Locally and traditionally used Ligusticum species - A review of their phytochemistry, pharmacology and pharmacokinetics.

BACKGROUND

Ligusticum species (Umbelliferae) have been widely used in traditional Chinese medicine, Korean folk medicine and Native American medicine for their medicinal and nutritional value. Decoctions of the rhizomes are used in treatment and prophylaxis of migraine, anemia and cardiovascular conditions including stroke.

OBJECTIVE

This review is intended to fully compile the constituents of locally and traditionally used Ligusticum species, present their bioactivities and highlight potential leads for future drug design, and thus, provide a reference for further research and application of these species. Emphasis is also placed on current trends in the pharmacokinetic studies of the major constituents.

METHODS

The literature discussed is derived from readily accessible papers spanning the early 1990s to the end of 2015. Information was collected from journals, books and online searches (Google Scholar, PubMed, ScienceDirect, SciFinder, Springerlink and CNKI).

RESULTS

The major phytoconstituents, 154 of which are presented in this review, include alkaloids, phthalides and phenolic acids. The crude extracts and isolated constituents have exhibited a wide range of in vitro and in vivo pharmacologic effects, including cardioprotective, antioxidant, anti-inflammatory and neuroprotective activities. The bioactive alkaloid tetramethylpyrazine (TMP) has attracted the most attention for its potent effect on calcium channels, anti-platelet as well as anti-inflammatory effects. Pharmacokinetic studies of major constituents have also been summarized.

CONCLUSIONS

The pthalides, organic acids and alkaloids of Ligusticum species have emerged as a good source of traditional medicines for the management of cardio- and cerebrovascular conditions, inflammation and neurogenerative disorders. The species discussed in this review have demonstrated wide pharmacological actions and have great potential to yield multipotent drugs if challenges such as poor bioavailability, solubility and toxicological profiles are addressed. Apart from the rhizomes, pharmacological activities of other botanical parts also need to be studied further. Expansion of research to cover other species in the Ligusticum genus would provide more opportunities for the discovery of new bioactive principles.