Qiang Lu, Ying Tang, Shuang Luo, Qihai Gong, Cailan Li
{"title":"黄连中的特征成分黄连素在治疗癌症、代谢性疾病和炎症性疾病方面具有显著的治疗潜力。","authors":"Qiang Lu, Ying Tang, Shuang Luo, Qihai Gong, Cailan Li","doi":"10.1142/S0192415X2350091X","DOIUrl":null,"url":null,"abstract":"<p><p>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 <i>Coptis chinensis</i> Franch., which is a famous traditional Chinese medicine. <i>C. chinensis</i> possesses many kinds of functions, including the ability to eliminate heat, expel dampness, purge fire, and remove noxious substances. In Asian countries, <i>C. chinensis</i> 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 <i>C. chinensis</i> 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.</p>","PeriodicalId":94221,"journal":{"name":"The American journal of Chinese medicine","volume":" ","pages":"2121-2156"},"PeriodicalIF":0.0000,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Coptisine, the Characteristic Constituent from <i>Coptis chinensis</i>, Exhibits Significant Therapeutic Potential in Treating Cancers, Metabolic and Inflammatory Diseases.\",\"authors\":\"Qiang Lu, Ying Tang, Shuang Luo, Qihai Gong, Cailan Li\",\"doi\":\"10.1142/S0192415X2350091X\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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 <i>Coptis chinensis</i> Franch., which is a famous traditional Chinese medicine. <i>C. chinensis</i> possesses many kinds of functions, including the ability to eliminate heat, expel dampness, purge fire, and remove noxious substances. In Asian countries, <i>C. chinensis</i> 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 <i>C. chinensis</i> 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.</p>\",\"PeriodicalId\":94221,\"journal\":{\"name\":\"The American journal of Chinese medicine\",\"volume\":\" \",\"pages\":\"2121-2156\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2023-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"The American journal of Chinese medicine\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1142/S0192415X2350091X\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2023/11/4 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"The American journal of Chinese medicine","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1142/S0192415X2350091X","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2023/11/4 0:00:00","PubModel":"Epub","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
摘要
天然来源的生物碱属于一类非常重要的有机化合物。黄连是一种苄基四氢异喹啉生物碱,是黄连的主要生物活性成分之一。,这是一种著名的中药。中药具有清热、利湿、泻火、解毒等多种功效。在亚洲国家,中药传统上用于治疗痈疽、糖尿病、黄疸、胃肠道疾病、红眼、牙痛和皮肤疾病。到目前为止,人们对黄连碱的药理作用进行了大量的研究。然而,迫切需要对coptisine相关研究进行全面综述。本文详细综述了黄连碱的药理、药代动力学、安全性和制剂的研究进展。本文中的相关研究来自以下学术数据库:The Web of Science、PubMed、Google scholar、Elsevier和CNKI。截止日期为2023年1月。黄连具有多种药理作用,包括抗癌、抗代谢疾病、抗炎症和抗胃肠道疾病等作用。根据其药代动力学,coptisine的主要代谢部位是肝脏。黄连在胃肠系统中吸收不良,大部分以原型的形式通过粪便排出。关于安全性,coptisine显示出潜在的肝毒性。一些新的制剂,包括[配方: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。中药的传统使用与黄连的药理作用密切相关。尽管存在一些缺点,包括溶解性差、生物利用度低和可能的肝毒性,但coptisine仍然是一种有前景的天然衍生候选药物,尤其是在治疗肿瘤以及代谢和炎症疾病方面。有必要对coptisine进行进一步的研究,以促进基于coptisine的药物在临床实践中的应用。
Coptisine, the Characteristic Constituent from Coptis chinensis, Exhibits Significant Therapeutic Potential in Treating Cancers, Metabolic and Inflammatory Diseases.
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.