Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: CAS:80-08-0 (DSS)
 2,544 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

An evaluation of the immune state in leprosy was done by the application of a system of graft-versus-host reaction. Peripheral blood lymphocytes obtained from patients with different forms of leprosy and from normal healthy individuals were injected intravenously into the irradiated mice. The rate of blast transformation of the donor cells was measured by the radio-active thymidine uptake. The number of cells labelled with tritiated-thymidine was much higher in the normal individuals and patients with tuberculoid leprosy than in the patients with lepromatous leprosy with the borderline group placed in between the two. However, following successful treatment with DDS, an increased responsiveness and active DNA synthesis could be observed in the previously less responsive lepromatous lymphocytes.
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PMID:An evaluation of the immune state in leprosy. 1 65

Histochemical studies were made of pigmented cutaneous lesions from three cases of lepromatous leprosy treated with B663 to determine the nature and histogenesis of the brown pigmentation which develops as a side effect of the drug. One case of DDS-treated leprosy and four cases of untreated leprosy were also investigated histochemically as controls. The brown pigmentation of the skin is due to deposition of a ceroid-like substance in the macrophages, which is a yellowish-brown, acid-fast lipid pigment. It is insoluble in fat solvents and accepts lipid dyes even after lipid extraction by fat solvents. The macrophages in the B663-treated leprosy contain more neutral fat and less phospholipid than the untreated lepromatous leprosy tissues. Ceroid in the macrophages probably originated from unsaturated fatty acids of the leprosy bacilli through oxidation or their binding with the drug. Crystals of the drug were not found in the macrophages in this series, even on the tissues embedded in carbowax or frozen sections.
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PMID:Histochemistry of B663 pigmentation: ceroid-like pigmentation in macrophages. 7 60

An array of nonclassical thioquinazoline analogues (VIII) of methotrexate was prepared by cyclization of the requisite 2-amino-5-(arylthio)benzonitrile with chloroformamidine hydrochloride (28--79%). The aminonitrile precursors were obtained by SnCl2-HCl reduction (28--99%) of the corresponding 2-nitro-5-(arylthio)benzonitriles, which were synthesized by the condensation of the appropriate 5-chloro-2-nitrobenzonitriles with various arylthiols (36--83%). Many of the thioquinazolines (VIII) showed suppressive antimalarial activity comparable with or superior to chloroquine, cycloguanil, and pyrimethamine against drug-sensitive lines of Plasmodium berghei in mice and Plasmodium gallinaceum in chicks, and several displayed potent prophylactic activity with P. gallinaceum. Moreover, the thioquinazolines retained potent antimalarial effects against chloroquine-, cycloguanil-, pyrimethamine- and DDS-resistant lines of P. berghei in mice and against chloroquine- and pyrimethamine-resistant strains of Plasmodium falciparum in owl monkeys. The most active compound, namely, 2,4-diamino-6-[alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline, was designated for preclinical toxicological studies. Numerous substances exhibited in vitro activity against a broad spectrum of pathogenic bacteria at concentrations of less than 0.25 microgram/mL. The thioquinazolines also prove to be potent folate antagonists, causing 50% inhibition of Streptococcus faecalis R (ATCC 8043) at drug concentrations ranging from 0.2 to 2.0 ng/mL. Structure--activity relationships are discussed.
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PMID:Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects. 10 92

Drug sensitivity was tested using liquid medium on three stains isolated from the subcutaneous nodules of L-type patients who have long been administered DDS alone. The results revealed that the first strain was resistant to DDS up to the concentration of 1.0 microgram/ml suggesting as if it were DDS dependent or enhanced strain, whereas the second strain was completely sensitive to DDS even at the lowest concentration of 0.01 microgram/ml suggesting possible inactivation of this drug in the host patient. The third strain was completely resistant to 0.1 microgram/ml, but sensitive to 1.0 microgram/ml of DDS, suggesting that the therapeutic effect can not be expected any more, when the strain becomes resistant to 0.1 microgram/ml of DDS. All of the three strains were sensitive to REP at the concentration of 0.01 microgram/ml, and the host patients of the former two strains showed rapid improvement of the clinical symptomes after REP administration. That the second strain was sensitive to INH at the concentratin of 0.01 microgram/ml suggested the availability of the combined use of INH in the chemotherapy of leprosy.
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PMID:Drug sensitivity of M. leprae isolated from leprosy patients administered DDS for long period of time. 10 9

Oxidation of an array of 2,4-diamino-6-(arylthio)quinazolines provided the corresponding arylsulfinyl and arylsulfonyl analogues. A variety of these nonclassical analogues of methotrexate exhibited suppressive antimalarial activity superior to that of the parent thioquinazolines against drug-sensitive lines of Plasmodium berghei in mice and P. gallinaceum in chicks, and several displayed potent prophylactic activity against P. gallinaceum. The sulfinyl- and sulfonylquinazolines also retained antimalarial effects against chloroquine-, cycloguanil-, and DDS-resistant lines of P. berghei in mice and against chloroquine- and pyrimethamine-resistant strains of P. falciparum in owl monkeys. Coadministration of one of the most active of these compounds, 2,4-diamino-6-(2-naphthylsulfonyl)-quinazoline (35), with sulfadiazine to monkeys infected with P. falciparum of P. vivax led to greatly enhanced activity and prevented the development of quinazoline resistance.
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PMID:Folate antagonists. 15. 2,3-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity. 11 7

Dehydroepiandrosterone (D) and dehydroepiandrosterone sulfate (DS) dynamics were studied in three obese female subjects following a single injection of [4-14-CA1D and [7 alpha-3-H]-DS tracers. Dynamic parameters were calculated simultaneously by both the urinary and blood method of compartmentalization; Estimates for the urinary secretion and production rates of D were found to be high, and those of DS varied within normal range. Calculation of the conversion factors, rho DDS and rho DSD, by the urinary method revealed a noraml extraglandular DS yields D conversion, while that for D yields DS appeared deficient in obese female subjects. Estimates of inner and outer pool distribution volumes were extremely increased for free D; in contrast to this, moderately increased inner and decreased outer pool volumes of DS were observed. The metabolic clearance rates of D were normal or decreased and those for DS were greater than normal. The blood production rates of both B and DS were higher in obese female subjects than those estimated for normal women in our previous study; These observations suggest a considerable uptake of unconjugated D by adipose tissue, an overall poor D yields DS conversion and an accelerated DS metabolism in obese female subjects.
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PMID:Dehydroepiandrosterone and dehydroepiandrosterone sulfate dynamics in obesity. 12 23

The macrophage migration inhibition activity [MI activity) was stable in sensitized lymphocyte-to-marcophage ratios of 1:5 to 1:20 in mice. Antigen protein concentrations under 100 mug/ml did not induce nonspecific macrophage migration inhibition. Inhibition of tumor proliferation and survival was observed after a combined injection of BCG and MH-134 cells. After a single injection of MH-134 tumor cells, MI activity was reinforced and prolonged, demonstrating the clear effects of BCG as adjuvant. In DDS mice MI activity was weakened in the regional lymph node after a subcutaneous injection of just above or below 10(5) Ehrlich cancer cells previously treated with mitomycin C. This finding suggests the presence of an optimal tumor antigen concentration.
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PMID:Experimental studies of tumor immunotherapy. I. Macrophage migration inhibitory activity as an immunological parameter. 13 89

A simple radiometric method has been developed for evaluating the effect of drugs on the metabolism of M. lepraemurium. The method is based on the measurement of the 14CO2 produced through bacterial metabolism of acetate-U-14C. Seventeen drugs were tested: bacitracin, cephaloridine, chloramphenicol, cycloserine, dactinomycin, DDS, ethionamide, INH, kanamycin, methenamine mandelate, nitrofurantoin, oxacillin, polymyxin B, rifampicin, streptomycin, sulfadimethoxine and vancomycin. The drugs which caused most marked inhibition were chloramphenicol, INH, ethionamide and nitrofurantoin in order of increasing effectiveness. The radiometric study which is completed in 15 days permits direct study of the drug effect on the metabolism of M. lepraemurium and a more rapid screening of antileprosy drugs than has previously been possible. Currently, these observations are being extended to studies of the structure-activity relationships of antileprosy drugs and the metabolism and drug susceptibility of M. leprae in vitro.
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PMID:A radiometric method for predicting effectiveness of chemotherapeutic agents in murine leprosy. 17 20

Subcorneal dermatosis is a chronic relapsing pustular eruption which has been recognised for 20 years. The diagnosis can be made only by combining the clinical features of a recurrent eruption mainly on the trunk which spares the mucosae and has the histological appearance of a subcorneal bullae filled with polymorphonuclear leucocytes situated on the surface of normal epidermis. No immunofluorescence either direct or indirect similar to that seen in pemphigus, pemphigoid or dermatitis herpetiformis has been reported. No jejunal abnormality has been found in any case but some, though not all, patients respond to treatment with Dapsone (DDS; diaminodiphenylsulfone). The condition can be distinguished from other cases of subcorneal pustular eruptions only by combining the clinical and histological features. The etiology remains unknown.
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PMID:[Subcorneal pustular dermatosis]. 32 98

The plasma DDS clearance rates and the acetylation rates of Sulphadimidine were studied in a group of 30 leprosy patients comprising of 17 non-responders and 13 responders to DDS treatment. No differences in the acetylator type or in the plasma DDS clearance were seen between the responders and non-responders. Acetylation rate did not bear any relation to the plasma clearance of DDS in the non-responders. The findings indicate that the resistance to DDS therapy in these patients is not related to any abnormal metabolic disposition of DDS.
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PMID:Blood DDS levels and acetylation rates of sulphadimidine in leprosy patients. 33 Sep 45


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