胶皂苷类成分分离及其抗真菌活性研究

目的获得汉麻果胶皂苷类成分的主要部位,进行抗真菌试验,测定其最小抑菌浓度值（M/C）。方法利用D101大孔树脂进行梯度洗脱,通过试管定性试验以及薄层色谱（TLC）法确定富集皂苷类成分洗脱部位,并采用微量液基稀释法研究其对4种常见致病真菌红色毛癣菌、须癣毛癣菌、犬小孢子菌和白色念珠菌的生物活性。结果80%浓度的洗脱物对红色毛癣菌、须毛癖菌、犬小孢子菌均具有抑制作用,其M/C值分别为16,8,2 ｜ig/mL。结论汉麻果胶皂苷类成分具有显著的抗真菌作用。     

Isolation and Preliminary Characterization of Proteinaceous Toxins with Insecticidal and Antibacterial Activities from Black Widow Spider (L. tredecimguttatus) Eggs

The eggs of black widow spider (L. tredecimguttatus) have been demonstrated to be rich in toxic proteinaceous components. The study on such active components is of theoretical and practical importance. In the present work, using a combination of multiple biochemical and biological strategies, we isolated and characterized the proteinaceous components from the aqueous extract of the black widow spider eggs. After gel filtration of the egg extract, the resulting main protein and peptide peaks were further fractionated by ion exchange chromatography and reversed-phase high performance liquid chromatography. Two proteinaceous components, named latroeggtoxin-III and latroeggtoxin-IV, respectively, were purified to homogeneity. Latroeggtoxin-III was demonstrated to have a molecular weight of about 36 kDa. Activity analysis indicated that latroeggtoxin-III exhibited neurotoxicity against cockroaches but had no obvious effect on mice, suggesting that it is an insect-specific toxin. Latroeggtoxin-IV, with a molecular weight of 3.6 kDa, was shown to be a broad-spectrum antibacterial peptide, showing inhibitory activity against all five species of bacteria tested, with the highest activity against Staphylococcus aureus. Finally, the implications of the proteinaceous toxins in egg protection and their potential applications were analyzed and discussed.     

蚯蚓中平喘蛋白组分的提取分离及其作用机制的初探

目的 初步研究蚯蚓平喘蛋白组分(Eisenia foetida protein,EP2)及其平喘活性.方法 以新鲜赤子爱胜蚓为原料,通过蛋白质的硫酸铵沉淀和离子交换色谱法,分离得到一组平喘活性蛋白成分(EP2).采用经典的肺阻力(RL)和动态肺顺应性(Cdyn)指标评价EP2对致敏豚鼠抗原攻击前后的肺功能变化;采用体外试验观察EP2拮抗白三烯D4引起豚鼠离体气管平滑肌的收缩反应;同时应用双向凝胶电泳-质谱技术对蛋白组分EP2进行了初步分析鉴定.结果 在整体试验中,EP2 16.8 mg·kg-1口含吞服预处理能明显抑制致敏豚鼠抗原攻击后引起的RL增加和Cdyn下降,作用稍弱于阳性对照药孟鲁司特;在离体试验中,EP2能明显拮抗白三烯D4收缩气管平滑肌的作用,作用强度与孟鲁司特接近;双向凝胶电泳-质谱技术分析证明蛋白组分EP2中含有蚯蚓种属中的蛋白F-I-0、F-I-1以及纤溶酶组分A,均为丝氨酸蛋白酶类胰蛋白酶家族成员.结论 EP2具有平喘作用,作用靶点可能通过拮抗白三烯受体,提示EP2的有效成分可能是白三烯拮抗剂.     

Synthesis and Antimicrobial Activity of 2-(4-Halophenyl)-2-(oxyaryl)propanes

Pharmaceutical Chemistry Journal -