Naturally derived alkaloids belong to a class of quite significant organic compounds. Coptisine, a benzyl tetrahydroisoquinoline alkaloid, is one of the major bioactive constituents in Coptis chinensis Franch., which is a famous traditional Chinese medicine. C. chinensis possesses many kinds of functions, including the ability to eliminate heat, expel dampness, purge fire, and remove noxious substances. In Asian countries, C. chinensis is traditionally employed to treat carbuncle and furuncle, diabetes, jaundice, stomach and intestinal disorders, red eyes, toothache, and skin disorders. Up to now, there has been plenty of research of coptisine with respect to its pharmacology. Nevertheless, a comprehensive review of coptisine-associated research is urgently needed. This paper was designed to summarize in detail the progress in the research of the pharmacology, pharmacokinetics, safety, and formulation of coptisine. The related studies included in this paper were retrieved from the following academic databases: The Web of Science, PubMed, Google scholar, Elsevier, and CNKI. The cutoff date was January 2023. Coptisine manifests various pharmacological actions, including anticancer, antimetabolic disease, anti-inflammatory disease, and antigastrointestinal disease effects, among others. Based on its pharmacokinetics, the primary metabolic site of coptisine is the liver. Coptisine is poorly absorbed in the gastrointestinal system, and most of it is expelled in the form of its prototype through feces. Regarding safety, coptisine displayed potential hepatotoxicity. Some novel formulations, including the [Formula: see text]-cyclodextrin-based inclusion complex and nanocarriers, could effectively enhance the bioavailability of coptisine. The traditional use of C. chinensis is closely connected with the pharmacological actions of coptisine. Although there are some disadvantages, including poor solubility, low bioavailability, and possible hepatotoxicity, coptisine is still a prospective naturally derived drug candidate, especially in the treatment of tumors as well as metabolic and inflammatory diseases. Further investigation of coptisine is necessary to facilitate the application of coptisine-based drugs in clinical practice.

中文翻译：

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黄连碱是黄连的特征成分，在治疗癌症、代谢性疾病和炎症性疾病方面具有显着的治疗潜力。


天然衍生的生物碱属于一类非常重要的有机化合物。黄连碱是一种苄基四氢异喹啉生物碱，是名优中药黄连中的主要生物活性成分之一。茶树具有清热、祛湿、泻火、解毒等多种功能。在亚洲国家，中华茶传统上用于治疗痈肿、糖尿病、黄疸、胃肠疾病、红眼、牙痛和皮肤病。迄今为止，黄连碱的药理学研究已经非常多。然而，迫切需要对黄连碱相关研究进行全面审查。本文旨在详细总结黄连碱的药理、药代动力学、安全性及剂型研究进展。本文纳入的相关研究检索自以下学术数据库：The Web of Science、PubMed、Google Scholar、Elsevier、CNKI。截止日期为2023年1月。黄连碱具有多种药理作用，包括抗癌、抗代谢疾病、抗炎、抗胃肠道疾病作用等。根据其药代动力学，黄连碱的主要代谢部位是肝脏。黄连碱在胃肠系统中吸收较差，大部分以原形形式通过粪便排出体外。就安全性而言，黄连碱表现出潜在的肝毒性。一些新颖的制剂，包括[分子式：见正文]-环糊精包合物和纳米载体，可以有效提高黄连碱的生物利用度。传统的用法是C. 黄连与黄连碱的药理作用密切相关。尽管存在溶解度差、生物利用度低和可能的肝毒性等缺点，但黄连碱仍然是一种有前景的天然衍生药物候选物，特别是在治疗肿瘤以及代谢和炎症疾病方面。有必要对黄连碱进行进一步的研究，以促进黄连碱药物在临床中的应用。