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Effect of 4-ethyl-4-aza-5[alpha]-cholestane (ND-497) on the carbohydrate metabolism of Staphylococcus aureus.

Certain azasteroids, possessing the properties of cationic surface active agents, have been shown to inhibit the growth of Gram-positive bacteria, yeasts and molds. It had been demonstrated that the antimicrobial activity of azasteroids is due, at least partly, to membrane damage followed by loss of cytoplasmic constituents. This suggested that their primary site of action is the cytoplasmic membrane. More recently, it was found that inhibition of bacterial growth may not be due entirely to leakage of cellular components.

The purpose of this investigation was to study the effect of an active azasteroid, 4-ethyl-4-aza-5[alpha]-cholestane (ND-497), on the carbohydrate metabolism of Staphylococcus aureus. ND-497 was found to be a more potent in vrtro inhibitor or S. aureus than tetracycline hydrochloride, erythromycin, streptomycin sulfate, polymyxin B sulfate or neomycin sulfate. Of special interest was the discovery of the synergistic actions of ND-497 with neomycin sulfate, streptomycin sulfate or polymyxin B sulfate. Uranyl nitrate behaved as a competitive inhibitor of ND-497.

The metabolism of glucose, fructose and sucrose was effectively inhibited at concentrations which did not lyse cells indicating that the lethal action of ND-497 involved enzymes. Other data suggest that ND-497 may inhibit the oxidation/reduction system of S. aureus in a manner which is similar to that exhibited by tetracycline hydrochloride or erythromycin.

Norman J. Doorenbos, Dept. Pharmacal Sci., Auburn Univ., Auburn, AL 36849, Samia A. EL Dardiry, Tanta University, Tanta, Egypt; Lyman A. Magee, Dept.Biology, Univ. Mississippi, University, MS 38655.
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Title Annotation:Biological Sciences
Author:Doorenbos, Norman J.; El Dardiry, Samia A.; Magee, Lyman A.
Publication:Journal of the Alabama Academy of Science
Article Type:Brief Article
Date:Apr 1, 2003
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