The effects of insecticides padan, bassa (carbamate) and acephate (OP) on P.ChE activity, MetHb rate and acid-base balance were determined in rabbits. The rabbits were treated by oral administration. Results: In the first group plasma cholinesterase (P.ChE) activity was significantly decreased while methemoglobin (MetHb) rate was significantly increased at 2h and 4h and returned to the before treatment at 24h. The rabbits were mixed alkalosis at 2h, respiratory alkalosis at 4h. In the second group P.ChE activity significantly decreased, MetHb rate significantly increased at 2h and 4h of treatment and then returned to the normal levels at 24h. The rabbits were mixed alkalosis at 2h, respiratory alkalosis at 4h. In the third group P.ChE activity significantly decreased, MetHb rate significantly increased at 3h and 6h and not returned to the before treatment at 24h. The rabbits have respiratory alkalosis at 3h, metabolic acidosis at 6h
Cholinesterases ; Acid-Base Equilibrium ; Therapeutics ; Thiocarbamates ; Organothiophosphorus Compounds

OBJECTIVETo establish a method for determining 2, 4-D butylate in serum by gas chromatography (GC)and to provide a basis for the diagnosis and treatment of clinical poisoning.

METHODSSerum 2, 4-D butylate level was determined by the following steps: mixing serum (0.5 ml)with trichloromethane (2.0 ml), adequately shaking for extraction, standing for 5 min, centrifuging at 4 000 rpm for 10 min, blow-drying the trichloromethane layer with nitrogen, adding ethanol (50 µl)to a certain volume, adding the sample (1.0 µl), and performing GC with a hydrogen flame ionization detector.

RESULTSSerum 2, 4-D butylate level showed a linear relationship within 5∼40 µg/ml, with a regression equation of y = 1 831.6.4x-899.4 (r = 0.999 2); the minimum detectable concentration was 1.0 µg/ml. The recovery rate was 88.7%∼103.0% (relative standard deviation (RSD) 3.8%∼5.0%). The intra-day RSD and inter-day RSD were 3.87-4.92% and 3.33%∼5.34%, respectively.

CONCLUSIONThis determination method is simple, efficient, and accurate and provides a good means for rapid diagnosis and treatment of 2, 4-D butylate poisoning.

Chromatography, Gas ; methods ; Humans ; Serum ; chemistry ; Thiocarbamates ; blood

Adult ; Delirium ; chemically induced ; Female ; Humans ; Thiocarbamates ; poisoning

BACKGROUND AND PURPOSE: Primary involvement of the peripheral nerves in myotonic dystrophy type I (MyD1) is controversial. We investigated whether the involvement of peripheral nerves is a primary event of MyD1 or secondary to another complication such as diabetes mellitus (DM). METHODS: The subjects comprised 12 patients with MyD1, 12 with DM and no peripheral nerve involvement, and 25 healthy volunteers. We measured multiple excitability indices in the median motor axons. The strength-duration time constant was calculated from the duration-charge curve, the threshold electrotonus and current-threshold relationships were calculated from the sequential subthreshold current, and the recovery cycle was derived from double suprathreshold stimulation. RESULTS: The depolarizing and hyperpolarizing threshold electrotonus were significantly reduced and exhibited increased refractoriness in the MyD1 group compared with the DM and control groups. The SDTC, superexcitability, and subexcitability were not significantly altered in the MyD1 group. CONCLUSIONS: The MyD1 group exhibited a depolarized axonal membrane potential. The significant differences in peripheral nerve excitability between the MyD1 group and the DM and normal control groups suggest that peripheral neuropathy is a primary event in MyD1 rather than a secondary complication of DM.
Axons ; Diabetes Mellitus ; Humans ; Membrane Potentials ; Myotonic Dystrophy ; Peripheral Nerves ; Peripheral Nervous System Diseases ; Sarcosine ; Thiocarbamates

Zinc released from excited glutamatergic neurons accelerates amyloid beta (A beta) aggregation, underscoring the therapeutic potential of zinc chelation for the treatment of Alzheimer's disease (AD). Zinc can also alter A beta concentration by affecting its degradation. In order to elucidate the possible role of zinc influx in secretase-processed A beta production, SH-SY5Y cells stably expressing amyloid precursor protein (APP) were treated with pyrrolidine dithiocarbamate (PDTC), a zinc ionophore, and the resultant changes in APP processing were examined. PDTC decreased A beta40 and A beta42 concentrations in culture media bathing APP-expressing SH-SY5Y cells. Measuring the levels of a series of C-terminal APP fragments generated by enzymatic cutting at different APP-cleavage sites showed that both beta- and alpha-cleavage of APP were inhibited by zinc influx. PDTC also interfered with the maturation of APP. PDTC, however, paradoxically increased the intracellular levels of A beta40. These results indicate that inhibition of secretase-mediated APP cleavage accounts -at least in part- for zinc inhibition of A beta secretion.
Alzheimer Disease ; Amyloid ; Baths ; Culture Media ; Neurons ; Proline ; Pyrrolidines ; Thiocarbamates ; Zinc

It has been reported that inflammatory diseases such as pneumonitis, retinitis, and hepatitis are associated with human cytomegalovirus (HCMV). Intercellular adhesion molecule (ICAM)-1 is an important inflammatory mediator, helping monocytes adhere to endothelial cells when tissues are infected by pathogen including the HCMV. However, little is known about the mechanism of ICAM-1 stimulation by the HCMV infection in monocytes. In this study, a monocytic cell line THP-1 was used to understand ICAM-1 expression by the HCMV infection. Flow cytometric analyses demonstrated that ICAM-1 was stimulated by the HCMV in THP-1 cells with maximum at 24 hours post infection. The stimulated ICAM-1 expression was dependent on the amount of input virus. In order to understand the mechanism of ICAM-1 stimulation during the HCMV infection, cells were treated with specific inhibitors of key elements in inflammation: NF-kappaB inhibitor PDTC, cyclooxygenase 2 inhibitor NS398, and MEK inhibitor PD98059. Flow cytometric analyses revealed that ICAM-1 expression was decreased when treated with PDTC, but not with NS398 or PD98059. Thus, it is suggested that HCMV-induced ICAM-1 expression in THP-1 cells is associates with NF-kappaB.
Cell Line ; Cyclooxygenase 2 ; Cytomegalovirus ; Endothelial Cells ; Flavonoids ; Hepatitis ; Humans ; Inflammation ; Intercellular Adhesion Molecule-1 ; Monocytes ; NF-kappa B ; Nitrobenzenes ; Pneumonia ; Proline ; Retinitis ; Sulfonamides ; Thiocarbamates ; Viruses

OBJECTIVETo assess the value of (99m)Tc-N-NOET ((99m)Tc-N-ethoxy-N-ethyl dithiocarbamato-nitrito) myocardial perfusion SPECT for the diagnosis of coronary artery disease.

METHODSA total of 42 patients [mean age (54 +/- 9) years, 35 men] with suspected chest pain were included in this study. 740 MBq of (99m)Tc-N-NOET was injected intravenously during bicycle exercise when the heart rate attained reached more than 85% of the expected maximum, or in cases of angina pectoris, severe arrhythmias and ischemic ST segment changes. (99m)Tc-N-NOET 740 MBq, SPECT myocardial imaging acquisitions were obtained at 15 minutes and 2 hours after (99m)Tc-N-NOET injection. Coronary angiography was performed in all patients.

RESULTSCoronary artery stenosis was detected in 26 patients and normal coronary angiography was shown in 16 patients. (99m)Tc-N-NOET myocardial perfusion imaging was abnormal in twenty-one patients out of the 26 patients with significant coronary artery stenosis (sensitivity, 81%); 14 out of 16 patients with normal angiography had a normal myocardial perfusion imaging (specificity, 88%). The positive predictive value, negative predictive value and predictive accuracy of (99m)Tc-N-NOET myocardial perfusion imaging for detection of CAD was 91%, 74% and 83%, respectively. The sensitivity of the imaging for detecting single vessel, double vessels and triple vessels disease were 60% (6/10), 86% (6/7) and 100% (9/9), respectively. There was mild (99m)Tc-N-NOET lung uptake in patients with coronary artery stenosis 15 minutes post (99m)Tc-N-NOET injection.

CONCLUSIONSPECT myocardial perfusion imaging with (99m)Tc-N-NOET supplied an important diagnostic tool for detecting coronary artery disease. Lung uptake with stress (99m)Tc-N-NOET might be related to coronary artery disease.

Adult ; Aged ; Coronary Artery Disease ; diagnostic imaging ; Exercise Test ; Female ; Humans ; Male ; Middle Aged ; Organotechnetium Compounds ; Thiocarbamates ; Tomography, Emission-Computed, Single-Photon

OBJECTIVETo investigate the expression of NF-kappaB in peripheral blood polymorphonuclear leukocyte (PMN) of acute pancreatitis (AP) and to assess the preventive effectiveness of pyrrolidine dithiocarbamate (PDTC) on NF-kappaB in vitro.

METHODSNineteen patients and 16 healthy individuals as control were enrolled in this study. The expression of NF-kappaB in PMNs was determined by gel electrophoretic mobility shift assay (EMSA). Routine clinical examination results and computed tomography findings of AP were recorded in all patients.

RESULTSThe PMNs from the patients with AP showed higher levels of NF-kappaB activities than those from control subjects (P < 0.01), severe acute pancreatitis (SAP) group showed much higher than mild acute pancreatitis (MAP) group (P < 0.05). In vitro, PDTC could reduce the NF-kappaB activity in PMNs of patients with AP, and its effectiveness at 2 mmol/L was stronger than at 1 mmol/L (P < 0.05). The PMNs from control subjects pretreated with 2 mmol/L PDTC before stimulation with the plasma from patients with SAP showed lower levels of NF-kappaB activities than did those untreated (P < 0.05).

CONCLUSIONThe NF-kappaB activation in peripheral blood PMNs participate in the course of acute pancreatitis and can be inhibited by PDTC in vitro.

Acute Disease ; Adult ; Aged ; Aged, 80 and over ; Female ; Humans ; Male ; Middle Aged ; NF-kappa B ; biosynthesis ; blood ; Neutrophils ; drug effects ; metabolism ; Pancreatitis ; metabolism ; Pyrrolidines ; pharmacology ; Thiocarbamates ; pharmacology

OBJECTIVETo study the safety, biodistribution, and dosimetry of myocardial perfusion imaging agent 99Tc(m)N-NOET in 10 healthy volunteers.

METHODS744-792 MBq of 99Tc(m)N-NOET was injected to each volunteer. Safety parameters and adverse event was measured in 24 hours of injection. Biodistribution was studied by whole-body imaging 1, 30 minutes, 1, 2, 4, 8, and 24 hours after the injection of 99Tc(m)N-NOET. The estimation of dosimetry was based on the standard medical internal radiation dose method using MIRDOSE 3.0 analysis program. Myocardial single photon emission computed tomography (SPECT) imaging was performed at 1 and 4 hours after injection.

RESULTSNo undesirable effects were reported by the subject during 24 hours after injection of 99Tc(m)N-NOET. No clinically significant changes were found in vital signs (heart rate, blood pressure, and electrocardiogram). No biochemical aspects and serology changes were measured. The myocardial SPECT imaging was clear. Cardiac uptake of 99Tc(m)N-NOET was as high as 2.68% at 2 hours after injection. The heart to lung ratio was more than 1 from 30 minutes after injection, reaching a maximum of 1.91 +/- 0.53 at 2 hours after injection. Radiation dosimetry calculations indicated an effective absorbed dose of 1.28 x 10(-5) Sv/MBq. The dosimetry in each main organ is lower then 50 mGy given 740 MBq of 99Tc(m)N-NOET in once imaging.

CONCLUSIONS99Tc(m)N-NOET exhibits high cardiac uptake and low estimated effective absorbed dose. It's a safe myocardial perfusion imaging agent.

Heart ; diagnostic imaging ; Humans ; Myocardium ; metabolism ; Organotechnetium Compounds ; adverse effects ; pharmacokinetics ; Radiation Dosage ; Radiopharmaceuticals ; adverse effects ; pharmacokinetics ; Thiocarbamates ; adverse effects ; pharmacokinetics ; Tissue Distribution ; Tomography, Emission-Computed, Single-Photon

Poorly differentiated thyroid cancer (PDTC) and anaplastic thyroid cancer (ATC) have poor prognosis and rare incidence compared to well differentiate thyroid cancer. Since the original description of PDTC in 1983, PDTC was introduced as a separate entity in the 2004 WHO Classification of Endocrine Tumors. PDTC was defined as a thyroid cancer with thyroglobulin-producing non-follicular non-papillary growth pattern and high-grade features, having an intermediate behavior between well differentiated thyroid cancer (WDTC) and ATC. But the criteria of PDTC are still controversial and heterogeneously applied in the diagnostic practice. Also the modalities of treatment, such as the extent of thyroid surgery, the use of radioiodine therapy and external radiation therapy are still controversial. ATC is rapidly progressing human carcinoma with a median survival of 4 to 12 months after diagnosis. Although the complete resection combined with external radiation therapy was reported to be effective recently and multimodality treatment has been recommended, current treatment of ATC has not been adequate for controlling the diseases. Therefore there are new attempts for treatment, such as chemotherapy with paclitaxel, clinical trials of combretastatin 4 phosphate and CS-7107 and multitargeted therapy of bevacizumab with doxorubicin, sorafenib, sunitinib etc. PDTC and ATC are an unexplored field like this, therefore, the studies for molecular pathology and therapeutic approach are necessary for improving survival and quality of life of patients.
Antibodies, Monoclonal, Humanized ; Bevacizumab ; Bibenzyls ; Doxorubicin ; Humans ; Incidence ; Indoles ; Niacinamide ; Paclitaxel ; Pathology, Molecular ; Phenylurea Compounds ; Prognosis ; Proline ; Pyrroles ; Quality of Life ; Thiocarbamates ; Thyroid Gland ; Thyroid Neoplasms