2'-(1-萘亚甲基)-2-羟基苯甲酰腙的合成、晶体结构及抑菌活性

某些席夫碱化合物具有抗肿瘤、抗菌等生物活性,在生化反应中起到转氨基作用,碳氨双键是该类化合物具有抗菌活性的效应基团。而含-CONHN=CH-基团的酰腙类化合物具有特殊的生物活性和强配位能力,在农药、医药和分析试剂等方面一直是人们广泛研究的对象,某些该类化合物在治疗一些疾病和抑菌方面已有广泛的应用。为了进一步探索高效抗菌药物,本研究组在从事席夫碱及腙类化合物的合成、生物活性的测定等工作中合成了标题化合物;并测定了标题化合物对枯草芽孢杆菌、肺炎克氏菌、铜绿脓杆菌、大肠杆菌和金黄色葡萄球菌的抑菌活性。     

钴镁铁水滑石的合成、表征及衍生复合氧化物酸碱催化活性研究

以Co(NO3)2.6(H2O)、Mg(NO3)2.6(H2O)和Fe(NO3)3.9(H2O)为原料,以NaOH和Na2CO3为沉淀剂采用低过饱和共沉淀法合成了CoMgFe系列的碳酸根水滑石,通过XRD,IR,TG-DTA,等手段对样品进行测试和表征,X-衍射结果显示,其M2 /M3 投料物质的量比为2-4得到的水滑石为理想构型。经焙烧后,发现其复合氧化物对乙醇催化脱水、脱氢反应有一定的活性。     

低聚水溶性壳聚糖修饰阿魏酸及细胞毒活性研究

阿魏酸（Ferulic acid,FA）,化学学名为4-羟基3-甲氧基苯丙烯酸,是当归、川芎、木贼、升麻、樟白皮等中药材水溶性提取物中主要的单体活性成份,属天然酚酸类化合物,由于其优良的抗氧化性,故对一些肿瘤表现出抑制作用,但活性不是很好。另外,由于FA的稳定性差,在人体内不参与肝肠循环等缺陷也影响其药效的发挥。     

Synthesis, Structure and Biological Activities of 2-Methylthio-3-cyano-7-（4-methoxyphenyl）- pyrazolo[1,5-a]pyrimidine

1INTRODUCTION Pyrazolo[1,5-a]pyrimidine derivatives have shown various biological activities in the terms of antibac-terial,antischistosomal and xanthine oxidase inhibi-tors[1~5].The enaminones are highly reactive inter-mediates and have been extensively used as build-ing blocks in organic synthesis especially in the he-terocyclic compounds[6~8].In addition,a great deal of interest has been focused on the synthesis of py-razolo[1,5-a]pyrimidine through versatile enamino-nes because of thei…     

Supercritical CO2 Plant Extracts Show Antifungal Activities against Crop-Borne Fungi

Fungal infections of cultivated food crops result in extensive losses of crops at the global level, while resistance to antifungal agents continues to grow. Supercritical fluid extraction using CO₂ (SFE-CO₂) has gained attention as an environmentally well-accepted extraction method, as CO₂ is a non-toxic, inert and available solvent, and the extracts obtained are, chemically, of greater or different complexities compared to those of conventional extracts. The SFE-CO₂ extracts of Achillea millefolium, Calendula officinalis, Chamomilla recutita, Helichrysum arenarium, Humulus lupulus, Taraxacum officinale, Juniperus communis, Hypericum perforatum, Nepeta cataria, Crataegus sp. and Sambucus nigra were studied in terms of their compositions and antifungal activities against the wheat- and buckwheat-borne fungi Alternaria alternata, Epicoccum nigrum, Botrytis cinerea, Fusarium oxysporum and Fusarium poae. The C. recutita and H. arenarium extracts were the most efficacious, and these inhibited the growth of most of the fungi by 80% to 100%. Among the fungal species, B. cinerea was the most susceptible to the treatments with the SFE-CO₂ extracts, while Fusarium spp. were the least. This study shows that some of these SFE-CO₂ extracts have promising potential for use as antifungal agents for selected crop-borne fungi.     

Effect of thermosonication pre-treatment on mung bean (Vigna radiata) and white kidney bean (Phaseolus vulgaris) proteins: Enzymatic hydrolysis,cholesterol lowering activity and structural characterization

Protein hydrolysates have attained great attention due to a good nutritive food ingredient and higher biological activities. In this study, thermosonication, ultrasound and heat were used as a pre-treatment to obtain (<3KDa) hydrolysate from mung bean and white kidney bean to understand the mechanism of cholesterol absorption into micelle and inhibition of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA) activity. Size exclusion high performance liquid chromatography (SE-HPLC) results of mung bean showed that the concentration of peptides (0.5KDa-1KDa and 1-3KDa) in the hydrolysate were significantly (p < 0.05) increased after thermosonication while, the peptides concentration (1-3KDa) in white kidney bean was significantly (p < 0.05) decreased. Thermosonication of mung bean hydrolysate exhibited higher inhibition of cholesterol solubilization, hydrophobicity and antioxidant activities. In addition, there was no difference observed in HMG-CoA activity and hydrophobicity between ultrasound alone and ultrasound combined with heat i.e. thermosonication treated hydrolysate of white kidney bean. Changes in secondary and tertiary structures were also analyzed under different processing conditions with maximum change due to thermosonication. Results indicated that mung bean hydrolysate had a great potential for inhibition of cholesterol synthesis and its solubility in the micelle, antioxidant activity and also convinced for its application in food and nutraceutical industries.     

Antifungal Sesquiterpenoids from Michelia formosana Leaf Essential Oil against Wood-Rotting Fungi

Michelia formosana (Kanehira) Masamune is a broad-leaved species widespread in East Asia; the wood extract and its constituents possess antifungal activity against wood-decay fungi. Antifungal activities of leaf essential oil and its constituents from M. formosana were investigated in the present study. Bioassay-guided isolation was applied to isolate the phytochemicals from leaf essential oil. 1D and 2D NMR, FTIR, and MS spectroscopic analyses were applied to elucidate the chemical structures of isolated compounds. Leaf essential oil displayed antifungal activity against wood decay fungi and was further separated into 11 fractions by column chromatography. Four sesquiterpenoids were isolated and identified from the active fractions of leaf essential oil through bioassay-guided isolation. Among these sesquiterpenoids, guaiol, bulnesol, and β-elemol have higher antifungal activity against brown-rot fungus Laetiporus sulphureus and white-rot fungus Lenzites betulina. Leaf essential oil and active compounds showed better antifungal activity against L. sulphureus than against L. betulina. The molecular structure of active sesquiterpenoids all contain the hydroxyisopropyl group. Antifungal sesquiterpenoids from M. formosana leaf essential oil show potential as natural fungicides for decay control of lignocellulosic materials.     

The Influence of Synthesis Conditions on the Antioxidant Activity of Selenium Nanoparticles

Selenium nanoparticles (SeNPs) have attracted great attention in recent years due to their unique properties and potential bioactivities. While the production of SeNPs has been long reported, there is little news about the influence of reaction conditions and clean-up procedure on their physical properties (e.g., shape, size) as well as their antioxidant activity. This study takes up this issue. SeNPs were synthesized by two methods using cysteine and ascorbic acid as selenium reductants. The reactions were performed with and without the use of polyvinyl alcohol as a stabilizer. After the synthesis, SeNPs were cleaned using various procedures. The antioxidant properties of the obtained SeNPs were investigated using DPPH and hydroxyl radical scavenging assays. It was found that their antioxidant activity does not always depend only on the nanoparticles size but also on their homogeneity. Moreover, the size and morphology of selenium nanoparticles are controlled by the clean-up step.     

A new flavonoid glycoside from Elsholtzia bodinieri

A new flavonoid glycoside, eriodictyol 7-O-(6″-caffeoyl)-β-D-glucopyranoside (1), along with 14 known compounds, were isolated from the whole plants of Elsholtzia bodinieri. All of the structures were determined by spectroscopic methods and chemical transformation. Compound 1 and luteolin (9) exhibited potent anti-HCV activities with a selective index of 135.85 and 20.84, respectively.     

Synthesis and Crystal Structure of 4-{[（1E）1- （2-Hydroxy-3-methoxyphenyl）methylidene]amino}- 1,5-dimethyl-2-phenyl-2,3-dihydro-1H-pyrazol-3-one

The title Schiff base compound,C19H19N3O3,a derivative of antipyrine,has been synthesized and characterized by elemental analysis,IR,and single-crystal X-ray diffraction.The crystal belongs to the monoclinic system,space group C2/c,with α = 27.935(5),b = 7.553(1),c =16.692(3) (A),β = 105.810(3)°,Z= 8,V= 3388.7(10) (A)3,Dc = 1.323 g/cm3,Mr = 337.37,λ(MoKα) =0.71073 (A),μ = 0.091 mm-1,F(000) = 1424,R = 0.0630 and wR = 0.1273.A total of 3513 unique reflections were collected,of which 2112 with I ＞ 2σ(I) were observed.The molecular structure adopts a trans configuration about the C=N double bond.The pyrazoline and C(1)～C(6) pheny1 ring are approximately coplanar (mean deviation from the combined plane is 0.069(3) (A)),with the dihedral angle of 9.7(2)°.The preliminary biological tests show that the compound has high antibacterial activities.