School of Pharmaceutical Science and Technology, Faculty of Medicine, Tianjin University, Tianjin, China.
School of Pharmaceutical Science and Technology, Faculty of Medicine, Tianjin University, Tianjin, China.
J Ethnopharmacol. 2025 Jan 30;337(Pt 2):118832. doi: 10.1016/j.jep.2024.118832. Epub 2024 Sep 19.
Aconitum carmichaelii Debx. is the most widely distributed species of Aconitum plants in China and has a long history of medicinal use. Because of its toxicity, A. carmichaelii is classified as lower class in the Shennong Bencao Jing (Shennong's Classic of Materia Medica). According to the theory of Chinese medicine, the roots can be used to revive yang for resuscitation, dispel wind, remove dampness, and relieve pain.
This review focuses on summarizing the latest reports on the components, pharmacology, toxicity, detoxification mechanism and application of A. carmichaelii. It aims to provide ideas for in-depth research on activity mechanism of A. carmichaelii and expanding the value of exploitation and utilization.
Information was collected from the following online scientific databases: PubMed, Web of Science, Wiley Online Library, SciFinder, Scopus, PubChem, China National Knowledge Internet (CNKI), etc. Additional data were obtained from other Chinese medicine books.
In this review, 224 compounds were categorized and new compounds discovered in the last five years were highlighted. The main components of A. carmichaelii are C-diterpene alkaloids(C-DAs), among which diester-type aconitine is the most toxic and also the main active ingredient, while monoester diterpene alkaloids (MDAs) and aminol diterpene alkaloids (ADAs) are greatly toxicity reduced due to the loss of ester bond. Heating and compatibility are the means to increase the efficiency and reduce the toxicity of A. carmichaelii. In addition, it also contains abundant C-diterpene alkaloids (C-DAs). Like C-DAs, these compounds also have cardiotonic, anticancer, anti-inflammatory and analgesic pharmacological effects, but their toxicity is weaker. The above-ground part contains not only a variety of MDAs and ADAs, but also contains abundant non-diterpenoid alkaloids and active polysaccharides. In addition to pharmacological effects, we further summarized the mechanisms of cardiotoxicity, neurotoxicity and other toxicity of A. carmichaelii. What's more, the application prospects are also discussed. Polysaccharides and diterpenoid alkaloids in A. carmichaelii and related traditional prescriptions have great promising prospects for the development of new drugs.
A. carmichaelii has rich alkaloids and polysaccharides, but the new compounds discovered in recent years are only in the activity screening stage. The toxic differences between C- and C- DAs and the dose that affect toxicity of A. carmichaelii are still not clear. The non-traditional medicinal parts, such as stems and leaves, show great potential for development and utilization. More extensive and in-depth exploration of low-toxic active compounds, as well as the mechanism of efficacy-enhancement and toxicity-attenuation, will help A. carmichaelii to be better and safer used for clinical.
乌头属植物是中国分布最广的乌头属植物,具有悠久的药用历史。由于其毒性,乌头属植物被归类为《神农本草经》中的低级类别。根据中医理论,其根可用于回阳救逆、祛风除湿、止痛。
本综述重点总结了近年来有关乌头属植物化学成分、药理学、毒性、解毒机制及应用的最新报道,旨在为深入研究乌头属植物的活性机制和扩大其开发利用价值提供思路。
从以下在线科学数据库收集信息:PubMed、Web of Science、Wiley Online Library、SciFinder、Scopus、PubChem、中国国家知识基础设施(CNKI)等。其他中药书籍也提供了额外的数据。
在本综述中,共分类出 224 种化合物,并重点介绍了过去五年新发现的化合物。乌头属植物的主要成分是 C-二萜生物碱(C-DAs),其中二酯型乌头碱毒性最大,也是主要的活性成分,而单酯二萜生物碱(MDAs)和氨基二萜生物碱(ADAs)由于酯键的丢失,毒性大大降低。加热和配伍是提高乌头属植物疗效和降低毒性的手段。此外,它还含有丰富的 C-二萜生物碱(C-DAs)。与 C-DAs 类似,这些化合物也具有强心、抗癌、抗炎和镇痛的药理作用,但毒性较弱。地上部分不仅含有多种 MDAs 和 ADAs,还含有丰富的非二萜生物碱和活性多糖。除了药理作用,我们还进一步总结了乌头属植物的心脏毒性、神经毒性等毒性机制。此外,还讨论了其应用前景。乌头属植物中的多糖和二萜生物碱以及相关的传统方剂在新药的开发方面具有广阔的前景。
乌头属植物含有丰富的生物碱和多糖,但近年来发现的新化合物仅处于活性筛选阶段。C-和 C-DAs 的毒性差异以及影响乌头属植物毒性的剂量尚不清楚。茎、叶等非传统药用部位具有很大的开发利用潜力。更广泛和深入地探索低毒活性化合物以及增效减毒的机制,将有助于乌头属植物更好、更安全地应用于临床。