水稻类病斑突变体在研究水稻细胞程序性死亡和广谱抗病性中具有重要作用,已报道的水稻类病斑主要发生在叶片上,少量发生在颖壳上。本研究中首次报道了水稻的一种穗叶类病斑突变体pls1(Panicle and leaf spot 1),其从三叶期叶片开始出现...水稻类病斑突变体在研究水稻细胞程序性死亡和广谱抗病性中具有重要作用,已报道的水稻类病斑主要发生在叶片上,少量发生在颖壳上。本研究中首次报道了水稻的一种穗叶类病斑突变体pls1(Panicle and leaf spot 1),其从三叶期叶片开始出现红褐色斑点,随生育进程扩大,并扩展到其他器官。与以往报道的水稻类病斑突变体不同的是,pls1抽穗后稻穗枝梗和颖壳逐渐产生红褐色病斑,成熟期稻穗干枯,严重影响产量,是一种新类型的水稻类病斑。结合图位克隆和全基因组重测序发现pls1突变体产生了173403 bp的大片段缺失,导致7个基因缺失和1个基因启动子缺失。这8个基因中4个编码醇溶蛋白,另外3个在叶片和穗部表达量较低,只有Os12g0268000在叶片和稻穗中较其他器官有较高的表达量,推测PLS1为Os12g0268000,基因功能注释显示其编码色胺5-羟化酶。pls1突变体叶片中活性氧、过氧化氢、超氧阴离子过量积累,抗氧系统相关酶氧化物歧化酶、抗坏血酸过氧化物酶、过氧化氢酶和谷胱甘肽还原酶活性提高,发生细胞程序性死亡和叶绿体降解,降低光合能力。褪黑素在植物耐盐性中起重要作用。进一步的功能分析发现,缺失PLS1会抑制水稻中褪黑素合成相关酶基因OsTDC1、OsTDC3、OsSNAT1、OsASMT1和OsCOMT的表达,进而导致pls1突变体的耐盐性下降。综上,穗叶类病斑突变体pls1是一种新类型的水稻类病斑突变体,将为水稻类病斑研究提供新的种质材料;耐盐性的分析揭示了色胺5-羟化酶的新功能,为研究其在细胞程序性死亡和耐盐性中的机制提供了新视角。展开更多
HIV/AIDS has been one of the most devastating global diseases. HIV-1 protease proteolytic action is responsible for the manufacture of grown, infectious species, consequently HIV-1 protease has become an attractive go...HIV/AIDS has been one of the most devastating global diseases. HIV-1 protease proteolytic action is responsible for the manufacture of grown, infectious species, consequently HIV-1 protease has become an attractive goal in the treatment and therapy of HIV. Several HIV-1 protease inhibitors based therapeutic agents are under investigation or currently in the market. Lopinavir (ABT-378) has a great value in this research field. Therefore, different methods have appeared aiming to develop efficient analogs by the utilization of variable techniques, since Lopinavir had showed low bioavailability when being prescribed alone, and various side effects after the combination of Lopinavir with another HIV-1 inhibitors such as Ritonavir, which is available in the markets nowadays under the brand name Kaletra. Replacement of the hydroxyethylene moiety in Lopinavir structure, which is responsible for the monohydroxylated metabolites with the stable to hydrolysis phosphinic group has been considered, since that hydroxyl group in the central core is responsible for the interaction with the carboxylic acid in the catalytic aspartyl residue of HIV-1 by hydrogen bonding and consequently supports the drug affinity to the protease. The small scale processes for the synthetic strategies for the new candidate phosphinic analog of Lopinavir protease inhibitor (PL1) is presented here in along with some preliminary pharmacological data.展开更多
文摘HIV/AIDS has been one of the most devastating global diseases. HIV-1 protease proteolytic action is responsible for the manufacture of grown, infectious species, consequently HIV-1 protease has become an attractive goal in the treatment and therapy of HIV. Several HIV-1 protease inhibitors based therapeutic agents are under investigation or currently in the market. Lopinavir (ABT-378) has a great value in this research field. Therefore, different methods have appeared aiming to develop efficient analogs by the utilization of variable techniques, since Lopinavir had showed low bioavailability when being prescribed alone, and various side effects after the combination of Lopinavir with another HIV-1 inhibitors such as Ritonavir, which is available in the markets nowadays under the brand name Kaletra. Replacement of the hydroxyethylene moiety in Lopinavir structure, which is responsible for the monohydroxylated metabolites with the stable to hydrolysis phosphinic group has been considered, since that hydroxyl group in the central core is responsible for the interaction with the carboxylic acid in the catalytic aspartyl residue of HIV-1 by hydrogen bonding and consequently supports the drug affinity to the protease. The small scale processes for the synthetic strategies for the new candidate phosphinic analog of Lopinavir protease inhibitor (PL1) is presented here in along with some preliminary pharmacological data.
