Abstract

Various medicinal compounds have been found in Ranunculaceae plants, many of which, such as alkaloids, terpenoids, saponins, and polysaccharides, have shown anticancer activities during in vitro and in vivo studies. Most concerns have been raised for two epiphany molecules, the monoterpene thymoquinone and the isoquinoline alkaloid berberine. At least 17 genera have been found to be rich in anticancer compounds. Some Ranunculaceae compounds induce the cell cycle arrest and apoptosis of cancer cells or enhance immune activities, while others inhibit the proliferation, invasion, angiogenesis, and metastasis, or reverse the multi-drug resistance of cancer cells. In fact, Ranunculaceae phytometabolites regulate all ten cancer hallmarks defined by Hanahan and Weinberg. The same class of phytometabolite could exert the anticancer activity via multiple pathways. In addition, absorption, distribution, metabolism, and excretion/toxicity properties and structure activity relationships of some phytometabolites have been revealed and are useful in the early drug discovery and development pipelines. However, a comprehensive review of the molecular mechanisms and functions of Ranunculaceae anticancer compounds is lacking. In this chapter, the recent progress of the anticancer chemodiversity and pharmacological diversity of Ranunculaceae medicinal plants is summarized, focusing on the emerging molecular machineries and functions of anticancer compounds. Gene expression profiling and relevant omics platforms could reveal differential effects of phytometabolites on the phenotypically heterogeneous cancer cells. Genomics, transcriptomics, proteomics, and metabolomics are highlighted as Rosetta Stone in deciphering novel anticancer mechanisms and utilities of Ranunculaceae phytometabolites.

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