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1.
Food Chem ; 352: 129415, 2021 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-33711728

RESUMO

Furazolidone (FZD) and its metabolite called 3-amino-2-oxazolidinone (AOZ) would induce carcinogenic and mutagenic effects to human. In this work, to develop a novel, stable, and simple point of care testing (POCT) with a potential to social applied for FZD detection, we utilized the aspect of protein staining of coomassie brilliant blue (CBB) to exploit a new CBB-LFIA strategy free of NPs. Only one mixing step is needed during the probe manufacturing process, which requires just 2 h and is a great time saving strategy compared with other methods (requiring 4-33 h for probe preparation). Besides, the cost of CBB-LFIA is 300 times lesser than other LFIA with respect to obtaining the label. The developed CBB-LFIA was successfully applied to detect AOZ with a detection limit of 2 ng mL-1, without any influence from other potential interfering compounds. The proposed CBB-LFIA exhibited prominent practical application, and possesses considerable utilization potential in the related field.


Assuntos
Custos e Análise de Custo , Furazolidona/análise , Furazolidona/química , Imunoensaio/economia , Imunoensaio/métodos , Sistemas Automatizados de Assistência Junto ao Leito/economia , Corantes de Rosanilina/química , Humanos , Limite de Detecção , Fatores de Tempo
2.
Oxid Med Cell Longev ; 2021: 6610726, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33613823

RESUMO

Exposure to total body irradiation (TBI) causes dose- and tissue-specific lethality. However, there are few effective and nontoxic radiation countermeasures for the radiation injury. In the current study, mice were pretreated with a traditional antimicrobial agent, FZD, before TBI; the protective effects of FZD on radiation injury were evaluated by using parameters such as the spleen index and thymus index, immunohistochemical staining of intestinal tissue, and frequency of micronuclei in polychromatophilic erythrocytes of bone marrow. The intestinal epithelial cell line IEC-6 was used to investigate the underlying mechanisms. Our results indicated that FZD administration significantly improved the survival of lethal dose-irradiated mice, decreased the number of micronuclei, upregulated the number of leukocytes and immune organ indices, and restored intestinal integrity in mice after TBI. TUNEL and western blot showed that FZD protected intestinal tissue by downregulating radiation-induced apoptosis and autophagy. Meanwhile, FZD protected IEC-6 cells from radiation-induced cell death by inhibiting apoptosis and autophagy. To sum up, FZD protected against radiation-induced cell death both in vitro and in vivo through antiapoptosis and antiautophagy mechanisms.


Assuntos
Apoptose , Autofagia , Furazolidona/uso terapêutico , Lesões Experimentais por Radiação/tratamento farmacológico , Lesões Experimentais por Radiação/patologia , Irradiação Corporal Total , Animais , Apoptose/efeitos dos fármacos , Apoptose/efeitos da radiação , Autofagia/efeitos dos fármacos , Autofagia/efeitos da radiação , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos da radiação , Linhagem Celular , Furazolidona/química , Furazolidona/farmacologia , Hematopoese/efeitos dos fármacos , Hematopoese/efeitos da radiação , Intestinos/efeitos dos fármacos , Intestinos/patologia , Intestinos/efeitos da radiação , Masculino , Camundongos Endogâmicos ICR , Microvilosidades/efeitos dos fármacos , Microvilosidades/patologia , Microvilosidades/efeitos da radiação , Tolerância a Radiação/efeitos dos fármacos , Tolerância a Radiação/efeitos da radiação , Radiação Ionizante , Protetores contra Radiação/química , Protetores contra Radiação/farmacologia , Protetores contra Radiação/uso terapêutico , Análise de Sobrevida , Fatores de Tempo
3.
Kaohsiung J Med Sci ; 36(12): 998-1003, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32767507

RESUMO

Targeting nuclear factor kappa B (NF-κB) signaling pathway has become a promising strategy for the development of new antitumor drugs. In this paper, we found that anti-infection drug furazolidone (FZD) could significantly inhibit NF-κB-driven luciferase activity, and FZD could markedly inhibit both of the constitutive and tumor necrosis factor-α (TNFα)-triggered phosphorylation of NF-κB p65 in small cell lung cancer (SCLC). Further studies revealed that FZD inhibited the expression of inhibitor of kappa B kinase ß (IKKß) in SCLC cells. In addition, we found that FZD had significant antitumor activities in SCLC cells. FZD could markedly suppress the cell viability of SCLC cells dose-dependently, and FZD could significantly induce the cleavages of poly ADP-ribose polymerase (PARP) and Caspase3, the biomarkers of cell apoptosis, in SCLC cells. The flow cytometry also revealed that FZD induced cell apoptosis in SCLC cells. Finally, we also found that overexpression of constitutively activated IKKß could significantly abolish FZD-induced cell growth inhibition in SCLC cells, which further confirmed that FZD displayed its anti-SCLC activity through regulating NF-κB signaling pathway.


Assuntos
Anti-Infecciosos/farmacologia , Apoptose , Furazolidona/farmacologia , Neoplasias Pulmonares/patologia , NF-kappa B/metabolismo , Transdução de Sinais , Carcinoma de Pequenas Células do Pulmão/patologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Furazolidona/química , Humanos , Quinase I-kappa B/metabolismo , Transdução de Sinais/efeitos dos fármacos
4.
Xenobiotica ; 43(12): 1095-102, 2013 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-23638824

RESUMO

A sensitive and specific HPLC-APCI-MS/MS method was developed and validated for the quantification of furanodiene, a natural antitumor compound in rat plasma and tissues. W/O/W multiple emulsions of furanodiene, identified through microscope-observation and eosin staining method, were prepared with a two-step-procedure. Pharmacokinetics and tissue distribution were studied in rats after oral, intraperitoneal and intravenous injection with the dose of 5, 10 and 50 mg/kg, respectively. The assay achieved a good sensitivity and specificity for the determination of furanodiene in biological samples. The results showed that the concentration-time curves of furanodiene in rats after intravenous injection were fitted to a two-compartment model and the linear pharmacokinetic characteristic. The highest concentration in rat tissue was observed in the spleen, followed by heart, liver, lung, kidney, small intestine and brain. Comparing with the low concentration in plasma, furanodiene could be detected in various tissue samples after oral or intraperitoneal injection which indicated furanodiene had good and rapid tissue uptake. The results suggested that the wide tissue distribution of furanodiene could conduce to the therapeutic effects, but the short biological half-life limited its further application as an antitumor agent. The results are helpful for the structure modification of furanodiene as an antitumor candidate.


Assuntos
Pressão Atmosférica , Cromatografia Líquida de Alta Pressão/métodos , Furanos/farmacocinética , Compostos Heterocíclicos com 2 Anéis/farmacocinética , Espectrometria de Massas/métodos , Óleos/química , Água/química , Animais , Calibragem , Emulsões , Furanos/administração & dosagem , Furanos/sangue , Furanos/química , Furazolidona/química , Compostos Heterocíclicos com 2 Anéis/administração & dosagem , Compostos Heterocíclicos com 2 Anéis/sangue , Compostos Heterocíclicos com 2 Anéis/química , Injeções Intravenosas , Fígado/metabolismo , Masculino , Ratos , Ratos Wistar , Reprodutibilidade dos Testes , Fatores de Tempo , Distribuição Tecidual
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