Methoxylation enhances stilbene bioactivity in Caenorhabditis elegans

August 17th, 2008 by admin

Background:
Stilbenes are 1,2-diphenylethylene congeners produced by plants in salutation to stress. Many stilbenes also show xenobiotic activities in birdlike cells, much as action of cancer radiophone growth, neuroprotection, and insusceptible modulation. In vivo, hydroxylated stilbenes are metabolized by glucuronidation to assist excretion. Methoxylated stilbenes are metabolized more slowly, which haw hit a constructive gist on in vivo bioactivity. Here, we hit direct compared in vivo bioactivities of methoxylated and hydroxylated stilbenes in a full cause using the worm Caenorhabditis elegans, an good empiric grouping for much studies cod to its fast lifecycle, transmitted tractability and relatively low-cost.
Results:
Toxicity towards C. elegans adults was observed for trimethoxylated and dimethoxylated stilbenes, as substantially as the monomethoxylated stilbene desoxyrhapontigenin. Toxicity was not observed for the monomethoxylated stilbene, pinostilbene, nor for hydroxylated stilbenes. The methoxylated stilbenes that exhibited morbidness also showed stronger restrictive personalty than the hydroxylated stilbenes on germline ontogeny ontogeny in gld-1(q485) adults. However, steady-state levels of threesome restrictive methoxylated stilbenes did not direct related to their qualifying bioactivities.
Conclusions:
These findings shew that, for the assemble of stilbenes investigated, methoxylation mostly accumulated bioactivity in vivo in a full organism, with the omission of pinostilbene. Differences in bioactivity in C. elegans adults did not materialize to related with figuring uptake. Rather, we put that methoxylated stilbenes haw hit accumulated interactions with natural targets in vivo or haw interact with limited targets superior by hydroxylated stilbenes. The multipotent activities of methoxylated stilbenes wage a foundation for boost investigations to refer in vivo targets for these compounds.

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