Overcoming hERG activity in the discovery of a series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists

A series of 4-azetidinyl-1-aryl-cyclohexanes as potent CCR2 antagonists with high selectivity over activity for the hERG potassium channel is discovered through divergent SARs of CCR2 and hERG.     

交替隔沟灌溉与施氮量对日光温室黄瓜光合作用、生长及产量的影响

以黄瓜“津育5号”为试材,研究了交替隔沟灌溉和施氮量(零氮肥、优化氮肥和常规氮肥)对日光温室黄瓜(冬春茬、秋冬茬)光合作用、生长特性、产量形成和果实品质的影响.结果表明:交替隔沟灌溉下,植株上、中、下叶位叶片的净光合速率(Pn)略低于常规灌溉下的相应叶位,而蒸腾速率(Tr)显著降低,上、中叶位叶片的瞬时水分利用效率(WUE)有所提高;交替隔沟灌溉下植株光合作用的限制因素是气孔因素.交替隔沟灌溉下施氮量的增加有助于促进黄瓜功能叶片Pn和WUE的提高.与常规灌溉相比,交替隔沟灌溉下叶片叶绿素含量和植株总生物产量有所降低,但根生物产量、根冠比以及根和果实器官的干物质分配比例增加,经济产量持平,经济产量水平的水分利用效率( WUEy)显著提高.交替隔沟灌溉有利于植株根系发育和果实形成.交替隔沟灌溉下随施氮量的增加,叶片叶绿素含量、叶绿素a/b、比叶重、植株总生物产量和经济产量呈增加趋势,果实Vc含量和可溶性糖含量升高,但优化氮肥与常规氮肥处理间差异不显著,氮肥施用对WUEy无显著影响.冬春茬黄瓜的经济产量和生物产量显著高于秋冬茬.     

Growth regulator-induced betacyanin accumulation and dopa-4,5-dioxygenase (<Emphasis Type="Italic">DODA</Emphasis>) gene expression in euhalophyte <Emphasis Type="Italic">Suaeda salsa</Emphasis> calli

Suaeda salsa calluses cultured in darkness for 28 d were transferred to Murashige and Skoog (MS) media containing various growth regulators under white light conditions for 10 d to investigate cell growth, betacyanin accumulation, and expression of dopa-4,5-dioxygenase (DODA). Callus growth was markedly promoted when 0.2 mg·L⁻¹ 2,4-D and 0.5 mg·L⁻¹ 6-BA were added to the MS medium. Surprisingly, of the auxins tested, IAA had no effect on betacyanin content, but 2,4-D strongly decreased betacyanin content. Betacyanin content was positively correlated with 6-BA concentrations in the range of 0.1–2.0 mg·L⁻¹. DODA mRNA levels were consistent with the response of betacyanin content to exogenous growth regulators. These results suggest that betacyanin metabolism in S. salsa calluses is regulated under white light conditions by growth regulators through the regulation of genes such as DODA that are involved in betacyanin synthesis.     

Essential oils of Cupressus funebris, Juniperus communis, and J. chinensis (Cupressaceae) as repellents against ticks (Acari: Ixodidae) and mosquitoes (Diptera: Culicidae) and as toxicants against mosquitoes

Juniperus communis leaf oil, J. chinensis wood oil, and Cupressus funebris wood oil (Cupressaceae) from China were analyzed by gas chromatography and gas chromatography-mass spectrometry. We identified 104 compounds, representing 66.8-95.5% of the oils. The major components were: α-pinene (27.0%), α-terpinene (14.0%), and linalool (10.9%) for J. communis; cuparene (11.3%) and δ-cadinene (7.8%) for J. chinensis; and α-cedrene (16.9%), cedrol (7.6%), and β-cedrene (5.7%) for C. funebris. The essential oils of C. funebris, J. chinensis, and J. communis were evaluated for repellency against adult yellow fever mosquitoes, Aedes aegypti (L.), host-seeking nymphs of the lone star tick, Amblyomma americanum (L.), and the blacklegged tick, Ixodes scapularis Say, and for toxicity against Ae. aegypti larvae and adults, all in laboratory bioassays. All the oils were repellent to both species of ticks. The EC(95) values of C. funebris, J. communis, and J. chinensis against A. americanum were 0.426, 0.508, and 0.917 mg oil/cm(2) filter paper, respectively, compared to 0.683 mg deet/cm(2) filter paper. All I. scapularis nymphs were repelled by 0.103 mg oil/cm(2) filter paper of C. funebris oil. At 4 h after application, 0.827 mg oil/cm(2) filter paper, C. funebris and J. chinensis oils repelled ≥80% of A. americanum nymphs. The oils of C. funebris and J. chinensis did not prevent female Ae. aegypti from biting at the highest dosage tested (1.500 mg/cm(2) ). However, the oil of J. communis had a Minimum Effective Dosage (estimate of ED(99) ) for repellency of 0.029 ± 0.018 mg/cm(2) ; this oil was nearly as potent as deet. The oil of J. chinensis showed a mild ability to kill Ae. aegypti larvae, at 80 and 100% at 125 and 250 ppm, respectively.