Pyrrolidine Dithiocarbamate (PDTC) Attenuates Luteolin-Induced Apoptosis in Human Leukemia HL-60 Cells

Studies have indicated that flavonoid luteolin is a potential inhibitor of tumor cell proliferation and may function as an anticarcinogenic agent. Pyrrolidine dithiocarbamate (PDTC), a synthetic compound, may exhibit biphasic effects on apoptosis depending on the experimental context. Previously, we found that luteolin induced the activation of the proapoptotic proteins, such as Bad, Bid, and Bax, in HL-60 human leukemia cells. We also explored the modulatory effects and molecular mechanisms of PDTC on the cytotoxicity of luteolin in HL-60 cells;PDTC could interfere with luteolin’s ability to cleave poly(ADP-ribose)-polymerase (PARP) and DNA fragmentation of factor-45 (DFF-45). In the current study, we further investigated the effect of PDTC on the luteolin-induced death-receptor pathway and the cleavage of the Bcl-2 family members. We found that the combination of luteolin and PDTC increased the survival of the HL-60 cells such that PDTC inhibited both extrinsic and intrinsic pathways in luteolin-induced apoptosis.

Pyrrolidine dithiocarbamate alleviates the anti-tuberculosis drug-induced liver injury through JAK2/STAT3 signaling pathway:An experimental study

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.

Protective effect of pyrrolidine dithiocarbamate on liver injury induced by intestinal ischemia-reperfusion in rats

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.

基于滑模控制的永磁同步电动机DTC仿真研究

针对传统永磁同步电动机(PMSM)直接转矩控制(DTC)中转矩和磁链脉动大的问题,在转矩和磁链控制中引入超螺旋滑模变结构,并采用基于莱维飞行的改进粒子群(PSO)算法对其可调参数优化整定。为加快系统动态响应速度,采用速度滑模控制器代替传统PI调节器。使用Matlab/Simulink对引入滑模变结构的DTC系统进行了仿真研究,分别对空载和带载条件下的转速、转矩以及磁链进行分析。仿真结果表明,滑模变结构的引入可有效抑制转矩和磁链脉动,降低转速超调,缩短过渡时间。仿真研究有助于学生更好地理解与应用滑模理论,并增强学生理论结合实际与自主创新意识。

Activation of nuclear factor-kappa B and effects of pyrrolidine dithiocarbamate on TNBS-induced rat colitis

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.

Evaluation of the effect of pyrrolidine dithiocarbamate in suppressing inflammation in mice with dextran sodium sulfate-induced colitis

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.

Complexation separation for vanadium and chromium by dithiocarbamate and its application in treatment of chromium-vanadium-bearing slag

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%.

数字化背景下,基于DTC独立站的品牌出海路径研究

当下,在数字经济与数字化技术的助力下,我国跨境企业面临难得的出海机遇。本文以S公司依托DTC独立站模式开展品牌出 海的成功经验为例,分析了数字化技术助力其品牌出海的机理与路径,最后提出了通过DTC模式进行品牌出海的几点启示。

Pyrrolidine dithiocarbamate and saxagliptin ameliorate ulcerative colitis in rats

Objective: To evaluate the antioxidant, immunomodulatory and anti-inflammatory activities of pyrrolidine dithiocarbamate and saxagliptin in rats with thioacetamide-induced ulcerative colitis. Methods: Animals were orally administered with a vehicle, sulfasalazine(500 mg/kg), pyrrolidine dithiocarbamate(100 mg/kg), and saxagliptin(10 mg/kg) for two weeks. Ulcerative colitis was induced by a single intrarectal instillation of thioacetamide on day 8. Colon samples were collected to assess mitogen-activated protein kinase(MAPK), phosphorylated extracellular signal-regulated kinase(ERK), c AMP response element-binding protein(CREB), interleukin-12(IL-12), caspase-3, β-defensin, inducible nitric oxide synthase(i NOS) and glucagon like peptide-1(GLP-1). Moreover, histopathological examination was performed. Results: Rats treated with thioacetamide caused increases in colonic MAPK, phosphorylated ERK, CREB, caspase-3, IL-12, β-defensin, i NOS, as well as decreases in body weight and GLP-1. In addition, distortion of colonic structure was found by histopathological examination. Pyrrolidine dithiocarbamate and saxagliptin mitigated colitis severity by improving body weight decrease and GLP-1, and reducing colonic MAPK, phosphorylated ERK, CREB, caspase-3, IL-12, β-defensin and i NOS. Conclusions: Pyrrolidine dithiocarbamate and saxagliptin are efficient against thioacetamide induced colitis through improving inflammatory and oxidative changes.

A Device for Rapid Detection of Dithiocarbamate Pesticide Residues in Fruits

Based on the chemical properties of dithiocarbamate pesticides,a device for rapid detection was developed in the paper,and the experimental conditions were optimized. Dithiocarbamate residues in fruits were successfully detected using molecular absorption spectro-photometry,and the recovery rate was over 80%.The rapid detection method was simple to operate with low cost,and was conducive to application in basic level and enterprise laboratories.

集成DTC的埋入硅桥式扇出型封装的去耦设计

对于供电网络面临的电源完整性挑战,采用一种集成深槽电容(DTC)的埋入硅桥式扇出型封装结构,以改善其供电性能。介绍了硅桥芯片和DTC的制作工艺以及DTC与埋入硅桥芯片的连接方式,并对硅桥芯片、DTC分别进行仿真,以验证DTC的去耦效果。进一步研究了集成DTC的埋入硅桥式扇出型封装、在基板背贴硅电容的扇出型封装和无去耦电容的扇出型封装3种方案对电源分配网络(PDN)阻抗的去耦效果。通过对比3种方案的仿真结果,发现埋入硅桥式扇出型封装结构的自阻抗值和转移阻抗值较在基板背贴硅电容的扇出型封装结构分别低74%和95%,较无去耦电容的扇出型封装结构分别低91%和97%。

Synthesis and Structure of a Ruthenium(Ⅱ)-dithiocarbamate Complex [RuH(CO)(PPh_3)_2(4-ClPhNHCS_2)]·C_6H_(14)

The title complex [RuH（CO）（PPh3）2（4-ClPhNHCS2）]·C6H14 has been prepared and characterized by X-ray diffraction analysis.It crystallizes in the triclinic system,space group P1 with a = 11.0817（2）,b = 14.3889（2）,c = 15.2136（2） ,α = 71.018（1）,β = 74.911（1）,γ = 85.146（1）°,V = 2214.86（6） 3,Z = 2,Mr = 900.4,Dc = 1.350 g/cm3,Mr = 900.40,μ（MoKα） = 0.616 mm-1,F（000） = 926,S = 1.016,the final R = 0.0478 and wR = 0.0947 for 6828 observed reflections with I 2σ（I） and 505 variables.The molecular structure of 1 consists of one neutral complex [RuH（CO）（PPh3）2（4-ClPhNHCS2）] and one hexane solvent molecule.The geometry around ruthenium is pseudo-octahedral with two trans-binding PPh3 ligands and one chelating bidentate 4-ClPhNHCS2- ligand via two sulfur atoms.The average Ru-S,Ru-P and Ru-H bond lengths are 2.4824（8）,2.3495（8） and 1.71（2）,respectively.The electrochemical properties of 1 have been studied in CH2Cl2 solution by cyclic voltammetry.

Syntheses,Characterization and Crystal Structures of Dithiocarbamate-based Mononuclear Palladium(Ⅱ) Complexes

By employing the dithiocarbamate salt （K（PPDC）, where PPDC = 4？-pyridyl-1-pipe-razine-4-dithiocarbamate） as the functional ligand and di-palladium complexes [（N^N）2Pd2（NO3ˉ）2]（NO3ˉ）2 （N^N = 2,2＇-bipyridine, bpy; 4,4＇-dimethylbipyridine, dmbpy） as corner, two novel single metal complexes with Pd（II） centers have been obtained. These organic-metal complexes were characterized by NMR, ESI-MS, elemental analysis, Uv-vis spectra and single-crystal X-ray diffraction analysis. Compound 1？（PF6）2 （[（bpy）Pd（PPDC）]·（PF6）2） crystallizes in triclinic, space group P , a = 8.3968（5）, b = 11.5565（7）, c = 18.2234（11）, α = 97.505（1）, β = 91.424（1）, γ = 106.146（1）o, C22H24N6S2P2F12Pd, Mr = 832.93, V = 1680.58（18） ？3, Z = 2, Dc = 1.646 Mg/m3, μ（MoKα） = 0.863 mm-1, F（000） = 828, the final R = 0.0455 and wR = 0.1390 for 6981 observed reflections with I 〉 2σ（I）. Similarly, compound 2？（PF6）2 （[（dmbpy）Pd（PPDC）]·（PF6）2） also crystallizes in triclinic, space group P , a = 13.9467（3）, b = 14.8390（2）, c = 17.0632（3） ？, α = 81.8680（10）, β = 87.051（2）, γ = 83.4590（10）o, C22H25N5S2P2F12Pd, Mr = 819.93, V = 3470.81（11） ？3, Z = 4, Dc = 1.569 Mg/m3, μ（CuKα） = 7.115 mm-1, F（000） = 1632, the final R = 0.0606 and wR = 0.1637 for 12835 observed reflections with I 〉 2σ（I）. Crystallography reveals that each metal center coordinates with two N atoms from bpy and two S atoms from PPDC in the square coordination mode. In the crystal structure of complex 1, a weak Pd……Pd interaction can be observed. Interestingly, it was also found that the mononuclear moieties of complex 2 could be packed into a 3-D porous framework via multiple intermolecular C–F……H hydrogen-boding interactions which extended in the a, b, and c axes with PF6ˉ anions frozen inside.

Synthesis, Crystal Structure and Antibacterial Activity of Dibenzyl Dithiocarbamate Bismuth Complex

A new complex, {Bi(Ⅲ)[S2CN(CH2C6H5)2]3}2·2CH3CN, was synthesized and characterized by elemental analysis, IR, TG, 1H NMR and X-ray single-crystal diffraction. The complex crystallizes in the triclinic system, space group P1, with a = 12.705(6), b = 13.430(6), c = 15.489(12) , α = 102.135(12), β = 99.649(12), γ = 111.521(9)°, Z = 1, V = 2315(2) A3, Dc = 1.531 g·cm-3, F(000) = 1068, μ = 4.116 mm-1, the final R = 0.0559, w R = 0.1069 and S =1.056. The coordinated geometry of Bi(Ⅲ) with six sulfur atoms from three ligands is a distorted pentagonal pyramidal configuration, and the structural system is formed by weak interactions of Bi···S between two molecules. The complex was valued for its antibacterial activity by agar-streak method. It was found that the complex is weakly active against three of the five tested bacterial organisms.

Synthesis and Crystal Structure of a Molybdenum Carbonyl Compound with Thiolate and Dithiocarbamate Ligands, [Bu_4N][(OC)_4Mo(μ-SC_6H_5)_2Mo(C_5H_(10)CNS_2)(CO)_2]

A di-molybdenum carbonyl compound containing thiolate and dithiocarbamate ligands, [Bu4N][（CO）4Mo（μ-SC6H5）2Mo（C5H10dtc）（CO）2] 1 （CsH10dtc = S2CNC5H10）, has been prepared by reaction of [Mo2（SC6H5）2（CO）8] with C5H10dtcNa and [NBu4]Br in acetone. It crystallizes in monoclinic, space group P21/n with a = 13.162（3）, b = 17.466（2）, c = 20.453（4） A,β= 100.77（1）°, Z = 4, V= 4619（2）A^3, C40H56Mo2N2O6S4, Mr = 980.95, De= 1.389 g/cm^3,μ = 7.66 cm^-1, F（000） = 1988 and R = 0.0746 for 5161 observed reflections with I 〉 2σ（I）. The complex contains a [Mo2S2]^2- planar core in which one Mo atom is chelated by a C5H10dtc ligand, leading to different coordination environments of the two Mo atoms. 95Mo NMR measurement indicates that the two Mo atoms are in different oxidation states.

Syntheses, Crystal Structures and Anticancer Activities of Dithiocarbamate Bismuth(Ⅲ) Complexes

Two novel complexes, [Bi（III）（S2CNBn Et）3] 1 and [Bi（III）（S2CNPPPy-2）3] 2, were synthesized and characterized by elemental analysis, IR, ^1H NMR, ^13C NMR, TG-DTG and X-ray single-crystal diffraction. The structure reveals that complex 1 belongs to the monoclinic system, space group P21/c with a = 11.457（5）, b = 17.437（8）, c = 33.439（14）, β= 98.499（8）o, Z = 4, V = 6607（5）3, Dc = 1.689 g·cm^-3, F（000） = 3328, μ= 5.742 mm^-1, the final R = 0.0906, w R = 0.1678 and S = 1.032. The structure indicates that complex 2 belongs to the triclinic system, space group P1 with a = 12.608（9）, b = 12.622（8）, c = 12.49（6）, α = 102.652（15）, β = 103.013（14）, γ = 109.698（10）o, Z = 1, V = 1762.3（19）3, Dc = 1.741 g·cm^-3, F（000） = 916, μ = 5.395 mm^-1, the final R = 0.048 2, w R = 0.1206 and S =1.046. In the two complexes, each six-coordinated Bi（III） atom adopts a pentagonal pyramidal configuration with six sulfur atoms from three ligands, and the dimmer structures are formed by weak interactions of Bi···S between two molecules. The anticancer activities of the two complexes were studied by evaluating their cytotoxicities against several human cancer cell lines using the MTT assay. Results indicated complex 2 showed moderate cytotoxic effects on the selected cancer cells.

Molybdenum Dithiocarbamates:A New Approach to "Old" Technology

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.

A Facile and Efficient One-Pot Regioselective Synthesis of 2-Hydroxyalkyl Dithiocarbamates under Catalyst-Free Conditions

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.

Synthesis, Characterization and Antimicrobial Activities of Sulfadiazine Schiff Base and Phenyl Dithiocarbamate Mixed Ligand Metal Complexes

Sulfadiazine Schiff base and Phenyl dithiocarbamate mixed ligand metal complexes have been synthesized and characterized. The characterization of metal complexes is based on the results of the solubility, colour, melting points and elemental analysis as well as the spectroscopic studies. The results obtained from the spectroscopic spectra revealed from the UV-visible showed the presence of chromophoric groups while the FTIR results confirmed that the metals coordinated through the two nitrogen atoms of Sulfadiazine Schiff base and sulphur atom of the N-phenyl dithiocarbamate. Also the antimicrobial activities of the metal complexes proved that the metal complexes are more active than the parent ligands.

The Lead-Chelating Effects of Substituted Dithiocarbamates

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.