Benzimidazole derivatives are widely studied because of their broad-spectrum biological activity,s uch as antitumor properties and excellent fluorescencep erformance. Herein, two typeso f2 -(5-phenylindol-3-yl)benzimidazole derivatives (1a-1h and 2a-2e)w ere rationally designed and synthesized. When these compounds were investigated in vitro anti-screeninga ssays,w ef ound that all of them possessed antitumor effect, in particular compound 1b,w hich showed an outstanding antiproliferativee ffect on MDA-MB-231 cells( IC 50 % 2.6 mm). As tudy of the drug action mechanisms in cells showedt hat the antitumor activity of the com-poundsi sp roportionalt ot heir lipophilicity and cellular uptake;t he tested compounds all enteredt he lysosome of MDA-MB-231c ellsa nd caused changes in the levels of reactive oxygen species( ROS), andt hen caused mitochondrial damage. Apparent differences in the ROS levels for each compound suggestt hat the lethality of thesec ompounds towardsM DA-MB-231c ells is closely relatedt ot he ROS levels. Taken together,t his study not only provides at heoretical basis for 2-(5-phenylindol-3-yl)benzimidazole anticarcinogensb ut also offers new thinking on the rational design of next-generation antitumor benzimidazole derivatives.
The
effects of selenium species on the Belousov–Zhabotinsky
(B–Z) reaction were investigated by adding them to the system
before and during oscillation. When selenium species were added into
the system before oscillation, sodium selenite prolonged the induction
period, whose effect was strong as sodium selenite could consume malonic
acid to prohibit the accumulation of bromomalonic acid. For selenomethionine
and selenocystine, their effects were derived from their reaction
with •CH2COOH and •Br2
– producing a radical cation of selenoamino
acids, which prohibited the accumulation of bromomalonic acid. Here,
the selenium atoms in selenoamino acids, as reactive centers, took
part in the redox reaction. As a result, the induction period was
prolonged. However, as a diselenide, selenocystine can reduce bromate
in acidic medium, which led to shortening of the induction period.
Therefore, the effect of selenocystine on the induction period was
the result of two opposite effects. Nanoselenium shortened the induction
period in a certain concentration range because bromate was directly
reduced by nanoselenium and the accumulation of bromomalonic acid
was promoted. Furthermore, the dose perturbation effect was investigated
by the injection of nanoselenium during oscillation. It was found
that the amplitude was increased or decreased in a dose-dependent
fashion when nanoselenium was injected at peak or trough of the time-dependent
redox potential curve.
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