Insecticidal and neuroblocking potencies of variants of the imidazolidine moiety of imidacloprid-related neonicotinoids and the relationship to partition coefficient and charge density on the pharmacophore

The pharmacophore of the neonicotinoid insecticide imidacloprid, nitroiminoimidazolidine, was modified to heterocycles such as thiazolidine, pyrrolidine, dihydroimidazole, dihydrothiazole, and pyridone conjugated to nitroimine (=NNO2) or nitromethylene (=CHNO2). Their 6-chloro-3-pyridylmethyl or 5-chloro-3-thiazolylmethyl derivatives were examined for insecticidal activity against the American cockroach by injection and for neuroblocking activity using the cockroach ganglion. Most of the compounds having the neonicotinoidal pharmacophore exhibited insecticidal activity at the nanomolar level, which was enhanced in the presence of synergists, and high neuroblocking activity at the micromolar level. Quantitative analysis for the compounds showed that the neuroblocking potency is proportional both to the Mulliken charge on the nitro oxygen atom and to the partition coefficient log P value. The equation for the insecticidal versus neuroblocking potencies indicated that both potencies are related proportionally with each other when the other factors are the same.     

吸波材料辅助发泡蓝莓果浆微波冷冻干燥的试验研究

针对常规冷冻干燥时间长、能耗高的问题,试验研究了吸波材料辅助的发泡蓝莓果浆微波冷冻干燥过程,并对产品质量进行了评价。制备了未发泡与发泡两种冷冻样品,分别使用石英和碳化硅底盘进行了常规和微波冷冻干燥试验。结果表明,采用石英底盘在30 ℃、15 Pa下,发泡物料的冷冻干燥时间相比于未发泡物料缩短了39.1%。采用碳化硅底盘在相同条件和2 W微波功率下,发泡物料微波冷冻干燥时间比发泡与未发泡物料常规冷冻干燥分别缩短了14.3%和47.8%;当功率提高至4 W时,干燥时间分别缩短了25.0%和54.3%。常规和微波冷冻干燥产品质量相当,总单体花色苷和总多酚的保留率相比于原果浆均分别在80%和75%以上。结果表明,吸波材料辅助的发泡物料微波冷冻干燥能够大幅度缩短干燥时间、提高干燥过程经济性。     

Transepithelial Transport of Theasinensins through Caco-2 Cell Monolayers and Their Absorption in Sprague-Dawley Rats after Oral Administration

The aim of this study is to illustrate the in vivo and in vitro absorption of theasinensins B and A that are (-)-epigallocatechin-3-O-gallate (EGCG)-(-)-epigallocatechin (EGC) dimer and EGCG dimer, respectively, and their transport pathway across the intestinal membrane. Our animal study by a single oral administration to rats demonstrated the intact absorption of theasinensins into the blood system, which was estimated to be a >10-fold lower absorption amount than EGCG. The in vitro absorption study indicated that theasinensins can be transported across Caco-2 cell monolayers, while their permeability coefficients were also >10-fold lower than those of EGCG and EGC. Transport experiments using cytochalasin D or quercetin as a tight junction (TJ) modulator and a non-saturable permeation revealed that theasinensins were transported across Caco-2 cells in a TJ paracellular diffusion route. In conclusion, the dimers of condensed catechins, theasinensins B and A, can be absorbed intact into rat blood and transported across Caco-2 cell monolayers probably through a TJ paracellular pathway.     

The muscle protein Dok-7 is essential for neuromuscular synaptogenesis

The formation of the neuromuscular synapse requires muscle-specific receptor kinase (MuSK) to orchestrate postsynaptic differentiation, including the clustering of receptors for the neurotransmitter acetylcholine. Upon innervation, neural agrin activates MuSK to establish the postsynaptic apparatus, although agrin-independent formation of neuromuscular synapses can also occur experimentally in the absence of neurotransmission. Dok-7, a MuSK-interacting cytoplasmic protein, is essential for MuSK activation in cultured myotubes; in particular, the Dok-7 phosphotyrosine-binding domain and its target in MuSK are indispensable. Mice lacking Dok-7 formed neither acetylcholine receptor clusters nor neuromuscular synapses. Thus, Dok-7 is essential for neuromuscular synaptogenesis through its interaction with MuSK.     

Comparative effectiveness of two alkylammonium compounds as wood preservatives

This study describes a laboratory evaluation of the efficacy of two alkylammonium compounds [didecyldimethylammonium tetrafluoroborate (DBF) and didecyldimethylammonium chloride (DDAC)] when applied via vacuum impregnation or superficial treatment. Treated wood specimens were tested for their termite and microbial resistance under controlled laboratory conditions. The higher chemical retentions were needed to suppress the feeding by Coptotermes formosanus ≦3% mass loss in the multichoice test than in the no-choice test. The DBF and DDAC retention levels necessary to meet the performance requirement ≦3% mass loss after 12-week fungal exposure varied with wood species. The retention level of 3 kg/m³ for DBF and DDAC was generally high to keep the nondurable wood species free of decay. Although there was no difference between DBF and DDAC in the efficacy against decay and termite attack, the former slightly outperformed the latter as an antimold and antisapstain agent.     

利用RAPD—BSA分子标记技术筛选金针菇色泽基因研究

色泽是金针菇的重要性状之一,受一对等位基因的控制。以FL19(黄色)、8801(白色)及其后代(F1代、F2代)菌株和相应单核菌株为材料,采用分离群体分组分析(BulkedSegregantAnalysis,BSA)方法,对金针菇基因组DNA进行RAPD分析,通过对200个引物的筛选,获得了一个与白色性状基因紧密连锁的RAPD标记S3751800,并在亲本及其后代菌株进行了验证,具有较好的重复性和稳定性。可用于白色金针菇新品种的辅助选育。     

Synthesis of morphiceptin (Tyr-Pro-Phe-Pro-NH(2)) by dipeptidyl aminopeptidase IV derived from Aspergillus oryzae

Morphiceptin (Tyr-Pro-Phe-Pro-NH(2)), tetrapeptide, was synthesized using dipeptidyl aminopeptidase IV (DP IV, EC 3.4.14.5) derived from Aspergillus oryzae RIB 915 as a catalyst. Tyr-Pro-OEt was incubated with Phe-Pro-NH(2) in the presence of DP IV under various conditions of temperature, concentrations of ethylene glycol, pH, reaction time, and others. Morphiceptin was obtained at 40% yield under the optimal reaction conditions: substrate, 4 mM Tyr-Pro-OEt.HCl and 20 mM Phe-Pro-NH(2).HCl; enzyme, DP IV, 0.275 nkat; solvent, 60% ethylene glycol containing 20 mM phosphate buffer at pH 7.0; amine, 4.2 mM diisopropylamine at 4 degrees C for 24 h. Amino group protection was unnecessary for synthesis of morphiceptin by DP IV.     

Characteristics of fertilizer uptake and biodistribution in strawberry plants in two Japanese cultivars in hydroponic culture

ABSTRACT

The fertilizer absorption characteristics of strawberries are not clear, although appropriate fertilization is definitely necessary to ensure produce quality and quantity. This study aimed to determine the amounts of macro- and micronutrients absorbed during cultivation of strawberries and their biodistribution and utilization in the plant body. We cultivated Japanese strawberries ‘Benihoppe’ and ‘Kirapika’ in small hydroponic equipment containing a nutrient solution and determined the amounts of N, P, K, Ca, Mg, Fe, Mn, B, Zn, Cu, and Mo absorbed during and at the end of cultivation. The results revealed the adsorption levels of these elements during the cultivation period. The nutrient concentrations varied greatly among plant organs. In particular, P and B accumulated at high levels in the leaves and stem, K, Ca, Mg, Mn, Zn, and Cu accumulated in the crown, and N, Fe, and Mo accumulated in the roots. In addition, the uptake levels of N, P, K, Mg, Mn, Zn, and Cu differed between Benihoppe and Kirapika. Our results provide useful information for determining fertilizer application rates in strawberry cultivation.     

Interaction of grammistins with lipids and their antibacterial activity

ABSTRACT: Grammistins are hemolytic and ichthyotoxic peptides in the skin secretion of soapfishes and are structurally characterized by their abundance in amphiphilic α-helicity. In the present study, their interaction with lipids and lipid vesicles as well as antibacterial activity were examined using four grammistins (Gs 1 and Gs 2 from Grammistes sexlineatus and Pp 1 and Pp 3 from Pogonoperca punctata ). The hemolytic activity of grammistins was inhibited by phospholipids but not by cholesterol. Moreover, grammistins released carboxyfluorescein entrapped within liposomes made of phosphatidylcholine. In contrast, grammistins were found to have antibacterial activity with a broad spectrum against nine species of bacteria, including both Gram-negative and Gram-positive groups. The potency of their antibacterial activity was not related to that of hemolytic activity, suggesting that grammistins bind to membrane phospholipids but lyse erythrocyte and bacterial membranes via different mechanisms. Conclusively, grammistins are new members of the family of cell non-selective membrane-lytic peptides with amphiphilic α-helices, being similar to pardaxins, which are secreted from the skin of soles, and to melittin, which is derived from bee venom.     

Interspecific differences in the post-settlement survival of <Emphasis Type="Italic">Acropora</Emphasis> corals under a common garden experiment

Extremely low post-settlement survival is one of the largest barriers for artificial rehabilitation of Acropora corals. However, little data have been found for interspecific difference of the post-settlement survival probably because the observation of coral juvenile is difficult in the field. Here, we analyzed the survival of three dominant species of Acropora corals (A. digitifera, A. tenuis, A. yongei), with different colony morphologies and habitat preferences, for 2 years after settlement under the same environmental conditions. The post-settlement survival was significantly higher for A. tenuis than for A. digitifera 3 months after settlement. Two years later, the survival rate of A. tenuis was approximately 15 times higher than A. digitifera. In a separate analysis of three bottle-brush species (A. awi, A. echinata, A. subglabra) and A. tenuis, post-settlement survival was always higher for A. awi than for other two bottle-brush species, suggesting that the initial survival was different among morphologically sister species. Low survival was possibly associated with slow growth rates during the first 7 months. Thus, species selection is important for successful artificial coral rehabilitation, with A. tenuis being the most viable option. Alternatively, new techniques are required to improve post-settlement survival of slow growing coral species.