化学结构与生物活性:取代苯基N-甲氨基甲酸酯的合成与活性

用异氰酸甲酯与适当的酸类反应,合成了一系列的取代苯基N-甲氨基甲酸酯类化合物。生物测定表明,在苯基N-甲氨基甲酸酯的苯环上引入取代基,均能增加对胆碱酯酶活性的抑制作用,在苯环上引入甲基增加对淡色库蚊(Culex pipiens pallens)幼虫的毒性。在苯环酯键的邻位上引入取代基时,除2,3-二甲苯基化合物外,均降低对蚊幼虫的毒性。 在各化合物对蚊幼虫的毒性和其对胆碱酯酶活性的抑制作用间,不能看出任何相互关系。     

几丁质合成抑制剂对小菜蛾的生物活性

几丁质合成抑制剂对小菜蛾户Plutella xylostella L.4龄幼虫毒力测定的结果显示, XRD-473 农梦特、卡死克、抑太保、灭幼脲1号、灭幼脲;号的毒力值(LC₅₀)分别为0.4768、0.8669、1.0754、1.2389、27.0680和36.8591ppm。 国外生产的几丁质合成抑制剂毒力显著高于国产的品种,这类药剂的毒力又明显高于常规药剂敌敌畏、氯氰菊酯、杀虫双等,它们的毒力值(LC₅₀)分别为818.0315、6419.9842、55,.4925ppm。抑太保对小菜蛾幼虫作用方式的研究结果表明,该药剂以胃毒为主,兼有触杀作用。以抑太保、卡死克50ppn的药液饲喂的小菜蛾雌、雄成蛾寿命比单用5%。蜜糖水饲喂的个体缩短1天和4天左右,产卵量减少2/3,卵孵化率显著降低。用抑太保、卡死克50ppm的药液浸渍的小菜蛾卵孵化串分别为5.35%和0。温度对抑太保的毒力有较大影响,在试验温度范围内(10-30℃),抑太保10ppm处理的小菜蛾种群50%或,75o、95%群体致死时间随着温度上升而缩短。     

几种几丁质合成抑制剂对棉铃虫生物活性的研究

几种几丁质合成抑制剂对棉铃虫Heliothis armigera(Hǖbner)生物活性的室内研究结果表明:以IKI-7899和昆调1055饲喂棉铃虫成虫能降低其产卵的孵化率,但对其寿命和产卵量均无影响.以IKI-7899浸卵,125ppm的浓度即可致使处理卵孵化出的幼虫在二、三龄前死亡50%以上.IKI-7899和昆调1055对棉铃虫幼虫的触杀毒力均高于其胃毒毒力,并表现较高的生物活性,而灭幼脲Ⅰ号和苏脲Ⅰ号的活性极低.以含毒人工饲料饲喂幼虫两天,IKI-7899、昆调1055和灭幼脲Ⅰ号的毒力值均比饲喂一天的高5倍以上;而连续饲喂至化蛹期的毒力值比饲喂一天的高50倍以上.     

卤代黄酮类化合物的合成及生物活性的研究

卤代黄酮类化合物具有很多种生物活性,本文综述目前国内外在黄酮不同位置引入卤原子的方法及一些卤代黄酮类化合物的生物活性,期待为黄酮类化合物开发出一批具有结构新颖的先导化合物.     

蒽醌衍生物结构及其对小麦白粉病菌生物活性的关系研究

蒽醌衍生物是植物产生的一类次生代谢产物,对植物病原真菌具有明显的活性。为明确蒽醌衍生物结构与其生物活性之间的关系,以小麦白粉病菌为研究对象,测定了蒽醌及16种蒽醌衍生物对该病菌的活性。结果表明,蒽醌衍生物对小麦白粉病菌的活性明显大于葸醌的活性;甲氧基的位置与活性关系密切,6位是决定活性的关键,活性顺序为5、6位〉1、6位〉6位〉8位。     

合成黑翅土白蚁踪迹信息素类似物的生物活性

合成了黑翅土白蚁踪迹信息素类似物(Z,Z)-3,6-十二碳二烯醇-1（DDE-OH）,该类似物对黑翅土白蚁工蚁具有和信息素提取物类似的行为反应。活性反应阈值为10^-3～10 ng/cm,大于10 ng/cm时产生较强的驱避作用。最佳活性浓度DDE-OH与信息素提取物的活性反应之间没有显著差别。     

小单胞菌属次级代谢产物及其生物活性研究进展

小单胞菌属(Micromonospora)为稀有放线菌,广泛分布在土壤、海洋和动植物中,其所产代谢产物不仅具有抗菌、抗肿瘤、抗HIV等多种生物活性,而且化学结构新颖多样。本文从化学结构分类、生物活性等方面对近几年已报道的小单胞菌属来源的重要天然产物做了简要综述,以期为小单胞菌天然产物的开发和应用奠定基础。     

A8—10替换的胰岛素似物的合成及生物活性

本文报道了用Ｆｍｏｅ固相法合成３种胰岛素Ａ链小环（Ａ８－１０）被不同碱性氨基酸取代的Ａ链类似物,并分别与天然胰岛素Ｂ链重组成相应胰岛素类似物;经受体结合,整体活性及抗体结合实验,均表现出相应的活性。从中可以推测出：Ａ链小环区域不是胰岛素表现生物活性的重要部位,而是胰岛素与其抗体结合较重要的区域。     

Salicylanilide N-monosubstituted carbamates: Synthesis and in vitro antimicrobial activity

The research of innovative antimicrobial agents represents a cutting edge topic. Hence, we synthesized and characterised novel salicylanilide N-monosubstituted carbamates. Twenty compounds were evaluated in vitro against eight bacterial strains and eight fungal species. The lowest minimum inhibitory concentrations (MICs) were found to be ⩽0.49 μM. Genus Staphylococcus, including methicillin-resistant Staphylococcus aureus, and fungus Trichophyton mentagrophytes showed uniformly the highest rate of susceptibility, whilst Gram-negative bacteria and most of the fungi were less susceptible. A wide range of carbamates provided comparable or superior in vitro antimicrobial activity in comparison to established drugs. Interestingly, extended-spectrum β-lactamase producing strain of Klebsiella pneumoniae was inhibited with MICs starting from 31.25 μM. With respect to Staphylococci, 2-[(4-bromophenyl)carbamoyl]-4-chlorophenyl phenylcarbamate exhibited the lowest MIC values (⩽0.98 μM). 2-[(4-Bromophenyl)carbamoyl]-4-chlorophenyl benzylcarbamate showed the widest spectrum of antifungal action. The results indicate that some salicylanilide carbamates can be considered to be promising candidates for future investigation.     

Synthesis and biological activity of new salicylanilide N,N-disubstituted carbamates and thiocarbamates

The development of novel antimicrobial drugs represents a cutting edge research topic. In this study, 20 salicylanilide N,N-disubstituted carbamates and thiocarbamates were designed, synthesised and characterised by IR, ¹H NMR and ¹³C NMR. The compounds were evaluated in vitro as potential antimicrobial agents against Mycobacterium tuberculosis and nontuberculous mycobacteria (Mycobacterium avium and Mycobacterium kansasii) as well as against eight bacterial and fungal strains. Additionally, we investigated the inhibitory effect of these compounds on mycobacterial isocitrate lyase and cellular toxicity. The minimum inhibitory concentrations (MICs) against mycobacteria were from 4 μM for thiocarbamates and from 16 μM for carbamates. Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus, were inhibited with MICs from 0.49 μM by thiocarbamates, whilst Gram-negative bacteria and most of the fungi did not display any significant susceptibility. All (thio)carbamates mildly inhibited isocitrate lyase (up to 22%) at a concentration of 10 μM. The (thio)carbamoylation of the parent salicylanilides led to considerably decreased cytotoxicity and thus improved the selectivity indices (up to 175). These values indicate that some derivatives are attractive candidates for future research.     

异甾体生物碱类化合物及药理活性研究进展

异甾体生物碱类结构多变,药理活性多样,主要分布于百合科贝母属和藜芦属植物中。近十五年内共报道了80个新发现的异甾体生物碱类成分,药理活性涉及抗炎、镇痛、降压、平喘、抗血栓、胆碱酯酶抑制、抗病毒和抗肿瘤等作用。本文综述了2006至2020年间该类化合物的植物来源、化学结构及药理活性,并对该类化合物的未来研究探索进行了讨论与展望。     

香茅醛缩醛类化合物的合成及其对小黄家蚁的驱避活性

【目的】香茅醛类化合物具有较好的蚂蚁驱避活性,本研究旨在筛选具有良好驱避活性的新的萜类蚂蚁驱避剂。【方法】以香茅醛为原料合成了香茅醛二甲缩醛、香茅醛二乙缩醛、香茅醛二正丙缩醛、香茅醛二异丁缩醛、香茅醛乙二缩醛、香茅醛1,2-丙二缩醛和香茅醛1,3-丙二缩醛等化合物。所得产品经纯化后,用IR, MS, ¹H NMR及¹³C NMR进行结构表征,并在不同浓度下对小黄家蚁Monomorium pharaonis进行驱避活性测试。【结果】各化合物对小黄家蚁具有一定的驱避活性：在10 mg/mL的浓度下,除香茅醛二甲缩醛以外,其他化合物的驱避率均达到70%以上,其中香茅醛二乙缩醛、香茅醛乙二缩醛和香茅醛1,3-丙二缩醛对小黄家蚁的驱避率分别为87.47%,100%和97.53%。浓度为2.5 mg/mL时,其中5个化合物的驱避效果明显下降,但香茅醛乙二缩醛和香茅醛1,3-丙二缩醛仍然表现出很好的驱避活性,驱避率分别为85.33%和97.10%。方差分析也表明,香茅醛1,3-丙二缩醛在同一浓度下驱避效果最佳,其次是香茅醛乙二缩醛。【结论】结果说明,香茅醛二乙缩醛、香茅醛乙二缩醛和香茅醛1,3 丙二缩醛可以用作小黄家蚁驱避剂,而香茅醛乙二缩醛和香茅醛1,3-丙二缩醛可以达到更好的驱避效果,使用浓度为2.5 mg/mL即可。本研究为良好萜类蚂蚁驱避剂的筛选提供了参考依据。     

Recent Advances in Isolation,Synthesis and Biological Evaluation of Terrein

Terrein is a small-molecule polyketide compound with a simple structure mainly isolated from fungi. Since its discovery in 1935, many scholars have conducted a series of research on its structure identification, isolation source, production increase, synthesis and biological activity. Studies have shown that terrein has a variety of biological activities, not only can inhibit melanin production and epidermal hyperplasia, but also has anti-cancer, anti-inflammatory, anti-angiopoietic secretion, antibacterial, insecticidal activities, and so on. It has potential application prospects in beauty, medicine, agriculture and other fields. This article reviews the process of structural identification of terrein since 1935, and summarizes the latest advances in its isolation, source, production increase, synthesis, and biological activity evaluation, with a view to providing a reference and helping for the in-depth research of terrein.     

Synthesis of serum thymic factor (FTS) and two analogs

Serum thymic factor (FTS) and [Gln¹]-FTS were synthesized by fragment condensation using the azide procedure. [d-Ala⁶]-FTS was prepared by stepwise amino acid condensation in combination with fragment condensation on solid-phase resin. Synthetic FTS and [Gln¹]-FTS both enhanced the delayed-type hypersensitivity (DTH) level to sheep red blood cells (SRBC) in mice at a dose of 0.1 ng/mouse per day, while a dose of 1.0 ng/mouse per day of [d-Ala⁶]-FTS was needed for the enhancement reaction.     

Catalytical oxidation of ecdysteroids to 3-dehydro products and their biological activities

Oxidation of ecdysone and ecdysterone with platinum as catalyst gives rise to several polar and 4–5 apolar substances, among them 3-dehydroecdysone and 3-dehydroecdysterone. Highest yields in the 3-dehydro products were reached after 4 to 8 hr of oxidation. 3-dehydroecdysone and 3-dehydroecdysterone are less active in inducing ecdysone specific puffs in Drosophila hydei salivary gland giant chromosomes but still contain a remarkable biological activity when compared with the original ecdysteroids. The activity of these two compounds is about one tenth that of ecdysone in the Calliphora assay.     

家蝇幼虫活性蛋白组分的提取及清除羟基自由基活性研究

以家蝇MuscadomesticaL.幼虫(蝇咀)为材料,根据溶解度的不同,从脱脂蝇蛆粉中分离出清蛋白、小分子肽、球蛋白、醇溶蛋白、碱溶蛋白等5类蛋白,并测定了它们的含量。结果表明:清蛋白、球蛋白和小分子肽是组成脱脂蝇蛆粉蛋白的主要成分。体外的抗氧化活性实验结果表明:清蛋白和球蛋白都有很好的清除羟基自由基的作用。     

Synthesis,antielastase, antioxidant and radical scavenging activities of 4-(aza substituted) methylene substituted dihydroxy coumarines

A series of some 4-(aza substituted) methylene substituted dihydroxy coumarines were evaluated for their antioxidant and antielastase activities. Different in vitro methodologies such as total reducing power, 1,1-diphenyl-2-picryl-hydrazil (DPPH·) free radical scavenging, ABTS radical scavenging activity were used as antioxidant activity. All the tested compounds exhibited potent free radical scavenging ability and antielastase activites.     

Synthesis of novel quinolinomatrine derivatives and their insecticidal/acaricidal activities

In continuation of our program to discover natural product-based pesticidal agents, a series of new quinolinomatrine derivatives were prepared. Especially three-dimensional structures of five compounds were unambiguously determined by single-crystal X-ray diffraction. Among them, 21-chloroquinolinomatrine exhibited good insecticidal and acaricidal activities against two crop-threatening insect pests, Mythimna separata and Tetranychus cinnabarinus. Their structure-activity relationships were also discussed.