Aconitine and its derivatives: bioactivities, structure-activity relationships and preliminary molecular mechanisms

Front Chem. 2024 Jan 22:12:1339364. doi: 10.3389/fchem.2024.1339364. eCollection 2024.

Abstract

Aconitine (AC), which is the primary bioactive diterpene alkaloid derived from Aconitum L plants, have attracted considerable interest due to its unique structural feature. Additionally, AC demonstrates a range of biological activities, such as its ability to enhance cardiac function, inhibit tumor growth, reduce inflammation, and provide analgesic effects. However, the structure-activity relationships of AC are remain unclear. A clear understanding of these relationships is indeed critical in developing effective biomedical applications with AC. In line with these challenges, this paper summarized the structural characteristics of AC and relevant functional and bioactive properties and the structure-activity relationships presented in biomedical applications. The primary temporal scope of this review was established as the period spanning from 2010 to 2023. Subsequently, the objective of this review was to provide a comprehensive understanding of the specific action mechanism of AC, while also exploring potential novel applications of AC derivatives in the biomedical field, drawing upon their structural characteristics. In conclusion, this review has provided a comprehensive analysis of the challenges and prospects associated with AC in the elucidation of structure-bioactivity relationships. Furthermore, the importance of exploring modern biotechnology approaches to enhance the potential biomedical applications of AC has been emphasized.

Keywords: Aconitine; biological activities; diterpenoid alkaloids; molecular mechanism; structure-activity relationships.

Publication types

  • Review

Grants and funding

The author(s) declare financial support was received for the research, authorship, and/or publication of this article. This review was supported by Guizhou Provincial Key Technology R&D Program: (2023) Ordinary 385 Clinical urgent need for the development of a new class of anti heart failure chemical drugs (GD-N1702); and Key Science and Technology R&D Projects in Sichuan Province (2023YFS0006).