Many herbal medicines have so far been utilized for the treatment of various ailments since the beginning of Chinese civilization. Aconitum is a botanical source for various pharmaceutically active components, which has been commonly used in traditional Chinese medicine for thousands of years. Increasing interest in Aconitum pharmaceutical resources has led to further discoveries of diterpenoid alkaloids, polysaccharides, flavonoids and many other compounds in various Aconitum species, and to investigations on their chemotaxonomy, molecular phylogeny and pharmacology. In continuation with our studies on Aconitum pharmacophylogeny, here we review the phytochemistry, chemotaxonomy, molecular biology and phylogeny of Aconitum and their relevance to therapeutic efficacy and toxicity. An exhaustive literature survey is used to summarize the global scientific effort in the phytochemical and biological studies of Aconitum. More diterpenoid alkaloids have been found in various Aconitum species, among which the aconitine type (type III) is predominant. The versatile bioactivities of alkaloids and extracts, as well as the bioactivities of polysaccharides and other ingredients, are summarized and discussed in this review. The morphology-based 11-series classification of section Aconitum, subgenus Aconitum, is not supported by chemotaxonomy and molecular phylogeny. Molecular phylogeny based on nuclear and chloroplast DNA sequences divided the nine morphologically similar series into two clusters, which is bolstered by the chemotaxonomic data. It is essential to integrate the emerging technologies into Aconitum studies for both the sustainable utilization of Aconitum pharmaceutical resources and finding novel compounds with potential clinical utility and less toxicity. Systems biology and omics technologies will play an increasingly important role in booming pharmaceutical research involving bioactive compounds of Aconitum.
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