Abstract
BackgroundCardol is a major bioactive constituent in the Trigona incisa propolis from Indonesia, with a strong in vitro antiproliferative activity against the SW620 colorectal adenocarcinoma cell line (IC50 of 4.51 ± 0.76 μg/mL). Cardol induced G0/G1 cell cycle arrest and apoptotic cell death. The present study was designed to reveal the mechanism of cardol’s antiproliferative effect and induction of apoptosis.MethodsChanges in cell morphology were observed by light microscopy. To determine whether the mitochondrial apoptotic pathway was involved in cell death, caspase-3 and caspase-9 activities, western blot analysis, mitochondrial membrane potential, and intracellular reactive oxygen species (ROS) levels were assayed.ResultsChanges in the cell morphology and the significantly increased caspase-3 and caspase-9 activities, plus the cleavage of pro-caspase-3, pro-caspase-9 and PARP, supported that cardol caused apoptosis in SW620 cells within 2 h after treatment by cardol. In addition, cardol decreased the mitochondrial membrane potential while increasing the intracellular ROS levels in a time- and dose-dependent manner. Antioxidant treatment supported that the cardol-induced cell death was dependent on ROS production.ConclusionCardol induced cell death in SW620 cells was mediated by oxidative stress elevation and the mitochondrial apoptotic pathway, and these could be the potential molecular mechanism for the antiproliferative effect of cardol.
Highlights
Cardol is a major bioactive constituent in the Trigona incisa propolis from Indonesia, with a strong in vitro antiproliferative activity against the SW620 colorectal adenocarcinoma cell line (IC50 of 4.51 ± 0.76 μg/mL)
The shape of the SW620 cells had changed after 2 h treatment with cardol, with apoptotic and bulb appearing cells being evident
After 72 h of treatment very few SW620 cells treated with cardol at 8 or 14 μg/mL or doxorubicin at 0.5 μg/mL had survived (Fig. 2)
Summary
Cardol is a major bioactive constituent in the Trigona incisa propolis from Indonesia, with a strong in vitro antiproliferative activity against the SW620 colorectal adenocarcinoma cell line (IC50 of 4.51 ± 0.76 μg/mL). The long 5-alkyl side chain containing cardol (C15:3) is a unique xanthine oxidase inhibitor without any pro-oxidant effects [7], and has an inhibition concentration at 50% (IC50) value for superoxide anion generation of 115 ± 10 μM. The 5-alkyl side chain seems to play an important role in eliciting the xanthine oxidase inhibitor activity that inhibits superoxide anion generation by binding cooperatively to the enzyme [8]. The C15:3 cardol, (2),5-[80(Z),110(Z),140-penta-decatrienyl] resorcinol, isolated from cashew nuts was a specific inhibitor for the superoxide anion generation catalysed by xanthine oxidase [10]
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