Abstract
Coptis, a traditional medicinal plant, has been used widely in the field of traditional Chinese medicine for many years. More recently, the chemical composition and bioactivity of Coptis have been studied worldwide. Berberine is a main component of Rhizoma Coptidis. Modern medicine has confirmed that berberine has pharmacological activities, such as anti-inflammatory, analgesic, antimicrobial, hypolipidemic, and blood pressure-lowering effects. Importantly, the active ingredient of berberine has clear inhibitory effects on various cancers, including colorectal cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, and cervical cancer. Cancer, ranked as one of the world’s five major incurable diseases by WHO, is a serious threat to the quality of human life. Here, we try to outline how berberine exerts antitumor effects through the regulation of different molecular pathways. In addition, the berberine-mediated regulation of epigenetic mechanisms that may be associated with the prevention of malignant tumors is described. Thus, this review provides a theoretical basis for the biological functions of berberine and its further use in the clinical treatment of cancer.
Highlights
Natural medicine plays a very important role in novel drug discovery (Zhang et al, 2013; Zhang L. et al, 2017)
Berberine significantly inhibited the vascular endothelial growth factor (VEGF)-induced migration and invasion of human umbilical vein endothelial cells Human umbilical vein endothelial cells (HUVEC) in a dose-dependent manner, and significantly reduced the expression of COX-2, Inos, and VEGF mRNA and downregulated pro-angiogenic factors to inhibit angiogenesis (Naveen et al, 2016; Wang et al, 2018). These results indicated the critical effects of berberine on the hypoxia-induced factor α (HIF1α)/VEGF pathway
BBR combined with the glucose analog 2-deoxy-D-glucose (2-dG) synergistic inducing the apoptosis of human lymphoblastoid TK6 cells BBR sensitized gastric cancer cells to 5-FU, the combination shows a synergistic inhibition of surviving and signal transducer and activator of transcription 3 (STAT3) level BBR combined with cinnamaldehyde prevented A549 cell substance permeability via AMP-activated protein kinase (AMPK)-reduced AQP-1 expression BBR sensitized MCF-7 cells to cisplatin through inducing DNA breaks and caspase-3-dependent apoptosis BBR in combination with d-limonene showed synergistic anticancer effects on MGC803 cells through inducing cell-cycle arrest, ROS production, and apoptosis via the mitochondria-mediated intrinsic pathway BBR combined with Doxorubicin inhibit melanoma tumor growth through casepase-3 depentdent apoptosis BBR sensitizes lung cancer cells to Doxorubicin by promoting STAT3 degradation, inhibiting doxorubicin mediated STAT3 activation
Summary
Specialty section: This article was submitted to Cancer Molecular Targets and Therapeutics, a section of the journal Frontiers in Pharmacology. A traditional medicinal plant, has been used widely in the field of traditional Chinese medicine for many years. The chemical composition and bioactivity of Coptis have been studied worldwide. Modern medicine has confirmed that berberine has pharmacological activities, such as anti-inflammatory, analgesic, antimicrobial, hypolipidemic, and blood pressure-lowering effects. The active ingredient of berberine has clear inhibitory effects on various cancers, including colorectal cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, and cervical cancer. We try to outline how berberine exerts antitumor effects through the regulation of different molecular pathways. This review provides a theoretical basis for the biological functions of berberine and its further use in the clinical treatment of cancer
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