Coptidis Rhizoma: a comprehensive review of its traditional uses, botany, phytochemistry, pharmacology and toxicology

Abstract

Context: Coptidis rhizome (CR), also known as Huanglian in Chinese, is the rhizome of Coptis chinensis Franch., C. deltoidea C.Y. Cheng et Hsiao, or C. teeta Wall (Ranunculaceae). It has been widely used to treat bacillary dysentery, diabetes, pertussis, sore throat, aphtha, and eczema in China. Objectives: The present paper reviews the latest advances of CR, focusing on the botany, phytochemistry, traditional usages, pharmacokinetics, pharmacology and toxicology of CR and its future perspectives. Methods: Studies from 1985 to 2018 were reviewed from books; PhD. and MSc. dissertations; the state and local drug standards; PubMed; CNKI; Scopus; the Web of Science; and Google Scholar using the keywords Coptis , Coptidis Rhizoma, Huanglian , and goldthread. Results: Currently, 128 chemical constituents have been isolated and identified from CR. Alkaloids are the characteristic components, together with organic acids, coumarins, phenylpropanoids and quinones. The extracts/compounds isolated from CR cover a wide pharmacological spectrum, including antibacterial, antivirus, antifungal, antidiabetic, anticancer and cardioprotective effects. Berberine is the most important active constituent and the primary toxic component of CR. Conclusions: As an important herbal medicine in Chinese medicine, CR has the potential to treat various diseases. However, further research should be undertaken to investigate the clinical effects, toxic constituents, target organs and pharmacokinetics, and to establish criteria for quality control, for CR and its related medications. In addition, the active constituents, other than alkaloids, in both raw and processed products of CR should be investigated.

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“…It is often widely prescribed by Chinese practitioners for the treatment of high fever, coma, and respiratory diseases [119]. According to Professor Zhao Zhi Li from Shanghai Traditional Chinese Medicine University, Scutellaria baicalensis is acknowledged as a middle class medicine and Forsythia suspense as a low class medicine recorded in Shennong's Classic of Materia Medica from Han dynasty according to its ranking for medicinal value with high class or A level as the most valued in terms of pharmacology, whereas Lonicera japonica has been used as a medicinal plant for the treatment of diseases since the Southern and Northern Dynasty in "Mingyi Bielu" [120,121]. There is a total of 12 companies that manufacture this antidote and one of the manufacturers, Hayao Company's Shuang Huang Lian Kou Fu Ye was categorized as an "A level" list drug, which is the best quality of drugs in TCM according to the categorization in 2019 National health insurance project in China [115].…”

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Metabolic profile of alkaloids in Rhizoma Coptidis in rat plasma, urine and feces after oral administration using ultra‐high‐performance liquid chromatography coupled with quadrupole time‐of‐flight mass spectrometry

“…Rhizoma Coptidis (RC), commonly known as Huanglian in China, is the rhizome from the family Ranunculaceae, including Coptis chinensis Franch, C. deltoidei C.Y. Cheng et Hsiaao, and C. teeta Wall . RC, first mentioned in Shennong's Classic of Materia Medica in the Eastern Han Dynasty, has been used to treat various diseases in traditional Chinese medicine (TCM) for thousands of years .…”

“…RC, first mentioned in Shennong's Classic of Materia Medica in the Eastern Han Dynasty, has been used to treat various diseases in traditional Chinese medicine (TCM) for thousands of years . Previous studies have demonstrated that RC has activities including anti‐hyperglycemic, anti‐cancer, anti‐bacterial, anti‐hyperlipidemic, anti‐inflammatory, anti‐obesity and anti‐hepatic steatosis . Currently, more than 120 components have been isolated and identified from RC, and alkaloids are most common in plants from RC .…”

“…Previous studies have demonstrated that RC has activities including anti‐hyperglycemic, anti‐cancer, anti‐bacterial, anti‐hyperlipidemic, anti‐inflammatory, anti‐obesity and anti‐hepatic steatosis . Currently, more than 120 components have been isolated and identified from RC, and alkaloids are most common in plants from RC . Protoberberine alkaloids, including berberine, jatrorrhizine, palmatine, coptisine, etc., are the main components of RC that play a pharmacological role.…”