水回流法提取河湟红花籽粕中5-羟色胺衍生物的工艺研究

[目的]优选水回流法提取河湟红花籽粕5-羟色胺衍生物的最佳工艺条件。[方法]以5-羟色胺衍生物含量为指标,采用正交试验法对影响水回流法提取河湟红花粉粕中5-羟色胺衍生物的提取温度、提取时间、提取次数和料液比4个因素进行考察,优选出最佳提取方案。[结果]影响蒸馏水回流法提取河湟红花籽粕中5-羟色胺衍生物含量的因素依次为提取温度提取时间提取次数料液比;提取温度对5-羟色胺衍生物提取率具有明显影响;最佳提取方案为:提取温度80℃,提取时间1.5 h,提取次数3次,料液比1∶20(g/ml);在此条件下提取的5-羟色胺衍生物含量为0.66%。[结论]优选出了最佳提取工艺,为河湟红花籽粕的开发利用提供了理论依据。     

不同加成数C_(60)-β-丙氨酸衍生物的还原能力及金属螯合能力

为研究水溶性富勒烯衍生物抗氧化性能,通过控制反应配比,合成三种具有不同加成数目的水溶性C60-β-丙氨酸衍生物,C6(0NHCH2CH2COONa)nHn。采用红外、紫外、核磁共振、元素分析等手段对其进行结构表征。元素分析表明,三种不同加成数目的水溶性C60-β-丙氨酸衍生物A、B、C的加成数分别为2、4、8。同时考察三种衍生物的还原能力及金属螯合能力。结果表明,在还原能力体系中,当三种衍生物A、B、C浓度为2.5μmol.mL-1时,吸光度分别为0.424、0.612和1.040;在金属螯合能力体系中,三种衍生物A、B、C的半螯合浓度(当螯合率达到50%时,所需螯合物的浓度)分别为0.348、0.261和0.135μmol.mL-1。随着加成数目的增多,C60-β-丙氨酸衍生物的还原能力及金属螯合能力增强。     

穿心莲内酯衍生物对粘虫3种保护酶活力的影响

【目的】比较4种穿心莲内酯衍生物（A2、A4b、A4d、A4e）与羟基马桑毒素（Tutin）对粘虫生理代谢影响的差异,为探索新型植物源杀虫剂提供依据。【方法】粘虫3龄幼虫采用Tutin和A2、A4b、A4d、A4e经活体和离体2种方法处理后制备粗酶液,用比色法测定试虫超氧化物歧化酶（SOD）、过氧化氢酶（CAT）和过氧化物酶（POD）3种保护酶的活力,通过酶比活力对比分析活体处理不同时间酶活力的变化及2种处理方法酶活力水平的一致性。【结果】活体试验结果表明,Tutin、A2、A4b、A4d、A4e对粘虫体内POD、CAT活力有抑制作用,而对SOD活力有促进作用;在5种化合物中,整体而言,A4b和A4e对3种保护酶的影响较大。离体测定结果表明,粘虫体内POD、CAT和SOD活力的变化趋势与活体测定结果相似。【结论】A2、A4b、A4d、A4e和Tutin通过对粘虫幼虫3种保护酶活性的干扰,削弱了其对氧自由基和H₂O₂的解毒代谢功能,表明4种穿心莲内酯衍生物可以作为新型植物源杀虫剂。采用活体与离体2种方法对粘虫比活力的测定结果一致。     

Characterization of new photosynthesis-inhibiting imidazolidine derivatives. 1. Interpretation of post-emergence herbicidal performance from photosynthesis-inhibiting activity and systemicity

An attempt was made to account for quantitatively measured herbicidal performance of foliage-applied 5-hydroxy-3-methyl-2–oxo-imidazolidine-1-carboxamide derivatives by their photosynthesis-inhibiting activity and systemicity. Photosynthesis-inhibiting activity was estimated from the increase of chlorophyll fluorescence intensity in Chlorella vulgaris Beijer cells measured by a microplate scanner, and systemicity was also evaluated by computer-aided chlorophyll fluorescence imaging. The highest herbicidal performance was recorded for N-cyclohexyl-5-hydroxy-3-methyl-2-oxo-imidazo～idine-l-carboxamide, a compound with the second strongest photosynthesis-inhibiting activity and intermediate systemicity. Though neither photosynthesis-inhibiting activity nor systemicity showed significant correlation with the actual herbicidal performance in simple regression analyses, a high predictability was found for a multiple regression on both parameters as two independent variables, suggesting that these two factors work cooperatively in the field performance.     

Phenolic compounds in plant disease resistance

We propose that an important first line in plant defense against infection is provided by the very rapid synthesis of phenolics and their polymerization in the cell wall. This rapid synthesis, which leaves no time forde novo enzyme synthesis, is regulated by the extreme pH-dependence of the hydroxylase, catalyzing the formation of caffeoyl-CoA from 4-coumaroyl-CoA. We further propose that elicitor treatment or infection causes rapid membrane changes leading to a decrease in cytoplasmic pH. This decrease would have the effect of activating the hydroxylase.     

分子修饰前后人参皂苷体外抗马立克氏病毒鸡胚成纤维细胞模型的建立

用雏鸡将马立克氏病毒(MDV)血毒复壮,分离发病鸡淋巴细胞并接种于鸡胚成纤维细胞,观察其病变。获得适应鸡胚成纤维细胞(CEF)的MD强毒,通过电镜观察、琼脂扩散实验进一步鉴定病毒,并建立了MDV感染CEF细胞模型,为研究人参皂苷及其衍生物的体外抗病毒作用及其机制奠定基础。     

Dermatophytosis due to Microsporum persicolor (13 cases) or Microsporum gypseum (20 cases) in dogs

A retrospective study of 20 cases of dermatophytosis due to Microsporum gypseum and 13 cases due to Microsporum persicolor seen over an 8-year period is reported. These skin diseases are rare (1.3% of our canine case load) and pleomorphic, from localized erythematous and squamous or suppurative lesions (kerions) to extensive or generalized erythematous, alopecic, scaling, crusting and eventually papular and pustular dermatoses. Such dermatophytoses are diagnosed by fungal culture, and in some instances rapidly by dermatohistopathology with periodic acid-Schiff staining (3/3 cases of Microsporum gypseum infection and 5/7 cases of Microsporum persicolor infection). Therapy with topical and/or systemic azole derivatives (topical enilconazole, miconazole, econazole and systemic ketoconazole, respectively) was successful in all cases, with only two relapses, which were easily controlled.     

Insecticidal and fungicidal activity of new synthesized chitosan derivatives

Chitosan, the N-deacetylated derivative of chitin, is a potential biopolysaccharide owing to its specific structure and properties. In this paper, we report on the synthesis of 24 new chitosan derivatives, N-alkyl chitosans (NAC) and N-benzyl chitosans (NBC), that are soluble in dilute aqueous acetic acid. The different derivatives were synthesized by reductive amination and analyzed by 1H NMR spectroscopy. A high degree of substitution (DS) was obtained with N-(butyl)chitosan (DS 0.36) at a 1:1 mole ratio for NAC derivatives and N-(2,4-dichlorobenzyl)chitosan (DS 0.52) for NBC derivatives. Their insecticidal and fungicidal activities were tested against larvae of the cotton leafworm Spodoptera littoralis (Boisduval) (Lepidoptera: Noctuidae), the grey mould Botrytis cinerea Pers (Leotiales: Sclerotiniaceae) and the rice leaf blast Pyricularia grisea Cavara (Teleomorph: Magnaporthe grisea (Hebert) Barr). The oral feeding bioassay indicated that all the derivatives had significant insecticidal activity at 5 g kg(-1) in artificial diet. The most active was N-(2-chloro-6-fluorobenzyl)chitosan, which caused 100% mortality at 0.625 g kg(-1), with an estimated LC50 of 0.32 g kg(-1). Treated larvae ceased feeding after 2-3 days; the mechanism of action remains unknown. In a radial hyphal growth bioassay with both plant pathogens, all derivatives showed a higher fungicidal action than chitosan. N-Dodecylchitosan, N-(p-isopropylbenzyl)chitosan and N-(2,6-dichlorobenzyl)chitosan were the most active against B cinerea, with EC50 values of 0.57, 0.57 and 0.52 g litre(-1), respectively. Against P grisea, N-(m-nitrobenzyl)chitosan was the most active, with 77% inhibition at 5 g litre(-1). The effect of different substitutions is discussed in relation to insecticidal and fungicidal activity.     

Acidic derivatives of the fungicide fenpiclonil: effect of adding a methyl group to the N-substituted chain on systemicity and fungicidal activity

A new acidic derivative of the fungicide fenpiclonil was synthesized containing a methyl group on the alpha-position of the carboxyl function of N-carboxymethyl-3-cyano-4-(2,3-dichlorophenyl)pyrrole. The phloem mobility of the resulting N-(1-carboxyethyl)-3-cyano-4-(2,3-dichlorophenyl)pyrrole was comparable with that of the former compound, but was higher at external pH 5.0. Unlike the derivatives previously synthesized, it was comparable with fenpiclonil in its fungicidal activity against the pathogenic fungus Eutypa lata.     

12-(取代苯氧异丁酰氧亚氨基)-1,15-十五内酯的合成及除草活性

通过取代苯氧异丁酸与12-(羟基亚氨基)十五内酯的反应,合成了取代苯氧异丁酰氧亚氨基十五内酯,并测定了其对苋菜的除草活性。所有化合物均经过1H NMR、13C NMR和元素分析确证。初步的生物活性测定结果表明,目标化合物 Ⅲa~Ⅲd 的EC50值分别为34.570、46.492、55.385、50.114 mg/L,其活性比对照药剂2,4-D(117.325 mg/L)高,而比苯磺隆(22.381 mg/L)低。