State Key Laboratory of Southwestern Chinese Medicine Resources, School of Ethnic Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China.
State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China.
J Ethnopharmacol. 2024 Mar 1;321:117505. doi: 10.1016/j.jep.2023.117505. Epub 2023 Nov 26.
Hypaconitine (HA), a diterpenoid alkaloid, mainly derived from Aconitum plants such as Acoitum carmichaeli Debx. And Aconitum nagarum Stapf., has recently piqued significant interest among the scientific community given its multifaceted attributes including anti-inflammatory, anticancer, analgesic, and cardio-protective properties.
This review presents a comprehensive exploration of the research advancements regarding the traditional uses, pharmacology, pharmacokinetics, toxicity, and toxicity reduction of HA. It aims to provide a thorough understanding of HA's multifaceted properties and its potential applications in various fields.
A systematic literature search was conducted using several prominent databases including PubMed, Web of Science, NCBI, and CNKI. The search was performed using specific keywords such as "hypaconitine," "heart failure," "anti-inflammatory," "aconite decoction," "pharmacological," "pharmacokinetics," "toxicity," "detoxification or toxicity reduction," and "extraction and isolation." The inclusion of these keywords ensured a comprehensive exploration of relevant studies and enabled the retrieval of valuable information pertaining to the various aspects of HA.
Existing research has firmly established that HA possesses a range of pharmacological effects, encompassing anti-cardiac failure, anti-inflammatory, analgesic, and anti-tumor properties. The therapeutic potential of HA is promising, with potential applications in heart failure, ulcerative colitis, cancer, and other diseases. Pharmacokinetic studies suggest that HA exhibits high absorption rates, broad distribution, and rapid metabolism. However, toxic effects of HA on the nerves, heart, and embryos have also been observed. To mitigate these risks, HA needs attenuation before use, with the most common detoxification methods being processing and combined use with other drugs. Extraction methods for HA most commonly include cold maceration, soxhlet reflux extraction, and ultrasonic-assisted extraction. Despite the potential therapeutic benefits of HA, further research is warranted to elucidate its anti-heart failure effects, particularly in vivo, exploring aspects such as in vivo metabolism, distribution, and metabolites. Additionally, the therapeutic effects of HA monomers on inflammation-induced diseases and tumors should be validated in a more diverse range of experimental models, while the mechanisms underlying the therapeutic effects of HA should be investigated in greater detail.
This review serves to emphasize the therapeutic potential of HA and highlights the crucial need to address its toxicity concerns before considering clinical application. Further research is required to comprehensively investigate the pharmacological properties of HA, with particular emphasis on its anti-cardiac failure and anti-inflammatory activities. Such research endeavors have the potential to unveil novel treatment avenues for a broad spectrum of diseases.
海乌头碱(HA)是一种二萜生物碱,主要来源于乌头属植物,如乌头(Acoitum carmichaeli Debx.)和草乌(Aconitum nagarum Stapf.),具有抗炎、抗癌、镇痛和心脏保护作用等多方面的特性,最近引起了科学界的极大兴趣。
本综述全面探讨了海乌头碱的传统用途、药理学、药代动力学、毒性和减毒作用的研究进展。旨在全面了解海乌头碱的多方面特性及其在各个领域的潜在应用。
采用系统文献检索方法,检索了 PubMed、Web of Science、NCBI 和中国知网(CNKI)等多个数据库,使用“hypaconitine”“heart failure”“anti-inflammatory”“aconite decoction”“pharmacological”“pharmacokinetics”“toxicity”“detoxification or toxicity reduction”“extraction and isolation”等关键词进行检索。纳入这些关键词可以全面探讨相关研究,并检索到与海乌头碱的各个方面相关的有价值信息。
现有研究证实,海乌头碱具有多种药理作用,包括抗心力衰竭、抗炎、镇痛和抗肿瘤作用。海乌头碱具有广阔的治疗前景,可应用于心力衰竭、溃疡性结肠炎、癌症等疾病。药代动力学研究表明,海乌头碱吸收快、分布广、代谢迅速。然而,海乌头碱对神经、心脏和胚胎也有一定的毒性作用。为了降低这些风险,海乌头碱在使用前需要减毒,常用的减毒方法是炮制和与其他药物合用。海乌头碱的提取方法主要包括冷浸、索氏回流提取和超声辅助提取。尽管海乌头碱具有潜在的治疗益处,但仍需要进一步研究以阐明其抗心力衰竭的作用,特别是在体内,探索体内代谢、分布和代谢物等方面。此外,还需要在更多种实验模型中验证海乌头碱单体对炎症性疾病和肿瘤的治疗作用,并更详细地研究海乌头碱治疗作用的机制。
本综述强调了海乌头碱的治疗潜力,并强调了在考虑临床应用之前解决其毒性问题的重要性。需要进一步研究全面探讨海乌头碱的药理学特性,特别是其抗心力衰竭和抗炎活性。这些研究有可能为广泛的疾病提供新的治疗途径。