一氧化氮(NO)是生命系统中普遍存在的气体递质,与内质网和溶酶体的病理生理过程密切相关。这种自由基气体在生物微环境中分布非常广泛但非常不均匀,这对特异性检测其在某些亚细胞区域的局部水平提出了巨大的挑战。在本研究中,我们通过合理的分子工程提出了六种亚细胞靶向探针,并选择了两种性能最佳的探针用于精确时空识别内质网(ER)和溶酶体NO波动。这些探针可以在铆接的亚细胞位置与NO快速发生N-亚硝化反应,阻断最初的光诱导电子转移(PET)过程并产生明亮的荧光,以精确定位ER和溶酶体中的NO。筛选出的探针对NO具有超灵敏的反应活性和超低的检测限,实现了相应亚细胞区域外源性和内源性NO的精确描绘。探针还成功地绘制了炎症过程中亚细胞 NO 水平的波动。我们的工作将有助于准确研究亚细胞NO在各种生物事件中的生理和病理后果。
Taskspecific ionic liquids and onium salts have been used as solublesupports for peptide synthesis. These new supports combine easy monitoring, high loading capacities, large scale preparation, and homogeneous kinetics characteristics while keeping advantages of solid-phase synthesis including easy purification and workup. Careful structural design of these supports allowed for fine tuning of physical
Disclosed is a novel anti-enterovirus 71 (EV71) 1,2,5-thiadiazolidine-1,1-dioxide derivative or a pharmaceutically acceptable salt thereof; and specifically, a compound represented by formula (II) or a pharmaceutically acceptable salt thereof.
Multitarget-directed resveratrol derivatives: anti-cholinesterases, anti-β-amyloid aggregation and monoamine oxidase inhibition properties against Alzheimer's disease
作者:Long-Fei Pan、Xiao-Bing Wang、Sai-Sai Xie、Su-Yi Li、Ling-Yi Kong
DOI:10.1039/c3md00376k
日期:——
Resveratrol derivatives were designed and synthesized as multitarget-directed agents for treating AD, and 6r was a balanced inhibitor toward all the tested targets.
The graphene oxide (GO) assisted allylic alkylation of thiophenes with alcohols is presented. Mild reaction conditions and a low GO loading enabled the isolation of a range of densely functionalized thienyl and bithienyl compounds in moderate to high yields (up to 90%). The cooperative action of the Brønsted acidity, epoxide moieties, and π-surface of the 2D-promoter is highlighted as crucial in the
Naphthalimide-benzimidazole conjugates were prepared using two different types of spacer
units; either a simple alkane chain or a substituted piperazine moiety with variable alkyl side chains.
Each set of conjugates was evaluated for their in vitro anticancer activity, and compounds 14a, 14b
and 20c were found to exhibit significant activity against a number of cancer cell lines. In particular,
compound 14a showed remarkable anticancer activity with GI50 values of 0.02 μM and 0.49 μM
against central nervous system (SNB-75) and leukemia (K-562) cell lines, respectively. Compound
14b showed noticeable activity against melanoma (MAME-3M) cell line with GI50 value 0.09 μM.
Compound 20c also displayed selectivity against leukemia cell lines with GI50 values up to 0.21 μM as
well as appreciable broad-spectrum cytotoxicity.