Pyrethroids as Promising Marine Antifoulants: Laboratory and Field Studies

Due to the regulations and bans regarding the use of traditional toxic chemicals against marine fouling organisms and the practical impediments to the commercialization of natural product antifoulants, there is an urgent need for compounds that are antifouling-active, environmentally friendly, and have a potential for commercial application. In this study, a series of common, commercially available pyrethroid products, which are generally used as environmentally safe insecticides, was evaluated for antifouling activity in the laboratory using an anti-settlement test with cyprids of the barnacle Balanus albicostatus and also in a field experiment. Laboratory assay showed that all eleven pyrethroids (namely, rich d-trans-allethrin, Es-biothrin, rich d-prallethrin, S-prallethrin, tetramethrin, rich d-tetramethrin, phenothrin, cyphenothrin, permethrin, cypermethrin, and high active cypermethrin) were able to inhibit barnacle settlement (EC₅₀ range of 0.0316 to 87.00 μg/ml) without significant toxicity. Analysis of structure–activity relationships suggested that the cyano group at the α-carbon position had a significant influence on the expression of antifouling activity in pyrethroids. In the field, the antifouling activity of pyrethroids was further confirmed, with the most potent pyrethroids being cypermethrin and high active cypermethrin, which displayed efficiency comparable with that of tributyltin. In summary, our investigation indicated that these pyrethroids have a great and practical commercial potential as antifouling agents.     

原位杂交检测lin-4 mRNA在Caenorhabditis elegans中的表达

lin-4是控制Caenorhabditis elegans(C.elegans)幼虫发育的异时性基因,也是一种小RNA分子(microRNA)。通过整体原位杂交检测小RNA lin-4在野生型和lin-14、lin-28突变体中的区域性表达,探讨lin-4在C.elegans发育时空控制中的作用。结果表明:lin-4 mRNA在胚胎发育的早期和中期表达,胚胎后期至L1期末没有表达,之后又持续表达,成虫中也可以检测到lin-4 mRNA的存在。在lin-14和lin-28突变体中,lin-4的表达基本与野生型一致,不受lin-14、lin-28基因突变的影响,说明lin-14和lin-28是lin-4的下游基因。     

转导外源总DNA培育棉花抗病新品种简报

棉花黄萎病是真菌病害,病原菌为大丽轮枝菌(Vertillium daliae),因致病力不同可分为不同的致病类型或生理小种。据统计,黄萎病对棉花的危害有逐年加重的趋势。1993年是我国棉花黄萎病大发生的一年,发病面积约占全国棉田的一半以上。尤其是北方棉区受害更重,重病棉田棉花病株率在80%以上,其中落叶成光秆的病株率高达50%,损失皮棉达1亿公斤。新疆棉区由于种植面积不断扩大(2000年皮棉总产占全国的1/3以上),引种不规范和     

Surface hydrophilic modification with well-defined glycopolymer for protein imprinting matrix

Well-defined lactose-containing glycopolymer has been synthesized by reversible addition-fragmentation chain transfer (RAFT) polymerization with (4-cyanopentanoic acid)-4- dithiobenozoate (CAD) as chain transfer agent. The glycopolymer was introduced onto the exterior surfaces of the bovine serum albumin (BSA) imprinted polymer beads by grafting copolymerization with methyl methacrylate and ethylene glycol dimethacrylate. After alcoholysis, the hydrophilic lactose residues of glycopolymer will stretched on the surface of the MIP beads and then the hydrophilicity of the surface will be enhanced. Rebinding test shows that the glycopolymer hydrophilic modified BSA imprinted polymer presents higher performance selectivity than that of unmodified one, which means that the hydrophobic-hydrophilic balance of the imprinted polymer surface is in favor of the improvement of specific recognition property of the material.     

Draft Genome Sequence of Paenibacillus sp. Strain OSY-SE,a Bacterium Producing the Novel Broad-Spectrum Lipopeptide Antibiotic Paenibacterin

A strain of Paenibacillus sp., OSY-SE, was isolated from soil and found to produce a novel lipopeptide antibiotic. The antibiotic, paenibacterin, is active against Gram-negative and Gram-positive bacterial pathogens. Paenibacterin is biosynthesized by a nonribosomal peptide synthetase pathway. Here we report the draft genome sequence of Paenibacillus sp. OSY-SE.     

Synthesis and structure–activity relationship studies of cytotoxic vinorelbine amide analogues

A series of 3-demethoxycarbonyl-3-acylamide methyl vinorelbine derivatives (compounds 7a–7z) were designed, synthesized, and evaluated for their inhibition activities against human non-small cell lung cancer cell line (A549). Most of the amide derivatives exhibited potent cytotoxicity, with the size of the introduced substituents being the foremost factor in determining the resultant cytotoxic activity. Test results in vivo against nude mice bearing A549 xenografts indicated that 7y showed comparable activities compared to the parent NVB.     

Topoisomerase I‐Mediated Antiproliferative Activity of 10‐Substituted and 12‐Substituted Homocamptothecins

Homocamptothecin (hCPT) is an E‐ring modified camptothecin (CPT) analogue, which showed pronounced inhibitory activity of topoisomerase I. In search of novel hCPT‐type anticancer agents, two series of hCPT derivatives were synthesized and evaluated in vitro against three human tumor cell lines. The results indicated that the 10‐substituted hCPT derivatives had a considerably higher cytotoxic activity than the 12‐substituted ones. Among the 10‐substituted compounds, 8a, 8b, 9b , and 9i showed an equivalent or even more potent activity than the positive control drug topotecan against the lung cancer cell line A‐549. Moreover, the hCPT analogues 8a and 8b exhibited a higher topoisomerase I inhibitory activity than CPT at a concentration of 100 μM .