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Nitrofuran cell cycle

Sijun Deng, Shusheng Tang, Chongshan Dai, Yan Zhou, Xiayun Yang, Daowen Li, Xilong Xiao
Furazolidone (FZD), a synthetic nitrofuran with a broad spectrum of antimicrobial activities, has been shown to exhibit marked genotoxity and cytotoxicity in vitro, but the proper mechanism was unclear. P21(Waf1/Cip1) (p21), a cyclin-dependent kinase, is critically involved in cell cycle arrest and apoptosis in response to DNA injury. This study was aimed to explore the role of p21 in FZD-induced apoptosis in HepG2 cells and uncover its possible mechanism. Firstly, we demonstrated that FZD (50 μg/mL) treatment increased the mRNA level of p21 but reduced the protein level of p21 by shortening its half-life...
February 2016: Food and Chemical Toxicology
Ru-Wei Lin, Chia-Ning Yang, ShengYu Ku, Cheng-Jung Ho, Shih-Bo Huang, Min-Chi Yang, Hsin-Wen Chang, Chun-Mao Lin, Jaulang Hwang, Yeh-Long Chen, Cherg-Chyi Tzeng, Chihuei Wang
CFS-1686 (chemical name (E)-N-(2-(diethylamino)ethyl)-4-(2-(2-(5-nitrofuran-2-yl)vinyl)quinolin-4-ylamino)benzamide) inhibits cell proliferation and triggers late apoptosis in prostate cancer cell lines. Comparing the effect of CFS-1686 on cell cycle progression with the topoisomerase 1 inhibitor camptothecin revealed that CFS-1686 and camptothecin reduced DNA synthesis in S-phase, resulting in cell cycle arrest at the intra-S phase and G1-S boundary, respectively. The DNA damage in CFS-1686 and camptothecin treated cells was evaluated by the level of ATM phosphorylation, γH2AX, and γH2AX foci, showing that camptothecin was more effective than CFS-1686...
2014: PloS One
Yu Sun, Shusheng Tang, Xi Jin, Chaoming Zhang, Wenxia Zhao, Xilong Xiao
Furazolidone (FZD), a synthetic nitrofuran with a broad spectrum of antimicrobial actions, is known to induce genotoxicity and potential carcinogenicity in several types of cells, but little is known about its p38 mitogen-activation protein kinase (p38 MAPK) and c-Jun N-terminal protein kinase (JNK) pathways in human hepatoblastoma cell line (HepG2). Given the previously described essential roles of p38 MAPK and JNK pathways in HepG2 cells, we undertook the present study to investigate the roles of p38 MAPK and JNK pathways in cell cycle arrest of HepG2 cells stimulated with FZD...
July 4, 2013: Mutation Research
Chih-Hua Tseng, Chi-Yi Li, Chien-Chih Chiu, Huei-Ting Hu, Chein-Hwa Han, Yeh-Long Chen, Cherng-Chyi Tzeng
A number of 2,4,5-triaryl-1H-imidazole derivatives were synthesized and evaluated for their antiproliferative activities against the growth of five cell lines including three non-small cell lung cancers (H460, H1299, and A549), one breast cancer (MCF-7), and one normal diploid embryonic lung cell line (MRC-5). Preliminary results indicated that both 2-(5-bromofuran-2-yl)-4,5-bis{4-[3-(dimethylamino) propoxy] phenyl}-1H-imidazole (10f) and 4,5-bis{4-[3-(dimethylamino)propoxy]phenyl}-2-(5-nitrofuran-2-yl)-1H -imidazole (10g) were selectively active against the growth of H1229 with an IC(50) of less than 0...
November 2012: Molecular Diversity
C Maria Aravena, A Claudio Olea, Hugo Cerecetto, Mercedes González, Juan Diego Maya, Jorge Rodríguez-Becerra
Cyclic voltammetry and electron spin resonance techniques were used in the investigation of several potential antiprotozoal containing thiosemicarbazone and carbamate nitrofurans. In the electrochemical behaviour, a self-protonation process involving the nitro group was observed. The reactivity of the nitro anion radical for these derivatives with glutathione, a biological relevant thiol, was also studied in means of cyclic voltammetry. These studies demonstrated that glutathione could react with radical species from 5-nitrofuryl system...
July 2011: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Mariana Boiani, Lucia Piacenza, Paola Hernández, Lucia Boiani, Hugo Cerecetto, Mercedes González, Ana Denicola
Chagas disease is caused by the trypanosomatid parasite Trypanosoma cruzi and threatens millions of lives in South America. As other neglected diseases there is almost no research and development effort by the pharmaceutical industry and the treatment relies on two drugs, Nifurtimox and Benznidazole, discovered empirically more than three decades ago. Nifurtimox, a nitrofurane derivative, is believed to exert its biological activity through the bioreduction of the nitro-group to a nitro-anion radical which undergoes redox-cycling with molecular oxygen...
June 15, 2010: Biochemical Pharmacology
Feng-Shuo Chang, Weichung Chen, Chihuei Wang, Cherng-Chyi Tzeng, Yeh-Long Chen
The present study describes the synthesis of 2-phenylvinylquinoline (styrylquinoline) and 2-furanylvinylquinoline derivatives and evaluation for their antiproliferative activities. (E)-2-Styrylquinolin-8-ol (14a) was inactive against a 3-cell line panel consisting of MCF-7 (Breast), NCI-H460 (Lung), and SF-268 (CNS). Replacement of the phenyl ring with 5-nitrofuran-2-yl group significantly enhanced antiproliferative activity in which (E)-2-(2-(5-nitrofuran-2-yl)vinyl)quinolin-8-ol (14i) and its 4-substituted derivatives 15-19 exhibited strong inhibitory effects against the growth of all three cancer cells...
January 1, 2010: Bioorganic & Medicinal Chemistry
Maria Polycarpou-Schwarz, Kerstin Müller, Stefanie Denger, Andrew Riddell, Joe Lewis, Frank Gannon, George Reid
A series of nitrofuran-based compounds were identified as inhibitors of estrogen signaling in a cell-based, high-throughput screen of a diverse library of small molecules. These highly related compounds were subsequently found to inhibit topoisomerase II in vitro at concentrations similar to that required for the inhibition of estrogen signaling in cells. The most potent nitrofuran discovered is approximately 10-fold more active than etoposide phosphate, a topoisomerase II inhibitor in clinical use. The nitrofurans also inhibit topoisomerase I activity, with approximately 20-fold less activity...
May 1, 2007: Cancer Research
Lucía Otero, Gabriela Aguirre, Lucía Boiani, Ana Denicola, Carolina Rigol, Claudio Olea-Azar, Juan Diego Maya, Antonio Morello, Mercedes González, Dinorah Gambino, Hugo Cerecetto
Rhenium and ruthenium complexes of the type [Re(V)OCl(2)(PPh(3))L] and [Ru(II)Cl(2)(DMSO)(2)L], where L are 5-nitrofurylsemicarbazone derivatives, were prepared in an effort to obtain new anti-trypanosomal agents combining the recognized biological activity of these metals and the trypanocidal activity of the free ligands. Rhenium complexes resulted unstable in aqueous solution not allowing their use as potential drugs. On the other hand, complexation to ruthenium of the bioactive ligands lead to the lack of antiprotozoa activity even though free radical production and redox cycling induction were detected when the compounds were incubated in presence of Trypanosoma cruzi cells...
November 2006: European Journal of Medicinal Chemistry
K Blumenstiel, R Schöneck, V Yardley, S L Croft, R L Krauth-Siegel
Lipoamide dehydrogenase (LipDH), trypanothione reductase (TR), and glutathione reductase (GR) catalyze the NAD(P)H-dependent reduction of disulfide substrates. TR occurs exclusively in trypanosomatids which lack a GR. Besides their physiological reactions, the flavoenzymes catalyze the single-electron reduction of nitrofurans with the concomitant generation of superoxide anions. Here, we report on the interaction of clinically used antimicrobial nitrofurans with LipDH and TR from Trypanosoma cruzi, the causative agent of Chagas' disease (South American trypanosomiasis), in comparison to mammalian LipDH and GR...
December 1, 1999: Biochemical Pharmacology
J Sarlauskas, E Dickancaite, A Nemeikaite, Z Anusevicius, H Nivinskas, J Segura-Aguilar, N Cenas
We have synthesized a number of nitrobenzimidazoles containing nitro groups in the benzene ring and found that they acted as relatively efficient substrates for rat liver DT-diaphorase (EC, their reactivity exceeding reactivities of nitrofurans and nitrobenzenes. Nitrobenzimidazoles were competitive with NADPH inhibitors of DT-diaphorase in menadione reductase reactions, their inhibition constant being unchanged in the presence of dicumarol and being increased in the presence of 2',5'-ADP. These data indicate that the poor reactivity of nitrobenzimidazoles and other nitroaromatics in comparison to quinones could be determined by their binding in the adenosine-phosphate binding region of the NADPH-binding site, whereas quinones bind at the nicotinamide-binding pocket at the vicinity of FAD of DT-diaphorase...
October 15, 1997: Archives of Biochemistry and Biophysics
R Schöneck, O Billaut-Mulot, P Numrich, M A Ouaissi, R L Krauth-Siegel
This work presents the complete sequences of a cDNA and the two allelic genes of dihydrolipoamide dehydrogenase (LipDH) from Trypanosoma cruzi, the causative agent of Chagas' disease (American trypanosomiasis). The full-length cDNA has an ORF of 1431 bp and encodes a protein of 477 amino acid residues. LipDH is a homodimeric protein with FAD as prosthetic group. The calculated molecular mass of the subunit of the mature protein with bound FAD is 50,066. Comparison of the deduced amino acid sequence of LipDH from T...
February 1, 1997: European Journal of Biochemistry
P Sur, S P Chatterjee, P Roy, B Sur
Compounds formed by 5-nitrofuran with hydrazides of formic, acetic and propionic acids, hereafter respectively known as SBF, SBA and SBP have been used to evaluate the differentiation-inducing properties on two established myeloid leukaemic cell lines ML-2 and EOL-1. SBP is found to be the most effective as an antineoplastic agent amongst the three. Induction of differentiation observed are in the order SBP > SBA > SBF, as assessed by morphology, NBT-reducing activity and surface marker antigens of the treated cells...
July 20, 1995: Cancer Letters
P L Olive
When thioguanine-resistant V79 cells are introduced into spinner flasks containing V79 multicell spheroids, the mutant cells attach to the surface of the spheroids. The composite spheroids thus formed consist of external, thioguanine-resistant (TGr) and internal, thioguanine-sensitive cells. Cell sorting with a Becton Dickinson FACS II was used to determine the relative position of TGr cells and sensitivity to fluorescent drugs. After 2-4 days, the TGr cells are found internally as well as externally. The initial percentage of TGr cells varies from 1 to 50%, depending on the size of the single-cell inoculum, size of spheroids and frequency of addition of cells during a 24th period...
January 1981: British Journal of Cancer
L Rossi, J M Silva, L G McGirr, P J O'Brien
Freshly isolated rat hepatocytes were used to study the mechanism(s) of toxicity of the antimicrobial drug nitrofurantoin. This 5-nitrofuran derivative stimulated hepatocyte oxygen uptake in the presence of the mitochondrial respiration inhibitors KCN or antimycin A. This could indicate the formation of O2- and H2O2, following intracellular nitrofurantoin reduction. Addition of nitrofurantoin to suspensions of isolated rat hepatocytes produced a dose- and time-dependent decrease of cell viability. H2O2 probably plays a significant role in the cytotoxic effects of nitrofurantoin as the catalase inhibitors azide or aminotriazole markedly enhanced cytotoxicity...
August 15, 1988: Biochemical Pharmacology
G B Henderson, P Ulrich, A H Fairlamb, I Rosenberg, M Pereira, M Sela, A Cerami
The trypanosomatid flavoprotein disulfide reductase, trypanothione reductase, is shown to catalyze one-electron reduction of suitably substituted naphthoquinone and nitrofuran derivatives. A number of such compounds have been chemically synthesized, and a structure-activity relationship has been established; the enzyme is most active with compounds that contain basic functional groups in side-chain residues. The reduced products are readily reoxidized by molecular oxygen and thus undergo classical enzyme-catalyzed redox cycling...
August 1988: Proceedings of the National Academy of Sciences of the United States of America
C R de Castro, E G de Toranzo, A S Bernacchi, M Carbone, J A Castro
Chagas' disease is a parasitic chronic condition affecting several million people in Latin America. Two drugs are used in the chemotherapy of Chagas' disease: nifurtimox (Nfx) and benznidazole (Bz). Both are nitroderivatives whose deleterious effects are related to their reductive biotransformation. In this work we report that rat ovaries exhibited Bz and Nfx nitroreductase activity. The Bz nitroreductase was only found in the mitochondrial fraction and was partially inhibited by CO. The Nfx nitroreductase activity was maximal in ovarian mitochondria but was also present in microsomes and in the cytosol...
June 1989: Experimental and Molecular Pathology
S Klee, F R Ungemach
The intestinal biotransformation and absorption of the nitrofuran furazolidone were investigated in isolated gut cells and in the isolated perfused gut. In case of inhibiting furazolidone metabolism by high oxygen tension almost equal concentrations of the parent compound were measured on the mucosal and serosal side of the perfused gut segments. Lowering oxygen supply in order to adjust it to physiological conditions caused a complete degradation of furazolidone in isolated gut cells. Accordingly, hardly any unchanged furazolidone was detected on the serosal side of the isolated perfused gut...
October 1992: DTW. Deutsche Tierärztliche Wochenschrift
N Inui, Y Nishi, M Taketomi
Hamster embryos were treated with 2-(2-furyl)-3-(5-nitro-2-furyl)acrylamide (AF-2) in vivo (in the mother) by transplacental application. The fetuses were isolated 24 h after administration of the AF-2 and cultured. Within the first 24h of primary culture, some parts of the cells were treated with colcemide for 3 h so that mitotic cells could be observed in the first cell cycle in vitro. Cultured embryonic fibroblasts in metaphase plates showed a marked dose-dependence in chromosomal aberrations. Transplacental application of AF-2 also caused slightly dose-dependent morphological transformation...
November 1978: Mutation Research
J A Dvorak, C L Howe
The effects of 3-methyl-4-(5'-nitrofurfurylidene-amino)-tetrahydro-4H-1,4-thiazine-1,1-dioxide [Lampit, Bayer 2502] on the intracellular cycle of Trypanosoma cruzi were studied with an in vitro steady-state culture system that permitted the continuous analysis of individual host cell-parasite interactions. Lampit concentrations of 10(-4) and 10(-5) M significantly affected the ability of trypomastigotes to penetrate vertebrate cells. Lampit concentrations above 10(-4) M were toxic to the host cell population and Lampit concentrations below 10(-5) M did not affect the ability of trypomastigotes to penetrate vertebrate cells...
January 1977: American Journal of Tropical Medicine and Hygiene
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