Twelve novel dithiocarbamates containing 1,2,3-trizaoles group were prepared via one step starting from organic halides, dithiocarbamic acid prop-2-ynyl ester, and sodium azide, using a very simple catalytic system co...Twelve novel dithiocarbamates containing 1,2,3-trizaoles group were prepared via one step starting from organic halides, dithiocarbamic acid prop-2-ynyl ester, and sodium azide, using a very simple catalytic system composed of copper（I） chloride and water at 70 8C. The structures of the new compounds were characterized and screened for their in vitro anti-tumor. Four of the compounds displayed varying levels of anti-tumor activity against the CDC25 B.展开更多
An eco-friendly and convenient method is developed herein for the synthesis of S-aryl dithiocarbamates via visible-light-induced SET process of an EDA complex between thianthrenium salt functionalized arenes and dithi...An eco-friendly and convenient method is developed herein for the synthesis of S-aryl dithiocarbamates via visible-light-induced SET process of an EDA complex between thianthrenium salt functionalized arenes and dithiocarbamate anions under mild aqueous micellar conditions.This strategy indirectly realizes the method for constructing S-aryl dithiocarbamates through site-selective C−H functionalization of arenes.Most importantly,the reaction proceeded smoothly without addition of any photocatalyst,and the by-product thianthrene is recycled in quantity,ultimately minimizing the production of chemical waste.This protocol provides a promising synthesis candidate for the construction of valuable S-aryl dithiocarbamates,which also opens up a new avenue for micellar photocatalysis.展开更多
The effectiveness of certain substituted dithiocarbamates in mobilizing lead from preexposed rats was investigated.The animals received 10mg Pb/kg/day, intragastrically.for 8 weeks and were treated thereafter with 400...The effectiveness of certain substituted dithiocarbamates in mobilizing lead from preexposed rats was investigated.The animals received 10mg Pb/kg/day, intragastrically.for 8 weeks and were treated thereafter with 400μmol/kg, intraperitoneally.of morpholine dithiocarbamate, tetraammonium ethylenediamine diacetic acid dithiocarbamate (EDDTC), ammonium diethanolamine dithiocarbamate (ADDTC), sodium diethyldithiocarbamate.N-benzyl-D-glucamine dithiocarbamate (NBGDTC), or dimercaptosuccinic acid, daily for 5 days.All the chelating agents were effective in lowering the hepatic and renal burden of Pb.ADDTC.EDDTC, and NBGDTC were also able to lower the long bone Pb content.The lowering of Pb burden had no relationship to restoration of Pb-induced hematopoietic alterations.The relatively lower lipophilicity of substituted dithiocarbamates, owing to the presence of hydrophilic groups, seems to be advantageous in preventing passage of metal chelale into the brain.None of the substituted dithiocarbamates caused excessive excretion of urinary Cu and Zn.ADDTC and EDDTC appear to be promising in the management of Pb poisoning. 1990 Academic Press.Inc.展开更多
A simple catalyst-free, and highly regioselective approach to 2-hydroxyalkyl dithiocarbamates is described which involves a one-pot reaction of various amines and carbon disulfide,CS2, with epoxides in ethanol at room...A simple catalyst-free, and highly regioselective approach to 2-hydroxyalkyl dithiocarbamates is described which involves a one-pot reaction of various amines and carbon disulfide,CS2, with epoxides in ethanol at room temperature.展开更多
This study reports the synthesis of metal complexes of mixed ligands p-Chlorophenyl-, p-Bromophenyl-dithiocarbamates. The spectral properties of the metal complexes [Zn(II), Cd(II), Hg(II), Cu(II), Co(II) and Ni(II)] ...This study reports the synthesis of metal complexes of mixed ligands p-Chlorophenyl-, p-Bromophenyl-dithiocarbamates. The spectral properties of the metal complexes [Zn(II), Cd(II), Hg(II), Cu(II), Co(II) and Ni(II)] were obtained using the FTIR and UV/Vis spectroscopic techniques. Their antibacterial studies revealed that these complexes as well as the ligands could serve as possible antibacterial agents against pathogens. Melting point and solubility measurements were also carried out. It was observed that these complexes were non-toxic, non-electrolytic and stable solids.展开更多
A new method for the preparation of dinuclear molybdenum dithiocarbamates(MoDDCs) is reported.This new method allows for the control of the amount of sulfurization of the Mo2SxO4-x core(x = 1 to 4) in the dinuclear Mo...A new method for the preparation of dinuclear molybdenum dithiocarbamates(MoDDCs) is reported.This new method allows for the control of the amount of sulfurization of the Mo2SxO4-x core(x = 1 to 4) in the dinuclear MoDDCs.This control assists in the tailoring of specific tribological properties of the MoDDCs in both greases and lubricating oils.展开更多
The in vitro antitumour efficacy of some novel metal complexes of piperazinedi thioformates （SR-M） was examined in six cancer cell lines. The activity was compared with that of piperazinedithioformates. Biological e...The in vitro antitumour efficacy of some novel metal complexes of piperazinedi thioformates （SR-M） was examined in six cancer cell lines. The activity was compared with that of piperazinedithioformates. Biological evaluations of a series of SR-M compounds suggest that the compounds 1 c （SR-Cu） and If （SR-Sn） show a potent antitumor activity. The stable conformation structure of SR-Cu as a representative of SR-M was investigated and confirmed by computer workshop.展开更多
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...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-1β(IL-1β)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(LC3Ⅱ),lysosome associated membrane protein 2(LAMP2),interleukin-1 receptor associated kinase 1(IRAK1),inhibitorαof nuclear transcription factor-κB(IκBα),nuclear transcription factor-κB 65(p65)in the pancreas tissues were detected by quantitative real-time polymerase chain reaction and Western blot,while the pIκBαand 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,IκBαand 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.展开更多
Produced water from polymer flooding is difficult to treat due to its high polymer concentration,high viscosity,and emulsified characteristics.The dithiocarbamate flocculant,DTC(T403),was prepared by the amine-termina...Produced water from polymer flooding is difficult to treat due to its high polymer concentration,high viscosity,and emulsified characteristics.The dithiocarbamate flocculant,DTC(T403),was prepared by the amine-terminated polyoxypropane-effier compound known as Jeffamine-T403.The product was characterized by IR spectra and elemental analysis.The DTC agent chelating with Fe2+produced a network polymer matrix,which captured and removed oil droplets efficiently.Oil removal by the flocculent on simulated produced water with 0,200,500,900 mg/L of partially hydrolyzed polyacrylamide(HPAM)was investigated for aspects of effectiveness of DTC(T403)dosage and concentrations of HPAM and Fe2+ions in the wastewater.Results showed that HPAM had a negative influence on oil removal efficiency when DTC(T403)dosage was lower than 20 mg/L.However,residual oil concentrations in tested samples with different concentrations of HPAM all decreased below 10 mg/L when DTC(T403)dosage reached 30 mg/L.The concentration of Fe2+in the initial wastewater had a slight effect on oil removal at the range of 2-12 mg/L.Results showed that Fe3+could not be used in place of Fe2+as Fe3+could not react with DTC under flocculated conditions.The effects of mineral salts ions were also investigated.展开更多
Objective:To investigate the effects of NF-κB inhibitor pyrrolidine dithiocarbamate hydrochloride(PDTC) on vascular endothelial growth factor(VEGF) and endostatin expression in mice with Lewis lung cance;and its mech...Objective:To investigate the effects of NF-κB inhibitor pyrrolidine dithiocarbamate hydrochloride(PDTC) on vascular endothelial growth factor(VEGF) and endostatin expression in mice with Lewis lung cance;and its mechanism.Methods:Mice survival rate and anti-tumor effects were observed in different concentrations of NF-κB inhibitor PDTC after the Lewis lung cancer mice model was established.VEGF and endostatin expressions were detected by immunohistochemical assay.Results:Lewis lung cancer was be inhibited by 0.5 mg/kg.1.5 mg/kg and 3.0 mg/kg of NF-κB inhibitor PDTC(P<0.05).Microvessel density(MVD) in 0.5 mg/kg.1.5 mg/kg and 3.0 mg/kg NF-κB inhibitor PDTC groups were significantly lower than the control group(P<0.05).Immunohistochemical assay results showed that VEGF and endostatin expressions in the 0.5 mg/kg.1.5 mg/kg and 3.0 mg/kg NF-κB inhibitor PDTC groups were significantly lower than the control group(P<0.05).Western blot results also showed that NF-κB inhibitor PDTC could inhibit VEGF and endostatin expressions in tumor tissues.Conclusions:NF-κB inhibitor PDTC can inhibit tumor formation and reduce tumor angiogenesis in mice with Lewis lung cancer;and its mechanism maybe associated to VEGF and endostatin down-regulation.展开更多
AIM: To evaluate the effect of pyrrolidine dithio- carbamate (PDTC; an NF-κB inhibitor) administered at low (50 mg/kg) and high (100 mg/kg) doses in suppressing colitis in mice with dextran sodium sulfate (DSS)-induc...AIM: To evaluate the effect of pyrrolidine dithio- carbamate (PDTC; an NF-κB inhibitor) administered at low (50 mg/kg) and high (100 mg/kg) doses in suppressing colitis in mice with dextran sodium sulfate (DSS)-induced colitis. METHODS: Mice were divided into a DSS-untreated group (normal group), DSS-treated control group, DSS+PDTC-treated groupⅠ(low-dose group), and DSS+PDTC-treated groupⅡ (high-dose group). In each group, the disease activity index score (DAI score), intestinal length, histological score, and the levels of activated NF-κB and inflammatory cytokines (IL-1β and TNF-α) in tissue were measured. RESULTS: The DSS+PDTC-treated groupⅡ exhibited suppression of shortening of intestinal length and reduction of DAI score. Activated NF-κB level and IL-1β and TNF-α levels were significantly lower in DSS+PDTC- treated groupⅡ. CONCLUSION: These findings suggest that PDTC is useful for the treatment of ulcerative colitis.展开更多
To find novel lead compound, seventy-four compound libraries were built through two rounds by a solution-phase CC on the basis of our developed method for the synthesis of dithiocarbamic acid ester. After evaluation f...To find novel lead compound, seventy-four compound libraries were built through two rounds by a solution-phase CC on the basis of our developed method for the synthesis of dithiocarbamic acid ester. After evaluation for the antitumor activities of libraries, six compounds were selected to be synthesized and examined their antitumor activities. It was found that compound 13 （HGWJ-11 C） with novel structure exhibited significant antitumor activities and the scaffold of dithiocarbamic acid was very crucial for the antitumor activity. The compound 13 is worth studying deeply as a potent hit compound.展开更多
Colorectal cancer （CRC） is one of the leading causes of cancer-related deaths, and inflammatory bowel diseases and dysregulated cell proliferation play important roles in colorectal carcinogenesis. Therefore, inhibi...Colorectal cancer （CRC） is one of the leading causes of cancer-related deaths, and inflammatory bowel diseases and dysregulated cell proliferation play important roles in colorectal carcinogenesis. Therefore, inhibition of inflammatory signaling and cell proliferation is used as a major strategy for chemoprevention of CRC. In the present study, it was found that IC5, a dithiocarbamate derivative, could inhibit the proliferation of LoVo human colon cancer cells in a concentration-dependent manner, with an IC50 of 22 gM. The anti-proliferation effect of IC5 was accompanied by a significant cell cycle arrest in G2/M phase. Further study revealed that IC5 significantly inhibited NF-~B signaling in LoVo cells, suggesting that IC5 could inhibit inflammatory responses. We then evaluated the in vivo efficacy of IC5 to inhibit colitis-associated colorectal carcinogenesis using an azoxymethane （AOM）/dextran sodium sulfate （DSS） mouse model. AOM/DSS treatment resulted in a CRC incidence of 58.3%, while the incidences were decreased to 37.5% and 25% in mice orally administered with 50 and 100 mg/kg IC5, respectively. In addition, IC5 also reduced the plasma levels of alanine aminotransferase and asparatate aminotransferase. Taken together, these results suggested that IC5 could prevent colitis-associated colorectal carcinogenesis, and more attention should be paid to it as a cancer chemopreventive agent in further investigation.展开更多
Compound 209 is a newly synthesized dithiocarbamate derivative with antiproliferation activity in vitro, however, its antitumor effect in vivo and the underlying mechanisms have yet to be identified. We explored the a...Compound 209 is a newly synthesized dithiocarbamate derivative with antiproliferation activity in vitro, however, its antitumor effect in vivo and the underlying mechanisms have yet to be identified. We explored the antitumor effect of compound 209 and the possible mechanisms for its inhibition of the growth of HT-29 xenograff tumor and proliferation of HT-29 cells. Cell proliferation was evaluated with SRB assay in vitro. The results showed that compound 209 had significant antiproliferation activity on HT-29 cells. Furthermore, the xenograff HT-29 nude mouse model was used to study the antitumor effect of compound 209 in vivo. We found that compound 209 significantly inhibited tumor growth and did not cause loss of body weight or leukocytopenia. Analysis by flow cytometry indicated that compound 209 arrested HT-29 cell cycle in G~ phase. Western blotting analysis suggested that compound 209 increased the expression of p27, cyclin E, CDK2, cyclin D1 and CDK4. These results demonstrated the antitumor effect of compound 209 and its potential use as an anticancer drug.展开更多
AIM: To explore the changes of nuclear factor-kappa B (NF-κB) DNA-binding activity, the expression of intercellular adhesion molecule-1(ICAM-1) regulated by IMF-κB at various times and to evaluate the effects of pyr...AIM: To explore the changes of nuclear factor-kappa B (NF-κB) DNA-binding activity, the expression of intercellular adhesion molecule-1(ICAM-1) regulated by IMF-κB at various times and to evaluate the effects of pyrrolidine dithiocarbamate (PDTC) on trinitrobenzene sulfonic acid (TNBS)-induced rat colitis. METHODS: TNBS of 0.6 mL was mixed with ethanol of 0.3 mL solution and instilled into the lumen of the rat colon. The rat models were divided into 6 groups, which were killed at 24 h, 3, 7,14, and 21 d after enema. Colonic inflammation and damage were assessed by macroscopical and histological criteria. Activity of NF-κB DNA-binding was analyzed by electrophoresis mobility shift assays (EMSA). Expression of ICAM-1 was detected by in situ hybridization (ISH) and immunohistochemistry (IH). Then various doses of PDTC were injected into rat abdomen 30 min before enema with TNBS/ethanol as pretreatment. The rats were killed 4 h after enema and the colonic inflammation, myeloperoxidase (MPO) activity, malondialdehyde (MDA) level, and DNA-binding activity of NF-κB were assessed. Finally, PDTC was injected intraperitoneally after colitis was induced. Changes of morphology were assayed. RESULTS: During the first week, hyperemia, hemorrhage, edema and ulceration of the colonic mucosa appeared with predominant infiltration of leukocytes. Neutrophils, macrophages, lymphocytes infiltrated in mucosa and submucosa 14 d later. Fibroblasts and granuloma-like structures were also obviously seen. The binding activity of NF-κB began to increase at 24 h time point and reached a peak at 14 d, then decreased but still was higher than control group at 21 d (P<0.01). Levels of ICAM-1 mRNA and protein significantly elevated at 24 h and the peak was at 21 d. Pretreatment with PDTC could attenuate the development of inflammation but not by reducing NF-KB activity. This attenuation of inflammation had a positive relationship with the dose of PDTC. PDTC at the dose of 100 mg/kg had no therapeutic effect after colitis was induced. CONCLUSION: NF-κB activation is an important event that may be involved in acute and chronic inflammation development and may contribute to self-protection against early inflammation damage. NF-κB also regulates ICAM-1 expression during colonic inflammation. Pretreatment of PDTC may attenuate the inflammation development. But PDTC has no therapeutic effect after the colitis is induced.展开更多
4-Methylpiperazine-l-carbodithioc-acid-3-cyano-3,3-diphenylpropyl ester hydrochloride（TM208）,a newly synthesized dithiocarbamate derivative,exhibits antitumor effect in vivo with low toxicity.However,the antitumor e...4-Methylpiperazine-l-carbodithioc-acid-3-cyano-3,3-diphenylpropyl ester hydrochloride（TM208）,a newly synthesized dithiocarbamate derivative,exhibits antitumor effect in vivo with low toxicity.However,the antitumor effect of TM208 in combination with drugs in clinical use for cytotoxic chemotherapy has not been identified.In our study,the antitumor effects and toxicities of TM208 in combination with cisplatin（DDP）,cyclophosphamide（CTX） and 5-fluorouracil（5-Fu）,respectively,were evaluated in vivo using a transplanted solid-type hepatocarcinoma H_（22） mice model.The results suggested that 5-Fu（5 mg/kg/2d） potentiated the antitumor effect of TM208（100 mg/kg/d） with significantly higher tumor inhibition rates（P0.01） and a slight elevation of toxicity;however,DDP and CTX in combination with TM208 did not exhibit similar enhanced antitumor effect.For further investigation,we found that the TM208 and 5-Fu combination therapy led to G_2/M cell cycle arrest of tumor cells in vivo by downregulating the protein expression of cyclin Bl,cdc2,cdk7,and upregulating the expression of p21 and p53.The protein expression levels of cyclin Dl and cyclin E were also downregulated in tumor cells treated with TM208 and 5-Fu,while those of cdk4 and cdk2 remained unchanged.The change of mRNA expression level of cdc2 was consistent with that of its protein in each group,while the mRNA expression of cyclin B1 remained unchanged among each group.These results demonstrated the dosage regimen of TM208 for combination therapy and could serve as evidence for clinical use of TM208 as an antineoplastic drug.展开更多
Objective:To study the effect of pyrrolidine dithiocarbamate(PDTC) on the anti-tuberculosis drug-induced liver injury and the molecular mechanism. Methods:Clean male SD rats were selected as experimental animals and r...Objective:To study the effect of pyrrolidine dithiocarbamate(PDTC) on the anti-tuberculosis drug-induced liver injury and the molecular mechanism. Methods:Clean male SD rats were selected as experimental animals and randomly divided into normal group,model group,PDTC group and AG490 group. Animal model of anti-tuberculosis drug-induced liver injury was established by intragastric administration isoniazid + rifampicin. PDTC group received intraperitoneal injection of PDTC,and AG490 group received intraperitoneal injection of AG490. Twenty-eight days after intervention,the rats were executed,and the liver injury indexes,inflammation indexes and oxidative stress indexes in serum as well as JAK2/STAT3 expression,liver injury indexes,inflammation indexes and oxidative stress indexes in liver tissue were determined. Results:p-JAK2,p-STAT3,TNF-α,IL-1β,IL-6,ROS,8-OHdG and MDA expression in liver tissue as well as TBIL,ALT,AST,γ-GT,TNF-α,IL-1β,IL-6,ROS,8-OHdG and MDA levels in serum of model group were significantly higher than those of normal group while p-JAK2,p-STAT3,TNF-α,IL-1β,IL-6,ROS,8-OHdG and MDA expression in liver tissu as well as TBIL,ALT,AST,γ-GT,TNF-α,IL-1β,IL-6,ROS,8-OHdG and MDA levels in serum of PDTC group and AG490 group were significantly lower than those of model group. Conclusions:PDTC can inhibit the inflammation and oxidative stress mediated by JAK2/STAT3 signaling pathway to alleviate the anti-tuberculosis drug-induced liver injury.展开更多
A novel method for the separation and reclamation of vanadium and chromium from acidic solution was proposed. The principle for the separation is based on selective complexation. In specific, V(V) can be complexated b...A novel method for the separation and reclamation of vanadium and chromium from acidic solution was proposed. The principle for the separation is based on selective complexation. In specific, V(V) can be complexated by dithiocarbamate to form VO(R1R2NCS2)3 precipitate, leaving Cr(Ⅲ) remained in the acidic solution. Then the reclamation of V and Cr from VO(R1R2NCS2)3 precipitate and Cr(Ⅲ)-bearing solution can be reached by decomplexation and neutralization, respectively. The kinetics of the complexation reaction was studied. In addition, the precipitation ratio of vanadium reached 97% and the loss of chromium was less than 4% after process optimization. The complexing agent could be regenerated with a high ratio of 99.5%. The method was successfully applied to treating chromium-vanadium-bearing slag produced in conventional vanadium production industry. Vanadium and chromium could be extracted from the slag in the form of calcium vanadate and Cr2O3 product with a purity of over 98%.展开更多
BACKGROUND: The nuclear translocation of transcription factors may be a critical factor in the intracellular pathway involved in ischemia/reperfusion(I/R) injury. The aim of the study was to evaluate the role of nucle...BACKGROUND: The nuclear translocation of transcription factors may be a critical factor in the intracellular pathway involved in ischemia/reperfusion(I/R) injury. The aim of the study was to evaluate the role of nuclear factor-kappa B (NF-κB) in the pathogenesis of liver injury induced by intestinal ischemia/reperfusion (IIR) and to investigate the effect of pyrrolidine dithiocarbamate (PDTC) on this liver injury. METHODS: Male Wistar rats were divided randomly into three experimental groups (8 rats in each): sham operation group (control group); intestinal/reperfusion group(I/R group): animals received 1-hour of intestinal ischemia and 2-hour reperfusion; and PDTC treatment group (PDTC group): animals that received I/R subject to PDTC treatment (100 mg/kg). The histological changes in the liver and intestine were observed, and the serum levels of tumor necrosis factor-α (TNF-α), alanine aminotransferase (ALT), aspartate aminotransferase (AST), liver superoxide dismutase (SOD), and nitrite/nitrate (NO) were measured. The immunohistochemical expression and Western blot analysis of liver NF-κB and intercellular adhesion molecule-1(ICAM-1) were observed. RESULTS: IIR induced liver injury characterized by the histological changes of liver edema, hemorrhage, polymorphonuclear neutrophil (PMN) infiltration, and elevated serum levels of AST and ALT. The serum TNF-α level was significantly higher than that of the control group(P<0.01) and a high level of liver oxidant product was observed (P<0.01). These changes were parallel to the positive expression of NF-κB and ICAM-1. After the administration of PDTC, the histological changes after liver injury were improved; the levels of SOD and NO in the liver were elevated and reduced, respectively (P<0.01). The expressions of ICAM-1 and NF-κB in the liver were weakened (P<0.01). CONCLUSION: NF-κB plays an important role in the pathogenesis of liver injury induced by HR. PDTC, an agent known to inhibit the activation of NF-κB, can reduce and prevent this injury.展开更多
Cloud point extraction (CPE) with Tergitol TMN-6 was applied for the extraction of trace amounts of palladium (Pd(Ⅱ)), platinum (Pt(Ⅳ)), and gold (Au(Ⅲ)) in the soil of industrial sewage. Ammonium pyrolysine dithio...Cloud point extraction (CPE) with Tergitol TMN-6 was applied for the extraction of trace amounts of palladium (Pd(Ⅱ)), platinum (Pt(Ⅳ)), and gold (Au(Ⅲ)) in the soil of industrial sewage. Ammonium pyrolysine dithiocarbamate (APDC) was adopted as the chelating agent prior to CPE and then was detected by atomic absorption spectrometry (AAS). Different parameters such as the concentration of surfactants, chelating agent and salt, sample pH, equilibration temperature and time, centrifugation time and rates, and the effect of foreign ions were studied. Under optimum conditions, the low limits of detections are 1.4, 2.8 and 1.2 ng·ml^-1 and the enrichment factors are 21, 12, and 24 for Pd(Ⅱ), Pt(Ⅳ), and Au(Ⅲ, respectively. The relative standard deviations vary from 0.6% to 1.0% (n=11). All correlation coefficients of the calibration curves are >0.9960. The proposed method was successfully applied for the determination of Pd(Ⅱ), Pt(Ⅳ), and Au(Ⅲ) in the real soil of industrial sewage samples.展开更多
基金the National Centre for Drug Screening,Shanghai,China,for evaluating the inhibitory activity against CDC25Bthe Fundamental Research Funds for the Central Universities,Southwest University for Nationalities(No.12NZYTH03)+1 种基金the Natural Science Foundation of Southwest University for Nationalities(No.381010)the Postgraduate Degree Construction Project of Southwest University for Nationalities(No.2013XWD-S0703)for financial support
文摘Twelve novel dithiocarbamates containing 1,2,3-trizaoles group were prepared via one step starting from organic halides, dithiocarbamic acid prop-2-ynyl ester, and sodium azide, using a very simple catalytic system composed of copper（I） chloride and water at 70 8C. The structures of the new compounds were characterized and screened for their in vitro anti-tumor. Four of the compounds displayed varying levels of anti-tumor activity against the CDC25 B.
基金supported by the National Natural Science Foundation of China(No.22271170)the Scientific Research Foundation of Qingdao University of Science and Technology。
文摘An eco-friendly and convenient method is developed herein for the synthesis of S-aryl dithiocarbamates via visible-light-induced SET process of an EDA complex between thianthrenium salt functionalized arenes and dithiocarbamate anions under mild aqueous micellar conditions.This strategy indirectly realizes the method for constructing S-aryl dithiocarbamates through site-selective C−H functionalization of arenes.Most importantly,the reaction proceeded smoothly without addition of any photocatalyst,and the by-product thianthrene is recycled in quantity,ultimately minimizing the production of chemical waste.This protocol provides a promising synthesis candidate for the construction of valuable S-aryl dithiocarbamates,which also opens up a new avenue for micellar photocatalysis.
文摘The effectiveness of certain substituted dithiocarbamates in mobilizing lead from preexposed rats was investigated.The animals received 10mg Pb/kg/day, intragastrically.for 8 weeks and were treated thereafter with 400μmol/kg, intraperitoneally.of morpholine dithiocarbamate, tetraammonium ethylenediamine diacetic acid dithiocarbamate (EDDTC), ammonium diethanolamine dithiocarbamate (ADDTC), sodium diethyldithiocarbamate.N-benzyl-D-glucamine dithiocarbamate (NBGDTC), or dimercaptosuccinic acid, daily for 5 days.All the chelating agents were effective in lowering the hepatic and renal burden of Pb.ADDTC.EDDTC, and NBGDTC were also able to lower the long bone Pb content.The lowering of Pb burden had no relationship to restoration of Pb-induced hematopoietic alterations.The relatively lower lipophilicity of substituted dithiocarbamates, owing to the presence of hydrophilic groups, seems to be advantageous in preventing passage of metal chelale into the brain.None of the substituted dithiocarbamates caused excessive excretion of urinary Cu and Zn.ADDTC and EDDTC appear to be promising in the management of Pb poisoning. 1990 Academic Press.Inc.
文摘A simple catalyst-free, and highly regioselective approach to 2-hydroxyalkyl dithiocarbamates is described which involves a one-pot reaction of various amines and carbon disulfide,CS2, with epoxides in ethanol at room temperature.
文摘This study reports the synthesis of metal complexes of mixed ligands p-Chlorophenyl-, p-Bromophenyl-dithiocarbamates. The spectral properties of the metal complexes [Zn(II), Cd(II), Hg(II), Cu(II), Co(II) and Ni(II)] were obtained using the FTIR and UV/Vis spectroscopic techniques. Their antibacterial studies revealed that these complexes as well as the ligands could serve as possible antibacterial agents against pathogens. Melting point and solubility measurements were also carried out. It was observed that these complexes were non-toxic, non-electrolytic and stable solids.
文摘A new method for the preparation of dinuclear molybdenum dithiocarbamates(MoDDCs) is reported.This new method allows for the control of the amount of sulfurization of the Mo2SxO4-x core(x = 1 to 4) in the dinuclear MoDDCs.This control assists in the tailoring of specific tribological properties of the MoDDCs in both greases and lubricating oils.
文摘The in vitro antitumour efficacy of some novel metal complexes of piperazinedi thioformates （SR-M） was examined in six cancer cell lines. The activity was compared with that of piperazinedithioformates. Biological evaluations of a series of SR-M compounds suggest that the compounds 1 c （SR-Cu） and If （SR-Sn） show a potent antitumor activity. The stable conformation structure of SR-Cu as a representative of SR-M was investigated and confirmed by computer workshop.
基金Supported by the Traditional Chinese Medicine Technology Development Plan Project of Jiangsu Province in 2020:Basic and Clinical Study on Salidroside in the Adjuvant Treatment of Severe Acute Pancreatitis(No.YB2020088)the Health Innovation Project of Lvyang Jinfeng Plan of Yangzhou City in 2020:Basic and Clinical Study on Salidroside in the Adjuvant Treatment of Severe Acute Pancreatitis(No.LJ202037)。
文摘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-1β(IL-1β)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(LC3Ⅱ),lysosome associated membrane protein 2(LAMP2),interleukin-1 receptor associated kinase 1(IRAK1),inhibitorαof nuclear transcription factor-κB(IκBα),nuclear transcription factor-κB 65(p65)in the pancreas tissues were detected by quantitative real-time polymerase chain reaction and Western blot,while the pIκBαand 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,IκBαand 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.
基金supported by the Scientific Technology Research and Development Program of Shandong,China(No. 2009GG10006003)
文摘Produced water from polymer flooding is difficult to treat due to its high polymer concentration,high viscosity,and emulsified characteristics.The dithiocarbamate flocculant,DTC(T403),was prepared by the amine-terminated polyoxypropane-effier compound known as Jeffamine-T403.The product was characterized by IR spectra and elemental analysis.The DTC agent chelating with Fe2+produced a network polymer matrix,which captured and removed oil droplets efficiently.Oil removal by the flocculent on simulated produced water with 0,200,500,900 mg/L of partially hydrolyzed polyacrylamide(HPAM)was investigated for aspects of effectiveness of DTC(T403)dosage and concentrations of HPAM and Fe2+ions in the wastewater.Results showed that HPAM had a negative influence on oil removal efficiency when DTC(T403)dosage was lower than 20 mg/L.However,residual oil concentrations in tested samples with different concentrations of HPAM all decreased below 10 mg/L when DTC(T403)dosage reached 30 mg/L.The concentration of Fe2+in the initial wastewater had a slight effect on oil removal at the range of 2-12 mg/L.Results showed that Fe3+could not be used in place of Fe2+as Fe3+could not react with DTC under flocculated conditions.The effects of mineral salts ions were also investigated.
基金supported by Natural Science Fund Project of Liaoning Province.No.:201102050
文摘Objective:To investigate the effects of NF-κB inhibitor pyrrolidine dithiocarbamate hydrochloride(PDTC) on vascular endothelial growth factor(VEGF) and endostatin expression in mice with Lewis lung cance;and its mechanism.Methods:Mice survival rate and anti-tumor effects were observed in different concentrations of NF-κB inhibitor PDTC after the Lewis lung cancer mice model was established.VEGF and endostatin expressions were detected by immunohistochemical assay.Results:Lewis lung cancer was be inhibited by 0.5 mg/kg.1.5 mg/kg and 3.0 mg/kg of NF-κB inhibitor PDTC(P<0.05).Microvessel density(MVD) in 0.5 mg/kg.1.5 mg/kg and 3.0 mg/kg NF-κB inhibitor PDTC groups were significantly lower than the control group(P<0.05).Immunohistochemical assay results showed that VEGF and endostatin expressions in the 0.5 mg/kg.1.5 mg/kg and 3.0 mg/kg NF-κB inhibitor PDTC groups were significantly lower than the control group(P<0.05).Western blot results also showed that NF-κB inhibitor PDTC could inhibit VEGF and endostatin expressions in tumor tissues.Conclusions:NF-κB inhibitor PDTC can inhibit tumor formation and reduce tumor angiogenesis in mice with Lewis lung cancer;and its mechanism maybe associated to VEGF and endostatin down-regulation.
文摘AIM: To evaluate the effect of pyrrolidine dithio- carbamate (PDTC; an NF-κB inhibitor) administered at low (50 mg/kg) and high (100 mg/kg) doses in suppressing colitis in mice with dextran sodium sulfate (DSS)-induced colitis. METHODS: Mice were divided into a DSS-untreated group (normal group), DSS-treated control group, DSS+PDTC-treated groupⅠ(low-dose group), and DSS+PDTC-treated groupⅡ (high-dose group). In each group, the disease activity index score (DAI score), intestinal length, histological score, and the levels of activated NF-κB and inflammatory cytokines (IL-1β and TNF-α) in tissue were measured. RESULTS: The DSS+PDTC-treated groupⅡ exhibited suppression of shortening of intestinal length and reduction of DAI score. Activated NF-κB level and IL-1β and TNF-α levels were significantly lower in DSS+PDTC- treated groupⅡ. CONCLUSION: These findings suggest that PDTC is useful for the treatment of ulcerative colitis.
基金National Natural Science Foundation of China(Grant No.21172011)
文摘To find novel lead compound, seventy-four compound libraries were built through two rounds by a solution-phase CC on the basis of our developed method for the synthesis of dithiocarbamic acid ester. After evaluation for the antitumor activities of libraries, six compounds were selected to be synthesized and examined their antitumor activities. It was found that compound 13 （HGWJ-11 C） with novel structure exhibited significant antitumor activities and the scaffold of dithiocarbamic acid was very crucial for the antitumor activity. The compound 13 is worth studying deeply as a potent hit compound.
基金National Natural Science Foundation(Grant No.81272468 and 21001011)the Scientific Research Foundation for the Returned Overseas Chinese Scholars,Ministry of Education
文摘Colorectal cancer （CRC） is one of the leading causes of cancer-related deaths, and inflammatory bowel diseases and dysregulated cell proliferation play important roles in colorectal carcinogenesis. Therefore, inhibition of inflammatory signaling and cell proliferation is used as a major strategy for chemoprevention of CRC. In the present study, it was found that IC5, a dithiocarbamate derivative, could inhibit the proliferation of LoVo human colon cancer cells in a concentration-dependent manner, with an IC50 of 22 gM. The anti-proliferation effect of IC5 was accompanied by a significant cell cycle arrest in G2/M phase. Further study revealed that IC5 significantly inhibited NF-~B signaling in LoVo cells, suggesting that IC5 could inhibit inflammatory responses. We then evaluated the in vivo efficacy of IC5 to inhibit colitis-associated colorectal carcinogenesis using an azoxymethane （AOM）/dextran sodium sulfate （DSS） mouse model. AOM/DSS treatment resulted in a CRC incidence of 58.3%, while the incidences were decreased to 37.5% and 25% in mice orally administered with 50 and 100 mg/kg IC5, respectively. In addition, IC5 also reduced the plasma levels of alanine aminotransferase and asparatate aminotransferase. Taken together, these results suggested that IC5 could prevent colitis-associated colorectal carcinogenesis, and more attention should be paid to it as a cancer chemopreventive agent in further investigation.
基金China International Science and Technology Cooperation Program for Key Projects (Grant No. 2008DFA31070)
文摘Compound 209 is a newly synthesized dithiocarbamate derivative with antiproliferation activity in vitro, however, its antitumor effect in vivo and the underlying mechanisms have yet to be identified. We explored the antitumor effect of compound 209 and the possible mechanisms for its inhibition of the growth of HT-29 xenograff tumor and proliferation of HT-29 cells. Cell proliferation was evaluated with SRB assay in vitro. The results showed that compound 209 had significant antiproliferation activity on HT-29 cells. Furthermore, the xenograff HT-29 nude mouse model was used to study the antitumor effect of compound 209 in vivo. We found that compound 209 significantly inhibited tumor growth and did not cause loss of body weight or leukocytopenia. Analysis by flow cytometry indicated that compound 209 arrested HT-29 cell cycle in G~ phase. Western blotting analysis suggested that compound 209 increased the expression of p27, cyclin E, CDK2, cyclin D1 and CDK4. These results demonstrated the antitumor effect of compound 209 and its potential use as an anticancer drug.
基金Supported by a Grant From Health Department Foundation of Guangdong Province, No. A2003554
文摘AIM: To explore the changes of nuclear factor-kappa B (NF-κB) DNA-binding activity, the expression of intercellular adhesion molecule-1(ICAM-1) regulated by IMF-κB at various times and to evaluate the effects of pyrrolidine dithiocarbamate (PDTC) on trinitrobenzene sulfonic acid (TNBS)-induced rat colitis. METHODS: TNBS of 0.6 mL was mixed with ethanol of 0.3 mL solution and instilled into the lumen of the rat colon. The rat models were divided into 6 groups, which were killed at 24 h, 3, 7,14, and 21 d after enema. Colonic inflammation and damage were assessed by macroscopical and histological criteria. Activity of NF-κB DNA-binding was analyzed by electrophoresis mobility shift assays (EMSA). Expression of ICAM-1 was detected by in situ hybridization (ISH) and immunohistochemistry (IH). Then various doses of PDTC were injected into rat abdomen 30 min before enema with TNBS/ethanol as pretreatment. The rats were killed 4 h after enema and the colonic inflammation, myeloperoxidase (MPO) activity, malondialdehyde (MDA) level, and DNA-binding activity of NF-κB were assessed. Finally, PDTC was injected intraperitoneally after colitis was induced. Changes of morphology were assayed. RESULTS: During the first week, hyperemia, hemorrhage, edema and ulceration of the colonic mucosa appeared with predominant infiltration of leukocytes. Neutrophils, macrophages, lymphocytes infiltrated in mucosa and submucosa 14 d later. Fibroblasts and granuloma-like structures were also obviously seen. The binding activity of NF-κB began to increase at 24 h time point and reached a peak at 14 d, then decreased but still was higher than control group at 21 d (P<0.01). Levels of ICAM-1 mRNA and protein significantly elevated at 24 h and the peak was at 21 d. Pretreatment with PDTC could attenuate the development of inflammation but not by reducing NF-KB activity. This attenuation of inflammation had a positive relationship with the dose of PDTC. PDTC at the dose of 100 mg/kg had no therapeutic effect after colitis was induced. CONCLUSION: NF-κB activation is an important event that may be involved in acute and chronic inflammation development and may contribute to self-protection against early inflammation damage. NF-κB also regulates ICAM-1 expression during colonic inflammation. Pretreatment of PDTC may attenuate the inflammation development. But PDTC has no therapeutic effect after the colitis is induced.
基金National High Technology Research and Development Program of China('863' Program,Grant No.2004AA2Z3783)National Natural Science Foundation(Grant No.20172006 and 20672009)
文摘4-Methylpiperazine-l-carbodithioc-acid-3-cyano-3,3-diphenylpropyl ester hydrochloride（TM208）,a newly synthesized dithiocarbamate derivative,exhibits antitumor effect in vivo with low toxicity.However,the antitumor effect of TM208 in combination with drugs in clinical use for cytotoxic chemotherapy has not been identified.In our study,the antitumor effects and toxicities of TM208 in combination with cisplatin（DDP）,cyclophosphamide（CTX） and 5-fluorouracil（5-Fu）,respectively,were evaluated in vivo using a transplanted solid-type hepatocarcinoma H_（22） mice model.The results suggested that 5-Fu（5 mg/kg/2d） potentiated the antitumor effect of TM208（100 mg/kg/d） with significantly higher tumor inhibition rates（P0.01） and a slight elevation of toxicity;however,DDP and CTX in combination with TM208 did not exhibit similar enhanced antitumor effect.For further investigation,we found that the TM208 and 5-Fu combination therapy led to G_2/M cell cycle arrest of tumor cells in vivo by downregulating the protein expression of cyclin Bl,cdc2,cdk7,and upregulating the expression of p21 and p53.The protein expression levels of cyclin Dl and cyclin E were also downregulated in tumor cells treated with TM208 and 5-Fu,while those of cdk4 and cdk2 remained unchanged.The change of mRNA expression level of cdc2 was consistent with that of its protein in each group,while the mRNA expression of cyclin B1 remained unchanged among each group.These results demonstrated the dosage regimen of TM208 for combination therapy and could serve as evidence for clinical use of TM208 as an antineoplastic drug.
基金supported by Surface Project of Shandong Provincial Natural Science Foundation(No.ZR2014HM081)
文摘Objective:To study the effect of pyrrolidine dithiocarbamate(PDTC) on the anti-tuberculosis drug-induced liver injury and the molecular mechanism. Methods:Clean male SD rats were selected as experimental animals and randomly divided into normal group,model group,PDTC group and AG490 group. Animal model of anti-tuberculosis drug-induced liver injury was established by intragastric administration isoniazid + rifampicin. PDTC group received intraperitoneal injection of PDTC,and AG490 group received intraperitoneal injection of AG490. Twenty-eight days after intervention,the rats were executed,and the liver injury indexes,inflammation indexes and oxidative stress indexes in serum as well as JAK2/STAT3 expression,liver injury indexes,inflammation indexes and oxidative stress indexes in liver tissue were determined. Results:p-JAK2,p-STAT3,TNF-α,IL-1β,IL-6,ROS,8-OHdG and MDA expression in liver tissue as well as TBIL,ALT,AST,γ-GT,TNF-α,IL-1β,IL-6,ROS,8-OHdG and MDA levels in serum of model group were significantly higher than those of normal group while p-JAK2,p-STAT3,TNF-α,IL-1β,IL-6,ROS,8-OHdG and MDA expression in liver tissu as well as TBIL,ALT,AST,γ-GT,TNF-α,IL-1β,IL-6,ROS,8-OHdG and MDA levels in serum of PDTC group and AG490 group were significantly lower than those of model group. Conclusions:PDTC can inhibit the inflammation and oxidative stress mediated by JAK2/STAT3 signaling pathway to alleviate the anti-tuberculosis drug-induced liver injury.
基金Project(51674230) supported by the National Natural Science Foundation of ChinaProject(2018YFC1900505) supported by the National Key R&D Program of China
文摘A novel method for the separation and reclamation of vanadium and chromium from acidic solution was proposed. The principle for the separation is based on selective complexation. In specific, V(V) can be complexated by dithiocarbamate to form VO(R1R2NCS2)3 precipitate, leaving Cr(Ⅲ) remained in the acidic solution. Then the reclamation of V and Cr from VO(R1R2NCS2)3 precipitate and Cr(Ⅲ)-bearing solution can be reached by decomplexation and neutralization, respectively. The kinetics of the complexation reaction was studied. In addition, the precipitation ratio of vanadium reached 97% and the loss of chromium was less than 4% after process optimization. The complexing agent could be regenerated with a high ratio of 99.5%. The method was successfully applied to treating chromium-vanadium-bearing slag produced in conventional vanadium production industry. Vanadium and chromium could be extracted from the slag in the form of calcium vanadate and Cr2O3 product with a purity of over 98%.
文摘BACKGROUND: The nuclear translocation of transcription factors may be a critical factor in the intracellular pathway involved in ischemia/reperfusion(I/R) injury. The aim of the study was to evaluate the role of nuclear factor-kappa B (NF-κB) in the pathogenesis of liver injury induced by intestinal ischemia/reperfusion (IIR) and to investigate the effect of pyrrolidine dithiocarbamate (PDTC) on this liver injury. METHODS: Male Wistar rats were divided randomly into three experimental groups (8 rats in each): sham operation group (control group); intestinal/reperfusion group(I/R group): animals received 1-hour of intestinal ischemia and 2-hour reperfusion; and PDTC treatment group (PDTC group): animals that received I/R subject to PDTC treatment (100 mg/kg). The histological changes in the liver and intestine were observed, and the serum levels of tumor necrosis factor-α (TNF-α), alanine aminotransferase (ALT), aspartate aminotransferase (AST), liver superoxide dismutase (SOD), and nitrite/nitrate (NO) were measured. The immunohistochemical expression and Western blot analysis of liver NF-κB and intercellular adhesion molecule-1(ICAM-1) were observed. RESULTS: IIR induced liver injury characterized by the histological changes of liver edema, hemorrhage, polymorphonuclear neutrophil (PMN) infiltration, and elevated serum levels of AST and ALT. The serum TNF-α level was significantly higher than that of the control group(P<0.01) and a high level of liver oxidant product was observed (P<0.01). These changes were parallel to the positive expression of NF-κB and ICAM-1. After the administration of PDTC, the histological changes after liver injury were improved; the levels of SOD and NO in the liver were elevated and reduced, respectively (P<0.01). The expressions of ICAM-1 and NF-κB in the liver were weakened (P<0.01). CONCLUSION: NF-κB plays an important role in the pathogenesis of liver injury induced by HR. PDTC, an agent known to inhibit the activation of NF-κB, can reduce and prevent this injury.
基金supported by the National Natural Science Foundation of China(No.20961012)the Medical Neurobiology Key Laboratory of Kunming University of Science and Technology,Basic and Applied Research Project in Yunnan Province(No.2008ZC082M)+3 种基金the Analysis and Testing Foundation of Kunming University of Science and Technology(No.2010121)Innovation Fund for Smalland Medium Technology Based Firms(No.11C26215305936)Natural and Science Foundation of Yunnan Province(No.2010ZC027)Focus Fund of Department of Education in Yunnan Province(No.2010Z016)
文摘Cloud point extraction (CPE) with Tergitol TMN-6 was applied for the extraction of trace amounts of palladium (Pd(Ⅱ)), platinum (Pt(Ⅳ)), and gold (Au(Ⅲ)) in the soil of industrial sewage. Ammonium pyrolysine dithiocarbamate (APDC) was adopted as the chelating agent prior to CPE and then was detected by atomic absorption spectrometry (AAS). Different parameters such as the concentration of surfactants, chelating agent and salt, sample pH, equilibration temperature and time, centrifugation time and rates, and the effect of foreign ions were studied. Under optimum conditions, the low limits of detections are 1.4, 2.8 and 1.2 ng·ml^-1 and the enrichment factors are 21, 12, and 24 for Pd(Ⅱ), Pt(Ⅳ), and Au(Ⅲ, respectively. The relative standard deviations vary from 0.6% to 1.0% (n=11). All correlation coefficients of the calibration curves are >0.9960. The proposed method was successfully applied for the determination of Pd(Ⅱ), Pt(Ⅳ), and Au(Ⅲ) in the real soil of industrial sewage samples.
