畜用抗生素埃珀利诺菌素的合成与应用

介绍了经阿维菌素化学结构改造而得的埃珀利诺菌素的合成方法,生物活性及残留情况,充分表明了埃珀利诺菌素是第一个可用于任何生长期的,防治家畜体内外寄生虫的高效,安全杀虫剂。     

阿维菌素与高效氯氰菊酯复配制剂及其生物活性的研究

本文用共毒系数法,研究了1%阿维菌素乳油和5%高效氯氰菊酯乳油不同配比的复配剂的增效作用。结果表明,1%阿维菌素乳油与5%高效氯氰菊酯乳油以体积比为1:1、1:5、1:10、1:15、1:20、1:30等六种配比的混剂,以桃蚜为供试昆虫,与相应的单剂相比,均具有一定程度的增效作用。在小田试验中试定1%阿维菌素乳油与5%高效氯氰菊酯乳油复配比例为1:20。以这种复配剂来防治桃蚜,田间使用浓度为2000倍,施药5天后的防效达93.12%,相当于1%阿维菌素乳油2000倍在施药后5天的效果。     

阿维菌素·哒螨灵微乳剂的配方研究

报道到了一种新型复配微乳剂—阿维菌素·哒螨灵微乳剂的研究情况 ,简述了它的制备方法 ,配方筛选及贮藏稳定性等实验研究结果 ,表明该配方优良、制剂稳定、价位低、药效高、使用安全 ,具有良好的开发应用前景     

采用紫外线连续诱变方法选育阿维菌素高产菌株

以除虫链霉菌（Streptomyces avermitilis）为出发菌株,采用连续3次紫外诱变,同时使用D-脱氧葡萄糖进行定向筛选,选育得到阿维菌素高产菌株,较出发菌株提高了34.4%。     

苏·阿防治花椰菜小菜蛾的效果

比较了苏·阿、Ｂ．ｔ．和虫螨克防治花椰菜小菜蛾的效果。药后１天,２％苏·阿可湿性粉 剂１００ｇ／６６７ｍ２的防效为９８．３％,高于Ｂ．ｔ．可湿性粉剂（１６０００ＩＵ／ｍｇ）５０ｇ／６６７ｍ２９５．９％的防效, 也高于０．９ ％虫螨克乳油 ５０ｍｌ／６６７ｍ２９５．４ ％的防效。药后１周,苏·阿的防效仍达 ９４．７７％,明显 高于Ｂ．ｔ．可湿性粉剂（１６０００ＩＵ／ｍｇ）５０ｇ／６６７ｍ２和０．９％虫螨克乳油５０ｍｌ／６６７ｍ２的防效。     

丙溴磷,杀螨隆,氟铃脲等防治小菜蛾及菜青虫试验

试验结果表明，丙溴磷、杀螨隆、氟铃脲等对小菜蛾均有效，且持效期长，丙溴磷具有速效性及对菜青虫高效。     

一种新型硫醇菊酯衍生物的合成修饰及其抗蚊杀虫活性

拟菊酯类杀虫剂具有高效、低毒、用量少、低残留和广谱性等优点,因而受到广泛使用。采用化学修饰方法合成一种含氟的硫醇菊酯衍生物,其结构表征通过1H NMR、~(13)C NMR确定。抗蚊杀虫测试表明:该化合物对白纹伊蚊幼虫的半致死浓度LC50值为11.55μmol/L,且在12.5μgobottle-1的30 min作用下对白纹伊蚊雌性成蚊,其致死率能够达到74%。     

Novel Radiolytic Rotenone Derivative,Rotenoisin B with Potent Anti-Carcinogenic Activity in Hepatic Cancer Cells

Rotenone, isolated from roots of derris plant, has been shown to possess various biological activities, which lead to attempting to develop a potent drug against several diseases. However, recent studies have demonstrated that rotenone has the potential to induce several adverse effects such as a neurodegenerative disease. Radiolytic transformation of the rotenone with gamma-irradiation created a new product, named rotenoisin B. The present work was designed to investigate the anticancer activity of rotenoisin B with low toxicity and its molecular mechanism in hepatic cancer cells compared to a parent compound, rotenone. Our results showed rotenoisin B inhibited hepatic cancer cells’ proliferation in a dose dependent manner and increased in apoptotic cells. Interestingly, rotenoisin B showed low toxic effects on normal cells compared to rotenone. Mitochondrial transmembrane potential has been decreased, which leads to cytochrome c release. Down regulation of anti-apoptotic Bcl-2 levels as well as the up regulation of proapoptotic Bax levels were observed. The cleaved PARP (poly ADP-ribose polymerase) level increased as well. Moreover, phosphorylation of extracellular signal regulated kinase (ERK) and p38 slightly up regulated and intracellular reactive oxygen species (ROS) increased as well as cell cycle arrest predominantly at the G₂/M phase observed. These results suggest that rotenoisin B might be a potent anticancer candidate similar to rotenone in hepatic cancer cells with low toxicity to normal cells even at high concentrations compared to rotenone.     

Novel Antitumor L‐Arabinose Derivative of Indolocarbazole with High Affinity to DNA

Novel indolocarbazole derivative 12‐(α‐L ‐arabinopyranosyl)indolo[2,3‐α]pyrrolo[3,4‐c]carbazole‐5,7‐dione (AIC) demonstrated high potency (at submicromolar concentrations) against the NCI panel of human tumor cell lines and transplanted tumors in vivo. In search of tentative targets for AIC, we found that the drug formed high affinity intercalative complexes with d(AT)₂₀, d(GC)₂₀ and calf thymus DNA (binding constants (1.6×10⁶) M ^?1≤K_a≤(3.3×10⁶) M ^?1). The drug intercalated preferentially into GC pairs of the duplex. Importantly, the concentrations at which AIC formed the intercalative complexes with DNA (C≤1 μM ) were identical to the concentrations that triggered p53‐dependent gene reporter transactivation, the replication block, the inhibition of topoisomerase I‐mediated DNA relaxation and death of HCT116 human colon carcinoma cells. We conclude that the formation of high affinity intercalative complexes with DNA is an important factor for anticancer efficacy of AIC.     

New WS9326A Derivatives and One New Annimycin Derivative with Antimalarial Activity are Produced by Streptomyces asterosporus DSM 41452 and Its Mutant

In this study, we report that Streptomyces asterosporus DSM 41452 is a producer of new molecules related to the nonribosomal cyclodepsipeptide WS9326A and the polyketide annimycin. S. asterosporus DSM 41452 is shown to produce six cyclodepsipeptides and peptides, WS9326A to G. Notably, the compounds WS9326F and WS9326G have not been described before. The genome of S. asterosporus DSM 41452 was sequenced, and a putative WS9326A gene cluster was identified. Gene‐deletion experiments confirmed that this cluster was responsible for the biosynthesis of WS9326A to G. Additionally, a gene‐deletion experiment demonstrated that sas16 encoding a cytochrome P450 monooxygenase was involved in the synthesis of the novel (E)‐2,3‐dehydrotyrosine residue found in WS9326A and its derivatives. An insertion mutation within the putative annimycin gene cluster led to the production of a new annimycin derivative, annimycin B, which exhibited modest inhibitory activity against Plasmodium falciparum.