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8 recordsLinked to original sources
PubMed2025

Genetic Incorporation of a Thioxanthone-Containing Amino Acid for the Design of Artificial Photoenzymes.

Genetically encodable photosensitizers allow the design of artificial photoenzymes to expand the scope of abiological reactions. Herein, we report the genetic incorporation of a thioxanthone-containing amino acid into a protein scaffold via an engineered pyrrolysyl-tRNA/pyrrolysyl-tRNA synthetase pair. The designer enzyme was engineered to catalyze a dearomative [2+2] cycloaddition reaction in high yields (up to>99 % yield) with excellent enantioselectivity (up to 98 : 2 e.r.). This work provides a robust and facile method for photoenzyme design and lays the foundation for the development of further photoenzymatic reactions.

Xanthones↗
PubMed1975

Determination of 3-(5-tetrazolyl) thioxanthone 10,10-dioxide in human plasma, urine and faeces.

A gas chromatographic method is described for assay of 3-(5-tetrazolyl) thioxanthone 10,10-dioxide (BW 59C) in human plasma, urine and faeces. After extraction into 1,2-dichloroethane from alkaline medium the compound is converted to the heptafluorobutyrate derivative which is injected into a gas chromatograph and measured using a 63Ni electron capture detector. The assay produces a linear calibration curve over the range 0-30 mug/ml when the internal standard method is used. Reproducibility is good and sensitivity down to 1 ng injected on column is possible. The method has been used to investigate the pharmacokinetic properties of BW 59C in man and has been semi-automated by the use of an autosampler and dedicated computer.

Chromatography, Gas↗
PubMed1976

The structure of Miracil D, a DNA-binding drug.

The crystal structure of the drug Miracil D has been determined. Although the accuracy of the analysis is limited by disorder, it is apparent that the thioxanthone ring system is planar. The proximal nitrogen atom of the side-chain probably forms an intramolecular hydrogen bond with the carbonyl oxygen. The rest of the side-chain has a large degree of conformational mobility.

Chemical Phenomena↗
PubMed1992

Studies on carbohydrates extracted from native and chemically treated Biomphalaria alexandrina snails.

1. Carbohydrates were extracted from total tissue extracts of Biomphalaria alexandrina snails and were analyzed to their monosaccharides using GLC. 2. The snails were chemically treated with thioxanthone derivatives (compounds I, II, III) and the change in the monosaccharide constituents of their carbohydrates was investigated. 3. The isolated monosaccharides from native and chemically pretreated snails were injected into mice and their protective effects were examined after infection of mice with cercariae of Schistosoma mansoni. 4. The results showed that the main monosaccharides in carbohydrates of snails were galactose, glucose, fucose and mannose and that chemical treatment caused a drop in the galactose content. 5. Moreover, monosaccharide fractions from snails treated with compound III were the most effective in inducing protection against Schistosoma infection in mice.

Animals↗
PubMed1976

Differential histamine release by dextran and the ionophore A23187: the actions of inhibitors.

Inhibitors of mast cell membrane activation reduced histamine release from rat mast cells induced by dextran and phosphatidyl serine but not that induced by the calcium ionophore A23187. Such inhibitors included cromoglycate, an orally-active anti-allergic agent 3-(5-tetrazolyl)thioxanthone 10,10-dioxide, dibutyryl cyclic 3':5'-AMP, theophylline and dicumarol. Inhibitors of mast cell metabolism reduced both types of release and these included oligomycin, papevevime, and the two uncouplers of oxidative phosphorylation-alpha2,4-dinitrophenol and CCCP. Inhibition of histamine release from rat isolated peritoneal mast cells by either a mixture of dextran and phosphatidyl serine or the ionophore A23187 thus allows inhibitors of mast cell membrane activation to be distinguished from those affecting cell metabolism or the later stages of the secretory process.

Animals↗
PubMed1977

Phototoxicity occurring during the manufacture of ultraviolet-cured ink.

Four workers employed in the manufacture of ultraviolet-cured inks complained of photosensitivity characterized by an intense burning sensation during sun exposure. Three of these workers developed dermatitis on exposed areas following sun exposure. Six compounds used as photoinitiators in the ink formulations were found to absorb solar ultraviolet radiation. Two preparations of mixed isomers (ortho and para) of amyl dimethylaminobenzoate were found to be phototoxic to Ehrlich ascites cells in vitro and to produce diphasic phototoxic reactions in vivo after topical application on symptomatic workers, asymptomatic workers, or previously unexposed subjects. These responses could be prevented in two subjects by the application of a 10% sulizobenzone sunscreen prior to sun exposure. Two other photoinitiators, Michler's ketone and thioxanthone were phototoxic in vitro but not after topical application in vivo.

Adult↗