Rhein induces apoptosis in human breast cancer cells

Area of Science:

• Biochemistry
• Pharmacology
• Oncology

Background:

• HER2/neu overexpression in breast cancer cells correlates with aggressive tumor behavior and chemoresistance.
• Anthraquinone derivatives from rhubarb root are investigated for their potential anticancer properties.

Purpose of the Study:

• To evaluate the antiproliferative and apoptotic effects of rhubarb root anthraquinone derivatives on human breast cancer cells.
• To determine the specific mechanisms underlying the action of active compounds, focusing on signaling pathways.

Main Methods:

• Screening of seven anthraquinone derivatives from rhubarb root for antiproliferative activity.
• Assessing the effects of active compounds on HER2-overexpressing (MCF-7/HER2) and control (MCF-7/VEC) breast cancer cells.
• Investigating the induction of apoptosis, caspase-9 activation, and the involvement of ROS, NF-κB, and p53 signaling pathways.

Main Results:

• Rhein was the sole anthraquinone derivative exhibiting significant antiproliferative and apoptotic effects on both MCF-7/HER2 and MCF-7/VEC cells.
• Rhein induced apoptosis in a dose- and time-dependent manner, mediated by caspase-9 activation.
• The apoptotic effects of rhein were linked to ROS-mediated activation of NF-κB and p53 signaling pathways.

Conclusions:

• Rhein demonstrates potent anti-proliferative activity against breast cancer cells with both HER2 overexpression and basal HER2 expression.
• Rhein plays a crucial role in inducing apoptosis in human breast cancer cells through specific molecular pathways.
• Rhein represents a promising natural compound for therapeutic development against aggressive breast cancers.