Zeylasteral and demethylZeylasteral are 6-oxophenolic triterpenoids isolated from the root of Maytenus blepharodes, which have antimicrobial activity against Gram-positive bacteria and the yeast Candida albicans.
METHODS AND RESULTS:
The time-kill curves for Zeylasteral and demethylZeylasteral at concentrations twice their MICs, against Bacillus subtilis showed that the colony forming units were reduced in 3-log10 and > 4-log10 respectively. This reduction was dependent on inoculum size and the growth phase of cells, and was greater when the compounds were incorporated in the exponential phase, indicating a bacteriolytic effect. Treatment with both agents, particularly with Zeylasteral (20 microg/mL) caused a reduction of optical density at 550 nm. With regard to the synthesis of DNA, RNA, protein and cell wall, the compounds exhibited the fastest inhibition against cell wall synthesis.
CONCLUSIONS:
Thus, the predisposition to lysis, the morphological changes seen by microscopy, and the complete inhibition in the incorporation the N-acetyl-d-[1 - 14C]glucosamine, suggest that the phenolic compounds compromise the cell wall synthesis and/or cytoplasmic membrane. |