Structural Effects of N-Arylcarbamoylpyrazolines on Calcium Uptake in Rat Brain Synaptosomes

N-Arylcarbamoylpyrazolines with various substituents at the para position of the carbamoyl benzene ring inhibited ATP-dependent Ca²⁺-uptake in synaptosomes prepared from the rat brain. The activity of these compounds was evaluated as log(1/I₅₀), the reciprocal logarithm of half inhibitory concentration, I₅₀ (m ), from the concentration–response curve for the inhibition of Ca²⁺-uptake. Among the compounds tested, methyl 3-(4-chlorophenyl)-4-methyl-1-[N-(4-trifluoromethylphenyl)carbamoyl]-2-pyrazoline-4-carboxylate was the most potent, the I₅₀ value of which as 9·12×10⁻⁷ m . Variations in the activity in terms of log(1/I₅₀) were quantitatively analysed using a substituent parameter, showing that the higher the electron-withdrawing effect of the substituent, the higher was the activity. The substituent effects were similar to those on insecticidal activity against the Americal cockroach. The higher the inhibitory activity against Ca²⁺ uptake, the higher seemed to be the insecticidal activity. Methyl(4S) - 3 - (4 - chlorophenyl) - 4 - methyl - 1 - [N - (4 - chlorophenyl)carbamoyl] - 2 - pyrazoline -4-carboxylate had higher inhibitory activity against Ca²⁺-uptake and higher in-secticidal activity than the R-isomer, but the difference was greater in theCa²⁺-uptake system.     

Synthesis and Structure–Activity Relationships of Miticidal 4,5-Dihydropyrazole-5-thiones

A series of novel 4,5-dihydropyrazole-5-thiones (DHPs) was synthesised by treating the corresponding dihydropyrazolones with ‘Lawesson’s reagent and evaluated for miticidal activity against two-spotted spider mites (Tetranychus urticae Koch). Of these, 3-(4-chlorophenyl)-4,4-dimethyl-1-phenyl-4,5-dihydropyrazole-5-thione, 3-(4-chlorophenyl)-4-ethyl-4-methyl-1-phenyl-4,5-dihydropyrazole-5-thione, 3-(4-chlorophenyl)-1-phenyl-4,5-dihydropyrazole-5-thione-4-spirocyclopentane and 4,4-dimethyl-1-phenyl-3-(4-trifluoromethyl-phenyl)-4,5-dihydropyrazole-5-thione were highly active (pEC₅₀>4·0) and were more effective than the miticide dicofol (pEC₅₀=3·879), which has traditionally been used for the control of phytophagous mites. Structure–activity relationship (SAR) studies were performed on each position of the pyrazole ring of DHPs. The results indicated that the unsubstituted phenyl, 4-substituted phenyl and thioxo groups on the 1-, 3- and 5-positions of DHPs respectively were required for activity. Quantitative SAR studies using physicochemical parameters of substituents and the capacity factor k′ as a hydrophobicity index suggested that: (a) the activities of all types of DHPs examined were mainly dominated by hydrophobicity, (b) the bulkiness of 4-substituents of the 3-phenyl ring favoured the activity and (c) the log k′ optimum for all DHPs was 1·675, equivalent to a log P_ow value of c. 5·0.     

一种可降解黄原胶的鞘氨醇单胞菌的凝集活性

采用血凝测试及血凝活性糖抑制测试方法,测定了一种可降解黄原胶的鞘氨醇单胞菌XT-11Sphingom onassp.对红细胞的凝集活性及糖抑制专一性,同时进行了温度、pH及Ca2 对红细胞凝集活性影响的试验。结果表明:XT-11菌悬液能凝集家兔、家鸡两种红细胞,其凝集效价分别为26和24;菌悬液对兔红细胞的凝集作用可以被肝素所抑制;鞘氨醇单胞菌的凝集活性不依赖于Ca2 ,且在pH为6.0~10.0时较稳定,在温度为60℃时完全丧失凝集活性。这说明该菌含有能凝集红细胞的活性物质。     

甲基盐霉素对鲤白细胞吞噬活性和溶菌酶活力的影响

选用60 g左右健康正常的鲤540尾,随机平均分为6组,每组设3个重复。试验设6种处理,即基础饲料中分别添加甲基盐霉素0(对照组)、10、20、40、80、160 mg/kg。研究了甲基盐霉素对鲤白细胞吞噬活性和溶菌酶活性的影响。试验结果表明,饲料中添加10 mg/kg甲基盐霉素对鲤白细胞吞噬活性和溶菌酶活性影响不显著,而添加20~160 mg/kg甲基盐霉素对鲤白细胞吞噬活性和溶菌酶活性有一个从促进到抑制的转变,剂量越高,这个转变越快,并且随饲喂时间的延长,其抑制作用越来越强。     

转移因子与重组转移因子及其在疾病防治中的应用

转移因子是来自于免疫淋巴细胞的一类可透析小分子多肽,它能够将致敏淋巴细胞的免疫信息传递给未致敏的受体淋巴细胞。转移因子具有特异性和非特异性免疫活性,特异性转移因子具有转移特异性细胞免疫的能力,非特异性转移因子具有促进淋巴细胞活化增殖,增强其免疫活性,并可诱导靶细胞产生大量的细胞因子。重组转移因子是利用基因工程技术将编码具有免疫增强活性的转移因子基因,进行克隆和体外表达,表达产物经纯化制备而成,试验表明其具有增强细胞免疫活性的作用。转移因子和重组转移因子是一种具有免疫增强活性的新型高效安全的生物药品,在临床上用于疾病的防治,具有广阔的应用前景。     

乳铁多肽及其生物学活性的研究进展

乳铁多肽(乳铁素)是乳铁蛋白在酸性环境下经胃蛋白酶水解,产生的具有特殊生理功能的活性多肽。乳铁素不仅保持乳铁蛋白的活性,而且活性要比乳铁蛋白更强。乳铁素具有抑菌、杀菌、抗癌、抗病毒、免疫调节等多种乳铁蛋白所具有的活性。乳铁素的抗菌活性很强,但其抗病毒活性相对较弱。文章讨论了乳铁素成员中活性较强的牛乳铁素和人乳铁素,内容涵盖了目前乳铁素研究的重点领域,讨论了乳铁素的作用范围及其作用机制,探讨了乳铁素结构与活性之间的联系。     

朱顶红叶片提取物抑菌效果的初步研究

为开发利用朱顶红提供依据,研究朱顶红叶片提取物对病原真菌的抑菌作用,以石油醚和丙酮为溶剂对朱顶红叶片中的活性物质进行索氏提取,并对其提取物进行了生物测定。结果表明,其活性物质对4种病原真菌菌丝生长都表现出抑制作用,0.06 g/mL以上浓度的抑菌效果明显。相同浓度下的孢子萌发试验结果显示:活性物质除了对枇杷叶斑病菌(Pes-tulotiopsis funerea)的抑制效果较差外,对其他3种病菌孢子的萌发抑制率均在73%以上。     

Synthesis and Antifouling Activity Evaluation of Analogs of Bromosphaerol,a Brominated Diterpene Isolated from the Red Alga Sphaerococcus coronopifolius

Marine biofouling is an epibiotic biological process that affects almost any kind of submerged surface, causing globally significant economic problems mainly for the shipping industry and aquaculture companies, and its prevention so far has been associated with adverse environmental effects for non-target organisms. Previously, we have identified bromosphaerol (1), a brominated diterpene isolated from the red alga Sphaerococcus coronopifolius, as a promising agent with significant antifouling activity, exerting strong anti-settlement activity against larvae of Amphibalanus (Balanus) amphitrite and very low toxicity. The significant antifouling activity and low toxicity of bromosphaerol (1) motivated us to explore its chemistry, aiming to optimize its antifouling potential through the preparation of a number of analogs. Following different synthetic routes, we successfully synthesized 15 structural analogs (2–16) of bromosphaerol (1), decorated with different functional groups. The anti-settlement activity (EC₅₀) and the degree of toxicity (LC₅₀) of the bromosphaerol derivatives were evaluated using cyprids and nauplii of the cirriped crustacean A. amphitrite as a model organism. Derivatives 2, 4, and 6–16 showed diverse levels of antifouling activity. Among them, compounds 9 and 13 can be considered as well-performing antifoulants, exerting their activity through a non-toxic mechanism.     

神秘果叶粗多糖提取工艺优化及其抗氧化活性研究

为了更好的开发和利用神秘果资源,优化神秘果叶粗多糖的提取工艺,并评价其抗氧化能力。本研究采用单因素实验对液料比、提取温度、提取时间和提取次数进行研究,在单因素实验基础上,建立三因素三水平的正交试验设计,对提取工艺进行优化,获得最佳提取条件,并测定神秘果叶粗多糖的总抗氧化能力(FRAP)。结果表明提取神秘果叶粗多糖的最佳工艺条件为：液料比25:1 (v/m)、提取温度85 °C、提取时间60 min,提取3次,在此条件下,神秘果叶粗多糖提取率为4.93 ± 0.022%;三个因素对神秘果叶粗多糖提取率影响大小顺序为：提取温度>提取时间>液料比。分析其总抗氧化能力(FRAP)发现,神秘果叶粗多糖具有一定的抗氧化活性(41.38 μmol/g)。     

胡椒和肉桂挥发性组成分析及对普通大蓟马的驱避作用

豇豆农药残留问题非常严峻, 对豇豆上普通大蓟马的化学防治是造成豇豆农残超标的主要原因, 开展普通大蓟马的绿色防治迫在眉睫。利用植物挥发物驱避害虫是一种重要的害虫绿色防控手段。本研究利用GC-MS分析了胡椒和肉桂的挥发性化合物组成, 并利用“Y”形嗅觉仪测定了胡椒和肉桂及5种主要挥发物对普通大蓟马的驱避作用。结果表明, 在胡椒中鉴定出27种挥发性成分, 主要成分为β-石竹烯, 含量占43.1%; 在肉桂中鉴定出21种挥发性成分, 主要成分为肉桂醛(28.4%)、α-可巴烯(15.4%)、α-依兰油烯(14.1%)、γ-杜松烯(14.9%)。行为反应测定结果表明胡椒和肉桂对普通大蓟马分别具有极显著和显著的驱避作用; β-石竹烯、肉桂醛、α-可巴烯浓度为10%和1%时对普通大蓟马具有极显著的驱避作用, 10%的α-依兰油烯和10%的γ-杜松烯对普通大蓟马分别具有极显著和显著的驱避作用。本研究对豇豆普通大蓟马绿色防控技术研发和驱避剂的开发具有一定指导意义。