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Capsaicinoids are the main metabolites produced by the Capsicum genus. This alkaloid-like class of chemicals is responsible for the characteristic pungency of chilli peppers. Found exclusively within the Capsicum genus, the capsaicinoid content varies among species and cultivars. The scientific interest in capsaicinoids is not only related to their pungency, but also to the diverse bioactivities that these metabolites present. Capsaicinoids have been used in several different types of product (e.g. medicines, cosmetics and foods). The control of pungency is essential. The heat from chilli peppers is not only a sensory characteristic, but can also have a toxic effect in humans. When over-induced, capsaicinoids are used by species of Capsicum against predator attacks. The capsaicinoid content can be managed by DNA modification and other endogenous and exogenous factors. This chapter provides an insight into capsaicinoid chemistry, which is fundamental in the development of bioproducts, and discusses the control of pungency and the evaluation of capsaicinoid analogues as pharmacological substitutes.

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