Radotinib, developed as a BCR/ABL tyrosine kinase inhibitor (TKI), is approved for the second-line treatment of chronic myeloid leukemia (CML) in South Korea. However, therapeutic effects of radotinib in acute myeloid leukemia (AML) are unknown. In the present study, we demonstrate that radotinib significantly decreases the viability of AML cells in a dose-dependent manner. Kasumi-1 cells were ...

The promyelocytic HL60 cell can be differentiated with dimethyl sulphoxide or dibutyryl cyclic AMP leading to the appearance of fMetLeuPhe receptors on the cell surface. G-protein-stimulated polyphosphoinositide phosphodiesterase (PPI-pde) activity was assessed in membranes prepared from both differentiated and non-differentiated HL60 cells. Both the extent of the response and the rank order of...

Telomere and Telomerase have recently been explored as anti-aging and anti-cancer drug targets with only limited success. Previously we showed that the Chinese herbal medicine Tianshengyuan-1 (TSY-1), an agent used to treat bone marrow deficiency, has a profound effect on stimulating Telomerase activity in hematopoietic cells. Here, the mechanism of TSY-1 on cellular Telomerase activity was fur...

ATP and UTP cause mobilization of Ca2+ from the intracellular stores with similar potency in several cell types including both undifferentiated and differentiated HL60 cells. We show here that, in HL60 cells with Ca2+ stores that had been fully and irreversibly emptied using the endomembrane Ca(2+)-ATPase inhibitor thapsigargin, both nucleotides produced a biphasic effect on Ca2+ entry, first r...

Part of the cytotoxic action of a lkyllysophosphol ip ids (ALP) on leukemic cells is known to result from the lack of an O-alkyl cleavage enzyme and its antimetabolic effect which results in a toxic lysophosphol ipid buildup. Further, ALP (5/.Lg/ml) suppresses c lonogenic i ty and trit iated thymidine uptake in HL60 cultures after 24 hr of exposure. The effect of ALP on two leukemic cell lines,...

An efficient method for the synthesis of 3-(1H-indol-3-yl)-2-(7,8,12,13-tetraoxa-10-azaspiro[5.7]tridecan-10-yl)propanoic acid) via condensation 7,8,10,12,13-pentaoxaspiro[5.7]tridecane with tryptophan under action a catalyst based on Sm(NO3)3·6H2O has been developed. A high cytotoxic activity eight-membered azadiperoxide against tumor cells Jurkat, K562, U937, and HL60 was established. Additio...

Violacein, a pigment isolated from Chromobacterium violaceum in the Amazon River, presents diverse biologic properties and attracts interest as a consequence of its antileukemic activity. Elucidation of the molecular mechanism mediating this activity will provide further relevant information for understanding its effects on the cellular physiology of untransformed cells and for considering its ...

Although increased Na+/H+ exchange (antiport) activity has been shown to precede both granulocytic and monocytic differentiation of HL60 cells, its requirement for this process remains controversial. We show here that, in the absence of HCO3-, the Na+/H+ exchanger is the predominant mechanism involved in rapid recovery of pHi from cytoplasmic acidosis; however, in the presence of HCO3-, other m...

2-(3,4-Dihydroxyphenyl)ethanol (DPE), a naturally occurring phenolic antioxidant molecule found in olive oil, has been reported to exert several biological and pharmacological activities. We studied the effect of this compound on the proliferation and survival of HL60 cell line. Concentrations from 50 to 100 microM DPE, comparable to its olive oil content, caused a complete arrest of HL60 cell ...

The protein tyrosine kinase Syk plays a central role in Fcgamma receptor-mediated phagocytosis in the adaptive immune system. We show here that Syk also plays an essential role in complement-mediated phagocytosis in innate immunity. Macrophage-like differentiated HL60 cells and C3bi-opsonized zymosan comprised the pathogen-phagocyte system. C3bi-opsonized zymosan particles promptly attached to ...