Method for the Detection and Quantitative Assay of Cephaloglycin and Its Biologically Active Metabolites

Hoehn, Marvin M.; Pugh, Charles T.

doi:10.1128/aem.16.8.1132-1133.1968

Cited by 6 publications

(1 citation statement)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The sheets were then immediately developed in one of two solvent systems; n-butanol-acetic acid-water (3:1:1) or ethyl acetate-acetic acid-water (3:1:1). Developed sheets were treated for bioautography on S. lutea plates as described by Hoehn and Pugh (6). The concentrations in the test sera were estimated by comparing the sizes of the zones of inhibition with the zones for the standards on the same bioautograph plate.…”

mentioning

confidence: 99%

Cephaloglycin and Its Biologically Active Metabolite Desacetylcephaloglycin

Wick¹,

Wright²,

Kuder³

1971

Applied Microbiology

View full text Add to dashboard Cite

Chromatographic studies and microbiological assays show that, after oral administration, cephaloglycin is partially converted in man to a biologically active metabolite desacetylcephaloglycin. The antibacterial activity of this metabolite compared to that of cephaloglycin is equivalent against gram-positive organisms but is lower against gram-negative bacilli. Successful therapy of urinary tract infections with cephaloglycin must be mainly attributed to the antibacterial activity of this metabolite. At the present time, it is not possible to assess what influence low amounts of unaltered cephaloglycin have on the outcome of therapy. Cephaloglycin is a broad-spectrum, orally absorbed, cephalosporin antibiotic (16). As with cephalothin (9), the cephaloglycin molecule possesses an acetyl group that can be removed by nonenzymatic hydrolysis or by esterase enzymatic activity. Cephaloglycin is also partially deacetylated in humans (5, 13). Desacetylcephaloglycin, a biologically active metabolite, can be prepared by deacetylation of cephaloglycin with a citrus acetyl esterase. The yields of crystalline compound using this complex procedure are very low. Nevertheless, limited quantities of desacetylcephaloglycin were prepared to assess the extent of deacetylation after oral administration of cephaloglycin to humans. In addition, data pertaining to chemical and biological comparisons of cephaloglycin and its metabolite are presented. MATERIALS AND METHODS Antibiotics. Cephaloglycin dihydrate was employed in these experiments. The desacetylcephaloglycin used was prepared in the Lilly Laboratories by S. Kukolja (8). Microbiological assays. Disc-plate assays with Bacillus subtilis strain ATCC 6633 or Sarcina lutea strain PCI-1001-FDA were used to determine concentrations of cephaloglycin or desacetylcephaloglycin in human serum or urine. Serum specimens were drawn at 0, 1, and 2 hr after oral administration of single doses of 500 mg of cephaloglycin to male volunteers. Urine was collected for periods of 0 to 2, 2 to 4, and 4 to 8 hr. All specimens were assayed immediately. Chromatography. Cephaloglycin levels in the presence of desacetylcephaloglycin in body fluids were determined by a modification of the paper chromatographic method of Hoehn and Pugh (6). Serum and

show abstract

mentioning

confidence: 99%