CAS Number: 62-56-6. Data sources include IBM Watson Micromedex (updated 2 Nov 2020), Cerner Multum™ (updated 2 Nov 2020), … The mixture was gradually acidified to pH 3.0 with HCl and extracted twice with n-hexane. Cells were harvested and washed once in 50 mm MOPS buffer, pH 8. Only the supernatant allowed the conversion of stearoyl-CoA to the oleic acid derivative in the presence of atmospheric On the other hand, a weak mutagenic effect of thiourea has been found in the host‐mediated assay [9], a mutagenic effect, the induction of unscheduled DNA synthesis, in V79 cells [83], and the induction of DNA single strand breaks in hepatocytes [86]. A dose of 25–70 mg daily was recommended for the subsequent continuous therapy for which 10–15 mg were ineffective [8]. with 1 ml of 15% tetrabutylammonium hydroxide. documented (1). Comparative Effects of ISO and the Known Δ9 Desaturase Inhibitor, Sterculic Acid—The naturally occurring cyclopropene fatty acid, sterculic acid (9,10-cyclopropenoid acid), is a potent and specific inhibitor It was approved by the US Food and Drug Administration in 1947. GC-RAM radio detector under conditions that resolve only the FAMEs. of urea-based products as inhibitors of membrane and CoA requiring desaturases. to Kodak X-Omat AR film. First, this comparison demonstrated that the inhibition of oleic acid synthesis is sufficient PTU also acts by inhibiting the enzyme 5'-deiodinase (tetraiodothyronine 5' deiodinase), which converts T4 to the more active form T3. Alignment of amino acid sequences was achieved with Multalign (www.toulouse.inra.fr/multalin.html). 2 and 3). Mostly observations of individuals are described. This was later reduced because of the associated gastrointestinal disorders. The attacks of feverishness which occur within 7 to 14 days after the start of the therapy are put down to sensitization, as are the skin reactions [5]. For this reason thiourea has been used in doses between 0.01 and 0.5 g/kg i.p. the inhibition of oleic acid synthesis by isoxyl. The animals die of lung oedema; pleural effusion is seen in the survivors. The maternal benefit may outweigh fetal risk in life-threatening situations. the manuscript. This effect, however, was only seen at high doses and was only marked in animals treated with phenobarbital [66]. That thiourea is observed to inhibit DNA strand break induction by various intercalating substances in mouse leukaemia cells [70] is perhaps a result of a change in chromatin structure which would alter the activity of a topoisomerase responsible for the production of strand breaks under the influence of intercalating substances. Thiourea is also used during the production of blueprint and photocopy paper, resins, dyes, drugs, cleaners, and other chemicals. The effects of sterculic acid and ISO on mycolic Little was known of its mode of action. of the drug. Doses of 35 mg/kg and less had no effects on the thyroid gland or the other organs. Later studies with 35S‐thiourea demonstrated that, in the presence of NADPH or ascorbic acid, microsomal proteins from the thyroid are able to desulfurate thiourea. of 0.1, 0.5, 1.0, 2.0, 3.0, 4.0, and 5.0 μg/ml. In these respects it is interesting that DesA3 shares closer sequence identity with the Δ6 acyllipid of cyanobacteria and The cell pellet (20 g wet weight) was subsequently resuspended in 30 ml of buffer A (50 mm MOPS, pH 8, 10 mm MgCl2, 10% glycerol, and 500 mm NaCl) and sonicated for 10 cycles (60 s on; 90 s off) on ice. The reduction of the GSH content after administration of thiourea was not stoichiometric, i.e., significantly more GSH disappeared than was expected for the thiourea dose [63]. This was considered to be evidence for a genotoxic effect of the substance [90]. Of note, the drug is approximately 70% protein-bound and significantly ionized at normal physiologic pH, while the antithyroid agent methimazole is substantially less protein bound. of the Δ9 desaturation of stearic to oleic acid (29-32) and, therefore, provided a useful means to compare the effects of ISO to those of an established inhibitor of acyl-CoA Δ9-desaturase. The eight conserved His residues are indicated by shading (two in region Ia, three in region Ib, and three in Region II). desaturase, a conclusion reinforced by Western blotting, demonstrating directly that DesA3 is localized in the bacterial membrane The products found included not only protein‐bound sulfur but also thiosulfate and sulfate. 14C-Labeled FAMEs and MAMEs were extracted from M. bovis BCG wild type (WT) and the M. bovis BCG/pVV16desA3. The Effects of Oleic Acid Supplement on Partial Rescue of M. tuberculosis from ISO—The observations that ISO inhibited oleic acid synthesis in M. tuberculosis and M. bovis BCG led to the concept that supplementation of the growth medium with oleic acid should rescue cells from the killing effect Presumably, a thio‐iodine complex is formed as an unstable intermediate [55]. The i.p. Under present growth conditions employing the broth partially reversed by supplementing growth medium with oleic acid. the resulting supernatant was collected and loaded onto a 1-ml metal BD-Talon™ resin-chelating column (BD Biosciences Clontech, All of the His motifs (amino acids 90-94, 125-130, and 303-308) are located in the hydrophilic The thiourea isoxyl (thiocarlide; 4,4′-diisoamyloxydiphenylthiourea) is known to be an effective anti-tuberculosis drug, active against a range of multidrug-resistant strains of Mycobacterium tuberculosis and has been used clinically. the synthesis of oleic acid (Fig. The oral LD50 for the mouse is about 1 g/kg [9], for the rat 125–1830 mg/kg, depending on the strain [10], for the rabbit 10000 mg/kg [11]. cytosol was recovered as the supernatant after centrifugation of cell lysate at 200,000 × g for 1 h, and the pellet represented the cell membrane fraction. 4). fatty acid methyl ester standards.

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