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The sesterterpenoids are one division of pentaprenyl terpenoid compounds whose structures are derived from geranylfarnesyl-PP. Although sesterterpenoids are a comparatively small group of terpenoids, their sources, pharmaceutical applications, and pharmacological activities are wide. In this chapter, the importance of sesterterpenoids, phytochemistry and classification of the group, main representatives of the group, ethnophytopharmacology, techniques of extraction and purification, techniques of identification and quantification, levels found in foods/plants, and effects of food processing on these phytochemicals were discussed.