保幼激素类似物对红火蚁的作用研究进展

我国发现红火蚁已有4年,但防治技术、产品依然匮乏。为了改善、提高我国红火蚁的防治技术水平,本文就保幼激素类似物(JHA)对红火蚁的作用表现和防治效果进行了总结分析。JHA可以造成蚁后卵巢萎缩、产卵量减少,导致发育畸形和蚁群等级比例失调,如工蚁数量减少、生殖型幼虫比例以及处女蚁后数量增加等,并最终导致整个蚁群死亡。JHA杀虫剂活性高、低残毒、对环境污染小,在田间防治红火蚁效果彻底,并可有效地防止防治区红火蚁种群的再入侵（re invasion）,但JHA毒饵也存在着防治效果缓慢等问题。本文就克服此类问题作了初步的探讨。     

Protective effect of curcumin analogue L6H4 on diaphragm of type 2 diabetic rats

AIM: To investigate the protective effect of curcumin analogue L6H4 on diaphragm of type 2 diabetic rats.METHODS: SPF male Sprague-Dawley rats (n=40) were randomly divided into 5 groups: normal control (NC) group, high fat (HF) group, high fat+L6H4 treatment (FT) group, diabetes mellitus (DM) group and DM+L6H4 treatment (DT) group. The rats in the later 4 groups were fed with high-fat diet. After 4 weeks of high-fat diet fee-ding, the rats in DM and DT groups were intraperitoneally injected with streptozotocin to induce type 2 diabetes melliutus. The rats in FT and DT groups were given L6H4 by gavage for 8 weeks. Blood glucose and blood lipid levels were detected biochemically. Fasting serum insulin (FINS) level was measured by radioimmunoassay and insulin resistance index (HOMA-IR) was calculated. Serum adiponectin (APN) level was measured by ELISA. The morphological changes of the diaphragm were observed under light and transmission electron microscopes. Lipid deposition and the activity of succinate dehydrogenase (SDH) and NADH-tetrazolium reductase (NADH-TR) were observed by enzyme histochemical staining. The content of malondialdehyde (MDA) and the activity of superoxide dismutase (SOD) in the diaphragm were measured by thiobarbituric acid method and hydroxylamine method, respectively. The protein expression of adiponectin receptor 1 (AdipoR1) in the diaphragm was determined by immunohistochemistry and Western blot. RESULTS: The levels of blood lipids, blood glucose, FINS and HOMA-IR in HF and DM groups were higher than those in NC group, but decreased after L6H4 treatment. The serum APN level in HF and DM groups was lower than that in NC group, but increased after treatment with L6H4. The muscle fibers of the diaphragm were shrunk, fat particles accumulated in the muscle fibers, and the mitochondria were slightly swollen in HF and DM groups. The diaphragmatic fibrosis was obvious in DM group. These lesions were relieved after L6H4 treatment. Compared with NC group, the level of MDA and the activity of SDH and NADH-TR in the diaphragm were increased in HF and DM groups, but decreased after treatment with L6H4. The activity of SOD and the expression of AdipoR1 in the diaphragm were lower than those in NC group, but increased after L6H4 treatment.CONCLUSION: The curcumin analogue L6H4 exerts a protective effect on diaphragm in type 2 diabetic rats. The strengthened protein expression of AdipoR1, the increased serum level of APN, and anti-lipid peroxidation may be involved in the process.     

Conus regius-Derived Conotoxins: Novel Therapeutic Opportunities from a Marine Organism

Conus regius is a marine venomous mollusk of the Conus genus that captures its prey by injecting a rich cocktail of bioactive disulfide bond rich peptides called conotoxins. These peptides selectively target a broad range of ion channels, membrane receptors, transporters, and enzymes, making them valuable pharmacological tools and potential drug leads. C. regius-derived conotoxins are particularly attractive due to their marked potency and selectivity against specific nicotinic acetylcholine receptor subtypes, whose signalling is involved in pain, cognitive disorders, drug addiction, and cancer. However, the species-specific differences in sensitivity and the low stability and bioavailability of these conotoxins limit their clinical development as novel therapeutic agents for these disorders. Here, we give an overview of the main pharmacological features of the C. regius-derived conotoxins described so far, focusing on the molecular mechanisms underlying their potential therapeutic effects. Additionally, we describe adoptable chemical engineering solutions to improve their pharmacological properties for future potential clinical translation.     

Quantitative structure—activity studies of insect growth regulators. XI. Stimulation and inhibition of N-acetylglucosamine incorporation in a cultured integument system by substituted N-tert-butyl-N,N′-dibenzoylhydrazines

The ability to stimulate N-acetylglucosamine (GluNAc) incorporation in-vitro of a number of N-tert-butyl-N,N′-dibenzoylhydrazines having various substituents on both phenyl rings was measured in cultured integument excised from the rice stem borer (Chilo suppressalis Walker). The relationship between in-vitro and larvicidal potency was approximately linear. The substituent effects on variations in the potency were similar between in-vitro and larvicidal activities. An inhibitor of oxidative detoxication, piperonyl butoxide, had no synergistic effects on the in-vitro potency. The ability of some dibenzoylhydrazines to inhibit GluNAc incorporation at exposure periods longer than the optimum for stimulation was also measured in a similar cultured integument system. The relationship between the inhibitory and stimulatory potency indices was linear, indicating that the larvicidal activity of dibenzoylhydrazines is closely related to its ability to stimulate as well as to inhibit GluNAc incorporation into the larval cuticle.     

Identification of resistance gene analogue markers closely linked to wheat powdery mildew resistance gene Pm31

Specific oligonucleotide primers, designed for the sequences of known plant disease resistance genes, were used to amplify resistance gene analogues (RGAs) from wheat genomic DNA. This method was applied in a bulked segregant analysis to screen for the RGA markers linked to the powdery mildew resistance gene Pm31, introgressed into common wheat from wild emmer. Two RGA markers (RGA200 and RGA390) were found to be closely linked to Pm31 and completely co‐segregating with the marker allele of Xpsp3029 linked to Pm31, with a genetic distance of 0.6 cM. These two RGA markers were then integrated into the formerly established microsatellite map of Pm31 region. The result showed the effectiveness of the RGA approach for developing molecular markers linked to disease resistance genes and demonstrated the efficiency of denaturing polyacrylamide‐gel electrophoresis for detecting polymerase chain reaction polymorphism.     

小麦抗病基因同源序列(RGAs)的克隆与分析

RGA(抗性基因同源序列)法是克隆植物抗性基因的一种经济有效的方法,成为近年来的研究热点。本实验综合分析了拟南芥,西红柿,水稻,烟草等植物已克隆的抗性基因,并以这些抗性基因的NBS(核酸结合位点),LRR(富含亮氨酸重复),STK(丝氨酸/苏氨酸激酶)保守结构域设计并合成了几十对RGA引物,对小麦抗条锈病材料进行PCR扩增,获得以Xal-NBS为引物的R88RGA片段,经克隆和序列比对分析,发现该片段与逆境条件下植物抗病信号传导相关,与蛋白激酶同源性达到96%。此项研究对抗病机理的研究和基因的发掘有重要的指导意义。     

复方苦参注射液对肺癌和肝癌细胞抑瘤作用研究

苦参碱及其类似物是一类来源于苦参和苦豆子的生物碱,具有抗癌、消炎、抗病毒、杀虫、杀螨和抑菌等广泛的医用及农用生物活性。本文概述了近10年来苦参碱及其类似物的农用生物活性研究进展,重点总结了近4年来苦参碱及其类似物在结构改造方面的研究情况,对其构效关系进行了分析,以期为今后更好地开发利用苦参碱及其类似物提供参考。     

蚜虫性信息素

蚜虫报警信息素 [(E)-β-farnesene,简称EBF] 是蚜虫腹管分泌的一种物质,它能对同种其他个体产生报警反应,使其迅速逃离危险现场。作为天然蚜虫信息素,EBF通过蚜虫嗅觉系统的气味结合蛋白OBPs和嗅觉受体ORs发挥作用,具有驱避、杀蚜、增效等多种生物活性,可用于蚜虫的行为调控,但由于其结构中存在的共轭双键而导致其稳定性差,从而限制了其实际应用。本文在简介蚜虫报警信息素EBF的基础上,系统介绍了EBF的结构修饰和改造进展,并对EBF及其类似物的生物活性和作用机制进行了综述,最后对EBF及其类似物的应用前景进行了展望,期望为开发具有实用价值的生态友好型蚜虫控制剂提供参考。     

Modification of Marine Natural Product Ningalin B and SAR Study Lead to Potent P-Glycoprotein Inhibitors

In this study, new marine ningalin B analogues containing a piperazine or a benzoloxy group at ring C have been synthesized and evaluated on their P-gp modulating activity in human breast cancer and leukemia cell lines. Their structure-activity relationship was preliminarily studied. Compounds 19 and 20 are potent P-gp inhibitors. These two synthetic analogues of permethyl ningalin B may be potentially used as effective modulators of P-gp-mediated drug resistance in cancer cells.