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。     

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。     

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.     

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.     

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.     

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.     

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.     

Isolation and Identification of Antifungal Ingredients from Artemisia hedinii北大核心CSCD

The extraction of Artemisia hedinii Ostenf. et Pauls(A. hedinii) were rough and further isolated by chromatographic separation technology, and the antifungal activity of the component was evaluated by the the spore germination method. Furthermore, the composition of antimicrobial components was analyzed by high performance liquid chromatography-mass spectrometry (HPLC-MS). The results showed that 13 kinds of components(Fr.1-Fr.13) were rough isolated from the extraction of A. hedinii, in which the component Fr.5 showed the best antifungal activity. Four kinds of components (Fr.5.1-Fr.5.4) were obtained by the further separation of the component Fr.5. The EC50 of A. hedinii crude extraction on Alternaria alternate (A.alternate) spores was 5.04 g/L, and that of the component Fr.5.2 was 0.57 g/L. The HPLC-MS results showed that the components of Fr.5.2 mainly contained deoxy double hydroxyl artemether (17 %),deoxy dihydroartemisinin (43.65 %) and deoxyartemisinin (16.15 %). The content of dihydroartemisinin of component Fr.5.2 was calculated as 40.95 % by using dihydroartemisinin as the standard. The EC50 of dihydroartemisinin on A.alternate was 2.70 g/L, indicating that the major antifungal matter in component Fr.5.2 was artemisinin derivatives. © 2018, Editorial Board of «Chemistry and Industry of Forest Products». All right reserved.     

寡聚酸碘抑制TMV活性测定及对番茄生长影响初探

为研究新型壳寡糖衍生物类农用制剂寡聚酸碘(寡聚N-乙酰基-D-氨基葡萄糖醛酸碘)对烟草花叶病毒(TMV)的抑制作用及对番茄生长、生理特性的影响,以番茄品种:L402、贝鲁特、粉多利作为供试材料,以氨基寡糖素及50%腐霉利L可湿粉剂作为对比,通过室内生测试验试验,测定寡聚酸碘对番茄病毒病中常见病原菌TMV的抑制效果、对番茄生长及及番茄幼苗茎尖中吲哚乙酸、赤霉素及叶绿素含量的影响。寡聚酸碘对TMV的抑制效果表现出良好的速效性和持效性,接种后17d,抑制效果从45.08%迅速提升到74.48%,接种21~35d,对TMV的抑制效果维持在80%以上。寡聚酸碘对TMV的EC50值为15.62mg/L,对TMV的抑制活性高于3%氨基寡糖素水剂寡聚酸碘处理,有效成分300.0mg/L的寡聚酸碘可作为抑制TMV活性的最优供试剂量;寡聚酸碘在300~1 200mg/L处理剂量下,对供试的3个番茄品种(L402、贝鲁特、粉多利)安全,未见任何药害症状,与CK、3%氨基寡糖素及50%腐霉利L可湿粉剂相比,可以明显提升番茄幼苗株高、茎尖内IAA、GA含量及叶片中总叶绿素含量。寡聚酸碘处理的番茄茎秆粗壮,叶色浓绿,生长性状良好。因此,寡聚酸碘具有抑制TMV活性及促进番茄生长的双重功效,开发利用前景良好。     

吡啶衍生物研究(Ⅷ):2-[(2-氯吡啶)-4-基]-5-烷氨基-1,3,4-噻二唑的合成及其除草活性

为寻找新的农药先导化合物 ,依据活性亚结构拼接原理 ,以异烟酸为起始原料 ,共合成了 12个标题化合物 ,其结构通过元素分析、1H和13 CNMR予以确认。所有化合物均具有一定的除草活性 ,且茎叶处理高于土壤处理 ,其中Ⅰ 0 4和Ⅰ 0 6在 1 5kg·hm-2 剂量下 ,茎叶处理对反枝苋、稗草、油菜和苜蓿的抑制率分别达 71 9%～89 2 %和 4 5 3%～ 87 0 % ;因此 ,该类化合物具有作为除草先导化合物进一步研究的价值