Abstract

Cancer is a serious disease with an increasing number of reported cases and high mortality worldwide. Gastrointestinal cancer defines a group of cancers in the digestive system, e.g., liver cancer, colorectal cancer, and gastric cancer. Coptidis Rhizoma (C. Rhizoma; Huanglian, in Chinese) is a classical Chinese medicinal botanical drug for the treatment of gastrointestinal disorders and has been shown to have a wide variety of pharmacological activity, including antifungal, antivirus, anticancer, antidiabetic, hypoglycemic, and cardioprotective effects. Recent studies on C. Rhizoma present significant progress on its anticancer effects and the corresponding mechanisms as well as its clinical applications. Herein, keywords related to C. Rhizoma, cancer, gastrointestinal cancer, and omics were searched in PubMed and the Web of Science databases, and more than three hundred recent publications were reviewed and discussed. C. Rhizoma extract along with its main components, berberine, palmatine, coptisine, magnoflorine, jatrorrhizine, epiberberine, oxyepiberberine, oxyberberine, dihydroberberine, columbamine, limonin, and derivatives, are reviewed. We describe novel and classic anticancer mechanisms from various perspectives of pharmacology, pharmaceutical chemistry, and pharmaceutics. Researchers have transformed the chemical structures and drug delivery systems of these components to obtain better efficacy and bioavailability of C. Rhizoma. Furthermore, C. Rhizoma in combination with other drugs and their clinical application are also summarized. Taken together, C. Rhizoma has broad prospects as a potential adjuvant candidate against cancers, making it reasonable to conduct additional preclinical studies and clinical trials in gastrointestinal cancer in the future.

Highlights

  • Jatrorrhizine has been reported to have an inhibitory effect on Hepatocellular carcinoma (HCC), breast cancer, and melanoma

  • The results indicated that berberine intervention along with the reduction of intestinal tumor development could improve metabolic abnormalities by reversing glucose metabolism, amino acid-related metabolism, and lipid metabolism

  • The percentage of estimated deaths of digestive system cancers is increased in recent years (25.69%, 153,030/595,690 for year 2016; 26.24%, 157,700/600,920 for year 2017; 26.38%, 160,820/609,640 for year 2018; 27.26%, 165,460/606,880 for year 2019; 27.66%, 167,790/606,520 for year 2020; 27.82%, 169,280/608,570 for year 2021) according to the cancer statistics over the past 5 years in the United States

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Summary

INTRODUCTION

Rhizoma; Huanglian, in Chinese) is a common botanical drug which has a long history in Asia, especially in China. It is constituted by the dried root of three Coptis species, namely, Coptis chinensis Franch. Its wide pharmacological activities include antiviral, Coptidis Rhizoma in Cancer Research antibacterial, antifungal, antihepatic steatosis, antiatherosclerotic, antiarrhythmic, antihypertensive, cardioprotective, antidiabetic, anti-inflammatory, antioxidative, neuroprotective, and anticancer effects (Meng et al, 2018; Lyu et al, 2021). Rhizoma, has been indicated to exert broad anticancer effects in a variety of human cancer cells (Fan S. et al, 2019).

Rhizoma Extracts and Its Main Component Berberine
Rhizoma extract
Participants Control
Findings
CONCLUSION AND FUTURE PERSPECTIVE
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