Abstract
BackgroundThe aim of this study was to evaluate the biological and pharmaceutical activities of 14 amphiphilic liquid-crystalline compounds (LCs), i.e, phenylpyrimidine derivatives possessing D-glucamine and cyanobiphenyl derivatives with a terminal hydroxyl unit.ResultsThe cytotoxic properties of the LCs on the cell growth, cell cycle distribution, and cell signaling pathway of U937 human leukemic monocyte lymphoma cells were assessed by flow cytometry and western blot analysis. Some LCs showed cytostatic effects, suppressing cell growth via S-phase arrest and without apoptosis in U937 cells. To investigate the mechanisms of the LC-induced S-phase arrest, proteins relevant to cell cycle regulation were investigated by western blot analysis. The rate of LC-induced S-phase arrest was congruent with the decreased expression of MCM2, cyclin A, cyclin B, CDK2, phospho-CDK1 and Cdc25C. Observed changes in cell cycle distribution by LC treated might be caused by insufficient preparation for G2/M transition. Considering the structure of the LCs, the rod-like molecules displaying cytotoxicity against U937 cells possessed flexible spacers with no bulky polar group attached via the flexible spacer.ConclusionsOur results revealed that some LCs showed cytotoxic properties against non-solid type tumor human leukemic cells via LC-induced S-phase arrest and decreasing expression of several cell cycle related proteins.
Highlights
The aim of this study was to evaluate the biological and pharmaceutical activities of 14 amphiphilic liquid-crystalline compounds (LCs), i.e, phenylpyrimidine derivatives possessing D-glucamine and cyanobiphenyl derivatives with a terminal hydroxyl unit
We investigated the cytotoxic properties of 14 amphiphilic LCs against the human leukemic monocyte lymphoma cell line U937
The pharmaceutical activities of 14 amphiphilic LCs were examined in human leukemic monocyte lymphoma U937 cells (Table 1)
Summary
The aim of this study was to evaluate the biological and pharmaceutical activities of 14 amphiphilic liquid-crystalline compounds (LCs), i.e, phenylpyrimidine derivatives possessing D-glucamine and cyanobiphenyl derivatives with a terminal hydroxyl unit. Several types of chemotherapeutic agents have been developed recently, such as molecular targetting drugs, the tyrosine kinase inhibitor Imatinib, only few drugs may result in complete recovery of cancer patients. Amphiphilic liquid crystals are thought to have structural affinity to the cell membranes, which are lamellar bilayer mesophases of phospholipids, glycolipids, and cholesterol. Some lyotropic LCs displaying a structural affinity to the cell membranes have been applied for the development of novel drug delivery systems [3]. These amphiphilic LCs seem promising for biological applications, the pharmacological properties of LCs are not well understood, and must be elucidated
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
