Berberine Benefits in Cancer

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.

Berberine Supplement

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.

Our Berber Clear supplies high potency berberine combined with alpha lipoic acid to help support optimal blood sugar and insulin levels, cardiovascular health, and liver health. Berberine is an alkaloid compound found in the roots, rhizomes, stems and bark of several plants commonly used in botanical and Chinese medicine, such as goldenseal, Oregon grape, barberry, and Berberis aristata.

Lipoic acid is best known for its antioxidant properties and its ability to support healthy insulin secretion and sensitivity. It is also a key cofactor for mitochondrial enzymes involved in cellular metabolism and energy (ATP) production. Made with non-GMO ingredients.

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.

A 2019 study on berberine and Triple-Negative Breast Cancer revealed, “Our results demonstrate that the anti-proliferation effects of Berberine occur via different mechanisms in different subtypes of TNBC cells, which suggests that Berberine has potential as a personalized treatment for TNBC patients.” (1) Another study published the same year on Berberine and Ovarian cancer concluded, “This study proposed that the combination therapy of Berberine and DDP (Cisplatin chemotherapy drug) markedly enhanced more ovarian cancer cell death by inducing apoptosis and necroptosis, which may improve the anticancer effect of chemotherapy drugs.” (2)

A summary article published in 2023 states, “Berberine (BBR) is a potential plant metabolite and has remarkable anticancer properties. Many kinds of research are being focused on the cytotoxic activity of berberine in in vitro and in vivo studies. A variety of molecular targets which lead to the anticancer effect of berberine ranges from p-53 activation, Cyclin B expression for arresting cell cycles; protein kinase B (AKT), MAP kinase and IKB kinase for antiproliferative activity; effect on beclin-1 involved in autophagy; reduced expression of MMP-9 and MMP-2 for the inhibition of invasion and metastasis etc. Berberine also interferes with transcription factor-1 (AP-1) activity responsible for the expression of oncogenes and neoplastic transformation of the cell. It also leads to the inhibition of various enzymes which are directly or indirectly involved in carcinogenesis like N acetyl transferase, Cyclo-oxygenase-2, Telomerase and Topoisomerase. In addition to these actions, Berberine plays a role in, the regulation of reactive oxygen species and inflammatory cytokines in preventing cancer formation. Berberine anticancer properties are demonstrated due to the interaction of berberine with micro-RNA.” (3)

(1) – Lin YS, Chiu YC, Tsai YH, Tsai YF, Wang JY, Tseng LM, Chiu JH. Different mechanisms involved in the berberine-induced antiproliferation effects in triple-negative breast cancer cell lines. J Cell Biochem. 2019 Aug;120(8):13531-13544. doi: 10.1002/jcb.28628. Epub 2019 Apr 7. PMID: 30957305.

(2) – Liu L, Fan J, Ai G, Liu J, Luo N, Li C, Cheng Z. Berberine in combination with cisplatin induces necroptosis and apoptosis in ovarian cancer cells. Biol Res. 2019 Jul 18;52(1):37. doi: 10.1186/s40659-019-0243-6. PMID: 31319879; PMCID: PMC6637630.

(3) – Goel A. Current understanding and future prospects on Berberine for anticancer therapy. Chem Biol Drug Des. 2023 Jul;102(1):177-200. doi: 10.1111/cbdd.14231. Epub 2023 Apr 1. PMID: 36905314.