Kaempferol is a flavonol that is relatively abundant in various plants and some edible berries. These compounds have antioxidative, anti-inflammatory, antihypertensive, lipolytic and anti-cancer effects. In this book, the authors discuss the chemistry, natural occurrences and health benefits of kaempferol. Topics include the effect of cyclodextrins complexation on the properties of kaempferol; kaempferitrin and kaempferol as nutraceutical compounds contributing to glucose homeostasis by acting at multiple biological sites; distribution of kaempferol glycosides and their function in plants; analytical approaches for kaempferol determination; chemoprotective effects of kaempferol in colorectal tumorigenesis; multipotent flavonoid kaempferol as molecular targets and mechanism of action in nanotechnology applications in cancer and human health; metal complexes of kaempferol and their speciation in human plasma; the action of kaempferol on oral cavity cancer and airway secretion; kaempferol as it regulates intestinal tight junction permeability; and identification of kaempferol in historical textiles.