Berberine Abstracts 7

© 2013

The natural alkaloid berberine targets multiple pathways to induce cell death in cultured human colon cancer cells

            (Chidambara Murthy, Jayaprakasha et al. 2012) Download

In the current paper, berberine, an isoquinoline alkaloid, was tested for its chemopreventive potential in colon cancer (SW480) cells. Berberine inhibited proliferation of colon cancer cells in a dose- and time-dependent manner. Interestingly, this compound exhibited minimum toxicity in normal cells at 200 muM. Berberine arrested SW480 cell cycle at G2/M phase, which was supported by induction of p21 expression. Induction of a series of biochemical events, including loss of mitochondrial membrane potential, release of cytochrome-c to cytosol, induction of Bcl-2 family proteins, caspases and cleavage of poly (ADP-ribose) polymerase (PARP), by berberine suggests its ability to induce apoptosis. In addition, berberine also inhibited inflammation, as evidenced by induction of expression of NFkappaB and Cox(2). Furthermore, berberine inhibited caspase-8 mediated angiogenesis, as confirmed through expression of tumor necrotic factor related apoptosis-inducing ligand (TRAIL), vascular endothelial growth factor (VEGF) and survivin. The results of the current study demonstrated that berberine has the ability to cause cell cycle arrest, induce apoptosis and inhibit inflammation in colon cancer cells. The magnitude of the effects observed suggests that berberine may be worth considering for further studies of its potential applications for improving health, either as a preventative or a potential treatment.

Aqueous extract of dried fruit of Berberis vulgaris L. in acne vulgaris, a clinical trial

            (Fouladi 2012) Download

Berberis vulgaris L. (barberry) is a very well-known herb in traditional medicine. Apart from its anti-inflammatory and antibacterial properties, the antilipogenic effect of barberry on the sebaceous glands in animals may further suggest it could be employed as an anti-acne agent. This study examined the effect of oral aqueous extract of barberry on acne vulgaris. Adolescents aged 12-17 years with moderate to severe acne vulgaris were randomly given oral gelatin capsules containing either aqueous extract of dried barberry (600 mg daily for 4 weeks, n = 25) or placebo (n = 24). Counts of facial noninflamed, inflamed, and total acne lesions, as well as the Michaelson's acne severity score were documented at baseline and at weeks 2 and 4. Both groups were comparable in terms of the patients' characteristics and baseline variables. After 4 weeks, the mean number of noninflamed, inflamed, and total lesions as well as mean Michaelson's acne severity score declined significantly by 43.25 +/- 10.88% (median: 42.11%), 44.53 +/- 11.78% (median: 45.45%), 44.64 +/- 8.46% (median: 46.15%), and 44.38 +/- 8.25% (median: 44.07%), respectively, among the extract receivers (p <.001 for all the changes). Similar changes were not significant in the placebo group. No notable complication or side effect was reported in relation to barberry. In conclusion, oral aqueous extract of dried barberry is a safe, well-tolerated, and effective choice in teenagers with moderate to severe acne vulgaris.

Berberine, an isoquinoline alkaloid, inhibits the metastatic potential of breast cancer cells via Akt pathway modulation

            (Kuo, Chuang et al. 2012) Download

Berberine (BBR) is a natural alkaloid with significant antitumor activities against many types of cancer cells. In this study, we investigated the molecular mechanisms by which BBR repressed the metastatic potential of breast cancer cells. BBR was found to downregulate the enzymatic activities and expression levels of matrix metalloproteinases 2 and 9 (MMP2 and MMP9, respectively). The BBR-mediated suppression of MMP2 and MMP9 involved the inhibition of the Akt/nuclear factor kappa B (NF-kappaB) and activator protein-1 (AP-1) signaling pathways. Furthermore, BBR repressed the expression of the Akt protein by modulating the mRNA expression level and protein degradation of Akt. In conclusion, this study suggests that BBR can reduce the metastatic potential of highly metastatic breast cancer cells and may be a useful adjuvant therapeutic agent in the treatment of breast cancer by targeting the Akt pathway.

Berberine and Coptidis rhizoma as novel antineoplastic agents: a review of traditional use and biomedical investigations

            (Tang, Feng et al. 2009) Download

ETHNOPHARMACOLOGICAL RELEVANCE: Coptidis rhizoma (huanglian) and its major component, berberine, have drawn extensive attention toward their antineoplastic effects in the recent years. The antineoplastic effects are related to the Chinese Medicine (CM) properties of huanglian in treating diseases by removing damp-heat and purging fire and counteracting toxicity. AIM OF THE REVIEW: To trace the long history of the traditional use of huanglian from folk medicines, especially from Chinese medicine, to recent pharmacological studies of huanglian and berberine, with an emphasis on their antineoplastic effects and the promise as novel antineoplastic agents. METHODS: A total of seven databases were extensively searched for literature research. The terms and keywords for searching included huanglian, berberine, Coptis, Coptidis rhizoma, anticancer, anti-invasion, antimatastasis and mechanism. The papers including ours with studies on anticancer and mechanism, pharmacology and toxicology of huanglian and/or berberine were focused. RESULTS: In view of traditional use, the anticancer effects of huanglian can be ascribed to its CM trait by removing damp-heat, fire and toxicity. From modern biomedical studies, anticancer effects have been demonstrated in both huanglian and berberine. The underlying molecular mechanisms involve cell-cycle arrest, apoptosis induction and anti-inflammation. Berberine is an essential anticancer compound in huanglian. In some studies, the use of huanglian was shown to be more effective and beneficial than the use of berberine alone. The presence of other protoberberine-type alkaloids in huanglian might give synergistic effects for the anticancer effects. Berberine also demonstrates effects of antiangiogenesis, anti-invasion and anti-metastasis in some cancer cell lines, however, more investigations are required to unravel the underlying mechanisms involved. CONCLUSIONS: The modern evidences of treating cancer with huanglian and berberine have a strong linkage with traditional concept and rules of using huanglian in CM practice. As anticancer candidates with low toxicity, berberine and its altered structure, as well as huanglian and its formulae, will attract scientists to pursue the potential anticancer effects and the mechanisms by using technologies of genomics, proteomics and other advanced approaches. On the other hand, relatively few in vivo studies have been conducted on anticancer effects of huanglian and berberine. The clinical application of berberine or huanglian as novel cancer therapeutic agents requires in vivo validations and further investigations of their anticancer mechanisms.


Chidambara Murthy, K. N., G. K. Jayaprakasha, et al. (2012). "The natural alkaloid berberine targets multiple pathways to induce cell death in cultured human colon cancer cells." Eur J Pharmacol 688(1-3): 14-21 PMID: 22617025

Fouladi, R. F. (2012). "Aqueous extract of dried fruit of Berberis vulgaris L. in acne vulgaris, a clinical trial." J Diet Suppl 9(4): 253-61 PMID: 23038982

Kuo, H. P., T. C. Chuang, et al. (2012). "Berberine, an isoquinoline alkaloid, inhibits the metastatic potential of breast cancer cells via Akt pathway modulation." J Agric Food Chem 60(38): 9649-58 PMID: 22950834

Tang, J., Y. Feng, et al. (2009). "Berberine and Coptidis rhizoma as novel antineoplastic agents: a review of traditional use and biomedical investigations." J Ethnopharmacol 126(1): 5-17 PMID: 19686830