Abstract
Triterpenes have been reported to induce cell death. One relevant group of this family of compounds is cucurbitacins, which have been studied as inducers of apoptosis in various cancer cell lines. The most significant mechanisms with regard to the apoptotic effects of cucurbitacins are their ability to modify transcriptional activities via nuclear factors or genes and their capability to activate or inhibit pro- or anti-apoptotic proteins. Still, while the majority of studies on these compounds have dealt with their apoptotic effects on cancer cell lines, several research groups have also explored their anti-inflammatory activities. In general, cucurbitacins are considered to be selective inhibitors of the JAK/STAT pathways; however, other mechanisms may be implicated in their apoptotic effects, including the MAPK pathway (known to be important for cancer cell proliferation and survival), PARP cleavage, expression of active caspase-3, decreased pSTAT3 and JAK3 levels, as well as decreases in various downstream STAT3 targets such as Mcl-1, Bcl-2, Bcl-xL, and cyclin D3, all of which are implicated in apoptosis and the cell cycle. Taking all these effects into account, cucurbitacins may prove useful in the treatment of different kinds of cancers, especially when used with other cytostatic agents.
Keywords: Cucurbitacins, cell death, apoptosis, JAK-STAT, cancer, triterpenes, transcriptional activities, anti-inflammatory activities, MAPK pathway, cytostatic agents
Current Pharmaceutical Design
Title:Cucurbitacins as Inducers of Cell Death and a Rich Source of Potential Anticancer Compounds
Volume: 18 Issue: 12
Author(s): J. L. Rios, I. Andujar, J. M. Escandell, R. M. Giner, M. C. Recio
Affiliation:
Keywords: Cucurbitacins, cell death, apoptosis, JAK-STAT, cancer, triterpenes, transcriptional activities, anti-inflammatory activities, MAPK pathway, cytostatic agents
Abstract: Triterpenes have been reported to induce cell death. One relevant group of this family of compounds is cucurbitacins, which have been studied as inducers of apoptosis in various cancer cell lines. The most significant mechanisms with regard to the apoptotic effects of cucurbitacins are their ability to modify transcriptional activities via nuclear factors or genes and their capability to activate or inhibit pro- or anti-apoptotic proteins. Still, while the majority of studies on these compounds have dealt with their apoptotic effects on cancer cell lines, several research groups have also explored their anti-inflammatory activities. In general, cucurbitacins are considered to be selective inhibitors of the JAK/STAT pathways; however, other mechanisms may be implicated in their apoptotic effects, including the MAPK pathway (known to be important for cancer cell proliferation and survival), PARP cleavage, expression of active caspase-3, decreased pSTAT3 and JAK3 levels, as well as decreases in various downstream STAT3 targets such as Mcl-1, Bcl-2, Bcl-xL, and cyclin D3, all of which are implicated in apoptosis and the cell cycle. Taking all these effects into account, cucurbitacins may prove useful in the treatment of different kinds of cancers, especially when used with other cytostatic agents.
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Cite this article as:
J. L. Rios, I. Andujar, J. M. Escandell, R. M. Giner, M. C. Recio , Cucurbitacins as Inducers of Cell Death and a Rich Source of Potential Anticancer Compounds , Current Pharmaceutical Design 2012; 18 (12) . https://dx.doi.org/10.2174/138161212799958549
DOI https://dx.doi.org/10.2174/138161212799958549 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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