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At least 19 recordsLinked to original sources
PubMedDate not supplied

The metabolism and toxicity of halogenated carbanilides. Biliary metabolites of 3,4,4'-trichlorocarbanilide and 3-trifluoromethyl-4,4'-dichlorocarbanilide in the rat.

In separate experiments, after repeated oral administration of 3,4,4'-trichlorocarbanilide (TCC) and 3-trifluoromethyl-4,4'-dichlorocarbanilide (TFC) to rats, the biliary metabolites of each were isolated and identified. The major TCC biliary metabolite was found to be 2'-hydroxy-TCC. This compound was isolated mainly from the nonconjugated and the glucuronide fractions. Other metabolites present in substantial quantities were 6-hydroxy-TCC and 2',6-dihydroxy-TCC mainly as glucuronides and 3'-hydroxy TCC mainly as the sulfate conjugate. Small amounts of 3',6-dihydroxy-TCC were isolated from each of the fractions. No unchanged TCC was found in the bile. Only traces of other metabolites were found, and no N-hydroxylated products were observed. The major TFC biliary metabolite was the glucuronide conjugate of 2'-hydroxy-TFC. The only other metabolite of TFC was 3'-hydroxy-TFC, which was the predominant metabolite in the sulfate-conjugated fraction.

Animals↗
PubMed1979

Curative effects of the antipiroplasms amicarbalide and imidocarb on Trypanosoma brucei infection in mice.

The babesicides imidocarb and amicarbalide, which have structural similarities to the antitrypanosomatid diamidines, proved active against Trypanosoma brucei mouse infections: both cured infections when doses were administered daily for 3 days 24 h post-inoculation (curative dose imidocarb, 10 mg/kg; amicarbalide, 25 mg/kg). Mice were considered cured after survival 30 days longer than untreated infected controls, with no trypanosomes present in blood or cerebrospinal fluid smears. Both agents also cured when administered 48 and 72 h after challenge with T. brucei and prolonged the lives of animals 94 h after challenge. The results are discussed in respect to the potential of these carbanilides and their precursors, the antitumor phthalanilides, as lead compounds in chemotherapy of mammalian trypanosomiases.

Amidines↗
PubMed2024

Integrated multi-omics approaches reveal the neurotoxicity of triclocarban in mouse brain.

Triclocarban (TCC) is an antimicrobial ingredient that commonly incorporated in many household and personal care products, raising public concerns about its potential health risks. Previous research has showed that TCC could cross the blood-brain barrier, but to date our understanding of its potential neurotoxicity at human-relevant concentrations remains lacking. In this study, we observed anxiety-like behaviors in mice with continuous percutaneous exposure to TCC. Subsequently, we combined lipidomic, proteomic, and metabolic landscapes to investigate the underlying mechanisms of TCC-related neurotoxicity. The results showed that TCC exposure dysregulated the proteins involved in endocytosis and neurodegenerative disorders in mouse cerebrum. Brain energy homeostasis was also altered, as evidenced by the perturbation of pyruvate metabolism, TCA cycle, and oxidative phosphorylation, which in turn caused mitochondrial dysfunction. Meanwhile, the changing trends of sphingolipid signaling pathway and overproduction of mitochondrial reactive oxygen species (mROS) could enhance the neural apoptosis. The in vitro approach further demonstrated that TCC exposure promoted apoptosis, accompanied by the overproduction of mROS and alteration in the mitochondrial membrane potential in N2A cells. Together, dysregulated endocytosis, mROS-related mitochondrial dysfunction and neural cell apoptosis are considered to be crucial factors for TCC-induced neurotoxicity, which may contribute to the occurrence and development of neurodegenerative disorders. Our findings provide novel perspectives for the mechanisms of TCC-triggered neurotoxicity.

Animals↗
PubMed1977

Ecological effects of a deodorant and a plain soap upon human skin bacteria.

The effects of a commercial trichlorocarbanilide-containing deodorant soap and a commercial plain soap upon the cutaneous flora of individuals were compared. Using a cross-over design, 21 volunteers (10 women and 11 men) washed their forearms at least once a day with one soap for 3 weeks and then switched soaps for another 4 weeks use. By analysis of variance no significant difference in total colony counts was noted among individuals in their use of the two soaps. With the exception of individual variation, neither sequence of use, sex, nor any combination was influential. However, in 20 of 21 subjects an alteration in the composition of skin flora was observed. The deodorant soap, which in six cases increased total flora, tended to reduce or eliminate diphtheroids in 12 to 17 carriers (71%). Fewer kinds of bacteria were also noted. More Staphylococcus epidermidis was seen with the plain soap, but washing with the deodorant soap seemed to favour Acinetobacter calcoaceticus and Micrococcus luteus. The impact of this alteration and the use of total counts to measure effectiveness of deodorant soaps were brought into question.

Adult↗
PubMed1979

The adverse effects of nicarbazin on reproductive activity in the hen.

The effects of the anticoccidial agent nicarbazin on reproductive activity in the female fowl have been studied. 2. The drug had no effect on the plasma concentration of luteinising hormone, but treated hens showed a reduced hypothalamic sensitivity to exogenous progesterone, whilst the capacity of the pituitary to respond to luteinising hormone releasing hormone was unimpaired. 3. It is suggested that nicarbazin not only prevents yolk deposition within the ovary but also adversely affects the stimulatory function of the hypothalamus, possibly through an unsuitable hormonal environment.

Animals↗
PubMed1979

Protective effect of nicarbazin on nutritional encephalopathy in chicks.

Nutritional encephalopathy was induced in young chicks by vitamin E-deficient diets containing either 4% methyl esters of safflower oil or 10% thermally oxidized safflower oil. The coccidiostat nicarbazin (an equimolecular complex of 4,4'-dinitrocarbanilide and 2-hydroxy 4,6-dimethylpyrimidine) reduced the incidence of encephalopathy, but zoalene (3,5-dinitro-o-toluamide) and amprolium [1-(4-amino-2-n-propyl-5-pyrimidinylmethyl)-2-picolinium chloride hydrochloride] did not. Neither of the two components of nicarbazin affected the rate of development of encephalopathy when fed separately, but when included together in the diet, they reduced the incidence of the disease.

Animals↗
PubMed1975

Acne detergicans.

Popular brands of soaps and shampoos were assayed for comedogenicity in the rabbit ear. Only a small number produced hyperkeratosis when applied at a 25% concentration. Bacteriostatic substances, especially hexachlorophene, were mildly comedogenic. Conventional soaps include salts of fatty acids; the latter are known comedogens. The obsessive use of soaps by patients with acne vulgaris may aggravate the disease and result in its extension to unusual locations.

Acne Vulgaris↗
PubMed1976

Clinical, histologic, and histochemical study of imidocarb diproprionate toxicosis in goats.

The toxic effects of imidocarb diproprionate (3,3'-bis [2 imidazolin-2yl]-carbanilde diproprionate) were evaluated in adult goats given (intramuscular injection) a lethal dose (6.75 mg/kg). The immediate clinical signs of toxicosis were transient excessive salivation and diarrhea. Anorexia, dyspnea, recumbency, and death occurred between postinjection days (PID) 4 and 8, during which time 7 goats died and 4 moribund goats were euthanatized. There were marked increases in mean serum urea nitrogen concentration and significant increases in serum glutamic oxalacetic transminase activity and in the mean number of circulating neutrophils after PID 4. Renal hyperemia and enlargement were evident by PID1. Serosanguineous fluid in the trachea and major bronchi, pulmonary congestion and edema, hydrothorax, hydroperitoneum, and less frequently hydropericardium were observed on and after day 4. Microscopic renal tubular lesions rapidly progressed from pyknotic epithelial nuclei observed at 6 and 12 hours to acute tubular necrosis of epithelium of the proximal convoluted tubules on days 1 and 2. Pulmonary congestion and edema; hemorrhage into alveoli, bronchioles, and bronchi; and intracytoplasmic lipid vacuoles within the hepatocytes in the periacinar zones of the hepatic lobules were observed on or after day 4. Succinic dehydrogenase and adenosine triphosphatase activities decreased progressively in the epithelial cells of the proximal convoluted tubules. The decreases in cellular enzymatic activity occurred shortly after the appearance of microscopic lesions in the tubular epithelium.

Adenosine Triphosphatases↗
PubMedDate not supplied

Identification of the metabolites of trichlorocarbanilide in the rat.

The metabolism and excretion of 14C-labeled 3,4,4'-trichlorodiphenylurea has been studied in the rat after oral and iv administration. More than 80% of the administered radioactivity was excreted in the feces and urine over 5 days. Five isolated metabolites were characterized by mass spectrometry and by comparative thin-layer chromatography with synthesized compounds. Metabolites found include 2'-hydroxy-, 3'-hydroxy-, 6-hydroxy-, 2',6-dihydroxy- and 3',6-dihydroxy-3,4,4'-trichlorodiphenylurea.

Animals↗
PubMedDate not supplied

Biotransformation products of 3,4,4'-trichlorocarbanilide in rat, monkey, and man.

3,4,4'-Trichlorocarbanilide (TCC), uniformly labeled with 14C in the monochloro ring, was administered to rats, rhesus monkeys, and humans. Radioactive materials in the plasma and urine of all three species and in the bile of rats and monkeys were separated by high performance liquid chromatography. The chromatography showed great similarity between the monkey and the human. Principal metabolites common to all species were the sulfate and glucuronide conjugates of 2'-, 3'-, and 6-hydroxy-TCC. The rat also produced the glucuronide and sulfate conjugates of 2',6-dihydroxy-TCC. The major urinary excretion products found in humans and monkeys were the N- and N'-TCC glucuronides.

Animals↗
PubMedDate not supplied

The absorption, excretion, and biotransformation of 3,4,4'-trichlorocarbanilide in humans.

The metabolism and disposition of 14C-TCC (3,4,4'-trichlorocarbanilide) have been evaluated in humans following oral exposure to 2.2 mumol/kg body wt. Fecal elimination (70% of dose) was complete 120 hr after dosing and the urinary excretion (27% of dose) was completed in 80 hr. The maximum plasma level occurred 2.8 hr after dosing and was 3.7 nmol-equivalents of TCC per g of plasma (approximately 1.2 ppm). Biotransformation of TCC was rapid but did not appear to involve splitting of the basic TCC structure. The major plasma metabolites were N- and N'-glucuronides of TCC which were eliminated with t1/2 approximately 2 hr to the urine and 2'-hydroxy-TCC sulfate and 6-hydroxy-TCC sulfate (the o-hydroxy-TCC sulfates) which were removed with t1/2 approximately 20 hr (presumably into the bile). It is concluded that a nonradioactive analytical method based on the urinary excretion of the N-glucuronides would be suitable for the determination of TCC absorption in humans.

Adult↗