10436-25-6Relevant articles and documents
Covalent inhibition of bacterial quorum sensing
Amara, Neri,Mashiach, Roi,Amar, Dotan,Krief, Pnina,Spieser, Stephane A. H.,Bottomley, Matthew J.,Aharoni, Amir,Meijler, Michael M.
, p. 10610 - 10619 (2009)
Chemical coordination of gene expression among bacteria as a function of population density is regulated by a mechanism known as 'quorum sensing' (QS). QS in Pseudomonas aeruginosa, an opportunistic pathogen that causes disease in immunocompromised patients, is mediated by binding of the transcriptional activator, LasR, to its ligand, 3-oxo-C12-HSL, leading to population-wide secretion of virulence factors and biofilm formation. We have targeted QS in P. aeruginosa with a set of electrophilic probes designed to covalently bind Cys79 in the LasR binding pocket, leading to specific inhibition of QS-regulated gene expression and concomitant reduction of virulence factor secretion and biofilm formation. This first example of covalent modification of a QS receptor provides a new tool to study molecular mechanisms of bacterial group behavior and could lead to new strategies for targeting bacterial virulence.
Sparrow
, p. 1350,1352 (1976)
The Synthesis of a Glucosyldiglyceride for Constructing pH-Sensitive Liposomes
Alshoaibi,Andryushina,Morozova,Serebrennikova
, p. 293 - 295 (2003)
A glucosyldiglyceride containing residues of 11-aminoundecanoic acid was synthesized for constructing pH-sensitive liposomes.
Helicity- and Molecular-Weight-Driven Self-Sorting and Assembly of Helical Polymers towards Two-Dimensional Smectic Architectures and Selectively Adhesive Gels
Li, Yan-Xiang,Xu, Lei,Kang, Shu-Ming,Zhou, Li,Liu, Na,Wu, Zong-Quan
, p. 7174 - 7179 (2021)
Self-sorting plays a crucial role in living systems such as the selective assembly of DNA and specific folding of proteins. However, the self-sorting of artificial helical polymers such as biomacromolecules has rarely been achieved. In this work, single-h
Synthesis and antibacterial evaluation of novel 3-substituted ocotillol-type derivatives as leads
Bi, Yi,Liu, Xian-Xuan,Zhang, Heng-Yuan,Yang, Xiao,Liu, Ze-Yun,Lu, Jing,Lewis, Peter John,Wang, Chong-Zhi,Xu, Jin-Yi,Meng, Qing-Guo,Ma, Cong,Yuan, Chun-Su
, (2017)
Due to the rapidly growing bacterial antibiotic-resistance and the scarcity of novel agents in development, bacterial infection is still a global problem. Therefore, new types of antibacterial agents, which are effective both alone and in combination with traditional antibiotics, are urgently needed. In this paper, a series of antibacterial ocotillol-type C-24 epimers modified from natural 20(S)-protopanaxadiol were synthesized and evaluated for their antibacterial activity. According to the screening results of Gram-positive bacteria (B. subtilis 168 and MRSA USA300) and Gram-negative bacteria (P. aer PAO1 and A. baum ATCC19606) in vitro, the derivatives exhibited good antibacterial activity, particularly against Gram-positive bacteria with an minimum inhibitory concentrations (MIC) value of 2-16 μg/mL. The subsequent synergistic antibacterial assay showed that derivatives 5c and 6c enhanced the susceptibility of B. subtilis 168 and MRSA USA300 to chloramphenicol (CHL) and kanamycin (KAN) (FICI 0.5). Our data showed that ocotillol-type derivatives with long-chain amino acid substituents at C-3 were good leads against antibiotic-resistant pathogens MRSA USA300, which could improve the ability of KAN and CHL to exhibit antibacterial activity at much lower concentrations with reduced toxicity.
ORGANIC COMPOSITIONS TO TREAT APOC3-RELATED DISEASES
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Paragraph 00708, (2016/02/26)
The present disclosure relates to compositions and methods for treating APOC3-related diseases such as: hypertriglyceridemia (e.g., Type V Hypertriglyceridemia), abnormal lipid metabolism, abnormal cholesterol metabolism, atherosclerosis, hyperlipidemia, diabetes, including Type 2 diabetes, obesity, cardiovascular disease, and coronary artery disease, among other disorders relating to abnormal metabolism or otherwise, using a therapeutically effective amount of a RNAi agent to APOC3.
