Cancer and Berberine

Understanding the Cancer-Fighting Properties of Berberine

There is an inflammatory enzyme called cyclooxygenase-2 (COX-2) that is abundantly expressed in colon cancer cells. It also plays a key role in colon tumorigenesis (new cancer growth). Therefore, compounds inhibiting COX-2 transcriptional activity (gene RNA replication) potentially have a chemopreventive property. Finding natural compounds to inhibit COX-2 pathways should prove exciting and promising.

In a recent study, an assay method for estimating COX-2 transcriptional activity in human colon cancer cells was established using a β-galactosidase reporter gene system. The study examined effects made of various medicinal herbs and their ingredients for an inhibitory effect on COX-2 transcriptional activity.

They found that berberine, an isoquinoline alkaloid present in plants of the genera Berberis and Coptis from Oregon grape root and Bayberry, effectively inhibits COX-2 transcriptional activity in colon cancer cells in a dose- and time-dependent manner at concentrations higher than 0.3 μM. These findings may further explain the mechanism of anti-inflammatory and anti-tumor promoting effects of berberine.

Berberine and Breast Cancer

Berberine has many other biological activities including the ability to induce cell cycle arrest and apoptosis, making it a potentially useful agent for targeting cancer cells other than just the colon. Another study analyzed the effects of berberine on MCF-7 breast cancer cells. Berberine was added to MCF-7 cells in culture, and proliferation, side population (SP) cells and expression of ABCG2 were examined resulting in very promising results:

1. Berberine caused a dose-dependent reduction in proliferation (new cancer growth).

2. Berberine treatment caused a decrease in SP cells (cells that become circulating tumor cells or cancer stem cells) relative to untreated controls.

3. In addition, berberine treatment was associated with a decrease in expression of ABCG2 relative to untreated controls (ABCG2 expression is associated with increased resistance to chemotherapeutic agents).

These results indicate that the growth inhibitory effects of berberine treatment on MCF-7  Cancer cells may be reason in itself for use.

Berberine limits Metastasis and Angiogenesis

Metastasis and angiogenesis is to be avoided at all cost. There is increasing evidence that two chemicals, urokinase-type plasminogen activator (u-PA) and matrix metalloproteinases (MMPs) play an important role in cancer spread and vasculization. Inhibition of u-PA and MMPs could suppress migration and invasion of cancer cells. Berberine reported to have anti-cancer effects in different human cancer cell lines by inhibiting u-PA and MMPs according to another study.

The treatment of human prostate cancer cells (PC-3) with berberine was shown to induce dose-dependent apoptosis.   Berberine-induced apoptosis was associated with the disruption of the mitochondrial membrane potential, release of apoptogenic molecules (cytochrome c and Smac/DIABLO) from mitochondria and cleavage of caspase-9,-3 and PARP proteins. In xenograft in vivo studies, berberine reduced tumor weights and volumes accompanied with apoptotic cell death and increased expression of apoptotic cell death proteins.

3 Great Reasons to Consider Berberine:

• Berberine is a "good guy" in our arsenal against cancer of all types!
• Berberine can be a great "killer" of chronic infections, H. pylori, and even Candida
• Berberine is one of my favorite picks to help reduce blood pressure and protect the heart and mitral valves
• Berberine can stimulate a Th1 reaction so use with caution.