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1.
FEMS Microbiol Lett ; 3702023 Jan 17.
Artigo em Inglês | MEDLINE | ID: mdl-36521844

RESUMO

Thiobencarb is a highly effective thiocarbamate herbicide frequently used in rice fields globally. In this study, three bacterial strains (Dechloromonas sp. Th1, Thauera sp. Th2, and Azoarcus sp. Th3) isolated from immobilized biomass were analyzed for thiobencarb degradation under anaerobic conditions, with nitrate serving as an electron acceptor. The experimental results showed that thiobencarb was transformed by Dechloromonas sp. Th1 and Thauera sp. Th2 to produce high concentrations of metabolites in a mineral medium. Dechloromonas sp. Th1 dechlorinated the herbicide to benzyl mercaptan, which was then degraded by Thauera sp. Th2 and Azoarcus sp. Th3. Azoarcus sp. Th3 effectively degraded intermediates, i.e. 4-chlorobenzyl alcohol, 4-chlorobenzoic acid, and benzoic acid, produced from the degradation by Dechloromonas sp. Th1 and Thauera sp. Th2. The cross-feeding, nutrient sharing, and cooperation of all isolates in the degradation process decreased the concentrations of intermediate products. The determination of the degradation kinetics showed that the utilization in the exponential phase of the mixed bacteria was consistent with the Michaelis-Menten model, with a maximum degradation rate of 1.56 ± 0.16 µM day-1. This study showed the degradation mechanisms in bacteria and the synergistic process in the degradation of thiobencarb and its metabolites.


Assuntos
Herbicidas , Anaerobiose , Herbicidas/metabolismo , Bactérias/metabolismo , Tiocarbamatos/metabolismo , Biodegradação Ambiental
2.
Chem Commun (Camb) ; 58(88): 12353-12356, 2022 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-36263456

RESUMO

Thiocarbamates could be synthesized in green solvents via thiol-dioxazolone modified Lossen rearrangement under transition-metal free, additive free, and mild conditions. Polythiocarbamates were further prepared with excellent self-healing and shape-memory properties, showing great potential in the development of functional materials.


Assuntos
Compostos de Sulfidrila , Tiocarbamatos
3.
Sci Rep ; 12(1): 16764, 2022 10 06.
Artigo em Inglês | MEDLINE | ID: mdl-36202878

RESUMO

Phenacoccus solenopsis Tinsley (Hemiptera: Pseudococcidae) an invasive mealybug on cotton is primarily controlled by conventional insecticides. An endoparasitoid Aenasius arizonenesis (Girault) (Hymenoptera: Encyrtidae) is a potential biocontrol agent of this pest. We assessed the susceptibility in field populations of P. solenopsis and A. arizonensis to commonly used insecticides: profenofos, imidacloprid and thiodicarb. Reproductive traits of the parasitoid and Environmental Risk Assessment (ERA) parameters viz., Reduction coefficient, Descriptive analysis, Risk Index (RI), Selectivity ratio and Hazard quotient were measured to assess the direct and indirect effects of these insecticides on the parasitoid. Probit analysis revealed heterogeneity in the insecticide resistance development for both the cotton mealybug and its parasitoid. The field populations of P. solenopsis exhibited resistance to profenofos (18.87-59.86 folds) and thiodicarb (20.07 folds) and susceptibility to imidacloprid. Development of resistance to profenofos was observed in field populations of A. arizonensis. Exposure to lethal doses of imidacloprid and profenofos caused a reduction in parasitization (19-23%) and adult emergence (62-69%) of the parasitoid. Profenofos, thiodicarb and imidacloprid were found to be hazardous, non-selective and harmful to the endoparasitoid, A. arizonensis. There is an urgent need for optimizing insecticide applications for sustainable management of this invasive mealybug in cotton.


Assuntos
Hemípteros , Himenópteros , Inseticidas , Animais , Gossypium , Resistência a Inseticidas , Inseticidas/farmacologia , Neonicotinoides , Nitrocompostos , Organotiofosfatos , Tiocarbamatos
4.
Biochem Biophys Res Commun ; 631: 102-109, 2022 11 26.
Artigo em Inglês | MEDLINE | ID: mdl-36183550

RESUMO

Radiation-induced intestinal injury (RIII) is one of the most common abdominal and pelvic radiation therapy complications. RIII seriously affects the treatment and prognosis of cancer patients, and there are no effective interventions. Radiation can cause intestinal tissue damage, inflammatory cell infiltration, and pro-inflammatory cytokine release. We established an RIII mouse model by subjecting C57BL/6 mice to abdominal irradiation. Our results show that both pyroptosis and ferroptosis play a key role in RIII. VX-765 and Ferrostatin-1 (Fer-1) can inhibit these two types of programmed cell death and ameliorate RIII, respectively. Activation of the nuclear factor-κB (NF-κB) signaling pathway exacerbates the chemotaxis of inflammatory cells. In the present study, we hypothesized that the activation of NF-κB signaling pathway plays an important role in intestinal inflammatory injury. We demonstrated that the nuclear expression levels of the NF-κB subunit p65 increased after irradiation treatment. Reduced release of inflammatory factors and intestinal tissue damage was observed after pretreatment with pyrrolidinedithiocarbamate ammonium (PDTC). Moreover, after PDTC treatment, the indicators related to pyroptosis and ferroptosis were reversed. Collectively, these results suggest that the activation of the intestinal NF-κB signaling pathway may be associated with pyroptosis, ferroptosis, and subsequent intestinal injury after irradiation.


Assuntos
Compostos de Amônio , Ferroptose , Lesões por Radiação , Animais , Citocinas/farmacologia , Camundongos , Camundongos Endogâmicos C57BL , NF-kappa B/metabolismo , Prolina/análogos & derivados , Piroptose , Pirrolidinas , Tiocarbamatos
5.
J Agric Food Chem ; 70(40): 12796-12806, 2022 Oct 12.
Artigo em Inglês | MEDLINE | ID: mdl-36135711

RESUMO

Frequent and improper use of herbicides disrupts a plant's metabolism, causing oxidative stress that degrades crop quality. However, few studies have examined the inhibitory effects of herbicides on plant growth and defense mechanisms in terms of their impact on soil quality and crop rhizosphere. Therefore, the current study investigated the detrimental impacts of six typical and multilevel herbicides on the microbial community and signal molecules in the soil as well as on the levels of hormones and secondary metabolites in wheat seedlings. Interestingly, bensulfuron-methyl, terbutylazine (TBA), and 2,4-D butylate significantly induced oxidative damage while reducing the number of phytohormones (salicylic acid and jasmonic acid) and secondary metabolites (tricin, quercetin, and caffeic acid) in the roots and leaves compared with the controls, isoproturon, fenoxaprop-p-ethyl, and pretilachlor. At twice the recommended levels (2×), they also decreased the microbial α diversity and, in particular, the abundance of Gammaproteobacteria, Alphaproteobacteria, Actinobacteria, Bacteroidia, Verrucomicrobia, Bacilli, Acidimicrobiia, Deltaproteobacteria, and Gemmatimonadetes by disrupting the level of enzymes (e.g., urease and sucrase) and metabolites (indole-3-acetic acid, salicylic acid, apigenin, 4-hydroxybenzoic acid, DIMBOA, and melatonin) in the rhizosphere soil. Overall, significant exposure to herbicides may inhibit wheat growth by disturbing the microbial composition in the rhizosphere soil and the distribution of secondary metabolites in wheat seedlings.


Assuntos
Herbicidas , Melatonina , Ácido 2,4-Diclorofenoxiacético/metabolismo , Ácido 2,4-Diclorofenoxiacético/farmacologia , Apigenina/farmacologia , Herbicidas/metabolismo , Herbicidas/farmacologia , Melatonina/farmacologia , Reguladores de Crescimento de Plantas/metabolismo , Reguladores de Crescimento de Plantas/farmacologia , Raízes de Plantas/metabolismo , Quercetina/metabolismo , Rizosfera , Ácido Salicílico/metabolismo , Metabolismo Secundário , Plântula/metabolismo , Solo , Microbiologia do Solo , Sacarase/metabolismo , Tiocarbamatos , Triazinas , Triticum/metabolismo , Urease/metabolismo
6.
Sci Rep ; 12(1): 15502, 2022 09 15.
Artigo em Inglês | MEDLINE | ID: mdl-36109598

RESUMO

Gulosibacter molinativorax ON4T is the only known organism to produce molinate hydrolase (MolA), which catalyses the breakdown of the thiocarbamate herbicide into azepane-1-carboxylic acid (ACA) and ethanethiol. A combined genomic and transcriptomic strategy was used to fully characterize the strain ON4T genome, particularly the molA genetic environment, to identify the potential genes encoding ACA degradation enzymes. Genomic data revealed that molA is the only catabolic gene of a novel composite transposon (Tn6311), located in a novel low copy number plasmid (pARLON1) harbouring a putative T4SS of the class FATA. pARLON1 had an ANI value of 88.2% with contig 18 from Agrococcus casei LMG 22410T draft genome. Such results suggest that pARLON1 is related to genomic elements of other Actinobacteria, although Tn6311 was observed only in strain ON4T. Furthermore, genomic and transcriptomic data demonstrated that the genes involved in ACA degradation are chromosomal. Based on their overexpression when growing in the presence of molinate, the enzymes potentially involved in the heterocyclic ring breakdown were predicted. Among these, the activity of a protein related to caprolactone hydrolase was demonstrated using heterologous expression. However, further studies are needed to confirm the role of the other putative enzymes.


Assuntos
Actinomycetales , Herbicidas , Actinobacteria , Actinomycetales/genética , Azepinas , Herbicidas/metabolismo , Hidrolases/genética , Hidrolases/metabolismo , Tiocarbamatos
7.
Chem Commun (Camb) ; 58(77): 10865-10868, 2022 Sep 27.
Artigo em Inglês | MEDLINE | ID: mdl-36074776

RESUMO

Cobalt(III)-catalyzed thiocarbamate directed aminocarbonylation and amination of C-H bonds are described to access diverse amides. Biologically relevant pyrrolo[1,2-c]imidazoles were readily accessed via one-pot intramolecular cyclization at the thiocarbamoyl directing group. Notably, C-N amidation proceeded smoothly with an elusive catalyst TON of 250 for this Cp*Co(III)-catalysis. Broad scope, scalability, and easy removal of DG are other key features of these methods. The mechanisms of these C-H amidation reactions were proposed through control experiments and DFT calculations.


Assuntos
Pirróis , Tiocarbamatos , Amidas , Aminação , Catálise , Cobalto/química , Imidazóis , Estrutura Molecular , Pirróis/química
8.
Zhonghua Wei Zhong Bing Ji Jiu Yi Xue ; 34(8): 831-836, 2022 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-36177926

RESUMO

OBJECTIVE: To observe the effects of Xiaoqinglong Decoction and Qingqi Huatan Pills on interleukin-1ß (IL-1ß)-induced mucushypersecretion model of human airway epithelial H292 cellsand related molecules of nuclear factor-κB/microRNA-494(NF-κB/miR-494) signaling pathway, and to explore the mechanism of the two medicines in improving pathological airway mucus. METHODS: Methyl thiazolyl tetrazolium (MTT) colorimetric method was used to detect the effects of different concentrations of Xiaoqinglong Decoction and Qingqi Huatan Pills on the activity of H292 cellsinduced by IL-1ß, and the appropriate concentration was selected for subsequent experiments. Cells were randomly divided into blank group, IL-1ß model group (5 µg/L IL-1ß), NF-κB inhibitor pyrrolidinedithiocarbamate (PDTC) group (5 µg/L IL-1ß+100 µmol/L PDTC), Xiaoqinglong Decoction (5 µg/L IL-1ß+1 000 mg/L Xiaoqinglong Decoction) and Qingqi Huatan Pill group (5 µg/L IL-1ß+1 000 mg/L Qingqi Huatan Pills). 5 µg/L IL-1ß was used to induce H292 cells for 24 hours to establish a model of airway epithelial mucus hypersecretion. Enzyme linked immunosorbent assay (ELISA) method was used to detect the levels of mucin 5AC (MUC5AC), tumor necrosis factor-α (TNF-α) and IL-8 and the synthesis of intracellular MUC5AC and cystic fibrosis transmembrane conductance regulator (CFTR). Real-time quantitative polymerase chain reaction (RT-qPCR) was used to detect the expression levels of MUC5AC mRNA, CFTR mRNA, miR-494. Western blotting was used to detect protein expression of key proteins (p65) and NF-κB inhibitors (IκB) in NF-κB signaling pathway. RESULTS: Xiaoqinglong Decoction and Qingqi Huatan Pills with the concentration of 1 000 mg/L were selected for the follow-up experiment. Compared with the blank group, the levels of MUC5AC, TNF-α and IL-8 were significantly increased in the model group, intracellular MUC5AC protein content and mRNA expression were also significantly increased, intracellular CFTR protein content and mRNA expression were significantly decreased, and intracellular p65 protein expression was significantly up-regulated, the expression of IκB protein was significantly down-regulated, and the expression of miR-494 was significantly increased. Compared with the model group, the levels of MUC5AC, TNF-α and IL-8 were significantly reduced in PDTC group, Xiaoqinglong Decoction group and Qingqi Huatan Pill group, intracellular MUC5AC protein content and mRNA expression were also significantly decreased, and intracellular p65 protein expression was significantly down-regulated, and IκB protein expression was significantly up-regulated, miR-494 expression was significantly reduced. Intracellular CFTR protein content and mRNA expression were significantly increased in both PDTC group and Qingqi Huatan Pill group. Compared with the PDTC group, the level of TNF-α in the Xiaoqinglong Decoction group was significantly increased (ng/L: 22.77±3.14 vs. 11.09±3.37, P < 0.05),the content and mRNA expression of CFTR and IκB protein expression was significantly decreased [CFTR protein (ng/L): 97.38±6.62 vs. 227.04±19.48, CFTR mRNA (2-ΔΔCt): 0.99±0.08 vs. 1.21±0.08, IκB/ß-actin: 1.69±0.11 vs. 2.00±0.18, all P < 0.05], the level of TNF-α in Qingqi Huatan Pill group was significantly higher (ng/L: 19.08±3.71 vs. 11.09±3.37, P < 0.05). Compared with Xiaoqinglong Decoction group, the protein content and mRNA expression of CFTR and IκB protein expression in Qingqi Huatan Pill group were significantly increased [CFTR protein (ng/L): 235.01±22.71 vs. 97.38±6.62, CFTR mRNA (2-ΔΔCt): 1.32±0.15 vs. 0.99±0.08, IκB/ß-actin: 1.94±0.16 vs. 1.69±0.11, all P < 0.05]. CONCLUSIONS: The effect of Xiaoqinglong Decoctionin improving the hypersecretion of mucus in the airway epithelium may be related to the inhibition of NF-κB/miR-494 inflammatory signal-mediated MUC5AC hypersecretion, while the effect of Qingqi Huatan Pills may be related to the inhibition of NF-κB/miR-494 inflammatory signal-mediated MUC5AC hypersecretion and CFTR dysfunction. Therefore, the difference in the mechanism of the two treatments of airway pathological mucus is mainly in the regulation of CFTR mRNA and protein.


Assuntos
MicroRNAs , NF-kappa B , Actinas/metabolismo , Regulador de Condutância Transmembrana em Fibrose Cística/metabolismo , Humanos , Interleucina-1beta/metabolismo , Interleucina-8/metabolismo , MicroRNAs/metabolismo , Mucina-5AC/genética , Mucina-5AC/metabolismo , Muco/metabolismo , NF-kappa B/metabolismo , Prolina/análogos & derivados , RNA Mensageiro/metabolismo , Transdução de Sinais , Tiocarbamatos , Fator de Necrose Tumoral alfa/metabolismo
9.
J Org Chem ; 87(17): 11329-11349, 2022 09 02.
Artigo em Inglês | MEDLINE | ID: mdl-35968929

RESUMO

The reaction of the HCl or trifluoroacetic acid salts of primary amines with carbonyldiimidazole (CDI) is shown to be a preparatively useful method for forming monosubstituted carbamoylimidazoles (28 examples) without the formation of symmetrical urea side products. The utility of these air- and water-stable crystalline carbamoylimidazole reagents was demonstrated by their reactions as blocked or masked isocyanate equivalents. Reaction with various classes of nucleophiles provides access to useful functional groups including ureas, carbamates, thiocarbamates, hydantoins, and oxazolidinones. A parallel synthesis library of 30 ureas was generated by the reaction of 6× carbamoylimidazole intermediates with 5× amines and triethylamine. The unsymmetrical urea-containing natural products macaurea A and pygmaniline A were also prepared in good yields (95% over four steps and 79% over three steps, respectively) using this approach. The reaction of carbamoylimidazoles with amino acid methyl esters followed by microwave irradiation in aqueous media gives hydantoins in high yields, further demonstrating the ability of carbamoylimidazoles as isocyanate surrogates. Three hydantoin-containing natural products including macahydantoin D and meyeniihydantoin A were prepared in nearly quantitative yields from proline methyl ester and carbamoylimidazoles. The reaction of carbamoylimidazoles with alcohols and thiols under basic conditions affords carbamates and thiocarbamates, respectively, in good yields. Lastly, a method for the preparation of chiral oxazolidinone heterocycles from chiral epoxy alcohols is demonstrated using a double displacement approach. The reactions occur with high regio- and stereoselectivity (dr ≥ 15:1 by 1H NMR) via a domino attack of the corresponding alkoxides with carbamoylimidazoles followed by an intramolecular attack of the in situ generated urea anion at the proximal position of the epoxide group.


Assuntos
Produtos Biológicos , Hidantoínas , Oxazolidinonas , Álcoois/química , Aminas/química , Carbamatos/química , Isocianatos , Tiocarbamatos , Ureia/química
10.
J Hazard Mater ; 440: 129786, 2022 10 15.
Artigo em Inglês | MEDLINE | ID: mdl-36007363

RESUMO

Fusarium and phenolic acids in apple replant soil have deleterious effects on soil, which affects the growth of young replanted apple trees. Here, we studied the effects of different chemical fumigants (metham sodium, dazomet, calcium cyanamide, 1,3-dichloropropene, and methyl bromide) on Fusarium and phenolic acids in soil. The chemical fumigants disturbed the apple replant soil microbial community to different degrees in the order from highest to the lowest as methyl bromide > 1,3-dichloropropene > dazomet > metham sodium > calcium cyanamide. Compared with the control, the total numbers of Operational Taxonomic Unit (OTU) were 104.63 % and 9.38 % lower in the methyl bromide and calcium cyanamide treatments, respectively while the average contents of Fusarium were 88.04 % and 59.18% lower in these treatments, respectively. Higher disturbance degrees resulted in a slower recovery rate of the soil microbial community, which facilitated the transformation of the soil into a disease-suppressing state. During the recovery process, the roots recruited Streptomyces OTU2796 and Bacillus OTU2243, which alleviated Fusarium-induced stress via the synthesis of polyketones and macrolides. The roots also recruited Sphingomonas OTU3488, OTU5572, and OTU8147, which alleviated phenolic acid-induced stress through the degradation of benzoate and polycyclic aromatic hydrocarbons.


Assuntos
Fusarium , Malus , Microbiota , Praguicidas , Hidrocarbonetos Policíclicos Aromáticos , Compostos Alílicos , Cianamida , Hidrocarbonetos Bromados , Hidrocarbonetos Clorados , Hidroxibenzoatos , Macrolídeos , Praguicidas/química , Solo , Tiadiazinas , Tiocarbamatos
11.
Artigo em Inglês | MEDLINE | ID: mdl-35961533

RESUMO

Thiobencarb is a representative herbicide used on rice paddies. Because thiobencarb is used extensively on agricultural lands, especially on paddy fields, there is a high risk of unintended leaks into aquatic ecosystems. For this reason, several studies have investigated and reported on the toxicity of thiobencarb to aquatic species. In European eels, thiobencarb affected acetylcholinesterase levels in plasma and impaired adenosine triphosphatase activity in their gills. In medaka, thiobencarb-exposed embryos showed lower viability. However, molecular mechanisms underlying thiobencarb-mediated embryotoxicity have yet to be clarified. Therefore, the objective of our study was to investigate its mechanism of toxicity using zebrafish embryos. The viability of zebrafish embryos decreased upon exposure to thiobencarb and various phenotypic abnormalities were observed at concentrations lower than the lethal dose. The developmental toxicity of thiobencarb was mediated by pro-inflammatory cytokines (il1b, cxcl8, cxcl18b, and cox2a) and excessive generation of reactive oxygen species due to the downregulation of genes such as catalase, sod1, and sod2, which encode antioxidant enzymes. In addition, severe defects of the cardiovascular system were identified in response to thiobencarb exposure. Specifically, deformed cardiac looping, delayed common cardinal vein (CCV) regression, and interrupted dorsal aorta (DA)-posterior cardinal vein (PCV) segregation were observed. Our results provide an essential resource that demonstrates molecular mechanisms underlying the toxicity of thiobencarb on non-target organisms, which may contribute to the establishment of a mitigation strategy.


Assuntos
Sistema Cardiovascular , Poluentes Químicos da Água , Acetilcolinesterase , Animais , Apoptose , Ecossistema , Embrião não Mamífero , Inflamação/induzido quimicamente , Estresse Oxidativo/genética , Tiocarbamatos , Poluentes Químicos da Água/toxicidade , Peixe-Zebra
12.
Endocr Relat Cancer ; 29(11): 625-634, 2022 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-36040800

RESUMO

The prognosis of poorly differentiated thyroid carcinomas (PDTC) defined by the Turin criteria is variable. The aim of this study on 51 PDTC patients was to determine clinical, histological and molecular prognostic factors associated with recurrence in patients with localized disease at initial treatment and with overall survival in patients with distant metastases. Of 40 patients for whom next-generation sequencing (NGS) by ThyroSeq v3 was able to be performed on historical samples, we identified high-risk molecular signature (TERT, TP53 mutations) in 24 (60%) cases, intermediate risk signature in 9 (22.5%) cases and low-risk signature in 7 (17.5%) cases. Potentially actionable mutations were identified in 10% of cases. After a median follow-up of 57.5 months, recurrence occurred in 11 (39%) of the 28 patients with localized disease. The American Thyroid Association (ATA) high risk of relapse, high mitotic count, high molecular risk signature and CD163 expression were associated with recurrence (P = 0.009, 0.01, 0.049, 0.03 respectively). After a median follow-up of 49.5 months, thyroid cancer-related death occurred in 53% of the patients with distant metastases. There was no significant prognostic factor associated with death in univariate analysis. However, none of the patients with intermediate ATA risk of recurrence and none of the patients with low-risk molecular signature died from the disease. In addition, high molecular-risk signature was associated with the presence of synchronous or metachronous distant metastasis (P = 0.007) and with poor overall survival (P = 0.01). In conclusion, ATA risk of relapse and high mitotic count was associated with higher rate of recurrence in localized PDTC. High molecular-risk signature was associated with the presence of distant metastasis and poor overall survival. Further studies are needed to determine if molecular testing adds to ATA risk stratification or response to therapy in predicting outcomes.


Assuntos
Adenocarcinoma Folicular , Neoplasias da Glândula Tireoide , Adenocarcinoma Folicular/patologia , Humanos , Recidiva Local de Neoplasia/patologia , Prognóstico , Prolina/análogos & derivados , Estudos Retrospectivos , Tiocarbamatos , Neoplasias da Glândula Tireoide/patologia , Tireoidectomia
13.
Artigo em Inglês | MEDLINE | ID: mdl-35877692

RESUMO

Dithiocarbamates (DTCs) belong to a group of compounds used as fungicides in food production and can be divided into three major groups. Since DTCs easily oxidise and hydrolyse in alkaline and acidic medium respectively, precautions have to be implemented during preparation/homogenisation and extraction of samples. As such, test samples are commonly prepared individually by cutting into small pieces just before the digestion of DTCs with a hot acid to give carbon disulphide (CS2) and the results are expressed as CS2 without any differentiation of individual DTCs. However, individual DTCs have different toxicological potencies whilst their metabolites are more toxic than the parent compound. Apart from the hot digestion method, chromatographic separation of three major groups of DTCs has been developed by a number of different researchers. This review provides a comprehensive examination of sample preparation, extraction, clean-up and chromatographic methods for the determination of individual DTCs and their more toxic metabolites in foodstuffs. Moreover, this review also studies on how dietary exposure of DTCs can be efficiently and effectively estimated using different methods of analysis.


Assuntos
Dissulfeto de Carbono , Fungicidas Industriais , Exposição Dietética/análise , Alimentos , Fungicidas Industriais/análise , Tiocarbamatos/análise
14.
Cancer Chemother Pharmacol ; 90(2): 161-174, 2022 08.
Artigo em Inglês | MEDLINE | ID: mdl-35896839

RESUMO

PURPOSE: NSC 161128, a phenylurea thiocarbamate, displays activity against the NCI60 anti-cancer cell line panel and xenograft models. The metabolite N-methyl-N'-phenylurea (M10) has been detected in animal plasma; however, detection and quantification of other putative NSC 161128 metabolites have not been undertaken. The purpose of this study was to characterize the pharmacokinetics and metabolism of NSC 161128 in mice and under in vitro conditions. METHODS: An LC-MS/MS assay was developed to evaluate stability and in vitro metabolism of NSC 161128 in liver microsomes and S9 fractions. Single-dose pharmacokinetic profiles for NSC 161128 and its metabolite M10 were obtained following intraperitoneal (I.P.) administration. RESULTS: A sensitive and specific positive ionization LC-MS/MS method for measuring NSC 161128 and its metabolites was developed. HPLC separation was achieved under gradient elution using an aqueous methanol mobile phase containing 0.05% formic acid and 0.05% ammonium hydroxide. The assay was linear over the range 1.0-1000 ng/mL. NSC 161128 was stable in aqueous solution and tissue culture media, but not in plasma, where rapid degradation of NSC 161128 to the metabolite M10 was observed. Following I.P. administration of a 200 mg/kg dose to male CD1 mice, the peak plasma concentration of NSC 161128 was 255 ng/mL after 5 min with a plasma half-life of 138 min. Potential bioactivation of NSC 161128 was explored using mouse S9. CONCLUSIONS: An analytical LC-MS/MS method was successfully developed for the detection and quantification of NSC 161128 and its metabolites. These results increase the understanding of NSC 161128 pharmacokinetic and metabolic properties.


Assuntos
Espectrometria de Massas em Tandem , Tiocarbamatos , Animais , Cromatografia Líquida de Alta Pressão/métodos , Cromatografia Líquida/métodos , Meia-Vida , Humanos , Masculino , Camundongos , Reprodutibilidade dos Testes , Espectrometria de Massas em Tandem/métodos
15.
Water Sci Technol ; 85(9): 2682-2692, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35576261

RESUMO

The health problems caused by water pollution cannot be ignored, and the contribution of pesticides to water pollution has also become increasingly unignorable. The modified semi-coke as an adsorbent for reducing pesticide pollution to water was obtained from activated semi-coke which was modified by nitric acid (HNO3). The semi-coke was obtained by carbonization using 60 mesh walnut shell powder. After acid-base deashing, the semi-coke is dipped into zinc chloride (ZnCl2) solution to obtain activated semi-coke. Through BET analysis, the specific surface areas of semi-coke, activated semi-coke and modified semi-coke were 26.8 m2/g, 243.9 m2/g, and 339.6 m2/g respectively. An extremely high adsorption capacity of the adsorbents which is used to treat wastewater was achieved. The optimum adsorption conditions for modified semi-coke on thiodicarb solution were 30 mg/L of thiodicarb solution, adsorbent dosage of 0.01 g, adsorption temperature of 25 °C and adsorption time of 90 min. The optimum adsorption amount of 29.54 mg/gsor was achieved (sor is the abbreviation for sorbent). Moreover, through kinetics study, the result manifests that the modified semi-coke adsorption process is more fitted to the second-order kinetic model. This study provided a research implication theoretically for the treatment of pesticides in water.


Assuntos
Coque , Juglans , Praguicidas , Poluentes Químicos da Água , Adsorção , Carbono , Coque/análise , Cinética , Tiocarbamatos , Água , Poluentes Químicos da Água/análise
16.
Int J Mol Sci ; 23(6)2022 Mar 18.
Artigo em Inglês | MEDLINE | ID: mdl-35328726

RESUMO

Tricyclodecan-9-yl xanthogenate (D609) is a synthetic tricyclic compound possessing a xanthate group. This xanthogenate compound is known for its diverse pharmacological properties. Over the last three decades, many studies have reported the biological activities of D609, including antioxidant, antiapoptotic, anticholinergic, anti-tumor, anti-inflammatory, anti-viral, anti-proliferative, and neuroprotective activities. Its mechanism of action is extensively attributed to its ability to cause the competitive inhibition of phosphatidylcholine (PC)-specific phospholipase C (PC-PLC) and sphingomyelin synthase (SMS). The inhibition of PCPLC or SMS affects secondary messengers with a lipidic nature, i.e., 1,2-diacylglycerol (DAG) and ceramide. Various in vitro/in vivo studies suggest that PCPLC and SMS inhibition regulate the cell cycle, block cellular proliferation, and induce differentiation. D609 acts as a pro-inflammatory cytokine antagonist and diminishes Aß-stimulated toxicity. PCPLC enzymatic activity essentially requires Zn2+, and D609 might act as a potential chelator of Zn2+, thereby blocking PCPLC enzymatic activity. D609 also demonstrates promising results in reducing atherosclerotic plaque formation, post-stroke cerebral infarction, and cancer progression. The present compilation provides a comprehensive mechanistic insight into D609, including its chemistry, mechanism of action, and regulation of various pharmacological activities.


Assuntos
Hidrocarbonetos Aromáticos com Pontes , Tionas , Hidrocarbonetos Aromáticos com Pontes/farmacologia , Hidrocarbonetos Aromáticos com Pontes/uso terapêutico , Norbornanos , Tiocarbamatos , Tionas/farmacologia , Fosfolipases Tipo C/metabolismo
17.
J Tradit Chin Med ; 42(1): 49-57, 2022 02.
Artigo em Inglês | MEDLINE | ID: mdl-35322632

RESUMO

OBJECTIVE: To evaluate the therapeutic effectiveness of salidroside (Sal) and pyrrolidine dithiocarbamate (PDTC) against severe acute pancreatitis (SAP) in a rat model. METHODS: Rat models of SAP were established by retrograde infusion of sodium taurocholate solution. SAP rats were randomly divided into 6 groups: SAP 3 h group, SAP 24 h group, low-dose Sal treatment group (Sal L+S), middle-dose Sal treatment group (Sal M+S), high-dose Sal treatment group (Sal H+S) and PDTC treatment group (PDTC+S). The serum amylase, tumor necrosis factor-α (TNF-α), interleukin-1ß (IL-1ß) and interleukin-10 (IL-10) levels were determined by optical turbidimetry and enzyme-linked immunosorbent assay. The expression of Beclin-1, microtubule-associated protein light chain 3II (LC3 II ), lysosome associated membrane protein 2 (LAMP2), interleukin-1 receptor associated kinase 1 (IRAK1) inhibitor α of nuclear transcription factor-kB (IkBα), nuclear transcription factor-kB 65 (p65) in the pancreas tissues were detected by quantitative real-time polymerase chain reaction and Western blot, while the pIkBα and p-p65 levels were detected by Western blot. Pathological changes of the pancreas and all the other indexes were observed at 3 and 24 h after operation. RESULTS: The serum IL-10 level, IkBα and LAMP2 levels in Sal M+S, Sal H+S and PDTC+S groups were higher than those in SAP 24 h group, while all the other indexes in these three groups were all lower significantly than those in SAP 24 h group. There was no significant difference in all indexes between Sal H+S and PDTC+S groups. CONCLUSION: High-dose Sal has an effectively therapeutic effect on SAP in rats, which was similar to PDTC.


Assuntos
Pancreatite , Doença Aguda , Animais , Glucosídeos , Humanos , Interleucina-10/genética , NF-kappa B/genética , NF-kappa B/metabolismo , Pancreatite/tratamento farmacológico , Pancreatite/patologia , Fenóis , Pirrolidinas , Ratos , Ratos Sprague-Dawley , Tiocarbamatos , Fatores de Transcrição/uso terapêutico , Fator de Necrose Tumoral alfa/metabolismo
18.
Int J Mol Sci ; 23(3)2022 Jan 24.
Artigo em Inglês | MEDLINE | ID: mdl-35163241

RESUMO

Dithiocarbamate ligands have the ability to form stable complexes with transition metals, and this chelating ability has been utilized in numerous applications. The complexes have also been used to synthesize other useful compounds. Here, the up-to-date applications of dithiocarbamate ligands and complexes are extensively discussed. Some of these are their use as enzyme inhibitor and treatment of HIV and other diseases. The application as anticancer, antimicrobial, medical imaging and anti-inflammatory agents is examined. Moreover, the application in the industry as vulcanization accelerator, froth flotation collector, antifouling, coatings, lubricant additives and sensors is discussed. The various ways in which they have been employed in synthesis of other compounds are highlighted. Finally, the agricultural uses and remediation of heavy metals via dithiocarbamate compounds are comprehensively discussed.


Assuntos
Tiocarbamatos/química , Tiocarbamatos/síntese química , Elementos de Transição/química , Antibacterianos/farmacologia , Inibidores Enzimáticos , Humanos , Ligantes , Metais Pesados , Tiocarbamatos/farmacologia
19.
J Physiol Biochem ; 78(2): 355-363, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35048323

RESUMO

Glucose uptake is stimulated by insulin via stimulation of glucose transporter 4 (GLUT4) translocation to the plasma membrane from intracellular compartments in adipose tissue and muscles. Insulin stimulation for prolonged periods depletes GLUT4 protein, particularly in highly insulin-responsive GLUT4 storage vesicles. This depletion mainly occurs via H2O2-mediated retromer inhibition. However, the post-receptor mechanism of insulin activation of oxidative stress remains unknown. Here, we show that phosphatidylcholine-specific phospholipase C (PC-PLC) plays an important role in insulin-mediated downregulation of GLUT4. In the study, 3T3-L1 adipocytes were exposed to a PC-PLC inhibitor, tricyclodecan-9-yl-xanthogenate (D609), for 30 min prior to the stimulation with 500 nM insulin for 4 h, weakening the depletion of GLUT4. D609 also prevents insulin-driven H2O2 generation in 3T3-L1 adipocytes. Exogenous PC-PLC and its product, phosphocholine (PCho), also caused GLUT4 depletion and promoted H2O2 generation in 3T3-L1 adipocytes. Furthermore, insulin-mediated the increase in the cellular membrane PC-PLC activity was observed in Amplex Red assays. These results suggested that PC-PLC plays an important role in insulin-mediated downregulation of GLUT4 and that PCho may serve as a signaling molecule.


Assuntos
Transportador de Glucose Tipo 4 , Insulina , Norbornanos , Tiocarbamatos , Fosfolipases Tipo C , Células 3T3-L1 , Adipócitos/metabolismo , Animais , Regulação para Baixo , Glucose/metabolismo , Transportador de Glucose Tipo 4/metabolismo , Peróxido de Hidrogênio/metabolismo , Insulina/farmacologia , Camundongos , Norbornanos/farmacologia , Tiocarbamatos/farmacologia , Fosfolipases Tipo C/metabolismo
20.
FEMS Microbiol Lett ; 368(21-24)2022 02 12.
Artigo em Inglês | MEDLINE | ID: mdl-34994381

RESUMO

Thiobencarb is a herbicide globally used in the agricultural sector, and its extensive application leads to severe environmental pollution. In this study, the thiobencarb supplementation caused a significant shift in the bacterial community in the sediment slurry. An analysis of the degradation metabolites of microorganisms from the sediment indicated that deschlorothiobencarb, S-4-chlorobenzyl ethylthiocarbamate, 4-chlorobenzyl mercaptan, 4-chlorobenzyl alcohol, 4-chlorobenzoic acid and chlorobenzene were the main intermediates. The degradation rates were significantly enhanced using a horizontal-flow anaerobic reactor with immobilized cells in polyurethane foam. The degradation rates at 2.6, 12.9 and 25.6 mg L-1 concentrations by suspended microorganisms from the sediment in the mineral medium supplemented with glucose were 0.085 ± 0.000, 0.383 ± 0.010 and 0.500 ± 0.045 mg day-1, respectively. The corresponding data for degradation in the reactor were 2.54 ± 0.03, 11.69 ± 0.72 and 18.58 ± 1.83 mg day-1 at the sixth operation period. Moreover, COD removal efficiencies were >90% achieved in the reactor. The proposed method facilitates degradation using a horizontal-flow anaerobic immobilized biomass bioreactor. Moreover, this study reveals the degradation of metabolites of thiobencarb under anaerobic conditions.


Assuntos
Reatores Biológicos , Tiocarbamatos , Anaerobiose , Bactérias Anaeróbias/metabolismo , Biomassa , Reatores Biológicos/microbiologia , Tiocarbamatos/metabolismo
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